The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof comprising an GLP 1/Glucagon agonist linker conjugate Z  L1 L2  L  Y  R20 wherein Y represents an GLP 1/Glucagon agonist moiety; and L is a linker moiety  by formula (Ia) wherein the dashed line indicates the attachment to one o...

The present invention relates to dual GLP 1 / glucagon receptor agonists and their medical use for example in the treatment of disorders of the metabolic syndrome including diabetes and obesity as well as for reduction of excess food intake.

The invention relates to spirocyclically substituted 1 3 propane dioxide derivatives and to their physiologically compatible salts. The invention relates to compounds of formula (I) in which R1 R2 R3 R4 R5 R6 R7 R8 A and X have the given meanings and to their physiologically compatible salts. The compounds are suita...

The present invention relates to a multilayer pharmaceutical composition that can be dispersed in water, containing one antimalarial agent in combination with at least one other antimalarial agent. The present invention also relates to a method for producing such a pharmaceutical composition. ...

The invention refers to an injection device comprising a housing (10) having a first aperture (11) or window, a dose indicator (120) positioned within the housing (10) and rotatable with respect to the housing (10) during dose setting and during dose dispensing, and a gauge element (110), which is interposed between...

The present invention relates to pharmaceutical compositions intended to be used in the form of a solid unit such as a tablet for oral administration comprising a high content of fexofenadine and/or of at least one pharmaceutically acceptable salt thereof and also to hot melt processes for manufacturing solid units....

The invention relates to derivatives of morphine-6-glucuronide having formula (I) wherein R1 is a 5-membered heteroaromatic group optionally substituted by one or more substituents selected from among halogen atoms and (C1-C4)alkyl, halogen, hydroxyl, halo(C1-C4)a]kyl, halo(C1-C4)alkyloxy, (C1-C4)alkyloxy, aryl(C1...

The present disclosure provides hNGAL muteins that bind a pyoverdine family member or pyochelin and can be used in various application including pharmaceutical applications for example to inhibit or reduce growth of P. aeruginosa. The present disclosure also concerns methods of making one or more pyoverdine or pyoch...

The present invention relates to new crystalline polymorphs of 6  (Piperidin 4 yloxy)  2H isoquinolin 1 one hydrochloride processes for their preparation and their use in particular for the preparation of medicaments.

The present invention discloses and claims a series of substituted N-phenyl- bipyrrolidine carboxamides of formula (I). Wherein R1, R2, R3, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, ...

The present invention relates to a Robo1-Fc recombinant protein and to the use thereof for treating diseases in which a Slit protein is overexpressed, in particular cancer. The invention also relates to a composition including such a recombinant protein. Another aspect of the invention involves using a Robo1-Fc mole...

A treatment for glomerulonephritis, and other renal dysfunctions is disclosed, using a compound of Formula I.

The invention relates to N-[(2-aza-bicyclo[2.2.1]hex-1-yl)-aryl-methyl]-benzamide derivatives of the general formula (I) where: R is a hydrogen atom or a (C1-C6)alkyl group, (C3-C7)-cycloalkyl, optionally substituted by one or more fluorine, (C3-C7)-cycloalkyl, (C2-C4)alkenyl, phenyl, (C1-C6)alkoxy, hydroxy; R1 is...

The invention relates to compounds having formula (I) wherein: R1 represents a hydrogen atom or a (C1-C4)alkyl group; R2 represents a hydroxyl group, a thiol group, a (C1-C4)alkyloxy group or a thio(C1-C4)alkyl group; and n is an integer equal to 1 or 2, in the form of a base or acid addition salt, as well as in h...

The invention relates to a method for synthesizing benzofuran derivatives in particular the dronedarone of formula (D) including carrying out a Fries rearrangement reaction using a sulfonamido benzofuran ester intermediate.

The invention relates to a pharmaceutical antitumor combination including AVE8062 of formula (I) and sorafenib of formula (II), wherein both of said antitumor agents can be in the form of a base or pharmaceutically acceptable acid salt.

The invention relates to a method for preparing a combretastatin derivative (I) or (II), said method including the following steps: triaryl(3,4,5- trimethoxybenzyl)phosphonium halide P3 (III), wherein Ar denotes an aryl group selected from among phenyl or thienyl, is reacted with P2 having formula (IV) or P"2...

The invention relates to hexafluoroisopropyl carbamate derivatives of general formula (I): wherein R,Z,A,m and n as defined in the description, in the form of the base or of an addition salt with an acid. The compounds can be used as inhibitors of the enzyme MGL (monoacyl glycerol lipase).

The present invention relates to crystalline solvates of 6 (Piperidin 4 yloxy) 2H isoquinolin 1 one hydrochloride processes for their preparation and the use thereof.

The present invention relates to compounds corresponding to formula (I): in which: - A represents a divalent aromatic radical; - X represents a -CH- group or a nitrogen atom; - R1 represents a (C1-C4)alkyl or a (C1-C4)alkoxy; - R2 represents a group Alk; - R3 represents a hydroxyl or a group -NR7R8; - R4 r...

The present disclosure is directed to solid forms of the compound of formula (I): to compositions comprising these forms, and to processes for their preparation. The disclosure also relates to methods for the treatment of neurological disorders through the administration of these forms.

The invention is directed to crystalline forms of 2-[4-(7-ethyl-5H-pyrrolo[2,3-b]pyrazin-6-yl)- phenyl]-propan-2-ol, characterized by physico-chemical data described herein.

The present invention concerns an anti-tumoral composition comprising the compound 1-(6-{[6-(4-fluorophenyl)[1,2,4]triazolo[4,3-b]pyridazin-3-yl]sulfanyl}-1,3- benzothiazol-2-yl)-3-(2-morpholin-4-ylethyl)urea and its use in the treatment of cancer.

2 (2 methylamino pyrimidin 4 yl) 1H indole 5 carboxylic acid [(S) 1 carbamoyl 2 (phenyl pyrimidin 2 yl amino) ethyl] amide for use in the treatment of pain associated with osteoarthritis in the knee.

The present invention is generally directed to an injection device for setting and dispensing a number of user variable doses of a medicament and a method of assembling same. The injection device comprises a housing (10) having a longitudinal axis (I) a dose setting member (60; 80) rotatable relative to the housing ...

The present invention is generally directed to a drug delivery device for selecting and dispensing a number of user variable doses of a medicament. The device comprises a housing (10) a dose selector (80) operable to set a dose by rotation relative to the housing (10) a number sleeve (60) arranged within the housing...

The present invention is generally directed to a clicker arrangement for use in a drug delivery device and a drug delivery device comprising such a clicker arrangement. The arrangement comprises a first rotatable element (60) and a second non rotatable element (110). One of the first element (60) and the second elem...

The present invention is generally directed to a spring arrangement for use in a drug delivery device and a drug delivery device comprising such a spring arrangement. The spring arrangement comprises a clutch spring (130) which is located axially interposed between a stationary housing component (10) and an axially ...

The present invention is generally directed to a drug delivery device for selecting and dispensing a number of user variable doses of a medicament comprising a clicker arrangement. The device comprises a housing (10) a dose selector (80) operable to set a dose by rotation relative to the housing (10) a number sleeve...

The present invention relates to a pen type drug injection device (1; 101) comprising a housing (4, 5; 104, 105), a dose dial member (6; 106), a torsion spring (12; 112) fixed between the housing and the dial member such that energy is accumulated in the torsion spring upon rotation of the dial member relative to th...

The invention provides antibodies that specifically bind to Plasminogen Activator inhibitor type-1 (PAI-1), The invention also provides pharmaceutical compositions, as well as nucleic acids encoding anti-PAI-1 antibodies, recombinant expression vectors and host cells for making such antibodies, or fragments thereof....

The present invention relates to fusion molecules that have binding specificity for pyoverdine type I II and III and pyochelin and can be used in various applications including diagnostic and/or therapeutic applications for example to inhibit or reduce growth of P. aeruginosa and/or to prevent or treat P. aeruginosa...

The present invention provides methods for treating or preventing asthma and associated conditions in a patient. The methods of the present invention comprise administering to a subject in need thereof a therapeutic composition comprising an interleukin 4 receptor (IL 4R) antagonist such as an anti IL 4R antibody. ...

Described is a cap (60) for covering a needle shield (29) on a needle (26) of a medicament container (20), the cap (60) comprising a cylindrical portion (61) having a first outer diameter, a disc portion (62) disposed on a distal end of the cylindical portion (61), the disc portion (62) having a second outer diamete...

The present invention is generally directed to a drug delivery device for selecting and dispensing a number of user variable doses of a medicament and to an insert(12 19) for such a device. The insert comprises a cup shaped body with a distal end and a proximal end. The body has a sidewall (13) and a tube (14) exten...

The present invention is directed to a drive sleeve (40) with a hollow body having a ring of crown teeth (42) with a first outer diameter forming a clutch interface at a first end and a thread (41) extending on an outer surface of the body. The thread (41) has a major diameter and a minor diameter wherein the ring o...

The present invention relates to a drive mechanism which is suitable for an injection device especially a pen type drug delivery device and to such a drug delivery device. The mechanism comprises a spring driven rotatable drive member (120) a rotatable driven member (40) a clutch (41 121) rotationally coupling the d...

The invention relates to a process for preparing 5- aminobenzoylbenzofuran derivatives of formula (I), in which R1 represents hydrogen or an alkyl group and R2 represents hydrogen, an alkyl, alkoxy or dialkylaminoalkoxy group, by reduction of a 5-nitrobenzofuran derivative of formula (II) using a hydrogen transfer a...

This invention relates to a process for the preparation of N-[2-n butyl-3-{4-[(3- dibutylamino)-propoxy] benzoyl} -1-benzofuran-5-yl]-methane-sulfonamide of formula (I) and its pharmaceutically acceptable salts, according to one of the methylsulfonyl groups of the 2-n- butyl-3-[(di-n-butylamino-3-propoxy)-benzoyl]-5...

The invention relates to compounds of formula (I): in which: n is equal to 0 or 1; D represents an oxygen atom or a bond; W represents a nitrogen atom or a -CH- group; X1 represents a nitrogen atom or a -CH=CH- group; X2 represents an oxygen atom or a nitrogen atom; X3 represents an oxygen atom or a nitrogen atom; o...

