[0001] The present invention relates to the field of medicinal chemistry and more particularly to the development of antimicrobial compounds effective against bacteria, virus, fungi and protozoa including a spectrum of Gram-negative and Gram-positive pathogens. The present disclosure relates to compounds of Formula I, and their stereoisomers, pharmaceutically acceptable salts, complexes, hydrates, solvates, tautomers, polymorphs, racemic mixtures, optically active forms and pharmaceutically active derivatives thereof and pharmaceutical compositions containing them as the active ingredient. The present disclosure further relates to the synthesis and characterization of aforementioned compounds.
[0002] The compounds of the present disclosure are useful as medicaments and their use in the manufacture of medicaments for treatment, prevention or suppression of diseases, and conditions mediated by microbes. The present invention also provides evidence for treating infection caused by microbes. BACKGROUND
[0003] Due to increasing antibiotic resistance, novel classes of antibacterial agents are acutely needed for the treatment of bacterial infection. In general, broad spectrum antibiotic compounds, which possess effective activity against both Gram-positive and Gram-negative pathogens are need of the hour. Current antibacterial drugs used to treat and prevent bacterial infections have been found to have limited effect. Further, there is a continuing need to identify new compounds with potent antibacterial activity with reduced possibility of pathogens developing resistance, which possess improved efficacy against bacterial infections that resist treatment with currently available antibiotics, or which possess selectivity against target microorganisms.
[0004] From the foregoing discussion, it is clear that compounds used in the state of the art to treat and prevent bacterial infection have been found to have limited effect. SUMMARY

[0005] The present disclosure is based on the surprising discovery that compounds of Formula I (see below) exhibit advantageous antimicrobial properties. Thus, the present disclosure provides a compound of Formula I
or its stereoisomers, pharmaceutically acceptable salts, complexes, hydrates, solvates, tautomers, polymorphs, racemic mixtures, optically active forms and pharmaceutically active derivatives thereof, wherein
Ri is selected from the group consisting of, Ci-6 alkyl, C2-6 alkenyl, C3-6 cycloalkyl, C1-6 alkylamino, Ci-6 aminoalkylene, 4-7 membered carbocyclyl or heterocyclyl ring which may be fully saturated or unsaturated or partially unsaturated optionally having upto three heteroatom independently selected from 0, N, or S, each of which is unsubstituted or substituted with 1 to 3 groups independently selected from halogen, amino, hydroxyl, Ci-6 alkoxy, SO3H, SO2R9, COOR9, CONHR9, or SO2NHR9, wherein R9 is selected from H, Ci-6 alkyl, methylsulfone, Ci-6 alkyl, OC1-6 alkyl, OC1-6 haloalkyl, C3-6 cycloalkyl, 3-7 membered heterocyclyl ring which may be fully saturated or unsaturated or partially unsaturated optionally having upto three heteroatom independently selected from 0, N, or S, C3-6 cycloalkylamino, C3-6 aminocycloalkyl, Ci-6 alkylamino, or di (Ci-6 alkyl)amino;

R2 and R3 are independently selected from the group consisting of hydrogen, C1-6 alkyl,
fluorine, OC1-6 alkyl, hydroxyl, and amino;
R is selected from the group consisting of hydrogen, fluorine, cyano, OC1-6 alkyl, and
hydroxyl;
Xi is -N or CR4;
R4 is selected from the group consisting of hydrogen, halogen, cyano, -OC1-6 alkyl, C1-6
haloalkyl, -OC1-6 haloalkyl, and C1-6 alkyl;
X2 is -N or CR5;
R5 is selected from the group consisting of hydrogen, halogen, cyano, -OC1-6 alkyl, C1-6
haloalkyl, -OC1-6 haloalkyl, and C1-6 alkyl;
X3 is N or CR6; and X4 is CH or C- C1-6 alkyl wherein dotted line (—) represents a
bond;
R6is selected from the group consisting of hydrogen, halogen, cyano, -OC1-6 alkyl, -OCi-
6 haloalkyl, and C1-6 alkyl, wherein C1-6 alkyl is optionally substituted with hydroxyl or
amino;
X4 is CH2 or 0; and X3 is CH2 when dotted line (—) represents no bond;
m is 0 or 1;
m is 0 to 2;
Y2 and Y3 are independently selected from N or CR7;
R7 is selected from the group consisting of hydrogen, halogen, cyano, -OC1-6 alkyl, C1-6
haloalkyl, -OC1-6 haloalkyl, and C1-6 alkyl;
Zi is selected from the group consisting of 0, S, and CH2; and
R8 is selected from the group consisting of hydrogen, C1-6 alkyl, and fluorine.
[0006] The present disclosure further relates to a compound of Formula I, or its
stereoisomers, pharmaceutically acceptable salts, complexes, hydrates, solvates,
tautomers, polymorphs, racemic mixtures, optically active forms and pharmaceutically
active derivatives thereof, for use in killing or inhibiting the growth of a microorganism
selected from the group consisting of bacteria, virus, fungi, and protozoa.

[0007] The present disclosure further relates to use of a compound of Formula I, or its stereoisomers, pharmaceutically acceptable salts, complexes, hydrates, solvates, tautomers, polymorphs, racemic mixtures, optically active forms and pharmaceutically active derivatives thereof, in killing or inhibiting the growth of a microorganism selected from the group consisting of bacteria, virus, fungi and protozoa.
[0008] The present disclosure further relates to a compound of Formula I, or its stereoisomers, pharmaceutically acceptable salts, complexes, hydrates, solvates, tautomers, polymorphs, racemic mixtures, optically active forms and pharmaceutically active derivatives thereof, for use in treating a disease or condition in a patient wherein said disease or condition is caused by a microorganism selected from the group consisting of Gram positive, and Gram negative pathogens.
[0009] The present disclosure further relates to use of a compound of Formula I, or its stereoisomers, pharmaceutically acceptable salts, complexes, hydrates, solvates, tautomers, polymorphs, racemic mixtures, optically active forms and pharmaceutically active derivatives thereof, in treating disease or condition in a patient, wherein said disease or condition is caused by a microorganism selected from the group consisting of Gram positive, and Gram negative pathogens. The patient is typically a mammal, preferably a human.
[00010] The present disclosure further relates to a method of treating a bacterial infection or condition in a subject, said method comprising administering to a subject a compound of Formula I, or its stereoisomers, pharmaceutically acceptable salts, complexes, hydrates, solvates, tautomers, polymorphs, racemic mixtures, optically active forms and pharmaceutically active derivatives thereof, wherein said bacterial infection or condition is caused by a microorganism selected from the group consisting of Gram positive, and Gram negative pathogens.
[00011] The present disclosure relates to a composition comprising a compound of Formula I, or its stereoisomers, pharmaceutically acceptable salts, complexes, hydrates, solvates, tautomers, polymorphs, racemic mixtures, optically active forms, and pharmaceutically active derivatives thereof together with a carrier.

