Laboratoires Serono S.a.

Merck Serono S. A.

Obseva S.a.

Laboratories Serono Sa

Kissei Pharmaceutical Co., Ltd.

Applied Research Systems Ars Holding N.v.

Ares Trading S.a.

Xoma (us) LLC

Preglem Sa

Jean-Pierre Gotteland

Thomas Rueckle

Dennis Church

Serge Halazy

Pascale Gaillard

Marco Antonio Biamonte

Montserrat Camps

Stephen Arkinstall

Matthias Schwarz

Ernest Loumaye

Oliver Pohl

Patrick Naxos Page

Anna Quattropani

Vincent Pomel

Catherine Jorand-LeBrun

Pierre-Alain Vitte

Isabelle Jeanclaude-Etter

Russel J Thomas

Russell Thomas

Yolande Chvatchko

Daniela Chicco

Pierandrea Esposito

Mario Maio

Luca Donati

Monstserrat Camps

Simone Grandolini

Stefania Bertero

Andrea Leonardi

Valérie Boujac

Marco Biamonte

Russell J Thomas

Pascale Domaine De La Prasle Gaillard

Valérie Cayron-Elizondo

The invention provides compositions and methods for reducing the volume of menstrual blood loss in a patient, such as a human patient, for instance, that has uterine fibroids, by administration of a gonadotropin-releasing hormone (GnRH) antagonist. Suitable GnRH antagonists useful in conjunction with the compositions and methods described herein include thieno[3,4d]pyrimidine derivatives, such as 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxypheny I]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4d]pyrimidine-5-carboxylic acid and the choline salt thereof.

Gonadotropin-releasing hormone antagonist dosing regimens for treating uterine fibroids and reducing menstrual blood loss

The invention provides compositions and methods for delaying the onset of delivery in a pregnant subject, such as a pregnant human subject, that is undergoing or at risk of undergoing preterm labor at a gestational age of from about 24 weeks to about 34 weeks. Using the compositions and methods described herein, such subjects may be administered nifedipine in combination with a prostaglandin F2&#x3b1; (PGF2&#x3b1;) antagonist. Exemplary PGF2&#x3b1; receptor antagonists that may be used for the treatment or prevention of preterm labor as described herein include 1,3-thiazolidine-2-carboxamide compounds, such as (3S)-3-({[(2S)-3-(biphenyl-4-ylsulfonyl)-1,3-thiazolidin-2-yl]carbonyl}-amino)-3-(4-fluorophenyl)propyl L-valinate or a pharmaceutically acceptable salt thereof (e.g., (3S)-3-({[(2S)-3-(biphenyl-4-ylsulfonyl)-1,3-thiazolidin-2-yl]carbonyl}-amino)-3-(4-fluorophenyl)propyl L-valinate hydrochloride. Using the compositions and methods described herein, a subject may be dosed with a PGF2&#x3b1; receptor antagonist and a reduced amount or frequency of nifedipine relative to the amount or frequency of nifedipine that would otherwise be used if the nifedipine were given in the absence of the PGF2&#x3b1; receptor antagonist.

Compositions and methods for delaying the incidence of labor

The invention provides &#x3b1;-amino esters of a hydroxypropylthiazolidine carboxamide derivative, (2S)-3-([1,1'-biphenyl]-4-ylsulfonyl)-N-[(1S)-3-hydroxy-1-phenylpropyl]-1,3-thiazolidine-2-carboxamide, as well as salts and crystal polymorphs thereof, that can be used to inhibit prostaglandin F receptor. The invention further encompasses methods of treating disorders such as preterm labor at the early gestational stage by the administration of these substances to a patient in need of treatment.

Alpha-amino esters of hydroxypropylthiazolidine carboxamide derivative and salt form, crystal polymorph thereof

The invention provides pharmaceutical compositions comprising a compound of formula (I) or (II) and an additional therapeutic agent Also provided is the HCI salt and crystalline form of the compound of formula (I). The compounds inhibit the prostaglandin F receptor (PGF2alpha) and thus useful in the treatment of disorders such as preterm labor at the early gestational stage.

The present invention relates generally to a combination for use in the treatment of gynaecological diseases and associated disabling symptoms thereof, in a subject in need thereof, said pharmaceutical combination for use comprising co-administering a suitable pharmaceutical composition for oral administration comprising a first progesterone receptor modulator and a pharmaceutical composition suitable for vaginal and/or intrauterine administration comprising a second progesterone receptor modulator.

Method for treating gynecological diseases

Sulfonyl hydrazide compounds according to formula I geometrical isomers thereof, optically active enantiomers thereof, diastereomers thereof, racemates thereof, and/or pharmaceutically acceptable salts thereof are useful in method for treating a neuronal disorder, an autoimmune disease, a cardiovascular disease, or cancer in a patient in need of such treatment.

Pharmaceutically active sulfonyl hydrazide derivatives

The present invention relates to benzsulfonamide derivatives of formula I and methods of use thereof. The benzsulfonamide derivatives of the present invention are efficient modulators of the JNK pathway. In particular the benzsulfonamide derivatives of the present invention are selective inhibitors of JNK 2 and 3. 