The invention relates to a process for preparing benzofuran derivatives of general formula I, in which R represents a nitro or ester-COOR" group, where R" represents an alkyl group, R1 represents hydrogen or an alkyl group and R2 represents hydrogen, a halogen, a hydroxyl, haloalkyl, alkyL alkoxy, dialkylaminoalkoxy...

The present invention is generally directed to a method for assembling a drive spring (90) especially into a drug delivery device comprising the steps of rotating a component part (60a) to which the drive spring (90) is attached in a first direction followed by a rotation of the component part (60a) in the opposite ...

The invention refers to an injection device (1) for automatic spring driven injection of a liquid drug by which doses of an individual size can be set by a user the injection device (1) comprising: a housing (3) defining an interior space and having a longitudinal window (7) a rotatable dose dial (2) axially retaine...

The invention relates to a pharmaceutical formulation including, as an active principle, the compound of formula (I) or a salt of said compound with a pharmaceutically acceptable acid.

The present invention relates to conjugales of pyrrolo[1,4]benzodiazepine (PBD) dimers, to compositions containing them and to their therapeutic use, especially as anticancer agents. The invention also relates to the process for preparing the conjugates and to their use as anticancer agents, and also to the dimers t...

The invention relates to the use of (2R 3R)-2-(3-carbamimidoyl-benzyl)-3-[4-(1-oxy-pyridin-4-yl) benzoylamino]-butyric acid methyl ester or a pharmaceutically acceptable salt thereof  for the preparation of a medicament for use in non-ST elevation myocardial infarction  said treatment comprising administering a ther...

Cyclic (aza)indolizinecarboxamides  their preparation and their use as pharmaceuticals The present invention relates to cyclic indolizinecarboxamides and azaindolizinecarboxamides of the formulae Ia and Ib  wherein R  Ra  R10  R20  R30  R40  Y  n  p and q have the meanings indicated in the claims  whic...

The present invention is directed to solid stable pharmaceutical fixed dose compositions comprising irbesartan, amlodipine besilate and pharmaceutically acceptable excipients, to their preparation and to their therapeutic application.

The present invention relates to exendin-4 derivatives and their medical use, for example in the treatment of disorders of the metabolic syndrome, including diabetes and obesity, as well as reduction of excess food intake.

The patent application relates to compounds of formula (I) below: formula (I) to a process for preparing them and to the therapeutic use thereof.

The present invention relates to cryptophycin compounds of formula (I). The invention also relates to cryptophycin payloads to cryptophycin conjugates to compositions containing them and to their therapeutic use especially as anticancer agents. The invention also relates to the process for preparing these conjugates...

ABSTRACT OF THE DISCLOSURE The present invention extends to the compound of formula I: or a prodrug, pharmaceutically acceptable salt, or solvate of said compound. Furthermore, the present invention is directed to a pharmaceutical composition comprising a pharmaceutically effective amount of the compound of formul...

Described is an injection device for administering a dose of a medicament comprising a case having a proximal end and a distal end, a carrier adapted to accommodate a syringe, and a trigger button. In a first state, the trigger button is coupled to the case and/or the carrier and abuts the distal end of the case. In...

Described is an injection device (1) for administering a dose of a medicament (M) comprising a carrier (7) adapted to contain a syringe (3) having a hollow injection needle (4) and a stopper (6), a drive spring (8), a plunger (9) adapted to forward load of the drive spring (8) to the stopper, and a noise component (...

Method for producing pyrazole glycoside derivatives A process for preparing pyrazole-glycoside derivatives of the general formula (I) I in which the meanings are R1 H and R2 F; or R1 F and R2 H; or R1 F and R2 F; R3 (C1-C8)-alkyl  where one  more than one or all hydrogen(s) may be replaced by fluo...

The present invention concerns a method for preparing certain steroidal derivatives alkylated in position 6, comprising a step of alkylating the corresponding compound halogenated in position 6 with an organometallic alkylating agent.

The invention provides a two step chromatography process for small and large scale purification of proteins specifically monoclonal antibodies using only four buffer solutions made from a mother solution.

The invention relates to FGF inhibiting pyrazolopyrimidine derivatives of general formula (I) to a process for preparing them and to the therapeutic use thereof.

Stabilized pharmaceutical formulations of insulin aspart are disclosed. In particular the application is directed to a pharmaceutical formulation comprising (a) insulin aspart; and (b) Zn(ll); and (e) optionally protamine; wherein the pharmaceutical formulation contains less than 0.17 mg/mL sodium chloride. ...

Stabilized pharmaceutical formulations of insulin analogues and/ or insulin derivatives are disclosed. In particular the application is directed to a pharmaceutical formulation comprising (a) at least one analogue and/or derivative of insulin; and (b). Zn(ll); and (c). optionally protamine; wherein the pharmaceuti...

The present invention relates to a process of preparation of Crystal Forms of 4- (cyclopropylmethoxy)-N-(3,5-dichloro-1-oxidopyridin-4-yl)-5-methoxypyridine-2- carboxamide of formula (I), said Crystal Forms which are designated as Crystal Forms A to I A and their use as a medicament.

Generally the present invention relates to the field of steroid hydroxylation. More specifically the present invention relates to a method for the 21 hydroxylation of steroids in cells. It also relates to cells expressing a steroid 21 hydroxylating enzyme or steroid 21 hydroxylase expression vectors comprising a nuc...

The present invention relates to compounds corresponding to formula (I). Process for the preparation thereof and therapeutic use thereof. The compounds are modulators of the activity of AMP activated protein kinase (AMPK) and are useful for treating e.g. diabetes and obesity.

The invention relates to new sulphonylaminopyrrolidinone compounds having antithrombotic activity which in particular inhibit blood clotting factor IXa and/ or factor Xa to processes for their preparation and to use thereof as drugs.

The present invention relates to a polypeptide or polypeptide complex comprising at least the two amino acid sequences arranged to allow for specific binding to the "receptor for advanced glycation endproducts" (RAGE), one or more nucleic acid(s) coding for the polypeptide or polypeptide complex, a cell producing an...

Stabilized pharmaceutical formulations of insulin analogues and/or insulin derivatives are disclosed. In particular the application is directed to a pharmaceutical formulation comprising (a) at least one analogue and/or derivative of insulin; and (b). Zn(ll); and (c). sorbitol; and (d). optionally protamine. ...

Fexinidazole is prepared according to a method which comprises the following steps: a) reacting 1-methyl-2-hydroxymethyl-5-nitro-imidazole with methanesulfonyl chloride in the presence of a suspension of powdered alkaline carbonate in an anhydrous organic solvent suitable for performing nucleophile substitution reac...

The present invention provides for the use of a p75 receptor antagonist or its pharmaceutically acceptable salts for the preparation of a medicament for use in the treatment and/or prevention of overactive bladder.

The present invention relates to a novel process for preparing the compound 4-(cyclopropylmethoxy)-N-(3,5-dichloro-l-oxido-4-pyridyl)-5-methoxypyridine-2-carboxamide of formula (1), in base or hydrate form or in the form of pharmaceutically acceptable salts, and also to several novel synthetic intermediates that are...

Process for the preparation of 3 (6 amino pyridin 3yl) 2 acrylic acid derivatives The present invention relates to a process for the preparation of a compound of the formula (I) which comprises reacting a compound of the formula IV (IV) with the compound of formula VII R15 A2 CHO and to novel intermediate compounds ...

121212The invention relates to novel heterocyclic compounds which are pyrazolopyridine derivatives that induce fibroblast growth factor receptor (FGFR) dimerization having the general formula: M L M in which M or M which may be identical or different each represent independently of one another a monomer unit M and L...

Use of compounds with SGLT-l/SGLT-2 inhibitor activity for producing medicaments for treatment of bone diseases. The invention relates to use of compounds with SGLT-l/SGLT-2 inhibitor activity for producing medicaments for treatment of bone diseases like osteoporosis. Preferred is the use of compounds of the formula...

The invention relates to novel heterocyclic compounds which are pyrazolopyridine derivatives that induce FGFR dimerization having the general formula: M L M 2 in which M and M 2 which may be identical or different each represent independently of one another a monomer unit Mand L represents a linker group which links...

vention is directed to a compound of formula (I);wherein R1,R2 and R3 are as defined a pharmaceutical composition comprising the compound, intermediates and process aking said compounds, and the use of the compound to treat allergic and/or matory disorders, particularly disorders such as allergic rhinitis, asthma, c...

The present invention relates to a method for identifying a cellular target involved in a cell phenotype comprising identifying an intrabody which can modify a cell phenotype and identifying a direct or indirect cellular target of the intrabody. The present invention also relates to intrabodies 3H2-1, 3H2-VH and 5H4...

The present invention relates to exendin-4 derivatives and their medical use, for example in the treatment of disorders of the metabolic syndrome, including diabetes and obesity, as well as reduction of excess food intake.

The present invention relates to exendin-4 derivatives and their medical use, for example in the treatment of disorders of the metabolic syndrome, including diabetes and obesity, as well as reduction of excess food intake.

The present invention relates to exendin-4 derivatives and their medical use, for example in the treatment of disorders of the metabolic syndrome, including diabetes and obesity, as well as reduction of excess food intake.

The invention generally relates to a pharmaceutical composition for oral administration, containing, as active principle, a benzofuran derivative having antiarrhythmic activity, in particular dronedarone and the pharmaceutically acceptable salts thereof, and at least one lipid carrier, said pharmaceutical compositio...

The invention relates to indolizine derivatives of general formula (I), where A, B, m, W, n and R2 are as defined in claim 1, as well as to the method for preparing same and to the therapeutic use thereof.

The present invention pertains to an isolated P450 enzyme comprising or consisting of an amino acid sequence at least 80% identical to SEQ ID NO: 1 wherein said sequence comprises a threonine at position corresponding to position 225 and/or an aspartic acid mutation at position corresponding to position 289. The in...

The invention relates to 6-cycloamino-3-(1H-pyrrolo[2,3-b]pyridin-yl)imidazo[1,2-b]pyridazine derivatives corresponding to the general formula (I) in which R2 represents an aryl group optionally substituted with one or more halogen atoms or C1-6-alkyl, C1-6-alkyloxy, C1-6-alkylthio, C1-6-fluoroalkyl, C1-6-fluoroal...