[00012] The present disclosure relates to a pharmaceutical composition comprising a compound of Formula I, or its stereoisomers, pharmaceutically acceptable salts, complexes, hydrates, solvates, tautomers, polymorphs, racemic mixtures, optically active forms, and pharmaceutically active derivatives thereof, together with a pharmaceutically acceptable carrier, optionally in combination with one or more other pharmaceutical compositions.
[00013] The present disclosure relates to a process of preparation of compound of Formula I, or its stereoisomers, pharmaceutically acceptable salts, complexes, hydrates, solvates, tautomers, polymorphs, racemic mixtures, optically active forms, and pharmaceutically active derivatives thereof.
[00014] The present disclosure relates to a process of preparation of a composition comprising a compound of Formula I, or its stereoisomers, pharmaceutically acceptable salts, complexes, hydrates, solvates, tautomers, polymorphs, racemic mixtures, optically active forms, and pharmaceutically active derivatives thereof together with a carrier. [00015] The present disclosure relates to a process of preparation of pharmaceutical composition comprising a compound of Formula I, or its stereoisomers, pharmaceutically acceptable salts, complexes, hydrates, solvates, tautomers, polymorphs, racemic mixtures, optically active forms, and pharmaceutically active derivatives thereof, together with a pharmaceutically acceptable carrier, optionally in combination with one or more other pharmaceutical compositions.
[00016] These and other features, aspects, and advantages of the present subject matter will become better understood with reference to the following description. This summary is provided to introduce a selection of concepts in a simplified form. This summary is not intended to identify key features or essential features of the disclosure, nor is it intended to be used to limit the scope of the subject matter. DETAILED DESCRIPTION
[00017] Those skilled in the art will be aware that the present disclosure is subject to variations and modifications other than those specifically described. It is to be understood that the present disclosure includes all such variations and modifications. The disclosure

also includes all such steps, features, compositions and compounds referred to or indicated
in this specification, individually or collectively, and any and all combinations of any or
more of such steps or features.
Definitions
[00018] For convenience, before further description of the present disclosure, certain terms
employed in the specification, and examples are collected here. These definitions should
be read in the light of the remainder of the disclosure and understood as by a person of skill
in the art. The terms used herein have the meanings recognized and known to those of skill
in the art, however, for convenience and completeness, particular terms and their meanings
are set forth below.
[00019] The articles "a", "an" and "the" are used to refer to one or to more than one (i.e.,
to at least one) of the grammatical object of the article.
[00020] The terms "comprise" and "comprising" are used in the inclusive, open sense,
meaning that additional elements may be included. Throughout this specification, unless
the context requires otherwise the word "comprise", and variations, such as "comprises"
and "comprising", will be understood to imply the inclusion of a stated element or step or
group of element or steps but not the exclusion of any other element or step or group of
element or steps.
[00021] The term "including" is used to mean "including but not limited to". "Including"
and "including but not limited to" are used interchangeably.
[00022] In the structural formulae given herein and throughout the present disclosure, the
following terms have been indicated meaning, unless specifically stated otherwise.
[00023] In this specification, the prefix Cx-y as used in terms such as Cx yalkyl and the like
(where x and y are integers) indicates the numerical range of carbon atoms that are present
in the group; for example, Ci-6 alkyl includes Cialkyl (methyl), Czalkyl (ethyl), Csalkyl
(propyl and isopropyl) and C4alkyl (butyl, 1-methylpropyl, 2-methylpropyl, and £-butyl).
Unless specifically stated, the bonding atom of a group may be any suitable atom of that
group; for example, propyl includes prop-1-yl and prop-2-yl.

[00024] The term "alkyl" refers to a monoradical branched or unbranched saturated hydrocarbon chain having from 1 to 10 carbon atoms. This term is exemplified by groups such as n-butyl, iso-butyl, t-butyl, n-hexyl, n-decyl, and the like. The groups may be optionally substituted.
[00025] The term "haloalkyl" as used herein refers to an alkyl group in which one or more hydrogen atoms are replaced by the same number of identical or different halogen atoms. The term "haloalkyl" is exemplified by groups such as chloromethyl, trifluoromethyl, 1-fluoroethyl, 2,2,2-trifluoroethyl, and the like.
[00026] The term "alkylene" refers to a diradical branched or unbranched saturated hydrocarbon chain having from 1 to 6 carbon atoms. This term is exemplified by groups such as methylene, ethylene, propylene, butylene, hexylene, and the like. The groups may be optionally substituted. Representative substituted alkylene groups include amino substituted alkyl en es.
[00027] The term "alkenyl" refers to a monoradical of a branched or unbranched unsaturated hydrocarbon group preferably having from 2, 3, 4, 5, or 6 carbon atoms and having 1, 2, or 3, double bond (vinyl), preferably 1 double bond. The groups may be optionally substituted.
[00028] The term "cycloalkyl" refers to carbocyclic groups of from 3 to 12 carbon atoms having a single cyclic ring or multiple condensed rings which may be partially unsaturated. Such cycloalkyl groups include, by way of example, single ring structures such as cyclopropyl, cyclobutyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl, and the like, or multiple ring structures or carbocyclic groups to which is fused an aryl group, for example indane, and the like. The groups may be optionally substituted. [00029] The terms "alkoxyl" or "alkoxy" refers to an alkyl group, as defined above, having an oxygen radical attached thereto. Representative alkoxyl groups include methoxy, ethoxy, propyloxy, tert-butoxy and the like. An "ether" is two hydrocarbons covalently linked by an oxygen. Accordingly, the substituent of an alkyl that renders that alkyl an ether, either is, or resembles an alkoxyl, such as can be represented by one of -O-alkyl, -0- alkenyl, -O-alkynyl.

[00030] "Halo" or "Halogen", alone or in combination with any other term means halogens such as chloro (CI), fluoro (F), bromo (Br) and iodo (I).
[00031] The term "heteroaryl" refers to an heteroaromatic carbocyclic group of 3 to 10
carbon atoms having a single ring (e.g. pyridine) or multiple rings (e.g. isoquinoline), or
multiple condensed (fused) rings. Preferred heteroaryls include thiophene, pyrazole,
thiazole, pyridine, and the like. The groups may be optionally substituted.
[00032] The term "carbocyclyl" or "carbocycle" refers to a saturated, unsaturated
ring having 4 to 7 carbon atoms as a monocycle. Representative carbocycles include cyclopropyl, cyclobutyl, cyclopentyl, 1-cyclopent-l-enyl, l-cyclopent-2-enyl, 1-cyclopent-3-enyl, cyclohexyl, 1-cyclohex-l-enyl, l-cyclohex-2-enyl, l-cyclohex-3-enyl, and the like.
[00033] The term "heterocyclyl" refers to a "carbocyclyl" as defined herein, wherein
one or more carbon atoms have been replaced with a heteroatom selected from 0, N, or S.
[00034] The term "haloalkoxy" refers to an alkoxy group as defined above further
attached via halo linkage. For example, Ci-6 haloalkoxy refers to an alkoxy group having from 1-6 carbon atoms, or 1 - 3 carbon atoms further attached via halo linkage. Preferred haloalkoxy groups include, without limitation, -OCH2CI, -OCHCI2, and the like. [00035] As used herein, the term "substituted" is contemplated to include all permissible substituents of organic compounds. In a broad aspect, the permissible substituents include acyclic and cyclic, branched and unbranched, carbocyclic and heterocyclic, aromatic and nonaromatic substituents of organic compounds. Illustrative substituents include, for example, those described herein above. The permissible substituents can be one or more and the same or different for appropriate organic compounds. For purposes of this disclosure, the heteroatoms such as nitrogen may have hydrogen substituents and/or any permissible substituents of organic compounds described herein which satisfy the valences of the heteroatoms.
[00036] The term "effective amount" means an amount of a compound or composition which is sufficient enough to significantly and positively modify the symptoms and/or conditions to be treated (e.g., provide a positive clinical response). The effective amount

