INHIBITORS OF DIACYLGLYCEROL ACYL TRANSFERASE

FIELD OF THE INVENTION

The present invention relates to heterocyclic compounds, to processes for their preparation, pharmaceutical compositions containing them, and their use in the prevention and treatment of diseases or disorders mediated by diacylglycerol acyl transferase (DGAT), particularly DGAT1 .

BACKGROUND OF THE INVENTION

Obesity is a disease of energy imbalance, when energy input is more than output. Excess energy is stored in the form of triglycerides (TGs) in the adipose tissue. Increased adipose cell size causes hypertrophic obesity and increased cell number causes hyperplastic obesity characteristic of a more severe condition. The key causes of obesity are the increased consumption of energy-rich but nutrient-poor diets (like saturated fats and sugars) and reduced physical activity. 65% of the US population is overweight, where body mass index (BMI) is greater than 25 and approximately 25 % of them are obese, having BMI > 30. The prevalence of obesity has increased dramatically over the last decade. Obesity leads to increased risk of chronic diseases such as type 2 diabetes, insulin resistance, hypertension, stroke, cardiovascular diseases, respiratory problems, gallbladder disease, osteoarthritis, sleep apnea and certain cancers (Expert Opin. Ther. Targets, 2009, 13, 2, 195-207). The increasing evidence that severe obesity has a genetic basis, resulting in maintaining and defending an elevated weight, may explain why long-term weight loss is very difficult to achieve. This has strengthened the argument that severe obesity should be treated with pharmacological agents along with conventional diet and exercise regimes.

Diacylglycerol acyltransferase (DGAT) is an enzyme that catalyses the biosynthesis of triglyceride at the final step of the process, converting diacylglycerol (DAG) and fatty acyl-coenzyme A (CoA) into triglyceride. The enzymatic activity is present in all cell types because of the necessity of producing triglyceride for cellular needs. The amount of triglyceride synthesized varies from cell to cell, with the adipocytes, hepatocytes and intestinal enterocytes producing much more triglyceride, for storage or incorporation into lipoproteins, than other cell types.

Because of its critical role in the biosynthesis of triglyceride, a neutral lipid that is the densest form of energy storage in animals, alteration of the expression and/or activity of DGAT in any of the tissues or organs would be expected to perturb the systemic energy metabolism. Diacyl glycerolacyltransferase 1 (DGAT1 ) is one of two known DGAT enzymes that catalyze the final step in triglyceride synthesis. Although most tissues generate triacylglycerols, DGAT1 is known to be highly expressed in the intestine and adipose with lower levels in the liver and muscle. Inhibition of DGAT1 in each of these tissues (intestine, adipose, liver and muscle) would Inhibit triacylglycerol synthesis and may reverse the pathophysiology of excessive lipid accumulation in human metabolic disease.

Inhibitors of varying structural types of DGAT1 have been reported to be potential agents for the treatment for obesity and other disorders. The particular interest in DGAT1 inhibition stems from the reported phenotype of DGAT1 deficient (Dgatl -/-) mice. These animals are viable, resistant to weight gain when fed a high-fat diet, and show increased insulin and leptin sensitivity (Nature Genetics, 2000, 25, 87-90). Resistance to weight gain results from increased energy expenditure rather than decreased food intake (the animals are in fact hyperphagic) and is associated with loss of adipose rather than lean tissue mass. Most aspects of this phenotype can be reproduced in rodents by treatment with a potent and selective small molecule inhibitor of DGAT1 .

XP620 (BMS) has been reported to be a selective DGAT1 inhibitor, which is able to block DGAT1 mediated retinyl-ester formation in Caco-2 cells. The potency against DGAT1 was in the order of 100 nM with no activity against DGAT2. Other small-molecule inhibitors reported are aryl alkyl acids from Bayer, phosphonic acid diesters from Otsuka, substituted ureas from Sankyo, pyrrolo [1 ,2-b]pyridazine derivatives from Tularik (now Amgen) and oxadiazoles from AstraZeneca (Expert Opin. Ther. Targets, 2006, 10, 5, 749-757). The PCT publication, WO2007016538 discloses biphenyl amino acid derivatives, and pharmaceutical salts and esters, thereof that have utility in the inhibition of DGAT1 and in the treatment of obesity and related diseases. The PCT publication, WO2009040410 discloses oxadiazolyl substituted benzimidazole and indole derivatives useful for treating conditions or disorders associated with DGAT1 activity in animals, particularly humans. However

to date, there is an unmet medical need for effective and safe pharmacotherapy for obesity thus leaving a significant challenge to pharmaceutical industry.

SUMMARY OF THE INVENTION

The present invention relates to heterocyclic compounds, processes for their preparation and their use in the prevention and treatment of diseases or disorders mediated by diacylglycerol acyltransferase (DGAT), particularly DGAT1 .

According to one aspect of the present invention, there are provided heterocyclic compounds of formula 1 (as provided herein below), as well as stereoisomers, tautomeric forms, pharmaceutically acceptable salts, solvates, polymorphs, prodrugs, N-oxides and carboxylic acid isosteres thereof.

According to another aspect of the present invention, there are provided processes for producing heterocyclic compounds of formula 1 .

According to yet another aspect, there is provided the use of heterocyclic compounds of formula 1 in the prevention and treatment of diseases or disorders mediated by diacylglycerol acyltransferase (DGAT), particularly DGAT1 .

According to a further aspect of the present invention, there are provided pharmaceutical compositions including heterocyclic compounds of formula 1 as active ingredient.

According to a still further aspect of the present invention, there is provided a method for the treatment of diseases or disorders mediated by diacylglycerol acyltransferase (DGAT), particularly DGAT1 , the method including administering to a mammal in need thereof a therapeutically effective amount of a compound of formula 1 .

According to another aspect of the present invention, there are provided methods for the manufacture of medicaments including compounds of formula 1 , which are useful for the prevention or treatment of diseases or disorders mediated by diacylglycerol acyltransferase (DGAT), particularly DGAT1 .

DETAILED DESCRIPTION OF THE INVENTION

The present invention provides compounds of formula 1 :

Formula 1

in all their stereoisomeric and tautomeric forms, their pharmaceutically acceptable salts, solvates, polymorphs, prodrugs, N-oxides and carboxylic acid isosteres;

wherein,

A is selected from unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted (C3-Ci2)-cycloalkyl, unsubstituted or substituted aryl and unsubstituted or substituted heterocyclyl; wherein the aryl group may be fused with an unsubstituted or substituted 5 or 6-membered cycloalkyi ring optionally containing heteroatoms selected from O, N or S;

n is 0 or 1 ;

L is selected from NHC(0)NH, NHC(S)NH, *NHS02, *CONH and *S02NH; wherein * indicates the point of attachment to A-[CH2]n-;

Xi , X2, X3, X4 and X5 are independently selected from N, N-oxide, C, CH and CR; wherein R is selected from halogen, hydroxy, (Ci-Ci2)-alkoxy, cyano, (CrCi2)-alkyl, CF3, OCF3, (C2-Ci2)-alkenyl, (C2-Ci2)-alkynyl, (C3-Ci2)-cycloalkyl, aryl, aryloxy, heterocyclyl, O-heterocyclyl, C(0)Rp, C(0)ORp, NRpRq, SRP, S(0)Rp, S02Rp and C(0)NRpRq;

Rp and Rq are independently selected from hydrogen, unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted aryl, unsubstituted or substituted aralkyl and unsubstituted or substituted heterocyclyl, or Rp and Rq can optionally form a 3-7 membered ring;

Yi and Y2 are independently selected from C=0 and CH2;

m is an integer selected from 1 to 4; wherein,

when m is 1 , Ra and Rb may be selected from R-\ and R2;

when m is 2, Ra and Rb may be selected from R1 ; R2, R3 and R4;

when m is 3, Ra and Rb may be selected from R1 ; R2, R3, R4, R5 and R6;

when m is 4, Ra and Rb may be selected from R1 ; R2, R3, R4, R5, Re, R7 and

Re!

Ri , R2, R3, R4, R5, Re, R7 and R8 are independently selected from hydrogen, unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted aryl, unsubstituted or substituted aralkyl and unsubstituted or substituted heterocyclyl;

or any two of Ri , R2, R3, R4, R5, Re, R7 and R8 can form a (C3-C12) cycloalkyl ring;

R9 is selected from hydrogen, unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted aryl, unsubstituted or substituted aralkyl and unsubstituted or substituted heterocyclyl;

wherein,

(Ci-Ci2)-alkyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (Ci-Ci2)-alkoxy, cyano, nitro, unsubstituted or substituted (C3-Ci2)-cycloalkyl, unsubstituted or substituted aryl, C(0)Rp, C(0)ORp, NRpRq, SRP, S(0)Rp and S02Rp;

(C3-Ci2)-cycloalkyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (Ci-Ci2)-alkoxy cyano, nitro, unsubstituted or substituted aryl, unsubstituted or substituted heterocyclyl, C(0)Rp, C(0)ORp, NRpRq, SRP, S(0)Rp and S02Rp;

aryl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (Ci-Ci2)-alkoxy, cyano, nitro, unsubstituted or substituted (C Ci2)-alkyl, CF3, OCF3, (C2-Ci2)-alkenyl, (C2-Ci2)-alkynyl, unsubstituted or substituted (C3-Ci2)-cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy, unsubstituted or substituted heterocyclyl, unsubstituted or substituted O-heterocyclyl, C(0)Rp, C(0)ORp, NRpRq, SRP, S(0)Rp and S02Rp, or aryl may be fused with an unsubstituted or substituted 5 or 6-membered cycloalkyl ring optionally containing heteroatoms selected from O, N and S;

heterocyclyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (Ci-Ci2)-alkoxy, cyano, nitro, unsubstituted or substituted (C Ci2)-alkyl, CF3, OCF3, (C2-Ci2)-alkenyl, (C2-Ci2)-alkynyl, unsubstituted or substituted (C3-Ci2)-cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy, unsubstituted or substituted heterocyclyl, unsubstituted or substituted O-heterocyclyl, C(0)Rp, C(0)ORp, NRpRq, SRP, S(0)Rp and S02RP; and

Rp and Rq are independently selected from hydrogen, unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted aryl, unsubstituted or substituted aralkyl and unsubstituted or substituted heterocyclyl, or Rp and Rq can optionally form a 3-7 membered ring.

Definitions

As used herein, the term "alkyl" whether used alone or as part of a substituent group, refers to the radical of saturated aliphatic groups, including straight or branched-chain alkyl groups. An alkyl group can have a straight chain or branched chain containing 1 to 12 carbon atoms. Alkyl groups include methyl, ethyl, n-propyl, isopropyl, n-butyl, t-butyl, iso-butyl, sec-butyl, neo-pentyl, n-pentyl, n-heptyl, n-octyl, n-nonyl and n-decyl groups.

A substituted alkyl refers to an alkyl group substituted with one or more groups selected from halogen, hydroxy, cyano, nitro, unsubstituted or substituted (CrCi2)-alkoxy, unsubstituted or substituted cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted heterocyclyl, C(0)Rp, C(0)ORP, SRP, S(0)Rp, S02RP, NRpRq and C(0)NRpRq; wherein Rp and Rq are independently selected from hydrogen, unsubstituted or substituted (C1-C12) alkyl, unsubstituted or substituted aryl, unsubstituted or substituted aralkyl and unsubstituted or substituted heterocyclyl, or Rp and Rq can optionally form a 3-7 membered ring;

Examples of substituted alkyls include benzyl, hydroxymethyl, hydroxyethyl, 2-hydroxyethyl, N-morpholinomethyl, N-indolomethyl, piperidinylmethyl, trifluoromethyl and aminoethyl.

As used herein, the term "alkenyl" whether used alone or as part of a substituent group, refers to a straight or branched chain hydrocarbon radical containing the indicated number of carbon atoms and at least one carbon-carbon double bond (two adjacent sp2 carbon atoms). For example, (C2-Ci2)-alkenyl refers to an alkenyl group having 2 to 12 carbon atoms. Depending on the placement of double bond and substituents if any, the geometry of the double bond may be

entgegen (E), or zusammen (Z), cis or trans. Examples of alkenyl include, but are not limited to, vinyl, allyl and 2-propenyl.

A substituted alkenyl refers to an alkenyl group substituted with one or more groups selected from halogen, hydroxy, cyano, nitro, unsubstituted or substituted (CrCi2)-alkoxy, unsubstituted or substituted aryl, unsubstituted or substituted heterocyclyl, C(0)Rp, C(0)ORp, SRP, S(0)Rp, S02RP, NRpRq and C(0)NRpRq; wherein Rp and Rq are independently selected from hydrogen, unsubstituted or substituted (C1-C12) alkyl, unsubstituted or substituted aryl, unsubstituted or substituted aralkyl and unsubstituted or substituted heterocyclyl, or Rp and Rq can optionally form a 3-7 membered ring.

As used herein, the term "alkynyl" whether used alone or as part of a substituent group, refers to a straight or branched chain hydrocarbon radical containing the indicated number of carbon atoms and at least one carbon-carbon triple bond (two adjacent sp carbon atoms). For example, (C2-Ci2)-alkynyl refers to an alkynyl group having 2-12 carbon atoms. Examples of alkynyl include, but are not limited to, ethynyl, 1 -propynyl, 3-propynyl and 3-butynyl.

A substituted alkynyl refers to an alkynyl group substituted with one or more groups selected from halogen, hydroxy, cyano, nitro, unsubstituted or substituted (CrCi2)-alkoxy, unsubstituted or substituted aryl, unsubstituted or substituted heterocyclyl, C(0)Rp, C(0)ORp, SRP, S(0)Rp, S02Rp, NRpRq and C(0)NRpRq; wherein Rp and Rq are independently selected from hydrogen, unsubstituted or substituted (Ci-Ci2) alkyl, unsubstituted or substituted aryl, unsubstituted or substituted aralkyl and unsubstituted or substituted heterocyclyl, or Rp and Rq can optionally form a 3-7 membered ring.

As used herein, the term "alkoxyl" or "alkoxy" refers to a (Ci-Ci2)-alkyl having an oxygen radical attached thereto. Representative alkoxy groups include methoxy, ethoxy, propoxy, isopropoxy, isobutoxy and tert-butoxy.

A substituted alkoxy refers to an alkoxy group in which the alkyl is substituted with one or more groups selected from halogen, hydroxy, cyano, nitro, unsubstituted or substituted aryl, unsubstituted or substituted heterocyclyl, C(0)Rp, C(0)ORp, SRP, S(0)Rp, S02Rp, NRpRq and C(0)NRpRq; wherein Rp and Rq are independently selected from hydrogen, unsubstituted or substituted (Ci-Ci2) alkyl, unsubstituted or substituted aryl, unsubstituted or substituted aralkyl and unsubstituted or substituted heterocyclyl, or Rp and Rq can optionally form a 3-7 membered ring. Examples of substituted alkoxy are chloromethoxy, 2-cyanoethoxy, trifluoromethoxy and benzyloxy group. A benzyloxy group refers to a benzyl having an oxygen radical attached thereto.

The term "(C3-Ci2) cycloalkyl" or "cycloalkyl" refers to monocyclic or polycyclic hydrocarbon groups of 3-12 carbon atoms, which may be optionally bridged such as adamantyl.

The term "(C3-C7) cycloalkyl" refers to monocyclic hydrocarbon groups of 3-7 carbon atoms.

A substituted (C3-Ci2) cycloalkyl refers to a "(C3-Ci2) cycloalkyl" substituted by one or more substituents such as halogen, hydroxy, unsubstituted or substituted (C Ci2)-alkyl, (Ci-Ci2)-alkoxy cyano, nitro, unsubstituted or substituted aryl, unsubstituted or substituted heterocyclyl, C(0)Rp, C(0)ORp, SRP, S(0)Rp, S02Rp, NRpRq and C(0)NRpRq; wherein Rp and Rq are independently selected from hydrogen, unsubstituted or substituted (Ci-Ci2) alkyl, unsubstituted or substituted aryl, unsubstituted or substituted aralkyl and unsubstituted or substituted heterocyclyl, or Rp and Rq can optionally form a 3-7 membered ring.

The term "aryl" as used herein refers to monocyclic or polycyclic hydrocarbon groups having 6 to 14 ring carbon atoms in which the carbocyclic ring(s) present have a conjugated pi electron system. Examples of (C6-Ci4)-aryl residues are phenyl, naphthyl, fluorenyl or anthracenyl. Examples of (C6-Ci0)-aryl residues are phenyl or naphthyl. Aryl groups can be unsubstituted or substituted by one or more, for example 1 , 2, 3, 4 or 5, identical or different substituents selected from halogen, hydroxy, cyano, nitro, unsubstituted or substituted (Ci-Ci2) alkyl, unsubstituted or substituted (C2-Ci2)-alkenyl, unsubstituted or substituted (C2-Ci2)-alkynyl, unsubstituted or substituted (Ci-Ci2)-alkoxy, unsubstituted or substituted cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy, unsubstituted or substituted heterocyclyl, O-heterocyclyl, CF3, OCF3, C(0)Rp, C(0)ORp, SRP, S(0)Rp, S02Rp, NRpRq and C(0)NRpRq; wherein Rp and Rq are independently selected from hydrogen, unsubstituted or substituted (Ci-Ci2) alkyl, unsubstituted or substituted aryl, unsubstituted or substituted aralkyl and unsubstituted or substituted heterocyclyl, or Rp and Rq can optionally form a 3-7 membered ring.

In monosubstituted phenyl residues the substituent can be located in the 2-position, the 3-position, the 4-position or the 5-position. If the phenyl carries two substituents, they can be located in 2, 3-position, 2,4-position, 2, 5-position, 2,6-position, 3,4-position or 3, 5-position. Examples of monosubstituted phenyl groups are biphenyl, 4-phenoxyphenyl, 3-trifluoromethylphenyl, 4-chlorophenyl and 4-cyanophenyl. Examples of disubstituted phenyl groups are 3,5-difluorophenyl, 3-chloro-5-phenoxy phenyl and 3,4-dimethoxyphenyl.

As used herein, the term "aryloxy" refers to an aryl group having an oxygen radical attached thereto. The aryl of aryloxy group as used herein may also be defined as given herein above and may be unsubstituted or substituted. Representative aryloxy groups include phenyloxy, 4-chlorophenoxy, 3,4-dimethoxy phenoxy, etc.

The term "aralkyl" refers to an aryl group bonded directly through an alkyl group, such as benzyl. The aryl of the aralkyl group may be unsubstituted or substituted as explained in the definition of substituted aryl herein above.

The term "heteroatom" as used herein includes nitrogen, oxygen and sulfur. Any heteroatom with unsatisfied valency is assumed to have a hydrogen atom to satisfy the valency.

Heterocyclyl includes saturated heterocyclic ring systems, which do not contain any double bonds within the rings, as well as unsaturated heterocyclic ring systems, which contain one or more, for example, 3 double bonds within a ring, provided that the resulting mono, bi or tricyclic ring system is stable. The heterocyclyl group may, for example, have 1 or 2 oxygen atoms and/or 1 or 2 sulfur atoms and/or 1 to 3 nitrogen atoms in the ring. Examples of heterocyclyls include pyrrolyl, pyrrolidinyl, pyrazolyl, imidazolyl, pyrazinyl, piperazinyl, oxazolyl, isoxazolyl, thiazolyl, furyl, thienyl, pyridyl, pyrimidyl, piperidyl, benzothiazolyl, purinyl, benzimidazolyl, benzooxazolyl, indolyl, isoindolyl, isoquinolyl, morpholinyl, quinoxalinyl, and quinolyl. Aromatic heterocyclyl groups may also be referred to by the customary term "heteroaryl" for which all the definitions and explanations relating to heterocyclyl apply.

A substituted heterocyclyl refers to a heterocyclyl substituted with one or more groups selected from halogen, hydroxy, cyano, nitro, unsubstituted or substituted

(CrCi2)-alkyl, CF3, (C2-Ci2)-alkenyl, (C2-Ci2)-alkynyl, unsubstituted or substituted (CrCi2)-alkoxy, OCF3, unsubstituted or substituted cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy, heterocyclyl, -O-heterocyclyl, C(0)Rp, C(0)ORp, SRP, S(0)Rp, S02Rp, NRpRq and C(0)NRpRq; wherein Rp and Rq are independently selected from hydrogen, unsubstituted or substituted (C1-C12) alkyl, unsubstituted or substituted aryl, unsubstituted or substituted aralkyl and unsubstituted or substituted heterocyclyl, Rp and Rq can optionally form a 3-7 membered ring.

The substituents may be present on either the ring carbon or the ring nitrogen atoms. The substituents can be present at one or more positions provided that a stable molecule results.

The term "halogen" refers to a fluorine, chlorine, bromine, or iodine atom. The term "solvate" describes a complex wherein the compound is coordinated with a proportional amount of a solvent molecule. Specific solvates, wherein the solvent is water, are referred to as hydrates.

The term "tautomer" refers to the coexistence of two (or more) compounds that differ from each other only in the position of one (or more) mobile atoms and in electron distribution, for example, keto-enol tautomers.

Carboxylic acid isosteres refer to groups or molecules that have physical and chemical similarities to a carboxylic acid group, producing similar biological effects as those produced by a carboxylic acid group. Examples of carboxylic acid isosteres include groups selected from hydroxamic, acylcyanamide, phosphonate, sulfonate, sulfonamide, tetrazole, hydroxylisoxazole and oxadiazolone (The Practice of Medicinal Chemistry, Edited by Camille G. Wermuth, Second Edition, 2003, 189-214).

The term "N-oxide" as used herein refers to the oxide of the nitrogen atom of a nitrogen-containing heteroaryl or heterocycle. N-oxide can be formed in presence of an oxidizing agent for example peroxide such as m-chloro-perbenzoic acid or hydrogen peroxide. N-oxide is also known as amine-N-oxide, and is a chemical compound that contains N-»0 bond.

It will be understood that "substitution" or "substituted with" includes the implicit proviso that such substitution is in accordance with permitted valence of the substituted atom and the substituent, as well as represents a stable compound,

which does not readily undergo undesired transformation such as by rearrangement, cyclization, or elimination.

As used herein, the term "compound of formula 1 " includes all the stereoisomeric and tautomeric forms and mixtures thereof in all ratios, and their pharmaceutically acceptable salts, solvates, polymorphs, prodrugs, carboxylic acid isosteres and N-oxides.

Embodiments of the Invention

In an embodiment, the present invention provides compounds of formula 1 , wherein A is an unsubstituted aryl or an aryl substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (CrCi2)-alkoxy, cyano, nitro, unsubstituted or substituted (CrCi2)-alkyl, CF3, OCF3, (C2-Ci2)-alkenyl, (C2-Ci2)-alkynyl, unsubstituted or substituted cycloalkyi, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy, unsubstituted or substituted heterocyclyl, unsubstituted or substituted O-heterocyclyl, C(0)Rp, C(0)ORp, NRpRq, SRP and S(0)Rp and S02Rp, where Rp and Rq are as defined in formula 1 .

In an embodiment, the present invention provides compounds of formula 1 , wherein A is an unsubstituted aryl or an aryl substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (Ci-Ci2)-alkoxy, cyano, unsubstituted or substituted (CrCi2)-alkyl, CF3, OCF3, unsubstituted or substituted cycloalkyi, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy and unsubstituted or substituted heterocyclyl.

In another embodiment, the present invention provides compounds of formula 1 , wherein the aryl group of A may be fused with an unsubstituted or substituted 5 or 6-membered cycloalkyi ring optionally containing heteroatoms selected from O, N or S.

In a further embodiment, the present invention provides compounds of formula 1 , wherein A is an unsubstituted heterocyclyl or a heterocyclyl substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (Ci-Ci2)-alkoxy, CF3, OCF3, cyano, nitro, unsubstituted or substituted (CrCi2)-alkyl, (C2-Ci2)-alkenyl, (C2-Ci2)-alkynyl, unsubstituted or substituted cycloalkyi, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy, unsubstituted or substituted heterocyclyl, unsubstituted or substituted O-heterocyclyl, C(0)Rp, C(0)ORp, NRpRq, SRP, S(0)Rp and S02RP, where Rp and Rq are as defined in formula 1.

In a further embodiment, the present invention provides compounds of formula 1 , wherein A is an unsubstituted heterocyclyl or a heterocyclyl substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (CrCi2)-alkoxy, CF3, OCF3, cyano, unsubstituted or substituted (C1-C12)-alkyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy and unsubstituted or substituted heterocyclyl.

In a still further embodiment, the present invention provides compounds of formula 1 , wherein A is an unsubstituted (CrCi2)-alkyl or (Ci-Ci2)-alkyl substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (Ci-Ci2)-alkoxy, cyano, nitro, unsubstituted or substituted cycloalkyl, unsubstituted or substituted aryl, C(0)Rp, C(0)ORp, NRpRq, SRP, S(0)Rp and S02Rp, where Rp and Rq are as defined in formula 1 .

In a still further embodiment, the present invention provides compounds of formula 1 , wherein A is an unsubstituted (Ci-Ci2)-alkyl or (Ci-Ci2)-alkyl substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (Ci-Ci2)-alkoxy, cyano, unsubstituted or substituted cycloalkyl and unsubstituted or substituted aryl.

In another embodiment, the present invention provides compounds of formula

1 , wherein A is an unsubstituted (C3-Ci2)-cycloalkyl or (C3-Ci2)-cycloalkyl substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted (Ci-Ci2)-alkoxy, cyano, nitro, unsubstituted or substituted aryl, unsubstituted or substituted heterocyclyl, C(0)Rp, C(0)ORp, NRpRq, SRP, S(0)Rp and S02Rp, where Rp and Rq are as defined in formula 1.

In another embodiment, the present invention provides compounds of formula 1 , wherein A is an unsubstituted (C3-Ci2)-cycloalkyl or (C3-Ci2)-cycloalkyl substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted (Ci-Ci2)-alkoxy, cyano, unsubstituted or substituted aryl and unsubstituted or substituted heterocyclyl.

In an embodiment, the present invention provides compounds of formula 1 , wherein n is 0.

In another embodiment, the present invention provides compounds of formula 1 , wherein n is 1 .

In an embodiment, the present invention provides compounds of formula 1 , wherein L is *CONH.

In another embodiment, the present invention provides compounds of formula

1 , wherein L is NHC(0)NH.

In yet another embodiment, the present invention provides compounds of formula 1 , wherein L is NHC(S)NH.

In a still further embodiment, the present invention provides compounds of formula 1 , wherein L is *S02NH.

In an embodiment, the present invention provides compounds of formula 1 , wherein X3 is C, to which A-(CH2)n-L- is attached; and Xi, X2, X4 and X5 are independently selected from CH and CR; wherein R is selected from halogen, hydroxy, unsubstituted or substituted (CrCi2)-alkoxy, cyano, unsubstituted or substituted (C Ci2)-alkyl, CF3, OCF3, (C2-Ci2)-alkenyl, (C2-Ci2)-alkynyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy, unsubstituted or substituted heterocyclyl, unsubstituted or substituted O-heterocyclyl, C(0)Rp, C(0)ORp, NRpRq, SRP, S(0)Rp and S02Rp, where Rp and Rq are as defined in formula 1.

In an embodiment, the present invention provides compounds of formula 1 , wherein X3 is C, to which A-(CH2)n-L- is attached; and Xi, X2, X4 and X5 are independently selected from CH and CR; wherein R is selected from halogen, hydroxy, unsubstituted or substituted (Ci-Ci2)-alkoxy, cyano, unsubstituted or substituted (Ci-Ci2)-alkyl, CF3, OCF3, unsubstituted or substituted cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy and unsubstituted or substituted heterocyclyl.

In another embodiment, the present invention provides compounds of formula 1 , wherein X3 is C, to which A-(CH2)n-L- is attached; X4 is N; and Xi, X2 and X5 are independently selected from CH and CR; wherein R is selected from halogen, hydroxy, unsubstituted or substituted (Ci-Ci2)-alkoxy, cyano, unsubstituted or substituted (C Ci2)-alkyl, CF3, OCF3, (C2-Ci2)-alkenyl, (C2-Ci2)-alkynyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy, unsubstituted or substituted heterocyclyl, unsubstituted or substituted O-heterocyclyl, C(0)Rp, C(0)ORp, NRpRq, SRP, S(0)Rp and S02RP, where Rp and Rq are as defined in formula 1

In another embodiment, the present invention provides compounds of formula 1 , wherein X3 is C, to which A-(CH2)n-L- is attached; X4 is N; and Xi, X2 and X5 are independently selected from CH and CR; wherein R is selected from halogen, hydroxy, unsubstituted or substituted (CrCi2)-alkoxy, cyano, unsubstituted or substituted (Ci-Ci2)-alkyl, CF3, OCF3, unsubstituted or substituted cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy and unsubstituted or substituted heterocyclyl.

In yet another embodiment, the present invention provides compounds of formula 1 , wherein X3 is C, to which A-(CH2)n-L- is attached; X4 and X5 are N, and Xi and X2 are independently selected from CH and CR; wherein R is selected from halogen, hydroxy, unsubstituted or substituted (Ci-Ci2)-alkoxy, cyano, unsubstituted or substituted (d-Ci2)-alkyl, CF3, OCF3, (C2-Ci2)-alkenyl, (C2-Ci2)-alkynyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy, unsubstituted or substituted heterocyclyl, unsubstituted or substituted O-heterocyclyl, C(0)Ri, C(0)ORp, NRpRq, SRP, S(0)Rp and S02Rp, where Rp and Rq are as defined in formula 1

In yet another embodiment, the present invention provides compounds of formula 1 , wherein X3 is C, to which A-(CH2)n-L- is attached; X4 and X5 are N, and Xi and X2 are independently selected from CH and CR; wherein R is selected from halogen, hydroxy, unsubstituted or substituted (Ci-Ci2)-alkoxy, cyano, unsubstituted or substituted (CrCi2)-alkyl, CF3, OCF3, unsubstituted or substituted cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy, unsubstituted or substituted heterocyclyl.

In a further embodiment, the present invention provides compounds of formula 1 , wherein X3 is C, to which A-(CH2)n-L- is attached; Xi and X4 are N, and X2 and X5 are independently selected from CH and CR; wherein R is selected from halogen, hydroxy, (Ci-Ci2)-alkoxy, cyano, unsubstituted or substituted (CrCi2)-alkyl, CF3, OCF3, (C2-Ci2)-alkenyl, (C2-Ci2)-alkynyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy, unsubstituted or substituted heterocyclyl, unsubstituted or substituted O-heterocyclyl, C(0)Rp, C(0)ORp, NRpRq, SRP, S(0)Rp and S02RP, where Rp and Rq are as defined in formula 1.

In a further embodiment, the present invention provides compounds of formula 1 , wherein X3 is C, to which A-(CH2)n-L- is attached; Xi and X4 are N, and X2 and X5 are independently selected from CH and CR; wherein R is selected from halogen, hydroxy, (CrCi2)-alkoxy, cyano, unsubstituted or substituted (CrCi2)-alkyl, CF3, unsubstituted or substituted cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy and unsubstituted or substituted heterocyclyl.

In an embodiment, the present invention provides compounds of formula 1 , wherein Yi is CH2 and Y2 is C=0.

In another embodiment, the present invention provides compounds of formula 1 , wherein Yi is C=0 and Y2 is CH2.

In a further embodiment, the present invention provides compounds of formula 1 , wherein Yi is C=0 and Y2 is C=0.

In a still further embodiment, the present invention provides compounds of formula 1 , wherein Yi is CH2 and Y2 is CH2.

In an embodiment, the present invention provides compounds of formula 1 , wherein m is 1 and Ra and Rb are selected from Ri and R2, wherein Ri and R2 are independently selected from hydrogen, unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted aryl, unsubstituted or substituted aralkyl and unsubstituted or substituted heterocyclyl.

In another embodiment, the present invention provides compounds of formula 1 , wherein m is 2, and Ra and Rb are selected from R1 ; R2, R3 and R4, wherein R1 ; R2, R3 and R4 are independently selected from hydrogen, unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted aryl, unsubstituted or substituted aralkyl and unsubstituted or substituted heterocyclyl.

In another embodiment, the present invention provides compounds of formula 1 , wherein m is 3, and Ra and Rb are selected from R1 ; R2, R3, R4, R5 and R6, wherein R1 ; R2, R3, R4, R5, R6, R7 and R8 are independently selected from hydrogen, unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted aryl, unsubstituted or substituted aralkyl and unsubstituted or substituted heterocyclyl.

In another embodiment, the present invention provides compounds of formula 1 , wherein m is 4, and Ra and Rb are selected from R1 ; R2, R3, R4, R5, R6, R7 and R8, wherein R1 ; R2, R3, R4, R5, Re, R7 and R8 are independently selected from hydrogen, unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted aryl, unsubstituted or substituted aralkyi and unsubstituted or substituted heterocyclyl.

In an embodiment, the present invention provides compounds of formula 1 , wherein m is 1 and Ri and R2 form a (C3-C12) cycloalkyl ring.

In an embodiment, the present invention provides compounds of formula 1 , wherein m is 1 and Ri and R2 form a (C3-C7) cycloalkyl ring.

In an embodiment, the present invention provides compounds of formula 1 , wherein m is 1 and Ri and R2 form an adamantyl ring.

In another embodiment, the present invention provides compounds of formula

1 , wherein m is 2 and any two of Ri , R2, R3 and R4 form a (C3-Ci2) cycloalkyl ring and the remaining substituents are hydrogen.

In another embodiment, the present invention provides compounds of formula 1 , wherein m is 2 and any two of Ri, R2, R3 and R4 form a (C3-C7) cycloalkyl ring and the remaining substituents are hydrogen.

In another embodiment, the present invention provides compounds of formula 1 , wherein m is 2 and any two of Ri , R2, R3 and R4 form an adamantyl ring and the remaining substituents are hydrogen.

In another embodiment, the present invention provides compounds of formula 1 , wherein m is 3 and any two of Ri , R2, R3, R4, R5 and R6 form a (C3-Ci2) cycloalkyl ring and the remaining substituents are hydrogen.

In another embodiment, the present invention provides compounds of formula 1 , wherein m is 3 and any two of Ri , R2, R3, R4, R5 and R6 form a (C3-C7) cycloalkyl ring and the remaining substituents are hydrogen.

In another embodiment, the present invention provides compounds of formula 1 , wherein m is 3 and any two of Ri , R2, R3, R4, R5 and R6 form an adamantyl ring and the remaining substituents are hydrogen.

In another embodiment, the present invention provides compounds of formula 1 , wherein m is 4 and any two of Ri , R2, R3, R4, R5, Re, R7 and R8 form a (C3-Ci2) cycloalkyl ring and the remaining substituents are hydrogen.

In another embodiment, the present invention provides compounds of formula 1 , wherein m is 4 and any two of Ri , R2, R3, R4, R5, Re, R7 and R8 form a (C3-C7) cycloalkyl ring and the remaining substituents are hydrogen.

In another embodiment, the present invention provides compounds of formula 1 , wherein m is 4 and any two of Ri, R2, R3, R4, R5, Re, R7 and R8 form an adamantyl ring and the remaining substituents are hydrogen.

In an embodiment, the present invention provides compounds of formula 1 , wherein, R9 is selected from hydrogen, unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted aryl, unsubstituted or substituted aralkyl and unsubstituted or substituted heterocyclyl.

In another embodiment, the present invention provides compounds of formula 1 , wherein R9 is unsubstituted or substituted (CrCi2)-alkyl, wherein (CrCi2)-alkyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, (Ci-Ci2)-alkoxy, cyano and aryl.

In another embodiment, the present invention provides compounds of formula 1 , wherein R9 is hydrogen.

In an embodiment, the compounds of formula 1 encompass compounds of formula 1 a:

Formula 1 a

in all their stereoisomeric and tautomeric forms, their pharmaceutically acceptable salts, solvates, polymorphs, prodrugs, N-oxides and carboxylic acid isosteres;

wherein,

A is selected from unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted (C3-Ci2)-cycloalkyl, unsubstituted or substituted aryl and unsubstituted or substituted heterocyclyl; wherein the aryl group may be fused with an unsubstituted or substituted 5 or 6-membered cycloalkyi ring optionally containing heteroatoms selected from O, N or S;

n is 0 or 1 ;

L is selected from NHC(0)NH, NHC(S)NH, *NHS02, *CONH and *S02NH; wherein * indicates the point of attachment to A-[CH2]n-;

Xi, X2, X4 and X5 are independently selected from N, N-oxide, CH and CR; wherein R is selected from halogen, hydroxy, (Ci-Ci2)-alkoxy, cyano, (CrCi2)-alkyl, CF3, OCF3, (C2-Ci2)-alkenyl, (C2-Ci2)-alkynyl, (C3-Ci2)-cycloalkyl, aryl, aryloxy, heterocyclyl, O-heterocyclyl, C(0)Rp, C(0)ORp, NRpRq, SRP, S(0)Rp, S02Rp and C(0)NRpRq;

Rp and Rq are independently selected from hydrogen, unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted aryl, unsubstituted or substituted aralkyi and unsubstituted or substituted heterocyclyl, or Rp and Rq can optionally form a 3-7 membered ring;

Yi and Y2 are independently selected from C=0 and CH2;

m is an integer selected from 1 to 4; wherein,

when m is 1 , Ra and Rb may be selected from R-\ and R2;

when m is 2, Ra and Rb may be selected from R1 ; R2, R3 and R4;

when m is 3, Ra and Rb may be selected from R1 ; R2, R3, R4, R5 and R6;

when m is 4, Ra and Rb may be selected from R1 ; R2, R3, R4, R5, R6, R7 and

Re!

Ri , R2, R3, R4, R5, Re, R7 and R8 are independently selected from hydrogen, unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted aryl, unsubstituted or substituted aralkyi and unsubstituted or substituted heterocyclyl;

or any two of Ri , R2, R3, R4, R5, Re, R7 and R8 can form a (C3-Ci2) cycloalkyl ring;

R9 is selected from hydrogen, unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted aryl, unsubstituted or substituted aralkyi and unsubstituted or substituted heterocyclyl;

wherein,

(Ci-Ci2)-alkyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (Ci-Ci2)-alkoxy, cyano, nitro, unsubstituted or substituted (C3-Ci2)-cycloalkyl, unsubstituted or substituted aryl, C(0)Rp, C(0)ORp, NRpRq, SRP, S(0)Rp and S02Rp;

(C3-Ci2)-cycloalkyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (Ci-Ci2)-alkoxy cyano, nitro, unsubstituted or substituted aryl, unsubstituted or substituted heterocyclyl, C(0)Rp, C(0)ORp, NRpRq, SRP, S(0)Rp and S02Rp;

aryl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (CrCi2)-alkoxy, cyano, nitro, unsubstituted or substituted (C Ci2)-alkyl, CF3, OCF3, (C2-Ci2)-alkenyl, (C2-Ci2)-alkynyl, unsubstituted or substituted (C3-Ci2)-cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy, unsubstituted or substituted heterocyclyl, unsubstituted or substituted O-heterocyclyl, C(0)Rp, C(0)ORp, NRpRq, SRP, S(0)Rp and S02Rp, or aryl may be fused with an unsubstituted or substituted 5 or 6-membered cycloalkyl ring optionally containing heteroatoms selected from O, N and S;

heterocyclyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (Ci-Ci2)-alkoxy, cyano, nitro, unsubstituted or substituted (C Ci2)-alkyl, CF3, OCF3, (C2-Ci2)-alkenyl, (C2-Ci2)-alkynyl, unsubstituted or substituted (C3-Ci2)-cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy, unsubstituted or substituted heterocyclyl, unsubstituted or substituted O-heterocyclyl, C(0)Rp, C(0)ORp, NRpRq, SRP, S(0)Rp and S02Rp; and

Rp and Rq are independently selected from hydrogen, unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted aryl, unsubstituted or substituted aralkyl and unsubstituted or substituted heterocyclyl, or Rp and Rq can optionally form a 3-7 membered ring.

In an embodiment, the compounds of formula 1 encompass compounds of formula 1 a, in all their stereoisomeric and tautomeric forms, their pharmaceutically acceptable salts, solvates, polymorphs, prodrugs, N-oxides and carboxylic acid isosteres;

wherein,

A is selected from unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted (C3-Ci2)-cycloalkyl, unsubstituted or substituted aryl and unsubstituted or substituted heterocyclyl; wherein the aryl group may be fused with an unsubstituted or substituted 5 or 6-membered cycloalkyl ring optionally containing heteroatoms selected from O, N or S;

n is 0 or 1 ;

L is selected from NHC(0)NH, NHC(S)NH, *NHS02, *CONH and *S02NH; wherein * indicates the point of attachment to A-[CH2]n-;

Χι , X2, X4 and X5 are independently selected from N, N-oxide, CH and CR; wherein R is selected from halogen, hydroxy, (CrCi2)-alkoxy, cyano, (CrCi2)-alkyl, CF3, OCF3, (C3-Ci2)-cycloalkyl, aryl, aryloxy, heterocyclyl;

Yi and Y2 are independently selected from C=0 and CH2;

m is an integer selected from 1 to 4; wherein,

when m is 1 , Ra and Rb may be selected from R-\ and R2;

when m is 2, Ra and Rb may be selected from R1 ; R2, R3 and R4;

when m is 3, Ra and Rb may be selected from R1 ; R2, R3, R4, R5 and R6;

when m is 4, Ra and Rb may be selected from R1 ; R2, R3, R4, R5, R6, R7 and R8;

Ri , R2, R3, R4, R5, Re, R7 and R8 are independently selected from hydrogen, unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted aryl, unsubstituted or substituted aralkyl and unsubstituted or substituted heterocyclyl;

or any two of Ri , R2, R3, R4, R5, Re, R7 and R8 can form a (C3-Ci2) cycloalkyi ring;

R9 is selected from hydrogen and unsubstituted or substituted (Ci -Ci2)-alkyl;

wherein,

(Ci -Ci2)-alkyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (Ci -Ci2)-alkoxy, cyano, nitro, unsubstituted or substituted (C3-Ci2)-cycloalkyl and unsubstituted or substituted aryl, (C3-Ci2)-cycloalkyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (Ci -Ci2)-alkoxy cyano, unsubstituted or substituted aryl and unsubstituted or substituted heterocyclyl;

aryl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (Ci -Ci2)-alkoxy, cyano, unsubstituted or substituted (CrCi2)-alkyl, CF3, OCF3, unsubstituted or substituted (C3-Ci2)-cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy and unsubstituted or substituted heterocyclyl, or aryl may be fused with an unsubstituted or substituted 5 or 6-membered cycloalkyi ring optionally containing heteroatoms selected from O, N and S; and

heterocyclyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (Ci -Ci2)-alkoxy, cyano, unsubstituted or substituted (CrCi2)-alkyl, CF3, OCF3, unsubstituted or substituted (C3-Ci2)-cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy and unsubstituted or substituted heterocyclyl.

In an embodiment, the compounds of formula 1 encompass compounds of formula 1 a, in all their stereoisomeric and tautomeric forms, their pharmaceutically acceptable salts, solvates, polymorphs, prodrugs, N-oxides and carboxylic acid isosteres;

wherein,

A is selected from unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted (C3-Ci2)-cycloalkyl, unsubstituted or substituted aryl and unsubstituted or substituted heterocyclyl; wherein aryl group may be fused with an unsubstituted or substituted 5 or 6-membered cycloalkyl ring optionally containing heteroatoms selected from O, N or S;

n is 0 or 1 ;

L is *C(0)NH wherein * indicates the point of attachment to A-[CH2]n-;

X2 is selected from CH and CR; Xi , X4 and X5 are independently selected from CH, CR and N; wherein R is selected from halogen, hydroxy, (Ci-Ci2)-alkoxy, cyano, (Ci-Ci2)-alkyl, CF3, OCF3 and cycloalkyl;

Yi and Y2 are independently selected from C=0 and CH2;

m is an integer selected from 1 to 4; wherein,

when m=1 , Ra and Rb may be selected from R-\ and R2;

when m=2, Ra and Rb may be selected from Ri , R2, R3 and R4;

when m=3, Ra and Rb may be selected from R1 ; R2, R3, R4, R5 and R6;

when m=4, Ra and Rb may be selected from R1 ; R2, R3, R4, R5, R6, R7 and R8; Ri , R2, R3, R4, R5, Re, R7 and R8 are independently selected from hydrogen, unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted aryl; and unsubstituted or substituted aralkyl; or any two of Ri, R2, R3, R4, R5, Re, R7 and R8 form a (C3-Ci2) cycloalkyl ring; and

R9 is selected from hydrogen and unsubstituted (CrC6)-alkyl;

wherein,

(Ci-Ci2)-alkyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (Ci-Ci2)-alkoxy, cyano, nitro, unsubstituted or substituted (C3-Ci2)-cycloalkyl and unsubstituted or substituted aryl, (C3-Ci2)-cycloalkyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (CrCi2)-alkoxy cyano, unsubstituted or substituted aryl and unsubstituted or substituted heterocyclyl;

aryl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (CrCi2)-alkoxy, cyano, unsubstituted or substituted (CrCi2)-alkyl, CF3, OCF3, unsubstituted or substituted (C3-Ci2)-cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy and unsubstituted or substituted heterocyclyl, or aryl may be fused with an unsubstituted or substituted 5 or 6-membered cycloalkyi ring optionally containing heteroatoms selected from O, N and S; and

heterocyclyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (Ci-Ci2)-alkoxy, cyano, unsubstituted or substituted (CrCi2)-alkyl, CF3, OCF3, unsubstituted or substituted (C3-Ci2)-cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy and unsubstituted or substituted heterocyclyl.

In an embodiment, the compounds of formula 1 encompass compounds of formula 1 a, in all their stereoisomeric and tautomeric forms, their pharmaceutically acceptable salts, solvates, polymorphs, prodrugs, N-oxides and carboxylic acid isosteres;

wherein,

A is selected from unsubstituted or substituted aryl and unsubstituted or substituted heterocyclyl;

n is 0;

L is *C(0)NH wherein * indicates the point of attachment to A-[CH2]n-;

Xi , X2, X4 and X5 are independently selected from CH and CR; wherein R is selected from halogen, hydroxy, (Ci-Ci2)-alkoxy, cyano, (CrCi2)-alkyl, CF3 and OCF3;

Yi is CH2 and Y2 is C=0;

m is 1 ; wherein Ra and Rb may be selected from R-\ and R2;

Ri and R2 are independently selected from hydrogen and unsubstituted or substituted (d-Ci2)-alkyl; and

R9 is selected from hydrogen and unsubstituted (CrC6)-alkyl;

wherein,

aryl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (CrCi2)-alkoxy, unsubstituted or substituted (CrCi2)-alkyl, CF3, OCF3, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy and unsubstituted or substituted heterocyclyl, or aryl may be fused with an unsubstituted or substituted 5 or 6-membered cycloalkyi ring optionally containing heteroatoms selected from O, N and S; and

heterocyclyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (CrCi2)-alkoxy, unsubstituted or substituted (CrCi2)-alkyl, CF3, OCF3, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy and unsubstituted or substituted heterocyclyl.