The present invention relates to combinations of N-[2-(2,l,3-benzothiadiazol-5- ylamino)-6-(2,6-dichlorophenyl)pyrido[2,3-d]pyrimidin-7-yl]-N"(l,l-dimethylethyl)-urea and cytarabine and their use for treating AML or CML.

The present invention relates to a handheld automatic injection device comprising a housing (10, 30, 40; 40"), a piston rod (80) located within the housing (10, 30, 40; 40"), a drive member (70) permanently coupled to the piston rod (80), a dose setting member (50), which during dose setting rotates relative to the ...

Pharmaceutical composition comprising an antibody specifically recognizing CD38 and bortezomib.

The invention relates to a method for preparing morphine-6-glucuronide or one of the derivatives thereof, comprising the following steps: (i) reacting a compound having formula (I), wherein R1 represents a carbonyl group, COR5CO or S02R6S02 with a glucuronic acid derivative having formula (II) wherein PG represent...

The invention refers to a dispensing speed control mechanism for use in an injection device having a release button (71), which is displaceable to initiate dispensing of a set dose, a first component part (42), which is driven by a power reservoir (90) during dose dispensing, and a second component part (12), which ...

The present invention relates to indanone compounds. The indanone compounds are GPR119 modulators and useful for the prevention and/or treatment of diabetes obesity dyslipidemia and related disorders. The invention furthermore relates to the use of indanone compounds as active ingredients in pharmaceuticals and p...

The present invention relates to substituted chroman-6-yloxy-cycloalkanes of the formula (I) in which Ar, R1 to R4, p and q are as defined in the claims. The compounds of the formula (I) are inhibitors of the sodium-calcium exchanger (NCX), especially of the sodium-calcium exchanger of subtype 1 (NCX1), and are suit...

The invention relates to derivatives of 6-cycloamino-3-(1 H-pyrrolo[2,3-b]pyridin-4-yl)imidazo[1,2b]pyridazine with general formula (I). The invention also relates to a method for the preparation and therapeutic application thereof, in the treatment or prevention of illnesses involving casein kinase 1 epsilon and/...

The present invention relates to the use a Robo1-Fc recombinant protein for treating cancer, in particular hepatocarcinoma.

The present invention concerns stable pharmaceutical compositions for monoclonal antibodies for example IgG antibodies. The invention further relates to medicaments and treatments using the pharmaceutical compositions of the invention. Additionally the invention relates to a kit comprising at least one of the pharma...

Provided herein are novel and useful methods for preventing, treating, or ameliorating a macular degeneration such as dry macular degeneration, wet macular degeneration and age related macular degeneration in a patient.

The invention relates to a formula (I), in which R is a hydrogen or halogen atom or a (C1-C6) alkyl group; X is one or more substituents selected from a hydrogen or halogen atom, a (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C6)alkoxy, halo(C1-C6)alkoxy, cyano, hydroxy, or hydroxy(C1-C6)alkyl group; Y is a hydrogen or ha...

The present invention relates to compounds of formula (I): wherein R6 is -CONH2 or a -C(Rα)(Rβ)(OH) group; R is a substituted phenyl or heteroaryl group; R7 is an optionally substituted aryl or heteroaryl group. Process for the preparation thereof and therapeutic use thereof.

The present invention relates to isoindolinone compounds. The isoindolinone compounds are GPR119 modulators and useful for the prevention and/or treatment of diabetes obesity dyslipidemia and related disorders. The invention furthermore relates to the use of isoindolinone compounds as active ingredients in pharmaceu...

A Myelin Basic Protein-luciferase bioimaging noninvasive model to visualize and quantify demyelination and remyelination events in the CNS at transcriptional level in vivo is provided. Luciferase-expressing transgenic animals were generated with myelin basic protein (MBP) promoter coupled to firefly luciferase repor...

The subject of the present invention is a novel process for the preparation of N- [2-n-butyl-3-{4-[(3-dibutylamino)propoxy]benzoyl}-1-benzofuran-5- yl] methanesulfonamide of formula (I) and the new intermediates of the preparation process.

101130405060Amino substituted 3 heteroaroylamino propionic acid derivatives and their use as pharmaceuticals The present invention relates to compounds of the formula (I) wherein A D E G R R R R R and R have the meanings indicated in the claims which are valuable pharmaceutical active compounds. They are inhibitors ...

The invention relates to a companion diagnostic antibody-like binding protein based on the humanized monoclonal antibody, DS6, to be used as diagnostic tool for in vivo detection and quantification of the tumor-associated MUCl-sialoglycotope, CA6.

A treatment for inflammatory bowel disease is disclosed, using a compound: as [4-(5-aminomethyl-2-fluorophenyl)piperidine-1 -y 1] [7-fluoro-1 -(2-methoxyethyl)-4-trifluoromethoxy-1 H-indol-3-yl]methanone.

The subject of the present invention is a novel process for the preparation of TV- [2-n-butyl-3-{4-[(3-dibutylamino)propoxy]benzoyl}-l-benzofuran-5- yl] methanesulfonamide of formula (I) and the new intermediates of the reparation process.

The present invention concerns a method for the treatment and/or prevention of pain and/or Chronic Obstructive Pulmonary Disease (COPD) comprising administering to a subject a composition comprising a polar glycolipid obtainable from cells of a cyanobacterium Oscillatoria species (CyP).

Methods of treating patients with cancer are provided wherein the methods comprise administering to the patient an effective amount of a MEK inhibitor and an effective amount of a PI3K inhibitor. Compositions in which the MEK and PI3K inhibitors are combined also are described.

Described is an an auto-injector (1) comprising a syringe carrier (7) adapted to contain a syringe (3). The syringe carrier (7) has a ramp member (7.1) with a first ramp (7.2) and a second ramp (7.3). The auto-injector (1) comprises a chassis (2) including a resilient beam having a beam head (2.1) adapted to engage ...

The present invention relates to the use of use of a long-acting insulin, in particular insulin glargine, in a method of reducing the risk of progression to type 2 diabetes in a patient, a method of reducing the risk of a new angina in a patient and a method of reducing the risk of a microvascular event in a patient...

The present invention concerns a combination of a ΡΙ3Κβ inhibitor with a RAF inhibitor for its use for the treatment of a patient resistant to at least one RAF inhibitor, a kit comprising the same, its pharmaceutical uses thereof and a method of monitoring the efficiency of said combination when administered to a pa...

The invention relates to pyridine-pyridinone derivatives general formula (I): in which R1, R2, R3, R4, n, n", V, W, Y, Z, Ar are as defined in the description, and to their methods of preparation and their therapeutic applications.

The present invention relates to dual GLP 1 / glucagon receptor agonists and their medical use for example in the treatment of disorders of the metabolic syndrome including diabetes and obesity as well as for reduction of excess food intake.

The invention relates to oxazolopyrimidine compounds of formula (I) where A R1, R2 and R 3 X and Y are defined as stated in the claims. The compounds of formula (I) are suitable for example for wound healing.

21 61 6891 61 6131 64The invention relates to compounds corresponding to the general formula (I) : in which R represents a hydrogen fluorine hydroxyl cyano trifluoromethyl C alkyl C alkoxy or NRR; n and m represent independently of one another an integer equal to 1 2 or 3 it being understood that the sum m+n is at m...

The invention relates to oxazolopyrimidine compounds of formula (I), where A, R , R2" R3, R4 and X are defined as stated in the claims. The compounds of formula I are suitable, for example, for wound healing.

The invention relates to dronedarone or one of its pharmaceutically acceptable salts for the treatment of leishmaniasis, formulations and associations comprising dronedarone or one of its pharmaceutically acceptable salts for the treatment of leishmaniasis.

The invention related to pyrazolonaphthyridinone derivatives of formula (I) to their preparation and to their therapeutic use as selective inhibitors of type 2 methionine aminopeptidase (hMETAP2).

The invention refers to an injection device comprising a housing (10), containing a cartridge (170) with an amount of liquid to be dispensed, a drive sleeve (41), which is rotationally constrained to the housing (10) during dose setting and spring driven rotatable relative to the housing (10) during dose dispensing,...

The present invention relates to a method of identifying a compound involved in pain the use of Il2rg nucleic acid or Il2rg protein for identifying a compound involved in pain as well as methods of diagnosing algesia involving the same.

The invention is directed to a pharmaceutical composition containing at least one FGF 21 (fibroblast growth factor 21) compound, at least one GLP 1R (glucagon - like peptide -1 receptor) agonist and optionally at least one anti - diabetic drug and/or at least one DPP 4 (dipeptidyl peptidase 4) inhibitor for the trea...

The invention relates to compounds of the formula (I) either (i) in the state of a base or an acid addition salt, or (ii) in the state of an acid or a base addition salt, as well as to a method for preparing same and to the therapeutic applications thereof.

The present invention relates herein to compounds and compositions for the treatment and amelioration of inflammatory disease. Specifically the present invention relates to compounds that having a tryptase inhibition activity and the intermediates thereof pharmaceutical compositions comprising such compounds and a m...

The present invention relates herein to compounds and compositions for the treatment and amelioration of inflammatory disease. Specifically the present invention relates to compounds that having a tryptase inhibition activity and the intermediates thereof pharmaceutical compositions comprising such compounds and a m...

The invention relates to novel products of the formula (I) where: - - - - is a single or double bond; Ra is -O- cycloalkyl or -NH-cycloalkyl; X is S, SO or SO2, A is NH or S; W is H, alkyl or COR with R being cycloalkyl; alkyl; alkoxy; O- phenyl; -O-(CH2)n-phenyl with n = 1 to 4; or NR1R2 with R1 is H or alk and R...

The present invention relates to compounds of the formula I wherein A D E G R R R R and R have the meanings indicated in the claims which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A and are useful for the treatment of diseases such as atherosclerosis heart failure re...

The invention relates to novel products of the formula (I) where: (II) is a single or double bond; F is a fluorine atom, Ra is H, HaI, alkoxy, O-cycloalkyl, -O- heterocycloalkyl; -NH-cycloalkyl, -NH-heterocycloalkyl, heteroaryl, phenyl, NHCOaIk, NHCOcycloalk or NR1 R2; X is S, SO or SO2, A is NH or S; W is H, alky...