of an active ingredient for use in a pharmaceutical composition will vary with the particular condition being treated, the severity of the condition, the duration of the treatment, the nature of concurrent therapy, the particular active ingredient(s) being employed, the particular pharmaceutically-acceptable excipient(s)/carrier(s) utilized, the route of administration, and like factors within the knowledge and expertise of the attending physician
[00037] The compounds described herein may contain one or more chiral centers and/or double bonds and therefore, may exist as stereoisomers, such as double-bond isomers (i.e., geometric isomers), regioisomers, enantiomers or diastereomers. Accordingly, the chemical structures depicted herein encompass all possible enantiomers and stereoisomers of the illustrated or identified compounds including the stereoisomerically pure form (e.g., geometrically pure, enantiomerically pure or diastereomerically pure) and enantiomeric and stereoisomeric mixtures. Enantiomeric and stereoisomeric mixtures can be resolved into their component enantiomers or stereoisomers using separation techniques or chiral synthesis techniques well known to the person skilled in the art. The compounds may also exist in several tautomeric forms including the enol form, the keto form, and mixtures thereof. Accordingly, the chemical structures depicted herein encompass all possible tautomeric forms of the illustrated or identified compounds.
[00038] The term "pharmaceutically acceptable" refers to those compounds, materials, compositions, and/or dosage forms which are, within the scope of sound medical judgment, suitable for use in contact with the tissues of human beings and animals without excessive toxicity, irritation, allergic response, or other problem or complication, commensurate with a reasonable benefit/risk ratio.
[00039] "Pharmaceutically acceptable salt" embraces salts with a pharmaceutically acceptable acid or base. Pharmaceutically acceptable acids include both inorganic acids, for example hydrochloric, sulphuric, phosphoric, diphosphoric, hydrobromic, hydroiodic and nitric acid and organic acids, for example citric, fumaric, maleic, malic, mandelic, ascorbic, oxalic, succinic, tartaric, benzoic, acetic, methanesulphonic, ethanesulphonic, benzenesulphonic or p-toluenesulphonic acid. Pharmaceutically acceptable bases include

alkali metal (e.g. sodium or potassium) and alkali earth metal (e.g. calcium or magnesium)
hydroxides and organic bases, for example alkyl amines, arylalkyl amines and heterocyclic
amines.
[00040] The compounds discussed herein in many instances may have been named and/or
checked with ACD/Name by ACD/Labs® and/or Chemdraw by CambridgeSoft®.
[00041] The term "polymorphs" refers to crystal forms of the same molecule, and
different polymorphs may have different physical properties such as, for example, melting
temperatures, heats of fusion, solubilities, dissolution rates and/or vibrational spectra as a
result of the arrangement or conformation of the molecules in the crystal lattice.
[00042] The term "solvate", as used herein, refers to a crystal form of a substance which
contains solvent.
[00043] The term "hydrate" refers to a solvate wherein the solvent is water.
[00044] The present disclosure relates to a compound of Formula I
or its stereoisomers, pharmaceutically acceptable salts, complexes, hydrates, solvates, tautomers, polymorphs, racemic mixtures, optically active forms and pharmaceutically active derivatives thereof, wherein

Ri is selected from the group consisting of, Ci-6 alkyl, C2-6 alkenyl, C3-6 cycloalkyl, C1-6
alkylamino, Ci-6 aminoalkylene, 4-7 membered carbocyclyl or heterocyclyl ring which
may be fully saturated or unsaturated or partially unsaturated optionally having upto three
heteroatom independently selected from 0, N, or S, each of which is unsubstituted or
substituted with 1 to 3 groups independently selected from halogen, amino, hydroxyl, Ci-6
alkoxy, SO3H, SO2R9, COOR9, CONHR9, or SO2NHR9, wherein R9 is selected from H, Ci-
6 alkyl, methylsulfone, Ci-6 alkyl, OC1-6 alkyl, OC1-6 haloalkyl, C3-6 cycloalkyl, 3-7
membered heterocyclyl ring which may be fully saturated or unsaturated or partially
unsaturated optionally having upto three heteroatom independently selected from 0, N, or
S, C3-6 cycloalkylamino, C3-6 aminocycloalkyl, Ci-6 alkylamino, or di (Ci-6 alkyl)amino;
R2 and R3 are independently selected from the group consisting of hydrogen, Ci-6 alkyl,
fluorine, OC1-6 alkyl, hydroxyl, and amino;
R is selected from the group consisting of hydrogen, fluorine, cyano, OC1-6 alkyl, and
hydroxyl;
Xi is -N or CR4;
R4 is selected from the group consisting of hydrogen, halogen, cyano, -OC1-6 alkyl, Ci-6
haloalkyl, -OC1-6 haloalkyl, and Ci-6 alkyl;
X2 is -N or CR5;
R5 is selected from the group consisting of hydrogen, halogen, cyano, -OC1-6 alkyl, Ci-6
haloalkyl, -OC1-6 haloalkyl, and Ci-6 alkyl;
X3 is N or CRe; and X4 is CH or C- Ci-6 alkyl wherein dotted line (—) represents a
bond;
R6is selected from the group consisting of hydrogen, halogen, cyano, -OC1-6 alkyl, -OCi-
6 haloalkyl, and Ci-6 alkyl, wherein Ci-6 alkyl is optionally substituted with hydroxyl or
amino;
X4 is CH2 or 0; and X3 is CH2 when dotted line (—) represents no bond;
m is 0 or 1;
n2 is 0 to 2;
Y2 and Y3 are independently selected from -N or CR7;

R7 is selected from the group consisting of hydrogen, halogen, cyano, -OCi-6 alkyl, Ci-6
haloalkyl, -OCi-6 haloalkyl, and Ci-6 alkyl;
Zi is selected from the group consisting of 0, S, and CH2; and
R8 is selected from the group consisting of hydrogen, Ci-6 alkyl, and fluorine.
[00045] According to an embodiment, the present disclosure relates to a compound
of Formula I or its stereoisomers, pharmaceutically acceptable salts, complexes, hydrates,
solvates, tautomers, polymorphs, racemic mixtures, optically active forms and
pharmaceutically active derivatives thereof, wherein
Ri is selected from the group consisting of, Ci-6 alkyl, C2-6 alkenyl, C3-6 cycloalkyl, Ci-6
alkylamino, Ci-6 aminoalkylene, 4-7 membered carbocyclyl or heterocyclyl ring which
may be fully saturated or unsaturated or partially unsaturated optionally having upto three
heteroatom independently selected from 0, N, or S, each of which is unsubstituted or
substituted with 1 to 3 groups independently selected from halogen, amino, hydroxyl, Ci-6
alkoxy, SO3H, SO2R9, COOR9, CONHR9, or SO2NHR9, wherein R9 is selected from H, Ci-
6 alkyl, methylsulfone, Ci-6 alkyl, OCi-6 alkyl, OCi-6 haloalkyl, C3-6 cycloalkyl, 3-7
membered heterocyclyl ring which may be fully saturated or unsaturated or partially
unsaturated optionally having upto three heteroatom independently selected from O, N, or
S, C3-6 cycloalkylamino, C3-6 aminocycloalkyl, Ci-6 alkylamino, or di (Ci-6 alkyl)amino;
R2 and R3 are independently selected from the group consisting of hydrogen, C1-4 alkyl,
fluorine, OC1-4 alkyl, hydroxyl, and amino;
R is selected from the group consisting of hydrogen, fluorine, cyano, OC1-4 alkyl, and
hydroxyl;
Xi is -N or CR4;
R4 is selected from the group consisting of hydrogen, halogen, cyano, -OCi-6 alkyl, Ci-6
haloalkyl, -OCi-6 haloalkyl, and Ci-6 alkyl;
X2 is -N or CR5;
R5 is selected from the group consisting of hydrogen, halogen, cyano, -OCi-6 alkyl, Ci-6
haloalkyl, -OCi-6 haloalkyl, and Ci-6 alkyl;
X3 is N or CRe; and X4 is CH or C- Ci-6 alkyl wherein dotted line (—) represents a