In an embodiment, the compounds of formula 1 encompass compounds of formula 1 a, in all their stereoisomeric and tautomeric forms, their pharmaceutically acceptable salts, solvates, polymorphs, prodrugs, N-oxides and carboxylic acid isosteres;

wherein,

A is selected from unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted aryl and unsubstituted or substituted heterocyclyl; wherein aryl group may be fused with an unsubstituted or substituted 5 or 6-membered cycloalkyi ring optionally containing heteroatoms selected from O, N or S;

n is 0 or 1 ;

L is selected from NHC(0)NH and NHC(S)NH ;

X2 is selected from CH and CR; Xi , X4 and X5 are independently selected from CH, CR and N; wherein R is selected from halogen, hydroxy, (Ci-Ci2)-alkoxy, cyano, (Ci-Ci2)-alkyl, CF3, OCF3 and cycloalkyi;

Yi and Y2 are independently selected from C=0 and CH2;

m is an integer selected from 1 to 4; wherein,

when m is 1 , Ra and Rb may be selected from R-\ and R2;

when m is 2, Ra and Rb may be selected from R1 ; R2, R3 and R4;

when m is 3, Ra and Rb may be selected from R1 ; R2, R3, R4, R5 and R6;

when m is 4, Ra and Rb may be selected from Ri , R2, R3, R4, R5, Re, R7 and

Rs; Ri , R2, R3, R4, R5, Re, R7 and R8 are independently selected from hydrogen, unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or

substituted aryl; and unsubstituted or substituted aralkyl; or any two of Ri , R2, R3, R4, R5, Re, R7 and R8 form a (C3-C12) cycloalkyi ring; and

R9 is selected from hydrogen and unsubstituted (CrC6)-alkyl;

wherein,

(CrCi2)-alkyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (CrCi2)-alkoxy, cyano, unsubstituted or substituted (C3-Ci2)-cycloalkyl and unsubstituted or substituted aryl,

(C3-Ci2)-cycloalkyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (Ci -Ci2)-alkoxy cyano, unsubstituted or substituted aryl and unsubstituted or substituted heterocyclyl;

aryl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (Ci -Ci2)-alkoxy, cyano, unsubstituted or substituted (CrCi2)-alkyl, CF3, OCF3, unsubstituted or substituted (C3-C12)-cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy and unsubstituted or substituted heterocyclyl, or aryl may be fused with an unsubstituted or substituted 5 or 6-membered cycloalkyi ring optionally containing heteroatoms selected from O, N and S; and

heterocyclyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (Ci -Ci2)-alkoxy, cyano, unsubstituted or substituted (CrCi2)-alkyl, CF3, OCF3, unsubstituted or substituted (C3-C12)-cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy and unsubstituted or substituted heterocyclyl.

In an embodiment, the compounds of formula 1 encompass compounds of formula 1 a, in all their stereoisomeric and tautomeric forms, their pharmaceutically acceptable salts, solvates, polymorphs, prodrugs, N-oxides and carboxylic acid isosteres;

wherein,

A is selected from unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted aryl and unsubstituted or substituted heterocyclyl; wherein aryl group may be fused with an unsubstituted or substituted 5 or 6-membered cycloalkyi ring optionally containing heteroatoms selected from O, N or S;

n is 0 or 1 ;

L is *S02NH wherein * indicates the point of attachment to A-[CH2]n-;

X2 is selected from CH and CR; Xi , X4 and X5 are independently selected from CH , CR and N ; wherein R is selected from halogen, hydroxy, (CrCi2)-alkoxy, cyano, (Ci -Ci2)-alkyl, CF3, OCF3 and cycloalkyi;

Yi and Y2 are independently selected from C=0 and CH2;

m is an integer selected from 1 to 4; wherein,

when m is 1 , Ra and Rb may be selected from R-\ and R2;

when m is 2, Ra and Rb may be selected from R1 ; R2, R3 and R4;

when m is 3, Ra and Rb may be selected from R1 ; R2, R3, R4, R5 and R6;

when m is 4, Ra and Rb may be selected from R1 ; R2, R3, R4, R5, R6, R7 and R8; Ri , R2, R3, R4, R5, Re, R7 and R8 are independently selected from hydrogen, unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted aryl; and unsubstituted or substituted aralkyl; or any two of Ri , R2,

R3, R4, R5, Re, R7 and R8 form a (C3-Ci2) cycloalkyi ring; and

Rg is selected from hydrogen and unsubstituted (CrCe)-alkyl.

wherein,

(Ci -Ci2)-alkyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (Ci -Ci2)-alkoxy, cyano, unsubstituted or substituted (C3-Ci2)-cycloalkyl and unsubstituted or substituted aryl,

(C3-Ci2)-cycloalkyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (Ci -Ci2)-alkoxy cyano, unsubstituted or substituted aryl and unsubstituted or substituted heterocyclyl;

aryl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (Ci -Ci2)-alkoxy, cyano, unsubstituted or substituted (CrCi2)-alkyl, CF3, OCF3, unsubstituted or substituted (C3-C12)-cycloalkyi, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy and unsubstituted or substituted heterocyclyl, or aryl may be fused with an unsubstituted or substituted 5 or 6-membered cycloalkyi ring optionally containing heteroatoms selected from O, N and S; and

heterocyclyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (Ci -Ci2)-alkoxy, cyano, unsubstituted or substituted (CrCi2)-alkyl, CF3, OCF3, unsubstituted or substituted (C3-Ci2)-cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy and unsubstituted or substituted heterocyclyl.

In an embodiment, the compounds of formula 1 encompass compounds of formula 1 b:

Formula 1 b

wherein,

A is selected from unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted (C3-Ci2)-cycloalkyl, unsubstituted or substituted aryl and unsubstituted or substituted heterocyclyl; wherein the aryl group may be fused with an unsubstituted or substituted 5 or 6-membered cycloalkyi ring optionally containing heteroatoms selected from O, N or S;

n is 0 or 1 ;

L is selected from NHC(0)NH, NHC(S)NH, *NHS02, *CONH and *S02NH; wherein * indicates the point of attachment to A-[CH2]n-;

Xi, X2, X4 and X5 are independently selected from N, N-oxide, CH and CR; wherein R is selected from halogen, hydroxy, (Ci-Ci2)-alkoxy, cyano, (CrCi2)-alkyl, CF3, OCF3, (C2-Ci2)-alkenyl, (C2-Ci2)-alkynyl, (C3-Ci2)-cycloalkyl, aryl, aryloxy, heterocyclyl, O-heterocyclyl, C(0)Rp, C(0)ORp, NRpRq, SRP, S(0)Rp, S02Rp and C(0)NRpRq;

Rp and Rq are independently selected from hydrogen, unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted aryl, unsubstituted or substituted aralkyl and unsubstituted or substituted heterocyclyl, or Rp and Rq can optionally form a 3-7 membered ring;

Yi and Y2 are independently selected from C=0 and CH2;

R9 is selected from hydrogen, unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted aryl, unsubstituted or substituted aralkyl and unsubstituted or substituted heterocyclyl; and

Y is a cycloalkyi ring selected from:

•o--o wherein m=4; and

wherein,

(CrCi2)-alkyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (CrCi2)-alkoxy, cyano, unsubstituted or substituted (C3-Ci2)-cycloalkyl, unsubstituted or substituted aryl;

(C3-Ci2)-cycloalkyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (Ci-Ci2)-alkoxy cyano, unsubstituted or substituted aryl, unsubstituted or substituted heterocyclyl;

aryl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (Ci-Ci2)-alkoxy, cyano, unsubstituted or substituted (CrCi2)-alkyl, CF3, OCF3, unsubstituted or substituted (C3-Ci2)-cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy, unsubstituted or substituted heterocyclyl, or aryl may be fused with an unsubstituted or substituted 5 or 6-membered cycloalkyi ring optionally containing heteroatoms selected from O, N and S; and

heterocyclyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (Ci-Ci2)-alkoxy, cyano, unsubstituted or substituted (CrCi2)-alkyl, CF3, OCF3, unsubstituted or substituted (C3-Ci2)- cycloalkyi, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy and unsubstituted or substituted heterocyclyl.

In an embodiment, the present invention provides compounds of formula 1 selected from:

(S)-Methyl 2-(6-(4-(3-(4-fluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate;

(S)-2-(6-(4-(3-(4-Fluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-Methyl 2-(6-(4-(3-(2,4-difluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(3-(2,4-Difluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(6-(4-(3-(2-fluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate;

(S)-2-(6-(4-(3-(2-Fluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-Methyl 2-(6-(4-(3-(3-fluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(3-(3-Fluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(3-phenylureido)phenyl)isoindolin-2-yl) butanoate; (S)-3-Methyl-2-(1 -oxo-6-(4-(3-phenylureido)phenyl)isoindolin-2-yl)butanoic acid; (S)-Methyl 2-(6-(4-(3-benzylureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate; (S)-2-(6-(4-(3-Benzylureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-Methyl 2-(6-(4-(3-(2,6-difluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(3-(2,6-Difluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(3-m-tolylureido)phenyl)isoindolin-2-yl) butanoate; (S)-3-Methyl-2-(1 -oxo-6-(4-(3-m-tolylureido)phenyl)isoindolin-2-yl)butanoic acid; (S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(3-p-tolylureido)phenyl)isoindolin-2-yl) butanoate; (S)-3-Methyl-2-(1 -oxo-6-(4-(3-p-tolylureido)phenyl)isoindolin-2-yl)butanoic acid; (S)-Methyl 2-(6-(4-(3-(3-methoxyphenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(3-(3-Methoxyphenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-Methyl-2-(6-(4-(3-(4-methoxyphenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(3-(4-Methoxyphenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl-2-(6-(4-(3-(3,5-difluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(3-(3,5-Difluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(6-(4-(3-(3,4-difluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(3-(3,4-Difluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(6-(4-(3-cyclohexylureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(3-Cyclohexylureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(3-(4-(trifluoromethyl)phenyl)ureido)phenyl) isoindolin-2-yl)butanoate;

(S)-3-Methyl-2-(1 -oxo-6-(4-(3-(4-(trifluoromethyl)phenyl)ureido)phenyl) isoindolin-2-yl)butanoic acid;

(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl) isoindolin-2-yl)butanoate;

(S)-3-Methyl-2-(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl) isoindolin-2-yl)butanoic acid;

(S)-Methyl 2-(6-(4-(3-(4-cyanophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(3-(4-Cyanophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-Methyl 2-(6-(4-(3-(3-cyanophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(3-(3-Cyanophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)- Methyl 2-(6-(4-(3-(4-chloro-2-phenoxyphenyl) ureido) phenyl)-1 -oxo isoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(3-(4-Chloro-2-phenoxyphenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(6-(4-(3-(5-chloro-2-phenoxyphenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(3-(5-Chloro-2-phenoxyphenyl) ureido) phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(3-(2-phenoxyphenyl)ureido)phenyl) isoindolin-2-yl)butanoate;

(S)-3-Methyl-2-(1 -oxo-6-(4-(3-(2-phenoxyphenyl)ureido)phenyl)isoindolin-2-yl)butanoic acid;

(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(3-(4-phenoxyphenyl)ureido)phenyl) isoindolin-2-yl)butanoate;

(S)-3-Methyl-2-(1 -oxo-6-(4-(3-(4-phenoxyphenyl)ureido)phenyl)isoindolin-2-yl)butanoic acid;

(S)-Methyl 2-(6-(4-(3-(2-fluorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(3-(2-Fluorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(3-p-tolylthioureido)phenyl)isoindolin-2-yl)butanoate;

(S)-3-Methyl-2-(1 -oxo-6-(4-(3-p-tolylthioureido)phenyl)isoindolin-2-yl)butanoic acid; (S)-Methyl 2-(6-(4-(3-(3-fluorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(3-(3-Fluorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(6-(4-(3-(4-methoxyphenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(3-(4-Methoxyphenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(6-(4-(3-(3-methoxyphenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(3-(3-Methoxyphenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(6-(4-(3-(4-chlorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(3-(4-Chlorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-Methyl 2-(6-(4-(3-(4-chlorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(3-(3-Chlorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(3-(2-(trifluoromethyl)phenyl)thioureido) phenyl) isoindolin-2-yl)butanoate;

(S)-3-Methyl-2-(1 -oxo-6-(4-(3-(2-trifluoromethyl)phenyl)thioureido)phenyl) isoindolin-2-yl)butanoic acid;

(S)-Methyl 2-(6-(4-(3-(4-cyanophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(3-(4-Cyanophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-Methyl 2-(6-(4-(3-(4-cyanophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(3-(3-Cyanophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(3-o-tolylthioureido)phenyl)isoindolin-2-yl)butanoate;

(S)-3-Methyl-2-(1 -oxo-6-(4-(3-o-tolylthioureido)phenyl)isoindolin-2-yl)butanoic acid; (S)-Methyl 2-(6-(4-(3-(2-methoxyphenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(3-(2-Methoxyphenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)thioureido) phenyl)isoindolin-2-yl)butanoate;

(S)-3-Methyl-2-(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)thioureido)phenyl) isoindolin-2-yl)butanoic acid;

(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(phenylsulfonamido)phenyl)isoindolin-2-yl)butanoate;

(S)-3-Methyl-2-(1 -oxo-6-(4-(phenylsulfonamido)phenyl)isoindolin-2-yl)butanoic acid; (S)-Methyl 2-(6-(4-(4-cyanophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(4-Cyanophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-Methyl 2-(6-(4-(3,4-difluorophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(3,4-Difluorophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(6-(4-(2,4-difluorophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(2,4-Difluorophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(6-(4-(3,4-dimethoxyphenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(3,4-Dimethoxyphenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(6-(4-(3-chlorophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(3-Chlorophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(6-(4-(4-methoxyphenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(4-Methoxyphenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(4-(trifluoromethyl)phenylsulfonamido)

phenyl)isoindolin-2-yl)butanoate;

(S)-3-Methyl-2-(1 -oxo-6-(4-(4-(trifluoromethyl)phenylsulfonamido)phenyl) isoindolin-2-yl)butanoic acid;

(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(phenylmethylsulfonamido)phenyl) isoindolin-2-yl)butanoate;

(S)-3-Methyl-2-(1 -oxo-6-(4-(phenylmethylsulfonamido)phenyl)isoindolin-2-yl)butanoic acid;

(S)-Methyl 3-methyl-2-(6-(4-(1 -methylethylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)butanoate;

(S)-3-Methyl-2-(6-(4-(1 -methylethylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)butanoic acid;

(S)-Methyl 2-(6-(4-benzamidophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate (S)-2-(6-(4-Benzamidophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(6-(4-(4-fluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(4-Fluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(4-(trifluoromethyl)benzamido)phenyl) isoindolin-2-yl)butanoate;

(S)-3-Methyl-2-(1 -oxo-6-(4-(4-(trifluoromethyl)benzamido)phenyl)isoindolin-2-yl)butanoic acid;

(S)-Methyl 2-(6-(4-(4-methoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(4-Methoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-Methyl 2-(6-(4-(3-fluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate;

(S)-2-(6-(4-(3-Fluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-Methyl 2-(6-(4-(3-chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(3-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-Methyl 2-(6-(4-(2,4-difluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(2,4-Difluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-Methyl 3-methyl-2-(6-(4-(4-methylbenzamido)phenyl)-1 -oxoisoindolin-2-yl) butanoate;

(S)-3-Methyl-2-(6-(4-(4-methylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)butanoic acid; (S)-Methyl 2-(6-(4-(4-chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(4-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-Methyl 2-(6-(4-(4-tert-butylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(4-tert-Butylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)- Methyl 2-(6-(4-(cyclohexanecarboxamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(Cyclohexanecarboxamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)- Methyl 2-(6-(4-biphenyl-4-ylcarboxamidophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-Biphenyl-4-ylcarboxamidophenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)- Methyl 2-(6-(4-(2-naphthamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate; (S)- 2-(6-(4-(2-Naphthamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(4-pentylbenzamido)phenyl)isoindolin-2-yl) butanoate;

(S)-3-Methyl-2-(1 -oxo-6-(4-(4-pentylbenzamido)phenyl)isoindolin-2-yl)butanoic acid; (S)- Methyl 2-(6-(4-(2-fluoro-6-(trifluoromethyl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate ;

(S)-2-(6-(4-(2-Fluoro-6-(trifluoromethyl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(6-(4-(benzo[d][1 ,3]dioxole-5-carboxamido)phenyl)-1 -oxo isoindolin-2-yl)-3-methylbutanoate ;

(S)-2-(6-(4-(Benzo[d][1 ,3]dioxole-5-carboxamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)- Methyl 2-(6-(4-(2,6-dichlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)- 2-(6-(4-(2,6-Dichlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)- Methyl 2-(6-(4-(2-chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate;

(S)-2-(6-(4-(2-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-Methyl 2-(6-(4-(2,4-dichlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate;

(S)- 2-(6-(4-(2,4-Dichlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)- Methyl 2-(6-(4-(4-butoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate;

(S)- 2-(6-(4-(4-Butoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-Methyl 2-(6-(4-(2,6-difluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(2,6-Difluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)- Methyl 2-(6-(4-(3,4-difluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)- 2-(6-(4-(3,4-Difluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)- Methyl 2-(6-(4-(3,4-dimethoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(3,4-Dimethoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(3,4,5-trimethoxybenzamido)phenyl)

isoindolin -2-yl)butanoate;

(S)- 3-Methyl-2-(1 -oxo-6-(4-(3,4,5-trimethoxybenzamido)phenyl)isoindolin-2-yl) butanoic acid;

(S)- Methyl 2-(6-(4-(3,5-diethoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)- 2-(6-(4-(3,5-Diethoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)- Methyl 3-methyl-2-(1 -oxo-6-(4-(3-phenoxybenzamido)phenyl)isoindolin-2-yl)butanoate;

(S)- 3-Methyl-2-(1 -oxo-6-(4-(3-phenoxybenzamido)phenyl)isoindolin-2-yl) butanoic acid;

(S)- Methyl 3-methyl-2-(1 -oxo-6-(4-(4-phenoxybenzamido)phenyl)isoindolin-2-yl)butanoate;

(S)-3-Methyl-2-(1 -oxo-6-(4-(4-phenoxybenzamido)phenyl)isoindolin-2-yl) butanoic acid;

(S)- Methyl 3-methyl-2-(1 -oxo-6-(4-(2-phenoxybenzamido)phenyl)isoindolin-2-yl)butanoate;

(S)- 3-Methyl-2-(1 -oxo-6-(4-(2-phenoxybenzamido)phenyl)isoindolin-2-yl) butanoic acid;

(S)- Methyl 3-methyl-2-(1 -oxo-6-(4-(2,4,6-trimethylbenzamido)phenyl)isoindolin-2-yl)butanoate;

(S)-3-Methyl-2-(1 -oxo-6-(4-(2,4,6-trimethylbenzamido)phenyl)isoindolin-2-yl) butanoic acid;

(S)-Methyl 2-(6-(4-(2,4-dimethoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)- 2-(6-(4-(2,4-Dimethoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(4-(trifluoromethoxy)benzamido)phenyl) isoindolin-2-yl)butanoate;

(S)-3-Methyl-2-(1 -oxo-6-(4-(4-(trifluoromethoxy)benzamido)phenyl)isoindolin-2-yl)butanoic acid;

(S)- Methyl 2-(6-(4-(2-methoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)- 2-(6-(4-(2-Methoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-Methyl 2-(6-(4-(4-fluoro-3-methylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)- 2-(6-(4-(4-Fluoro-3-methylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)- Methyl 2-(6-(4-(4-butylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate;

(S)- 2-(6-(4-(4-Butylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-Methyl 2-(6-(4-(2,6-difluoro-3-methylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)- 2-(6-(4-(2,6-Difluoro-3-methylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)- Methyl 2-(6-(4-(4-ethylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate;

(S)-2-(6-(4-(4-Ethylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)- Methyl 3-methyl-2-(1 -oxo-6-(4-(4-propylbenzamido)phenyl)isoindolin-2-yl) butanoate;

(S)- 3-Methyl-2-(1 -oxo-6-(4-(4-propylbenzamido)phenyl)isoindolin-2-yl)butanoic acid; (S)-Methyl 3-methyl-2-(6-(4-(4-octylbenzamido)phenyl)-1 -oxoisoindolin-2-yl) butanoate;

(S)- 3-Methyl-2-(6-(4-(4-octylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)butanoic acid; (S)- Methyl 2-(6-(4-(4-cyclohexylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)- 2-(6-(4-(4-Cyclohexylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)- Methyl 3-methyl-2-(1 -oxo-6-(4-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydro

naphthalene-2-carboxamido)phenyl)isoindolin-2-yl)butanoate;

(S)-3-Methyl-2-(1 -oxo-6-(4-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydro naphthalene-2-carboxamido)phenyl)isoindolin-2-yl)butanoic acid;

(S)- Methyl 2-(6-(4-(1 -naphthamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate; (S)- 2-(6-(4-(1 -Naphthamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-Methyl 2-(6-(4-(3,5-dimethoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(3,5-Dimethoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-Methyl 2-(6-(4-(4-hexylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate;

(S)- 2-(6-(4-(4-Hexylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-Methyl 2-(6-(4-(4-heptylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate;

(S)- 2-(6-(4-(4-Heptylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)- Methyl 3-methyl-2-(6-(4-(4-nonylbenzamido)phenyl)-1 -oxoisoindolin-2-yl) butanoate;

(S)- 3-Methyl-2-(6-(4-(4-nonylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)butanoic acid; (S)- Methyl 2-(6-(4-(4-decylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate;

(S)- 2-(6-(4-(4-Decylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid; (S)- (Methyl 2-(6-(4-(adamentyl-2-carboxamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(Adamantyl-2-carboxamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)- Methyl 2-(6-(4-(2-fluoro-4-(trifluoromethyl)benzamido)phenyl)-1 -oxoiso indolin-2-yl)-3-methylbutanoate ;

(S)-2-(6-(4-(2-Fluoro-4-(trifluoromethyl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(6-(4-(2-fluoro-3-(trifluoromethyl)benzamido)phenyl)-1 -oxoiso indolin-2-yl)-3-methylbutanoate ;

(S)-2-(6-(4-(2-Fluoro-3-(trifluoromethyl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)- Methyl 2-(6-(4-(3-fluoro-4-(trifluoromethyl)benzamido)phenyl)-1 -oxoiso indolin-2-yl)-3-methylbutanoate ;

(S)- 2-(6-(4-(3-Fluoro-4-(trifluoromethyl)benzamido)phenyl)-1 -oxoisoindolin-2-yl) -3-methylbutanoic acid;

(S)- Methyl 2-(6-(4-(4-fluoro-2-(trifluoromethyl)benzamido)phenyl)-1 -oxoiso indolin-2-yl)-3-methylbutanoate ;

(S)-2-(6-(4-(4-Fluoro-2-(trifluoromethyl)benzamido)phenyl)-1 -oxoisoindolin-2-yl) -3-methylbutanoic acid;

(S)- Methyl 3-methyl-2-(1 -oxo-6-(4-(2-(trifluoromethyl)benzamido)phenyl)iso indolin-2-yl)butanoate;

(S)-3-Methyl-2-(1 -oxo-6-(4-(2-(trifluoromethyl)benzamido)phenyl)isoindolin-2-yl)butanoic acid;

(S)- Methyl 2-(6-(4-(2-ethoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate;

(S)-2-(6-(4-(2-Ethoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)- Methyl 2-(6-(4-(4-cyanobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate;

(S)- Methyl 2-(6-(4-(3-chloro-2-fluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-Methyl 2-(6-(4-(4-fluoro-3-(trifluoromethyl)benzamido)phenyl)-1 -oxoiso indolin-2-yl)-3-methylbutanoate ;

(S)-Methyl 3-methyl-2-(6-(4-(nicotinamido)phenyl)-1 -oxoisoindolin-2-yl) butanoate; (S)-3-Methyl-2-(6-(4-(nicotinamido)phenyl)-1 -oxoisoindolin-2-yl)butanoic acid;

(S)- Methyl 2-(6-(4-(2-chloronicotinamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)- 2-(6-(4-(2-Chloronicotinamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)- Methyl 3-methyl-2-(1 -oxo-5-(4-(6-(trifluoromethyl)nicotinamido)phenyl)iso indolin-2-yl)butanoate;

(S)-Methyl 2-(6-(4-(6-chloronicotinamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate;

(S)- Methyl 3-methyl-2-(6-(4-(6-morpholinonicotinamido)phenyl)-1 -oxoiso indolin-2-yl)butanoate;

(S)-3-Methyl-2-(6-(4-(6-morpholinonicotinamido)phenyl)-1 -oxoisoindolin-2-yl) butanoic acid;

(S)- Methyl 3-methyl-2-(1 -oxo-6-(4-(6-(piperidin-1 -yl)nicotinamido)phenyl)iso indolin-2-yl)butanoate;

(S)- 3-Methyl-2-(1 -oxo-6-(4-(6-(piperidin-1 -yl)nicotinamido)phenyl)isoindolin-2-yl)butanoic acid;

(S)- Methyl 3-methyl-2-(1 -oxo-6-(4-(6-(pyrrolidin-1 -yl)nicotinamido)phenyl)iso indolin-2-yl)butanoate;

(S)-3-Methyl-2-(1 -oxo-6-(4-(6-(pyrrolidin-1 -yl)nicotinamido)phenyl) isoindolin-2-yl)butanoic acid;

(S)- Methyl 3-methyl-2-(6-(4-(6-(4-methylpiperazin-1 -yl)nicotinamido)phenyl)-1 -oxoisoindolin-2-yl)butanoate;

(S)-Methyl 2-(5-(4-(3-(4-fluorophenyl) ureido) phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(5-(4-(3-(4-Fluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(5-(4-(3-(2-fluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(5-(4-(3-(2-Fluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-Methyl 2-(5-(4-(3-(3-fluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(5-(4-(3-(3-Fluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-Methyl 3-methyl-2-(1 -oxo-5-(4-(3-phenylureido)phenyl)isoindolin-2-yl) butanoate; (S)-3-Methyl-2-(1 -oxo-5-(4-(3-phenylureido)phenyl)isoindolin-2-yl)butanoic acid; (S)-Methyl 2-(5-(4-(3-benzylureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate; (S)-2-(5-(4-(3-Benzylureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-Methyl 2-(5-(4-(3-cyclohexylureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate;

(S)-2-(5-(4-(3-Cyclohexylureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid; (S)-Methyl 2-(5-(4-(3-(2,4-difluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(5-(4-(3-(2,4-Difluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(5-(4-(3-(3,4-difluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(5-(4-(3-(3,4-Difluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 3-methyl-2-(1 -oxo-5-(4-(3-p-tolylureido)phenyl)isoindolin-2-yl) butanoate; (S)-3-Methyl-2-(1 -oxo-5-(4-(3-p-tolylureido)phenyl)isoindolin-2-yl)butanoic acid; (S)-Methyl 3-methyl-2-(1 -oxo-5-(4-(3-m-tolylureido)phenyl)isoindolin-2-yl) butanoate; (S)-3-Methyl-2-(1 -oxo-5-(4-(3-m-tolylureido)phenyl)isoindolin-2-yl)butanoic acid; (S)-Methyl 3-methyl-2-(1 -oxo-5-(4-(3-(4-(trifluoromethyl)phenyl)ureido)phenyl) isoindolin-2-yl)butanoate;

(S)-3-Methyl-2-(1 -oxo-5-(4-(3-(4-(trifluoromethyl)phenyl)ureido)phenyl) isoindolin-2-yl)butanoic acid;

(S)-Methyl 3-methyl-2-(1 -oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl) isoindolin-2-yl)butanoate;

(S)-3-Methyl-2-(1 -oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl) isoindolin -2-yl)butanoic acid;

(S)-Methyl 2-(5-(4-(3-(4-methoxyphenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(5-(4-(3-(4-Methoxyphenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(5-(4-(3-(3-methoxyphenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(5-(4-(3-(3-Methoxyphenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(5-(4-(3-(4-cyanophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(5-(4-(3-(4-Cyanophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(5-(4-(3-(3-cyanophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(5-(4-(3-(3-Cyanophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(5-(4-(3-(2-fluorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(5-(4-(3-(2-Fluorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(5-(4-(3-(3-fluorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(5-(4-(3-(3-Fluorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-Methyl 2-(5-(4-(3-(4-methoxyphenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(5-(4-(3-(4-Methoxyphenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(5-(4-(3-(3-methoxyphenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(5-(4-(3-(3-Methoxyphenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-Methyl 2-(5-(4-(3-(4-chlorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(5-(4-(3-(4-Chlorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(5-(4-(3-(3-chlorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(5-(4-(3-(3-Chlorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(5-(4-(3-(4-cyanophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(5-(4-(3-(4-Cyanophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-Methyl 3-methyl-2-(1 -oxo-5-(4-(3-(2-(trifluoromethyl)phenyl)thioureido) phenyl)isoindolin-2-yl)butanoate;

(S)-3-Methyl-2-(1 -oxo-5-(4-(3-(2-(trifluoromethyl)phenyl)thioureido)phenyl) isoindolin-2-yl)butanoic acid;

(S)-Methyl 3-methyl-2-(1 -oxo-5-(4-(3-o-tolylthioureido)phenyl)isoindolin-2-yl)butanoate;

(S)-3-Methyl-2-(1 -oxo-5-(4-(3-o-tolylthioureido)phenyl)isoindolin-2-yl)butanoic acid; (S)-Methyl 3-methyl-2-(1 -oxo-5-(4-(3-p-tolylthioureido)phenyl)isoindolin-2-yl) butanoate;

(S)-3-Methyl-2-(1 -oxo-5-(4-(3-p-tolylthioureido)phenyl)isoindolin-2-yl)butanoic acid; (S)-Methyl 2-(5-(4-(3-(3-fluorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(5-(4-(3-(3-Fluorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-Methyl 2-(5-(4-(3-(3-methoxyphenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(5-(4-(3-(3-Methoxyphenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(5-(4-(3-(2-methoxyphenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(5-(4-(3-(2-Methoxyphenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 3-methyl-2-(1 -oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)thioureido) phenyl)isoindolin-2-yl)butanoate;

(S)-3-Methyl-2-(1 -oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)thioureido)phenyl) isoindolin-2-yl)butanoic acid;

(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(phenylsulfonamido)phenyl)isoindolin-2-yl)butanoate;

(S)-3-Methyl-2-(1 -oxo-6-(4-(phenylsulfonamido)phenyl)isoindolin-2-yl)butanoic acid; (S)-Methyl 2-(5-(4-(4-cyanophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(5-(4-(4-Cyanophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-Methyl 2-(5-(4-(3,4-difluorophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(5-(4-(3,4-Difluorophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(5-(4-(2,4-difluorophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(5-(4-(2,4-Difluorophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(5-(4-(3,4-dimethoxyphenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(5-(4-(3,4-Dimethoxyphenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(5-(4-(3-chlorophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(5-(4-(3-Chlorophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-Methyl 2-(5-(4-(4-methoxyphenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(5-(4-(4-Methoxyphenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 3-methyl-2-(1 -oxo-5-(4-(4-(trifluoromethyl)phenylsulfonamido) phenyl) isoindolin-2-yl)butanoate;

(S)-3-Methyl-2-(1 -oxo-5-(4-(4-(trifluoromethyl)phenylsulfonamido)phenyl) isoindolin-2-yl)butanoic acid;

(S)-Methyl 3-methyl-2-(1 -oxo-5-(4-(phenylmethylsulfonamido)phenyl) isoindolin-2-yl)butanoate;

(S)-3-Methyl-2-(1 -oxo-5-(4-(phenylmethylsulfonamido) phenyl) isoindolin-2-yl)butanoic acid;

(S)-Methyl 2-(5-(4-(cyclohexanesulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(5-(4-(Cyclohexanesulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(5-(4-benzamidophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(5-(4-Benzamidophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(5-(4-(4-fluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate;

(S)-2-(5-(4-(4-Fluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-Methyl 3-methyl-2-(1 -oxo-5-(4-(4-(trifluoromethyl)benzamido)phenyl) isoindolin-2-yl)butanoate;

(S)-3-Methyl-2-(1 -oxo-5-(4-(4-(trifluoromethyl)benzamido)phenyl)isoindolin-2-y/l)butanoic acid;

(S)-Methyl 2-(5-(4-(4-methoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(5-(4-(4-Methoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-Methyl 2-(5-(4-(3-fluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate;

(S)-2-(5-(4-(3-Fluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-Methyl 2-(5-(4-(3-chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate;

(S)-2-(5-(4-(3-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-Methyl 2-(5-(4-(2,4-difluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(5-(4-(2,4-Difluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 3-methyl-2-(5-(4-(4-methylbenzamido)phenyl)-1 -oxoisoindolin-2-yl) butanoate;

(S)-3-Methyl-2-(5-(4-(4-methylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)butanoic acid; (S)-Methyl 2-(5-(4-(4-chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate;

(S)-2-(5-(4-(4-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-Methyl 2-(5-(4-(4-tert-butylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(5-(4-(4-tert-Butylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-Methyl 3-methyl-2-(1 -oxo-5-(4-(4-pentylbenzamido)phenyl)isoindolin-2-yl) butanoate;

(S)-3-Methyl-2-(1 -oxo-5-(4-(4-pentylbenzamido)phenyl)isoindolin-2-yl)butanoic acid; (R)-Methyl-3-methyl-2-(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido) phenyl) isoindolin-2-yl)butanoate;

(R)-3-Methyl-2-(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)iso indolin-2-yl)butanoic acid;

Methyl 2-(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)acetate;

2-(1 -Oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)acetic acid; (S)-Methyl 2-(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)propanoate;

(S)-2-(1 -Oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl) propanoic acid;

Methyl 2-methyl-2-(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl) isoindolin-2-yl)propanoate;

2-Methyl-2-(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)propanoic acid;

Methyl 1 -(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl) cyclopentanecarboxylate ;

1 - (1 -Oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)

cyclopentanecarboxylic acid;

(S)-Methyl 2-(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)- 2- phenylacetate;

(S)-2-(1 -Oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)-2-phenylacetic acid;

Methyl 4-(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl) butanoate;

4-(1 -Oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)butanoic acid;

(S)-Methyl 4-methyl-2-(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl) isoindolin-2-yl)pentanoate;

(S)-4-Methyl-2-(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)iso indolin-2-yl)pentanoic acid;

(S)-Methyl 3-methoxy-2-(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)

phenyl)isoindolin-2-yl)propanoate;

(S)-3-Methoxy-2-(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)iso indolin-2-yl)propanoic acid;

(R)-Methyl 3-methyl-2-(1 -oxo-5-(4-(3-(3-(trifluoromethyl)phenyl) ureido)phenyl) isoindolin-2-yl)butanoate;

(R)-3-Methyl-2-(1 -oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl) isoindolin-2-yl)butanoic acid;

Methyl 2-(1 -oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)acetate;

2-(1 -Oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)acetic acid; (S)-Methyl 2-(1 -oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)propanoate;

(S)-2-(1 -Oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl) propanoic acid;

Methyl 1 -(1 -oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)cyclopentanecarboxylate;

1 - (1 -Oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)

cyclopentanecarboxylic acid;

(S)-Methyl 2-(1 -oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)- 2- phenylacetate;

(S)-2-(1 -Oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)-2-phenylacetic acid;

Methyl 4-(1 -oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl) butanoate;

4-(1 -Oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl) butanoic acid;

Ethyl 3-(1 -oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl) propanoate;

3- (1 -Oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)propanoic acid;

(S)-Methyl 2-(1 -oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)-3-phenylpropanoate;

(S)-2-(1 -Oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)-3-phenylpropanoic acid;

(S)-Methyl 3-methoxy-2-(1 -oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido) phenyl) isoindolin-2-yl)propanoate;

(S)-3-Methoxy-2-(1 -oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl) isoindolin-2-yl)propanoic acid;

(S)-Methyl 4-methyl-2-(1 -oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl) isoindolin-2-yl)pentanoate;

(S)-4-Methyl-2-(1 -oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)iso indolin-2-yl)pentanoic acid;

(S)- Methyl 2-(6-(5-(3-(2-chlorophenyl)ureido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)- 2-(6-(5-(3-(2-Chlorophenyl)ureido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(6-(5-(3-(4-chloro-2-phenoxyphenyl)ureido)pyridin-2-yl)-1 -oxoiso indolin-2-yl)-3-methylbutanoate;

(S)- 2-(6-(5-(3-(4-Chloro-2-phenoxyphenyl)ureido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(6-(5-(3-(3,4-dimethylphenyl)ureido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)- 2-(6-(5-(3-(3,4-Dimethylphenyl)ureido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)- Methyl 2-(6-(5-(3-(3,4-difluorophenyl)ureido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)- 2-(6-(5-(3-(3,4-Difluorophenyl)ureido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(6-(5-(3-(2,3-dihydro-1 H-inden-5-yl)ureido)pyridin-2-yl)-1 -oxoiso indolin-2-yl)-3-methylbutanoate;

(S)- 2-(6-(5-(3-(2,3-Dihydro-1 H-inden-5-yl)ureido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(6-(5-(4-tert-butylbenzamido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(5-(4-tert-Butylbenzamido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)- Methyl 3-methyl-2-(1 -oxo-6-(5-(4-pentylbenzamido)pyridin-2-yl)isoindolin-2-yl)butanoate;

(S)- 3-Methyl-2-(1 -oxo-6-(5-(4-pentylbenzamido)pyridin-2-yl)isoindolin-2-yl)butanoic acid;

(S)-Methyl 2-(6-(5-biphenyl-4-ylcarboxamidopyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)- 2-(6-(5-Biphenyl-4-ylcarboxamidopyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(6-(5-(2-naphthamido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate;

(S)-2-(6-(5-(2-Naphthamido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)- Methyl 2-(6-(5-(4-butoxybenzamido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)- 2-(6-(5-(4-Butoxybenzamido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)- Methyl 2-(6-(4-(3-(2-chlorophenyl)ureido)-2-(trifluoromethyl)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)- 2-(6-(4-(3-(2-Chlorophenyl)ureido)-2-(trifluoromethyl)phenyl)-1 -oxoiso indolin-2-yl)-3-methylbutanoic acid;

(S)- Methyl 2-(6-(4-(3-(3,4-difluorophenyl)ureido)-2-(trifluoromethyl)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)- 2-(6-(4-(3-(3,4-Difluorophenyl)ureido)-2-(trifluoromethyl)phenyl)-1 -oxoiso indolin- 2- yl)-3-methylbutanoic acid;

(S)- Methyl 2-(6-(4-(3-(2,3-dihydro-1 H-inden-5-yl)ureido)-2-(trifluoromethyl) phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(3-(2,3-Dihydro-1 H-inden-5-yl)ureido)-2-(trifluoromethyl)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)- Methyl 2-(6-(4-(3-(3,4-dimethylphenyl)ureido)-2-(trifluoromethyl)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)- 2-(6-(4-(3-(3,4-Dimethylphenyl)ureido)-2-(trifluoromethyl)phenyl)-1 -oxoiso indolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(6-(4-(4-tert-butylbenzamido)-2-(trifluoromethyl)phenyl)-1 -oxoiso indolin-2-yl)-3-methylbutanoate;

(S)- 2-(6-(4-(4-tert-Butylbenzamido)-2-(trifluoromethyl)phenyl)-1 -oxoisoindolin-2-yl)- 3- methylbutanoic acid;

(S)- Methyl 2-(6-(4-biphenyl-4-ylcarboxamido-2-(trifluoromethyl)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)- 2-(6-(4-Biphenyl-4-ylcarboxamido-2-(trifluoromethyl)phenyl)-1 -oxoiso indolin-2-yl)-3-methylbutanoic acid;

(S)- Methyl 2-(6-(4-(2-naphthamido)-2-(trifluoromethyl)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)- 2-(6-(4-(2-Naphthamido)-2-(trifluoromethyl)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(4-pentylbenzamido)-2-(trifluoromethyl) phenyl)isoindolin-2-yl)butanoate;

(S)- 3-Methyl-2-(1 -oxo-6-(4-(4-pentylbenzamido)-2-(trifluoromethyl) phenyl) isoindolin-2-yl)butanoic acid;

(S)- Methyl 2-(6-(4-(4-butoxybenzamido)-2-(trifluoromethyl)phenyl)-1 -oxoiso indolin-2-yl)-3-methylbutanoate;

(S)- 2-(6-(4-(4-Butoxybenzamido)-2-(trifluoromethyl)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(6-(4-(3-(3,4-dimethylphenyl)ureido)-3-fluorophenyl)-1 -oxoiso indolin-2-yl)-3-methylbutanoate ;

(S)-2-(6-(4-(3-(3,4-Dimethylphenyl)ureido)-3-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)- Methyl 2-(6-(4-(3-(2,3-dihydro-1 H-inden-5-yl)ureido)-3-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)- 2-(6-(4-(3-(2,3-Dihydro-1 H-inden-5-yl)ureido)-3-fluorophenyl)-1 -oxoiso indolin-2-yl)-3-methylbutanoic acid;

(S)- Methyl 2-(6-(4-(3-(3,4-difluorophenyl)ureido)-3-fluorophenyl)-1 -oxoiso indolin-2-yl)-3-methylbutanoate ;

(S)- 2-(6-(4-(3-(3,4-Difluorophenyl)ureido)-3-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)- Methyl 2-(6-(4-(3-(2-chlorophenyl)ureido)-3-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(3-(2-Chlorophenyl)ureido)-3-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)- Methyl 2-(6-(4-(4-tert-butylbenzamido)-3-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)- 2-(6-(4-(4-tert-Butylbenzamido)-3-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(6-(3-fluoro-4-(4-pentylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(3-Fluoro-4-(4-pentylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(6-(4-biphenyl-4-ylcarboxamido-3-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)- 2-(6-(4-Biphenyl-4-ylcarboxamido-3-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)- Methyl 2-(6-(4-(2-naphthamido)-3-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)- 2-(6-(4-(2-Naphthamido)-3-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)- Methyl 2-(6-(4-(4-butoxybenzamido)-3-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)- 2-(6-(4-(4-Butoxybenzamido)-3-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-Methyl 2-(6-(4-(4-tert-butylbenzamido)-2-methoxyphenyl)-1 -oxoiso indolin -2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(4-tert-Butylbenzamido)-2-methoxyphenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(6-(4-biphenyl-4-ylcarboxamido-2-methoxyphenyl)-1 -oxoiso indolin-2-yl)-3-methylbutanoate ;

(S)-2-(6-(4-Biphenyl-4-ylcarboxamido-2-methoxyphenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(6-(4-(4-butoxybenzamido)-2-methoxyphenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(4-Butoxybenzamido)-2-methoxyphenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(6-(2-methoxy-4-(4-pentylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(2-Methoxy-4-(4-pentylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(6-(2-methoxy-4-(4-(trifluoromethoxy)benzamido)phenyl)-1 -oxo isoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(2-Methoxy-4-(4-(trifluoromethoxy)benzamido)phenyl)-1 -oxoiso indolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(6-(4-(4-tert-butylbenzamido)-2-methylphenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(4-tert-Butylbenzamido)-2-methylphenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(6-(4-biphenyl-4-ylcarboxamido-2-methylphenyl)-1 -oxoiso indolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-Biphenyl-4-ylcarboxamido-2-methylphenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(6-(4-(4-butoxybenzamido)-2-methylphenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(4-Butoxybenzamido)-2-methylphenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 3-methyl-2-(6-(2-methyl-4-(4-pentylbenzamido)phenyl)-1 -oxoiso indolin-2-yl)butanoate;

(S)-3-Methyl-2-(6-(2-methyl-4-(4-pentylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)butanoic acid;

(S)-Methyl 3-methyl-2-(6-(2-methyl-4-(4-(trifluoromethoxy)benzamido) phenyl)-1 -oxoisoindolin-2-yl)butanoate;

(S)-3-Methyl-2-(6-(2-methyl-4-(4-(trifluoromethoxy)benzamido)phenyl)-1 -oxoisoindolin-2-yl)butanoic acid;

(S)-Methyl 2-(6-(4-(4-tert-butylbenzamido)-2-chlorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(4-tert-Butylbenzamido)-2-chlorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(6-(4-biphenyl-4-ylcarboxamido-2-chlorophenyl)-1 -oxoiso indolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-Biphenyl-4-ylcarboxamido-2-chlorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(6-(4-(4-butoxybenzamido)-2-chlorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(4-Butoxybenzamido)-2-chlorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(6-(2-chloro-4-(4-pentylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(2-Chloro-4-(4-pentylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(6-(2-chloro-4-(4-(trifluoromethoxy)benzamido)phenyl)-1 -oxo isoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(2-Chloro-4-(4-(trifluoromethoxy)benzamido)phenyl)-1 -oxoiso indolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(6-(6-(4-tert-butylbenzamido)pyridin-3-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(6-(4-tert-Butylbenzamido)pyridin-3-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(6-(6-biphenyl-4-ylcarboxamidopyridin-3-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-Methyl 3-methyl-2-(1 -oxo-6-(6-(4-pentylbenzamido)pyridin-3-yl)iso indolin-2-yl)butanoate;

(S)-Methyl 3-methyl-2-(1 -oxo-6-(6-(4-(trifluoromethoxy)benzamido)pyridin-3-yl)isoindolin-2-yl)butanoate;

(S)-Methyl 2-(6-(6-(4-tert-butylbenzamido)pyridazin-3-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(6-(4-tert-Butylbenzamido)pyridazin-3-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 3-methyl-2-(1 -oxo-6-(6-(4-pentylbenzamido)pyridazin-3-yl)iso indolin-2-yl)butanoate;

(S)-3-Methyl-2-(1 -oxo-6-(6-(4-pentylbenzamido)pyridazin-3-yl)isoindolin-2-yl)butanoic acid;

(S)-Methyl 3-methyl-2-(1 -oxo-6-(6-(4-(trifluoromethoxy)benzamido)pyridazin-3-yl) isoindolin-2-yl)butanoate;

(S)-3-Methyl-2-(1 -oxo-6-(6-(4-(trifluoromethoxy)benzamido)pyridazin-3-yl)isoindolin-2-yl)butanoic acid;

(S)-Methyl 2-(6-(5-(4-tert-butylbenzamido)pyrazin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(5-(4-tert-Butylbenzamido)pyrazin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(6-(5-biphenyl-4-ylcarboxamidopyrazin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(5-Biphenyl-4-ylcarboxamidopyrazin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(6-(5-(4-butoxybenzamido)pyrazin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(5-(4-Butoxybenzamido)pyrazin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 3-methyl-2-(1 -oxo-6-(5-(4-pentylbenzamido)pyrazin-2-yl)isoindolin-2-yl)butanoate;

(S)-3-Methyl-2-(1 -oxo-6-(5-(4-pentylbenzamido)pyrazin-2-yl)isoindolin-2-yl)butanoic acid;

(S)-Methyl 3-methyl-2-(1 -oxo-6-(5-(4-(trifluoromethoxy)benzamido)pyrazin-2-yl)isoindolin-2-yl)butanoate;

(S)-3-Methyl-2-(1 -oxo-6-(5-(4-(trifluoromethoxy)benzamido)pyrazin-2-yl)isoindolin-2-yl)butanoic acid;

Methyl 2-(6-(4-([1 ,1 '-biphenyl]-4-ylcarboxamido)phenyl)-1 -oxoisoindolin-2-yl)-2-methylpropanoate;

2-(6-(4-([1 ,1 '-Biphenyl]-4-ylcarboxamido)phenyl)-1 -oxoisoindolin-2-yl)-2-methyl propanoic acid;

Methyl 2-(6-(4-(4-(tert-butyl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)-2-methyl propanoate;

2-(6-(4-(4-(tert-Butyl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)-2-methyl propanoic acid;

Methyl 2-(6-(4-(4-chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-2-methyl propanoate;

2-(6-(4-(4-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-2-methylpropanoic acid; Methyl 2-methyl-2-(1 -oxo-6-(4-(4-(trifluoromethoxy)benzamido)phenyl)iso indolin-2-yl)propanoate

2-Methyl-2-(1 -oxo-6-(4-(4-(trifluoromethoxy)benzamido)phenyl)isoindolin-2-yl)propanoic acid;

Methyl 2-methyl-2-(1 -oxo-6-(4-(4-pentylbenzamido)phenyl)isoindolin-2-yl) propanoate;