N-(4-(Azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals The present invention relates to N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides of the formula I, wherein Ar, n, X, Z, R1, R2 and R3 have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically activ...

The present invention relates to dual GLP 1 / glucagon receptor agonists and their medical use for example in the treatment of disorders of the metabolic syndrome including diabetes and obesity as well as for reduction of excess food intake.

The invention refers to an injection device comprising a housing (10; 410), a resilient member (90; 510) adapted to provide a force necessary for ejecting a dose from the injection device, and a dose setting member (80, 60; 420, 440) operatively connected to a dose indicator (120; 480) which is positioned within the...

The present invention relates to methods for treating diseases or conditions in which proprotein convertase subtilisin/kexin type 9 (PCSK9) expression or activity causes an impact by administration of PCSK9 specific antibodies or antigen binding fragments thereof and preferably by additional administration of an inh...

The invention relates to the FGF receptor- activating oligosaccharides corresponding to formula (I) in which R1 represents an optionally substituted -O-alkyl group, R2 represents a hydroxyl group or an -O-alkyl group, R3,R5,R6,R7 and R8 represent -OSO3- or hydroxyl groups, Rrepresents an NH-CO-alkyl or -O-alkyl grou...

The present invention relates to exendin 4 peptide analogues and their medical use for example in the treatment of disorders of the metabolic syndrome including diabetes and obesity as well as reduction of excess food intake.

The present invention is within the field of industrial protein production. The inventors have designed and constructed a new expression system comprising an expression vector coding for a glutamine synthetase of human or dog origin and a CHO cell line. More specifically the invention pertains to a combination of (i...

The invention relates to a method for preparing 3-keto-benzofurane derivatives of the general formula: Formula (I), where R is an alkyl or aryl group R1 is hydrogen or an alkyl or aryl group, and R2 is a substituted alkyl or phenyl group. Said preparation method involves coupling a derivative of Formula III, where ...

A treatment for a dermatological allergic condition is disclosed using a compound: as [4 (5 Aminomethyl 2 fluorophenyl)piperidine 1 yl][7 fluoro 1 (2 methoxyethyl) 4 trifluoromethoxy 1H indol 3 yl]methanone.

The invention relates to a novel process for preparation of drohedarone of formula (I) and pharmaceutically acceptable salts thereof characterized in that a compound of formula (II) is reacted in the presence of a reductive agent with butyraldehyde and/or butanoic acid and isolating the obtained product and if desir...

The invention relates to a process for preparing 5-aminobenzofuran derivatives of general formula: Formula (I), in which R1 is hydrogen or an alkyl group and R2 is an alkyl or dialkylaminoalkyl group. According to the invention, the compounds of formula (I) are prepared by treating a 5-N-alkylamidobenzofuran derivat...

The present invention relates to substituted 2-(chroman-6-yloxy)-thiazoles of the formula I, in which Ar, R2, R3 and R4 are as defined in the claims. The compounds of the formula I are inhibitors of the sodium-calcium exchanger (NCX), especially of the sodium-calcium exchanger of subtype 1 (NCX1), and are suitabl...

The present invention relates to a process for deuteration of amines in the alpha and/or beta position of the N atom by using a deuterium source and a Ruthenium(II) based catalyst.

N-[4-(1 H-Pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides and their use as pharmaceuticals The present invention relates to N-[4-(1H-pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides of the formula I, wherein Ar, R1, R2 and n have the meanings indicated in the claims. The compounds of the formula I ...

The invention relates to a process for preparing 5-sulfonamido-benzofuran derivatives of general formula: formula (I) in which R represents an alkyl or aryl group and R1 and R2 represent hydrogen or an alkyl or aryl group. According to the invention, the compounds of formula I are prepared by coupling a benzofuran d...

Peptidic dual GLP 1 / Glucagon Receptor Agonists derived from Exendin 4 The present invention relates to dual GLP 1 / glucagon receptor agonists or optionally trigonal GLP 1 / glucagon / GIP receptor agonists and their medical use for example in the treatment of disorders of the metabolic syndrome including diabetes...

The invention relates to novel 9H-pyrrolo[2,3-b: 5,4-c'] dipyridine azacarbolines of formula (I), Where: Z2, Z3, and Z4 are CH, CRa, CRs, or N; R3 is H, Hal; CF3, CHF2; OH, alkoxy; NH2, NH (alkyl), N(alkyl)2; C(O)O alkyl; CONH(alkyl), CON(alkyl)2; C1-C10 alkyl; aryl; heteroaryl; R6 is heteroaryl; Ra is CONH2, CONH...

The invention relates to a pharmaceutical composition comprising methyl (2R.3R)-2-{3-[amino(imino)methyl]benzyl}-3-{[4-(1-oxidopyridin-4-yl)benzoyl]amino}butanoate or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable acidic reacting compound or to an aqueous solution or dispersion of the c...

The present invention relates to fexofenadine granules, to a composition containing them and to a process for the hot melt coating of fexofenadine. The process for the hot melt coating of fexofenadine allows efficient masking of its bitter taste without, however unacceptably slowing down its dissolution. ...

The instant invention relates to derivatives of formula (I) and their application in therapeutics.

The invention relates to the compounds of general formula (I): Preparation process and therapeutic use.

The invention provides a three step chromatography process for small and large scale purification of proteins specifically monoclonal antibodies using only four buffer solutions made from a mother solution.

The present invention is generally directed to an injection device for selecting and dispensing a number of user variable doses of a medicament. The injection device comprises a housing (10) having a longitudinal axis (I) a dose setting member (60; 80) rotatable relative to the housing (10) during dose setting a dri...

The present invention relates to ketobenzofuran derivatives of the general formula (D) shown below, as well as to a method for synthesising same by coupling a quinonimine and an enaminone by a Nenitzescu reaction and to the intermediates of the synthesis thereof.

The invention relates to a benzoic acid salt of methyl (2R,3R)-2-{3-[amino (imino) methyl]benzyl}-3-{[4-(1 -oxidopyridin-4-yl)benzoyl]amino}butanoate, and to a benzoic acid salt of methyl (2R,3R)-2-{3-[amino(imino)methyl]benzyl}-3-{[4-(1 -oxidopyridin-4- yl)benzoyl]amino}butanoate which is in a crystalline form or i...

The subject of the present invention is a novel process for the preparation of the [4-(2-chloro-4-methoxy-5-methylphenyl)-5-methyl-thiazolo-2-yl]-[2-cyclopropyl- 1-(3-fluoro-4-methylphenyl)-ethyl]-amine of formula (I) and the new intermediates of the preparation process.

The present invention relates to compounds corresponding to formula (I) and their use as P2Y12 antagonists for the treatment of cardiovascular diseases.

An anti CD19 maytansinoid immunoconjugate is used for treating B-cell malignancies symptom, in particular Non-Hodgkin"s lymphoma.

The present invention relates to nicotinamide derivatives of formula (I), to compositions containing same, and to the therapeutic use thereof, in particular as anticancer drugs. The invention also relates to the method for preparing said compounds, as well as to some of the intermediate products. ...

6-(4-Hydroxy-phenyl)-3-styryl-1 H-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors The present invention relates to pyrazolo[3,4-b]pyridine compounds of the formula I, in which R1, R2, R3, R4 and R5 are defined as indicated below. The compounds of the formula I are kinase inhibitors...

The invention relates to novel pyrimidinone-based heterocyclic compounds which are parasite growth inhibitors, having the general formula (I) in which Y is a morpholine chosen from three bridged morpholines, L is a bond or a linker, n = 0 or 1 and R2 is a methyl group when n = 0 and a hydrogen atom when n = 1. Proce...

Indanyl-substituted 4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridines, their use as medicament, and pharmaceutical preparations comprising them The invention relates to substituted 4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridines of formula I, their use as medicament, and pharmaceutical preparations comprising...

The inventions relates to the compounds of formula (I) where: R is a hydrogen atom or a group selected from the (C1d- C6)alkyl and (C3-C7)-cycloalkyl groups, optionally substituted by one or more groups independently selected from a fluorine atom, the (C3-C7)-cycloalkyl, (C2-C4)alkenyl, phenyl, (C1-C6)alkoxy, and hy...

Formula I An improved synthesis method for making diazaindoles using a Chichibabin cyclization is disclosed. In particular, this method is useful for making the compound of Formula I.

The present invention relates to macrocydic urea derivatives of the formula I (I) in which R1, R2, R3, V and Y are as defined below. The compounds of the formula I are inhibitors of the enzyme TAFIa (activated thrombin-activatable fibrinolysis inhibitor). The invention further relates to the process for the preparat...

The subject of the present invention is compounds corresponding to the formula (l) in which: X represents a divalent (C2-C5)alkylene radical which is imsubstituted or substituted one or more times by an Alk group; R1 represents a phenyl, a naphthyl, n pyridyl, a 1-benzoin ienyi or a 1,3- benzodioxolyl; R2 repr...

The present invention relates to a method of identifying a compound involved in pain the use of Car3 nucleic acid or Car3 protein for identifying a compound involved in pain as well as methods of diagnosing algesia involving the same.

The subject matter of the invention is quinazolinedione derivatives of formula (I) with A being a sulphur or oxygen atom or a sulphoxide or a sulphone group, methods for obtaining same and therapeutic uses thereof, such as cancer, diabetes, muscle diseases, bone diseases, cardiovascular diseases, central nervo...

Pharmaceutical composition comprising aflibercept, folinic acid, 5-fluorouracil (5-FU) and irinocetan (FOLFIRI) useful in the treatment of Colorectal cancer (CRC).

The invention relates to a pharmaceutical antitumor combination including cabazitaxel and capccitabinc, wherein both of said antitumor agents may be in the form of a base, in the form of a pharmacemically acceptable acid salt or in the form of a hydrate or solvate, intended for the treatment of metastatic breast c...

The invention relates to novel products having formula (I), wherein: R4 represents H, CH3, CH2CH3, CF3, F, Cl, Br, I; Het represents a heterocycle optionally substituted by one or more R1 or R'1 radicals selected from H, halogen, CF3, nitro, cyano, alkyl, hydroxy, mercapto, amino, alkylamino, dialkylamino, alkoxy,...