bond;
R6is selected from the group consisting of hydrogen, halogen, cyano, -OCi-6 alkyl, -OCi-
6 haloalkyl, and Ci-6 alkyl, wherein Ci-6 alkyl is optionally substituted with hydroxyl or
amino;
X4 is CH2 or 0; and X3 is CH2 when dotted line (—) represents no bond;
ni is 0 or 1;
m is 0 to 2;
Y2 and Y3 are independently selected from -N or CR7;
R7 is selected from the group consisting of hydrogen, halogen, cyano, -OC1-6 alkyl, Ci-6
haloalkyl, -OC1-6 haloalkyl, and Ci-6 alkyl;
Zi is selected from the group consisting of 0, S, and CH2; and
R8 is selected from the group consisting of hydrogen, Ci-6 alkyl, and fluorine.
[00046] According to an embodiment, the present disclosure relates to a compound
of Formula I or its stereoisomers, pharmaceutically acceptable salts, complexes, hydrates,
solvates, tautomers, polymorphs, racemic mixtures, optically active forms and
pharmaceutically active derivatives thereof, wherein
Ri is selected from the group consisting of, Ci-6 alkyl, C2-6 alkenyl, C3-6 cycloalkyl, Ci-6
alkylamino, Ci-6 aminoalkylene, 4-7 membered carbocyclyl or heterocyclyl ring which
may be fully saturated or unsaturated or partially unsaturated optionally having upto three
heteroatom independently selected from 0, N, or S, each of which is unsubstituted or
substituted with 1 to 3 groups independently selected from halogen, amino, hydroxyl, Ci-6
alkoxy, SO3H, SO2R9, COOR9, CONHR9, or SO2NHR9, wherein R9 is selected from H, Ci-
6 alkyl, methylsulfone, Ci-6 alkyl, OC1-6 alkyl, OC1-6 haloalkyl, C3-6 cycloalkyl, 3-7
membered heterocyclyl ring which may be fully saturated or unsaturated or partially
unsaturated optionally having upto three heteroatom independently selected from 0, N, or
S, C3-6 cycloalkylamino, C3-6 aminocycloalkyl, Ci-6 alkylamino, or di (Ci-6 alkyl)amino;
R2 and R3 are independently selected from the group consisting of hydrogen, C1-2 alkyl,
fluorine, OC1-2 alkyl, hydroxyl, and amino;
R is selected from the group consisting of hydrogen, fluorine, cyano, OC1-2 alkyl, and

hydro xyl;
Xi is -N or CR4;
R4 is selected from the group consisting of hydrogen, halogen, cyano, -OC1-6 alkyl, C1-6
haloalkyl, -OC1-6 haloalkyl, and C1-6 alkyl;
X2 is -N or CR5;
R5 is selected from the group consisting of hydrogen, halogen, cyano, -OC1-6 alkyl, C1-6
haloalkyl, -OC1-6 haloalkyl, and C1-6 alkyl;
X3 is N or CRe; and X4 is CH or C- C1-6 alkyl wherein dotted line (—) represents a
bond;
R6is selected from the group consisting of hydrogen, halogen, cyano, -OC1-6 alkyl, -OCi-
6 haloalkyl, and C1-6 alkyl, wherein C1-6 alkyl is optionally substituted with hydroxyl or
amino;
X4 is CH2 or 0; and X3 is CH2 when dotted line (—) represents no bond;
m is 0 or 1;
m is 0 to 2;
Y2 and Y3 are independently selected from -N or CR7;
R7 is selected from the group consisting of hydrogen, halogen, cyano, -OC1-6 alkyl, C1-6
haloalkyl, -OC1-6 haloalkyl, and C1-6 alkyl;
Zi is selected from the group consisting of 0, S, and CH2; and
R8 is selected from the group consisting of hydrogen, C1-6 alkyl, and fluorine.
[00047] According to an embodiment, the present disclosure relates to a compound
of Formula I or its stereoisomers, pharmaceutically acceptable salts, complexes, hydrates,
solvates, tautomers, polymorphs, racemic mixtures, optically active forms and
pharmaceutically active derivatives thereof, wherein
Ri is selected from the group consisting of, C1-6 alkyl, C2-6 alkenyl, C3-6 cycloalkyl, C1-6
alkylamino, Ci 6 aminoalkylene, 4-7 membered carbocyclyl or heterocyclyl ring which
may be fully saturated or unsaturated or partially unsaturated optionally having upto three
heteroatom independently selected from 0, N, or S, each of which is unsubstituted or
substituted with 1 to 3 groups independently selected from halogen, amino, hydroxyl, Ci-6

alkoxy, S03H, S02R9) COORg, CONHRg, or S02NHR9) wherein R9 is selected from H, Ci-
6 alkyl, methylsulfone, OCi-6 alkyl, OCi-6 haloalkyl, C3-6 cycloalkyl, 3-7 membered
heterocyclyl ring which may be fully saturated or unsaturated or partially unsaturated
optionally having upto three heteroatom independently selected from 0, N, or S, C3-6
cycloalkylamino, C3-6 aminocycloalkyl, C1-6 alkylamino, or di(Ci-6 alkyl)amino;
R2 and R3 are independently selected from the group consisting of hydrogen, fluorine,
methoxy, hydroxyl, and amino; provided that at least one of R2 and R3 is hydrogen;
R is selected from the group consisting of hydrogen, fluorine, methoxy, cyano, and
hydroxyl;
Xi is N or CR4;
R4 is selected from the group consisting of hydrogen, halogen, cyano, -OCi-6 alkyl, C1-6
haloalkyl, -OCi-6 haloalkyl, and C1-6 alkyl;
X2 is N or CR5;
R5 is selected from the group consisting of hydrogen, halogen, cyano, -OCi-6 alkyl, C1-6
haloalkyl, -OCi-6 haloalkyl, and C1-6 alkyl;
X3 is N or CRe; and X4 is CH or C-C1-6 alkyl wherein dotted line (—) represents a bond;
R6is selected from the group consisting of hydrogen, halogen, cyano, -OCi-6 alkyl, -OCi-
6 haloalkyl, and C1-6 alkyl, wherein C1-6 alkyl is optionally substituted with hydroxyl or
amino;
X4 is CH2 or 0; and X3 is CH2 when dotted line (—) represents no bond;
m is 0 or 1;
n2 is 0 to 2;
Y2 and Y3 are independently selected from -N or CR7;
R7 is selected from the group consisting of hydrogen, halogen, cyano, -OCi-6 alkyl, C1-6
haloalkyl, -OCi-6 haloalkyl, and C1-6 alkyl;
Zi is selected from the group consisting of 0, S, and CH2; and
R8 is selected from the group consisting of hydrogen, C1-6 alkyl, and fluorine.
[00048] According to an embodiment, the present disclosure relates to a compound
of Formula I or its stereoisomers, pharmaceutically acceptable salts, complexes, hydrates,