2- Methyl-2-(1 -oxo-6-(4-(4-pentylbenzamido)phenyl)isoindolin-2-yl)propanoic acid; Methyl 1 -(6-(4-([1 ,1 '-biphenyl]-4-ylcarboxamido)phenyl)-1 -oxoisoindolin-2-yl) cyclopentanecarboxylate ;

1 -(6-(4-([1 ,1 '-Biphenyl]-4-ylcarboxamido)phenyl)-1 -oxoisoindolin-2-yl) cyclopentane carboxylic acid;

Methyl 1 -(6-(4-(4-(tert-butyl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)

cyclopentanecarboxylate ;

1 -(6-(4-(4-(tert-Butyl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclopentane carboxylic acid;

Methyl 1 -(6-(4-(4-chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclopentane carboxylate;

1 -(6-(4-(4-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclopentane carboxylic acid;

Methyl 1 -(1 -oxo-6-(4-(4-(trifluoromethoxy)benzamido)phenyl)isoindolin-2-yl) cyclopentanecarboxylate ;

1 -(1 -Oxo-6-(4-(4-(trifluoromethoxy)benzamido)phenyl)isoindolin-2-yl) cyclopentane carboxylic acid;

Methyl 1 -(1 -oxo-6-(4-(4-pentylbenzamido)phenyl)isoindolin-2-yl)cyclopentane carboxylate;

1 -(1 -Oxo-6-(4-(4-pentylbenzamido)phenyl)isoindolin-2-yl)cyclopentane carboxylic acid;

(R)-Methyl 2-(6-(4-([1 ,1 '-biphenyl]-4-ylcarboxamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(R)-2-(6-(4-([1 ,1 '-Biphenyl]-4-ylcarboxamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

Methyl 3-(6-(4-([1 ,1 '-biphenyl]-4-ylcarboxamido)phenyl)-1 -oxoisoindolin-2-yl) cyclohexanecarboxylate;

3- (6-(4-([1 ,1 '-Biphenyl]-4-ylcarboxamido)phenyl)-1 -oxoisoindolin-2-yl)cyclo hexane carboxylic acid;

Methyl 3-(6-(4-(3-chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclohexane carboxylate;

3-(6-(4-(3-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclohexane carboxylic acid;

Methyl 3-(6-(4-(4-chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclohexane carboxylate;

3-(6-(4-(4-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclohexane carboxylic acid;

Methyl 3-(1 -oxo-6-(4-(4-(trifluoromethyl)benzamido)phenyl)isoindolin-2-yl) cyclohexanecarboxylate;

3-(1 -Oxo-6-(4-(4-(trifluoromethyl)benzamido)phenyl)isoindolin-2-yl)cyclo

hexanecarboxylic acid;

Methyl 3-(6-(4-(5-methyl-2-phenyloxazole-4-carboxamido)phenyl)-1 -oxo isoindolin-2-yl)cyclohexanecarboxylate;

3-(6-(4-(5-Methyl-2-phenyloxazole-4-carboxamido)phenyl)-1 -oxoisoindolin-2-yl)cyclohexanecarboxylic acid ;

(1 r,4r)-Methyl 4-(6-(4-([1 ,1 '-biphenyl]-4-ylcarboxamido)phenyl)-1 -oxoisoindolin-2-yl)cyclohexanecarboxylate;

(1 r,4r)-4-(6-(4-([1 ,1 '-Biphenyl]-4-ylcarboxamido)phenyl)-1 -oxoisoindolin-2-yl) cyclohexanecarboxylic acid;

(1 r,4r)-Methyl 4-(6-(4-(3-chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl) cyclo hexanecarboxylate;

(1 r,4r)-4-(6-(4-(3-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclohexane carboxylic acid;

(1 r,4r)-Methyl 4-(6-(4-(4-chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)

cyclohexanecarboxylate;

(1 r,4r)-4-(6-(4-(4-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclohexane carboxylic acid;

(1 r,4r)-Methyl 4-(1 -oxo-6-(4-(4-(trifluoromethyl)benzamido)phenyl)isoindolin-2-yl)cyclohexanecarboxylate;

(1 r,4r)-4-(1 -Oxo-6-(4-(4-(trifluoromethyl)benzamido)phenyl)isoindolin-2-yl) cyclohexanecarboxylic acid;

(1 r,3s,5R,7S)-Methyl 3-(6-(4-(3-chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)adamantane-1 -carboxylate;

(1 r,3s,5R,7S)-3-(6-(4-(3-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)

adamantane-1 -carboxylic acid;

(1 r,3s,5R,7S)-Methyl 3-(6-(4-(4-chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)adamantane-1 -carboxylate;

(1 r,3s,5R,7S)-3-(6-(4-(4-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)

adamantane-1 -carboxylic acid;

(1 r,3s,5R,7S)-Methyl 3-(1 -oxo-6-(4-(4-(trifluoromethyl)benzamido)phenyl) isoindolin-2-yl)adamantane-1 -carboxylate;

(1 r,3s,5R,7S)-3-(1 -Oxo-6-(4-(4-(trifluoromethyl)benzamido)phenyl)isoindolin-2-yl)adamantane-1 -carboxylic acid;

(1 r,3s,5R,7S)-3-(6-(4-(4-Methylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)

adamantane-1 -carboxylic acid;

Methyl 1 -(6-(4-([1 ,1 '-biphenyl]-4-ylcarboxamido)phenyl)-1 -oxoisoindolin-2-yl) cyclobutanecarboxylate;

1 -(6-(4-([1 ,1 '-Biphenyl]-4-ylcarboxamido)phenyl)-1 -oxoisoindolin-2-yl) cyclo butanecarboxylic acid;

Methyl 1 -(6-(4-(4-chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl) cyclobutane carboxylate;

1 -(6-(4-(4-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclobutane carboxylic acid;

Methyl 1 -(1 -Oxo-6-(4-(4-(trifluoromethyl)benzamido)phenyl)isoindolin-2-yl) cyclobutanecarboxylate;

1 -(1 -Oxo-6-(4-(4-(trifluoromethyl)benzamido)phenyl)isoindolin-2-yl) cyclo

butanecarboxylic acid;

Methyl 1 -(6-(4-(4-methylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclobutane carboxylate;

1 -(6-(4-(4-Methylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclobutane carboxylic acid;

Methyl 1 -(6-(4-biphenyl-4-ylcarboxamidophenyl)-1 -oxoisoindolin-2-yl) cyclo propanecarboxylate;

1 -(6-(4-([1 ,1 '-Biphenyl]-4-ylcarboxamido)phenyl)-1 -oxoisoindolin-2-yl)

cyclopropanecarboxylic acid;

Methyl 1 -(6-(4-(4-chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclopropane carboxylate;

1 -(6-(4-(4-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclopropane carboxylic acid;

Methyl 1 -(1 -oxo-6-(4-(4-(trifluoromethyl)benzamido)phenyl)isoindolin-2-yl) cyclopropane carboxylate;

1 -(1 -Oxo-6-(4-(4-(trifluoromethyl)benzamido)phenyl)isoindolin-2-yl)cyclo propane carboxylic acid;

(1 S,2R)-Methyl 2-(6-(4-([1 ,1 '-biphenyl]-4-ylcarboxamido)phenyl)-1 -oxo isoindolin-2-yl)cyclopentanecarboxylate;

(1 S,2R)-2-(6-(4-([1 ,1 '-Biphenyl]-4-ylcarboxamido)phenyl)-1 -oxoisoindolin-2-yl)cyclopentanecarboxylic acid;

(1 S,2R)-Methyl 2-(6-(4-(4-chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)

cyclopentanecarboxylate ;

(1 S,2R)-2-(6-(4-(4-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclopentane carboxylic acid;

(1 S,2R)-Methyl 2-(1 -oxo-6-(4-(4-(trifluoromethyl)benzamido)phenyl)isoindolin-2-yl)cyclopentanecarboxylate;

(1 S,2R)-2-(1 -Oxo-6-(4-(4-(trifluoromethyl)benzamido)phenyl)isoindolin-2-yl) cyclopentanebcarboxylic acid;

(S)-Methyl 2-(6-(4-([1 ,1 '-biphenyl]-4-ylcarboxamido)-2-fluorophenyl)-1 -oxo isoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-([1 ,1 '-Biphenyl]-4-ylcarboxamido)-2-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(6-(4-(4-(tert-butyl)benzamido)-2-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(4-(tert-Butyl)benzamido)-2-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(6-(4-(4-chlorobenzamido)-2-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(4-Chlorobenzamido)-2-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-Methyl 2-(6-(2-fluoro-4-(4-(trifluoromethoxy)benzamido)phenyl)-1 -oxo isoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(2-Fluoro-4-(4-(trifluoromethoxy)benzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(6-(2-fluoro-4-(4-pentylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(2-Fluoro-4-(4-pentylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(5-phenylthiazole-2-carboxamido)phenyl) isoindolin-2-yl)butanoate;

(S)-3-Methyl-2-(1 -oxo-6-(4-(5-phenylthiazole-2-carboxamido)phenyl)isoindolin-2-yl)butanoic acid;

(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(5-phenyloxazole-2-carboxamido)phenyl) isoindolin-2-yl)butanoate;

(S)-3-Methyl-2-(1 -oxo-6-(4-(5-phenyloxazole-2-carboxamido)phenyl) isoindolin-2-yl)butanoic acid;

(S)-Methyl 2-(6-(4-(3-(4-fluorophenyl)isoxazole-5-carboxamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(3-(4-Fluorophenyl)isoxazole-5-carboxamido)phenyl)-1 -oxo isoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(6-(4-(3-(4-chlorophenyl)isoxazole-5-carboxamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(3-(4-Chlorophenyl)isoxazole-5-carboxamido)phenyl)-1 -oxo

isoindolin-2-yl)-3-methylbutanoic acid ;

(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(3-(4-(trifluoromethyl)phenyl)isoxazole-5-carboxamido)phenyl)isoindolin-2-yl)butanoate;

(S)-3-Methyl-2-(1 -oxo-6-(4-(3-(4-(trifluoromethyl)phenyl)isoxazole-5-carboxamido)phenyl)isoindolin-2-yl)butanoic acid;

(S)-Methyl 3-methyl-2-(6-(4-(4-(oxazol-5-yl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)butanoate;

(S)-3-Methyl-2-(6-(4-(4-(oxazol-5-yl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)butanoic acid;

(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(4-phenylthiazole-2-carboxamido)phenyl) isoindolin-2-yl)butanoate;

(S)-3-methyl-2-(1 -oxo-6-(4-(4-phenylthiazole-2-carboxamido)phenyl)isoindolin-2-yl)butanoic acid;

(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(5-phenyl-1 ,3,4-oxadiazole-2-carboxamido) phenyl)isoindolin-2-yl)butanoate;

(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(5-phenyl-1 ,3,4-thiadiazole-2-carboxamido) phenyl)isoindolin-2-yl)butanoate;

(S)-3-Methyl-2-(1 -oxo-6-(4-(5-phenyl-1 ,3,4-thiadiazole-2-carboxamido)

phenyl)isoindolin-2-yl)butanoic acid;

(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(5-phenyl-4H-1 ,2,4-triazole-3-carboxamido) phenyl)isoindolin-2-yl)butanoate;

(S)-3-Methyl-2-(1 -oxo-6-(4-(5-phenyl-4H-1 ,2,4-triazole-3-carboxamido) phenyl) isoindolin-2-yl)butanoic acid;

(S)-Methyl 2-(6-(4-(4-(2-cyanopropan-2-yl)benzamido)phenyl)-1 -oxoisoindolin-2-yl) 3-methylbutanoate;

(S)-2-(6-(4-(4-(2-Cyanopropan-2-yl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(6-(4-(4-(3-cyanopentan-3-yl)benzamido)phenyl)-1 -oxoisoindolin-2-yl) 3-methylbutanoate;

(S)-2-(6-(4-(4-(3-Cyanopentan-3-yl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 3-methyl-2-(1 -oxo-6-(5-(5-phenyloxazole-2-carboxamido)pyridin-2-yl)isoindolin-2-yl)butanoate;

(S)-3-Methyl-2-(1 -oxo-6-(5-(5-phenyloxazole-2-carboxamido)pyridin-2-yl) isoindolin 2-yl)butanoic acid;

(S)-Methyl 3-methyl-2-(1 -oxo-6-(5-(5-phenylthiazole-2-carboxamido)pyridin-2-yl)isoindolin-2-yl)butanoate;

(S)-3-Methyl-2-(1 -oxo-6-(5-(5-phenylthiazole-2-carboxamido)pyridin-2-yl) isoindolin 2-yl)butanoic acid;

(S)-Methyl 2-(6-(5-(3-(4-fluorophenyl)isoxazole-5-carboxamido)pyridin-2-yl)-1 -oxo isoindolin-2-yl)-3-methylbutanaote;

(S)-2-(6-(5-(3-(4-Fluorophenyl)isoxazole-5-carboxamido)pyridin-2-yl)-1 -oxo isoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 2-(6-(4-(4-(1 ,3,4-oxadiazol-2-yl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(4-(1 ,3,4-Oxadiazol-2-yl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-Methyl 3-methyl-2-(6-(4-(5-methyl-2-phenyloxazole-4-carboxamido) phenyl)-1 -oxoisoindolin-2-yl)butanoate;

(S)-3-Methyl-2-(6-(4-(5-methyl-2-phenyloxazole-4-carboxamido)phenyl)-1 -oxoisoindolin-2-yl)butanoic acid;

(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(2-phenyl-5-(trifluoromethyl)oxazole-4-carboxamido)phenyl)isoindolin-2-yl)butanoate;

(S)-3-Methyl-2-(1 -oxo-6-(4-(2-phenyl-5-(trifluoromethyl)oxazole-4-carboxamido) phenyl)isoindolin-2-yl)butanoic acid;

(S)-Methyl 3-methyl-2-(6-(2-methyl-4-(4-pentylbenzamido)phenyl)-1 -oxoiso indolin-2-yl)butanoate;

(S)-3-Methyl-2-(1 -oxo-6-(4-(4-(thiazol-2-yl)benzamido)phenyl)isoindolin-2-yl) butanoic acid;

(S)-Methyl 2-(6-(4-(5-butylpicolinamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;

(S)-2-(6-(4-(5-Butylpicolinamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(quinoline-3-carboxamido)phenyl)isoindolin-2-yl)butanoate;

(S)-3-Methyl-2-(1 -oxo-6-(4-(quinoline-3-carboxamido)phenyl)isoindolin-2-yl) butanoic acid;

(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(4-(pyrimidin-5-yl)benzamido) phenyl) isoindolin-2-yl)butanoate;

(S)-3-Methyl-2-(1 -oxo-6-(4-(4-(pyrimidin-5-yl)benzamido)phenyl)isoindolin-2-yl)butanoic acid;

(S)-Methyl 3-methyl-2-(6-(5-(5-methyl-2-phenyloxazole-4-carboxamido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)butanoate;

(S)-3-Methyl-2-(6-(5-(5-methyl-2-phenyloxazole-4-carboxamido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)butanoic acid;

(S)-Methyl 3-methyl-2-(1 -oxo-6-(5-(2-phenyl-5-(trifluoromethyl)oxazole-4-carboxamido)pyridin-2-yl)isoindolin-2-yl)butanoate;

(S)-3-Methyl-2-(1 -oxo-6-(5-(2-phenyl-5-(trifluoromethyl)oxazole-4-carboxamido) pyridin-2-yl)isoindolin-2-yl)butanoic acid;

(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(2-phenylacetamido)phenyl)isoindolin-2-yl)butanoate;

(S)-3-Methyl-2-(1 -oxo-6-(4-(2-phenylacetamido)phenyl)isoindolin-2-yl)butanoic acid; Methyl 2-(5-(4-biphenyl-4-ylcarboxamidophenyl)-1 ,3-dioxoisoindolin-2-yl)-3-methyl butanoate;

Methyl 2-(5-(4-(4-tert-butylbenzamido)phenyl)-1 ,3-dioxoisoindolin-2-yl)-3-methyl butanoate;

Methyl 2-(5-(4-(2,4-dimethoxybenzamido)phenyl)-1 ,3-dioxoisoindolin-2-yl)-3-methylbutanoate;

Methyl 2-(5-(4-(3-(2-chlorophenyl)ureido)phenyl)-1 ,3-dioxoisoindolin-2-yl)-3-methylbutanoate;

Methyl 2-(5-(4-(3-(3,4-dimethylphenyl)ureido)phenyl)-1 ,3-dioxoisoindolin-2-yl)-3-methylbutanoate;

Methyl 2-(5-(4-(4-tert-butylbenzamido)phenyl)isoindolin-2-yl)-3-methyl butanoate; Methyl 3-methyl-2-(5-(4-(4-pentylbenzamido)phenyl)isoindolin-2-yl)butanoate;

Methyl 2-(5-(4-biphenyl-4-ylcarboxamidophenyl)isoindolin-2-yl)-3-methyl butanoate; Methyl 2-(5-(4-(2,4-dimethoxyphenylsulfonamido)phenyl)isoindolin-2-yl)-3-methyl butanoate; and

Methyl 3-methyl-2-(5-(4-(3-(2-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)butanoate;

or a stereoisomer, tautomer, pharmaceutically acceptable salt, pharmaceutically acceptable solvate, pharmaceutically acceptable polymorph, pharmaceutically acceptable prodrug, N-oxide or carboxylic acid isostere thereof.

In another embodiment, the present invention provides compounds of formula 1 selected from:

(S)-2-(6-(4-(3-(4-Fluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-2-(6-(4-(3-(2,4-Difluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(6-(4-(3-(2-Fluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-2-(6-(4-(3-(3-Fluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-3-Methyl-2-(1 -oxo-6-(4-(3-phenylureido)phenyl)isoindolin-2-yl)butanoic acid; (S)-2-(6-(4-(3-Benzylureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-2-(6-(4-(3-(2,6-Difluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-3-Methyl-2-(1 -oxo-6-(4-(3-p-tolylureido)phenyl)isoindolin-2-yl)butanoic acid; (S)-2-(6-(4-(3-(3-Methoxyphenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-2-(6-(4-(3-(4-Methoxyphenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(6-(4-(3-(3,5-Difluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(6-(4-(3-(3,4-Difluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(6-(4-(3-Cyclohexylureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-3-Methyl-2-(1 -oxo-6-(4-(3-(4-(trifluoromethyl)phenyl)ureido)phenyl) isoindolin-2-yl)butanoic acid;

(S)-3-Methyl-2-(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl) isoindolin-2-yl)butanoic acid;

(S)-2-(6-(4-(3-(4-Cyanophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-2-(6-(4-(3-(3-Cyanophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-2-(6-(4-(3-(4-Chloro-2-phenoxyphenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(6-(4-(3-(5-Chloro-2-phenoxyphenyl) ureido) phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-3-Methyl-2-(1 -oxo-6-(4-(3-(2-phenoxyphenyl)ureido)phenyl)isoindolin-2-yl)butanoic acid;

(S)-3-Methyl-2-(1 -oxo-6-(4-(3-(4-phenoxyphenyl)ureido)phenyl)isoindolin-2-yl)butanoic acid;

(S)-2-(6-(4-(3-(2-Fluorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-3-Methyl-2-(1 -oxo-6-(4-(3-p-tolylthioureido)phenyl)isoindolin-2-yl)butanoic acid; (S)-2-(6-(4-(3-(3-Fluorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(6-(4-(3-(4-Methoxyphenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(6-(4-(3-(3-Methoxyphenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(6-(4-(3-(4-Chlorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-2-(6-(4-(3-(3-Chlorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-3-Methyl-2-(1 -oxo-6-(4-(3-(2-trifluoromethyl)phenyl)thioureido)phenyl) isoindolin-2-yl)butanoic acid;

(S)-2-(6-(4-(3-(4-Cyanophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-2-(6-(4-(3-(3-Cyanophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-3-Methyl-2-(1 -oxo-6-(4-(3-o-tolylthioureido)phenyl)isoindolin-2-yl)butanoic acid; (S)-2-(6-(4-(3-(2-Methoxyphenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-3-Methyl-2-(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)thioureido)phenyl) isoindolin-2-yl)butanoic acid;

(S)-3-Methyl-2-(1 -oxo-6-(4-(phenylsulfonamido)phenyl)isoindolin-2-yl)butanoic acid; (S)-2-(6-(4-(4-Cyanophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-2-(6-(4-(3,4-Difluorophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(6-(4-(2,4-Difluorophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(6-(4-(3,4-Dimethoxyphenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(6-(4-(3-Chlorophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(6-(4-(4-Methoxyphenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-3-Methyl-2-(1 -oxo-6-(4-(4-(trifluoromethyl)phenylsulfonamido)phenyl) isoindolin-2-yl)butanoic acid;

(S)-3-Methyl-2-(1 -oxo-6-(4-(phenylmethylsulfonamido)phenyl)isoindolin-2-yl)butanoic acid;

(S)-3-Methyl-2-(6-(4-(1 -methylethylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)butanoic acid;

(S)-2-(6-(4-Benzamidophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(6-(4-(4-Fluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-3-Methyl-2-(1 -oxo-6-(4-(4-(trifluoromethyl)benzamido)phenyl)isoindolin-2-yl)butanoic acid;

(S)-2-(6-(4-(4-Methoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-2-(6-(4-(3-Fluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-2-(6-(4-(3-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-2-(6-(4-(2,4-Difluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-3-Methyl-2-(6-(4-(4-methylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)butanoic acid; (S)-2-(6-(4-(4-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-2-(6-(4-(4-tert-Butylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-2-(6-(4-(Cyclohexanecarboxamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(6-(4-Biphenyl-4-ylcarboxamidophenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)- 2-(6-(4-(2-Naphthamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-3-Methyl-2-(1 -oxo-6-(4-(4-pentylbenzamido)phenyl)isoindolin-2-yl)butanoic acid; (S)-2-(6-(4-(2-Fluoro-6-(trifluoromethyl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(6-(4-(Benzo[d][1 ,3]dioxole-5-carboxamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)- 2-(6-(4-(2,6-Dichlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)- 2-(6-(4-(2-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)- 2-(6-(4-(2,4-Dichlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)- 2-(6-(4-(4-Butoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-2-(6-(4-(2,6-Difluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)- 2-(6-(4-(3,4-Difluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-2-(6-(4-(3,4-Dimethoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)- 3-Methyl-2-(1 -oxo-6-(4-(3,4,5-trimethoxybenzamido)phenyl)isoindolin-2-yl) butanoic acid;

(S)- 2-(6-(4-(3,5-Diethoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)- 3-Methyl-2-(1 -oxo-6-(4-(3-phenoxybenzamido)phenyl)isoindolin-2-yl) butanoic acid;

(S)-3-Methyl-2-(1 -oxo-6-(4-(4-phenoxybenzamido)phenyl)isoindolin-2-yl) butanoic acid;

(S)- 3-Methyl-2-(1 -oxo-6-(4-(2-phenoxybenzamido)phenyl)isoindolin-2-yl) butanoic acid;

(S)-3-Methyl-2-(1 -oxo-6-(4-(2,4,6-trimethylbenzamido)phenyl)isoindolin-2-yl) butanoic acid;

(S)- 2-(6-(4-(2,4-Dimethoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-3-Methyl-2-(1 -oxo-6-(4-(4-(trifluoromethoxy)benzamido)phenyl)isoindolin-2-yl)butanoic acid;

(S)- 2-(6-(4-(2-Methoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)- 2-(6-(4-(4-Fluoro-3-methylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)- 2-(6-(4-(4-Butylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)- 2-(6-(4-(2,6-Difluoro-3-methylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(6-(4-(4-Ethylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)- 3-Methyl-2-(1 -oxo-6-(4-(4-propylbenzamido)phenyl)isoindolin-2-yl)butanoic acid; (S)- 3-Methyl-2-(6-(4-(4-octylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)butanoic acid; (S)- 2-(6-(4-(4-Cyclohexylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-3-Methyl-2-(1 -oxo-6-(4-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydro naphthalene-2-carboxamido)phenyl)isoindolin-2-yl)butanoic acid;

(S)- 2-(6-(4-(1 -Naphthamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-2-(6-(4-(3,5-Dimethoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)- 2-(6-(4-(4-Hexylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)- 2-(6-(4-(4-Heptylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)- 3-Methyl-2-(6-(4-(4-nonylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)butanoic acid; (S)- 2-(6-(4-(4-Decylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid; (S)-2-(6-(4-(Adamantyl-2-carboxamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(6-(4-(2-Fluoro-4-(trifluoromethyl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(6-(4-(2-Fluoro-3-(trifluoromethyl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)- 2-(6-(4-(3-Fluoro-4-(trifluoromethyl)benzamido)phenyl)-1 -oxoisoindolin-2-yl) -3-methylbutanoic acid;

(S)-2-(6-(4-(4-Fluoro-2-(trifluoromethyl)benzamido)phenyl)-1 -oxoisoindolin-2-yl) -3-methylbutanoic acid;

(S)-3-Methyl-2-(1 -oxo-6-(4-(2-(trifluoromethyl)benzamido)phenyl)isoindolin-2-yl)butanoic acid;

(S)-2-(6-(4-(2-Ethoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-3-Methyl-2-(6-(4-(nicotinamido)phenyl)-1 -oxoisoindolin-2-yl)butanoic acid;

(S)- 2-(6-(4-(2-Chloronicotinamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-3-Methyl-2-(6-(4-(6-morpholinonicotinamido)phenyl)-1 -oxoisoindolin-2-yl) butanoic acid;

(S)- 3-Methyl-2-(1 -oxo-6-(4-(6-(piperidin-1 -yl)nicotinamido)phenyl)isoindolin-2-yl)butanoic acid;

(S)-3-Methyl-2-(1 -oxo-6-(4-(6-(pyrrolidin-1 -yl)nicotinamido)phenyl) isoindolin-2-yl)butanoic acid;

(S)-2-(5-(4-(3-(4-Fluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(5-(4-(3-(2-Fluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-2-(5-(4-(3-(3-Fluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-3-Methyl-2-(1 -oxo-5-(4-(3-phenylureido)phenyl)isoindolin-2-yl)butanoic acid; (S)-2-(5-(4-(3-Cyclohexylureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid; (S)-2-(5-(4-(3-(2,4-Difluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(5-(4-(3-(3,4-Difluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-3-Methyl-2-(1 -oxo-5-(4-(3-p-tolylureido)phenyl)isoindolin-2-yl)butanoic acid; (S)-3-Methyl-2-(1 -oxo-5-(4-(3-m-tolylureido)phenyl)isoindolin-2-yl)butanoic acid; (S)-3-Methyl-2-(1 -oxo-5-(4-(3-(4-(trifluoromethyl)phenyl)ureido)phenyl) isoindolin-2-yl)butanoic acid;

(S)-3-Methyl-2-(1 -oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl) isoindolin -2-yl)butanoic acid;

(S)-2-(5-(4-(3-(4-Methoxyphenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(5-(4-(3-(3-Methoxyphenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(5-(4-(3-(4-Cyanophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(5-(4-(3-(3-Cyanophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(5-(4-(3-(2-Fluorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(5-(4-(3-(3-Fluorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-2-(5-(4-(3-(4-Methoxyphenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(5-(4-(3-(3-Methoxyphenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-2-(5-(4-(3-(4-Chlorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(5-(4-(3-(3-Chlorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(5-(4-(3-(4-Cyanophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-3-Methyl-2-(1 -oxo-5-(4-(3-(2-(trifluoromethyl)phenyl)thioureido)phenyl) isoindolin-2-yl)butanoic acid;

(S)-3-Methyl-2-(1 -oxo-5-(4-(3-o-tolylthioureido)phenyl)isoindolin-2-yl)butanoic acid; (S)-3-Methyl-2-(1 -oxo-5-(4-(3-p-tolylthioureido)phenyl)isoindolin-2-yl)butanoic acid; (S)-2-(5-(4-(3-(3-Fluorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-2-(5-(4-(3-(3-Methoxyphenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(5-(4-(3-(2-Methoxyphenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-3-Methyl-2-(1 -oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)thioureido)phenyl) isoindolin-2-yl)butanoic acid;

(S)-3-Methyl-2-(1 -oxo-6-(4-(phenylsulfonamido)phenyl)isoindolin-2-yl)butanoic acid; (S)-2-(5-(4-(4-Cyanophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-2-(5-(4-(3,4-Difluorophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(5-(4-(2,4-Difluorophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(5-(4-(3,4-Dimethoxyphenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(5-(4-(3-Chlorophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-2-(5-(4-(4-Methoxyphenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-3-Methyl-2-(1 -oxo-5-(4-(4-(trifluoromethyl)phenylsulfonamido)phenyl) isoindolin-2-yl)butanoic acid;

(S)-3-Methyl-2-(1 -oxo-5-(4-(phenylmethylsulfonamido) phenyl) isoindolin-2-yl)butanoic acid;

(S)-2-(5-(4-(Cyclohexanesulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(5-(4-Benzamidophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(5-(4-(4-Fluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-3-Methyl-2-(1 -oxo-5-(4-(4-(trifluoromethyl)benzamido)phenyl)isoindolin-2-y/l)butanoic acid;

(S)-2-(5-(4-(4-Methoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-2-(5-(4-(3-Fluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-2-(5-(4-(3-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-2-(5-(4-(2,4-Difluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-3-Methyl-2-(5-(4-(4-methylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)butanoic acid; (S)-2-(5-(4-(4-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-2-(5-(4-(4-tert-Butylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-3-Methyl-2-(1 -oxo-5-(4-(4-pentylbenzamido)phenyl)isoindolin-2-yl)butanoic acid; (R)-3-Methyl-2-(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)iso indolin-2-yl)butanoic acid;

2-(1 -Oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)acetic acid; (S)-2-(1 -Oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl) propanoic acid;

2-Methyl-2-(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)propanoic acid;

1 - (1 -Oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl) cyclopentanecarboxylic acid;

(S)-2-(1 -Oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)-2-phenylacetic acid;

4-(1 -Oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)butanoic acid;

(S)-4-Methyl-2-(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)iso indolin-2-yl)pentanoic acid;

(S)-3-Methoxy-2-(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)iso indolin-2 yl)propanoic acid;

(R)-3-Methyl-2-(1 -oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl) isoindolin-2-yl)butanoic acid;

2- (1 -Oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)acetic acid; (S)-2-(1 -Oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl) propanoic acid;

1 -(1 -Oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl) cyclopentanecarboxylic acid;

(S)-2-(1 -Oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)-2-phenylacetic acid;

4-(1 -Oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl) butanoic acid;

3- (1 -Oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)propanoic acid;

(S)-2-(1 -Oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)-3-phenylpropanoic acid;

(S)-3-Methoxy-2-(1 -oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl) isoindolin-2 yl)propanoic acid;

(S)-4-Methyl-2-(1 -oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)iso indolin-2-yl)pentanoic acid;

(S)- 2-(6-(5-(3-(2-Chlorophenyl)ureido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)- 2-(6-(5-(3-(4-Chloro-2-phenoxyphenyl)ureido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)- 2-(6-(5-(3-(3,4-Dimethylphenyl)ureido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)- 2-(6-(5-(3-(3,4-Difluorophenyl)ureido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)- 2-(6-(5-(3-(2,3-Dihydro-1 H-inden-5-yl)ureido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(6-(5-(4-tert-Butylbenzamido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)- 3-Methyl-2-(1 -oxo-6-(5-(4-pentylbenzamido)pyridin-2-yl)isoindolin-2-yl)butanoic acid;

(S)- 2-(6-(5-Biphenyl-4-ylcarboxamidopyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-2-(6-(5-(2-Naphthamido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)- 2-(6-(5-(4-Butoxybenzamido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)- 2-(6-(4-(3-(2-Chlorophenyl)ureido)-2-(trifluoromethyl)phenyl)-1 -oxoiso indolin-2-yl)-3-methylbutanoic acid;

(S)- 2-(6-(4-(3-(3,4-Difluorophenyl)ureido)-2-(trifluoromethyl)phenyl)-1 -oxoiso indolin- 2- yl)-3-methylbutanoic acid;

(S)-2-(6-(4-(3-(2,3-Dihydro-1 H-inden-5-yl)ureido)-2-(trifluoromethyl)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)- 2-(6-(4-(3-(3,4-Dimethylphenyl)ureido)-2-(trifluoromethyl)phenyl)-1 -oxoiso indolin-2-yl)-3-methylbutanoic acid;

(S)- 2-(6-(4-(4-tert-Butylbenzamido)-2-(trifluoromethyl)phenyl)-1 -oxoisoindolin-2-yl)- 3- methylbutanoic acid;

(S)- 2-(6-(4-Biphenyl-4-ylcarboxamido-2-(trifluoromethyl)phenyl)-1 -oxoiso indolin-2-yl)-3-methylbutanoic acid;

(S)- 2-(6-(4-(2-Naphthamido)-2-(trifluoromethyl)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)- 3-Methyl-2-(1 -oxo-6-(4-(4-pentylbenzamido)-2-(trifluoromethyl) phenyl) isoindolin-2-yl)butanoic acid;

(S)- 2-(6-(4-(4-Butoxybenzamido)-2-(trifluoromethyl)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(6-(4-(3-(3,4-Dimethylphenyl)ureido)-3-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)- 2-(6-(4-(3-(2,3-Dihydro-1 H-inden-5-yl)ureido)-3-fluorophenyl)-1 -oxoiso indolin-2-yl)-3-methylbutanoic acid; (S)- 2-(6-(4-(3-(3,4-Difluorophenyl)ureido)-3-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(6-(4-(3-(2-Chlorophenyl)ureido)-3-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)- 2-(6-(4-(4-tert-Butylbenzamido)-3-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(6-(3-Fluoro-4-(4-pentylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)- 2-(6-(4-Biphenyl-4-ylcarboxamido-3-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)- 2-(6-(4-(2-Naphthamido)-3-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)- 2-(6-(4-(4-Butoxybenzamido)-3-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-2-(6-(4-(4-tert-Butylbenzamido)-2-methoxyphenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(6-(4-Biphenyl-4-ylcarboxamido-2-methoxyphenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(6-(4-(4-Butoxybenzamido)-2-methoxyphenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(6-(2-Methoxy-4-(4-pentylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(6-(2-Methoxy-4-(4-(trifluoromethoxy)benzamido)phenyl)-1 -oxoiso indolin-2-yl)-3-methylbutanoic acid;

(S)-2-(6-(4-(4-tert-Butylbenzamido)-2-methylphenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(6-(4-Biphenyl-4-ylcarboxamido-2-methylphenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(6-(4-(4-Butoxybenzamido)-2-methylphenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-3-Methyl-2-(6-(2-methyl-4-(4-pentylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)butanoic acid;

(S)-3-Methyl-2-(6-(2-methyl-4-(4-(trifluoromethoxy)benzamido)phenyl)-1 -oxoisoindolin-2-yl)butanoic acid;

(S)-2-(6-(4-(4-tert-Butylbenzamido)-2-chlorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(6-(4-Biphenyl-4-ylcarboxamido-2-chlorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(6-(4-(4-Butoxybenzamido)-2-chlorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(6-(2-Chloro-4-(4-pentylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(6-(2-Chloro-4-(4-(trifluoromethoxy)benzamido)phenyl)-1 -oxoiso indolin-2-yl)-3-methylbutanoic acid;

(S)-2-(6-(6-(4-tert-Butylbenzamido)pyridin-3-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(6-(6-(4-tert-Butylbenzamido)pyridazin-3-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-3-Methyl-2-(1 -oxo-6-(6-(4-pentylbenzamido)pyridazin-3-yl)isoindolin-2-yl)butanoic acid;

(S)-3-Methyl-2-(1 -oxo-6-(6-(4-(trifluoromethoxy)benzamido)pyridazin-3-yl)isoindolin-2-yl)butanoic acid;

(S)-2-(6-(5-(4-tert-Butylbenzamido)pyrazin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(6-(5-Biphenyl-4-ylcarboxamidopyrazin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(6-(5-(4-Butoxybenzamido)pyrazin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-3-Methyl-2-(1 -oxo-6-(5-(4-pentylbenzamido)pyrazin-2-yl)isoindolin-2-yl)butanoic acid;

(S)-3-Methyl-2-(1 -oxo-6-(5-(4-(trifluoromethoxy)benzamido)pyrazin-2-yl)isoindolin-2-yl)butanoic acid;

2-(6-(4-([1 ,1 '-Biphenyl]-4-ylcarboxamido)phenyl)-1 -oxoisoindolin-2-yl)-2-methyl propanoic acid;

2-(6-(4-(4-(tert-Butyl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)-2-methyl propanoic acid;

2-(6-(4-(4-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-2-methylpropanoic acid; 2-Methyl-2-(1 -oxo-6-(4-(4-(trifluoromethoxy)benzamido)phenyl)isoindolin-2-yl)propanoic acid;

2- Methyl-2-(1 -oxo-6-(4-(4-pentylbenzamido)phenyl)isoindolin-2-yl)propanoic acid; 1 -(6-(4-([1 ,1 '-Biphenyl]-4-ylcarboxamido)phenyl)-1 -oxoisoindolin-2-yl) cyclopentane carboxylic acid;

1 -(6-(4-(4-(tert-Butyl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclopentane carboxylic acid;

1 -(6-(4-(4-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclopentane carboxylic acid;

1 -(1 -Oxo-6-(4-(4-(trifluoromethoxy)benzamido)phenyl)isoindolin-2-yl) cyclopentane carboxylic acid;

1 -(1 -Oxo-6-(4-(4-pentylbenzamido)phenyl)isoindolin-2-yl)cyclopentane carboxylic acid;

(R)-2-(6-(4-([1 ,1 '-Biphenyl]-4-ylcarboxamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

3- (6-(4-([1 ,1 '-Biphenyl]-4-ylcarboxamido)phenyl)-1 -oxoisoindolin-2-yl)cyclo hexane carboxylic acid;

3-(6-(4-(3-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclohexane carboxylic acid;

3-(6-(4-(4-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclohexane carboxylic acid;

3-(1 -Oxo-6-(4-(4-(trifluoromethyl)benzamido)phenyl)isoindolin-2-yl)cyclo

hexanecarboxylic acid;

3-(6-(4-(5-Methyl-2-phenyloxazole-4-carboxamido)phenyl)-1 -oxoisoindolin-2-yl)cyclohexanecarboxylic acid;

(1 r,4r)-4-(6-(4-([1 ,1 '-Biphenyl]-4-ylcarboxamido)phenyl)-1 -oxoisoindolin-2-yl) cyclohexanecarboxylic acid;

(1 r,4r)-4-(6-(4-(3-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclohexane carboxylic acid;

(1 r,4r)-4-(6-(4-(4-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclohexane carboxylic acid;

(1 r,4r)-4-(1 -Oxo-6-(4-(4-(trifluoromethyl)benzamido)phenyl)isoindolin-2-yl) cyclohexanecarboxylic acid;

(1 r,3s,5R,7S)-3-(6-(4-(3-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl) adamantane-1 -carboxylic acid;

(1 r,3s,5R,7S)-3-(6-(4-(4-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl) adamantane-1 -carboxylic acid;

(1 r,3s,5R,7S)-3-(1 -Oxo-6-(4-(4-(trifluoromethyl)benzamido)phenyl)isoindolin-2-yl)adamantane-1 -carboxylic acid;

(1 r,3s,5R,7S)-3-(6-(4-(4-Methylbenzamido)phenyl)-1 -oxoisoindolin-2-yl) adamantane-1 -carboxylic acid;

1 -(6-(4-([1 ,1 '-Biphenyl]-4-ylcarboxamido)phenyl)-1 -oxoisoindolin-2-yl) cyclobutane carboxylic acid;

1 -(6-(4-(4-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclobutane carboxylic acid;

1 -(1 -Oxo-6-(4-(4-(trifluoromethyl)benzamido)phenyl)isoindolin-2-yl) cyclo butanecarboxylic acid;

1 -(6-(4-(4-Methylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclobutane carboxylic acid;

1 -(6-(4-([1 ,1 '-Biphenyl]-4-ylcarboxamido)phenyl)-1 -oxoisoindolin-2-yl)

cyclopropanecarboxylic acid;

1 -(6-(4-(4-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclopropane carboxylic acid;

1 -(1 -Oxo-6-(4-(4-(trifluoromethyl)benzamido)phenyl)isoindolin-2-yl)cyclo propane carboxylic acid;

(1 S,2R)-2-(6-(4-(4-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclopentane carboxylic acid;

(1 S,2R)-2-(1 -Oxo-6-(4-(4-(trifluoromethyl)benzamido)phenyl)isoindolin-2-yl) cyclopentanebcarboxylic acid;

(S)-2-(6-(4-([1 ,1 '-Biphenyl]-4-ylcarboxamido)-2-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(6-(4-(4-(tert-Butyl)benzamido)-2-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(6-(4-(4-Chlorobenzamido)-2-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-2-(6-(2-Fluoro-4-(4-(trifluoromethoxy)benzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(6-(2-Fluoro-4-(4-pentylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;

(S)-3-Methyl-2-(1 -oxo-6-(4-(5-phenylthiazole-2-carboxamido)phenyl)isoindolin-2-yl)butanoic acid;

(S)-3-Methyl-2-(1 -oxo-6-(4-(5-phenyloxazole-2-carboxamido)phenyl) isoindolin-2-yl)butanoic acid;

(S)-2-(6-(4-(3-(4-Fluorophenyl)isoxazole-5-carboxamido)phenyl)-1 -oxo isoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(6-(4-(3-(4-Chlorophenyl)isoxazole-5-carboxamido)phenyl)-1 -oxo

isoindolin-2-yl)-3-methylbutanoic acid ;

(S)-3-Methyl-2-(1 -oxo-6-(4-(3-(4-(trifluoromethyl)phenyl)isoxazole-5-carboxamido)phenyl)isoindolin-2-yl)butanoic acid;

(S)-3-Methyl-2-(6-(4-(4-(oxazol-5-yl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)butanoic acid;

(S)-3-Methyl-2-(1 -oxo-6-(4-(4-phenylthiazole-2-carboxamido)phenyl)isoindolin-2-yl)butanoic acid;

(S)-3-Methyl-2-(1 -oxo-6-(4-(5-phenyl-1 ,3,4-thiadiazole-2-carboxamido)

phenyl)isoindolin-2-yl)butanoic acid;

(S)-3-Methyl-2-(1 -oxo-6-(4-(5-phenyl-4H-1 ,2,4-triazole-3-carboxamido) phenyl) isoindolin-2-yl)butanoic acid;

(S)-2-(6-(4-(4-(2-Cyanopropan-2-yl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(6-(4-(4-(3-Cyanopentan-3-yl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-3-Methyl-2-(1 -oxo-6-(5-(5-phenyloxazole-2-carboxamido)pyridin-2-yl) isoindolin-2-yl)butanoic acid;

(S)-3-Methyl-2-(1 -oxo-6-(5-(5-phenylthiazole-2-carboxamido)pyridin-2-yl) isoindolin-2-yl)butanoic acid;

(S)-2-(6-(5-(3-(4-Fluorophenyl)isoxazole-5-carboxamido)pyridin-2-yl)-1 -oxo isoindolin-2-yl)-3-methylbutanoic acid;

(S)-2-(6-(4-(4-(1 ,3,4-Oxadiazol-2-yl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;

(S)-3-Methyl-2-(6-(4-(5-methyl-2-phenyloxazole-4-carboxamido)phenyl)-1 -oxoisoindolin-2-yl)butanoic acid;

(S)-3-Methyl-2-(1 -oxo-6-(4-(2-phenyl-5-(trifluoromethyl)oxazole-4-carboxamido) phenyl)isoindolin-2-yl)butanoic acid;

(S)-3-Methyl-2-(1 -oxo-6-(4-(4-(thiazol-2-yl)benzamido)phenyl)isoindolin-2-yl) butanoic acid;

(S)-2-(6-(4-(5-Butylpicolinamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-3-Methyl-2-(1 -oxo-6-(4-(quinoline-3-carboxamido)phenyl)isoindolin-2-yl) butanoic acid;

(S)-3-Methyl-2-(1 -oxo-6-(4-(4-(pyrimidin-5-yl)benzamido)phenyl)isoindolin-2-yl)butanoic acid;

(S)-3-Methyl-2-(6-(5-(5-methyl-2-phenyloxazole-4-carboxamido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)butanoic acid;

(S)-3-Methyl-2-(1 -oxo-6-(5-(2-phenyl-5-(trifluoromethyl)oxazole-4-carboxamido) pyridin-2-yl)isoindolin-2-yl)butanoic acid; and

(S)-3-Methyl-2-(1 -oxo-6-(4-(2-phenylacetamido)phenyl)isoindolin-2-yl)butanoic acid; or a stereoisomer, tautomer, pharmaceutically acceptable salt, pharmaceutically acceptable solvate, pharmaceutically acceptable polymorph, pharmaceutically acceptable prodrug, N-oxide or carboxylic acid isostere thereof.

The compounds of the present invention also include all stereoisomeric and tautomeric forms and mixtures thereof in all ratios and their pharmaceutically

acceptable salts, solvates, polymorphs, prodrugs, carboxylic acid isosteres and N-oxides.

According to another aspect of present invention, a compound of formula 1 can be prepared in a number of ways including using methods well known to the person skilled in the art. Examples of methods to prepare the present compounds are described below and illustrated in Schemes 1 to 10 but not limited thereto. It will be appreciated by persons skilled in the art that within certain of the processes described herein, the order of the synthetic steps employed may be varied and will depend inter alia on factors such as the nature of functional groups present in a particular substrate and the protecting group strategy (if any) to be adopted. Clearly, such factors will also influence the choice of reagent to be used in the synthetic steps.

The reagents, reactants and intermediates used in the following processes are either commercially available or can be prepared according to standard literature procedures known in the art. The starting compounds and the intermediates used for the synthesis of compounds of the present invention are referred to numerically . Throughout the process description, the corresponding substituent groups in the various formulae representing starting compounds and intermediates have the same meanings as that for the compound of formula I unless stated otherwise.

The schemes of the present invention are referred to numerically (1 A to 1 E;

2A to 2E; 3A to 3E; 4A to 4E; 5A to 5E; 6A to 6E; 7A to 7E; 8A to 8E; 9A to 9E and 10A to 10E). The processes used in various schemes of the present invention, are referred to with general symbols such as 1 a to 1 t, 2a to 2s, 3a to 3y, 4a to 4n, 5a to 5q, 6a to 6q, 7a to 7q, 8a to 8s, 9a, 9b and 10a. The schemes depict the preparation of compounds of formula 1 , wherein m is 1 . The compounds of formula 1 , wherein m is an integer selected from 2 to 4, may be analogously prepared. Processes for the preparation of compounds of the present invention are set forth in the following schemes:

Scheme 1 A: Preparation of compound of formula 1 ; wherein Y^=C 2, Y2=C(0); Xi, X2, X4 and X5 are selected from CH or CR, X3=C; L= NHC(0)NH; m=1 ; A, n, R, Ri, R2 and R9 are as defined in formula 1 ;

Scheme 1 A

Step 1

Preparation of compound of formula 3:

Commercially available compound of formula 2 can be subjected to bromination using bromine in presence of suitable catalyst such as Fe at temperature ranging from 0-30 °C to yield compound of formula 3 (Reaction 1 a).

Step 2

Preparation of compound of formula 4:

Compound of formula 3 can be converted to its corresponding methyl ester by reaction with methanol and SOCI2 at temperature ranging from 0-30 °C or by heating with methanol and inorganic acid such as sulfuric acid or hydrochloric acid at temperature ranging from 50-100 °C to yield compound of formula 4 (Reaction 1 b).