The present invention concerns the use of dronedarone or a pharmaceutically acceptable salt thereof, for the preparation of a medicament for use in the prevention and/or treatment of patients with atrial fibrillation (AF) or atrial Flutter (AFL), shortly after discontinuation of a previous treatment with amiodarone....

The invention relates to the novel products of formula (I) with p, q = 0, 1 or 2; R1 = phenyl, pyridyl; -(CH2) m -Ra; alkylene; cycloalkyl; heterocycloalkyl; alkyl; -SO2 -Rb; -CO-Re; m = 1 or 2; Ra = aryl, heteroaryl, -CO-cycloalkyl, -CO-heterocycloalkyl, -CO-Rb, -C(Rb)=N-ORc, -CO 2 Rd, -CONRxRy; Rb = alkyl, aryl, h...

The subject of the present invention is a process for preparing a genetically modified yeast by multicopy integration of at least four expression cassettes, allowing the production of a molecule of interest at high titre. The subject of the present invention is also yeasts transformed according to said process, and ...

The invention relates to compounds of the general formula (I) where: R2 is a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy, or NR8R9 group; m, n, o and p independently are a number from 0 to 3; A is a covalent bond, an oxygen atom, a C1-6-alkylene group or a -O-C1-6-alkyl...

The invention concerns an antitumoral combination comprising ombrabulin, a taxane derivative and a platinum derivative and its use in the treatment of advanced solid tumors.

The subject of the invention is a novel process for the preparation of N-[2-n-butyl-3-{4-[(3-di- n-butylamino)-propoxy]benzoyl}benzofuran-5-yl]- methanesulfonamide of formula (I), and pharmaceutically acceptable salts thereof characterized in that, the acyl group of the benzofuran derivative of the general formula (...

The invention relates to compounds corresponding to formula (I): N R1 O R3 R4 R2 (I) in which - R3 and R4 together form, with the carbon atoms of the phenyl nucleus to which they are attached, a 6-membered nitrogenous heterocycle corresponding to one of formula (A), (B) or (C) below: N N O O Ra Ra" N N O Rb Rb" N O ...

The invention relates to a targeting agent, to which at least one cryptophycin is attached, of the formula (I), where: R1 is a halogen atom and R2 is an OH group, an acyl group derived from an amino acid AA or a (C1-C4)alkanoyloxy group; or else R1 and R2 together form an epoxy unit; AA denotes a natural or artifi...

The disclosure relates to fumarate salts of 2-(cyclohexylmethyl)-A/-{2-[(2S)-1-methylpyrrollclin-2-yl]ethyl}-1,2,3,4-tetrahydroisoquinolie-7-sulfonamide, to pharmaceutical compositions thereof, processes for making the same, and methods of use thereof.

The present invention relates to an extracellular binding domain for an allosteric inhibitor, whereby said binding domain is derived from a single membrane span tyrosine kinase receptor. More specifically, the invention relates to an extracellular domain derived from a Fibroblast Growth Factor Receptor (FGFR). It fu...

The invention relates to the novel materials of formula (I), where: R1 is an optionally substituted aryl or heteroaryl; R is an II or, when formed with R1, a 5- or 6-member ring fused with an aryl or heretoaryl group optionally containing one or more of 0, S, N, NH, and Nalk, being optionally substituted; R2 and R...

The subject of the invention is indolin-2-one derivatives of formula: in which: - W represents a -CH2- or -SO2- group; - Cy forms, with the carbon to which it is bonded, a non-aromatic, saturated or unsaturated C3-C12 hydrocarbon ring which is optionally condensed or substituted by one or a number of (C1-C7)alkyl...

The invention relates to a pharmaceutical composition containing as active ingredients - a compound (a) selected from 1-(2-naphth-2-ylethyl)-4-(3-trifluoromethylphenyl)-1,2,3,6-tetrahydropyridine and a compound of formula (I) : in which Y is -CH- or -N- ; Rl is hydrogen, halogen, a CF3, (03-04) alkyl or (C1-C...

The invention relates to a sequential antitumor combination of AVE8062, or a salt thereof, and docetaxel, characterized in that AVE8062 is administered to a patient in a dose of 10 to 50 mg/m2, and then, on a different day of the week, preferably after a 24-hour interval, docetaxel is administered in a dose of 50 ...

The present invention discloses and claims a series of substituted N-phenyl- bipyrrolidine carboxamides of formula (I). Wherein R1, R2, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especi...

The invention relates to derivatives of 6-cycloamino-2-thienyl-3-(pyridin-4-yl)imidazo[1,2-b]-pyridazine and 6-cycloamino -2-furanyl-3-(pyridin-4-yl)imidazo[1,2-b]-pyridazine with general formula (I). The invention also relates to a method for the preparation and therapeutic application thereof, in the treatment o...

The invention relates to compounds according to the formula (I): R is a -S02-NR3R4 group, a hydrogen atom, a halogen atom, a -halogeno(C 1 -C5)alkyl group, a -CO2R5 group or a -SO2-R4 group; Rl is a heterocycloalkyl group containing no nitrogen atoms, a -W-(C3-C6)cycloalkyl group, a -W-aryl group, a -W-heteroaryl ...

The invention relates to compounds with the formula (I), in a basic state or as an acid addition salt: (I) where n is equal to 0, 1, 2, 3 or 4; m is equal to 0, 1 or 2; o is equal to 0 or 1; X is a -CH2,-CH(R")-, -NH(R")- group or a heteroatom selected from among O and S, where R" is a -(C1 -C5)alkyl, -(C1-C5)alco...

The invention relates to a compound of the general formula (I) in which R2 is a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy, NR8R9 group; m, n, o and p are independently an integer equal to 0, 1, 2 or 3; A is a covalent bond or a C1-8-alkylene group; R1 is an optionally...

The invention relates to novel products of the formula (I) where: (II) is a single double bond; Ra is -O-Z-Rc with Z being a single bond or optionally substituted alkylene and Rc being optionally substituted cycloalkyl, heterocycloalkyl, aryl or heteroaryl; Rb is H or F; if Rb is H, then Rc is not cycloalkyl when ...

The invention relates to disubstituted 3-benzofuranyl-indol-2-one-3-acetamidopiperazine derivatives of the general formula (I) where R1, R2, R3, R4, R5, R6, R7, R8, R9 and n are such as defined in claim 1, to a method for preparing same, and to the therapeutic use of said compounds.

The present invention relates to a process for the preparation of a compound of the formula (I), which comprises reacting a compound of the formula (IV) with an oxalic acid diester and to novel intermediate compounds used therein.

The invention relates to compounds of the general formula (I) where: R2 is a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy, or NR8R9 group; m and p have a value of 1; n and o have the same value which is 0 or 1; A is a covalent bond or a C1-8-alkylene group; R1 is an opti...

The present application relates to humanized antibodies specific to the protofibrillar form of the beta-amyloid peptide, and to the use of said antibodies in the field of Alzheimer's disease.

The invention relates to compounds of the general formula (I) where: R2 is a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy, or NR8R9 group; m, n, o and p independently are a number from 0 to 3, provided that m+n ≤ 7 and that o+p ≤ 7; A is a covalent bond, an oxygen atom, ...

The invention relates to a compound of formula (I), more specifically in the levorotatory form (1a) thereof, in particular the form having a rotatory power [α]D= -38.6+0.7 at a concentration of 0.698 mg/ml in methanol. The compound may be in the form of a base or an acid addition salt, in particular a pharmaceu...

The invention relates to the novel materials of formula (I), where R1 is an optionally substituted L-aryl or L- heteroaryl, such that L is: an alkyl or CO, or L□X, with L□being an alkyl and X being O or S; R2 is H or an alkyl; R3 is an alkyl optionally substituted by Hal; and R4 is Hou Hal, wherein said materials ...

A process for the production of 2-alkyl-3-aroyl-5-nitrobenzofurans by acylation of 2-(2-hydroxy-5-nitrophenyl)-1-aryl-ethanones and subsequent treatment of the esters with combinations of bases and proton acids or Lewis acids. This process can be used for the production of Dronedarone. Furthermore, novel intermedi...

Process for the production of Dronedarone intermediates A process for the production of Dronedarone intermediates of the formula I by acylation of 2-(2-hydroxy-5-nitrophenyl)-1-(4-methoxyphenyl)-ethanone, subsequent treatment of the ester with bases and a zeolite (alumosilicate) catalyst and optional subseque...

The invention relates to FGF receptor-activating N-acyl octasaccharides having Formula (I), wherein: R1 is an O- alkyl group optionally replaced by one or more aryl or cycloalkyl groups, R2 is an OSO3- or hydroxyl group, R3 is an alkyl, cycloalkyl, or alky-cycloalkyl group, R4 is a disaccharide having Formula (II)...

The invention relates to FGF receptor-activating N-sulfate oligosaccharides having Formula (I), wherein R1, R4, R6, and R2 are -OSO3- or hydroxyl groups, R2 is an -O-alkyl group or a monosaccharide having Formula (II), R3 is a disaccharide having Formula (III), R3 is a disaccharide having Formula (IV), R7 is ...

(57) Abstract : The invention relates to novel conjugates of pyrrolo[l,4]benzodiazepine dimers (I) which can be used as anticancer agents.

Abstract Novel crystalline heteroaromatic fluoroglycoside hydrates  pharmaceuticals comprising these compounds and their use The invention relates to crystalline hydrates of the formula I I in which n has a value of from 2.1 to 2.5. The compound is suitable  for example  as an antidiabetic. ...

Present invention concerns the use of Cathepsin H. Other aspects of the invention concern methods for screening pharmaceuticals  for diagnosing pain susceptibility and for the treatment of pain.

The present invention relates to a series of substituted dihydro benzocycloalkyl-oxymethyl oxazolopyrimidinones of formula (I): (I) Wherein n  R1  R2  R3  R4  R5 and R6 are as defined herein. This invention also relates to methods of making these compounds including novel intermediates. The compounds of this i...

The invention relates to solid pharmaceutical compositions comprising (Z)-2-cyano-3-hydroxy-but-2-enoic acid-(4'-trifluoromethylphenyl)-amide, as well as a process for the preparation of the same, methods of using such compositions to treat subjects suffering from autoimmune diseases in particular systemic lupus ery...