solvates, tautomers, polymorphs, racemic mixtures, optically active forms and
pharmaceutically active derivatives thereof, wherein
Ri is selected from the group consisting of, Ci-6 alkyl, C2-6 alkenyl, C3-6 cycloalkyl, C1-6
alkylamino, Ci-6 aminoalkylene, 4-7 membered carbocyclyl or heterocyclyl ring which
may be fully saturated or unsaturated or partially unsaturated optionally having upto three
heteroatom independently selected from 0, N, or S, each of which is unsubstituted or
substituted with 1 to 3 groups independently selected from halogen, amino, hydroxyl, Ci-6
alkoxy, SO3H, SO2R9, COOR9, CONHR9, or SO2NHR9, wherein R9 is selected from H, Ci-
6 alkyl, methylsulfone, OC1-6 alkyl, OC1-6 haloalkyl, C3-6 cycloalkyl, 3-7 membered
heterocyclyl ring which may be fully saturated or unsaturated or partially unsaturated
optionally having upto three heteroatom independently selected from 0, N, or S, C3-6
cycloalkylamino, C3-6 aminocycloalkyl, Ci-6 alkylamino, or di(Ci-6 alkyl)amino;
R2 and R3 are independently selected from the group consisting of hydrogen, fluorine,
methoxy, hydroxyl, and amino; provided that at least one of R2 and R3 is hydrogen;
R is selected from the group consisting of hydrogen, fluorine, methoxy, cyano, and
hydroxyl;
Xi is N or CR4;
R4 is selected from the group consisting of hydrogen, halogen, cyano, -OC1-4 alkyl, C1-4
haloalkyl, -OC1-6 haloalkyl, and Ci-6 alkyl;
X2 is N or CR5;
R5 is selected from the group consisting of hydrogen, halogen, cyano, -OC1-4 alkyl, C1-4
haloalkyl, -OC1-6 haloalkyl, and Ci-6 alkyl;
X3 is N or CRe; and X4 is CH or C-C1-6 alkyl wherein dotted line (—) represents a bond;
R6is selected from the group consisting of hydrogen, halogen, cyano, -OC1-6 alkyl, -OCi-
6 haloalkyl, and Ci-6 alkyl, wherein Ci-6 alkyl is optionally substituted with hydroxyl or
amino;
X4 is CH2 or 0; and X3 is CH2 when dotted line (—) represents no bond;
m is 0 or 1;
n2 is 0 to 2;

Y2 and Y3 are independently selected from -N or CR7;
R7 is selected from the group consisting of hydrogen, halogen, cyano, -OC1-6 alkyl, C1-6
haloalkyl, -OC1-6 haloalkyl, and C1-6 alkyl;
Zi is selected from the group consisting of 0, S, and CH2; and
R8 is selected from the group consisting of hydrogen, C1-6 alkyl, and fluorine.
[00049] According to an embodiment, the present disclosure relates to a compound
of Formula I or its stereoisomers, pharmaceutically acceptable salts, complexes, hydrates,
solvates, tautomers, polymorphs, racemic mixtures, optically active forms and
pharmaceutically active derivatives thereof, wherein
Ri is selected from the group consisting of, C1-6 alkyl, C2-6 alkenyl, C3-6 cycloalkyl, C1-6
alkylamino, Ci 6 aminoalkylene, 4-7 membered carbocyclyl or heterocyclyl ring which
may be fully saturated or unsaturated or partially unsaturated optionally having upto three
heteroatom independently selected from 0, N, or S, each of which is unsubstituted or
substituted with 1 to 3 groups independently selected from halogen, amino, hydroxyl, Ci-6
alkoxy, SO3H, SO2R9, COOR9, CONHR9, or SO2NHR9, wherein R9 is selected from H, Ci-
6 alkyl, methylsulfone, OC1-6 alkyl, OC1-6 haloalkyl, C3-6 cycloalkyl, 3-7 membered
heterocyclyl ring which may be fully saturated or unsaturated or partially unsaturated
optionally having upto three heteroatom independently selected from O, N, or S, C3-6
cycloalkylamino, C3-6 aminocycloalkyl, C1-6 alkylamino, or di(Ci-6 alkyl)amino;
R2 and R3 are independently selected from the group consisting of hydrogen, fluorine,
methoxy, hydroxyl, and amino; provided that at least one of R2 and R3 is hydrogen;
R is selected from the group consisting of hydrogen, fluorine, methoxy, cyano, and
hydroxyl;
Xi is N or CR4;
R4 is selected from the group consisting of hydrogen, halogen, cyano, -OC1-4 alkyl, C1-4
haloalkyl, -OC1-6 haloalkyl, and C1-6 alkyl;
X2 is N or CR5;
R5 is selected from the group consisting of hydrogen, halogen, cyano, -OC1-4 alkyl, C1-4
haloalkyl, and C1-4 alkyl;

X3 is N or CR6; and X4 is CH or C-C1-6 alkyl wherein dotted line (—) represents a bond;
R6is selected from the group consisting of hydrogen, halogen, cyano, -OC1-6 alkyl, -OCi-
6 haloalkyl, and C1-6 alkyl, wherein C1-6 alkyl is optionally substituted with hydroxyl or
amino;
X4 is CH2 or 0; and X3 is CH2 when dotted line (—) represents no bond;
ni is 0 or 1;
m is 0 to 2;
Y2 and Y3 are independently selected from -N or CR7;
R7 is selected from the group consisting of hydrogen, halogen, cyano, -OC1-6 alkyl, C1-6
haloalkyl, -OC1-6 haloalkyl, and C1-6 alkyl;
Zi is selected from the group consisting of 0, S, and CH2; and
R8 is selected from the group consisting of hydrogen, C1-6 alkyl, and fluorine.
[00050] According to an embodiment, the present disclosure relates to a
compound of Formula I or its stereoisomers, pharmaceutically acceptable salts, complexes,
hydrates, solvates, tautomers, polymorphs, racemic mixtures, optically active forms and
pharmaceutically active derivatives thereof, wherein
Ri is selected from the group consisting of, C1-6 alkyl, C2-6 alkenyl, C3-6 cycloalkyl, C1-6
alkylamino, Ci-6 aminoalkylene, 4-7 membered carbocyclyl or heterocyclyl ring which
may be fully saturated or unsaturated or partially unsaturated optionally having upto three
heteroatom independently selected from 0, N, or S, each of which is unsubstituted or
substituted with 1 to 3 groups independently selected from halogen, amino, hydroxyl, Ci-6
alkoxy, SO3H, SO2R9, COOR9, CONHR9, or SO2NHR9, wherein R9 is selected from H, Ci-
6 alkyl, methylsulfone, Ci-6 alkyl, OC1-6 alkyl, OC1-6 haloalkyl, C3-6 cycloalkyl, 3-7
membered heterocyclyl ring which may be fully saturated or unsaturated or partially
unsaturated optionally having upto three heteroatom independently selected from 0, N, or
S, C3-6 cycloalkylamino, C3-6 aminocycloalkyl, Ci-6 alkylamino, or di(Ci-6 alkyl)amino;
R2 and R3 are independently selected from the group consisting of hydrogen, hydroxyl,
fluorine, methyl, methoxy, and amino; provided that at least one of R2 and R3 is hydrogen;
R is selected from the group consisting of hydrogen, fluorine, methoxy, cyano, and