Step 3

Preparation of compound of formula 5:

Compound of formula 4 can be treated with compound of formula 4P:

and bis(pinacolo)diboron, in presence of suitable reagent such as palladium acetate or tetrakis palladium and a suitable base such as potassium acetate, sodium carbonate or cesium carbonate in a suitable solvent such as toluene, dioxane, dimethoxyethane, DMF or acetone at a temperature ranging from 70-120 °C to obtain compound of formula 5 (Reaction 1 c).

Step 4

Preparation of compound of formula 6:

Compound of formula 5 can be refluxed with N-bromosuccinimide and a catalytic amount of AIBN or benzoyl peroxide in a suitable solvent such as CCI4 using irradiation (200 watt bulb) at a temperature ranging from 80-100 °C to obtain compound of formula 6 (Reaction 1 d).

Step 5

Preparation of compound of formula 7:

Compound of formula 6 can be treated with com ound of formula 6P:

6P (HCI salt)

wherein Ri and R2 are as defined in formula 1 ;

in presence of a suitable base such as triethylamine in a suitable solvent such as benzene or toluene at a temperature ranging from 70-120 °C to obtain compound of formula 7 (Reaction 1e).

Alternatively, potassium carbonate may be used as a base in a suitable solvent such as DMF or THF at a temperature ranging from 50-80 °C.

Step 6

Preparation of compound of formula 8:

Compound of formula 7 can be reduced using a suitable reducing agent such as Fe and ammonium chloride in a suitable solvent such as aqueous EtOH or EtOH: THF: H20 at a temperature ranging from 70-100 °C to obtain compound of formula 8 (Reaction 1f).

Alternatively, other reducing agents such as Fe and HCI in a solvent such as H20 or ethanol or combination thereof; SnCI2 in a solvent such as ethyl acetate; hydrogen over Raney Ni, Pd/C or Pt/C catalyst in a solvent such as methanol (pressure ranging from 50-80 psi and temperature ranging from 20-65 °C); or cobalt chloride and zinc in a solvent such as DMF or water (temperature ranging from 20-100 °C) may be used.

Step 7

Preparation of compound of formula 9:

Compound of formula 8 can be treated with compound of formula 8P:

A-(CH2)n-NCO

8P

wherein A and n are as defined in formula 1 ;

in a suitable solvent such as dichloromethane or THF at a temperature ranging from 20-35 °C to obtain compound of formula 9 (Reaction 1 g).

Step 8

Preparation of compound of formula 10:

Compound of formula 9 can be hydrolysed using a suitable reagent such as 1 N LiOH or 1 N NaOH in a suitable solvent such as MeOH or THF at a temperature ranging from 20-35 °C to obtain compound of formula 10 (Reaction 1 h).

Step 9

The carboxylic acid (compound of formula 10) may be optionally converted to its corresponding ester prodrugs by any suitable method well known in the art.

Scheme 1 B: Preparation of compound of formula 1 ; wherein Y^=C 2, Y2=C(0); Xi, X2, X4 and X5 are selected from CH or CR, X3=C; L= NHC(S)NH; m=1 , A, n, R, Ri, R2 and R9 are as defined in formula 1 ;

Scheme 1 B

Step 1

Preparation of compound of formula 11 :

Compound of formula 8 (obtained in Step 6 of Scheme 1 A) can be treated with compound of formula 8Q:

A-(CH2)n-NCS

8Q

wherein A and n are as defined in formula 1 ;

in presence of a suitable solvent such as THF or dichloromethane at temperature ranging from 20-35 °C to obtain compound of formula 11 (Reaction 1j).

Step 2

Preparation of compound of formula 12:

Compound of formula 11 can be hydrolysed using suitable reagent such as 1 N LiOH or 1 N NaOH in a suitable solvent such as MeOH or THF at temperature ranging from 20-35 °C to obtain compound of formula 12 (Reaction 1 k).

Step 3

The carboxylic acid (compound of formula 12) may be optionally converted to its corresponding ester prodrugs by any suitable method well known in the art.

Scheme 1 C: Preparation of compound of formula 1 ; wherein Y†=CH2, Y2=C(0); Xi, X2, X4 and X5 are selected from CH or CR, X3=C; L= *S02NH; m=1 ; A, n, R, Ri, R2 and R9 are as defined in formula 1 ;

Scheme 1 C

Step 1

Preparation of compound of formula 13:

Compound of formula 8 (obtained in Step 6 of Scheme 1 A) can be treated with compound of formula 8R:

A-(CH2)n-S02CI

8R

wherein A and n are as defined in formula 1 ;

in presence of a suitable base such as pyridine or triethylamine in a suitable solvent such as dichloromethane at temperature ranging from 20-35 °C to obtain compound of formula 13 (Reaction 1 m).

Step 2

Preparation of compound of formula 14:

Compound of formula 13 can be hydrolysed using suitable reagent such as 1 N LiOH or 1 N NaOH in a suitable solvent such as MeOH or THF at temperature ranging from 20-35 °C to obtain compound of formula 14 (Reaction 1 n).

Step 3

The carboxylic acid (compound of formula 14) may be optionally converted to its corresponding ester prodrugs by any suitable method well known in the art.

Scheme 1 D: Preparation of compound of formula 1 ; wherein Y^=C 2, Y2=C(0); Xi, X2, X4 and X5 are selected from CH or CR, X3=C; L= *CONH; m=1 ; A, n, R, R15 R2 and R9 are as defined in formula 1 ;

Scheme 1 D

Step 1

Preparation of compound of formula 15:

Compound of formula 8 (obtained in Step 6 of Scheme 1 A) can be treated with compound of formula 8S:

A-(CH2)n-COCI

8S

wherein A and n are as defined in formula 1 ;

in presence of a suitable base such as pyridine in a suitable solvent such as dichloromethane or THF at temperature ranging from 20-35 °C to obtain compound of formula 15 (Reaction 1 p).

Alternatively, compound of formula 8 (obtained in Step 6 of Scheme 1 A) can be treated with the acid A-(CH2)n-COOH, wherein A and n are as defined in formula 1 ; in presence of a reagent such as isobutylchloroformate and a base such as N-methylmorpholine in a suitable solvent such as THF at a temperature range of 0 °C to room temperature (20-35 °C) for about 2-4 h to obtain compound of formula 15.

Alternatively, compound of formula 8 (obtained in Step 6 of Scheme 1 A) may be heated with the ester A-(CH2)nCOO-(Ci-C6)-alkyl, wherein A represents a 5-membered heteroaryl ring containing one or more heteroatoms selected from 1 -3 N, O and S, and substituted with a phenyl group, wherein both phenyl and heteroaryl rings may be substituted with one or more groups selected from halogen, hydroxy, (CrCi2)-alkoxy, cyano, (CrCi2)-alkyl, CF3 and OCF3; n is as defined in formula 1 ; in a solution of 2M AIMe3 in toluene at 60-80 °C in a sealed tube for about 2-4 h to obtain compound of example 15.

In another alternate scheme, compound of formula 8 (obtained in Step 6 of Scheme 1 A) may be heated with ester A-(CH2)nCOO-(Ci-C6)-alkyl, wherein A represents a phenyl group substituted with a 5-membered heteroaryl ring optionally containing heteroatoms selected from 1 -3 N, O and S, and substituted with a phenyl group; wherein both phenyl and heteroaryl rings may be substituted with one or more groups selected from halogen, hydroxy, (CrCi2)-alkoxy, cyano, (Ci-Ci2)-alkyl, CF3 and OCF3; n is as defined in formula 1 ; in presence of carbonyl chloride in a solvent mixture of dichloromethane and DMF at 20-35 °C for about 2-4 h to obtain compound of example 15,

Step 2

Preparation of compound of formula 16:

Compound of formula 15 can be hydrolysed using suitable reagent such as 1 N LiOH or 1 N NaOH in a suitable solvent such as MeOH or THF at temperature ranging from 20-35 °C to obtain compound of formula 16 (Reaction 1 q).

Step 3

The carboxylic acid (compound of formula 16) may be optionally converted to its corresponding ester prodrugs by any suitable method well known in the art.

Scheme 1 E: Preparation of compound of formula 1 ; wherein Y†=CH2, Y2=C(0); Xi, X2, X4 and X5 are selected from CH or CR, X3=C; L= *NHS02; m=1 ; A, n, R, Ri, R2 and R9 are as defined in formula 1 ;

Scheme 1 E

Step 1

Preparation of compound of formula 17:

Compound of formula 8 (obtained in Step 6 of Scheme 1 A) can be treated with NaN02 and concentrated HCI to form a diazonium salt, which is treated with acetic acid saturated with S02 gas, followed by treatment with CuCI2 at a temperature ranging from 0-35 °C to obtain compound of formula 17 (Reaction 1 r).

Step 2

Preparation of compound of formula 18:

Compound of formula 17 can be treated with compound of formula 8T:

A-(CH2)n-NH2

8T

wherein A and n are as defined in formula 1 ;

in a suitable solvent such as dichloromethane and a base such as pyridine at temperature ranging from 20-35 °C to obtain compound of formula 18 (Reaction 1s).

Step 3

Preparation of compound of formula 19:

Compound of formula 18 can be hydrolysed using suitable reagent such as 1 N LiOH or 1 N NaOH in a suitable solvent such as MeOH or THF at temperature ranging from 20-35 °C to obtain compound of formula 19 (Reaction 1 t).

Step 4

The carboxylic acid (compound of formula 19) may be optionally converted to its corresponding ester prodrugs by any suitable method well known in the art.

Scheme 2A: Preparation of compound of formula 1 ; wherein Y^=C{0), Y2=CH2; Xi, X2, X4 and X5 are selected from CH or CR, X3=C; L=NHC(0)NH; m=1 ; A, n, R, Ri, R2 and R9 are as defined in formula 1 ;

Scheme 2A

Step 1

Preparation of compound of formula 21 :

Commercially available compound of formula 20 can be converted to its corresponding methyl ester by reaction with methanol and SOCI2 at temperature ranging from 0-30 °C or by heating with methanol and inorganic acid such as sulfuric acid or hydrochloric acid at a temperature ranging from 50-100 °C to yield compound of formula 21 (Reaction 2a).

Step 2

Preparation of compound of formula 22:

The preparation involves two steps.

i) Preparation of compound of formula 21 B wherein Xi, X2, X4 and X5 are selected from CH or CR; R

21 B

Compound of formula 21 A:

21 A

wherein Xi, X2, X4 and X5 are selected from CH or CR, R is as defined in formula 1 ; can be treated with bis(pinacolo)diboron with a suitable catalyst such as palladium acetate and a suitable base such as potassium acetate, sodium carbonate or cesium carbonate in a solvent such as toluene, dioxane, dimethoxyethane, DMF or acetone at a temperature ranging from 70-120 °C to obtain compound of formula 21 B.

ii) Preparation of compound of formula 22:

Compound of formula 21 can be treated with compound of formula 21 B in presence of a catalyst such as Pd(dppf)CI2:CH2Cl2 and a base such as potassium carbonate, cesium carbonate or 2M Na2C03 (in water) in a suitable solvent such as DMF, dioxane, dimethoxyethane or acetone at a temperature ranging from 70-120 °C under an atmosphere of argon, to obtain compound of formula 22 (Reaction 2b).

Alternatively, compound of formula 21 can be treated with compound of formula 21 A in presence of bis(pinacolo)diboron with a suitable catalyst such as palladium acetate or tetrakis palladium and a suitable base such as potassium acetate, sodium carbonate or cesium carbonate in a solvent such as toluene, dioxane, dimethoxyethane, DMF or acetone at a temperature ranging from 70-120 °C to obtain compound of formula 22.

Step 3

Preparation of compound of formula 23:

Compound of formula 22 can be refluxed with N-bromosuccinimide and a catalytic amount of AIBN or benzoyl peroxide in a suitable solvent such as CCI4 using irradiation (200 watt bulb) at a temperature ranging from 80-100 °C to obtain compound of formula 23 (Reaction 2c).

Step 4

Preparation of compound of formula 24:

Compound of formula 23 can be treated with compound of formula 6P:

6P (HCI salt)

wherein Riand R2 are as defined in formula 1 ;

in presence of a suitable base such as triethylamine in a suitable solvent such as benzene or toluene at a temperature ranging from 70-120 °C to obtain compound of formula 24 (Reaction 2d).

Alternatively, potassium carbonate may be used as a base in a suitable solvent such as DMF or THF at a temperature ranging from 50-80 °C.

Step 5

Preparation of compound of formula 25:

Compound of formula 24 can be reduced using a suitable reducing agent such as Fe and ammonium chloride in a suitable solvent such as aqueous EtOH or EtOH: THF: H20 at a temperature ranging from 70-100 °C to obtain compound of formula 25 (Reaction 2e).

Alternatively, other reducing agents such as Fe and HCI in a solvent such as H20 or ethanol or combination thereof; SnCI2 in a solvent such as ethyl acetate; hydrogen over Raney Ni, Pd/C or Pt/C catalyst in a solvent such as methanol (pressure ranging from 50-80 psi and temperature ranging from 20-65 °C); or cobalt chloride and zinc in a solvent such as DMF or water (temperature ranging from 20-100 °C) may be used.

Step 6

Preparation of compound of formula 26:

Compound of formula 25 can be treated with compound of formula 8P:

A-(CH2)n-NCO

8P

wherein A and n are as defined in formula 1 ;

in a suitable solvent such as dichloromethane or THF at temperature ranging from 20-35 °C to obtain compound of formula 26 (Reaction 2f).

Step 7

Preparation of compound of formula 27:

Compound of formula 26 can be hydrolysed using suitable reagent such as 1 N LiOH or 1 N NaOH in a suitable solvent such as MeOH or THF at temperature ranging from 20-35 °C to obtain compound of formula 27 (Reaction 2g).

Step 8

The carboxylic acid (compound of formula 27) may be optionally converted to its corresponding ester prodrugs by any suitable method well known in the art.

Scheme 2B: Preparation of compound of formula 1 ; wherein Y^CiO), Y2=CH2; Xi, X2, X4 and X5 are selected from CH or CR, X3=C; L= NHC(S)NH; m=1 ; A, n, R, Ri, R2 and R9 are as defined in formula 1 ;

Scheme 2B

Step 1

Preparation of compound of formula 28:

Compound of formula 25 (obtained in Step 5 of Scheme 2A) can be treated with compound of formula 8Q:

A-(CH2)n-NCS

8Q

wherein A and n are as defined in formula 1 ;

in presence of a suitable solvent such as THF or dichloromethane at temperature ranging from 20-35 °C to obtain compound of formula 28 (Reaction 2h).

Step 2

Preparation of compound of formula 29:

Compound of formula 28 can be hydrolysed using suitable reagent such as 1 N LiOH or 1 N NaOH in a suitable solvent such as MeOH or THF at temperature ranging from 20-35 °C to obtain compound of formula 29 (Reaction 2j).

Step 3

The carboxylic acid (compound of formula 29) may be optionally converted to its corresponding ester prodrugs by any suitable method well known in the art.

Scheme 2C: Preparation of compound of formula 1 ; wherein Y^C^O), Y2=CH2; Xi, X2, X4 and X5 are selected from CH or CR, X3=C; L= *S02NH; m=1 ; A, n, R, Ri, R2 and R9 are as defined in formula 1 ;

Scheme 2C

Step 1

Preparation of compound of formula 30:

Compound of formula 25 (obtained in Step 5 of Scheme 2A) can be treated with compound of formula 8R:

A-(CH2)n-S02CI

8R

wherein A and n are as defined in formula 1 ;

in presence of a suitable base such as pyridine or triethylamine in a suitable solvent such as dichloromethane at temperature ranging from 20-35 °C to obtain compound of formula 30 (Reaction 2k).

Step 2

Preparation of compound of formula 31 :

Compound of formula 30 can be hydrolysed using suitable reagent such as 1 N LiOH or 1 N NaOH in a suitable solvent such as MeOH or THF at temperature ranging from 20-35 °C to obtain compound of formula 31 (Reaction 2m).

Step 3

The carboxylic acid (compound of formula 31 ) may be optionally converted to its corresponding ester prodrugs by any suitable method well known in the art.

Scheme 2D: Preparation of compound of formula 1 ; wherein Y =C(0), Y2=CH2; Xi, X2, X4 and X5 are selected from CH or CR, X3=C; L= *CONH; m=1 ; A, n, R, Ri, R2 and R9 are as defined in formula 1 ;

Scheme 2D

Step 1

Preparation of compound of formula 32:

Compound of formula 25 (obtained in Step 5 of Scheme 2A) can be treated with optionally substituted benzoyl chloride of formula 8S:

A-(CH2)n-COCI

8S

wherein A and n are as defined in formula 1 ;

in presence of a suitable base such as pyridine in a suitable solvent such as dichloromethane or THF at temperature ranging from 20-35 °C to obtain compound of formula 32 (Reaction 2n).

Step 2

Preparation of compound of formula 33:

Compound of formula 32 can be hydrolysed using suitable reagent such as 1 N LiOH or 1 N NaOH in a suitable solvent such as MeOH or THF at temperature ranging from 20-35 °C to obtain compound of formula 33 (Reaction 2p).

Step 3

The carboxylic acid (compound of formula 33) may be optionally converted to its corresponding ester prodrugs by any suitable method well known in the art.

Scheme 2E: Preparation of compound of formula 1 ; wherein Y^=C{0), Y2=CH2; Xi, X2, X4 and X5 are selected from CH or CR, X3=C; L= *NHS02; m=1 ; A, n, R, Ri, R2 and R9 are as defined in formula 1 ;

Scheme 2E

Step 1

Preparation of compound of formula 34:

Compound of formula 25 (obtained in Step 5 of Scheme 2A) can be treated with NaN02 and concentrated HCI to form a diazonium salt, which is treated with acetic acid saturated with S02 gas, followed by treatment with CuCI2 at a temperature ranging from 0-35 °C to obtain compound of formula 34 (Reaction 2q).

Step 2

Preparation of compound of formula 35:

Compound of formula 34 can be treated with compound of formula 8T:

A-(CH2)n-NH2

8T

wherein A and n are as defined in formula 1 ;

in a suitable solvent such as dichloromethane and a base such as pyridine at temperature ranging from 20-35 °C to obtain compound of formula 35 (Reaction 2r).

Step 3

Preparation of compound of formula 36:

Compound of formula 35 can be hydrolysed using suitable reagent such as 1 N LiOH or 1 N NaOH in a suitable solvent such as MeOH or THF at temperature ranging from 20-35 °C to obtain compound of formula 36 (Reaction 2s).

Step 4

The carboxylic acid (compound of formula 36) may be optionally converted to its corresponding ester prodrugs by any suitable method well known in the art.

Scheme 3A: Preparation of compound of formula 1 ; wherein Y†=CH2, Y2=C(0); Xi, X2, X4 and X5 are selected from CH or CR, X3=C; L=NHC(0)NH; m=1 ; A, n, R, Ri, R2 and R9 are as defined in formula 1 ;

Scheme 3A

37

Step 1

Preparation of compound of formula 38:

Compound of formula 37 is reacted with compound of formula 8P:

A-(CH2)n-NCO

8P

wherein A and n are as defined in formula 1 ;

in a suitable solvent such as dichloromethane or THF at temperature ranging from 20-35 °C to obtain compound of formula 38 (Reaction 3a).

Step 2

Preparation of compound of formula 39:

Compound of formula 38 can be treated with bis(pinacolato)diboron, Pd(dppf)CI2 and Pd(dppf)CI2:CH2Cl2 in a suitable solvent such as dioxane, dimethoxyethane, DMSO or DMF at temperature ranging from 50-100 °C to obtain compound of formula 39 (Reaction 3b).

Step 3

Preparation of compound of formula 40:

Compound of formula 4 can be refluxed with N-bromosuccinimide and a catalytic amount of AIBN or benzoyl peroxide in a suitable solvent such as CCI4 using irradiation (200 watt bulb) at a temperature ranging from 80-100 °C to obtain compound of formula 40 (Reaction 3c).

Step 4

Preparation of compound of formula 41 :

Compound of formula 40 can be treated with compound of formula 6P:

6P (HCI salt)

wherein Ri and R2 are as defined in formula 1 ;

in presence of a suitable base such as triethylamine in a suitable solvent such as benzene or toluene at a temperature ranging from 70-120 °C to obtain compound of formula 41 (Reaction 3d).

Alternatively, potassium carbonate may be used as a base in a suitable solvent such as DMF or THF at a temperature ranging from 50-80 °C.

Step 5

Preparation of compound of formula 9:

Compound of formula 39 can be reacted with compound of formula 41 in presence of Pd(dppf)CI2:CH2CI2 and a suitable base such as potassium carbonate, cesium carbonate or 2M Na2C03 (in water) in a suitable solvent such as DMF, dioxane, dimethoxyethane or acetone under an atmosphere of argon at temperature ranging from 50-100 °C to obtain compound of formula 9 (Reaction 3e).

Step 6

Preparation of compound of formula 10:

Compound of formula 9 can be can be hydrolysed using suitable reagent such as 1 N NaOH or 1 N LiOH in a suitable solvent such as MeOH or THF at temperature ranging from 20-35 °C to obtain compound of formula 10 (Reaction 3f).

Step 7

The carboxylic acid (compound of formula 10) may be optionally converted to its corresponding ester prodrugs by any suitable method well known in the art.

Scheme 3B: Preparation of compound of formula 1 ; wherein Y^=C 2, Y2=C(0); Xi, X2, X4 and X5 are selected from CH or CR, X3=C; L=NHC(S)NH; m=1 ; A, n, R, Ri, R2 and R9 are as defined in formula 1 ;

Scheme 3B

12

Step 1

Preparation of compound of formula 42:

Compound of formula 37 is reacted with compound of formula 8Q:

A-(CH2)n-NCS

8Q

wherein A and n are as defined in formula 1 ;

in a suitable solvent such as dichloromethane or THF at temperature ranging from 20-35 °C to obtain compound of formula 42 (Reaction 3g).

Step 2

Preparation of compound of formula 43:

Compound of formula 42 can be treated with bis(pinacolato)diboron, Pd(dppf)CI2 and Pd(dppf)CI2:CH2Cl2 in a suitable solvent such as dioxane, dimethoxyethane, DMSO or DMF at temperature ranging from 50-100 °C to obtain compound of formula 43 (Reaction 3h).

Step 3

Preparation of compound of formula 11 :

Compound of formula 43 can be reacted with compound of formula 41 (obtained in Step 4 of Scheme 3A) in presence of Pd(dppf)CI2:CH2Cl2 and a suitable base such as potassium carbonate, cesium carbonate or 2M Na2C03 (in water) in a suitable solvent such as DMF, dioxane, dimethoxyethane or acetone under an atmosphere of argon at temperature ranging from 50-100 °C to obtain compound of formula 11 (Reaction 3j).

Step 4

Preparation of compound of formula 12:

Compound of formula 11 can be can be hydrolysed using suitable reagent such as 1 N NaOH or 1 N LiOH in a suitable solvent such as MeOH or THF at temperature ranging from 20-35 °C to obtain compound of formula 12 (Reaction 3k).

Step 5

The carboxylic acid (compound of formula 12) may be optionally converted to its corresponding ester prodrugs by any suitable method well known in the art.

Scheme 3C: Preparation of compound of formula 1 ; wherein Y^CI-k, Y2=C(0); Xi, X2, X4 and X5 are selected from CH or CR, X3=C; L=*S02NH; m=1 ; A, n, R, R1 ; R2 and R9 are as defined in formula 1 ;

Scheme 3C

37 44 45

14

Step 1

Preparation of compound of formula 44:

Compound of formula 37 is reacted with compound of formula 8R:

A-(CH2)n-S02CI

8R

wherein A and n are as defined in formula 1 ;

in presence of a suitable base such as pyridine or triethylamine in a suitable solvent such as dichloromethane at temperature ranging from 20-35 °C to obtain compound of formula 44 (Reaction 3m).

Step 2

Preparation of compound of formula 45:

Compound of formula 44 can be treated with bis(pinacolato)diboron, Pd(dppf)CI2 and Pd(dppf)CI2:CH2CI2 in a suitable solvent such as dioxane, dimethoxyethane, DMSO

or DMF at temperature ranging from 50-100 °C to obtain compound of formula 45 (Reaction 3n).

Step 3

Preparation of compound of formula 13:

Compound of formula 45 can be reacted with compound of formula 41 (obtained in Step 4 of Scheme 3A) in presence of Pd(dppf)CI2:CH2Cl2 and a suitable base such as potassium carbonate, cesium carbonate or 2M Na2C03 (in water) in a suitable solvent such as DMF, dioxane, dimethoxyethane or acetone under an atmosphere of argon at temperature ranging from 50-100 °C to obtain compound of formula 13 (Reaction 3p).

Step 4

Preparation of compound of formula 14:

Compound of formula 13 can be can be hydrolysed using suitable reagent such as 1 N NaOH or 1 N LiOH in a suitable solvent such as MeOH or THF at temperature ranging from 20-35 °C to obtain compound of formula 14 (Reaction 3q).

Step 5

The carboxylic acid (compound of formula 14) may be optionally converted to its corresponding ester prodrugs by any suitable method well known in the art.

Scheme 3D: Preparation of compound of formula 1 ; wherein Y1=CH2, Y2=C(0); Xi, X2, X4 and X5 are selected from CH or CR, X3=C; L=*CONH; m=1 ; A, n, R, R1 s R2 and R9 are as defined in formula 1 ;

Scheme 3D

Step 1

Preparation of compound of formula 46:

Compound of formula 37 is reacted with compound of formula 8S:

A-(CH2)n-COCI

8S

wherein A and n are as defined in formula 1 ;

in presence of a suitable base such as pyridine in a suitable solvent such as dichloromethane or THF at temperature ranging from 20-35 °C to obtain compound of formula 46 (Reaction 3r).

Step 2

Preparation of compound of formula 47:

Compound of formula 46 can be treated with bis(pinacolato)diboron, Pd(dppf)CI2 and Pd(dppf)CI2:CH2CI2 in a suitable solvent such as dioxane, dimethoxyethane, DMSO or DMF at temperature ranging from 50-100 °C to obtain compound of formula 47 (Reaction 3s).

Step 3

Preparation of compound of formula 15:

Compound of formula 47 can be reacted with compound of formula 41 (obtained in Step 4 of Scheme 3A) in presence of Pd(dppf)CI2:CH2Cl2 and a suitable base such as potassium carbonate, cesium carbonate or 2M Na2C03 (in water) in a suitable solvent such as DMF, dioxane, dimethoxyethane or acetone under an atmosphere of argon at temperature ranging from 50-100 °C to obtain compound of formula 15 (Reaction 3t).

Step 4

Preparation of compound of formula 16:

Compound of formula 15 can be can be hydrolysed using suitable reagent such as 1 N NaOH or 1 N LiOH in a suitable solvent such as MeOH or THF at temperature ranging from 20-35 °C to obtain compound of formula 16 (Reaction 3u).

Step 5

The carboxylic acid (compound of formula 16) may be optionally converted to its corresponding ester prodrugs by any suitable method well known in the art.

Scheme 3E: Preparation of compound of formula 1 ; wherein Y†=CH2, Y2=C(0); Xi, X2, X4 and X5 are selected from CH or CR, X3=C; L=*NHS02; m=1 ; A, n, R, R1 s R2 and R9 are as defined in formula 1 ;

Scheme 3E

Step 1

Preparation of compound of formula 48:

Compound of formula 37 can be treated with NaN02 and concentrated HCI to form a diazonium salt, which is treated with acetic acid saturated with S02 gas, followed by treatment with CuCI2 at a temperature ranging from 0-35 °C to obtain compound of formula 48 (Reaction 3v).

Step 2

Preparation of compound of formula 49:

The preparation involves two steps.

i) Preparation of compound of formula 48A wherein Xi, X2, X4 and X5 are selected from CH or CR, X3=C; A, n and R are as defined in formula 1 :

48A

Compound of formula 48 can be treated with compound of formula 8T:

A-(CH2)n-NH2

8T

wherein A and n are as defined in formula 1 ;

in a suitable solvent such as dichloromethane and a base such as pyridine at temperature ranging from 20-35 °C to obtain compound of formula 48A.

ii) Preparation of compound of formula 49:

Compound of formula 48A can be treated with bis(pinacolato)diboron, Pd(dppf)CI2 and Pd(dppf)CI2:CH2Cl2 in a suitable solvent such as dioxane, dimethoxyethane, DMSO or DMF at temperature ranging from 50-100 °C to obtain compound of formula 49 (Reaction 3w).

Step 3

Preparation of compound of formula 18:

Compound of formula 49 can be reacted with compound of formula 41 (obtained in Step 4 of Scheme 3A) in presence of Pd(dppf)CI2:CH2CI2 and a suitable base such as potassium carbonate, cesium carbonate or 2M Na2C03 (in water) in a suitable solvent such as DMF, dioxane, dimethoxyethane or acetone under an atmosphere of argon at temperature ranging from 50-100 °C to obtain compound of formula 18 (Reaction 3x).

Step 4

Preparation of compound of formula 19:

Compound of formula 18 can be can be hydrolysed using suitable reagent such as 1 N NaOH or 1 N LiOH in a suitable solvent such as MeOH or THF at temperature ranging from 20-35 °C to obtain compound of formula 19 (Reaction 3y).

Step 5

The carboxylic acid (compound of formula 19) may be optionally converted to its corresponding ester prodrugs by any suitable method well known in the art.

Scheme 4A: Preparation of compound of formula 1 ; wherein Y^CiO), Y2=CH2; Xi, X2, X4 and X5 are selected from CH or CR, X3=C; L=NHC(0)NH; m=1 ; A, n, R, Ri, R2 and R9 are as defined in formula 1 ;

Scheme 4A

Step 1

Preparation of compound of formula 50:

Compound of formula 21 can be refluxed with N-bromosuccinimide and a catalytic amount of AIBN or benzoyl peroxide in a suitable solvent such as CCI4 using irradiation (200 watt bulb) at a temperature ranging from 80-100 °C to obtain compound of formula 50 (Reaction 4a).

Step 2

Preparation of compound of formula 51 :

Compound of formula 50 can be treated with compound of formula 6P:

6P (HCI salt)

wherein Ri and R2 are as defined in formula 1 ;

in presence of a suitable base such as triethylamine in a suitable solvent such as benzene or toluene at a temperature ranging from 70-120 °C to obtain compound of formula 51 (Reaction 4b).

Alternatively, potassium carbonate may be used as a base in a suitable solvent such as DMF or THF at a temperature ranging from 50-80 °C.

Step 3

Preparation of compound of formula 26:

Compound of formula 51 can be reacted with compound of formula 39 in presence of Pd(dppf)CI2:CH2Cl2 in a suitable base such as potassium carbonate, cesium carbonate or 2M Na2C03 (in water) in a suitable solvent such as DMF, dioxane, dimethoxyethane or acetone under an atmosphere of argon at temperature ranging from 50-100 °C to obtain compound of formula 26 (Reaction 4c).

Step 4

Preparation of compound of formula 27:

Compound of formula 26 can be can be hydrolysed using suitable reagent such as 1 N NaOH or 1 N LiOH in a suitable solvent such as MeOH or THF at temperature ranging from 20-35 °C to obtain compound of formula 27 (Reaction 4d).

Step 5

The carboxylic acid (compound of formula 27) may be optionally converted to its corresponding ester prodrugs by any suitable method well known in the art.

Scheme 4B: Preparation of compound of formula 1 ; wherein Y†=C(0), Y2=CH2; Xi, X2, X4 and X5 are selected from CH or CR, X3=C; L=NHC(S)NH; m=1 ; A, n, R, Ri, R2 and R9 are as defined in formula 1 ;

Scheme 4B

29 28

Step 1

Preparation of compound of formula 28:

Compound of formula 51 can be reacted with compound of formula 43 in presence of Pd(dppf)CI2:CH2Cl2 in a suitable base such as potassium carbonate, cesium carbonate or 2M Na2C03 (in water) in a suitable solvent such as DMF, dioxane, dimethoxyethane or acetone under an atmosphere of argon at temperature ranging from 50-100 °C to obtain compound of formula 28 (Reaction 4e).

Step 2

Preparation of compound of formula 29:

Compound of formula 28 can be can be hydrolysed using suitable reagent such as 1 N NaOH or 1 N LiOH in a suitable solvent such as MeOH or THF at temperature ranging from 20-35 °C to obtain compound of formula 29 (Reaction 4f).

Step 3

The carboxylic acid (compound of formula 29) may be optionally converted to its corresponding ester prodrugs by any suitable method well known in the art.

Scheme 4C: Preparation of compound of formula 1 ; wherein Y^C^O), Y2=CH2; Xi, X2, X4 and X5 are selected from CH or CR, X3=C; L=*S02NH; m=1 ; A, n, R1 s R2 and R9 are as defined in formula 1 ;

Scheme 4C

31 30

Step 1

Preparation of compound of formula 30:

Compound of formula 51 can be reacted with compound of formula 45 in presence of Pd(dppf)CI2:CH2CI2 in a suitable base such as potassium carbonate, cesium carbonate or 2M Na2C03 (in water) in a suitable solvent such as DMF, dioxane, dimethoxyethane or acetone under an atmosphere of argon at temperature ranging from 50-100 °C to obtain compound of formula 30 (Reaction 4g).

Step 2

Preparation of compound of formula 31 :

Compound of formula 30 can be can be hydrolysed using suitable reagent such as 1 N NaOH or 1 N LiOH in a suitable solvent such as MeOH or THF at temperature ranging from 20-35 °C to obtain compound of formula 31 (Reaction 4h).

Step 3

The carboxylic acid (compound of formula 31 ) may be optionally converted to its corresponding ester prodrugs by any suitable method well known in the art.

Scheme 4D: Preparation of compound of formula 1 ; wherein Y^C^O), Y2=CH2; Xi, X2, X4 and X5 are selected from CH or CR, X3=C; L=*CONH; m=1 ; A, n, R, R15 R2 and R9 are as defined in formula 1 ;

Scheme 4D

Step 1

Preparation of compound of formula 32:

Compound of formula 51 can be reacted with compound of formula 47 in presence of Pd(dppf)CI2:CH2Cl2 in a suitable base such as potassium carbonate, cesium carbonate or 2M Na2C03 (in water) in a suitable solvent such as DMF, dioxane, dimethoxyethane or acetone under an atmosphere of argon at temperature ranging from 50-100 °C to obtain compound of formula 32 (Reaction 4j).

Step 2

Preparation of compound of formula 33:

Compound of formula 32 can be can be hydrolysed using suitable reagent such as 1 N NaOH or 1 N LiOH in a suitable solvent such as MeOH or THF at temperature ranging from 20-35 °C to obtain compound of formula 33 (Reaction 4k).

Step 3

The carboxylic acid (compound of formula 33) may be optionally converted to its corresponding ester prodrugs by any suitable method well known in the art.

Scheme 4E: Preparation of compound of formula 1 ; wherein Y^=C{0), Y2=CH2; Xi, X2, X4 and X5 are selected from CH or CR, X3=C; L=*NHS02; m=1 ; A, n, R, R1 s R2 and R9 are as defined in formula 1 ;

Scheme 4E

Step 1

Preparation of compound of formula 35:

Compound of formula 51 can be reacted with compound of formula 49 in presence of Pd(dppf)CI2:CH2Cl2 in a suitable base such as potassium carbonate, cesium carbonate or 2M Na2C03 (in water) in a suitable solvent such as DMF, dioxane, dimethoxyethane or acetone under an atmosphere of argon at temperature ranging from 50-100 °C to obtain compound of formula 35 (Reaction 4m).

Step 2

Preparation of compound of formula 36:

Compound of formula 35 can be can be hydrolysed using suitable reagent such as 1 N NaOH or 1 N LiOH in a suitable solvent such as MeOH or THF at temperature ranging from 20-35 °C to obtain compound of formula 36 (Reaction 4n).

Step 3

The carboxylic acid (compound of formula 36) may be optionally converted to its corresponding ester prodrugs by any suitable method well known in the art.

Scheme 5A: Preparation of compound of formula 1 ; wherein CH2, Y2=C Xi, X2, X4 and X5 are independently selected from CH, CR and N, X L=NHC(0)NH; m=1 ; A, n, R, Ri, R2 and R9 are as defined in formula 1 ;

Scheme 5A

Preparation of compound of formula 52:

Compound of formula 41 can be treated with bis(pinacolato)diboron, Pd(dppf)CI2 and Pd(dppf)CI2:CH2Cl2 in a suitable solvent such as dioxane, dimethoxyethane, DMSO or DMF at temperature ranging from 50-100 °C to obtain compound of formula 52 (Reaction 5a).

Step 2

Preparation of compound of formula 54:

Compound of formula 52 can be treated with commercially available compound of formula 53 in presence of Pd(dppf)CI2:CH2Cl2 in a suitable base such as potassium carbonate, cesium carbonate or 2M Na2C03 (in water) in a suitable solvent such as DMF, dioxane, dimethoxyethane or acetone under an atmosphere of argon at

temperature ranging from 50-100 °C to obtain compound of formula 54 (Reaction 5b).

Step 3

Preparation of compound of formula 55:

Compound of formula 54 can be reduced using a suitable reducing agent such as Fe and ammonium chloride in a suitable solvent such as aqueous EtOH or EtOH: THF: H20 at a temperature ranging from 70-100 °C to obtain compound of formula 55 (Reaction 5c).

Alternatively, other reducing agents such as Fe and HCI in solvent such as H20 or ethanol or combination thereof, SnCI2 in solvent such as ethyl acetate, hydrogen over Raney Ni, Pd/C or Pt/C catalyst in solvent such as methanol (pressure ranging from 50-80 psi and temperature ranging from 20-65 °C) or cobalt chloride and zinc in a solvent such as DMF or water (temperature ranging from 20-100 °C) may be used.

Step 4

Preparation of compound of formula 56:

Compound of formula 55 can be treated with compound of formula 8P:

A-(CH2)n-NCO

8P

wherein A and n are as defined in formula 1 ;

in a suitable solvent such as dichloromethane or THF at temperature ranging from 20-35 °C to obtain compound of formula 56 (Reaction 5d).

Step 5

Preparation of compound of formula 57:

Compound of formula 56 can be hydrolysed using suitable reagent such as 1 N NaOH or 1 N LiOH in a suitable solvent such as MeOH or THF at temperature ranging from 20-35 °C to obtain compound of formula 57 (Reaction 5e).

Step 6

The carboxylic acid (compound of formula 57) may be optionally converted to its corresponding ester prodrugs by any suitable method well known in the art.

Scheme 5B: Preparation of compound of formula 1 ; wherein CH2, Y2=C(0); Xi, X2, X4 and X5 are independently selected from CH, CR and N, X3=C; L=-NHC(S)NH; m=1 ; A, n, R, Ri, R2 and R9 are as defined in formula 1 ;

Scheme 5B

Step 1

Preparation of compound of formula 58:

Compound of formula 55 (as obtained in Step 3 of Scheme 5A) can be treated with compound of formula 8Q:

A-(CH2)n-NCS

8Q

wherein A and n are as defined in formula 1 ;

in presence of a suitable solvent such as THF or dichloromethane at temperature ranging from 20-35 °C to obtain compound of formula 58 (Reaction 5f).

Step 2

Preparation of compound of formula 59:

Compound of formula 58 can be hydrolysed using suitable reagent such as 1 N LiOH or 1 N NaOH in a suitable solvent such as MeOH or THF at temperature ranging from 20-35 °C to obtain compound of formula 59 (Reaction 5g).

Step 3

The carboxylic acid (compound of formula 59) may be optionally converted to its corresponding ester prodrugs by any suitable method well known in the art.

Scheme 5C: Preparation of compound of formula 1 ; wherein CH2, Y2=C Xi, X2, X4 and X5 are independently selected from CH, CR and N, X L=*S02NH; m=1 ; A, n, R, Ri, R2 and R9 are as defined in formula 1 ;

Scheme 5C

5j

Step 1

Preparation of compound of formula 60:

Compound of formula 55 (as obtained in Step 3 of Scheme 5A) can be treated with compound of formula 8R:

A-(CH2)n-S02CI

8R

wherein A and n are as defined in formula 1 ;

in presence of a suitable base such as pyridine or triethylamine in a suitable solvent such as dichloromethane at temperature ranging from 20-35 °C to obtain compound of formula 60 (Reaction 5h).

Step 2

Preparation of compound of formula 61 :

Compound of formula 60 can be hydrolysed using suitable reagent such as 1 N LiOH or 1 N NaOH in a suitable solvent such as MeOH or THF at temperature ranging from 20-35 °C to obtain compound of formula 61 (Reaction 5j).

Step 3

The carboxylic acid (compound of formula 61 ) may be optionally converted to its corresponding ester prodrugs by any suitable method well known in the art.

Scheme 5D: Preparation of compound of formula 1 ; wherein CH2, Y2=C(0); Xi, X2, X4 and X5 are independently selected from CH, CR and N, X3=C; L=*CONH; m=1 ; A, n, R, Ri, R2 and R9 are as defined in formula 1 ;

Scheme 5D

Step 1

Preparation of compound of formula 62:

Compound of formula 55 (as obtained in Step 3 of Scheme 5A) can be treated with compound of formula 8S:

A-(CH2)n-COCI

8S

wherein A and n are as defined in formula 1 ;

in presence of a suitable base such as pyridine in a suitable solvent such as dichloromethane or THF at temperature ranging from 20-35 °C to obtain compound of formula 62 (Reaction 5k).

Step 2

Preparation of compound of formula 63:

Compound of formula 62 can be hydrolysed using suitable reagent such as 1 N LiOH or 1 N NaOH in a suitable solvent such as MeOH or THF at temperature ranging from 20-35 °C to obtain compound of formula 63 (Reaction 5m).

Step 3

The carboxylic acid (compound of formula 63) may be optionally converted to its corresponding ester prodrugs by any suitable method well known in the art.

Scheme 5E: Preparation of compound of formula 1 ; wherein CH2, Y2=C(0); Xi, X2, X4 and X5 are independently selected from CH, CR and N, X3=C; L=*NHS02; m=1 ; A, n, R, Ri, R2 and R9 are as defined in formula 1 ;

Scheme 5E

Step 1

Preparation of compound of formula 64:

Compound of formula 55 (obtained in Step 3 of Scheme 5A) can be treated with NaN02 and concentrated HCI to form a diazonium salt, which is treated with acetic acid saturated with S02 gas, followed by treatment with CuCI2 at a temperature ranging from 0-35 °C to obtain compound of formula 64 (Reaction 5n).

Step 2

Preparation of compound of formula 65:

Compound of formula 64 can be treated with compound of formula 8T:

A-(CH2)n-NH2

8T

wherein A and n are as defined in formula 1 ;

in a suitable solvent such as dichloromethane and a base such as pyridine at temperature ranging from 20-35 °C to obtain compound of formula 65 (Reaction 5p).

Step 3

Preparation of compound of formula 66:

Compound of formula 65 can be hydrolysed using suitable reagent such as 1 N LiOH or 1 N NaOH in a suitable solvent such as MeOH or THF at temperature ranging from 20-35 °C to obtain compound of formula 66 (Reaction 5q).

Step 4

The carboxylic acid (compound of formula 66) may be optionally converted to its corresponding ester prodrugs by any suitable method well known in the art.

Scheme 6A: Preparation of compound of formula 1 ; wherein Y^=C{0), Y2=CH2; Xi, X2, X4 and X5 are independently selected from CH, CR and N, X3=C; L=NHC(0)NH; m=1 ; A, n, R, Ri, R2 and R9 are as defined in formula 1 ;

Scheme 6A

Step 1

Preparation of compound of formula 67:

Compound of formula 51 can be treated with bis(pinacolato)diboron, Pd(dppf)CI2 and Pd(dppf)CI2:CH2Cl2 in a suitable solvent such as dioxane, dimethoxyethane, DMSO or DMF at temperature ranging from 50-100 °C to obtain compound of formula 67 (Reaction 6a).

Step 2

Preparation of compound of formula 68:

Compound of formula 67 can be treated with compound of formula 53 in presence of Pd(dppf)CI2:CH2Cl2 in a suitable base such as potassium carbonate, cesium carbonate or 2M Na2C03 (in water) in a suitable solvent such as DMF, dioxane, dimethoxyethane or acetone under an atmosphere of argon at temperature ranging from 50-100 °C to obtain compound of formula 68 (Reaction 6b).

Step 3

Preparation of compound of formula 69:

Compound of formula 68 can be reduced using a suitable reducing agent such as Fe and ammonium chloride in a suitable solvent such as aqueous EtOH or EtOH: THF: H20 at a temperature ranging from 70-100 °C to obtain compound of formula 69 (Reaction 6c).

Alternatively, other reducing agents such as Fe and HCI in solvent such as H20 or ethanol or combination thereof; SnCI2 in solvent such as ethyl acetate; hydrogen over Raney Ni, Pd/C or Pt/C catalyst in solvent such as methanol (pressure ranging from 50-80 psi and temperature ranging from 20-65 °C); or cobalt chloride and zinc in a solvent such as DMF or water (temperature ranging from 20-100 °C) may be used.

Step 4

Preparation of compound of formula 70:

Compound of formula 69 can be treated with compound of formula 8P:

A-(CH2)n-NCO

8P

wherein A and n are as defined in formula 1 ;

in a suitable solvent such as dichloromethane or THF at temperature ranging from 20-35 °C to obtain compound of formula 70 (Reaction 6d).

Step 5

Preparation of compound of formula 71 :

Compound of formula 70 can be hydrolysed using suitable reagent such as 1 N NaOH or 1 N LiOH in a suitable solvent such as MeOH or THF at temperature ranging from 20-35 °C to obtain compound of formula 71 (Reaction 6e).

Step 6

The carboxylic acid (compound of formula 71 ) may be optionally converted to its corresponding ester prodrugs by any suitable method well known in the art.

Scheme 6B: Preparation of compound of formula 1 ; wherein C(O), Y2=CH2; Xi, X2, X4 and X5 are independently selected from CH, CR and N, X3=C; L=NHC(S)NH; m=1 ; A, n, R, Ri, R2 and R9 are as defined in formula 1 ;

Scheme 6B

Step 1

Preparation of compound of formula 72:

Compound of formula 69 (obtained in Step 3 of Scheme 6A) can be treated with compound of formula 8Q:

A-(CH2)n-NCS

8Q

wherein A and n are as defined in formula 1 ;

in presence of a suitable solvent such as THF or dichloromethane at temperature ranging from 20-35 °C to obtain compound of formula 72 (Reaction 5f).

Step 2

Preparation of compound of formula 73:

Compound of formula 72 can be hydrolysed using suitable reagent such as 1 N LiOH or 1 N NaOH in a suitable solvent such as MeOH or THF at temperature ranging from 20-35 °C to obtain compound of formula 73 (Reaction 5g).

Step 3

The carboxylic acid (compound of formula 73) may be optionally converted to its corresponding ester prodrugs by any suitable method well known in the art.

Scheme 6C: Preparation of compound of formula 1 ; wherein C(O), Y2=CH2; Xi, X2, X4 and X5 are independently selected from CH, CR and N, X3=C; L=-*S02NH; m=1 ; A, n, Ri, R2 and R9 are as defined in formula 1 ;

Scheme 6C

Step 1

Preparation of compound of formula 74:

Compound of formula 69 (obtained in Step 3 of Scheme 6A) can be treated with compound of formula 8R:

A-(CH2)n-S02CI

8R

wherein A and n are as defined in formula 1 ;

in presence of a suitable base such as pyridine or triethylamine in a suitable solvent such as dichloromethane at temperature ranging from 20-35 °C to obtain compound of formula 74 (Reaction 6h).

Step 2

Preparation of compound of formula 75:

Compound of formula 74 can be hydrolysed using suitable reagent such as 1 N LiOH or 1 N NaOH in a suitable solvent such as MeOH or THF at temperature ranging from 20-35 °C to obtain compound of formula 75 (Reaction 6j).