The invention relates to a compound of formula (I): wherein : • ALK is a (C1-C6)alkylene group; • X1 et X2 are each independently one of the following groups : -CH=CH-, -CO-, -CONR-, - NRCO-. -COO-. --OCO-. -OCONR-. -NRCOO-. -NRCONR'-. -NR-. -S(O)n (n=0,1 or 2) or O-; • R and R' are independently H or a (C1-C6)alk...

The present disclosure relates to an antibody or an epitope-binding fragment thereof that specifically binds to an EphA2 receptor. It further relates to a conjugate comprising a cytotoxic agent which is covalently bound to the antibody and a method for preparing such a conjugate.

The present invention relates to the use of ferroquine, the N-demethylated metabolite or any of the pharmaceutically acceptable salts thereof for treating and/or preventing infections caused by a parasite belonging to the Plasmodium genus, the life cycle of which includes a phase of hepatic latency in the human host...

The invention relates (i) to pyridine-pyridinone derivatives with the formula (I): where R1 is a hydrogen atom or a (C1-C4)alkyl group; R2 is a (CH2)n-B group, in which n" = 0, 1, 2, 3 or 4 and B is a (C3-C5)cycloalkyl group, a (C1-C4)alkyl group or a (C1-C4)alkoxy group; Y, Z, V and W are, independently from one ...

The invention relates to (heterocycle/tetrahydropyridine)-(piperazinyl)-1-alcanone and (heterocycle/dihydropyrrolidine)-(piperazinyl)-1-alcanone derivatives of the general formula (I), where A, W, n, and R2 are as defined in claim 1. The invention moreover relates to the method for preparing said derivatives and t...

The invention relates to (heterocycle/condensed piperidine)- (piperazinyl)-1-alcanone or heterocycle/condensed pyrrolidine)- (piperazinyl)-1-alcanone derivatives of the general formula (I), where A, W, n, and R2 are as defined in claim 1. The invention moreover relates to the method for preparing said derivat...

FR2009/113 PCT PATENT APPLICATION TITLE Novel antagonist antibodies and their Fab fragments against GPVI and uses thereof SANOFI-AVENTIS ABSTRACT The present invention discloses novel antibodies that specifically bind to the human platelet membrane protein Glycoprotein VI (GPVI) and their monovalent fragments or d...

The present invention relates generally to transgene constructs, transgenic non-human animals comprising transgene constructs, methods of making and methods of using the transgenic non-human animals comprising transgene constructs. An embodiment of the invention relates to methods of assaying the activation of GPCR ...

The invention relates to oxazolopyrimidine compounds of formula (I), where A, R , R " R , R4 and X are defined as stated in the claims. The compounds of formula I are suitable, for wound healing.

The invention relates to 5-oxo-5, 8-dihydropyrido [2, 3-d] pyrimidine derivatives of the general Formula (I). The invention also relates to the method for preparing same and to therapeutic use thereof.

The invention relates to oxazolopyrimidine compounds of formula (I), where A, R , R2" R3, R4" X and Yare defined as stated in the claims. The compounds of formula I are suitable, for example, for wound healing.

The invention relates to oxazolopyrimidine compounds of formula I  where A  R1 and R2 are defined as stated in the claims. The compounds of formula I are suitable  for example  for hound healing.

The present invention relates to a method of identifying a compound involved in pain the use of Lrrfip1 nucleic acid or Lrrfip1 protein for identifying a compound involved in pain as well as methods of diagnosing algesia involving the same.

NIndustrially applicable process for preparing 2 (cyclohexylmethyl) {2 [(2S) 1 methylpyrrolidin 2 yl]ethyl} 1 2 3 4 tetrahydroisoquinoline 7 sulfonamide and salts thereof.

Industrially applicable process for preparing 2 (cyclohexylmethyl) N {2 [(2S) 1 methylpyrrolidin 2 yl]ethyl} 1 2 3 4 tetrahydroisoquinoline 7 sulfonamide and salts thereof.

2 1 103 103 71 61 63 73 73 71 61 101 61 101 101 63 71 63 101 103 101 101 63 73 71 61 6Compounds corresponding to the general formula (I) in which R represents a group C alkyl C cycloalkyl C cycloalkyl C alkyl C alkyl C cycloalkyl C cycloalkyl C cycloalkyl C alkylthio C alkyl C alkoxy C alkyl hydroxy C al...

The invention relates to aryloxy alkylene substituted hydroxyphenyl hexynoic acid derivatives of formula (I) and to their physiologically compatible salts. The compounds are suitable for for example the treatment of diabetes because they cause an increased insulin release by activating the GPR40 receptor. ...

The present invention concerns a method of managing the risk of liver injury in patients receiving treatment with dronedarone or pharmaceutically acceptable salts thereof.

1030405060The present invention relates to compounds of the formula (I) wherein A D E L G R R R R and R have the meanings indicated in the claims which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A and are useful for the treatment of diseases such as atherosclerosis he...

The present invention relates to Pharmaceutical compositions comprising an antibody specifically binding to human proprotein convertase subtilisin/kexin type 9 (PCSK9) to methods for treating diseases or conditions in which proprotein convertase subtilisin/kexin type 9 (PCSK9) expression or activity causes an impact...

233The invention relates to a novel process for preparation of dronedarone (I) and pharmaceutically acceptable salts thereof where the compound of formula (II) or salt thereof is reacted with a compound of formula L (CH) CH (III) where L is a leaving group and isolating the obtained product and if desired converting...

The invention provides antibody like binding proteins comprising four polypeptide chains that form four antigen binding sites wherein each pair of polypeptides forming an antibody like binding protein possesses dual variable domains having a cross over orientation. The invention also provides methods for making such...

Antibodies are provided which specifically bind human and Macaca fascicularis lysosomal-associated membrane protein 1 (LAMP1) proteins and immunoconjugates comprising said antibodies conjugated or linked to a growth inhibitory agent. Pharmaceutical compositions comprising antibodies or immunoconjugates of the invent...

The disclosure provides antibodies that specifically bind to Kallidin or des-Arg10-Kallidin. The disclosure also provides pharmaceutical compositions, as well as nucleic acids encoding anti-Kallidin or des- Arg10-Kallidin antibodies, recombinant expression vectors and host cells for making such antibodies, or fragme...

The invention relates to a compound of the general formula (I), where: R is a hydrogen atom or a group selected from the (C1-C6)alkyl or (C3-C7)-cycloalkyl groups, optionally substituted by one or more groups independently selected from a halogen atum and the (C3-C7)-cycloalkyl, (C1-C6)alkyl, (C1-C6)alkoxy, and hy...

Pharmaceutical composition containing a combination of a non steroidal anti inflammatory drug and a colchicoside derivative, the active ingredients being present in the free state or in the form of a salt.

The invention relates to 3-benzofuranyl-indol-2-one derivatives substituted at the 3 position and of the formula (I) where R1, R2, R3, R4, R5 and n are such as defined in claim 1, to a method for preparing same, and to the therapeutic use of said compounds.

The invention relates to a method of synthesis of ferroquine of formula (F) or of its metabolite of formula (Fm): comprising a reaction of reductive amination, said reaction comprising: (i) a stage of condensation of the aldhehyde-amino ferrocene of formula (1 ), which R represents a hydrogen atom or a methyl group,...

The invention relates to compounds corresponding to formula (I): R4 NN R1 O R2 R3 (I) 5 6 7 8 in which - R2 and R3 together form, with the carbon atoms of the phenyl nucleus to which they are attached, a 6-membered nitrogenous heterocycle corresponding to one of formula (A), (B) or (C) below: N N O O Ra Ra" N N O Rb...

The invention refers to an injection device comprising a housing (10; 410), a resilient member (90; 510) adapted to provide a force necessary for ejecting a dose from the injection device, and a dose setting member (80, 60) operatively connected to a dose indicator (120; 480) which is positioned within the housing (...

A subject-matter of the present invention is the use of compounds of formula (I) in the base, hydrate or solvate form or in the form of their mixtures, as medicaments or for the preparation of medicaments intended for the treatment of at least one cardiovascular disease and/or to prevent the appearance of at l...

Functional PLA-PEG copolymers, the nanoparticles thereof, their preparation and use for targeted drug delivery and imaging The present invention concerns novel functional PEG-PLA containing copolymers, the nanoparticles containing the same, their process of preparation and their use for site specific targeted drug d...

The invention relates to a method for preparing an activated ester of the formula (I), where R is a (C1-C6) alkyl, aryl, heteroaryl, cycloalkyl, or heterocycloalkyl group, and ALK is a (C1-C6) alkylene group, said method consisting of reacting the dicyclohexylamine P1 salt and the disuccinimidyl carbonate (DSC) ...

Provided are methods for the treatment or prevention of microbial infections (e.g., nocosomial infection) in which the underlying pathology involves a PNAG-containing microbial bio film. The methods the invention generally involve administering to the subject an effective amount of an antibody that specifically bind...

The invention relates to a dose of 10 mg of AVE5026 for the treatment of venous thromboembolism in patients with severe renal impairment.

The invention relates to compounds of general formula (I) wherein R is a hydrogen atom or a group selected from the groups (C1-C6) aIkyI, (C3-C7) cycloalkyl, benzyl or allyl optionally substituted by at least one group selected independently from each other from the halogen atoms, the groups (C3-C7) cycloalkyl, (C1-...

The present invention refers to the gene cluster and genes comprised by the gene cluster which are involved in the biosynthesis of griselimycin and methylgriselimycin and to the use of the gene cluster genes comprised thereby and proteins encoded thereby for the production of antibiotic agents. ...

The invention relates to compounds corresponding to formula (I) in which R1, R2 and R3 are as defined in Claim 1, and also to the process for preparing them and to their therapeutic use.

The present invention relates to compounds of formula 1 that are useful as an active ingredient of a medicament for preventive and/or therapeutic treatment of diseases caused by abnormal activation of CXCR3 chemokines. The invention relates furthermore to a process for the preparation of said compounds to pharmaceut...

The present invention relates to pharmaceutical compositions to be used in a solid galenic form for oral administration and primarily including dronedarone and/or at least one of the derivatives thereof as well as to solid galenic forms manufactured as such from said compositions preferably in the form of tablets or...