hydro xyl;
Xi is -N or CR4;
R4 is selected from the group consisting of hydrogen, fluorine, cyano, -OC1-3 alkyl, and
C1-3 alkyl;
X2 is -N or CR5;
R5 is selected from the group consisting of hydrogen, fluorine, cyano, -OC1-3 alkyl, and
C1-3 alkyl;
X3 is N or CRe; and X4 is CH or C-CH3 wherein dotted line (—) represents a bond;
R6is selected from the group consisting of hydrogen, fluorine, cyano, -OC1-3 alkyl, and Ci-
3 alkyl, wherein C1-3 alkyl is optionally substituted with hydroxyl or amino;
X4 is CH2 or 0; and X3 is CH2 when dotted line (—) represents no bond;
m is 0 or 1;
m is 0 to 2;
Y2 and Y3 are independently selected from -N or CR7;
R7 is selected from the group consisting of hydrogen, halogen, cyano, -OC1-3 alkyl, , and
C1-3 alkyl;
Zi is selected from the group consisting of 0, S, and CH2; and
R8is selected from the group consisting of hydrogen, C1-6 alkyl, and fluorine.
[00051] According to an embodiment, the present disclosure relates to a
compound of Formula I or its stereoisomers, pharmaceutically acceptable salts, complexes,
hydrates, solvates, tautomers, polymorphs, racemic mixtures, optically active forms and
pharmaceutically active derivatives thereof, wherein
Ri is selected from the group consisting of CH3, CH2CH3, CH(CH3)2, cylopropyl,
cyclobutyl, CH2CF3, CH2CHFCH3, CH2CF2CH3, CH2CH(OH)CH3, CH2CH2OH,
CH2CH2OCH3, CH2CH(OCH3)CH3, CH2CH2NH2, CH2CH2NHCH3, CH2CH(NH2)CH3,
CH2CH2N(CH3)2,CH2CHFCH2NH2, CH2CF2CH2NH2, CH2CH2SO2CH3,

R2 and R3 are independently selected from the group consisting of hydrogen, hydroxyl,
fluorine, methyl, methoxy, and amino; provided that at least one of R2 and R3 is hydrogen;
R is selected from the group consisting of hydrogen, fluorine, methoxy, cyano, and
hydroxyl;
Xi is -N or CR4;
R4 is selected from the group consisting of hydrogen, fluorine, cyano, -OC1-3 alkyl, and
C1-3 alkyl;
X2 is -N or CR5;
R5 is selected from the group consisting of hydrogen, fluorine, cyano, -OC1-3 alkyl, and
C1-3 alkyl;
X3 is N or CRe; and X4 is CH or C-CH3 wherein dotted line (—) represents a bond;
R6is selected from the group consisting of hydrogen, fluorine, cyano, -OC1-3 alkyl, and Ci-
3 alkyl, wherein C1-3 alkyl is optionally substituted with hydroxyl or amino;
X4 is CH2 or 0; and X3 is CH2 when dotted line (—) represents no bond;
m is 0 or 1;
n2 is 0 to 2;
Y2 and Y3 are independently selected from -N or CR7;
R7 is selected from the group consisting of hydrogen, halogen, cyano, -OC1-3 alkyl, , and
C1-3 alkyl;
Zi is selected from the group consisting of 0, S, and CH2; and

R8is selected from the group consisting of hydrogen, Ci-6 alkyl, and fluorine.
[00052] According to an embodiment, the present disclosure relates to a compound
of Formula I or its stereoisomers, pharmaceutically acceptable salts, complexes, hydrates, solvates, tautomers, polymorphs, racemic mixtures, optically active forms and i pharmaceutically active derivatives thereof, wherein
Ri is selected from the group consisting of CH3, CH2CH3, CH(CH3)2, cylopropyl, cyclobutyl, CH2CF3, CH2CHFCH3, CH2CF2CH3, CH2CH(OH)CH3, CH2CH2OH, CH2CH2OCH3, CH2CH(OCH3)CH3, CH2CH2NH2, CH2CH2NHCH3, CH2CH(NH2)CH3, CH2CH2N(CH3)2,CH2CHFCH2NH2, CH2CF2CH2NH2, CH2CH2SO2CH3,
R2 and R3 are independently selected from the group consisting of hydrogen, fluorine, Ci-
6 alkyl, OC1-6 alkyl, hydroxyl, and amino; provided that at least one of R2 and R3 is
hydrogen;
R is selected from the group consisting of hydrogen, fluorine, cyano, OC1-6 alkyl, and
hydroxyl;
Xi is -N or CR4;
R4 is selected from the group consisting of hydrogen, halogen, cyano, -OC1-6 alkyl, C1-6
haloalkyl, OC1-6 haloalkyl, and C1-6 alkyl;
X2 is -N or CR5;
R5 is selected from the group consisting of hydrogen, halogen, cyano, -OC1-6 alkyl, C1-6
haloalkyl, OC1-6 haloalkyl, and C1-6 alkyl;
X3 is N or CRe; and X4 is CH or C-C1-6 alkylwherein dotted line (—) represents a bond;

R6is selected from the group consisting of hydrogen, halogen, cyano, -OC1-3 alkyl, and Ci-
6 alkyl, wherein C1-3 alkyl is optionally substituted with hydroxyl or amino;
X4 is CH2 or 0; and X3 is CH2 when dotted line (—) represents no bond;
m is 0 or 1;
m is 0 to 2;
Y2 and Y3 are independently selected from -N or CR7;
R7 is selected from the group consisting of hydrogen, halogen, cyano, -OC1-3 alkyl, and
C1-3 alkyl;
Zi is selected from the group consisting of 0, S, and CH2; and
R8 is selected from the group consisting of hydrogen, C1-6 alkyl, and fluorine.
[00053] According to an embodiment, the present disclosure relates to a compound
of Formula I or its stereoisomers, pharmaceutically acceptable salts, complexes, hydrates,
solvates, tautomers, polymorphs, racemic mixtures, optically active forms and
pharmaceutically active derivatives thereof, wherein
Ri is selected from the group consisting of CH3, CH2CH3, CH(CH3)2, cylopropyl,
cyclobutyl, CH2CF3, CH2CHFCH3, CH2CF2CH3, CH2CH(OH)CH3, CH2CH2OH,
CH2CH2OCH3, CH2CH(OCH3)CH3, CH2CH2NH2, CH2CH2NHCH3, CH2CH(NH2)CH3,
CH2CH2N(CH3)2,CH2CHFCH2NH2, CH2CF2CH2NH2, CH2CH2SO2CH3,
R2 and R3 are independently selected from the group consisting of hydrogen, fluorine, OCi-
4 alkyl, hydroxyl, and amino; provided that at least one of R2 and R3 is hydrogen;
R is selected from the group consisting of hydrogen, fluorine, cyano, OC1-6 alkyl, and