Step 3

The carboxylic acid (compound of formula 75) may be optionally converted to its corresponding ester prodrugs by any suitable method well known in the art.

Scheme 6D: Preparation of compound of formula 1 ; wherein C(O), Y2=CH2; Xi, X2, X4 and X5 are independently selected from CH, CR and N, X3=C; L=*CONH; m=1 ; A, n, R, Ri, R2 and R9 are as defined in formula 1 ;

Scheme 6D

Step 1

Preparation of compound of formula 76:

Compound of formula 69 (obtained in Step 3 of Scheme 6A) can be treated with compound of formula 8S:

A-(CH2)n-COCI

8S

wherein A and n are as defined in formula 1 ;

in presence of a suitable base such as pyridine in a suitable solvent such as dichloromethane or THF at temperature ranging from 20-35 °C to obtain compound of formula 76 (Reaction 5k).

Step 2

Preparation of compound of formula 77:

Compound of formula 76 can be hydrolysed using suitable reagent such as 1 N LiOH or 1 N NaOH in a suitable solvent such as MeOH or THF at temperature ranging from 20-35 °C to obtain compound of formula 77 (Reaction 5m).

Step 3

The carboxylic acid (compound of formula 77) may be optionally converted to its corresponding ester prodrugs by any suitable method well known in the art.

Scheme 6E: Preparation of compound of formula 1 ; wherein C(O), Y2=CH2; Xi, X2, X4 and X5 are independently selected from CH, CR and N, X3=C; L=*NHS02; m=1 ; A, n, R, Ri, R2 and R9 are as defined in formula 1 ;

Scheme 6E

Step 1

Preparation of compound of formula 78:

Compound of formula 69 (obtained in Step 3 of Scheme 6A) can be treated with NaN02 and concentrated HCI to form a diazonium salt, which is treated with acetic acid saturated with S02 gas, followed by treatment with CuCI2 at a temperature ranging from 0-35 °C to obtain compound of formula 78 (Reaction 6n).

Step 2

Preparation of compound of formula 79:

Compound of formula 78 can be treated with compound of formula 8T:

A-(CH2)n-NH2

8T

wherein A and n are as defined in formula 1 ;

in a suitable solvent such as dichloromethane and a base such as pyridine at temperature ranging from 20-35 °C to obtain compound of formula 79 (Reaction 6p).

Step 3

Preparation of compound of formula 80:

Compound of formula 79 can be hydrolysed using suitable reagent such as 1 N LiOH or 1 N NaOH in a suitable solvent such as MeOH or THF at temperature ranging from 20-35 °C to obtain compound of formula 80 (Reaction 6q).

Step 4

The carboxylic acid (compound of formula 80) may be optionally converted to its corresponding ester prodrugs by any suitable method well known in the art.

Scheme 7A: Preparation of compound of formula 1 ; wherein Y†=C(0), Y2=C Xi, X2, X4 and X5 are independently selected from CH and CR, X: L=NHC(0)NH; m=1 ; A, n, R, Ri, R2 and R9 are as defined in formula 1 ;

Scheme 7A

Step 1

Preparation of compound of formula 82:

Commercially available compound of formula 81 can be treated with compound of formula 6P:

6P (HCI salt)

wherein Ri and R2 are as defined in formula 1 ;

in presence of a suitable base such as triethylamine in a suitable solvent such as benzene or toluene at a temperature ranging from 70-120 °C to obtain compound of formula 82 (Reaction 7a).

Alternatively, potassium carbonate may be used as a base in a suitable solvent such as DMF or THF at a temperature ranging from 50-80 °C.

Step 2

Preparation of compound of formula 83:

Compound of formula 82 can be treated with compound of formula 21 B:

21 B

wherein Xi , X2, X4 and X5 are selected from CH and CR; R is as defined in formula 1 ; in presence of a catalyst such as Pd(dppf)CI2:CH2Cl2 and a base such as potassium carbonate, cesium carbonate or 2M Na2C03 (in water) in a suitable solvent such as DMF, dioxane, dimethoxyethane or acetone at a temperature ranging from 70-120 °C under an atmosphere of argon, to obtain compound of formula 83 (Reaction 7b). Alternatively, compound of formu with compound of formula 21 A:

in presence of bis(pinacolo)diboron (to form compound of formula 21 B in situ) with a suitable catalyst such as palladium acetate or tetrakis palladium and a suitable base such as potassium acetate, sodium carbonate and cesium carbonate in a solvent such as toluene, dioxane, dimethoxyethane, DMF or acetone at a temperature ranging from 70-120 °C to obtain compound of formula 83.

Step 3

Preparation of compound of formula 84:

Compound of formula 83 can be reduced using a suitable reducing agent such as Fe and ammonium chloride in a suitable solvent such as aqueous EtOH or EtOH: THF:

H20 at a temperature ranging from 70-100 °C to obtain compound of formula 84 (Reaction 7c).

Alternatively, other reducing agents such as Fe and HCI in solvent such as H20 or ethanol or combination thereof; SnCI2 in solvent such as ethyl acetate; hydrogen over Raney Ni, Pd/C or Pt/C catalyst in solvent such as methanol (pressure ranging from 50-80 psi and temperature ranging from 20-65 °C); or cobalt chloride and zinc in a solvent such as DMF or water (temperature ranging from 20-100 °C) may be used.

Step 4

Preparation of compound of formula 85:

Compound of formula 84 can be treated with compound of formula 8P:

A-(CH2)n-NCO

8P

wherein A and n are as defined in formula 1 ;

in a suitable solvent such as dichloromethane or THF at temperature ranging from 20-35 °C to obtain compound of formula 85 (Reaction 7d).

Step 5

Preparation of compound of formula 86:

Compound of formula 85 can be hydrolysed using suitable reagent such as 1 N NaOH or 1 N LiOH in a suitable solvent such as MeOH or THF at temperature ranging from 20-35 °C to obtain compound of formula 86 (Reaction 7e).

Step 6

The carboxylic acid (compound of formula 86) may be optionally converted to its corresponding ester prodrugs by any suitable method well known in the art.

Scheme 7B: Preparation of compound of formula 1 ; wherein Y†=C(0), Y2=C Xi, X2, X4 and X5 are independently selected from CH and CR, X: L=NHC(S)NH; m=1 ; A, n, R, Ri, R2 and R9 are as defined in formula 1 ;

Scheme 7B

Step 1

Preparation of compound of formula 87:

Compound of formula 84 (obtained in Step 3 of Scheme 7A) can be treated with compound of formula 8Q:

A-(CH2)n-NCS

8Q

wherein A and n are as defined in formula 1 ;

in presence of a suitable solvent such as THF or dichloromethane at temperature ranging from 20-35 °C to obtain compound of formula 87 (Reaction 7f).

Step 2

Preparation of compound of formula 88:

Compound of formula 87 can be hydrolysed using suitable reagent such as 1 N LiOH or 1 N NaOH in a suitable solvent such as MeOH or THF at temperature ranging from 20-35 °C to obtain compound of formula 88 (Reaction 7g).

Step 3

The carboxylic acid (compound of formula 88) may be optionally converted to its corresponding ester prodrugs by any suitable method well known in the art.

Scheme 7C: Preparation of compound of formula 1 ; wherein Y^=C{0), Y2=C(0); Xi, X2, X4 and X5 are independently selected from CH and CR, X3=C; L=*S02NH; m=1 ; A, n, R, Ri, R2 and R9 are as defined in formula 1 ;

Scheme 7C

Step 1

Preparation of compound of formula 89:

Compound of formula 84 (obtained in Step 3 of Scheme 7A) can be treated with compound of formula 8R:

A-(CH2)n-S02CI

8R

wherein A and n are as defined in formula 1 ;

in presence of a suitable base such as pyridine or triethylamine in a suitable solvent such as dichloromethane at temperature ranging from 20-35 °C to obtain compound of formula 89 (Reaction 7h).

Step 2

Preparation of compound of formula 90:

Compound of formula 89 can be hydrolysed using suitable reagent such as 1 N LiOH or 1 N NaOH in a suitable solvent such as MeOH or THF at temperature ranging from 20-35 °C to obtain compound of formula 90 (Reaction 7j).

Step 3

The carboxylic acid (compound of formula 90) may be optionally converted to its corresponding ester prodrugs by any suitable method well known in the art.

Scheme 7D: Preparation of compound of formula 1 ; wherein Y^C^O), Y2=C(0); Xi, X2, X4 and X5 are independently selected from CH and CR, X3=C; L=*CONH; A, n, R, Ri, R2 and R9 are as defined in formula 1 ;

Scheme 7D

Step 1

Preparation of compound of formula 91 :

Compound of formula 84 (obtained in Step 3 of Scheme 7A) can be treated with compound of formula 8S:

A-(CH2)n-COCI

8S

wherein A and n are as defined in formula 1 ;

in presence of a suitable base such as pyridine in a suitable solvent such as dichloromethane or THF at temperature ranging from 20-35 °C to obtain compound of formula 91 (Reaction 7k).

Step 2

Preparation of compound of formula 92:

Compound of formula 91 can be hydrolysed using suitable reagent such as 1 N LiOH or 1 N NaOH in a suitable solvent such as MeOH or THF at temperature ranging from 20-35 °C to obtain compound of formula 92 (Reaction 7m).

Step 3

The carboxylic acid (compound of formula 92) may be optionally converted to its corresponding ester prodrugs by any suitable method well known in the art.

Scheme 7E: Preparation of compound of formula 1 ; wherein Y =C(0), Y2=C(0); Xi, X2, X4 and X5 are independently selected from CH and CR, X3=C; L=*NHS02; m=1 ; A, n, R, Ri, R2 and R9 are as defined in formula 1 ;

Scheme 7E

Step 1

Preparation of compound of formula 93:

Compound of formula 84 (obtained in Step 3 of Scheme 7A) can be treated with NaN02 and concentrated HCI to form a diazonium salt, which is treated with acetic acid saturated with S02 gas, followed by treatment with CuCI2 at a temperature ranging from 0-35 °C to obtain compound of formula 93 (Reaction 7n).

Step 2

Preparation of compound of formula 94:

Compound of formula 93 can be treated with compound of formula 8T:

A-(CH2)n-NH2

8T

wherein A and n are as defined in formula 1 ;

in a suitable solvent such as dichloromethane and a base such as pyridine at temperature ranging from 20-35 °C to obtain compound of formula 94 (Reaction 7p).

Step 3

Preparation of compound of formula 95:

Compound of formula 94 can be hydrolysed using suitable reagent such as 1 N LiOH or 1 N NaOH in a suitable solvent such as MeOH or THF at temperature ranging from 20-35 °C to obtain compound of formula 95 (Reaction 7q).

Step 4

The carboxylic acid (compound of formula 95) may be optionally converted to its corresponding ester prodrugs by any suitable method well known in the art.

Scheme 8A: Preparation of compound of formula 1 ; wherein
Y2= CH2; Xi, X2, X4 and X5 are independently selected from CH and CR, X3=C; L=NHC(0)NH; m=1 ; A, n, R, R15 R2 and R9 are as defined in formula 1 ;

Scheme 8A

Step 1

Commercially available compound of formula 96 can be treated with LiAIH4 in a suitable solvent such as THF or diethyl ether at the temperature ranging from 0-70 °C to obtain compound of formula 97.

Alternatively, commercially available compound of formula 81 can be treated with LiAIH4 in a suitable solvent such as THF or diethyl ether at the temperature ranging from 0-70 °C to obtain compound of formula 97.

Step 2

Compound of formula 97 can be treated with N-bromosuccinimide in dichloromethane or PBr3 in diethyl ether at temperature ranging from 0-35 °C to obtain compound of formula 98.

Step 3

Preparation of compound of formula 99:

Compound of formula 98 can be treated with compound of formula 6P:

6P (HCI salt)

wherein Ri and R2 are as defined in formula 1 ;

in presence of a suitable base such as triethylamine in a suitable solvent such as benzene or toluene at a temperature ranging from 70-120 °C to obtain compound of formula 99 (Reaction 8c).

Alternatively, potassium carbonate may be used as a base in a suitable solvent such as DMF or THF at a temperature ranging from 50-80 °C.

Step 4

Preparation of compound of formula 100:

Compound of formula 99 can be treated with compound of formula 21 B:

21 B

wherein Xi, X2, X4 and X5 are selected from CH and CR, R is as defined in formula 1 ;

in presence of a catalyst such as Pd(dppf)CI2:CH2Cl2 and a base such as potassium carbonate, cesium carbonate or 2M Na2C03 (in water) in a suitable solvent such as DMF, dioxane, dimethoxyethane or acetone at a temperature ranging from 70-120 °C under an atmosphere of argon, to obtain compound of formula 100 (Reaction 8d).

Alternatively, compound of formula 99 can be treated with compound of formula 21 A:

21 A

in presence of bis(pinacolo)diboron with a suitable catalyst such as palladium acetate or tetrakis palladium and a suitable base such as potassium acetate, sodium carbonate and cesium carbonate in a solvent such as toluene, dioxane, dimethoxyethane, DMF or acetone at a temperature ranging from 70-120 °C to obtain compound of formula 100.

Step 5

Preparation of compound of formula 101 :

Compound of formula 100 can be reduced using a suitable reducing agent such as Fe and ammonium chloride in a suitable solvent such as aqueous EtOH or EtOH: THF: H20 at a temperature ranging from 70-100 °C to obtain compound of formula 101 (Reaction 8e).

Alternatively, other reducing agents such as Fe and HCI in solvent such as H20 or ethanol or combination thereof; SnCI2 in solvent such as ethyl acetate; hydrogen over Raney Ni, Pd/C or Pt/C catalyst in solvent such as methanol (pressure ranging from 50-80 psi and temperature ranging from 20-65 °C); or cobalt chloride and zinc in a solvent such as DMF or water (temperature ranging from 20-100 °C) may be used.

Step 6

Preparation of compound of formula 102:

Compound of formula 101 can be treated with compound of formula 8P:

A-(CH2)n-NCO

8P

Where in A and n are as defined in formula 1 ;

in a suitable solvent such as dichloromethane or THF at temperature ranging from 20-35 °C to obtain compound of formula 102 (Reaction 8f).

Step 7

Preparation of compound of formula 103:

Compound of formula 102 can be hydrolysed using suitable reagent such as 1 N NaOH or 1 N LiOH in a suitable solvent such as MeOH or THF at temperature ranging from 20-35 °C to obtain compound of formula 103 (Reaction 8g).

Step 8

The carboxylic acid (compound of formula 103) may be optionally converted to its corresponding ester prodrugs by any suitable method well known in the art.

Scheme 8B: Preparation of compound of formula 1 ; wherein Y^=C 2, Y2= CH2; Xi, X2, X4 and X5 are independently selected from CH and CR, X3=C; L=NHC(S)NH; m=1 ; A, n, R, Ri, R2 and R9 are as defined in formula 1 ;

Scheme 8B

Step 1

Preparation of compound of formula 104:

Compound of formula 101 (obtained in Step 5 of Scheme 8A) can be treated with compound of formula 8Q:

A-(CH2)n-NCS

8Q

wherein A and n are as defined in formula 1 ;

in presence of a suitable solvent such as THF or dichloromethane at temperature ranging from 20-35 °C to obtain compound of formula 104 (Reaction 8h).

Step 2

Preparation of compound of formula 105:

Compound of formula 104 can be hydrolysed using suitable reagent such as 1 N LiOH or 1 N NaOH in a suitable solvent such as MeOH or THF at temperature ranging from 20-35 °C to obtain compound of formula 105 (Reaction 8j).

Step 3

The carboxylic acid (compound of formula 105) may be optionally converted to its corresponding ester prodrugs by any suitable method well known in the art.

Scheme 8C: Preparation of compound of formula 1 ; wherein Y^=C 2, Y2= CH2; Xi, X2, X4 and X5 are independently selected from CH and CR, X3=C; L=*S02NH; m=1 ; A, n, R, Ri, R2 and R9 are as defined in formula 1 ;

Scheme 8C

Step 1

Preparation of compound of formula 106:

Compound of formula 101 (obtained in Step 5 of Scheme 8A) can be treated with compound of formula 8R:

A-(CH2)n-S02CI

8R

wherein A and n are as defined in formula 1 ;

in presence of a suitable base such as pyridine or triethylamine in a suitable solvent such as dichloromethane at temperature ranging from 20-35 °C to obtain compound of formula 106 (Reaction 8k).

Step 2

Preparation of compound of formula 107:

Compound of formula 106 can be hydrolysed using suitable reagent such as 1 N LiOH or 1 N NaOH in a suitable solvent such as MeOH or THF at temperature ranging from 20-35 °C to obtain compound of formula 107 (Reaction 8m).

Step 3

The carboxylic acid (compound of formula 107) may be optionally converted to its corresponding ester prodrugs by any suitable method well known in the art.

Scheme 8D: Preparation of compound of formula 1 ; wherein Y^=C 2, Y2= CH2; Xi, X2, X4 and X5 are independently selected from CH and CR, X3=C; L=*CONH; m=1 ; A, n, R, Ri, R2 and R9 are as defined in formula 1 ;

Scheme 8D

Step 1

Preparation of compound of formula 108:

Compound of formula 101 (obtained in Step 5 of Scheme 8A) can be treated with compound of formula 8S:

A-(CH2)n-COCI

8S

wherein A and n are as defined in formula 1 ;

in presence of a suitable base such as pyridine in a suitable solvent such as dichloromethane or THF at temperature ranging from 20-35 °C to obtain compound of formula 108 (Reaction 8n).

Step 2

Preparation of compound of formula 109:

Compound of formula 108 can be hydrolysed using suitable reagent such as 1 N LiOH or 1 N NaOH in a suitable solvent such as MeOH or THF at temperature ranging from 20-35 °C to obtain compound of formula 109 (Reaction 8p).

Step 3

The carboxylic acid (compound of formula 109) may be optionally converted to its corresponding ester prodrugs by any suitable method well known in the art.

Scheme 8E: Preparation of compound of formula 1 ; wherein
Y2=CH2; Xi, X2, X4 and X5 are independently selected from CH and CR, X3=C; L=*NHS02; m=1 ; A, n, R, Ri, R2 and R9 are as defined in formula 1 ;

Scheme 8E

Step 1

Preparation of compound of formula 1 10:

Compound of formula 101 (obtained in Step 5 of Scheme 8A) can be treated with NaN02 and concentrated HCI to form a diazonium salt, which is treated with acetic acid saturated with S02 gas, followed by treatment with CuCI2 at a temperature ranging from 0-35 °C to obtain compound of formula 1 10 (Reaction 8q).

Step 2

Preparation of compound of formula 1 1 1 :

Compound of formula 1 10 can be treated with compound of formula 8T:

A-(CH2)n-NH2

8T

wherein A and n are as defined in formula 1 ;

in a suitable solvent such as dichloromethane and a base such as pyridine at temperature ranging from 20-35 °C to obtain compound of formula 111 (Reaction 8r).

Step 3

Preparation of compound of formula 112:

Compound of formula 111 can be hydrolysed using suitable reagent such as 1 N LiOH or 1 N NaOH in a suitable solvent such as MeOH or THF at temperature ranging from 20-35 °C to obtain compound of formula 112 (Reaction 8s).

Step 4

The carboxylic acid (compound of formula 112) may be optionally converted to its corresponding ester prodrugs by any suitable method well known in the art.

Scheme 9A: Preparation of compound of formula 1 b; wherein Y^CI-k, Y2= C=0; Xi, X2, X4 and X5 are independently selected from CH and CR, X3=C; L=NHCONH; m=1 -4; A, n, R and R9 are as defined in formula 1 ;

wherein Y is a cycloalk l ring selected from:

Scheme 9A

M (HCI salt)

9b

115

9d

116

Step 1

Preparation of compound of formula 113:

Compound of formula 6 can be treated with compound M:

M (HCI salt);

in presence of a suitable base such as triethylamine in a suitable solvent such as benzene or toluene at a temperature ranging from 70-120 °C to obtain compound of formula 113 (Reaction 9a).

Alternatively, potassium carbonate may be used as a base in a suitable solvent such as DMF or THF at a temperature ranging from 50-80 °C.

Step 2

Preparation of compound of formula 114:

Compound of formula 113 can be reduced using a suitable reducing agent such as Fe and ammonium chloride in a suitable solvent such as aqueous EtOH or EtOH: THF: H20 at a temperature ranging from 70-100 °C to obtain compound of formula 114 (Reaction 9b).

Alternatively, other reducing agents such as Fe and HCI in a solvent such as H20 or ethanol or combination thereof; SnCI2 in a solvent such as ethyl acetate; hydrogen over Raney Ni, Pd/C or Pt/C catalyst in a solvent such as methanol (pressure ranging from 50-80 psi and temperature ranging from 20-65 °C); or cobalt chloride and zinc in a solvent such as DMF or water (temperature ranging from 20-100 °C) may be used.

Step 3

Compound of formula 114 can be treated with compound of formula 8P:

A-(CH2)n-NCO

8P

wherein A and n are as defined in formula 1 ;

in a suitable solvent such as dichloromethane or THF at a temperature ranging from 20-35 °C to obtain compound of formula 115 (Reaction 9c).

Step 4

Preparation of compound of formula 116:

Compound of formula 115 can be hydrolysed using a suitable reagent such as 1 N LiOH or 1 N NaOH in a suitable solvent such as MeOH or THF at a temperature ranging from 20-35 °C to obtain compound of formula 116 (Reaction 9d).

Step 5

The carboxylic acid (compound of formula 116) may be optionally converted to its corresponding ester prodrugs by any suitable method well known in the art.

Scheme 9B: Preparation of compound of formula 1 b; wherein Y†=CH2, Y2= C=0; Xi, X2, X4 and X5 are independently selected from CH and CR, X3=C; L= NHC(S)NH; m=1 -4; A, n, R and R9 are as defined in formula 1 ;

Scheme 9B

8

Step 1

Preparation of compound of formula 117:

Compound of formula 114 (obtained in Step 2 of Scheme 9A) can be treated with compound of formula 8Q:

A-(CH2)n-NCS

8Q

wherein A and n are as defined in formula 1 ;

in presence of a suitable solvent such as THF or dichloromethane at temperature ranging from 20-35 °C to obtain compound of formula 117 (Reaction 9e).

Step 2

Preparation of compound of formula 118:

Compound of formula 117 can be hydrolysed using suitable reagent such as 1 N LiOH or 1 N NaOH in a suitable solvent such as MeOH or THF at temperature ranging from 20-35 °C to obtain compound of formula 118 (Reaction 9f).

Step 3

The carboxylic acid (compound of formula 118) may be optionally converted to its corresponding ester prodrugs by any suitable method well known in the art.

Scheme 9C: Preparation of compound of formula 1 b; wherein Y†=CH2, Y2= C=0; Xi, X2, X4 and X5 are independently selected from CH and CR, X3=C; L= *S02NH; m=1-4; A, n, R and R9 are as defined in formula 1 ;

Scheme 9C

Step 1

Preparation of compound of formula 119:

Compound of formula 114 (obtained in Step 2 of Scheme 9A) can be treated with compound of formula 8R:

A-(CH2)n-S02CI

8R

wherein A and n are as defined in formula 1 ;

in presence of a suitable base such as pyridine or triethylamine in a suitable solvent such as dichloromethane at temperature ranging from 20-35 °C to obtain compound of formula 119 (Reaction 9g).

Step 2

Preparation of compound of formula 120:

Compound of formula 119 can be hydrolysed using suitable reagent such as 1 N LiOH or 1 N NaOH in a suitable solvent such as MeOH or THF at temperature ranging from 20-35 °C to obtain compound of formula 120 (Reaction 9h).

Step 3

The carboxylic acid (compound of formula 120) may be optionally converted to its corresponding ester prodrugs by any suitable method well known in the art.

Scheme 9D: Preparation of compound of formula 1 b; wherein

C=0; Xi, X2, X4 and X5 are independently selected from CH and CR, X3= *CONH; m=1 -4; A, n, R and R9 are as defined in formula 1 ;

Scheme 9D

Step 1

Preparation of compound of formula 121 :

Compound of formula 114 (obtained in Step 2 of Scheme 9A) can be treated with compound of formula 8S:

A-(CH2)n-COCI

8S

wherein A and n are as defined in formula 1 ;

in presence of a suitable base such as pyridine in a suitable solvent such as dichloromethane or THF at temperature ranging from 20-35 °C to obtain compound of formula 121 (Reaction 9j).

Step 2

Preparation of compound of formula 122:

Compound of formula 121 can be hydrolysed using suitable reagent such as 1 N LiOH or 1 N NaOH in a suitable solvent such as MeOH or THF at temperature ranging from 20-35 °C to obtain compound of formula 122 (Reaction 9k).

Step 3

The carboxylic acid (compound of formula 122) may be optionally converted to its corresponding ester prodrugs by any suitable method well known in the art.

Scheme 9E: Preparation of compound of formula 1 b; wherein Y†=CH2, Y2= C=0; Xi, X2, X4 and X5 are independently selected from CH and CR, X3=C; L= *NHS02; m=1-4; A, n, R and R9 are as defined in formula 1 ;

Scheme 9E

9n

9p

Step 1

Preparation of compound of formula 123:

Compound of formula 114 (obtained in Step 2 of Scheme 9A) can be treated with NaN02 and concentrated HCI to form a diazonium salt, which is treated with acetic acid saturated with S02 gas, followed by treatment with CuCI2 at a temperature ranging from 0-35 °C to obtain compound of formula 123 (Reaction 9m).

Step 2

Preparation of compound of formula 124:

Compound of formula 123 can be treated with compound of formula 8T:

A-(CH2)n-NH2

8T

wherein A and n are as defined in formula 1 ;

in a suitable solvent such as dichloromethane and a base such as pyridine at temperature ranging from 20-35 °C to obtain compound of formula 124 (Reaction 9n).

Step 3

Preparation of compound of formula 125:

Compound of formula 124 can be hydrolysed using suitable reagent such as 1 N LiOH or 1 N NaOH in a suitable solvent such as MeOH or THF at temperature ranging from 20-35 °C to obtain compound of formula 125 (Reaction 9p).

Step 4

The carboxylic acid (compound of formula 125) may be optionally converted to its corresponding ester prodrugs by any suitable method well known in the art.

Scheme 10A: Preparation of compound of formula 1 ; wherein Y†=CH2, Y2=C(0); Xi, X2, X4 and X5 are selected from CH and CR, X3=C; L= NHC(0)NH; m=1 ; A, n, R, Ri, R2 and R9 are as defined in formula 1 ;

Scheme 10A

10

Step 1 :

Preparation of compound of formula 7

The compound of formula 41 may be treated with a reagent such as commercially available 4-nitrophenyl boronic acid (Aldrich, USA) and commercially available Pd(dppf)CI2: CH2CI2 (Aldrich, USA) in a suitable solvent such as DMF or dioxane at about 80 °C for about 3 h to obtain the compound of formula 7 (Reaction 10a).

Step 2:

Preparation of compound of formula 8

The compound of formula 8 is prepared analogous to Step 6 of Scheme 1 A (Reaction 1f).

Step 3:

Preparation of compound of formula 10

The compound of formula 10 is prepared analogous to Steps 7, 8 and 9 of Scheme 1 A (Reaction 1 g and Reaction 1 h).

In all the above mentioned schemes 1 -10, the carboxylic acids formed may be optionally converted to their pharmaceutically acceptable salts.

The present invention also includes within its scope all isotopically labeled forms of compounds of formula 1 , wherein one or more atoms of compounds of formula 1 are replaced by their respective isotopes. Examples of isotopes that may be incorporated into the compounds disclosed herein include, but are not limited to, isotopes of hydrogen such as 2H and 3H, carbon such as 11C, 13C and 14C, nitrogen such as 13N and 15N, oxygen such as 150, 170 and 180, chlorine such as 36CI, fluorine such as 18F and sulphur such as 35S.

Substitution with heavier isotopes, for example, replacing one or more key carbon-hydrogen bonds with carbon-deuterium bond may show certain therapeutic advantages, for example, longer metabolism cycles, improved safety or greater effectiveness.

Isotopically labeled forms of compounds of formula 1 , can be prepared by conventional techniques known to those skilled in the art or by processes analogous to those described above and in the subsequent section on examples by using an appropriate isotopically labeled reagent instead of non-labeled reagent.

The compounds of the present invention can also be converted into their corresponding pharmaceutically acceptable salts or solvates. The pharmaceutically acceptable salts of the compounds of the present invention are in particular salts, which can be used physiologically.

The term "pharmaceutically acceptable salts" is meant to include salts of the active compounds which are prepared with acids or bases, depending on the particular substituents found on the compounds described herein.

When compounds of the present invention contain relatively acidic functionalities, base addition salts can be obtained by contacting the neutral form of such compounds with a sufficient amount of the desired base, either neat or in a suitable inert solvent. Examples of pharmaceutically acceptable base addition salts include sodium, potassium, calcium, magnesium, ammonium or organic base salt, or a similar salt. Examples of pharmaceutically acceptable organic base addition salts include those derived from organic bases like lysine, arginine, guanidine, diethanolamine and the like.

When compounds of the present invention contain relatively basic functionalities, acid addition salts can be obtained by contacting the neutral form of such compounds with a sufficient amount of the desired acid, either neat or in a suitable inert solvent. Examples of pharmaceutically acceptable acid addition salts include those derived from inorganic acids like hydrochloric, hydrobromic, nitric, carbonic, monohydrogencarbonic, phosphoric, monohydrogenphosphoric, dihydrogenphosphoric, sulfuric, monohydrogensulfuric, hydriodic, or phosphorous acids and the like, as well as the salts derived from organic acids like acetic, propionic, isobutyric, oxalic, maleic, malonic, benzoic, succinic, suberic, fumaric, mandelic, phthalic, benzenesulfonic, p-tolylsulfonic, citric, tartaric, methanesulfonic, glucuronic or galacturonic acids and the like. Certain specific compounds of the present invention contain both basic and acidic functionalities that allow the compounds to be converted into either base or acid addition salts.

The neutral forms of the compounds may be regenerated by contacting the salt with a base or acid and isolating the parent compound in the conventional manner. The parent form of the compound differs from the various salt forms in certain physical properties. An example of physical properties that may differ is solubility in polar solvents.

Certain compounds of the present invention can exist in unsolvated forms as well as solvated forms, including hydrated forms. Certain compounds of the present invention may exist in multiple crystalline or amorphous forms. In general, all physical forms are equivalent for the uses contemplated by the present invention and are intended to be within the scope of the present invention.

Various polymorphs of compounds of formula 1 can be prepared by crystallization of the compounds under different conditions. The different conditions are, for example, using different commonly used solvents or their mixtures for crystallization; crystallization at different temperatures; various modes of cooling, ranging from very fast to very slow cooling during crystallizations. Polymorphs can also be obtained by heating or melting the compound followed by gradual or fast

cooling. The presence of polymorphs can be determined by IR (Infra-red) spectroscopy, solid probe NMR (Nuclear Magnetic Resonance) spectroscopy, differential scanning calorimetry, powder X-ray diffraction or such other techniques.

As used herein, the term "stereoisomer" is a general term used for all isomers of individual compounds that differ only in the orientation of their atoms in space. The term stereoisomer includes mirror image isomers (enantiomers), mixtures of mirror image isomers (racemates, racemic mixtures), geometric (cis/trans or E/Z) isomers, and isomers of compounds with more than one chiral center that are not mirror images of one another (diastereoisomers). The compounds of the present invention may have asymmetric centers and occur as racemates, racemic mixtures, individual diastereoisomers, or enantiomers, or may exist as geometric isomers, with all isomeric forms of said compounds being included in the present invention. When a compound of formula 1 is desired as a single enantiomer, it may be obtained either by resolution of the final product or by stereospecific synthesis from either isomerically pure starting material or any convenient intermediate. Resolution of the final product, an intermediate or a starting material may be effected by any suitable method known in the art for example Chiral reagents for Asymmetric Synthesis by Leo A. Paquette; John Wiley & Sons Ltd.

Additionally, in situations wherein tautomers of the compounds of formula 1 are possible, the present invention is intended to include all tautomeric forms of the compounds.

The present invention also envisages prodrugs of the compound of formula 1 . Prodrug derivatives of any compound of the invention are derivatives of said compounds which following administration release the parent compound in vivo via some chemical or physiological process, e.g., a prodrug on being brought to the physiological pH or through enzyme action is converted to the parent compound. The preferable prodrugs are those that are converted intracellular^, more preferably where the cellular converting location is the site of therapeutic action. For instance, preferred produgs are pharmaceutically acceptable ester derivatives convertible by solvolysis under physiological conditions to the parent carboxylic acid, e.g., lower alkyl esters, cycloalkyl esters, lower alkenyl esters, benzyl esters, mono- or di-substituted lower alkyl esters such as the pivaloyloxymethyl ester and the like conventionally used in the art (An introduction to Medicinal Chemistry, Graham. L.

Patrick, Second Edition, Oxford University Press, pg 239-248; Prodrugs: Challenges and Rewards, Part 1 and Part 2, AAPS Press, Edited by Valentino J. Stella, Renald T. Borchardt, Michael J. Hagemon, Reza Oliyai, Hans Maag, Jefferson W. Tilley).

The present invention also envisages carboxylic acid isosteres of the compound of formula 1 . The present invention further envisages N-oxide derivatives of the compound of formula 1 .

The present invention furthermore relates to pharmaceutical compositions that contain an effective amount of at least one compound of formula 1 or its physiologically tolerable salt in addition to a customary pharmaceutically acceptable carrier, and to a process for the production of a pharmaceutical composition, which includes bringing at least one compound of formula 1 , into a suitable administration form using a pharmaceutically suitable and physiologically tolerable excipient and, if appropriate, further suitable active compounds, additives or auxiliaries.

As used herein, the term "pharmaceutically acceptable carrier" refers to a material that is non-toxic, inert, solid, semi-solid or liquid filler, diluent, encapsulating material or formulation auxiliary of any type which is compatible with a subject, preferably a mammal, more preferably a human, and is suitable for delivering an active agent to the target site without terminating the activity of the agent.

The present invention also envisages the use of a compound of formula 1 or a pharmaceutically acceptable salt of the compound in combination with other pharmaceutically active compounds. For instance, a pharmaceutical composition including a compound of formula 1 or a pharmaceutically acceptable salt can be administered to a mammal, in particular a human, with any other anti-diabetic compound, in mixtures with one another or in the form of pharmaceutical preparations.

The term, "therapeutically effective amount" as used herein means an amount of compound or composition comprising compound of formula 1 , effective in producing the desired therapeutic response in a particular patient suffering from DGAT1 mediated disorders. The therapeutically effective amount of the compound or composition will vary with the particular condition being treated, the age and physical condition of the end user, the severity of the condition being treated/prevented, the duration of the treatment, the nature of concurrent therapy,

the specific compound or composition employed, the particular pharmaceutically acceptable carrier utilized, and like factors.

The term "subject" as used herein refers to an animal, preferably a mammal, and most preferably a human.

The term "mammal" used herein refers to warm-blooded vertebrate animals of the class Mammalia, including humans, characterized by a covering of hair on the skin and, in the female, milk-producing mammary glands for nourishing the young. The term mammal includes animals such as cat, dog, rabbit, bear, fox, wolf, monkey, deer, mouse, pig as well as human.

As used herein, the terms "treatment" "treat" and "therapy" and the like refer to alleviate, slow the progression, prophylaxis, attenuation or cure of existing disease (e.g., diabetes). "Prevent", as used herein, refers to delaying, slowing, inhibiting, reducing or ameliorating the onset of diseases or disorders mediated by diacylglycerol acyltransferase (DGAT), particularly DGAT1 .

In an embodiment, the compounds of the present invention are particularly useful for the delay or treatment of a range of DGAT1 mediated diseases or disorders selected from obesity, diabetes, impaired glucose tolerance, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, anorexia nervosa, bulimia, cachexia, syndrome X, insulin resistance, hypoglycemia, hyperglycemia, hyperuricemia, hyperinsulinemia, hypercholesterolemia, hyperlipidemia, dyslipidemia, mixed dyslipidemia, hypertriglyceridemia, pancreatitis, metabolic acidosis, ketosis, steatosis, dysmetabolic syndrome and nonalcoholic fatty liver disease; cardiovascular diseases, such as atherosclerosis, arteriosclerosis, acute heart failure, congestive heart failure, coronary artery disease, cardiomyopathy, myocardial ischaemia, myocardial infarction, angina pectoris, hypertension, hypotension, stroke, ischemia, ischemic reperfusion injury, aneurysm, restenosis, peripheral vascular disease and vascular stenosis, diseases of the skin such as acne, infertility and polycystic ovary syndrome. The compounds of the present invention may be useful for the treatment of Hepatitis C infection.

In another embodiment, the DGAT1 mediated disorders of the present invention are selected from obesity, diabetes, impaired glucose tolerance, insulin resistance, impaired glucose tolerance, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, hypercholesterolemia, hypertriglyceridemia and hyperlipidemia.

In another embodiment, the present invention provides a method for the treatment of diseases or disorders mediated by DGAT1 , comprising administering to a mammal in need thereof a therapeutically effective amount of a compound of formula 1 , or a pharmaceutically acceptable salt or prodrug thereof.

In a further embodiment, the present invention provides a method for the treatment of obesity comprising administering to a mammal in need thereof a therapeutically effective amount of a compound of formula 1 , or a pharmaceutically acceptable salt or prodrug thereof.

In an embodiment, the present invention provides the use of a compound of formula 1 in the treatment of diseases or disorders mediated by DGAT1 .

In another embodiment, the present invention provides the use of a compound of formula 1 in the treatment of obesity.

In an embodiment, the present invention provides the use of a compound of formula 1 or a pharmaceutically acceptable salt or a produg thereof, for the manufacture of a medicament for the treatment of diseases or disorders mediated by DGAT1 .

According to another embodiment of the present invention, there is provided the use of a compound of formula 1 or a pharmaceutically acceptable salt or a prodrug thereof, for the manufacture of a medicament for the treatment of obesity.

In an embodiment, the methods for treating DGAT1 associated disorders described herein use the pharmaceutical compositions described above and can be administered by the following administration routes, modes, etc.

Pharmaceutical Compositions and Methods:

The pharmaceuticals can be administered orally, for example in the form of pills, tablets, coated tablets, capsules, granules or elixirs. Administration, however, can also be carried out rectally, for example in the form of suppositories, or parenterally, for example intravenously, intramuscularly or subcutaneously, in the form of injectable sterile solutions or suspensions, or topically, for example in the form of solutions or transdermal patches, or in other ways, for example in the form of aerosols or nasal sprays.

As used herein, the term "pharmaceutically acceptable" means that the carrier, diluent, excipients, and/or salt must be compatible with the other ingredients of the formulation, and not deleterious to the recipient thereof.

The pharmaceutical preparations according to the invention are prepared in a manner known and familiar to one skilled in the art. Pharmaceutically acceptable inert inorganic and/or organic carriers and/or additives can be used in addition to the compound(s) of formula 1 , and/or its (their) physiologically tolerable salt(s). For the production of pills, tablets, coated tablets and hard gelatin capsules it is possible to use, for example, lactose, corn starch or derivatives thereof, gum arabica, magnesia or glucose, etc. Carriers for soft gelatin capsules and suppositories are, for example, fats, waxes, natural or hardened oils, etc. Suitable carriers for the production of solutions, for example injection solutions, or of emulsions or syrups are, for example, water, physiological sodium chloride solution or alcohols, for example, ethanol, propanol or glycerol, sugar solutions, such as glucose solutions or mannitol solutions, or a mixture of the various solvents which have been mentioned.

The pharmaceutical preparations normally contain about 1 to 99 %, for example, about 5 to 70 %, or from about 10 to about 30 % by weight of the compound of the formula 1 or its physiologically tolerable salt. The amount of the compound of the formula 1 or its physiologically tolerable salt in the pharmaceutical preparations normally is from about 5 to 500 mg. The dose of the compounds of this invention, which is to be administered, can cover a wide range. The dose to be administered daily is to be selected to suit the desired effect. A suitable dosage is about 0.001 to 100 mg/kg/day of the compound of formula 1 or their physiologically tolerable salt, for example, about 0.01 to 50 mg/kg/day of a compound of formula 1 or a pharmaceutically acceptable salt of the compound. If required, higher or lower daily doses can also be administered.

The selected dosage level will depend upon a variety of factors including the activity of the particular compound of the present invention employed, or the ester, salt or amide thereof, the route of administration, the time of administration, the rate of excretion of the particular compound being employed, the duration of the treatment, other drugs, compounds and/or materials used in combination with the particular compounds employed, the age, sex, weight, condition, general health and prior medical history of the patient being treated, and like factors well known in the medical arts.

In addition to the compound of the formula 1 or its physiologically acceptable salt and carrier substances, the pharmaceutical preparations can contain additives such as, for example, fillers, antioxidants, dispersants, emulsifiers, defoamers, flavors, preservatives, solubilizers or colorants. They can also contain two or more compounds of formula 1 or their physiologically tolerable salts. Furthermore, in addition to at least one compound of formula 1 or its physiologically tolerable salt, the pharmaceutical preparations can also contain one or more other therapeutically or prophylactically active ingredients.

It is understood that modifications that do not substantially affect the activity of the various embodiments of this invention are included within the invention disclosed herein. Accordingly, the following examples are intended to illustrate but not to limit the present invention.

The following abbreviations or terms are used herein:

AIBN 2,2'-Azobisisobutyronitrile

AIMe3 Trimethylaluminium

CD3OD Deuteriated methanol

CDC Deuteriated chloroform

CHC Chloroform

CCU Carbon tetrachloride

C02 Carbon dioxide

CuCI2 Cupric chloride

DCC Ν,Ν'-Dicyclohexyl carbodimide

DCM Dichloromethane

DMF N,N-Dimethylformamide

DMSO Dimethylsulfoxide

DMSO-de Deuteriated dimethylsulfoxide

EtOH Ethanol

EtOAc Ethyl Acetate

eq equivalent

Fe Iron

g gram

h hour(s)

HCI Hydrochloric acid

H2S04 Sulfuric acid

H20 Water

LiAIH4 Lithium aluminium hydride

LiOH Lithium hydroxide

mg/kg/day milligram/ kilogram/ day

MeOH Methanol

mg milligram(s)

mL milliliter

min minute(s)

mol Moles

mmol Millimoles

MgS04 Magnesium sulfate

N Normal

NBS N-bromosuccinimide

NaOH Sodium hydroxide

NaHC03 Sodium bicarbonate

Na2C03 Sodium carbonate

NaN02 Sodium nitrite

Na2S04 Sodium sulfate

nM nanomolar

Ni Nickel

PBr3 phosphorus tribromide

Pd/C Palladium over activated carbon

Pd(dppf)CI2:CH2CI2 [1 ,1 '-bis(diphenylphosphino)-ferrocene] dichloropalladium (II), complex with dichloromethane, Sigma-Aldrich, USA

Pd(PPh3) Triphenylphosphine Palladium

Pt/C platinum over activated carbon

Psi pounds per square inches

Room temperature 20-35 °C

SOCI2 Thionyl chloride

S02 Sulfur dioxide

SnCI2 Stannous chloride

TBAF Tributyl ammonium fluoride

TBDMS-CI Tetrabutyl dimethyl silyl chloride

THF Tetrahydrofuran

Example 1 :

5-Bromo-2-methyl benzoic acid

To a mixture of bromine (4 mL, 78 mmol) and iron (300 mg) cooled to 0 °C, 2-methyl benzoic acid (5.0 g, 37 mmol) was added and the slurry was stirred at room temperature for about 16 h. The reaction mixture was triturated with water to provide a solid, which was isolated by filtration and dried at 50 °C for 4 h. The material obtained (8 g) was determined by 1 HNMR to be a 60:40 mixture of the 5-bromo-2-methyl benzoic acid and 3-bromo-2-methyl benzoic acid isomers.

Further purification was performed on a separate batch of the 60:40 mixture by taking 12.5 g of the mixture and dissolving it in 200 mL of methanol. While stirring at room temperature, 250 mL of 0.1 N aqueous hydrochloric acid was added slowly producing a white solid. This solid was filtered and dried at 60 °C to afford the title compound.

Ref:-US2007/0213342 A1

Example 2:

5-Bromo-2-methyl benzoic acid methyl ester

The compound of example 1 (20.3 g, 0.0944 mol) was dissolved in 150 mL methanol and cooled to 0 °C. To this reaction mixture, thionyl chloride (28.07 g, 0.236 mol) was added slowly within 15-20 min. The reaction mixture was stirred at room temperature for 2- 3 h. After completion of the reaction, MeOH was removed under vacuum. The oily material obtained was dissolved in ethyl acetate and washed with sodium bicarbonate, water and brine and dried over anhydrous sodium sulfate. The organic layer was concentrated to obtain the title compound.

Yield: 20.5 g (95.2 %)

Ref:-US2007/0213342 A1

Example 3:

Methyl 4-methyl-4'-nitrobiphenyl-3-carboxylate

The compound of example 2 (0.592 g, 0.0026 mol, 1 .0 eq), bis(pinacolato) diboron (0.71 1 g, 0.0028 mol, 1 .05 eq), palladium acetate (17.4 mg, 0.0007 mol, 3 mol % eq) and potassium acetate (0.765 g, 0.0078 mol, 3 eq) were taken in 10 mL of dry DMF. The mixture was degassed by gently bubbling argon through it for 30 min at room temperature. The mixture was then heated at 80 °C under argon atmosphere until completion of reaction (3 h). After completion of of reaction, the reaction mixture was cooled to room temperature, followed by addition of 1 -bromo-4-nitrobenzene (0.52 g, 0.0026 mol, 1 .0 eq), cesium carbonate (1 .27 g, 0.00039 mol, 1 .5 eq) and Pd(PPh3)4 (0.090 g, 0.078 mol, 3 mol %). The reaction mixture was then heated at 80 °C for about 16 h under argon, then cooled to room temperature and diluted with water (20 mL) and ethyl acetate (20 mL). Black particles were removed by passing through a pad of celite The organic layer was separated and washed twice with 15 mL of brine solution. After drying over anhydrous sodium sulfate, the solvent was removed to give crude 2-(4'-nitro-biphenyl-4-methyl)methyl benzoate, which was purified by column chromatography (silicagel, 1 -5 % ethyl acetate in petroleum ether) to obtain the title compound.

Yield: 0.650 mg (93 %); 1 H NMR (DMSO-d6, 300MHz): δ 8.282-8.244 (d, J=9Hz, 2H), 8.126-8.191 (d, J=2.1 Hz, 1 H), 7.947-7.917 (d, J=9Hz, 2H), 7.844-7.850 (dd, J= 2.1 , 8.1 Hz, 1 H), 7.474-7.448 (d, J=7.8Hz, 1 H), 3.853 (s, 3H), 2.539 (s, 3H); MS (ESI): m/z 272 (M+H).

Example 4:

Methyl 4-(bromomethyl)-4'-nitrobiphenyl-3-carboxylate

The compound of example 3 (5.7 g, 0.021 mol) was dissolved in carbon tetrachloride (125 mL). AIBN (350 mg) and NBS (4.1 g, 0.0231 mol) were added and the reaction mixture was refluxed at 80 °C. After completion of the reaction, the reaction mixture was cooled to room temperature and filtered through celite. The filtrate was concentrated to obtain a crude material containing 85 % mono bromo and 10 % dibromo product and 5 % starting material.The crude was used directly without purification for the preparation of the compound of example 5.