The invention refers to a handheld injection device comprising a housing (10; 410)and a dose indicator (90; 480) positioned within and axially constrained to the housing (10; 410) and rotatable with respect to the housing (10; 410) during dose setting and during dose dispensing. The dose indicator (90; 480) may comp...

The present invention relates to an oral pharmaceutical fixed dose composition for use in the treatment of tuberculosis, said oral pharmaceutical composition comprising: a) granules comprising isoniazid and at least one intragranular excipient, b) granules comprising rifapentine and at least one intragranular excipi...

The present invention relates to an oral pharmaceutical fixed dose composition in a form of a dispersible tablet for use in the treatment of tuberculosis, said oral pharmaceutical composition comprising: a) granules comprising isoniazid and at least one intragranular excipient, b) granulescomprising rifapentine and ...

The present invention relates to a monolayer tablet for use in the treatment of tuberculosis comprising a mixture of: - granules comprising isoniazid, pyrazinamide, ethambutol or a pharmaceutically acceptable salt thereof and at least one granulation binder, - rifampicine in powder form, - extragranular excipients, ...

The present invention is generally directed to a drug delivery device for selecting and dispensing a number of user variable doses of a medicament and to a housing for such a device. The housing comprises an outer housing (10) with a distal end and a cartridge holder (20) with a proximal end which when the cartridge...

The present invention relates to glucagon receptor agonists and their medical use for example in the treatment of severe hypoglycemia. Provided are exendin 4 analogues which potently and selectively activate the glucagon receptor and show a higher solubility at a near neutral pH and an enhanced chemical stability in...

The present invention refers to a drug delivery device comprising a housing (5, 10) with an opening (12), a piston rod (11) having a proximal end and a distal end, at least a portion with an interface (14) adapted to engage the opening (12) for guiding the piston rod (11) during a distal or proximal movement of the ...

A drug delivery device (1) is proposed, comprising: a housing (10, 350); a drive mechanism (5); a cartridge (301) containing a drug (307), the cartridge being retained in a defined position relative to the housing, wherein the drive mechanism is configured to dispense drug from the cartridge; a cartridge bias system...

An arrangement of drug delivery devices (1) is provided with interchangeable members and non-interchangeable members.

A cartridge assembly (300) for a drug delivery device is proposed, comprising a cartridge (301) containing a drug (307), the cartridge comprising a dispensing end (306), a cartridge holder (302), the cartridge holder defining an interior cartridge holding section (303), where the cartridge is arranged within the car...

A system for a drug delivery device (1) is provided, comprising: a housing (10, 350), a cartridge unit (300), which is attachable to the housing or releasably attached to the housing, wherein the cartridge unit comprises a cartridge unit guide feature (327), the cartridge unit guide feature being provided to establi...

The present invention concerns antibody-like binding protein specifically binding to CD3 and CD123. The invention also relates to pharmaceutical compositions comprising said antibody-like binding protein and the use of said pharmaceutical compositions and antibody-like binding protein to treat cancer. The invention ...

High concentration antibody formulations capable of stable long-term storage are disclosed.

The present disclosure relates to compounds of formula (I) or a pharmaceutically acceptable salt thereof wherein R1 means a fluorine atom or a perhalogeno linear alkyl radical containing 1, 2 or 3 carbon atoms; R2 means a chlorine atom, a linear alkyl radical containing 1, 2 or 3 carbon atoms or a perhalogeno linear...

The present invention relates to 8-aryl-substituted and 8-heteroaryl-substituted 9H-pyrido[3,4-b]indoles of the formula (I), in which A, E, G, R1 to R6 and R10 are as defined in the claims, which stimulate chondrogenesis and cartilage matrix synthesis and can be used in the treatment of cartilage disorders and condi...

The present invention is within the field of industrial protein production. The invention provides a novel expression system using dehydroorotate dehydrogenase (DHODH) as a selection marker in combination with leflunomide or a metabolite thereof notably for use in mammalian cell lines. Expression vectors encoding DH...

The present invention provides stable pharmaceutical antibody formulations, including lyophilized formulations, comprising an anti-IL-4/anti-IL-13 bispecific antibody and a buffering system, wherein the pH of the formulation is about pH 7, and wherein the formulation has a low salt concentration in order to reduce t...

The subject matter of the present invention is the use of compounds of formula (I) in the form of a base, a hydrate or a solvate, or of mixtures thereof as a medicament or for preparing a medicament intended for the treatment and/or prevention of disorders associated with the central nervous system (abbreviated to...

The present invention relates to compounds of the formula I, wherein A, Y, Z, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by ly...

The invention relates to a compound of formula (I), where: R1 is a phenyl group optionally substituted by one or more halogen atoms; R2 is: a hydrogen atom or a halogen atom or a cyano group; a -C(=O)Y group where Y is a hydrogen atom, or a - NH2 or -OR3 group; a -C(=S)NH2 group; a -C(=NH)NH-OH group; a -CH2OH or ...

The present invention discloses and claims a series of substituted indolyl piperidinyl benzylamines of formula (I) wherein R1 R2 and R3 are as described herein. More specifically the compounds of this invention are inhibitors of ß tryptase and are therefore useful as pharmaceutical agents. Additionally this inventio...

123The invention relates to oxazolopyrimidine compounds of formula (I) where A R R and R are defined as stated in the claims. The compounds of formula (I) are suitable for example for wound healing.

The present invention relates to a method for "hot melt coating" of pharmaceutical active ingredients characterized by organoleptic or physicochemical properties that it is desirable to mask. The invention also relates to the resulting medicinal active ingredients with masked organoleptic orphysicochemical propertie...

The invention provides a packaging for a container (2) filled with a liquid pharmaceutical product and comprising a head (4) and a body (3) both made from a single piece and a neck portion (5) configured to form a frangible junction (6) between said head (4) and said body (3), said packaging (11) being made from pla...

Described is a safety device (30) for a medicament container (20) comprising a first sheath (31) having a first ledge (35) and a second ledge (36), a second sheath (32) telescopically arranged with the first sheath and releasably coupled to the first ledge (35), and a finger flange (50, 500) having at least one resi...

An aqueous pharmaceutical formulation comprising 200 -1000 U/mL of insulin glulisine.

The present invention relates to substituted fused heterocyclic compounds. The substituted fused heterocyclic compounds are GPR1 19 modulators and useful for the prevention and/or treatment of diabetes obesity dyslipidemia and related disorders. The invention furthermore relates to the use of substituted fused heter...

The present invention is generally directed to an assembly for a drug delivery device comprising a first threaded member (50 50 ) a second threaded member (40 60 ) with a longitudinal axis and a thread (61) having at least two consecutive portions (62 63 64) with different leads. The first threaded member (50 50 ) a...

The present invention relates to polypeptide variants of human fibroblast growth factor 21 (FGF21) and fusion molecules thereof, as well as to nucleic acid molecules encoding the same. It further relates to their use as medicaments, in particularfor the treatment of obesity, overweight, metabolic syndrome, diabetes ...

Provided herein are compositions comprising trispecifie and/or trivalent binding proteins comprising four polypeptide chains that form three antigen binding sites that specifically bind one or more HIV target proteins or one or more T-cell receptors where in a first pair of polypeptides forming the binding protein p...

Methods for determining an in vitro release profile of peanut allergens in a sample are provided. Methods for determining one or more signatures of peanut allergens in a sample are provided.

The present invention relates to exendin-4 peptide analogues which selectively bind and activate the glucagon receptor and comprise a chelating moiety capable of binding a metal ion and their use for example in PET imaging.

The present invention relates to compounds of formula (I): wherein R1 and R2 represent hydrogen or deuterium atoms; R3 represents a hydrogen atom or a -COOH, a -OH or a -OPO(OH)2 group; R4 represents a hydrogen atom or a fluorine atom; R5 represents a hydrogen atom or a -OH group; wherein at least one of R3 or R5 is...

The invention provides antibody-like binding proteins comprising four polypeptide chains that form four antigen binding sites, wherein each pair of polypeptides forming an antibody¬like binding protein possesses dual variable domains having a cross- over orientation. The invention also provides methods for making su...

The present application relates to humanized antibodies specific to the protofibrillar form of the beta-amyloid peptide, and to the use of said antibodies in the field of Alzheimer"s disease.

Generally, the present invention relates to the field of antibodies. In particular, it relates to multispecific antibodies, e.g. bispecific antibodies, which are modified such that the desired chain pairing takes place and/or can be selected for. Specifically, this is achieved by using different dimerization domains...

The present invention relates to novel substituted N-(3-fluoropropyl)-pyrrolidine compounds of formula (l-A): wherein R1 and R2 represent independently a hydrogen atom or a deuterium atom; A represents an oxygen or nitrogen atom; and SERM-F represents a selective estrogen receptor modulator fragment comprising an ar...

The present invention concerns antibodies and antigen-binding fragments of antibodies which specifically bind to and neutralize Chikungunya virus (CHIKV) and which are engineered to develop therapeutics in order to treat CHIKV disease or prevent CHIKV infection. The invention also relates to pharmaceutical compositi...

The present invention relates to a method of preparing a lysine side-chain modified peptide by solid phase peptide synthesis.

This disclosure relates to the field of therapeutic RNAs for treatment of solid tumor cancers.

Herein are provided a combination of palbociclib and of 6-(2,4-dichlorophenyl)-5-[4-[(3S)-1 -(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7H-benzo[7]annulene-2- carboxylic acid or a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing such a combination, and the therapeutic use...

The present disclosure relates to medicament injection devices. According to a first aspect, this disclosure describes an injection device comprising: a movable dosage programming component comprising a rotary encoder system having a predefined angular periodicity; a sensor arrangement comprising a first optical sen...

This disclosure relates to antigenic respiratory syncytial virus (RSV) polypeptides for use in eliciting antibodies against RSV. Also disclosed are antigenic polypeptides comprising an RSV polypeptide and a ferritin protein.

The present invention concerns a method for purifying a protein comprising in a continuous mode: one filtration step involving the use of at least one chelating agent, an exchanging step involving the use of at least one diafiltration membrane, and a polishing step involving the use of a combination of membrane adso...