hydro xyl;
Xi is -N or CR4;
R4 is selected from the group consisting of hydrogen, halogen, cyano, -OC1-6 alkyl, C1-6
haloalkyl, OC1-6 haloalkyl, and C1-6 alkyl;
X2 is -N or CR5;
R5 is selected from the group consisting of hydrogen, halogen, cyano, -OC1-6 alkyl, C1-6
haloalkyl, OC1-6 haloalkyl, and C1-6 alkyl;
X3 is N or CRe; and X4 is CH or C-C1-6 alkylwherein dotted line (—) represents a bond;
R6is selected from the group consisting of hydrogen, halogen, cyano, -OC1-3 alkyl, and Ci-
3 alkyl, wherein C1-3 alkyl is optionally substituted with hydroxyl or amino;
X4 is CH2 or 0; and X3 is CH2 when dotted line (—) represents no bond;
m is 0 or 1;
m is 0 to 2;
Y2 and Y3 are independently selected from -N or CR7;
R7 is selected from the group consisting of hydrogen, halogen, cyano, -OC1-3 alkyl, and
C1-3 alkyl;
Zi is selected from the group consisting of 0, S, and CH2; and
R8 is selected from the group consisting of hydrogen, C1-6 alkyl, and fluorine.
[00054] According to an embodiment, the present disclosure relates to a compound
of Formula I or its stereoisomers, pharmaceutically acceptable salts, complexes, hydrates,
solvates, tautomers, polymorphs, racemic mixtures, optically active forms and
pharmaceutically active derivatives thereof, wherein
Ri is independently selected from the group consisting of CH3, CH2CH3, CH(CH3)2,
cylopropyl, cyclobutyl, CH2CF3, CH2CHFCH3, CH2CF2CH3, CH2CH(OH)CH3,
CH2CH2OH, CH2CH2OCH3, CH2CH(OCH3)CH3, CH2CH2NH2, CH2CH2NHCH3,
CH2CH(NH2)CH3, CH2CH2N(CH3)2, CH2CHFCH2NH2, CH2CH2SO2CH3,

R2 and R3 are is independently selected from the group consisting of hydrogen, hydroxyl,
methoxy, fluorine, and amino; provided that at least one of R2 and R3 is hydrogen;
R is selected from the group consisting of hydrogen, fluorine, methoxy, cyano, and
hydroxyl;
Xi is N or CR4;
R4 is selected from the group consisting of hydrogen, halogen, cyano, -OC1-6 alkyl, C1-6
haloalkyl, OC1-6 haloalkyl, and C1-6 alkyl;
X2 is N or CR5;
R5 is selected from the group consisting of hydrogen, halogen, cyano, -OC1-6 alkyl, C1-6
haloalkyl, OC1-6 haloalkyl, and C1-6 alkyl;
X3 is N or CRe; and X4 is CH or C-CH3 wherein dotted line (—) represents a bond;
R6is selected from the group consisting of hydrogen, halogen, cyano, -OC1-6 alkyl, -OCi-
6 haloalkyl, and C1-6 alkyl, wherein C1-6 alkyl is optionally substituted with hydroxyl or
amino;
X4 is CH2 or 0; and X3 is CH2 when dotted line (—) represents no bond;
m is 0 or 1;
n2 is 0 to 2;
Y2 and Y3 are independently selected from -N or CR7;
R7 is selected from the group consisting of hydrogen, halogen, cyano, C1-6 alkoxy, C1-6
haloalkyl, OC1-6 haloalkyl, and C1-6 alkyl;

Zi is selected from the group consisting of 0, S, and CH2; and
R8 is selected from the group consisting of hydrogen, methyl, and fluorine.
[00055] According to an embodiment, the present disclosure relates to a compound
of Formula I or its stereoisomers, pharmaceutically acceptable salts, complexes, hydrates,
solvates, tautomers, polymorphs, racemic mixtures, optically active forms and
pharmaceutically active derivatives thereof, wherein
Ri is independently selected from the group consisting of CH3, CH2CH3, CH(CH3)2,
cylopropyl, cyclobutyl, CH2CF3, CH2CHFCH3, CH2CF2CH3, CH2CH(OH)CH3,
CH2CH2OH, CH2CH2OCH3, CH2CH(OCH3)CH3, CH2CH2NH2, CH2CH2NHCH3,
CH2CH(NH2)CH3, CH2CH2N(CH3)2, CH2CHFCH2NH2, CH2CH2SO2CH3,
R2 and R3 are is independently selected from the group consisting of hydrogen, hydroxyl,
fluorine, and amino; provided that at least one of R2 and R3 is hydrogen;
R is selected from the group consisting of hydrogen, fluorine, methoxy, cyano, and
hydroxyl;
Xi is N or CR4;
R4 is selected from the group consisting of hydrogen, halogen, cyano, -OC1-6 alkyl, and
C1-6 alkyl;
X2 is N or CR5;
R5 is selected from the group consisting of hydrogen, halogen, cyano, -OC1-6 alkyl, C1-6
haloalkyl, OC1-6 haloalkyl, and C1-6 alkyl;

X3 is N or CR6; and X4 is CH or C-CH3 wherein dotted line (—) represents a bond;
R6is selected from the group consisting of hydrogen, halogen, cyano, -OC1-6 alkyl, -OCi-
6 haloalkyl, and C1-6 alkyl, wherein C1-6 alkyl is optionally substituted with hydroxyl or
amino;
X4 is CH2 or 0; and X3 is CH2 when dotted line (—) represents no bond;
ni is 0 or 1;
m is 0 to 2;
Y2 and Y3 are independently selected from -N or CR7;
R7 is selected from the group consisting of hydrogen, halogen, cyano, -OC1-3 alkyl, C1-3
haloalkyl, OC1-6 haloalkyl, and C1-3 alkyl;
Zi is selected from the group consisting of 0, S, and CH2; and
R8 is selected from the group consisting of hydrogen, methyl, and fluorine.
[00056] According to an embodiment, the present disclosure relates to a compound
of Formula I or its stereoisomers, pharmaceutically acceptable salts, complexes, hydrates,
solvates, tautomers, polymorphs, racemic mixtures, optically active forms and
pharmaceutically active derivatives thereof, wherein
Ri is selected from the group consisting of CH3, CH2CH3, CH(CH3)2, cylopropyl,
cyclobutyl, CH2CF3, CH2CHFCH3, CH2CF2CH3, CH2CH(OH)CH3, CH2CH2OH,
CH2CH2OCH3, CH2CH(OCH3)CH3, CH2CH2NH2, CH2CH2NHCH3, CH2CH(NH2)CH3,
CH2CH2N(CH3)2, CH2CHFCH2NH2, CH2CF2CH2NH2, CH2CH2SO2CH3,