Example 5:

(S)-Methyl 3-methyl-2-(6-(4-nitrophenyl)-1-oxoisoindolin-2-yl) butanoate

A mixture of the compound of example 4 (1 .54 g, 0.0044 mol) and L-valine methyl ester hydrochloride (0.813 g, 0.0048 mol) was taken in toluene (30 mL) in a round bottom flask. To this reaction mixture, triethyl amine (0.98 g, 0.0097 mol) was added and refluxed for 3-4 h. After completion of the reaction, the reaction mixture was diluted with ethyl acetate and washed with water and brine, dried over anhydrous sodium sulfate and concentrated to obtain an oily material, which was purified by column chromatography (silicagel, 30 % ethyl acetate in petroleum ether).

Yield: 1 .2 g (75 %); 1 H NMR (DMSO-d6, 300MHz): δ 8.312-8.283 (d, J=8.7Hz, 2H), 8.077-8.019 (m, 4H), 7.789-7.761 (d, J=8.4Hz, 1 H), 4.698-4.568 (m, 3H), 3.668 (s, 3H), 2.353-2.233 (s, 1 H), 0.995-0.973 (d, J= 6.6Hz, 3H ), 0.847-0.825 (d, J= 6.6 Hz, 3H); MS (ESI): m/z 369 (M+H).

Example 6:

(S)-Methyl 2-(6-(4-aminophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate

The compound of example 5 (0.9 g, 0.00244 mol), iron (0.32 g, 0.0057 mol) and ammonium chloride (0.551 g, 0.0103 mol) were taken in EtOH:THF:H20 (15.5 mL, 9:4.5:2.25). The reaction mixture was refluxed for about 16 h. After completion of the reaction, the reaction mixture was filtered through celite. The filtrate was concentrated to obtain a solid residue which was dissolved in ethyl acetate and washed with water and brine, dried over anhydrous sodium sulfate and concentrated to obtain a crude product, which was purified by column chromatography (silicagel, 30 % ethyl acetate in petroleum ether).

Yield: 0.76 g (92 %); 1 H NMR (DMSO-d6, 300MHz): δ 7.824-7.785 (m, 2H), 7.627-7.601 (d, J=7.8Hz, 1 H), 7.433-7.404 (d, J=8.7Hz, 2H), 6.673-6.644 (d, J=8.7Hz, 2H), 5.302 (s, 2H), 4.625-4.495 (m, 3H), 3.680 (s, 3H), 2.380-2.258 (s, 1 H), 1 .007-0.985 (d, J=6.6Hz, 3H ), 0.854-0.831 (d, J=6.9 Hz, 3H); MS (ESI): m/z 339 (M+H).

Example 7:

(S)-Methyl 2-(6-(4-(3-(4-fluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate

The compound of example 6 (0.520 g, 0.00153 mol) was dissolved in 5 mL of dichloromethane and 4-fluorophenyl isocyanate (0.238 g, 0.00169 mol) was added and stirred at room temperature for 8-10 h. The reaction mixture was concentrated and purified by column chromatography (silicagel, 30-40 % ethyl acetate in petroleum ether).

Yield: 0.690 g (94.5 %)

Example 8:

(S)-2-(6-(4-(3-(4-Fluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid

The compound of example 7 (0.300 g, 0.00631 mol) was taken in THF (4 mL) and MeOH (1 mL) and to this reaction mixture, 1 N LiOH (0.0654 g, 0.001547 mol) was added and stirred at room temperature for 2-3 h. After completion of the reaction, the solvent was removed and the residue obtained was dissolved in water and acidified with 1 N HCI to obtain the title compound, which was filtered and dried.

Yield: 0.285 g (98 %); 1 H NMR (DMSO-d6, 300MHz): δ 13.061 (s, 1 H), 8.868 (s, 1 H), 8.833 (s, NH), 7.721 -7.680 (t, J=3Hz, 9Hz, 2H), 7.638-7.630 (dd, J=3Hz, 8Hz, 1 H), 7.630-7.600 (d, J=9 Hz, 2H), 7.614-7.581 (d, J=8.7Hz, 2H), 7.581 -7.552 (d, 8.7Hz, 2H), 7.175-7.1 16 (t, J=9 Hz, 2H), 4.692-4.589 (dd, J=6.6 & 17.7 Hz, 2H), 4.548-4.515 (d, J=9.9Hz,1 H), 2.416-2.291 (m,1 H), 1 .036-1 .014 (d, J=6.6Hz, 3H), 0.868-0.846 (d, J=6.6Hz, 3H); MS (ESI): m/z 460(M-H), 462 (M+H)

Example 9:

(S)-Methyl 2-(6-(4-(3-(2.4-difluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate

The compound of example 9 was prepared analogous to compound of example 7 by reaction of compound of example 6 with 2,4-difluorophenyl isocyanate. The compound of example 9 was used directly without isolation for the preparation of compound of example 10.

Example 10:

(S)-2-(6-(4-(3-(2.4-Difluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid

The compound of example 10 was prepared analogous to compound of example 8 by hydrolysis of compound of example 7.

Yield: 83 %; 1 H NMR (DMSO-d6, 300MHz): δ 12.999 (s, 1 H), 9.216 (s, 1 H), 8.600 (s, NH), 8.125-8.086 (dd, J=2.7Hz, 9Hz, 1 H), 7.719-7.677 (d, J=8Hz, 2H), 7.635 (d, J=8 Hz, 2H), 7.597-7.588 (d, J=2.7Hz, 1 H), 7.635 (dd, J=2.7&8 Hz, 1 H), 7.588-7.558 (d, 9Hz,1 H), 7.370-7.293 (m, 1 H), 7.099-7.045 (m, 1 H), 4.686-4.667 (dd, J=6.6 & 17.7 Hz, 2H), 4.541 -4.508 (d, J=9.9Hz, 1 H), 2.338-2.306 (m,1 H), 1 .031 -1 .009 (d, J=6.6Hz, 3H), 0.862-0.840 (d, J=6.6Hz, 3H); MS (ESI): m/z 478 (M-H), m/z 480 (M+H).

Example 11 :

(S)-Methyl 2-(6-(4-(3-(2-fluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate

The compound of example 11 was prepared analogous to compound of example 7 by reaction of compound of example 6 with 2-fluorophenyl isocyanate. The compound of example 11 was used directly without isolation for the preparation of compound of example 12.

Example 12:

(S)-2-(6-(4-(3-(2-Fluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid

The compound of example 12 was prepared analogous to compound of example 8 by hydrolysis of compound of example 11 .

Yield: 83 %; 1 H NMR (DMSO-d6, 300MHz): δ 12.990 (s, 1 H), 9.236 (s, 1 H), 8.608 (s, NH), 8.158-8.125 (t, J=8 &8.5Hz, 1 H), 7.683-7.6 (d, J=9.5Hz, 2H), 7.595-7.577 (d, J=9Hz, 2H), 7.556 (d, 1 H), 7.556-7.539 (d, 9Hz, 2H), 7.241 -7.202 (t, J=8.5Hz,1 H), 7.144-7.1 13 (t, J=8Hz, 1 H), 7.013-6.973 (m,1 H), 4.693-4.601 (dd, J=6.6 & 17.7 Hz, 2H), 4.504-4.484 (d, J=10Hz,1 H), 2.330-2.269 (m,1 H), 0.996-0.983 (d, J=6.5Hz, 3H), 0.828-0.815 (d, J=6.6Hz, 3H); MS (ESI): m/z 460(M-H), m/z 462 (M+H).

Example 13:

(S)-Methyl 2-(6-(4-(3-(3-fluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate

The compound of example 13 was prepared analogous to compound of example 7 by reaction of compound of example 6 with 3-fluorophenyl isocyanate. The

compound of example 13 was used directly without isolation for the preparation of compound of example 14.

Example 14:

(S)-2-(6-(4-(3-(3-Fluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid

The compound of example 14 was prepared analogous to compound of example 8 by hydrolysis of compound of example 13.

Yield: 95.8 %; 1 H NMR (DMSO-d6, 300MHz): δ 13.009 (s, 1 H), 8.992 (s, 1 H), 8.934 (S, NH), 7.723-7.720 (d, J=7.2Hz, 2H), 7.679 (d, J=7.5Hz, 1 H), 7.637 (s,1 H), 7.612-7.603 (d, J=2.7Hz, 2H), 7.587-7.557 (d, J=9Hz, 2H), 7.557-7.529 (m, 1 H), 7.362-7.284 (dd, J=8.1 Hz, 1 H), 7.164-7.133 (d, J=8.1 Hz, 1 H), 6.833-6.797 (dd, J=8.4Hz, 1 H), 4.747-4.609 (dd, J=6.3 & 17.7 Hz, 2H), 4.545-4.512 (d, J=9.9Hz, 1 H), 2.364-2.287 (m, 1 H), 1 .033-1 .01 1 (d, J=6.6Hz, 3H), 0.865-0.843 (d, J=6.6Hz, 3H);

MS (ESI): m/z 460 (M-H), m/z 462 (M+H)

Example 15:

(S)-Methyl 3-methyl-2-(1-oxo-6-(4-(3-phenylureido)phenyl)isoindolin-2-yl) butanoate

The compound of example 15 was prepared analogous to compound of example 7 by reaction of compound of example 6 with phenyl isocyanate. The compound of example 15 was used directly without isolation for the preparation of compound of example 16.

Example 16:

(S)-3-Methyl-2-(1-oxo-6-(4-(3-phenylureido)phenyl)isoindolin-2-yl)butanoic acid

The compound of example 16 was prepared analogous to compound of example 8 by hydrolysis of compound of example 14.

Yield: 88 %; 1 H NMR (DMSO-d6, 300MHz): δ 13.042 (s, 1 H), 8.949 (s, 1 H), 8.736 (s, NH), 7.696-7.663 (t, J=9.9Hz, 2H), 7.663-7.589 (d, J=8.5 Hz, 2H), 7.589 (s, 1 H), 7.558-7.541 (d, J=.7Hz, 2H), 7.470-7.454 (d, J=8Hz, 2H), 7.297-7.266 (t, J=5, 7.5, 12.5Hz, 2H), 6.984-6.955 (t, J=7, 7.5, 14.5Hz, 1 H), 4.71 1 -4.522 (dd, J=17.5Hz, 2H), 4.522-4.502 (d, J=10Hz, 1 H), 2.32-2.301 (m, 1 H), 1 .012-0.999 (d, J=6.5Hz, 3H), 0.844-0.831 (d, J=6.6Hz, 3H); MS (ESI): m/z 442 (M+H).

Example 17:

(S)-Methyl 2-(6-(4-(3-benzylureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate

The compound of example 17 was prepared analogous to compound of example 7 by reaction of compound of example 6 with benzyl isocyanate. The compound of example 17 was used directly without isolation for the preparation of compound of example 18.

Example 18:

(S)-2-(6-(4-(3-Benzylureido)phenyl)-1-oxoisoindolin-2-yl)-3-methylbutanoic acid

The compound of example 18 was prepared analogous to compound of example 8 by hydrolysis of compound of example 17.

Yield: 88.49 %; 1 H NMR (DMSO-d6, 300MHz): δ 13.124 (s, 1 H), 8.803 (s, 1 H), 7.698-7.674 (t, J=7.2Hz, 2H), 7.618-7.593 (d, J=7.5Hz,1 H), 7.583-7.568 (m, 1 H), 7.554-7.520 (d, J=10.2Hz, 2H), 7.520-7.491 (d, J=8.7Hz, 1 H), 7.375-7.292 (m, 2H), 7.248-7.197 (dd, J=2.7, 8.1 Hz, 2H), 6.799-6.680 (m, 1 H), 4.725-4.596 (dd, J=2.7,18 Hz, 2H), 4.532-4.499 (d, J=9.9Hz, 1 H), 4.338-4.319 (d, J=5.7Hz, 2H), 4.244-4.224 (d, J=6 Hz, 1 H), 2.378-2.279 (m, 1 H), 1 .027-1 .005 (d, J=6.6Hz, 3H), 0.856-0.834 (d, J=6.6Hz, 3H); MS (ESI): m/z 458 (M+H).

Example 19:

(S)-Methyl 2-(6-(4-(3-(2,6-difluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate

The compound of example 19 was prepared analogous to compound of example 7 by reaction of compound of example 6 with 2,6-difluorophenyl isocyanate. The compound of example 19 was used directly without isolation for the preparation of compound of example 20.

Example 20:

(S)-2-(6-(4-(3-(2,6-Difluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid

The compound of example 20 was prepared analogous to compound of example 8 by hydrolysis of compound of example 19.

Yield: 90 %; 1 H NMR (DMSO-d6, 300MHz): δ 13.008 (s, 1 H), 9.158 (s, 1 H), 8.372 (s, NH), 7.717-7.713 (dd, J=1 .3, 7.2Hz, 2H), 7.629 (d, J=7.2Hz, 2H), 7.598-7.572 (d, J=7.8 Hz, 1 H), 7.572-7.542 (d, J=9Hz, 2H), 7.378-7.280 (m, 1 H), 7.196-7.143 (t, J=7.8Hz, 2H), 4.741 -4.602 (dd, J=6.3 & 17.7 Hz, 2H), 4.539-4.506 (d, J=9.9Hz, 1 H), 2.383-2.317 (m, 1 H), 1 .029-1 .007 (d, J=6.6Hz, 3H), 0.860-0.838 (d, J=6.6Hz, 3H); MS (ESI): m/z 480 (M+H).

Example 21 :

(S)-Methyl 3-methyl-2-(1-oxo-6-(4-(3-m-tolylureido)phenyl)isoindolin-2-yl) butanoate

The compound of example 21 was prepared analogous to compound of example 7 by reaction of compound of example 6 with 3-methyl phenyl isocyanate. The compound of example 21 was used directly without isolation for the preparation of compound of example 22.
Example 22:

(S)-3-Methyl-2-(1-oxo-6-(4-(3-m-tolylureido)phenyl)isoindolin-2-yl)butanoic acid

The compound of example 22 was prepared analogous to compound of example 8 by hydrolysis of compound of example 21 .

Yield: 85 %; 1 H NMR (DMSO-d6, 300MHz): δ 13.013 (s, 1 H), 8.842 (s, 1 H), 8.670 (s, NH), 7.713-7.677 (dd, J=6, 7.2Hz, 2H), 7.634-7.608 (dd, J=7.8, 7.8Hz, 2H), 7.598-7.574 (d, J=7.2Hz, 2H), 7.574-7.545 (d, J=8.7Hz, 1 H), 7.317 (s,1 H), 7.276-7.248 (d, J=8.4Hz, 1 H), 7.197-7.146 (t, J=7.5, 7.8Hz, 1 H), 6.813-6.793 (d, J=7.5Hz,1 H), 4.747-4.610 (dd, J=5.7, 17.7Hz, 2H), 4.547-4.514 (d, J=9.9Hz, 1 H), 2.365-2.320 (m, 1 H), 2.290 (s, 3H), 1 .034-1 .012 (d, J=6.6Hz, 3H), 0.866-0.844 (d, J=6.6Hz, 3H); MS (ESI): m/z 456 (M-H), m/z 458 (M+H).

Example 23:

(S)-Methyl 3-methyl-2-(1-oxo-6-(4-(3-p-tolylureido)phenyl)isoindolin-2-yl) butanoate

The compound of example 23 was prepared analogous to compound of example 7 by reaction of compound of example 6 with 4-methyl phenyl isocyanate. The compound of example 23 was used directly without isolation for the preparation of compound of example 24.
Example 24:

(S)-3-Methyl-2-(1-oxo-6-(4-(3-p-tolylureido)phenyl)isoindolin-2-yl)butanoic acid
The compound of example 22 was prepared analogous to compound of example 8 by hydrolysis of compound of example 21

We claim:
1 . A compound of formula 1 ,

Formula 1
wherein,
A is selected from unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted (C3-Ci2)-cycloalkyl, unsubstituted or substituted aryl and unsubstituted or substituted heterocyclyl; wherein the aryl group may be fused with an unsubstituted or substituted 5 or 6-membered cycloalkyi ring optionally containing heteroatoms selected from O, N or S;
n is 0 or 1 ;
L is selected from NHC(0)NH, NHC(S)NH, *NHS02, *CONH and *S02NH; wherein * indicates the point of attachment to A-[CH2]n-;
Xi , 2, X3, X4 and X5 are independently selected from N, N-oxide, C, CH and CR; wherein R is selected from halogen, hydroxy, (CrCi2)-alkoxy, cyano, (CrCi2)-alkyl, CF3, OCF3, (C2-Ci2)-alkenyl, (C2-Ci2)-alkynyl, (C3-Ci2)-cycloalkyl, aryl, aryloxy, heterocyclyl, O-heterocyclyl, C(0)Rp, C(0)ORp, NRpRq, SRP, S(0)Rp, S02Rp and C(0)NRpRq;
Rp and Rq are independently selected from hydrogen, unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted aryl, unsubstituted or substituted aralkyl and unsubstituted or substituted heterocyclyl, or Rp and Rq can optionally form a 3-7 membered ring;
Yi and Y2 are independently selected from C=0 and CH2;
m is an integer selected from 1 to 4; wherein:
when m is 1 , Ra and Rb may be selected from
and R2;
when m is 2, Ra and Rb may be selected from R1 ; R2, R3 and R4;
when m is 3, Ra and Rb may be selected from R1 ; R2, R3, R4, R5 and R6;
when m is 4, Ra and Rb may be selected from R1 ; R2, R3, R4, R5, R6, R7 and
R8;
Ri , R2, R3, R4, R5, Re, R7 and R8 are independently selected from hydrogen, unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted aryl, unsubstituted or substituted aralkyl and unsubstituted or substituted heterocyclyl;
or any two of Ri , R2, R3, R4, R5, Re, R7 and R8 can form a (C3-C12) cycloalkyl ring;
R9 is selected from hydrogen, unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted aryl, unsubstituted or substituted aralkyl and unsubstituted or substituted heterocyclyl;
wherein,
(CrCi2)-alkyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (CrCi2)-alkoxy, cyano, nitro, unsubstituted or substituted (C3-Ci2)-cycloalkyl, unsubstituted or substituted aryl, C(0)Rp, C(0)ORp, NRpRq, SRP, S(0)Rp and S02Rp;
(C3-Ci2)-cycloalkyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (CrCi2)-alkoxy cyano, nitro, unsubstituted or substituted aryl, unsubstituted or substituted heterocyclyl, C(0)Rp, C(0)ORp, NRpRq, SRP, S(0)Rp and S02Rp;
aryl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (CrCi2)-alkoxy, cyano, nitro, unsubstituted or substituted (C Ci2)-alkyl, CF3, OCF3, (C2-Ci2)-alkenyl, (C2-Ci2)-alkynyl, unsubstituted or substituted (C3-Ci2)-cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy, unsubstituted or substituted heterocyclyl, unsubstituted or substituted O-heterocyclyl, C(0)Rp, C(0)ORp, NRpRq, SRP, S(0)Rp and S02Rp, or aryl may be fused with an unsubstituted or substituted 5 or 6-membered cycloalkyl ring optionally containing heteroatoms selected from O, N and S;
heterocyclyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (CrCi2)-alkoxy, cyano, nitro, unsubstituted or substituted (d-Ci2)-alkyl, CF3, OCF3, (C2-Ci2)-alkenyl, (C2-Ci2)-alkynyl, unsubstituted or substituted (C3-Ci2)-cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy, unsubstituted or substituted heterocyclyl, unsubstituted or substituted O-heterocyclyl, C(0)Rp, C(0)ORp, NRpRq, SRP, S(0)Rp and S02RP; and
Rp and Rq are independently selected from hydrogen, unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted aryl, unsubstituted or substituted aralkyl and unsubstituted or substituted heterocyclyl, or Rp and Rq can optionally form a 3-7 membered ring;
or a stereoisomer, tautomer or a pharmaceutically acceptable salt, solvate, polymorph, prodrug, carboxylic acid isostere or N-oxide thereof.
2. The compound of formula 1 a, according to claim 1 ,

Formula 1 a
wherein,
A is selected from unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted (C3-Ci2)-cycloalkyl, unsubstituted or substituted aryl and unsubstituted or substituted heterocyclyl; wherein the aryl group may be fused with an unsubstituted or substituted 5 or 6-membered cycloalkyl ring optionally containing heteroatoms selected from O, N or S;
n is 0 or 1 ;
L is selected from NHC(0)NH, NHC(S)NH, *NHS02, *CONH and *S02NH; wherein * indicates the point of attachment to A-[CH2]n-;
Xi , X2, X4 and X5 are independently selected from N, N-oxide, CH and CR; wherein R is selected from halogen, hydroxy, (CrCi2)-alkoxy, cyano, (CrCi2)-alkyl, CF3, OCF3, (C2-Ci2)-alkenyl, (C2-Ci2)-alkynyl, (C3-Ci2)-cycloalkyl, aryl, aryloxy, heterocyclyl, O-heterocyclyl, C(0)Rp, C(0)ORp, NRpRq, SRP, S(0)Rp, S02Rp and C(0)NRpRq;
Rp and Rq are independently selected from hydrogen, unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted aryl, unsubstituted or substituted aralkyl and unsubstituted or substituted heterocyclyl, or Rp and Rq can optionally form a 3-7 membered ring;
Yi and Y2 are independently selected from C=0 and CH2;
m is an integer selected from 1 to 4; wherein:
when m is 1 , Ra and Rb may be selected from R-\ and R2;
when m is 2, Ra and Rb may be selected from R1 ; R2, R3 and R4;
when m is 3, Ra and Rb may be selected from R1 ; R2, R3, R4, R5 and R6;
when m is 4, Ra and Rb may be selected from R1 ; R2, R3, R4, R5, R6, R7 and
Re!
Ri , R2, R3, R4, R5, Re, R7 and R8 are independently selected from hydrogen, unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted aryl, unsubstituted or substituted aralkyl and unsubstituted or substituted heterocyclyl;
or any two of Ri , R2, R3, R4, R5, Re, R7 and R8 can form a (C3-Ci2) cycloalkyl ring;
Rg is selected from hydrogen, unsubstituted or substituted (Ci-Ci2)-alkyl, unsubstituted or substituted aryl, unsubstituted or substituted aralkyl and unsubstituted or substituted heterocyclyl;
wherein,
(CrCi2)-alkyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (CrCi2)-alkoxy, cyano, nitro, unsubstituted or substituted (C3-Ci2)-cycloalkyl, unsubstituted or substituted aryl, C(0)Rp, C(0)ORp, NRpRq, SRP, S(0)Rp and S02Rp;
(C3-Ci2)-cycloalkyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (CrCi2)-alkoxy cyano, nitro, unsubstituted or substituted aryl, unsubstituted or substituted heterocyclyl, C(0)Rp, C(0)ORp, NRpRq, SRP, S(0)Rp and S02Rp;
aryl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (CrCi2)-alkoxy, cyano, nitro, unsubstituted or substituted (C Ci2)-alkyl, CF3, OCF3, (C2-Ci2)-alkenyl, (C2-Ci2)-alkynyl, unsubstituted or substituted (C3-Ci2)-cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy, unsubstituted or substituted heterocyclyl, unsubstituted or substituted O-heterocyclyl, C(0)Rp, C(0)ORp, NRpRq, SRP, S(0)Rp and S02Rp, or aryl may be fused with an unsubstituted or substituted 5 or 6-
membered cycloalkyi ring optionally containing heteroatoms selected from O, N and S;
heterocyclyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (CrCi2)-alkoxy, cyano, nitro, unsubstituted or substituted (C Ci2)-alkyl, CF3, OCF3, (C2-Ci2)-alkenyl, (C2-Ci2)-alkynyl, unsubstituted or substituted (C3-Ci2)-cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy, unsubstituted or substituted heterocyclyl, unsubstituted or substituted O-heterocyclyl, C(0)Rp, C(0)ORp, NRpRq, SRP, S(0)Rp and S02Rp; and
Rp and Rq are independently selected from hydrogen, unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted aryl, unsubstituted or substituted aralkyl and unsubstituted or substituted heterocyclyl, or Rp and Rq can optionally form a 3-7 membered ring;
or a stereoisomer, tautomer or a pharmaceutically acceptable salt, solvate, polymorph, prodrug, carboxylic acid isostere or N-oxide thereof.
3. The compound of formula 1 or formula 1 a, according to claim 1 or claim 2, wherein,
A is selected from unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted (C3-Ci2)-cycloalkyl, unsubstituted or substituted aryl and unsubstituted or substituted heterocyclyl; wherein the aryl group may be fused with an unsubstituted or substituted 5 or 6-membered cycloalkyi ring optionally containing heteroatoms selected from O, N or S;
n is 0 or 1 ;
L is selected from NHC(0)NH, NHC(S)NH, *NHS02, *CONH and *S02NH; wherein * indicates the point of attachment to A-[CH2]n-;
X3 is C, to which A-(CH2)n-L- is attached; Xi, X2, X4 and X5 are independently selected from N, N-oxide, CH and CR; wherein R is selected from halogen, hydroxy, (CrCi2)-alkoxy, cyano, (Ci-Ci2)-alkyl, CF3, OCF3, (C3-Ci2)-cycloalkyl, aryl, aryloxy, heterocyclyl;
Yi and Y2 are independently selected from C=0 and CH2;
m is an integer selected from 1 to 4; wherein:
when m is 1 , Ra and Rb may be selected from Ri and R2;
when m is 2, Ra and Rb may be selected from R15 R2, R3 and R4;
when m is 3, Ra and Rb may be selected from R1 ; R2, R3, R4, R5 and R6;
when m is 4, Ra and Rb may be selected from R1 ; R2, R3, R4, R5, Re, R7 and
Re!
Ri, R2, R3, R4, R5, Re, R7 and R8 are independently selected from hydrogen, unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted aryl, unsubstituted or substituted aralkyl and unsubstituted or substituted heterocyclyl;
or any two of Ri, R2, R3, R4, R5, Re, R7 and R8 can form a (C3-Ci2) cycloalkyi ring;
R9 is selected from hydrogen and unsubstituted or substituted (CrCi2)-alkyl;
wherein,
(CrCi2)-alkyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (Ci-Ci2)-alkoxy, cyano, unsubstituted or substituted (C3-Ci2)-cycloalkyl and unsubstituted or substituted aryl,
(C3-Ci2)-cycloalkyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (CrCi2)-alkoxy cyano, unsubstituted or substituted aryl and unsubstituted or substituted heterocyclyl;
aryl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (CrCi2)-alkoxy, cyano, unsubstituted or substituted (CrCi2)-alkyl, CF3, OCF3, unsubstituted or substituted (C3-Ci2)-cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy and unsubstituted or substituted heterocyclyl, or aryl may be fused with an unsubstituted or substituted 5 or 6-membered cycloalkyi ring optionally containing heteroatoms selected from O, N and S; and
heterocyclyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (CrCi2)-alkoxy, cyano, unsubstituted or substituted (CrCi2)-alkyl, CF3, OCF3, unsubstituted or substituted (C3-Ci2)-cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy and unsubstituted or substituted heterocyclyl;
or a stereoisomer, tautomer or a pharmaceutically acceptable salt, solvate, polymorph, prodrug, carboxylic acid isostere or N-oxide thereof.
4. The compound of formula 1 or formula 1 a, according to any one of the claims
1 to 3,
wherein,
A is selected from unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted (C3-Ci2)-cycloalkyl, unsubstituted or substituted aryl and unsubstituted or substituted heterocyclyl; wherein aryl group may be fused with an unsubstituted or substituted 5 or 6-membered cycloalkyi ring optionally containing heteroatoms selected from O, N or S;
n is 0 or 1 ;
L is *C(0)NH wherein * indicates the point of attachment to A-[CH2]n-;
X3 is C, to which A-(CH2)n-L- is attached; X2 is selected from CH and CR, Xi , X4 and X5 are independently selected from CH, CR and N; wherein R is selected from halogen, hydroxy, (CrCi2)-alkoxy, cyano, (CrCi2)-alkyl, CF3, OCF3 and cycloalkyi; Yi and Y2 are independently selected from C=0 and CH2;
m is an integer selected from 1 to 4; wherein:
when m is 1 , Ra and Rb may be selected from R-\ and R2;
when m is 2, Ra and Rb may be selected from R1 ; R2, R3 and R4;
when m is 3, Ra and Rb may be selected from R1 ; R2, R3, R4, R5 and R6;
when m is 4, Ra and Rb may be selected from R1 ; R2, R3, R4, R5, R6, R7 and R8; Ri , R2, R3, R4, R5, Re, R7 and R8 are independently selected from hydrogen, unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted aryl; and unsubstituted or substituted aralkyl; or any two of Ri , R2, R3, R4, R5, Re, R7 and R8 form a (C3-Ci2) cycloalkyi ring; and
R9 is selected from hydrogen and unsubstituted (CrC6)-alkyl;
wherein,
(CrCi2)-alkyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (CrCi2)-alkoxy, cyano, unsubstituted or substituted (C3-Ci2)-cycloalkyl and unsubstituted or substituted aryl,
(C3-Ci2)-cycloalkyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (Ci-Ci2)-alkoxy cyano, unsubstituted or substituted aryl and unsubstituted or substituted heterocyclyl;
aryl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (CrCi2)-alkoxy, cyano, unsubstituted or
substituted (CrCi2)-alkyl, CF3, OCF3, unsubstituted or substituted (C3-Ci2)-cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy and unsubstituted or substituted heterocyclyl, or aryl may be fused with an unsubstituted or substituted 5 or 6-membered cycloalkyi ring optionally containing heteroatoms selected from O, N and S; and
heterocyclyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (CrCi2)-alkoxy, cyano, unsubstituted or substituted (CrCi2)-alkyl, CF3, OCF3, unsubstituted or substituted (C3-Ci2)-cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy and unsubstituted or substituted heterocyclyl;
or a stereoisomer, tautomer or a pharmaceutically acceptable salt, solvate, polymorph, prodrug, carboxylic acid isostere or N-oxide thereof.
5. The compound of formula 1 or formula 1 a, according to any one of the claims 1 to 4, wherein,
A is selected from unsubstituted or substituted aryl and unsubstituted or substituted heterocyclyl;
n is 0;
L is *C(0)NH wherein * indicates the point of attachment to A-[CH2]n-;
X3 is C, to which A-(CH2)n-L- is attached; Xi , X2, X4 and X5 are independently selected from CH and CR; wherein R is selected from halogen, hydroxy, (C1-C12)-alkoxy, cyano, (Ci-Ci2)-alkyl, CF3 and OCF3;
Yi is CH2 and Y2 is C=0;
m is 1 ; wherein Ra and Rb may be selected from
and R2;
Ri and R2 are independently selected from hydrogen and unsubstituted or substituted (CrCi2)-alkyl; and
R9 is selected from hydrogen and unsubstituted (CrC6)-alkyl;
wherein,
aryl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (Ci-Ci2)-alkoxy, unsubstituted or substituted (CrCi2)-alkyl, CF3, OCF3, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy and unsubstituted or substituted heterocyclyl, or aryl may be fused with an unsubstituted or substituted 5 or 6-membered cycloalkyi ring optionally containing heteroatoms selected from O, N and S; and
heterocyclyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (CrCi2)-alkoxy, unsubstituted or substituted (CrCi2)-alkyl, CF3, OCF3, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy and unsubstituted or substituted heterocyclyl;
or a stereoisomer, tautomer or a pharmaceutically acceptable salt, solvate, polymorph, prodrug, carboxylic acid isostere or N-oxide thereof.
6. The compound of formula 1 or formula 1 a, according to any one of the claims 1 to 3, wherein,
A is selected from unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted aryl and unsubstituted or substituted heterocyclyl; wherein aryl group may be fused with an unsubstituted or substituted 5 or 6-membered cycloalkyi ring optionally containing heteroatoms selected from O, N or S;
n is 0 or 1 ;
L is selected from NHC(0)NH and NHC(S)NH;
X3 is C, to which A-(CH2)n-L- is attached; X2 is selected from CH and CR, Xi , X4 and
X5 are independently selected from CH, CR and N; wherein R is selected from halogen, hydroxy, (CrCi2)-alkoxy, cyano, (CrCi2)-alkyl, CF3, OCF3 and cycloalkyi;
Yi and Y2 are independently selected from C=0 and CH2;
m is an integer selected from 1 to 4; wherein:
when m is 1 , Ra and Rb may be selected from R-\ and R2;
when m is 2, Ra and Rb may be selected from R1 ; R2, R3 and R4;
when m is 3, Ra and Rb may be selected from R1 ; R2, R3, R4, R5 and R6;
when m is 4, Ra and Rb may be selected from R1 ; R2, R3, R4, R5, R6, R7 and Rs; Ri , R2, R3, R4, R5, Re, R7 and R8 are independently selected from hydrogen, unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted aryl; and unsubstituted or substituted aralkyl; or any two of Ri , R2, R3, R4, R5, Re, R7 and R8 form a (C3-Ci2) cycloalkyi ring; and
R9 is selected from hydrogen and unsubstituted (CrC6)-alkyl;
wherein,
(CrCi2)-alkyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (CrCi2)-alkoxy, cyano, unsubstituted or substituted (C3-Ci2)-cycloalkyl and unsubstituted or substituted aryl,
(C3-Ci2)-cycloalkyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (CrCi2)-alkoxy cyano, unsubstituted or substituted aryl and unsubstituted or substituted heterocyclyl;
aryl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (CrCi2)-alkoxy, cyano, unsubstituted or substituted (CrCi2)-alkyl, CF3, OCF3, unsubstituted or substituted (C3-Ci2)-cycloalkyi, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy and unsubstituted or substituted heterocyclyl, or aryl may be fused with an unsubstituted or substituted 5 or 6-membered cycloalkyi ring optionally containing heteroatoms selected from O, N and S; and
heterocyclyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (CrCi2)-alkoxy, cyano, unsubstituted or substituted (CrCi2)-alkyl, CF3, OCF3, unsubstituted or substituted (C3-Ci2)-cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy and unsubstituted or substituted heterocyclyl;
or a stereoisomer, tautomer or a pharmaceutically acceptable salt, solvate, polymorph, prodrug, carboxylic acid isostere or N-oxide thereof.
7. The compound of formula 1 or formula 1 a, according to any one of the claims 1 to 3, wherein,
A is selected from unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted aryl and unsubstituted or substituted heterocyclyl; wherein aryl group may be fused with an unsubstituted or substituted 5 or 6-membered cycloalkyi ring optionally containing heteroatoms selected from O, N or S;
n is 0 or 1 ;
L is *S02NH wherein * indicates the point of attachment to A-[CH2]n-;
X3 is C, to which A-(CH2)n-L- is attached; X2 is selected from CH and CR, Xi, X4 and X5 are independently selected from CH, CR and N; wherein R is selected from halogen, hydroxy, (CrCi2)-alkoxy, cyano, (CrCi2)-alkyl, CF3, OCF3 and cycloalkyi; Yi and Y2 are independently selected from C=0 and CH2;
m is an integer selected from 1 to 4; wherein:
when m is 1 , Ra and Rb may be selected from R-\ and R2;
when m is 2, Ra and Rb may be selected from R1 ; R2, R3 and R4;
when m is 3, Ra and Rb may be selected from R1 ; R2, R3, R4, R5 and R6;
when m is 4, Ra and Rb may be selected from R1 ; R2, R3, R4, R5, Re, R7 and
Rs; Ri , R2, R3, R4, R5, Re, R7 and R8 are independently selected from hydrogen, unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted aryl; and unsubstituted or substituted aralkyl; or any two of Ri , R2, R3, R4, R5, Re, R7 and R8 form a (C3-C12) cycloalkyi ring; and
R9 is selected from hydrogen and unsubstituted (CrC6)-alkyl.
wherein,
(CrCi2)-alkyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (CrCi2)-alkoxy, cyano, unsubstituted or substituted (C3-Ci2)-cycloalkyl and unsubstituted or substituted aryl,
(C3-Ci2)-cycloalkyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (CrCi2)-alkoxy cyano, unsubstituted or substituted aryl and unsubstituted or substituted heterocyclyl;
aryl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (CrCi2)-alkoxy, cyano, unsubstituted or substituted (C Ci2)-alkyl, CF3, OCF3, unsubstituted or substituted (C3-C12)-cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy and unsubstituted or substituted heterocyclyl, or aryl may be fused with an unsubstituted or substituted 5 or 6-membered cycloalkyi ring optionally containing heteroatoms selected from O, N and S; and
heterocyclyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (CrCi2)-alkoxy, cyano, unsubstituted or substituted (CrCi2)-alkyl, CF3, OCF3, unsubstituted or substituted (C3-C12)-cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy and unsubstituted or substituted heterocyclyl;
or a stereoisomer, tautomer or a pharmaceutically acceptable salt, solvate, polymorph, prodrug, carboxylic acid isostere or N-oxide thereof.
8. The compound of formula 1 b, according to any one of the claims 1 to 3,

Formula 1 b
wherein,
A is selected from unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted (C3-Ci2)-cycloalkyl, unsubstituted or substituted aryl and unsubstituted or substituted heterocyclyl; wherein the aryl group may be fused with an unsubstituted or substituted 5 or 6-membered cycloalkyi ring optionally containing heteroatoms selected from O, N or S;
n is 0 or 1 ;
L is selected from NHC(0)NH, NHC(S)NH, *NHS02, *CONH and *S02NH; wherein * indicates the point of attachment to A-[CH2]n-;
X3 is C, to which A-(CH2)n-L- is attached; Xi, X2, X4 and X5 are independently selected from N, N-oxide, CH and CR; wherein R is selected from halogen, hydroxy, (Ci-Ci2)-alkoxy, cyano, (C Ci2)-alkyl, CF3, OCF3, (C2-Ci2)-alkenyl, (C2-Ci2)-alkynyl, (C3-Ci2)-cycloalkyl, aryl, aryloxy, heterocyclyl, O-heterocyclyl, C(0)Rp, C(0)ORp, NRpRq, SRP, S(0)Rp, S02Rp and C(0)NRpRq;
Rp and Rq are independently selected from hydrogen, unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted aryl, unsubstituted or substituted aralkyl and unsubstituted or substituted heterocyclyl, or Rp and Rq can optionally form a 3-7 membered ring;
Yi and Y2 are independently selected from C=0 and CH2;
Y is a cycloalkyi ring selected from:

and R9 is selected from hydrogen, unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted aryl, unsubstituted or substituted aralkyl and unsubstituted or substituted heterocyclyl;
wherein,
(CrCi2)-alkyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (CrCi2)-alkoxy, cyano, unsubstituted or substituted (C3-Ci2)-cycloalkyl, unsubstituted or substituted aryl;
(C3-Ci2)-cycloalkyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (CrCi2)-alkoxy cyano, unsubstituted or substituted aryl, unsubstituted or substituted heterocyclyl;
aryl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (CrCi2)-alkoxy, cyano, unsubstituted or substituted (CrCi2)-alkyl, CF3, OCF3, unsubstituted or substituted (C3-Ci2)-cycloalkyi, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy, unsubstituted or substituted heterocyclyl, or aryl may be fused with an unsubstituted or substituted 5 or 6-membered cycloalkyi ring optionally containing heteroatoms selected from O, N and S; and
heterocyclyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (CrCi2)-alkoxy, cyano, unsubstituted or substituted (CrCi2)-alkyl, CF3, OCF3, unsubstituted or substituted (C3-Ci2)-cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy and unsubstituted or substituted heterocyclyl;
or a stereoisomer, tautomer or a pharmaceutically acceptable salt, solvate, polymorph, prodrug, carboxylic acid isostere or N-oxide thereof.
9. The compound of formula 1 , according to any one of the claims 1 to 3, wherein,
A is an unsubstituted aryl or an aryl substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (CrCi2)-alkoxy, cyano, unsubstituted or substituted (CrCi2)-alkyl, CF3, OCF3, unsubstituted or substituted cycloalkyi, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy and unsubstituted or substituted heterocyclyl.
10. The compound of formula 1 , according to any one of the claims 1 to 3, wherein,
A is an unsubstituted heterocyclyl or a heterocyclyl substituted with one or more groups selected from halogen, hydroxy, unsubstituted or substituted (CrCi2)-alkoxy, CF3, OCF3, cyano, unsubstituted or substituted (CrCi2)-alkyl, unsubstituted or substituted cycloalkyi, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy and unsubstituted or substituted heterocyclyl.
1 1 . The compound of formula 1 , according to any one of the claims 1 to 3, wherein n is 0.
12. The compound of formula 1 , according to any one of the claims 1 to 3, wherein L is *CONH.
13. The compound of formula 1 , according to any one of the claims 1 to 3, wherein L is NHC(0)NH.
14. The compound of formula 1 , according to any one of the claims 1 to 3, wherein X3 is C, to which A-(CH2)n-L- is attached; and Xi, X2, X4 and X5 are independently selected from CH and CR; wherein R is selected from halogen, hydroxy, unsubstituted or substituted (CrCi2)-alkoxy, cyano, unsubstituted or substituted (CrCi2)-alkyl, CF3, OCF3, unsubstituted or substituted cycloalkyi, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy and unsubstituted or substituted heterocyclyl.
15. The compound of formula 1 , according to any one of the claims 1 to 3, wherein X3 is C, to which A-(CH2)n-L- is attached; X2 is selected from CH and CR;
Xi, X4 and X5 are independently selected from CH, CR and N; wherein R is selected from halogen, hydroxy, unsubstituted or substituted (CrCi2)-alkoxy, cyano, unsubstituted or substituted (CrCi2)-alkyl, CF3, OCF3, unsubstituted or substituted cycloalkyi, unsubstituted or substituted aryl, unsubstituted or substituted aryloxy and unsubstituted or substituted heterocyclyl.
16. The compound of formula 1 , according to any one of the claims 1 to 3, wherein Yi is CH2 and Y2 is C=0.
17. The compound of formula 1 , according to any one of the claims 1 to 3, wherein m is 1 and Ra and Rb are selected from Ri and R2, wherein Ri and R2 are independently selected from hydrogen, unsubstituted or substituted (Ci-Ci2)-alkyl, unsubstituted or substituted aryl, unsubstituted or substituted aralkyl and unsubstituted or substituted heterocyclyl.
18. The compound of formula 1 , according to any one of the claims 1 to 3, wherein R9 is selected from hydrogen and unsubstituted or substituted (CrCi2)-alkyl, wherein (CrCi2)-alkyl is unsubstituted or substituted with one or more groups selected from halogen, hydroxy, (CrCi2)-alkoxy, cyano and aryl.
19. The compound of formula 1 , formula 1 a or formula 1 b, according to any one of the claims 1 to 18, selected from:
(S)-Methyl 2-(6-(4-(3-(4-fluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate;
(S)-2-(6-(4-(3-(4-Fluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-Methyl 2-(6-(4-(3-(2,4-difluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(3-(2,4-Difluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(6-(4-(3-(2-fluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate;
(S)-2-(6-(4-(3-(2-Fluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-Methyl 2-(6-(4-(3-(3-fluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(3-(3-Fluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(3-phenylureido)phenyl)isoindolin-2-yl) butanoate; (S)-3-Methyl-2-(1 -oxo-6-(4-(3-phenylureido)phenyl)isoindolin-2-yl)butanoic acid; (S)-Methyl 2-(6-(4-(3-benzylureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate; (S)-2-(6-(4-(3-Benzylureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-Methyl 2-(6-(4-(3-(2,6-difluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(3-(2,6-Difluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(3-m-tolylureido)phenyl)isoindolin-2-yl) butanoate; (S)-3-Methyl-2-(1 -oxo-6-(4-(3-m-tolylureido)phenyl)isoindolin-2-yl)butanoic acid; (S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(3-p-tolylureido)phenyl)isoindolin-2-yl) butanoate; (S)-3-Methyl-2-(1 -oxo-6-(4-(3-p-tolylureido)phenyl)isoindolin-2-yl)butanoic acid; (S)-Methyl 2-(6-(4-(3-(3-methoxyphenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(3-(3-Methoxyphenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-Methyl-2-(6-(4-(3-(4-methoxyphenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(3-(4-Methoxyphenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl-2-(6-(4-(3-(3,5-difluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(3-(3,5-Difluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(6-(4-(3-(3,4-difluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(3-(3,4-Difluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(6-(4-(3-cyclohexylureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(3-Cyclohexylureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(3-(4-(trifluoromethyl)phenyl)ureido)phenyl) isoindolin-2-yl)butanoate;
(S)-3-Methyl-2-(1 -oxo-6-(4-(3-(4-(trifluoromethyl)phenyl)ureido)phenyl) isoindolin-2-yl)butanoic acid;
(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl) isoindolin-2-yl)butanoate;
(S)-3-Methyl-2-(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl) isoindolin-2-yl)butanoic acid;
(S)-Methyl 2-(6-(4-(3-(4-cyanophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(3-(4-Cyanophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-Methyl 2-(6-(4-(3-(3-cyanophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(3-(3-Cyanophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)- Methyl 2-(6-(4-(3-(4-chloro-2-phenoxyphenyl) ureido) phenyl)-1 -oxo isoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(3-(4-Chloro-2-phenoxyphenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(6-(4-(3-(5-chloro-2-phenoxyphenyl)ureido)phenyl)-1 -oxoisoindolin-2-y l)-3-methy Ibutanoate ;
(S)-2-(6-(4-(3-(5-Chloro-2-phenoxyphenyl) ureido) phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(3-(2-phenoxyphenyl)ureido)phenyl) isoindolin-2 yl)butanoate;
(S)-3-Methyl-2-(1 -oxo-6-(4-(3-(2-phenoxyphenyl)ureido)phenyl)isoindolin-2-yl)butanoic acid;
(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(3-(4-phenoxyphenyl)ureido)phenyl) isoindolin-2 yl)butanoate;
(S)-3-Methyl-2-(1 -oxo-6-(4-(3-(4-phenoxyphenyl)ureido)phenyl)isoindolin-2-yl)butanoic acid;
(S)-Methyl 2-(6-(4-(3-(2-fluorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(3-(2-Fluorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(3-p-tolylthioureido)phenyl)isoindolin-2-yl)butanoate;
(S)-3-Methyl-2-(1 -oxo-6-(4-(3-p-tolylthioureido)phenyl)isoindolin-2-yl)butanoic acid; (S)-Methyl 2-(6-(4-(3-(3-fluorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(3-(3-Fluorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(6-(4-(3-(4-methoxyphenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(3-(4-Methoxyphenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(6-(4-(3-(3-methoxyphenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(3-(3-Methoxyphenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(6-(4-(3-(4-chlorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(3-(4-Chlorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-Methyl 2-(6-(4-(3-(4-chlorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(3-(3-Chlorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(3-(2-(trifluoromethyl)phenyl)thioureido) phenyl) isoindolin-2-yl)butanoate;
(S)-3-Methyl-2-(1 -oxo-6-(4-(3-(2-trifluoromethyl)phenyl)thioureido)phenyl) isoindolin-2-yl)butanoic acid;
(S)-Methyl 2-(6-(4-(3-(4-cyanophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(3-(4-Cyanophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-Methyl 2-(6-(4-(3-(4-cyanophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(3-(3-Cyanophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(3-o-tolylthioureido)phenyl)isoindolin-2-yl)butanoate;
(S)-3-Methyl-2-(1 -oxo-6-(4-(3-o-tolylthioureido)phenyl)isoindolin-2-yl)butanoic acid; (S)-Methyl 2-(6-(4-(3-(2-methoxyphenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(3-(2-Methoxyphenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)thioureido) phenyl)isoindolin-2-yl)butanoate;
(S)-3-Methyl-2-(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)thioureido)phenyl) isoindolin-2-yl)butanoic acid;
(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(phenylsulfonamido)phenyl)isoindolin-2-yl)butanoate;
(S)-3-Methyl-2-(1 -oxo-6-(4-(phenylsulfonamido)phenyl)isoindolin-2-yl)butanoic acid; (S)-Methyl 2-(6-(4-(4-cyanophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(4-Cyanophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-Methyl 2-(6-(4-(3,4-difluorophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(3,4-Difluorophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(6-(4-(2,4-difluorophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(2,4-Difluorophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(6-(4-(3,4-dimethoxyphenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(3,4-Dimethoxyphenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(6-(4-(3-chlorophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(3-Chlorophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(6-(4-(4-methoxyphenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(4-Methoxyphenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(4-(trifluoromethyl)phenylsulfonamido) phenyl)isoindolin-2-yl)butanoate;
(S)-3-Methyl-2-(1 -oxo-6-(4-(4-(trifluoromethyl)phenylsulfonamido)phenyl) isoindolin-2-yl)butanoic acid;
(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(phenylmethylsulfonamido)phenyl) isoindolin-2-yl)butanoate;
(S)-3-Methyl-2-(1 -oxo-6-(4-(phenylmethylsulfonamido)phenyl)isoindolin-2-yl)butanoic acid;
(S)-Methyl 3-methyl-2-(6-(4-(1 -methylethylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)butanoate;
(S)-3-Methyl-2-(6-(4-(1 -methylethylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)butanoic acid;
(S)-Methyl 2-(6-(4-benzamidophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate (S)-2-(6-(4-Benzamidophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(6-(4-(4-fluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(4-Fluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(4-(trifluoromethyl)benzamido)phenyl) isoindolin-2-yl)butanoate;
(S)-3-Methyl-2-(1 -oxo-6-(4-(4-(trifluoromethyl)benzamido)phenyl)isoindolin-2-yl)butanoic acid;
(S)-Methyl 2-(6-(4-(4-methoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(4-Methoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-Methyl 2-(6-(4-(3-fluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate;
(S)-2-(6-(4-(3-Fluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-Methyl 2-(6-(4-(3-chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(3-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-Methyl 2-(6-(4-(2,4-difluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(2,4-Difluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-Methyl 3-methyl-2-(6-(4-(4-methylbenzamido)phenyl)-1 -oxoisoindolin-2-yl) butanoate;
(S)-3-Methyl-2-(6-(4-(4-methylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)butanoic acid; (S)-Methyl 2-(6-(4-(4-chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(4-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-Methyl 2-(6-(4-(4-tert-butylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(4-tert-Butylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)- Methyl 2-(6-(4-(cyclohexanecarboxamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(Cyclohexanecarboxamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)- Methyl 2-(6-(4-biphenyl-4-ylcarboxamidophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-Biphenyl-4-ylcarboxamidophenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)- Methyl 2-(6-(4-(2-naphthamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate; (S)- 2-(6-(4-(2-Naphthamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(4-pentylbenzamido)phenyl)isoindolin-2-yl) butanoate;
(S)-3-Methyl-2-(1 -oxo-6-(4-(4-pentylbenzamido)phenyl)isoindolin-2-yl)butanoic acid; (S)- Methyl 2-(6-(4-(2-fluoro-6-(trifluoromethyl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(2-Fluoro-6-(trifluoromethyl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(6-(4-(benzo[d][1 ,3]dioxole-5-carboxamido)phenyl)-1 -oxo isoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(Benzo[d][1 ,3]dioxole-5-carboxamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)- Methyl 2-(6-(4-(2,6-dichlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)- 2-(6-(4-(2,6-Dichlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)- Methyl 2-(6-(4-(2-chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate;
(S)-2-(6-(4-(2-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-Methyl 2-(6-(4-(2,4-dichlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate;
(S)- 2-(6-(4-(2,4-Dichlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)- Methyl 2-(6-(4-(4-butoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate;
(S)- 2-(6-(4-(4-Butoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-Methyl 2-(6-(4-(2,6-difluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(2,6-Difluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)- Methyl 2-(6-(4-(3,4-difluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)- 2-(6-(4-(3,4-Difluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)- Methyl 2-(6-(4-(3,4-dimethoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(3,4-Dimethoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(3,4,5-trimethoxybenzamido)phenyl)
isoindolin -2-yl)butanoate;
(S)- 3-Methyl-2-(1 -oxo-6-(4-(3,4,5-trimethoxybenzamido)phenyl)isoindolin-2-yl) butanoic acid;
(S)- Methyl 2-(6-(4-(3,5-diethoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)- 2-(6-(4-(3,5-Diethoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)- Methyl 3-methyl-2-(1 -oxo-6-(4-(3-phenoxybenzamido)phenyl)isoindolin-2-yl)butanoate;
(S)- 3-Methyl-2-(1 -oxo-6-(4-(3-phenoxybenzamido)phenyl)isoindolin-2-yl) butanoic acid;
(S)- Methyl 3-methyl-2-(1 -oxo-6-(4-(4-phenoxybenzamido)phenyl)isoindolin-2-yl)butanoate;
(S)-3-Methyl-2-(1 -oxo-6-(4-(4-phenoxybenzamido)phenyl)isoindolin-2-yl) butanoic acid;
(S)- Methyl 3-methyl-2-(1 -oxo-6-(4-(2-phenoxybenzamido)phenyl)isoindolin-2-yl)butanoate;
(S)- 3-Methyl-2-(1 -oxo-6-(4-(2-phenoxybenzamido)phenyl)isoindolin-2-yl) butanoic acid;
(S)- Methyl 3-methyl-2-(1 -oxo-6-(4-(2,4,6-trimethylbenzamido)phenyl)isoindolin-2-yl)butanoate;
(S)-3-Methyl-2-(1 -oxo-6-(4-(2,4,6-trimethylbenzamido)phenyl)isoindolin-2-yl) butanoic acid;
(S)-Methyl 2-(6-(4-(2,4-dimethoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)- 2-(6-(4-(2,4-Dimethoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(4-(trifluoromethoxy)benzamido)phenyl) isoindolin-2-yl)butanoate;
(S)-3-Methyl-2-(1 -oxo-6-(4-(4-(trifluoromethoxy)benzamido)phenyl)isoindolin-2-yl)butanoic acid;
(S)- Methyl 2-(6-(4-(2-methoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)- 2-(6-(4-(2-Methoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-Methyl 2-(6-(4-(4-fluoro-3-methylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)- 2-(6-(4-(4-Fluoro-3-methylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)- Methyl 2-(6-(4-(4-butylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate;
(S)- 2-(6-(4-(4-Butylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-Methyl 2-(6-(4-(2,6-difluoro-3-methylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)- 2-(6-(4-(2,6-Difluoro-3-methylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)- Methyl 2-(6-(4-(4-ethylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate;
(S)-2-(6-(4-(4-Ethylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)- Methyl 3-methyl-2-(1 -oxo-6-(4-(4-propylbenzamido)phenyl)isoindolin-2-yl) butanoate;
(S)- 3-Methyl-2-(1 -oxo-6-(4-(4-propylbenzamido)phenyl)isoindolin-2-yl)butanoic acid; (S)-Methyl 3-methyl-2-(6-(4-(4-octylbenzamido)phenyl)-1 -oxoisoindolin-2-yl) butanoate;
(S)- 3-Methyl-2-(6-(4-(4-octylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)butanoic acid; (S)- Methyl 2-(6-(4-(4-cyclohexylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)- 2-(6-(4-(4-Cyclohexylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)- Methyl 3-methyl-2-(1 -oxo-6-(4-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydro
naphthalene-2-carboxamido)phenyl)isoindolin-2-yl)butanoate;
(S)-3-Methyl-2-(1 -oxo-6-(4-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydro naphthalene-2-carboxamido)phenyl)isoindolin-2-yl)butanoic acid;
(S)- Methyl 2-(6-(4-(1 -naphthamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate; (S)- 2-(6-(4-(1 -Naphthamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-Methyl 2-(6-(4-(3,5-dimethoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(3,5-Dimethoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-Methyl 2-(6-(4-(4-hexylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate;
(S)- 2-(6-(4-(4-Hexylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-Methyl 2-(6-(4-(4-heptylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate;
(S)- 2-(6-(4-(4-Heptylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)- Methyl 3-methyl-2-(6-(4-(4-nonylbenzamido)phenyl)-1 -oxoisoindolin-2-yl) butanoate;
(S)- 3-Methyl-2-(6-(4-(4-nonylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)butanoic acid; (S)- Methyl 2-(6-(4-(4-decylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate;
(S)- 2-(6-(4-(4-Decylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid; (S)- (Methyl 2-(6-(4-(adamentyl-2-carboxamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(Adamantyl-2-carboxamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)- Methyl 2-(6-(4-(2-fluoro-4-(trifluoromethyl)benzamido)phenyl)-1 -oxoiso indolin-2-y l)-3-methy Ibutanoate ;
(S)-2-(6-(4-(2-Fluoro-4-(trifluoromethyl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(6-(4-(2-fluoro-3-(trifluoromethyl)benzamido)phenyl)-1 -oxoiso indolin-2-yl)-3-methy Ibutanoate ;
(S)-2-(6-(4-(2-Fluoro-3-(trifluoromethyl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)- Methyl 2-(6-(4-(3-fluoro-4-(trifluoromethyl)benzamido)phenyl)-1 -oxoiso indolin-2-yl)-3-methylbutanoate;
(S)- 2-(6-(4-(3-Fluoro-4-(trifluoromethyl)benzamido)phenyl)-1 -oxoisoindolin-2-yl) -3-methylbutanoic acid;
(S)- Methyl 2-(6-(4-(4-fluoro-2-(trifluoromethyl)benzamido)phenyl)-1 -oxoiso indolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(4-Fluoro-2-(trifluoromethyl)benzamido)phenyl)-1 -oxoisoindolin-2-yl) -3-methylbutanoic acid;
(S)- Methyl 3-methyl-2-(1 -oxo-6-(4-(2-(trifluoromethyl)benzamido)phenyl)iso indolin-2-yl)butanoate;
(S)-3-Methyl-2-(1 -oxo-6-(4-(2-(trifluoromethyl)benzamido)phenyl)isoindolin-2-yl)butanoic acid;
(S)- Methyl 2-(6-(4-(2-ethoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate;
(S)-2-(6-(4-(2-Ethoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)- Methyl 2-(6-(4-(4-cyanobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate;
(S)- Methyl 2-(6-(4-(3-chloro-2-fluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-Methyl 2-(6-(4-(4-fluoro-3-(trifluoromethyl)benzamido)phenyl)-1 -oxoiso indolin-2-y l)-3-methy Ibutanoate ;
(S)-Methyl 3-methyl-2-(6-(4-(nicotinamido)phenyl)-1 -oxoisoindolin-2-yl) butanoate; (S)-3-Methyl-2-(6-(4-(nicotinamido)phenyl)-1 -oxoisoindolin-2-yl)butanoic acid;
(S)- Methyl 2-(6-(4-(2-chloronicotinamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)- 2-(6-(4-(2-Chloronicotinamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)- Methyl 3-methyl-2-(1 -oxo-5-(4-(6-(trifluoromethyl)nicotinamido)phenyl)iso indolin-2-yl)butanoate;
(S)-Methyl 2-(6-(4-(6-chloronicotinamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate;
(S)- Methyl 3-methyl-2-(6-(4-(6-morpholinonicotinamido)phenyl)-1 -oxoiso indolin-2-yl)butanoate;
(S)-3-Methyl-2-(6-(4-(6-morpholinonicotinamido)phenyl)-1 -oxoisoindolin-2-yl) butanoic acid;
(S)- Methyl 3-methyl-2-(1 -oxo-6-(4-(6-(piperidin-1 -yl)nicotinamido)phenyl)iso indolin-2-yl)butanoate;
(S)- 3-Methyl-2-(1 -oxo-6-(4-(6-(piperidin-1 -yl)nicotinamido)phenyl)isoindolin-2-yl)butanoic acid;
(S)- Methyl 3-methyl-2-(1 -oxo-6-(4-(6-(pyrrolidin-1 -yl)nicotinamido)phenyl)iso indolin-2-yl)butanoate;
(S)-3-Methyl-2-(1 -oxo-6-(4-(6-(pyrrolidin-1 -yl)nicotinamido)phenyl) isoindolin-2-yl)butanoic acid;
(S)- Methyl 3-methyl-2-(6-(4-(6-(4-methylpiperazin-1 -yl)nicotinamido)phenyl)-1 -oxoisoindolin-2-yl)butanoate;
(S)-Methyl 2-(5-(4-(3-(4-fluorophenyl) ureido) phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(5-(4-(3-(4-Fluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(5-(4-(3-(2-fluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(5-(4-(3-(2-Fluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-Methyl 2-(5-(4-(3-(3-fluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(5-(4-(3-(3-Fluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-Methyl 3-methyl-2-(1 -oxo-5-(4-(3-phenylureido)phenyl)isoindolin-2-yl) butanoate; (S)-3-Methyl-2-(1 -oxo-5-(4-(3-phenylureido)phenyl)isoindolin-2-yl)butanoic acid; (S)-Methyl 2-(5-(4-(3-benzylureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate; (S)-2-(5-(4-(3-Benzylureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-Methyl 2-(5-(4-(3-cyclohexylureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate;
(S)-2-(5-(4-(3-Cyclohexylureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid; (S)-Methyl 2-(5-(4-(3-(2,4-difluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(5-(4-(3-(2,4-Difluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(5-(4-(3-(3,4-difluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(5-(4-(3-(3,4-Difluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 3-methyl-2-(1 -oxo-5-(4-(3-p-tolylureido)phenyl)isoindolin-2-yl) butanoate; (S)-3-Methyl-2-(1 -oxo-5-(4-(3-p-tolylureido)phenyl)isoindolin-2-yl)butanoic acid; (S)-Methyl 3-methyl-2-(1 -oxo-5-(4-(3-m-tolylureido)phenyl)isoindolin-2-yl) butanoate; (S)-3-Methyl-2-(1 -oxo-5-(4-(3-m-tolylureido)phenyl)isoindolin-2-yl)butanoic acid; (S)-Methyl 3-methyl-2-(1 -oxo-5-(4-(3-(4-(trifluoromethyl)phenyl)ureido)phenyl) isoindolin-2-yl)butanoate;
(S)-3-Methyl-2-(1 -oxo-5-(4-(3-(4-(trifluoromethyl)phenyl)ureido)phenyl) isoindolin-2-yl)butanoic acid;
(S)-Methyl 3-methyl-2-(1 -oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl) isoindolin-2-yl)butanoate;
(S)-3-Methyl-2-(1 -oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl) isoindolin -2-yl)butanoic acid;
(S)-Methyl 2-(5-(4-(3-(4-methoxyphenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(5-(4-(3-(4-Methoxyphenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(5-(4-(3-(3-methoxyphenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(5-(4-(3-(3-Methoxyphenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(5-(4-(3-(4-cyanophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(5-(4-(3-(4-Cyanophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(5-(4-(3-(3-cyanophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(5-(4-(3-(3-Cyanophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(5-(4-(3-(2-fluorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(5-(4-(3-(2-Fluorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(5-(4-(3-(3-fluorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(5-(4-(3-(3-Fluorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-Methyl 2-(5-(4-(3-(4-methoxyphenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(5-(4-(3-(4-Methoxyphenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(5-(4-(3-(3-methoxyphenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(5-(4-(3-(3-Methoxyphenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-Methyl 2-(5-(4-(3-(4-chlorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(5-(4-(3-(4-Chlorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(5-(4-(3-(3-chlorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(5-(4-(3-(3-Chlorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(5-(4-(3-(4-cyanophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(5-(4-(3-(4-Cyanophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-Methyl 3-methyl-2-(1 -oxo-5-(4-(3-(2-(trifluoromethyl)phenyl)thioureido) phenyl)isoindolin-2-yl)butanoate;
(S)-3-Methyl-2-(1 -oxo-5-(4-(3-(2-(trifluoromethyl)phenyl)thioureido)phenyl) isoindolin-2-yl)butanoic acid;
(S)-Methyl 3-methyl-2-(1 -oxo-5-(4-(3-o-tolylthioureido)phenyl)isoindolin-2-yl)butanoate;
(S)-3-Methyl-2-(1 -oxo-5-(4-(3-o-tolylthioureido)phenyl)isoindolin-2-yl)butanoic acid; (S)-Methyl 3-methyl-2-(1 -oxo-5-(4-(3-p-tolylthioureido)phenyl)isoindolin-2-yl) butanoate;
(S)-3-Methyl-2-(1 -oxo-5-(4-(3-p-tolylthioureido)phenyl)isoindolin-2-yl)butanoic acid; (S)-Methyl 2-(5-(4-(3-(3-fluorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(5-(4-(3-(3-Fluorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-Methyl 2-(5-(4-(3-(3-methoxyphenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(5-(4-(3-(3-Methoxyphenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(5-(4-(3-(2-methoxyphenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(5-(4-(3-(2-Methoxyphenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 3-methyl-2-(1 -oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)thioureido) phenyl)isoindolin-2-yl)butanoate;
(S)-3-Methyl-2-(1 -oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)thioureido)phenyl) isoindolin-2-yl)butanoic acid;
(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(phenylsulfonamido)phenyl)isoindolin-2-yl)butanoate;
(S)-3-Methyl-2-(1 -oxo-6-(4-(phenylsulfonamido)phenyl)isoindolin-2-yl)butanoic acid; (S)-Methyl 2-(5-(4-(4-cyanophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(5-(4-(4-Cyanophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-Methyl 2-(5-(4-(3,4-difluorophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(5-(4-(3,4-Difluorophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(5-(4-(2,4-difluorophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(5-(4-(2,4-Difluorophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(5-(4-(3,4-dimethoxyphenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(5-(4-(3,4-Dimethoxyphenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(5-(4-(3-chlorophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(5-(4-(3-Chlorophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-Methyl 2-(5-(4-(4-methoxyphenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(5-(4-(4-Methoxyphenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 3-methyl-2-(1 -oxo-5-(4-(4-(trifluoromethyl)phenylsulfonamido) phenyl) isoindolin-2-yl)butanoate;
(S)-3-Methyl-2-(1 -oxo-5-(4-(4-(trifluoromethyl)phenylsulfonamido)phenyl) isoindolin-2-yl)butanoic acid;
(S)-Methyl 3-methyl-2-(1 -oxo-5-(4-(phenylmethylsulfonamido)phenyl) isoindolin-2-yl)butanoate;
(S)-3-Methyl-2-(1 -oxo-5-(4-(phenylmethylsulfonamido) phenyl) isoindolin-2-yl)butanoic acid;
(S)-Methyl 2-(5-(4-(cyclohexanesulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(5-(4-(Cyclohexanesulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(5-(4-benzamidophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(5-(4-Benzamidophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(5-(4-(4-fluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate;
(S)-2-(5-(4-(4-Fluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-Methyl 3-methyl-2-(1 -oxo-5-(4-(4-(trifluoromethyl)benzamido)phenyl) isoindolin-2-yl)butanoate;
(S)-3-Methyl-2-(1 -oxo-5-(4-(4-(trifluoromethyl)benzamido)phenyl)isoindolin-2-y/l)butanoic acid;
(S)-Methyl 2-(5-(4-(4-methoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(5-(4-(4-Methoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-Methyl 2-(5-(4-(3-fluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate;
(S)-2-(5-(4-(3-Fluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-Methyl 2-(5-(4-(3-chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate;
(S)-2-(5-(4-(3-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-Methyl 2-(5-(4-(2,4-difluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(5-(4-(2,4-Difluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 3-methyl-2-(5-(4-(4-methylbenzamido)phenyl)-1 -oxoisoindolin-2-yl) butanoate;
(S)-3-Methyl-2-(5-(4-(4-methylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)butanoic acid; (S)-Methyl 2-(5-(4-(4-chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate;
(S)-2-(5-(4-(4-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-Methyl 2-(5-(4-(4-tert-butylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(5-(4-(4-tert-Butylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-Methyl 3-methyl-2-(1 -oxo-5-(4-(4-pentylbenzamido)phenyl)isoindolin-2-yl) butanoate;
(S)-3-Methyl-2-(1 -oxo-5-(4-(4-pentylbenzamido)phenyl)isoindolin-2-yl)butanoic acid; (R)-Methyl-3-methyl-2-(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido) phenyl) isoindolin-2-yl)butanoate;
(R)-3-Methyl-2-(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)iso indolin-2-yl)butanoic acid;
Methyl 2-(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)acetate;
2-(1 -Oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)acetic acid; (S)-Methyl 2-(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)propanoate;
(S)-2-(1 -Oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl) propanoic acid;
Methyl 2-methyl-2-(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl) isoindolin-2-yl)propanoate;
2-Methyl-2-(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)propanoic acid;
Methyl 1 -(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl) cyclopentanecarboxy late ;
1 - (1 -Oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)
cyclopentanecarboxylic acid;
(S)-Methyl 2-(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)- 2- phenylacetate;
(S)-2-(1 -Oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)-2-phenylacetic acid;
Methyl 4-(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl) butanoate;
4-(1 -Oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)butanoic acid;
(S)-Methyl 4-methyl-2-(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl) isoindolin-2-yl)pentanoate;
(S)-4-Methyl-2-(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)iso indolin-2-yl)pentanoic acid;
(S)-Methyl 3-methoxy-2-(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)
phenyl)isoindolin-2-yl)propanoate;
(S)-3-Methoxy-2-(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)iso indolin-2-yl)propanoic acid;
(R)-Methyl 3-methyl-2-(1 -oxo-5-(4-(3-(3-(trifluoromethyl)phenyl) ureido)phenyl) isoindolin-2-yl)butanoate;
(R)-3-Methyl-2-(1 -oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl) isoindolin-2-yl)butanoic acid;
Methyl 2-(1 -oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)acetate;
2-(1 -Oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)acetic acid; (S)-Methyl 2-(1 -oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)propanoate;
(S)-2-(1 -Oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl) propanoic acid;
Methyl 1 -(1 -oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)cyclopentanecarboxylate;
1 - (1 -Oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)
cyclopentanecarboxylic acid;
(S)-Methyl 2-(1 -oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)- 2- phenylacetate;
(S)-2-(1 -Oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)-2-phenylacetic acid;
Methyl 4-(1 -oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl) butanoate;
4-(1 -Oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl) butanoic acid;
Ethyl 3-(1 -oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl) propanoate;
3- (1 -Oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)propanoic acid;
(S)-Methyl 2-(1 -oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)-3-phenylpropanoate;
(S)-2-(1 -Oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)-3-phenylpropanoic acid;
(S)-Methyl 3-methoxy-2-(1 -oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido) phenyl) isoindolin-2-yl)propanoate;
(S)-3-Methoxy-2-(1 -oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl) isoindolin-2-yl)propanoic acid;
(S)-Methyl 4-methyl-2-(1 -oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl) isoindolin-2-yl)pentanoate;
(S)-4-Methyl-2-(1 -oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)iso indolin-2-yl)pentanoic acid;
(S)- Methyl 2-(6-(5-(3-(2-chlorophenyl)ureido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)- 2-(6-(5-(3-(2-Chlorophenyl)ureido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(6-(5-(3-(4-chloro-2-phenoxyphenyl)ureido)pyridin-2-yl)-1 -oxoiso indolin-2-yl)-3-methylbutanoate;
(S)- 2-(6-(5-(3-(4-Chloro-2-phenoxyphenyl)ureido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(6-(5-(3-(3,4-dimethylphenyl)ureido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)- 2-(6-(5-(3-(3,4-Dimethylphenyl)ureido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)- Methyl 2-(6-(5-(3-(3,4-difluorophenyl)ureido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)- 2-(6-(5-(3-(3,4-Difluorophenyl)ureido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(6-(5-(3-(2,3-dihydro-1 H-inden-5-yl)ureido)pyridin-2-yl)-1 -oxoiso indolin-2-yl)-3-methylbutanoate;
(S)- 2-(6-(5-(3-(2,3-Dihydro-1 H-inden-5-yl)ureido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(6-(5-(4-tert-butylbenzamido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(5-(4-tert-Butylbenzamido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)- Methyl 3-methyl-2-(1 -oxo-6-(5-(4-pentylbenzamido)pyridin-2-yl)isoindolin-2-yl)butanoate;
(S)- 3-Methyl-2-(1 -oxo-6-(5-(4-pentylbenzamido)pyridin-2-yl)isoindolin-2-yl)butanoic acid;
(S)-Methyl 2-(6-(5-biphenyl-4-ylcarboxamidopyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)- 2-(6-(5-Biphenyl-4-ylcarboxamidopyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(6-(5-(2-naphthamido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methyl butanoate;
(S)-2-(6-(5-(2-Naphthamido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)- Methyl 2-(6-(5-(4-butoxybenzamido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)- 2-(6-(5-(4-Butoxybenzamido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)- Methyl 2-(6-(4-(3-(2-chlorophenyl)ureido)-2-(trifluoromethyl)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)- 2-(6-(4-(3-(2-Chlorophenyl)ureido)-2-(trifluoromethyl)phenyl)-1 -oxoiso indolin-2-yl)-3-methylbutanoic acid;
(S)- Methyl 2-(6-(4-(3-(3,4-difluorophenyl)ureido)-2-(trifluoromethyl)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)- 2-(6-(4-(3-(3,4-Difluorophenyl)ureido)-2-(trifluoromethyl)phenyl)-1 -oxoiso indolin- 2- yl)-3-methylbutanoic acid;
(S)- Methyl 2-(6-(4-(3-(2,3-dihydro-1 H-inden-5-yl)ureido)-2-(trifluoromethyl) phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(3-(2,3-Dihydro-1 H-inden-5-yl)ureido)-2-(trifluoromethyl)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)- Methyl 2-(6-(4-(3-(3,4-dimethylphenyl)ureido)-2-(trifluoromethyl)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)- 2-(6-(4-(3-(3,4-Dimethylphenyl)ureido)-2-(trifluoromethyl)phenyl)-1 -oxoiso indolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(6-(4-(4-tert-butylbenzamido)-2-(trifluoromethyl)phenyl)-1 -oxoiso indolin-2-yl)-3-methylbutanoate;
(S)- 2-(6-(4-(4-tert-Butylbenzamido)-2-(trifluoromethyl)phenyl)-1 -oxoisoindolin-2-yl)- 3- methylbutanoic acid;
(S)- Methyl 2-(6-(4-biphenyl-4-ylcarboxamido-2-(trifluoromethyl)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)- 2-(6-(4-Biphenyl-4-ylcarboxamido-2-(trifluoromethyl)phenyl)-1 -oxoiso indolin-2-yl)-3-methylbutanoic acid;
(S)- Methyl 2-(6-(4-(2-naphthamido)-2-(trifluoromethyl)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)- 2-(6-(4-(2-Naphthamido)-2-(trifluoromethyl)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(4-pentylbenzamido)-2-(trifluoromethyl) phenyl)isoindolin-2-yl)butanoate;
(S)- 3-Methyl-2-(1 -oxo-6-(4-(4-pentylbenzamido)-2-(trifluoromethyl) phenyl) isoindolin-2-yl)butanoic acid;
(S)- Methyl 2-(6-(4-(4-butoxybenzamido)-2-(trifluoromethyl)phenyl)-1 -oxoiso indolin-2-yl)-3-methylbutanoate;
(S)- 2-(6-(4-(4-Butoxybenzamido)-2-(trifluoromethyl)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(6-(4-(3-(3,4-dimethylphenyl)ureido)-3-fluorophenyl)-1 -oxoiso indolin-2-y l)-3-methy Ibutanoate ;
(S)-2-(6-(4-(3-(3,4-Dimethylphenyl)ureido)-3-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)- Methyl 2-(6-(4-(3-(2,3-dihydro-1 H-inden-5-yl)ureido)-3-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)- 2-(6-(4-(3-(2,3-Dihydro-1 H-inden-5-yl)ureido)-3-fluorophenyl)-1 -oxoiso indolin-2-yl)-3-methylbutanoic acid;
(S)- Methyl 2-(6-(4-(3-(3,4-difluorophenyl)ureido)-3-fluorophenyl)-1 -oxoiso indolin-2-yl)-3-methy Ibutanoate ;
(S)- 2-(6-(4-(3-(3,4-Difluorophenyl)ureido)-3-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)- Methyl 2-(6-(4-(3-(2-chlorophenyl)ureido)-3-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(3-(2-Chlorophenyl)ureido)-3-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)- Methyl 2-(6-(4-(4-tert-butylbenzamido)-3-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)- 2-(6-(4-(4-tert-Butylbenzamido)-3-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(6-(3-fluoro-4-(4-pentylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(3-Fluoro-4-(4-pentylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(6-(4-biphenyl-4-ylcarboxamido-3-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)- 2-(6-(4-Biphenyl-4-ylcarboxamido-3-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)- Methyl 2-(6-(4-(2-naphthamido)-3-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)- 2-(6-(4-(2-Naphthamido)-3-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)- Methyl 2-(6-(4-(4-butoxybenzamido)-3-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)- 2-(6-(4-(4-Butoxybenzamido)-3-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-Methyl 2-(6-(4-(4-tert-butylbenzamido)-2-methoxyphenyl)-1 -oxoiso indolin -2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(4-tert-Butylbenzamido)-2-methoxyphenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(6-(4-biphenyl-4-ylcarboxamido-2-methoxyphenyl)-1 -oxoiso indolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-Biphenyl-4-ylcarboxamido-2-methoxyphenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(6-(4-(4-butoxybenzamido)-2-methoxyphenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(4-Butoxybenzamido)-2-methoxyphenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(6-(2-methoxy-4-(4-pentylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(2-Methoxy-4-(4-pentylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(6-(2-methoxy-4-(4-(trifluoromethoxy)benzamido)phenyl)-1 -oxo isoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(2-Methoxy-4-(4-(trifluoromethoxy)benzamido)phenyl)-1 -oxoiso indolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(6-(4-(4-tert-butylbenzamido)-2-methylphenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(4-tert-Butylbenzamido)-2-methylphenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(6-(4-biphenyl-4-ylcarboxamido-2-methylphenyl)-1 -oxoiso indolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-Biphenyl-4-ylcarboxamido-2-methylphenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(6-(4-(4-butoxybenzamido)-2-methylphenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(4-Butoxybenzamido)-2-methylphenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 3-methyl-2-(6-(2-methyl-4-(4-pentylbenzamido)phenyl)-1 -oxoiso indolin-2-yl)butanoate;
(S)-3-Methyl-2-(6-(2-methyl-4-(4-pentylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)butanoic acid;
(S)-Methyl 3-methyl-2-(6-(2-methyl-4-(4-(trifluoromethoxy)benzamido) phenyl)-1 -oxoisoindolin-2-yl)butanoate;
(S)-3-Methyl-2-(6-(2-methyl-4-(4-(trifluoromethoxy)benzamido)phenyl)-1 -oxoisoindolin-2-yl)butanoic acid;
(S)-Methyl 2-(6-(4-(4-tert-butylbenzamido)-2-chlorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(4-tert-Butylbenzamido)-2-chlorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(6-(4-biphenyl-4-ylcarboxamido-2-chlorophenyl)-1 -oxoiso indolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-Biphenyl-4-ylcarboxamido-2-chlorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(6-(4-(4-butoxybenzamido)-2-chlorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(4-Butoxybenzamido)-2-chlorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(6-(2-chloro-4-(4-pentylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(2-Chloro-4-(4-pentylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(6-(2-chloro-4-(4-(trifluoromethoxy)benzamido)phenyl)-1 -oxo isoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(2-Chloro-4-(4-(trifluoromethoxy)benzamido)phenyl)-1 -oxoiso indolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(6-(6-(4-tert-butylbenzamido)pyridin-3-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(6-(4-tert-Butylbenzamido)pyridin-3-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(6-(6-biphenyl-4-ylcarboxamidopyridin-3-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-Methyl 3-methyl-2-(1 -oxo-6-(6-(4-pentylbenzamido)pyridin-3-yl)iso indolin-2-yl)butanoate;
(S)-Methyl 3-methyl-2-(1 -oxo-6-(6-(4-(trifluoromethoxy)benzamido)pyridin-3-yl)isoindolin-2-yl)butanoate;
(S)-Methyl 2-(6-(6-(4-tert-butylbenzamido)pyridazin-3-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(6-(4-tert-Butylbenzamido)pyridazin-3-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 3-methyl-2-(1 -oxo-6-(6-(4-pentylbenzamido)pyridazin-3-yl)iso indolin-2-yl)butanoate;
(S)-3-Methyl-2-(1 -oxo-6-(6-(4-pentylbenzamido)pyridazin-3-yl)isoindolin-2-yl)butanoic acid;
(S)-Methyl 3-methyl-2-(1 -oxo-6-(6-(4-(trifluoromethoxy)benzamido)pyridazin-3-yl) isoindolin-2-yl)butanoate;
(S)-3-Methyl-2-(1 -oxo-6-(6-(4-(trifluoromethoxy)benzamido)pyridazin-3-yl)isoindolin-2-yl)butanoic acid;
(S)-Methyl 2-(6-(5-(4-tert-butylbenzamido)pyrazin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(5-(4-tert-Butylbenzamido)pyrazin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(6-(5-biphenyl-4-ylcarboxamidopyrazin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(5-Biphenyl-4-ylcarboxamidopyrazin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(6-(5-(4-butoxybenzamido)pyrazin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(5-(4-Butoxybenzamido)pyrazin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 3-methyl-2-(1 -oxo-6-(5-(4-pentylbenzamido)pyrazin-2-yl)isoindolin-2-yl)butanoate;
(S)-3-Methyl-2-(1 -oxo-6-(5-(4-pentylbenzamido)pyrazin-2-yl)isoindolin-2-yl)butanoic acid;
(S)-Methyl 3-methyl-2-(1 -oxo-6-(5-(4-(trifluoromethoxy)benzamido)pyrazin-2-yl)isoindolin-2-yl)butanoate;
(S)-3-Methyl-2-(1 -oxo-6-(5-(4-(trifluoromethoxy)benzamido)pyrazin-2-yl)isoindolin-2-yl)butanoic acid;
Methyl 2-(6-(4-([1 ,1 '-biphenyl]-4-ylcarboxamido)phenyl)-1 -oxoisoindolin-2-yl)-2-methylpropanoate;
2-(6-(4-([1 ,1 '-Biphenyl]-4-ylcarboxamido)phenyl)-1 -oxoisoindolin-2-yl)-2-methyl propanoic acid;
Methyl 2-(6-(4-(4-(tert-butyl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)-2-methyl propanoate;
2-(6-(4-(4-(tert-Butyl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)-2-methyl propanoic acid;
Methyl 2-(6-(4-(4-chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-2-methyl propanoate;
2-(6-(4-(4-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-2-methylpropanoic acid; Methyl 2-methyl-2-(1 -oxo-6-(4-(4-(trifluoromethoxy)benzamido)phenyl)iso indolin-2-yl)propanoate
2-Methyl-2-(1 -oxo-6-(4-(4-(trifluoromethoxy)benzamido)phenyl)isoindolin-2-yl)propanoic acid;
Methyl 2-methyl-2-(1 -oxo-6-(4-(4-pentylbenzamido)phenyl)isoindolin-2-yl) propanoate;
2-Methyl-2-(1 -oxo-6-(4-(4-pentylbenzamido)phenyl)isoindolin-2-yl)propanoic acid;
Methyl 1 -(6-(4-([1 ,1 '-biphenyl]-4-ylcarboxamido)phenyl)-1 -oxoisoindolin-2-yl) cyclopentanecarboxy late ;
1 -(6-(4-([1 ,1 '-Biphenyl]-4-ylcarboxamido)phenyl)-1 -oxoisoindolin-2-yl) cyclopentane carboxylic acid;
Methyl 1 -(6-(4-(4-(tert-butyl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)
cyclopentanecarboxy late ;
1 -(6-(4-(4-(tert-Butyl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclopentane carboxylic acid;
Methyl 1 -(6-(4-(4-chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclopentane carboxylate;
1 -(6-(4-(4-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclopentane carboxylic acid;
Methyl 1 -(1 -oxo-6-(4-(4-(trifluoromethoxy)benzamido)phenyl)isoindolin-2-yl) cyclopentanecarboxy late ;
1 -(1 -Oxo-6-(4-(4-(trifluoromethoxy)benzamido)phenyl)isoindolin-2-yl) cyclopentane carboxylic acid;
Methyl 1 -(1 -oxo-6-(4-(4-pentylbenzamido)phenyl)isoindolin-2-yl)cyclopentane carboxylate;
1 -(1 -Oxo-6-(4-(4-pentylbenzamido)phenyl)isoindolin-2-yl)cyclopentane carboxylic acid;
(R)-Methyl 2-(6-(4-([1 ,1 '-biphenyl]-4-ylcarboxamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(R)-2-(6-(4-([1 ,1 '-Biphenyl]-4-ylcarboxamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
Methyl 3-(6-(4-([1 ,1 '-biphenyl]-4-ylcarboxamido)phenyl)-1 -oxoisoindolin-2-yl) cyclohexanecarboxylate;
3-(6-(4-([1 ,1 '-Biphenyl]-4-ylcarboxamido)phenyl)-1 -oxoisoindolin-2-yl)cyclo hexane carboxylic acid;
Methyl 3-(6-(4-(3-chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclohexane carboxylate;
3-(6-(4-(3-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclohexane carboxylic acid;
Methyl 3-(6-(4-(4-chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclohexane carboxylate;
3-(6-(4-(4-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclohexane carboxylic acid;
Methyl 3-(1 -oxo-6-(4-(4-(trifluoromethyl)benzamido)phenyl)isoindolin-2-yl) cyclohexanecarboxylate;
3-(1 -Oxo-6-(4-(4-(trifluoromethyl)benzamido)phenyl)isoindolin-2-yl)cyclo
hexanecarboxylic acid;
Methyl 3-(6-(4-(5-methyl-2-phenyloxazole-4-carboxamido)phenyl)-1 -oxo isoindolin-2-yl)cyclohexanecarboxylate;
3-(6-(4-(5-Methyl-2-phenyloxazole-4-carboxamido)phenyl)-1 -oxoisoindolin-2-yl)cyclohexanecarboxylic acid ;
(1 r,4r)-Methyl 4-(6-(4-([1 ,1 '-biphenyl]-4-ylcarboxamido)phenyl)-1 -oxoisoindolin-2-yl)cyclohexanecarboxylate;
(1 r,4r)-4-(6-(4-([1 ,1 '-Biphenyl]-4-ylcarboxamido)phenyl)-1 -oxoisoindolin-2-yl) cyclohexanecarboxylic acid;
(1 r,4r)-Methyl 4-(6-(4-(3-chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl) cyclo hexanecarboxylate;
(1 r,4r)-4-(6-(4-(3-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclohexane carboxylic acid;
(1 r,4r)-Methyl 4-(6-(4-(4-chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)
cyclohexanecarboxylate;
(1 r,4r)-4-(6-(4-(4-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclohexane carboxylic acid;
(1 r,4r)-Methyl 4-(1 -oxo-6-(4-(4-(trifluoromethyl)benzamido)phenyl)isoindolin-2-yl)cyclohexanecarboxylate;
(1 r,4r)-4-(1 -Oxo-6-(4-(4-(trifluoromethyl)benzamido)phenyl)isoindolin-2-yl) cyclohexanecarboxylic acid;
(1 r,3s,5R,7S)-Methyl 3-(6-(4-(3-chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)adamantane-1 -carboxylate;
(1 r,3s,5R,7S)-3-(6-(4-(3-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)
adamantane-1 -carboxylic acid;
(1 r,3s,5R,7S)-Methyl 3-(6-(4-(4-chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)adamantane-1 -carboxylate;
(1 r,3s,5R,7S)-3-(6-(4-(4-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)
adamantane-1 -carboxylic acid;
(1 r,3s,5R,7S)-Methyl 3-(1 -oxo-6-(4-(4-(trifluoromethyl)benzamido)phenyl) isoindolin-2-yl)adamantane-1 -carboxylate;
(1 r,3s,5R7S)-3-(1 -Oxo-6-(4-(4-(trifluoromethyl)benzamido)phenyl)isoindolin-2-yl)adamantane-1 -carboxylic acid;
(1 r,3s,5R,7S)-3-(6-(4-(4-Methylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)
adamantane-1 -carboxylic acid;
Methyl 1 -(6-(4-([1 ,1 '-biphenyl]-4-ylcarboxamido)phenyl)-1 -oxoisoindolin-2-yl) cyclobutanecarboxylate;
1 -(6-(4-([1 ,1 '-Biphenyl]-4-ylcarboxamido)phenyl)-1 -oxoisoindolin-2-yl) cyclo butanecarboxylic acid;
Methyl 1 -(6-(4-(4-chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl) cyclobutane carboxylate;
1 -(6-(4-(4-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclobutane carboxylic acid;
Methyl 1 -(1 -Oxo-6-(4-(4-(trifluoromethyl)benzamido)phenyl)isoindolin-2-yl) cyclobutanecarboxylate;
1 -(1 -Oxo-6-(4-(4-(trifluoromethyl)benzamido)phenyl)isoindolin-2-yl) cyclo
butanecarboxylic acid;
Methyl 1 -(6-(4-(4-methylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclobutane carboxylate;
1 -(6-(4-(4-Methylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclobutane carboxylic acid;
Methyl 1 -(6-(4-biphenyl-4-ylcarboxamidophenyl)-1 -oxoisoindolin-2-yl) cyclo propanecarboxylate;
1 -(6-(4-([1 ,1 '-Biphenyl]-4-ylcarboxamido)phenyl)-1 -oxoisoindolin-2-yl)
cyclopropanecarboxylic acid;
Methyl 1 -(6-(4-(4-chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclopropane carboxylate;
1 -(6-(4-(4-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclopropane carboxylic acid;
Methyl 1 -(1 -oxo-6-(4-(4-(trifluoromethyl)benzamido)phenyl)isoindolin-2-yl) cyclopropane carboxylate;
1 -(1 -Oxo-6-(4-(4-(trifluoromethyl)benzamido)phenyl)isoindolin-2-yl)cyclo propane carboxylic acid;
(1 S,2R)-Methyl 2-(6-(4-([1 ,1 '-biphenyl]-4-ylcarboxamido)phenyl)-1 -oxo isoindolin-2-yl)cyclopentanecarboxylate;
(1 S,2R)-2-(6-(4-([1 ,1 '-Biphenyl]-4-ylcarboxamido)phenyl)-1 -oxoisoindolin-2-yl)cyclopentanecarboxylic acid;
(1 S,2R)-Methyl 2-(6-(4-(4-chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)
cyclopentanecarboxy late ;
(1 S,2R)-2-(6-(4-(4-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclopentane carboxylic acid;
(1 S,2R)-Methyl 2-(1 -oxo-6-(4-(4-(trifluoromethyl)benzamido)phenyl)isoindolin-2-yl)cyclopentanecarboxylate;
(1 S,2R)-2-(1 -Oxo-6-(4-(4-(trifluoromethyl)benzamido)phenyl)isoindolin-2-yl) cyclopentanebcarboxylic acid;
(S)-Methyl 2-(6-(4-([1 ,1 '-biphenyl]-4-ylcarboxamido)-2-fluorophenyl)-1 -oxo isoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-([1 ,1 '-Biphenyl]-4-ylcarboxamido)-2-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(6-(4-(4-(tert-butyl)benzamido)-2-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(4-(tert-Butyl)benzamido)-2-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(6-(4-(4-chlorobenzamido)-2-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(4-Chlorobenzamido)-2-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-Methyl 2-(6-(2-fluoro-4-(4-(trifluoromethoxy)benzamido)phenyl)-1 -oxo isoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(2-Fluoro-4-(4-(trifluoromethoxy)benzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(6-(2-fluoro-4-(4-pentylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(2-Fluoro-4-(4-pentylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(5-phenylthiazole-2-carboxamido)phenyl) isoindolin-2-yl)butanoate;
(S)-3-Methyl-2-(1 -oxo-6-(4-(5-phenylthiazole-2-carboxamido)phenyl)isoindolin-2-yl)butanoic acid;
(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(5-phenyloxazole-2-carboxamido)phenyl) isoindolin-2-yl)butanoate;
(S)-3-Methyl-2-(1 -oxo-6-(4-(5-phenyloxazole-2-carboxamido)phenyl) isoindolin-2-yl)butanoic acid;
(S)-Methyl 2-(6-(4-(3-(4-fluorophenyl)isoxazole-5-carboxamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(3-(4-Fluorophenyl)isoxazole-5-carboxamido)phenyl)-1 -oxo isoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(6-(4-(3-(4-chlorophenyl)isoxazole-5-carboxamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(3-(4-Chlorophenyl)isoxazole-5-carboxamido)phenyl)-1 -oxo
isoindolin-2-yl)-3-methylbutanoic acid ;
(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(3-(4-(trifluoromethyl)phenyl)isoxazole-5-carboxamido)phenyl)isoindolin-2-yl)butanoate;
(S)-3-Methyl-2-(1 -oxo-6-(4-(3-(4-(trifluoromethyl)phenyl)isoxazole-5-carboxamido)phenyl)isoindolin-2-yl)butanoic acid;
(S)-Methyl 3-methyl-2-(6-(4-(4-(oxazol-5-yl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)butanoate;
(S)-3-Methyl-2-(6-(4-(4-(oxazol-5-yl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)butanoic acid;
(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(4-phenylthiazole-2-carboxamido)phenyl) isoindolin-2-yl)butanoate;
(S)-3-methyl-2-(1 -oxo-6-(4-(4-phenylthiazole-2-carboxamido)phenyl)isoindolin-2-yl)butanoic acid;
(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(5-phenyl-1 ,3,4-oxadiazole-2-carboxamido) phenyl)isoindolin-2-yl)butanoate;
(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(5-phenyl-1 ,3,4-thiadiazole-2-carboxamido) phenyl)isoindolin-2-yl)butanoate;
(S)-3-Methyl-2-(1 -oxo-6-(4-(5-phenyl-1 ,3,4-thiadiazole-2-carboxamido)
phenyl)isoindolin-2-yl)butanoic acid;
(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(5-phenyl-4H-1 ,2,4-triazole-3-carboxamido) phenyl)isoindolin-2-yl)butanoate;
(S)-3-Methyl-2-(1 -oxo-6-(4-(5-phenyl-4H-1 ,2,4-triazole-3-carboxamido) phenyl) isoindolin-2-yl)butanoic acid;
(S)-Methyl 2-(6-(4-(4-(2-cyanopropan-2-yl)benzamido)phenyl)-1 -oxoisoindolin-2-yl) 3-methylbutanoate;
(S)-2-(6-(4-(4-(2-Cyanopropan-2-yl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(6-(4-(4-(3-cyanopentan-3-yl)benzamido)phenyl)-1 -oxoisoindolin-2-yl) 3-methylbutanoate;
(S)-2-(6-(4-(4-(3-Cyanopentan-3-yl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 3-methyl-2-(1 -oxo-6-(5-(5-phenyloxazole-2-carboxamido)pyridin-2-yl)isoindolin-2-yl)butanoate;
(S)-3-Methyl-2-(1 -oxo-6-(5-(5-phenyloxazole-2-carboxamido)pyridin-2-yl) isoindolin 2-yl)butanoic acid;
(S)-Methyl 3-methyl-2-(1 -oxo-6-(5-(5-phenylthiazole-2-carboxamido)pyridin-2-yl)isoindolin-2-yl)butanoate;
(S)-3-Methyl-2-(1 -oxo-6-(5-(5-phenylthiazole-2-carboxamido)pyridin-2-yl) isoindolin 2-yl)butanoic acid;
(S)-Methyl 2-(6-(5-(3-(4-fluorophenyl)isoxazole-5-carboxamido)pyridin-2-yl)-1 -oxo isoindolin-2-yl)-3-methylbutanaote;
(S)-2-(6-(5-(3-(4-Fluorophenyl)isoxazole-5-carboxamido)pyridin-2-yl)-1 -oxo isoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 2-(6-(4-(4-(1 ,3,4-oxadiazol-2-yl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(4-(1 ,3,4-Oxadiazol-2-yl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-Methyl 3-methyl-2-(6-(4-(5-methyl-2-phenyloxazole-4-carboxamido) phenyl)-1 -oxoisoindolin-2-yl)butanoate;
(S)-3-Methyl-2-(6-(4-(5-methyl-2-phenyloxazole-4-carboxamido)phenyl)-1 -oxoisoindolin-2-yl)butanoic acid;
(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(2-phenyl-5-(trifluoromethyl)oxazole-4-carboxamido)phenyl)isoindolin-2-yl)butanoate;
(S)-3-Methyl-2-(1 -oxo-6-(4-(2-phenyl-5-(trifluoromethyl)oxazole-4-carboxamido) phenyl)isoindolin-2-yl)butanoic acid;
(S)-Methyl 3-methyl-2-(6-(2-methyl-4-(4-pentylbenzamido)phenyl)-1 -oxoiso indolin-2-yl)butanoate;
(S)-3-Methyl-2-(1 -oxo-6-(4-(4-(thiazol-2-yl)benzamido)phenyl)isoindolin-2-yl) butanoic acid;
(S)-Methyl 2-(6-(4-(5-butylpicolinamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoate;
(S)-2-(6-(4-(5-Butylpicolinamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(quinoline-3-carboxamido)phenyl)isoindolin-2-yl)butanoate;
(S)-3-Methyl-2-(1 -oxo-6-(4-(quinoline-3-carboxamido)phenyl)isoindolin-2-yl) butanoic acid;
(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(4-(pyrimidin-5-yl)benzamido) phenyl) isoindolin-2-yl)butanoate;
(S)-3-Methyl-2-(1 -oxo-6-(4-(4-(pyrimidin-5-yl)benzamido)phenyl)isoindolin-2-yl)butanoic acid;
(S)-Methyl 3-methyl-2-(6-(5-(5-methyl-2-phenyloxazole-4-carboxamido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)butanoate;
(S)-3-Methyl-2-(6-(5-(5-methyl-2-phenyloxazole-4-carboxamido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)butanoic acid;
(S)-Methyl 3-methyl-2-(1 -oxo-6-(5-(2-phenyl-5-(trifluoromethyl)oxazole-4-carboxamido)pyridin-2-yl)isoindolin-2-yl)butanoate;
(S)-3-Methyl-2-(1 -oxo-6-(5-(2-phenyl-5-(trifluoromethyl)oxazole-4-carboxamido) pyridin-2-yl)isoindolin-2-yl)butanoic acid;
(S)-Methyl 3-methyl-2-(1 -oxo-6-(4-(2-phenylacetamido)phenyl)isoindolin-2-yl)butanoate;
(S)-3-Methyl-2-(1 -oxo-6-(4-(2-phenylacetamido)phenyl)isoindolin-2-yl)butanoic acid; Methyl 2-(5-(4-biphenyl-4-ylcarboxamidophenyl)-1 ,3-dioxoisoindolin-2-yl)-3-methyl butanoate;
Methyl 2-(5-(4-(4-tert-butylbenzamido)phenyl)-1 ,3-dioxoisoindolin-2-yl)-3-methyl butanoate;
Methyl 2-(5-(4-(2,4-dimethoxybenzamido)phenyl)-1 ,3-dioxoisoindolin-2-yl)-3-methylbutanoate;
Methyl 2-(5-(4-(3-(2-chlorophenyl)ureido)phenyl)-1 ,3-dioxoisoindolin-2-yl)-3-methylbutanoate;
Methyl 2-(5-(4-(3-(3,4-dimethylphenyl)ureido)phenyl)-1 ,3-dioxoisoindolin-2-yl)-3-methylbutanoate;
Methyl 2-(5-(4-(4-tert-butylbenzamido)phenyl)isoindolin-2-yl)-3-methyl butanoate; Methyl 3-methyl-2-(5-(4-(4-pentylbenzamido)phenyl)isoindolin-2-yl)butanoate;
Methyl 2-(5-(4-biphenyl-4-ylcarboxamidophenyl)isoindolin-2-yl)-3-methyl butanoate; Methyl 2-(5-(4-(2,4-dimethoxyphenylsulfonamido)phenyl)isoindolin-2-yl)-3-methyl butanoate; and
Methyl 3-methyl-2-(5-(4-(3-(2-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)butanoate;
or a stereoisomer, tautomer or a pharmaceutically acceptable salt, solvate, polymorph, prodrug, carboxylic acid isostere or N-oxide thereof.
20. The compound of formula 1 , formula 1 a or formula 1 b, according to any one of the claims 1 to 19, selected from:
(S)-2-(6-(4-(3-(4-Fluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-2-(6-(4-(3-(2,4-Difluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(6-(4-(3-(2-Fluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-2-(6-(4-(3-(3-Fluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-3-Methyl-2-(1 -oxo-6-(4-(3-phenylureido)phenyl)isoindolin-2-yl)butanoic acid; (S)-2-(6-(4-(3-Benzylureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-2-(6-(4-(3-(2,6-Difluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-3-Methyl-2-(1 -oxo-6-(4-(3-p-tolylureido)phenyl)isoindolin-2-yl)butanoic acid; (S)-2-(6-(4-(3-(3-Methoxyphenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-2-(6-(4-(3-(4-Methoxyphenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(6-(4-(3-(3,5-Difluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(6-(4-(3-(3,4-Difluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(6-(4-(3-Cyclohexylureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-3-Methyl-2-(1 -oxo-6-(4-(3-(4-(trifluoromethyl)phenyl)ureido)phenyl) isoindolin-2-yl)butanoic acid;
(S)-3-Methyl-2-(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl) isoindolin-2-yl)butanoic acid;
(S)-2-(6-(4-(3-(4-Cyanophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-2-(6-(4-(3-(3-Cyanophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-2-(6-(4-(3-(4-Chloro-2-phenoxyphenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(6-(4-(3-(5-Chloro-2-phenoxyphenyl) ureido) phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-3-Methyl-2-(1 -oxo-6-(4-(3-(2-phenoxyphenyl)ureido)phenyl)isoindolin-2-yl)butanoic acid;
(S)-3-Methyl-2-(1 -oxo-6-(4-(3-(4-phenoxyphenyl)ureido)phenyl)isoindolin-2-yl)butanoic acid;
(S)-2-(6-(4-(3-(2-Fluorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-3-Methyl-2-(1 -oxo-6-(4-(3-p-tolylthioureido)phenyl)isoindolin-2-yl)butanoic acid; (S)-2-(6-(4-(3-(3-Fluorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(6-(4-(3-(4-Methoxyphenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(6-(4-(3-(3-Methoxyphenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(6-(4-(3-(4-Chlorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-2-(6-(4-(3-(3-Chlorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-3-Methyl-2-(1 -oxo-6-(4-(3-(2-trifluoromethyl)phenyl)thioureido)phenyl) isoindolin-2-yl)butanoic acid;
(S)-2-(6-(4-(3-(4-Cyanophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-2-(6-(4-(3-(3-Cyanophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-3-Methyl-2-(1 -oxo-6-(4-(3-o-tolylthioureido)phenyl)isoindolin-2-yl)butanoic acid; (S)-2-(6-(4-(3-(2-Methoxyphenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-3-Methyl-2-(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)thioureido)phenyl) isoindolin-2-yl)butanoic acid;
(S)-3-Methyl-2-(1 -oxo-6-(4-(phenylsulfonamido)phenyl)isoindolin-2-yl)butanoic acid; (S)-2-(6-(4-(4-Cyanophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-2-(6-(4-(3,4-Difluorophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(6-(4-(2,4-Difluorophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(6-(4-(3,4-Dimethoxyphenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(6-(4-(3-Chlorophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(6-(4-(4-Methoxyphenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-3-Methyl-2-(1 -oxo-6-(4-(4-(trifluoromethyl)phenylsulfonamido)phenyl) isoindolin-2-yl)butanoic acid;
(S)-3-Methyl-2-(1 -oxo-6-(4-(phenylmethylsulfonamido)phenyl)isoindolin-2-yl)butanoic acid;
(S)-3-Methyl-2-(6-(4-(1 -methylethylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)butanoic acid;
(S)-2-(6-(4-Benzamidophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(6-(4-(4-Fluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-3-Methyl-2-(1 -oxo-6-(4-(4-(trifluoromethyl)benzamido)phenyl)isoindolin-2-yl)butanoic acid;
(S)-2-(6-(4-(4-Methoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-2-(6-(4-(3-Fluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-2-(6-(4-(3-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-2-(6-(4-(2,4-Difluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-3-Methyl-2-(6-(4-(4-methylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)butanoic acid; (S)-2-(6-(4-(4-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-2-(6-(4-(4-tert-Butylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-2-(6-(4-(Cyclohexanecarboxamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(6-(4-Biphenyl-4-ylcarboxamidophenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)- 2-(6-(4-(2-Naphthamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-3-Methyl-2-(1 -oxo-6-(4-(4-pentylbenzamido)phenyl)isoindolin-2-yl)butanoic acid; (S)-2-(6-(4-(2-Fluoro-6-(trifluoromethyl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(6-(4-(Benzo[d][1 ,3]dioxole-5-carboxamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)- 2-(6-(4-(2,6-Dichlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)- 2-(6-(4-(2-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)- 2-(6-(4-(2,4-Dichlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)- 2-(6-(4-(4-Butoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-2-(6-(4-(2,6-Difluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)- 2-(6-(4-(3,4-Difluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-2-(6-(4-(3,4-Dimethoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)- 3-Methyl-2-(1 -oxo-6-(4-(3,4,5-trimethoxybenzamido)phenyl)isoindolin-2-yl) butanoic acid;
(S)- 2-(6-(4-(3,5-Diethoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)- 3-Methyl-2-(1 -oxo-6-(4-(3-phenoxybenzamido)phenyl)isoindolin-2-yl) butanoic acid;
(S)-3-Methyl-2-(1 -oxo-6-(4-(4-phenoxybenzamido)phenyl)isoindolin-2-yl) butanoic acid;
(S)- 3-Methyl-2-(1 -oxo-6-(4-(2-phenoxybenzamido)phenyl)isoindolin-2-yl) butanoic acid;
(S)-3-Methyl-2-(1 -oxo-6-(4-(2,4,6-trimethylbenzamido)phenyl)isoindolin-2-yl) butanoic acid;
(S)- 2-(6-(4-(2,4-Dimethoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-3-Methyl-2-(1 -oxo-6-(4-(4-(trifluoromethoxy)benzamido)phenyl)isoindolin-2-yl)butanoic acid;
(S)- 2-(6-(4-(2-Methoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)- 2-(6-(4-(4-Fluoro-3-methylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)- 2-(6-(4-(4-Butylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)- 2-(6-(4-(2,6-Difluoro-3-methylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(6-(4-(4-Ethylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)- 3-Methyl-2-(1 -oxo-6-(4-(4-propylbenzamido)phenyl)isoindolin-2-yl)butanoic acid; (S)- 3-Methyl-2-(6-(4-(4-octylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)butanoic acid; (S)- 2-(6-(4-(4-Cyclohexylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-3-Methyl-2-(1 -oxo-6-(4-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydro naphthalene-2-carboxamido)phenyl)isoindolin-2-yl)butanoic acid;
(S)- 2-(6-(4-(1 -Naphthamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-2-(6-(4-(3,5-Dimethoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)- 2-(6-(4-(4-Hexylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)- 2-(6-(4-(4-Heptylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)- 3-Methyl-2-(6-(4-(4-nonylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)butanoic acid; (S)- 2-(6-(4-(4-Decylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid; (S)-2-(6-(4-(Adamantyl-2-carboxamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(6-(4-(2-Fluoro-4-(trifluoromethyl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(6-(4-(2-Fluoro-3-(trifluoromethyl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)- 2-(6-(4-(3-Fluoro-4-(trifluoromethyl)benzamido)phenyl)-1 -oxoisoindolin-2-yl) -3-methylbutanoic acid;
(S)-2-(6-(4-(4-Fluoro-2-(trifluoromethyl)benzamido)phenyl)-1 -oxoisoindolin-2-yl) -3-methylbutanoic acid;
(S)-3-Methyl-2-(1 -oxo-6-(4-(2-(trifluoromethyl)benzamido)phenyl)isoindolin-2-yl)butanoic acid;
(S)-2-(6-(4-(2-Ethoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-3-Methyl-2-(6-(4-(nicotinamido)phenyl)-1 -oxoisoindolin-2-yl)butanoic acid;
(S)- 2-(6-(4-(2-Chloronicotinamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-3-Methyl-2-(6-(4-(6-morpholinonicotinamido)phenyl)-1 -oxoisoindolin-2-yl) butanoic acid;
(S)- 3-Methyl-2-(1 -oxo-6-(4-(6-(piperidin-1 -yl)nicotinamido)phenyl)isoindolin-2-yl)butanoic acid;
(S)-3-Methyl-2-(1 -oxo-6-(4-(6-(pyrrolidin-1 -yl)nicotinamido)phenyl) isoindolin-2-yl)butanoic acid;
(S)-2-(5-(4-(3-(4-Fluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(5-(4-(3-(2-Fluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-2-(5-(4-(3-(3-Fluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-3-Methyl-2-(1 -oxo-5-(4-(3-phenylureido)phenyl)isoindolin-2-yl)butanoic acid; (S)-2-(5-(4-(3-Cyclohexylureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid; (S)-2-(5-(4-(3-(2,4-Difluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(5-(4-(3-(3,4-Difluorophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-3-Methyl-2-(1 -oxo-5-(4-(3-p-tolylureido)phenyl)isoindolin-2-yl)butanoic acid; (S)-3-Methyl-2-(1 -oxo-5-(4-(3-m-tolylureido)phenyl)isoindolin-2-yl)butanoic acid; (S)-3-Methyl-2-(1 -oxo-5-(4-(3-(4-(trifluoromethyl)phenyl)ureido)phenyl) isoindolin-2-yl)butanoic acid;
(S)-3-Methyl-2-(1 -oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl) isoindolin -2-yl)butanoic acid;
(S)-2-(5-(4-(3-(4-Methoxyphenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(5-(4-(3-(3-Methoxyphenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(5-(4-(3-(4-Cyanophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(5-(4-(3-(3-Cyanophenyl)ureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(5-(4-(3-(2-Fluorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(5-(4-(3-(3-Fluorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-2-(5-(4-(3-(4-Methoxyphenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(5-(4-(3-(3-Methoxyphenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-2-(5-(4-(3-(4-Chlorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(5-(4-(3-(3-Chlorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(5-(4-(3-(4-Cyanophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-3-Methyl-2-(1 -oxo-5-(4-(3-(2-(trifluoromethyl)phenyl)thioureido)phenyl) isoindolin-2-yl)butanoic acid;
(S)-3-Methyl-2-(1 -oxo-5-(4-(3-o-tolylthioureido)phenyl)isoindolin-2-yl)butanoic acid; (S)-3-Methyl-2-(1 -oxo-5-(4-(3-p-tolylthioureido)phenyl)isoindolin-2-yl)butanoic acid; (S)-2-(5-(4-(3-(3-Fluorophenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-2-(5-(4-(3-(3-Methoxyphenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(5-(4-(3-(2-Methoxyphenyl)thioureido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-3-Methyl-2-(1 -oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)thioureido)phenyl) isoindolin-2-yl)butanoic acid;
(S)-3-Methyl-2-(1 -oxo-6-(4-(phenylsulfonamido)phenyl)isoindolin-2-yl)butanoic acid; (S)-2-(5-(4-(4-Cyanophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-2-(5-(4-(3,4-Difluorophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(5-(4-(2,4-Difluorophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(5-(4-(3,4-Dimethoxyphenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(5-(4-(3-Chlorophenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-2-(5-(4-(4-Methoxyphenylsulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-3-Methyl-2-(1 -oxo-5-(4-(4-(trifluoromethyl)phenylsulfonamido)phenyl) isoindolin-2-yl)butanoic acid;
(S)-3-Methyl-2-(1 -oxo-5-(4-(phenylmethylsulfonamido) phenyl) isoindolin-2-yl)butanoic acid;
(S)-2-(5-(4-(Cyclohexanesulfonamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(5-(4-Benzamidophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(5-(4-(4-Fluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-3-Methyl-2-(1 -oxo-5-(4-(4-(trifluoromethyl)benzamido)phenyl)isoindolin-2-y/l)butanoic acid;
(S)-2-(5-(4-(4-Methoxybenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-2-(5-(4-(3-Fluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-2-(5-(4-(3-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-2-(5-(4-(2,4-Difluorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-3-Methyl-2-(5-(4-(4-methylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)butanoic acid; (S)-2-(5-(4-(4-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-2-(5-(4-(4-tert-Butylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-3-Methyl-2-(1 -oxo-5-(4-(4-pentylbenzamido)phenyl)isoindolin-2-yl)butanoic acid; (R)-3-Methyl-2-(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)iso indolin-2-yl)butanoic acid;
2-(1 -Oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)acetic acid; (S)-2-(1 -Oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl) propanoic acid;
2-Methyl-2-(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)propanoic acid;
1 - (1 -Oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl) cyclopentanecarboxylic acid;
(S)-2-(1 -Oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)-2-phenylacetic acid;
4-(1 -Oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)butanoic acid;
(S)-4-Methyl-2-(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)iso indolin-2-yl)pentanoic acid;
(S)-3-Methoxy-2-(1 -oxo-6-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)iso indolin-2 yl)propanoic acid;
(R)-3-Methyl-2-(1 -oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl) isoindolin-2-yl)butanoic acid;
2- (1 -Oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)acetic acid; (S)-2-(1 -Oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl) propanoic acid;
1 -(1 -Oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl) cyclopentanecarboxylic acid;
(S)-2-(1 -Oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)-2-phenylacetic acid;
4-(1 -Oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl) butanoic acid;
3- (1 -Oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)propanoic acid;
(S)-2-(1 -Oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)isoindolin-2-yl)-3-phenylpropanoic acid;
(S)-3-Methoxy-2-(1 -oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl) isoindolin-2 yl)propanoic acid;
(S)-4-Methyl-2-(1 -oxo-5-(4-(3-(3-(trifluoromethyl)phenyl)ureido)phenyl)iso indolin-2-yl)pentanoic acid;
(S)- 2-(6-(5-(3-(2-Chlorophenyl)ureido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)- 2-(6-(5-(3-(4-Chloro-2-phenoxyphenyl)ureido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)- 2-(6-(5-(3-(3,4-Dimethylphenyl)ureido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)- 2-(6-(5-(3-(3,4-Difluorophenyl)ureido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)- 2-(6-(5-(3-(2,3-Dihydro-1 H-inden-5-yl)ureido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(6-(5-(4-tert-Butylbenzamido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)- 3-Methyl-2-(1 -oxo-6-(5-(4-pentylbenzamido)pyridin-2-yl)isoindolin-2-yl)butanoic acid;
(S)- 2-(6-(5-Biphenyl-4-ylcarboxamidopyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-2-(6-(5-(2-Naphthamido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)- 2-(6-(5-(4-Butoxybenzamido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)- 2-(6-(4-(3-(2-Chlorophenyl)ureido)-2-(trifluoromethyl)phenyl)-1 -oxoiso indolin-2-yl)-3-methylbutanoic acid;
(S)- 2-(6-(4-(3-(3,4-Difluorophenyl)ureido)-2-(trifluoromethyl)phenyl)-1 -oxoiso indolin- 2- yl)-3-methylbutanoic acid;
(S)-2-(6-(4-(3-(2,3-Dihydro-1 H-inden-5-yl)ureido)-2-(trifluoromethyl)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)- 2-(6-(4-(3-(3,4-Dimethylphenyl)ureido)-2-(trifluoromethyl)phenyl)-1 -oxoiso indolin-2-yl)-3-methylbutanoic acid;
(S)- 2-(6-(4-(4-tert-Butylbenzamido)-2-(trifluoromethyl)phenyl)-1 -oxoisoindolin-2-yl)- 3- methylbutanoic acid;
(S)- 2-(6-(4-Biphenyl-4-ylcarboxamido-2-(trifluoromethyl)phenyl)-1 -oxoiso indolin-2-yl)-3-methylbutanoic acid;
(S)- 2-(6-(4-(2-Naphthamido)-2-(trifluoromethyl)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)- 3-Methyl-2-(1 -oxo-6-(4-(4-pentylbenzamido)-2-(trifluoromethyl) phenyl) isoindolin-2-yl)butanoic acid;
(S)- 2-(6-(4-(4-Butoxybenzamido)-2-(trifluoromethyl)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(6-(4-(3-(3,4-Dimethylphenyl)ureido)-3-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)- 2-(6-(4-(3-(2,3-Dihydro-1 H-inden-5-yl)ureido)-3-fluorophenyl)-1 -oxoiso indolin-2-yl)-3-methylbutanoic acid; (S)- 2-(6-(4-(3-(3,4-Difluorophenyl)ureido)-3-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(6-(4-(3-(2-Chlorophenyl)ureido)-3-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)- 2-(6-(4-(4-tert-Butylbenzamido)-3-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(6-(3-Fluoro-4-(4-pentylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)- 2-(6-(4-Biphenyl-4-ylcarboxamido-3-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)- 2-(6-(4-(2-Naphthamido)-3-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)- 2-(6-(4-(4-Butoxybenzamido)-3-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-2-(6-(4-(4-tert-Butylbenzamido)-2-methoxyphenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(6-(4-Biphenyl-4-ylcarboxamido-2-methoxyphenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(6-(4-(4-Butoxybenzamido)-2-methoxyphenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(6-(2-Methoxy-4-(4-pentylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(6-(2-Methoxy-4-(4-(trifluoromethoxy)benzamido)phenyl)-1 -oxoiso indolin-2-yl)-3-methylbutanoic acid;
(S)-2-(6-(4-(4-tert-Butylbenzamido)-2-methylphenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(6-(4-Biphenyl-4-ylcarboxamido-2-methylphenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(6-(4-(4-Butoxybenzamido)-2-methylphenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-3-Methyl-2-(6-(2-methyl-4-(4-pentylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)butanoic acid;
(S)-3-Methyl-2-(6-(2-methyl-4-(4-(trifluoromethoxy)benzamido)phenyl)-1 -oxoisoindolin-2-yl)butanoic acid;
(S)-2-(6-(4-(4-tert-Butylbenzamido)-2-chlorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(6-(4-Biphenyl-4-ylcarboxamido-2-chlorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(6-(4-(4-Butoxybenzamido)-2-chlorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(6-(2-Chloro-4-(4-pentylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(6-(2-Chloro-4-(4-(trifluoromethoxy)benzamido)phenyl)-1 -oxoiso indolin-2-yl)-3-methylbutanoic acid;
(S)-2-(6-(6-(4-tert-Butylbenzamido)pyridin-3-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(6-(6-(4-tert-Butylbenzamido)pyridazin-3-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-3-Methyl-2-(1 -oxo-6-(6-(4-pentylbenzamido)pyridazin-3-yl)isoindolin-2-yl)butanoic acid;
(S)-3-Methyl-2-(1 -oxo-6-(6-(4-(trifluoromethoxy)benzamido)pyridazin-3-yl)isoindolin-2-yl)butanoic acid;
(S)-2-(6-(5-(4-tert-Butylbenzamido)pyrazin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(6-(5-Biphenyl-4-ylcarboxamidopyrazin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(6-(5-(4-Butoxybenzamido)pyrazin-2-yl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-3-Methyl-2-(1 -oxo-6-(5-(4-pentylbenzamido)pyrazin-2-yl)isoindolin-2-yl)butanoic acid;
(S)-3-Methyl-2-(1 -oxo-6-(5-(4-(trifluoromethoxy)benzamido)pyrazin-2-yl)isoindolin-2-yl)butanoic acid;
2-(6-(4-([1 ,1 '-Biphenyl]-4-ylcarboxamido)phenyl)-1 -oxoisoindolin-2-yl)-2-methyl propanoic acid;
2-(6-(4-(4-(tert-Butyl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)-2-methyl propanoic acid;
2-(6-(4-(4-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)-2-methylpropanoic acid; 2-Methyl-2-(1 -oxo-6-(4-(4-(trifluoromethoxy)benzamido)phenyl)isoindolin-2-yl)propanoic acid;
2- Methyl-2-(1 -oxo-6-(4-(4-pentylbenzamido)phenyl)isoindolin-2-yl)propanoic acid; 1 -(6-(4-([1 ,1 '-Biphenyl]-4-ylcarboxamido)phenyl)-1 -oxoisoindolin-2-yl) cyclopentane carboxylic acid;
1 -(6-(4-(4-(tert-Butyl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclopentane carboxylic acid;
1 -(6-(4-(4-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclopentane carboxylic acid;
1 -(1 -Oxo-6-(4-(4-(trifluoromethoxy)benzamido)phenyl)isoindolin-2-yl) cyclopentane carboxylic acid;
1 -(1 -Oxo-6-(4-(4-pentylbenzamido)phenyl)isoindolin-2-yl)cyclopentane carboxylic acid;
(R)-2-(6-(4-([1 ,1 '-Biphenyl]-4-ylcarboxamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
3- (6-(4-([1 ,1 '-Biphenyl]-4-ylcarboxamido)phenyl)-1 -oxoisoindolin-2-yl)cyclo hexane carboxylic acid;
3-(6-(4-(3-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclohexane carboxylic acid;
3-(6-(4-(4-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclohexane carboxylic acid;
3-(1 -Oxo-6-(4-(4-(trifluoromethyl)benzamido)phenyl)isoindolin-2-yl)cyclo
hexanecarboxylic acid;
3-(6-(4-(5-Methyl-2-phenyloxazole-4-carboxamido)phenyl)-1 -oxoisoindolin-2-yl)cyclohexanecarboxylic acid;
(1 r,4r)-4-(6-(4-([1 ,1 '-Biphenyl]-4-ylcarboxamido)phenyl)-1 -oxoisoindolin-2-yl) cyclohexanecarboxylic acid;
(1 r,4r)-4-(6-(4-(3-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclohexane carboxylic acid;
(1 r,4r)-4-(6-(4-(4-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclohexane carboxylic acid;
(1 r,4r)-4-(1 -Oxo-6-(4-(4-(trifluoromethyl)benzamido)phenyl)isoindolin-2-yl) cyclohexanecarboxylic acid;
(1 r,3s,5R,7S)-3-(6-(4-(3-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl) adamantane-1 -carboxylic acid;
(1 r,3s,5R,7S)-3-(6-(4-(4-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl) adamantane-1 -carboxylic acid;
(1 r,3s,5R,7S)-3-(1 -Oxo-6-(4-(4-(trifluoromethyl)benzamido)phenyl)isoindolin-2-yl)adamantane-1 -carboxylic acid;
(1 r,3s,5R,7S)-3-(6-(4-(4-Methylbenzamido)phenyl)-1 -oxoisoindolin-2-yl) adamantane-1 -carboxylic acid;
1 -(6-(4-([1 ,1 '-Biphenyl]-4-ylcarboxamido)phenyl)-1 -oxoisoindolin-2-yl) cyclobutane carboxylic acid;
1 -(6-(4-(4-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclobutane carboxylic acid;
1 -(1 -Oxo-6-(4-(4-(trifluoromethyl)benzamido)phenyl)isoindolin-2-yl) cyclo butanecarboxylic acid;
1 -(6-(4-(4-Methylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclobutane carboxylic acid;
1 -(6-(4-([1 ,1 '-Biphenyl]-4-ylcarboxamido)phenyl)-1 -oxoisoindolin-2-yl)
cyclopropanecarboxylic acid;
1 -(6-(4-(4-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclopropane carboxylic acid;
1 -(1 -Oxo-6-(4-(4-(trifluoromethyl)benzamido)phenyl)isoindolin-2-yl)cyclo propane carboxylic acid;
(1 S,2R)-2-(6-(4-(4-Chlorobenzamido)phenyl)-1 -oxoisoindolin-2-yl)cyclopentane carboxylic acid;
(1 S,2R)-2-(1 -Oxo-6-(4-(4-(trifluoromethyl)benzamido)phenyl)isoindolin-2-yl) cyclopentanebcarboxylic acid;
(S)-2-(6-(4-([1 ,1 '-Biphenyl]-4-ylcarboxamido)-2-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(6-(4-(4-(tert-Butyl)benzamido)-2-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(6-(4-(4-Chlorobenzamido)-2-fluorophenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-2-(6-(2-Fluoro-4-(4-(trifluoromethoxy)benzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(6-(2-Fluoro-4-(4-pentylbenzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methyl butanoic acid;
(S)-3-Methyl-2-(1 -oxo-6-(4-(5-phenylthiazole-2-carboxamido)phenyl)isoindolin-2-yl)butanoic acid;
(S)-3-Methyl-2-(1 -oxo-6-(4-(5-phenyloxazole-2-carboxamido)phenyl) isoindolin-2-yl)butanoic acid;
(S)-2-(6-(4-(3-(4-Fluorophenyl)isoxazole-5-carboxamido)phenyl)-1 -oxo isoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(6-(4-(3-(4-Chlorophenyl)isoxazole-5-carboxamido)phenyl)-1 -oxo
isoindolin-2-yl)-3-methylbutanoic acid ;
(S)-3-Methyl-2-(1 -oxo-6-(4-(3-(4-(trifluoromethyl)phenyl)isoxazole-5-carboxamido)phenyl)isoindolin-2-yl)butanoic acid;
(S)-3-Methyl-2-(6-(4-(4-(oxazol-5-yl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)butanoic acid;
(S)-3-Methyl-2-(1 -oxo-6-(4-(4-phenylthiazole-2-carboxamido)phenyl)isoindolin-2-yl)butanoic acid;
(S)-3-Methyl-2-(1 -oxo-6-(4-(5-phenyl-1 ,3,4-thiadiazole-2-carboxamido)
phenyl)isoindolin-2-yl)butanoic acid;
(S)-3-Methyl-2-(1 -oxo-6-(4-(5-phenyl-4H-1 ,2,4-triazole-3-carboxamido) phenyl) isoindolin-2-yl)butanoic acid;
(S)-2-(6-(4-(4-(2-Cyanopropan-2-yl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(6-(4-(4-(3-Cyanopentan-3-yl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-3-Methyl-2-(1 -oxo-6-(5-(5-phenyloxazole-2-carboxamido)pyridin-2-yl) isoindolin-2-yl)butanoic acid;
(S)-3-Methyl-2-(1 -oxo-6-(5-(5-phenylthiazole-2-carboxamido)pyridin-2-yl) isoindolin-2-yl)butanoic acid;
(S)-2-(6-(5-(3-(4-Fluorophenyl)isoxazole-5-carboxamido)pyridin-2-yl)-1 -oxo isoindolin-2-yl)-3-methylbutanoic acid;
(S)-2-(6-(4-(4-(1 ,3,4-Oxadiazol-2-yl)benzamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid;
(S)-3-Methyl-2-(6-(4-(5-methyl-2-phenyloxazole-4-carboxamido)phenyl)-1 -oxoisoindolin-2-yl)butanoic acid;
(S)-3-Methyl-2-(1 -oxo-6-(4-(2-phenyl-5-(trifluoromethyl)oxazole-4-carboxamido) phenyl)isoindolin-2-yl)butanoic acid;
(S)-3-Methyl-2-(1 -oxo-6-(4-(4-(thiazol-2-yl)benzamido)phenyl)isoindolin-2-yl) butanoic acid;
(S)-2-(6-(4-(5-Butylpicolinamido)phenyl)-1 -oxoisoindolin-2-yl)-3-methylbutanoic acid; (S)-3-Methyl-2-(1 -oxo-6-(4-(quinoline-3-carboxamido)phenyl)isoindolin-2-yl) butanoic acid;
(S)-3-Methyl-2-(1 -oxo-6-(4-(4-(pyrimidin-5-yl)benzamido)phenyl)isoindolin-2-yl)butanoic acid;
(S)-3-Methyl-2-(6-(5-(5-methyl-2-phenyloxazole-4-carboxamido)pyridin-2-yl)-1 -oxoisoindolin-2-yl)butanoic acid;
(S)-3-Methyl-2-(1 -oxo-6-(5-(2-phenyl-5-(trifluoromethyl)oxazole-4-carboxamido) pyridin-2-yl)isoindolin-2-yl)butanoic acid; and
(S)-3-Methyl-2-(1 -oxo-6-(4-(2-phenylacetamido)phenyl)isoindolin-2-yl)butanoic acid; or a stereoisomer, tautomer or a pharmaceutically acceptable salt, solvate, polymorph, prodrug, carboxylic acid isostere or N-oxide thereof.
21 . A pharmaceutical composition comprising a compound of formula 1 , a stereoisomer, tautomer or a pharmaceutically acceptable salt, solvate, polymorph, prodrug, carboxylic acid isostere or N-oxide thereof, according to any one of the claims 1 to 20, along with a pharmaceutically acceptable excipient or a carrier.
22. A method of treatment of DGAT1 mediated disease or disorder, comprising administering to a subject in need thereof, a therapeutically effective amount of compound of formula 1 , according to any one of the claims 1 to 20, or a stereoisomer, tautomer or a pharmaceutically acceptable salt, solvate, polymorph, prodrug, carboxylic acid isostere or N-oxide thereof.
23. The method according to claim 22, wherein the DGAT1 mediated disease or disorder is selected from obesity, diabetes, impaired glucose tolerance, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, anorexia nervosa, bulimia, cachexia, syndrome X, insulin resistance, hypoglycemia, hyperglycemia, hyperuricemia, hyperinsulinemia, hypercholesterolemia, hyperlipidemia, dyslipidemia, mixed dyslipidemia, hypertriglyceridemia, pancreatitis, metabolic acidosis, ketosis, steatosis, dysmetabolic syndrome and nonalcoholic fatty liver disease; cardiovascular diseases, such as atherosclerosis, arteriosclerosis, acute heart failure, congestive heart failure, coronary artery disease, cardiomyopathy, myocardial ischaemia, myocardial infarction, angina pectoris, hypertension, hypotension, stroke, ischemia, ischemic reperfusion injury, aneurysm, restenosis, peripheral vascular disease and vascular stenosis, diseases of skin such as acne, infertility, polycystic ovary syndrome and Hepatitis C infection.
24. The method according to claim 22 or claim 23, wherein the DGAT1 mediated disease or disorder is selected from obesity, diabetes, insulin resistance, impaired glucose tolerance, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, hypercholesterolemia, hypertriglyceridemia and hyperlipidemia.
25. The method according to any one of the claims 22 to 24, wherein the DGAT1 mediated disease or disorder is obesity.
26. Use of a compound of formula 1 , according to any one of the claims 1 to 20, or a stereoisomer, tautomer or a pharmaceutically acceptable salt, solvate,
polymorph, prodrug, carboxylic acid isostere or N-oxide thereof, for the treatment of DGAT1 mediated disease or disorder.
27. The use according to claim 26, wherein the DGAT1 mediated disease or disorder is selected from obesity, diabetes, impaired glucose tolerance, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, anorexia nervosa, bulimia, cachexia, syndrome X, insulin resistance, hypoglycemia, hyperglycemia, hyperuricemia, hyperinsulinemia, hypercholesterolemia, hyperlipidemia, dyslipidemia, mixed dyslipidemia, hypertriglyceridemia, pancreatitis, metabolic acidosis, ketosis, steatosis, dysmetabolic syndrome and nonalcoholic fatty liver disease; cardiovascular diseases, such as atherosclerosis, arteriosclerosis, acute heart failure, congestive heart failure, coronary artery disease, cardiomyopathy, myocardial ischaemia, myocardial infarction, angina pectoris, hypertension, hypotension, stroke, ischemia, ischemic reperfusion injury, aneurysm, restenosis, peripheral vascular disease and vascular stenosis, diseases of skin such as acne, infertility, polycystic ovary syndrome and and Hepatitis C infection.
28. The use according to claim 26 or claim 27, wherein the DGAT1 mediated disease or disorder is selected from obesity, diabetes, insulin resistance, impaired glucose tolerance, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, hypercholesterolemia, hypertriglyceridemia and hyperlipidemia.
29. The use according to any one of the claims 26 to 28, wherein the DGAT1 mediated disease or disorder is obesity.
30. Use of a compound of formula 1 , according to any one of the claims 1 to 20, or a stereoisomer, tautomer or a pharmaceutically acceptable salt, solvate, polymorph, prodrug, carboxylic acid isostere or N-oxide thereof, for the manufacture of a medicament for the treatment of diseases or disorders mediated by DGAT1 .
31 . The use according to claim 30, wherein the DGAT1 mediated disease or disorder is selected from obesity, diabetes, insulin resistance, impaired glucose tolerance, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, hypercholesterolemia, hypertriglyceridemia and hyperlipidemia.
32. A process for the preparation of compound of formula 1 a,