The invention relates to methods of treating a hepatitis B virus (HBV) infection in a subject in need thereof, comprising administering to the subject a combination of a tumor necrosis factor receptor superfamily (TNFRSF) agonist (e.g., a an agonistic antibody directed against the receptor, a soluble TNFRSF agonist ...

The present invention relates to a biologically active single chain Relaxin peptide having the following formula (I): Nter-Ac-X10-E-G-R-E-X15-V-R-X18-X19-I-X21-X22-E-G-X25-S-X27-X28-X29-X30-X31-X32-X33-NH2-Cter or a salt or solvate thereof. It also concerns a pharmaceutical composition comprising at least one peptid...

Binding proteins comprising a pseudoFab domain including a stabilised knockout domain and a second VH/VL that form a first functional antigen binding domain are provided. Multispecific binding proteins comprising at least one pseudoFab are also provided. Multispecific binding proteins, nucleic acids encoding binding...

Binding proteins comprising a VL region paired with a VH region, and a CH1 region paired with a CL region, wherein the VL region and VH region comprise opposite charged mutations to facilitate pairing, and wherein the CH1 region and CL region comprise mutations to facilitate pairing, are provided. Binding proteins c...

The present invention relates to a method for producing a fusion polynucleotide encoding a polypeptide of interest. The method comprises the steps of providing a first polynucleotide and a second polynucleotide, and contacting said first polynucleotide and second polynucleotide with a type IIs restriction endonuclea...

The present disclosure provides methods for treating multiple myeloma (such as refractory multiple myeloma or relapsed and refractory multiple myeloma) in an individual who received at least two prior therapies for multiple myeloma. The methods comprise administering to the individual an anti-CD38 antibody, pomalido...

The disclosure relates to an injection device for setting and injecting pre-set or user-selectable doses of a medicament, the injection device comprising: -an elongated housing (10) defining a longitudinal direction (z) and configured to accommodate a cartridge (20) containing the medicament, -a detector arrangement...

Herein is provided a novel process for the preparation of methyl 6-(2,4-dichlorophenyl)- 5-[4-[(3S)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7H-benzo[7]annulene-2- carboxylate by a Suzuki coupling of compound (3), wherein LG represents a leaving group, with an organoboron reagent: (3). Compound (3) i...

The present invention relates to a sulfonamide of formula (A); a conjugate comprising a sulfonamide of formula (I) and an active pharmaceutical ingredient; a process for preparing a conjugate comprising a sulfonamide of formula (I) and an active pharmaceutical ingredient; a pharmaceutical composition comprising the ...

Provided herein are insulin analogs comprising at least one mutation relative to the parent insulin, wherein the insulin analogs comprise a mutation at position B16 which is substituted with a hydrophobic amino acid and/or a mutation at position B25 which is substituted with a hydrophobic amino acid. ...

The present invention relates to a conjugate comprising a sulfonamide of formula (I) and an active pharmaceutical ingredient such as an insulin analog comprising at least one mutation relative to the parent insulin, wherein the insulin analog comprises a mutation at position B16 which is substituted with a hydrophob...

Herein are provided novel salts of methyl 6-(2,4-dichlorophenyl)-5-[4-[(3S)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7H-benzo[7]annulene-2-carboxylate namely the oxalate salt (I) and the dibenzoyltartrate salt (II).

The present disclosure provides methods of treating high CEACAM5 expressing cancers including lung cancers such NSQ NSCLC using immunoconjugates comprising an antibody that specifically binds human CEACAM5.

The present disclosure relates to compounds of formula (I): RCG1-L-P (I) wherein RCG1 represents a reactive chemical group being reactive towards a chemical group present on a polypeptide such as an antibody; P represents H OH or an activated O; and L represents a specific linker. The disclosure also relates to cryp...

AS ATTACHED

AS ATTACHED

Provided herein are methods for monitoring production of a multispecific binding protein and one or more mispaired species by a cell line, as well as methods of production and screening related thereto. In some embodiments, the methods comprise detecting an amount (e.g., a relative amount) of a multispecific binding...

The present disclosure relates to a compound of formula (1) as an anhydrate which is in a crystalline Form 2, characterized by having a powder-X-ray diffractogram displaying peaks expressed as degree 2-Theta angles at about 9.5; 11.8; 14.1; 14.6; 17.7 and 18.5 and a solid form thereof. The present disclosure also re...

The present disclosure relates to an electronic module (320; 420; 520; 620) configured for attachment to a proximal end (P) of a drug delivery device (100) in a predefined fastening configuration, the drug delivery device (100) comprising an elongated housing extending in a longitudinal direction and comprising a di...

A method of forming a conjugate of a sulfonamide and a polypeptide, the method comprising: a) Providing an activated sulfonamide, wherein the activated sulfonamide corresponds to Formula (I); b) Providing an aqueous solution of a polypeptide having a free amino group, wherein the aqueous solution optionally comprise...

The invention relates to a cartridge assembly (300) for a drug delivery device, comprising: - a cartridge (301) containing a drug (307), - a cartridge holder (302), the cartridge holder defining an interior cartridge holding section (303), where the cartridge is arranged within the cartridge holding section, wherein...

The present invention refers to an injection device (1) comprising a housing (2) containing a dose setting mechanism, a cartridge holder (3) containing a cartridge with a medicament, and a heat shrinkable label (8) which comprises information (9) and/or symbols about the medicament. The injection device (1) is a dis...

The present invention relates to a pharmaceutical combination, comprising (a) a pharmaceutical formulation comprising (i) lixisenatide or/and a pharmaceutically acceptable salt thereof, and (II) insulin glargine or/and a pharmaceutically acceptable salt thereof, and (b) an SGLT2 inhibitor, or/and a pharmaceutically ...

The present invention relates to compounds that are IL-17A modulators. The compounds have the structural Formula I defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of diseases or d...

The present invention relates to compounds that are IL-17A modulators. The compounds have the structural Formula I defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of diseases or d...

The invention relates to pyrazole derivatives of the general formula (I), where X is chlorine or fluorine. The invention also relates to a method for preparing same and to the therapeutic use thereof.

The invention relates to the novel materials of formula (I), where: R1 is an optionally substituted L-aryl or □L- heteroaryl, such that L is a single bond, alkyl, CO, or CO-alk, or L□X, with L□being an alkyl and X being O or S; R2 is H or alkyl; R3 is an alkyl optionally substituted by Hal; and R4 is Hou Hal, wher...

The present invention relates to a dispensing speed control mechanism for use in an injection device. The injection device may have a housing (10, 30, 40; 40"; 40""; 40""") and a drive member (70), which is driven by a power reservoir (100, 100")and axially movable between a dose setting position, in which the drive...

The subject of the present invention is a whole-cell catalysis process for converting substrates of cytochrome P450 monooxygenases of eukaryotic origin into valuable biotechnological products. The subject of the present invention is also microorganisms genetically engineered to achieve those biotransformations with ...

A display assembly is proposed, comprising: a body (4) defining a window (17) having an axial extension, an indication member (2) for providing information to be displayed in the window (17), wherein the indication member(2)is movable relative to the body (4) for changing the information displayed in the window (17)...

The present invention concerns antibody like binding protein specifically binding to CD3 and binding specifically to at least one further antigen for example CD123. The present invention also concerns antibody like binding protein specifically binding to CD123 and binding specifically to at least one further antigen...

The invention relates to benzylhydroxyde derivatives of formula (I): The invention also relates to the preparation and the therapeutic use of the compounds of formula (I).

The present application relates to compositions and methods for treating allergy, e.g., peanut allergy, in patients. The methods involve administering glucopyranosyl lipid adjuvant (GLA) and peanut allergen(s) to the patient via a sublingual route.

The disclosure provides trispecific and/or trivalent binding proteins comprising four polypeptide chains that form three antigen binding sites that specifically bind one or more target proteins wherein a first pair of polypeptides forming the binding protein possess dual variable domains having a cross-over orientat...

The invention describes novel conjugates of formula (I) of a pharmaceutical agent and a moiety capable of binding to a glucose sensing protein allowing a reversible release of the pharmaceutical agent depending on the glucose concentration.

The invention provides an improved pan-TGF-ß antibody for treatment of conditions that are mediated by TGF-ß including autoimmune diseases fibrotic conditions and cancers. Also provided are methods and uses of the antibody in conjunction with other immunomodulatory agents such as an anti-PD-1 antibody. ...

The present invention relates to trigonal GLP-1 / glucagon / GIP receptor agonists and their medical use, for example in the treatment of disorders of the metabolic syndrome, including diabetes and obesity, as well as for reduction of excess food intake.

The present invention relates to trigonal GLP-1 / glucagon / GIP receptor agonists and their medical use, for example in the treatment of disorders of the metabolic syndrome, including diabetes and obesity, as well as for reduction of excess food intake.

The present invention relates to a conjugate or a pharmaceutically acceptable salt thereof comprising an GLP-1/Glucagon receptor agonist, a linker and a hyaluronic acid hydrogel bearing - L1 −L2 - L - Y - R20 groups, wherein Y represents an GLP-1/Glucagon receptor agonist moiety; and -L is a linker moiety - by formu...

The present invention relates to combinations pharmaceutical compositions and fusion molecules comprising an FGF21 (fibroblast growth factor 21) compound and a GLP-1R (glucagon-like peptide-1 receptor) agonist with optimized GLP-1R agonist / FGF21 compound activity ratio. It further relates to their use as medicamen...

The disclosure provides binding proteins that bind CD38 polypeptides, e.g., human and cynomolgus monkey CD38 polypeptides. For example, the binding proteins can be monospecific, bispecific, or trispecific binding proteins with at least one antigen binding domain that binds a CD38 polypeptide. The disclosure also pro...

The present disclosure relates to combination cancer therapies targeting CD38 and TGF-ß using antibodies specific for these targets. Also provided are compositions useful in the therapies.

The disclosure provides methods of treating viral infection using trispecific binding proteins comprising four polypeptide chains that form three antigen binding sites that specifically bind a CD38 polypeptide (e.g, human and/or cynomolgus monkey CD38 polypeptides), a CD28 polypeptide, and a CD 3 polypeptide. ...

The present invention concerns a cell line comprising an endogenous dehydroorotate dehydrogenase (DHODH) gene which is partially or fully inactivated, and its use for producing recombinant proteins.