methyl, methoxy, and amino; provided that at least one of R2 and R3 is hydrogen;
R is selected from the group consisting of hydrogen, fluorine, cyano, and hydroxyl;
Xi is -N or CR4;
R4 is selected from the group consisting of hydrogen, fluorine, cyano, -OC1-3 alkyl, and
C1-3 alkyl;
X2 is -N or CR5;
R5 is selected from the group consisting of hydrogen, fluorine, cyano, -OC1-3 alkyl, and
C1-3 alkyl;
X3 is N or CRe; and X4 is CH or C-CH3 wherein dotted line (—) represents a bond;
R6is selected from the group consisting of hydrogen, fluorine, cyano, -OC1-3 alkyl, and Ci-
3 alkyl, wherein C1-3 alkyl is optionally substituted with hydroxyl or amino;
X4 is CH2 or 0; and X3 is CH2 when dotted line (—) represents no bond;
m is 0 or 1;
m is 0 to 2;
Y2 and Y3 are independently selected from -N or CR7;
R7 is selected from the group consisting of hydrogen, fluorine, cyano, -OC1-3 alkyl, and Ci-
3 alkyl;
Zi is selected from the group consisting of 0, S, and CH2; and
R8 is selected from the group consisting of hydrogen, methyl, and fluorine.
[00057] According to an embodiment, the present disclosure relates to a compound
of Formula I or its stereoisomers, pharmaceutically acceptable salts, complexes, hydrates,
solvates, tautomers, polymorphs, racemic mixtures, optically active forms and
pharmaceutically active derivatives thereof, wherein
Ri is selected from the group consisting of CH3, CH2CH3, CH(CH3)2, cylopropyl,
cyclobutyl, CH2CF3, CH2CHFCH3, CH2CF2CH3, CH2CH(OH)CH3, CH2CH2OH,
CH2CH2OCH3, CH2CH(OCH3)CH3, CH2CH2NH2, CH2CH2NHCH3, CH2CH(NH2)CH3,
CH2CH2N(CH3)2, CH2CHFCH2NH2, CH2CF2CH2NH2, CH2CH2SO2CH3,

R2 and R3 are independently selected from the group consisting of hydrogen, hydroxyl,
methoxy, and amino; provided that at least one of R2 and R3 is hydrogen;
R is selected from the group consisting of hydrogen, fluorine, cyano, and hydroxyl;
Xi is -N or CR4;
R4 is selected from the group consisting of hydrogen, fluorine, cyano, -OC1-3 alkyl, and
C1-3 alkyl;
X2 is -N or CR5;
R5 is selected from the group consisting of hydrogen, fluorine, cyano, -OC1-3 alkyl, and
C1-3 alkyl;
X3 is N or CRe; and X4 is CH or C-CH3 wherein dotted line (—) represents a bond;
R6 is selected from the group consisting of hydrogen, fluorine, cyano, -OC1-3 alkyl,
CH2OH, CH2NH2;
X4 is CH2 or 0; and X3 is CH2 when dotted line (—) represents no bond;
ni is 0 or 1;
n2 is 0 to 2;
Y2 and Y3 are independently selected from -N or CR7;
R7 is selected from the group consisting of hydrogen, fluorine, cyano, -OC1-3 alkyl, and Ci-
3 alkyl;
Zi is selected from the group consisting of 0, S, and CH2; and
R8 is selected from the group consisting of hydrogen, methyl, and fluorine.

[00058] According to an embodiment, the present disclosure relates to a compound
of Formula I or its stereoisomers, pharmaceutically acceptable salts, complexes, hydrates, solvates, tautomers, polymorphs, racemic mixtures, optically active forms and pharmaceutically active derivatives thereof, wherein
Ri is selected from the group consisting of CH3, CH2CH3, CH(CH3)2, cylopropyl, cyclobutyl, CH2CF3, CH2CHFCH3, CH2CF2CH3, CH2CH(OH)CH3, CH2CH2OH, CH2CH2OCH3, CH2CH(OCH3)CH3, CH2CH2NH2, CH2CH2NHCH3, CH2CH(NH2)CH3, CH2CH2N(CH3)2, CH2CHFCH2NH2, CH2CF2CH2NH2, CH2CH2SO2CH3,
R2 and R3 are independently selected from the group consisting of hydrogen, methoxy,
fluorine, and hydroxyl; provided that at least one of R2 and R3 is hydrogen;
R is selected from the group consisting of hydrogen, fluorine, methoxy, cyano, and
hydro xyl;
Xi is -N or CR4;
R4 is selected from the group consisting of hydrogen, fluorine, cyano, -OC1-3 alkyl, and
C1-3 alkyl;
X2 is -N or CR5;
R5 is selected from the group consisting of hydrogen, fluorine, cyano, -OC1-3 alkyl, and
C1-3 alkyl;
X3 is N or CRe; and X4 is CH or C-CH3 wherein dotted line (—) represents a bond;
R6is selected from the group consisting of hydrogen, fluorine, cyano, -OC1-3 alkyl, and Ci-

Xi is -N or CR4;
R4 is selected from the group consisting of hydrogen, halogen, cyano, -OC1-6 alkyl, C1-6
haloalkyl, -OC1-6 haloalkyl, and C1-6 alkyl;
X2 is -N or CR5;
R5 is selected from the group consisting of hydrogen, halogen, cyano, -OC1-6 alkyl, C1-6
haloalkyl, -OC1-6 haloalkyl, and C1-6 alkyl;
X4 is is absent or CH2 or O; and X3 is CH2 when dotted line (—) represents no bond;
ni is 0 to 1;
n2 is 0 to 2;
W is O or CH2;
Yi is -N or CH; Y2 is -N or CR7;
Y3 is -N or CR7;
R7 is selected from the group consisting of hydrogen, halogen, cyano, -OC1-6 alkyl, C1-6
haloalkyl, -OC1-6 haloalkyl, and C1-6 alkyl;
Zi is selected from the group consisting of O, S, and CH2;
Z2 is selected from the group consisting of CH2, and C=0;
Z3 is selected from the group consisting of NH, O, and CH2;
R8 is selected from the group consisting of hydrogen, C1-6 alkyl, and fluorine.
[00055] According to an embodiment, the present disclosure relates to a compound
of Formula I, or its stereoisomers, pharmaceutical^ acceptable salts, complexes,
hydrates, solvates, tautomers, polymorphs, racemic mixtures, optically active forms and
pharmaceutically active derivatives thereof,
wherein
Ri is selected from the group consisting of, C1-6 alkyl, C2-6 alkenyl, C3-6 cycloalkyl, C1-6
alkylamino, Ci-6 aminoalkylene, 4-7 membered carbocyclyl or heterocyclyl ring which
may be fully saturated or unsaturated or partially unsaturated optionally having upto three
heteroatom independently selected from O, N, or S, each of which is unsubstituted or
substituted with 1 to 3 groups independently selected from halogen, amino, hydroxyl,
SO3H, COOR9, CONHR9, or S02NHR9, wherein R9 is selected from H, Ci_6 alkyl,