Pharmaceutically active benzsulfonamide derivatives as inhibitors of protein junkinases

The present invention is related to pyridinyl acetonitriles as well as to pharmaceutical formulations containing such pyridinyl acetonitriles. Said pyridinyl acetonitriles are modulators of the protein kinase signalling pathways, particularly the one involving Glycogen Kinase Synthase 3 or JNK. The present invention is furthermore related to methods of preparing pyridinyl acetonitriles. X is a substituted or unsubstituted pyridinyl. G is an unsubstituted or substituted pyrimidinyl or triazinyl.

Pyridinyl acetonitriles

The present invention is related to macrogol glyceride pharmaceutical formulations containing benzothiazole derivatives. In particular, the invention is related to benzothiazole stearoyl macrogol pharmaceutical formulations, method of preparation and use thereof.

Benzothiazole formulations and use thereof

The present invention is related to the use of benzazole derivatives of formula (I) for the treatment and/or prevention of scleroderma and its therapeutic implications selected in the group consisting of systemic sclerosis, scleroderma-like disorders, sine scleroderma, liver cirrhosis, interstitial pulmonary fibrosis, Dupuytren's contracture, keloid and other scarring/wound healing abnormalities, postoperative adhesions and reactive fibrosis, as well as chronic heart failure, in particular after myocardial infarction. 

Benzazole derivatives for the treatment of scleroderma

The present invention is related to the use of sulfonamide derivatives in the treatment of metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type II, inadequate glucose tolerance, insulin resistance, obesity, polycystic ovary syndrome (PCOS). Formula (I). Ris selected from the group comprising or consisting of hydrogen, C-C-alkoxy, C-C-alkyl, C-C-alkenyl, C-C-alkynyl, amino, sulfanyl, sulfinyl, sulfonyl, sulfonyloxy, sulfonamide, acylamino, aminocarbonyl, C-Calkoxycarbonyl, aryl, heteroaryl, carboxy, cyano, halogen, hydroxy, nitro, hydrazides. Ris selected from the group comprising or consisting of hydrogen, COOR3, &#x2014;CONRR, OH, a C-Calkyl substituted with an OH or amino group, a hydrazido carbonyl group, a sulfate, a sulfonate, an amine or an ammonium salt. Y is an 4-12-membered saturated cyclic or bicyclic alkyl containing at least one nitrogen atom, whereby one nitrogen atom within said ring is forming a bond with the sulfonyl group of formula I thus providing the sulfonamide. 

Sulfonamide derivatives for the treatment of diabetes

The present invention relates to sulfonamide derivatives of formula (I) notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such sulfonamide derivatives. Said sulfonamide derivatives are useful in the treatment of neuronal disorders, autoimmune diseases, cancer and cardiovascular diseases. Furthermore, said sulfonamide derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK2 and -3. The present invention is furthermore related to novel sulfonamide derivatives as well as to methods of their preparation. Formula (I) IAris a substituted or unsubstituted aryl or heteroaryl group; X is O or S, preferably O; Ara substituted or unsubstituted arylene or heteroarylene group; Rand Rare independently selected from the group consisting of hydrogen and a C-C-alkyl group. 

Arylsulfonamide derivatives as C-Jun-N-Terminal Kinases (JNK's) inhibitors

The present invention is related to sulfonyl amino acid derivatives of formula (I), notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such sulfonyl amino acid derivatives. Said sulfonyl amino acid are efficient modulators of the JNK pathway, they are in particular efficient inhibitors of JNK 2 and 33. The present invention is furthermore related to novel sulfonyl amino acid derivatives as well as to methods of their preparation. 

Pharmaceutically active sulfonyl amino acid derivatives

The present invention is related to sulfonamide derivatives having a lipophilic moiety and which are substantially soluble. Said compounds are notably for use as pharmaceutically active compounds. The present invention also related to pharmaceutical formulations containing such sulfonamide derivatives. Said sulfonamide derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK 2 and 3. The present invention is furthermore related to novel sulfonamide derivatives as well as to methods of their preparation. The compounds of formula (I) according to the present invention being suitable pharmaceutical agents are those wherein Ar1 and Ar2 are independently from each other substituted or unsubstituted aryl or heteroaryl groups, X is O or S, preferably O; R1 is hydrogen or a C1-C6-alkyl group, or R1 forms a substituted or unsubstituted 5-6-membered saturated or unsaturated ring with Ar1; n is an integer from 0 to 5, preferably between 1-3 and most preferred 1; Y within formula (I) is an unsubstituted or a substituted 4-12-membered saturated cyclic or bicyclic alkyl which is substituted with at least one ionizable moiety to which a lipophilic chain is attached and which is containing at least one nitrogen atom, whereby one nitrogen atom within said ring is forming a bond with the sulfonyl group of formula (I) thus providing a sulfonamide.

Pharmaceutically active sulfonamide derivatives bearing both lipophilic and ionisable moieties as inhibitors of protein JunKinases

The present invention is related to benzazole derivatives notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such benzazole derivatives. Said benzazole derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK2 and/or 3. The present invention is furthermore related to novel benzazole derivatives as well as to methods of their preparation. X is O, S or NR, with Rbeing H or an unsubstantiated or substituted C-Calkyl;G is an unsubstantiated or substituted pyrimidinyl group.

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Beaumont, France

Jean-Pierre Gotteland