Formula 1 a
wherein Yi=CH2, Y2=C(0); Xi, X2, X4 and X5 are selected from CH or CR; L= *C(0)NH; * indicates the point of attachment to A-(CH2)n-; m=1 ; A, n, R, Ra=Ri, and R9 are as defined in formula 1 ;
the steps comprising:
a) Reacting compound of formula 8:

with a reagent and the reaction condition selected from:
i) A-(CH2)n-COCI, wherein A and n are as defined in formula 1 ; in presence of a base such as pyridine in a solvent such as dichloromethane or
THF at temperature ranging from 20-35 °C;
ii) A-(CH2)n-COOH, wherein A and n are as defined in formula 1 ; in presence of a reagent such as isobutylchloroformate and a base such as N- methylmorpholine in a solvent such as THF at a temperature range of 0 °C to room temperature (20-35 °C) for 2-4 h;
iii) A-(CH2)nCOO-(Ci-C6)-alkyl, wherein A represents a 5-membered heteroaryl ring containing one or more heteroatoms selected from 1 -3 N, O and S, and substituted with a phenyl group; wherein both phenyl and heteroaryl rings may be substituted with one or more groups selected from halogen, hydroxy, (C1-C12)- alkoxy, cyano, (CrCi2)-alkyl, CF3 and OCF3; n is as defined in formula 1 ; in a solution of 2M AIMe3 in toluene at 60-80 °C in a sealed tube for 2-4 h; iv) A-(CH2)nCOO-(Ci-C6)-alkyl, wherein A represents a phenyl group substituted with a 5-membered heteroaryl ring optionally containing heteroatoms selected from 1 -3 N, O and S, and substituted with a phenyl group; wherein both phenyl and heteroaryl rings may be substituted with one or more groups selected from halogen, hydroxy, (CrCi2)-alkoxy, cyano, (CrCi2)-alkyl, CF3 and OCF3; n is as defined in formula 1 ;
in presence of carbonyl chloride in a solvent mixture of dichloromethane and DMF at 20-35 °C for about 2-4 h; and
v) A-(CH2)n-COOH, wherein A and n are as defined in formula 1 ; in presence of a reagent such as isobutylchloroformate and a base such as N- methylmorpholine in a solvent such as THF at a temperature range of 0 °C to room temperature (20-35 °C) for 2-4 h;
to obtain compound o

b) Hydrolysis of compound of formula 15 using a reagent such as 1 N LiOH or 1 N NaOH in a solvent such as MeOH or THF at a temperature ranging from 20-35 °C to obtain compound of

c) Optionally converting the compound of formula 16 to its corresponding ester prodrugs or pharmaceutically acceptable salts.
A process for the preparation of a compound of formula 1 a;

Formula 1 a
wherein Yi=CH2, Y2=C(0); Xi, X2, X4 and X5 are selected from CH or CR; L= NHC(0)NH; m=1 ; A, n, R, Ra=Ri,
and R9 are as defined in formula 1 ;
the steps comprising:
a) Reacting compound of formula 8:

with A-(CH2)n-NCO; wherein A and n are as defined in formula 1 ;
in a solvent such as dichloromethane or THF at a temperature ranging from 20-35 °C, to obtain compo

9
b) Hydrolysis of compound of formula 9 using a reagent such as 1 N LiOH or 1 N NaOH in a solvent such as MeOH or THF at a temperature ranging from 20-35 °C to obtain compound of fo

10
c) Optionally converting the compound of formula 10 to its corresponding ester prodrugs or pharmaceutically acceptable salts.
34. A process for the preparation of compound of formula 8:

wherein X1 ; X2, X4, Xs, Ri and R2 are as defined in formula 1 ; the steps comprising:
a) Reacting compound of formula 4:

with compound of formula 4P:

and bis(pinacolo)diboron, in presence of a reagent such as palladium acetate or tetrakis palladium and a base such as potassium acetate, sodium carbonate or cesium carbonate in a solvent such as toluene, dioxane, dimethoxyethane, DMF or acetone at a temperature rang btain compound of formula 5;

b) Refluxing compound of formula 5 with N-bromosuccinimide and a catalytic amount of AIBN or benzoyl peroxide in a solvent such as CCI4 using irradiation (200 watt bulb) at a temperature ranging from 80-100 °C to obtain compound of formula 6;

c) Reacting compound of formula 6 with compound of formula 6P:

6P (HCI salt)
wherein ^ and R2 are as defined in formula 1 ; in presence of a base and reaction condition selected from:
i) triethylamine in a solvent such as benzene or toluene at a temperature ranging from 70-120 °C; and
ii) potassium carbonate in a solvent such as DMF or THF at a temperature ranging from 50-80 °C,
to obtain compound of form

d) Reducing compound of formula 7 using a reducing agent and condition selected from:
i) Fe and ammonium chloride in a solvent such as aqueous EtOH or EtOH:
THF: H20 at a temperature ranging from 70-100 °C;
ii) Fe and HCI in a solvent such as H20 or ethanol or combination thereof; iii) SnCI2 in a solvent such as ethyl acetate;
iv) hydrogen over Raney Ni, Pd/C or Pt/C catalyst in a solvent such as methanol at pressure ranging from 50-80 psi and temperature ranging from 20-65 °C; and
v) cobalt chloride and zinc in a solvent such as DMF or water at a temperature ranging from 20-100 °C;
to obtain compound of formula 8.

A process for the preparation of compound of formula 1 a,

Formula 1 a
wherein
Y2=C(0); Xi , X2, X4 and X5 are selected from CH or CR, L= *C(0)NH; * indicates the point of attachment to A-(CH2)n-; m=1 ; A, n, R, Ra=Ri , Rb=R2 and R9 are as defined in formula 1 ;
the steps comprising:
a) Preparing compound of formula 46:

46
by reacting compound of formula

37
with A-(CH2)n-COCI, wherein A and n are as defined in formula 1 ; in presence of a base such as pyridine in a solvent such as dichloromethane or THF at temperature ranging from 20-35 °C;
b) Preparing compound of formula 47:

47
by reacting compound of formula 46 with bis(pinacolato)diboron, Pd(dppf)CI2 and Pd(dppf)CI2:CH2CI2 in a solvent such as dioxane, dimethoxyethane, DMSO or DMF at temperature ranging from 50-100 °C;
c) Preparing compound of formula 41 :

41
by reacting compound of formula

40
with compound of formula 6P:

6P (HCI salt)
wherein R-\ and R2 are as defined in formula 1 ; in presence of a base selected from: i) triethylamine in a solvent such as benzene or toluene at a temperature ranging from 70-120 °C; and
ii) potassium carbonate in a solvent such as DMF or THF at a temperature ranging from 50-80 °C;
d) Reacting compound of formula 47 with compound of formula 41 in presence of Pd(dppf)CI2:CH2Cl2 and a base such as potassium carbonate, cesium carbonate or 2M Na2C03 (in water) in a solvent such as DMF, dioxane, dimethoxyethane or acetone under an atmosphere of argon at temperature ranging from 50-100 °C to obtain compound of f

e) Hydrolysis of compound of formula 15 using a reagent such as 1 N LiOH or 1 N
NaOH in a solvent such as MeOH or THF at a temperature ranging from 20-35 °C to obtain compound of formula 16, and

Optionally converting the compound of formula 16 to its corresponding ester rugs or pharmaceutically acceptable salts.
36. A process for the preparation of compound of formula 1 a,

Formula 1 a
wherein
Y2=C(0); Xi , X2, X4 and X5 are selected from CH or CR; L= NHC(0)NH; m=1 ; A, n, R, Ra=R-i , Rb=R2 and R9 are as defined in formula 1 ;
the steps comprising:
a) Preparing compound of formula 38:

38
by reacting compound of formula

37
with A-(CH2)n-NCO, wherein A and n are as defined in formula 1 ; in a suitable solvent such as dichloromethane or THF at temperature ranging from 20-35 °C; b) Preparing compound of formula 39:

39
by reacting compound of formula 38 with bis(pinacolato)diboron, Pd(dppf)CI2 and Pd(dppf)CI2:CH2Cl2 in a solvent such as dioxane, dimethoxyethane, DMSO or DMF at temperature ranging from 50-100 °C;
c) Preparing compound of formula 41 :

by reacting compound of formula 40:

with compound of formula 6P:

6P (HCI salt)
wherein
and R2 are as defined in formula 1 ; in presence of a base selected from: i) triethylamine in a solvent such as benzene or toluene at a temperature ranging from 70-120 °C; and
ii) potassium carbonate in a solvent such as DMF or THF at a temperature ranging from 50-80 °C;
d) Reacting compound of formula 39 with compound of formula 41 in presence of Pd(dppf)CI2:CH2Cl2 and a base such as potassium carbonate, cesium carbonate or 2M Na2C03 (in water) in a solvent such as DMF, dioxane, dimethoxyethane or acetone under an atmosphere of argon at temperature ranging from 50-100 °C to obtain compound of formula 9;

9
e) Hydrolysis of compound of formula 9 using a reagent such as 1 N LiOH or 1 N NaOH in a solvent such as MeOH or THF at a temperature ranging from 20-35 °C to obtain compound of formula 10, and

10
Optionally converting the compound of formula 10 to its corresponding ester rugs or pharmaceutically acceptable salts.
A process for the preparation of compound of formula 55

wherein Xi , X2, X4 and X5 are selected from CH, CR and N; wherein R, Ri and R2 are as defined in formula 1 ;
the steps comprising:
a) Reacting compound of formula 41 , as prepared by the method claimed in claim 36:

41
with bis(pinacolato)diboron, Pd(dppf)CI2 and Pd(dppf)CI2:CH2Cl2 in a solvent such as dioxane, dimethoxyethane, DMSO or DMF at temperature ranging from 50-100 °C to obtain compound of formula 52;

b) Reacting compound of formula 52 with commercially available compound of formula 53:

in presence of Pd(dppf)CI2:CH2Cl2 in a base selected from potassium carbonate, cesium carbonate and 2M Na2C03 (in water) in a solvent such as DMF, dioxane, dimethoxyethane or acetone under an atmosphere of argon at temperature ranging from 50-100 °C to obtain compound of formula 54;

c) Reducing compound of formula 54 using a reducing agent selected from:
i) Fe and ammonium chloride in a solvent such as aqueous EtOH or EtOH: THF: H20 at a temperature ranging from 70-100 °C;
ii) Fe and HCI in a solvent such as H20 or ethanol or combination thereof; iii) SnCI2 in a solvent such as ethyl acetate;
iv) hydrogen over Raney Ni, Pd/C or Pt/C catalyst in a solvent such as methanol at pressure ranging from 50-80 psi and temperature ranging from 20-65 °C; and
v) cobalt chloride and zinc in a solvent such as DMF or water at a temperature ranging from 20-100 °C.
to obtain compound of formula 55.
A process for the preparation of compound of formula 7

wherein Xi , X2, X4 and X5 are selected from CH and CR; wherein R, Ri and R2 are as defined in formula 1 ; by reacting compound of formula 41 , as prepared by the method claimed in claim 36:

41
with commercially available 4-nitrophenyl boronic acid and commercially available Pd(dppf)CI2: CH2CI2 in a solvent such as DMF or dioxane at 70 °C to 90 °C for 2-4 h.