Other

Genentech, Inc.

Sanofi-Aventis

Hoechst Aktiengesellschaft

Aventis Pharma S.a.

Galapagos Sas

Sanofi-A Ventis Deutschland Gmbh

Sanofi

Aventis Pharma Deutschland, Gmbh

Aventis Pharma S.a. Deutschland Gmbh Genentech, Inc.

Jean-Marie Ruxer

Thomas Gadek

Anuschirwan Peyman

Jean-Michel Lefrancois

Robert S McDowell

Denis Carniato

Jochen Knolle

Volkmar Wehner

Patrick Mailliet

Luc Bertin

Joachim Brendel

Klaus Wirth

Gerhard Breipohl

Jean-Francois Gourvest

Hans Ulrich Stilz

Fabienne Pilorge

Karlheinz Scheunemann

Michael Wagner

Sarah Catherine Bodary

Fabienne Thompson

Maria Mendez-Perez

Bertrand Heckmann

Hervé Minoux

Karl-Heinz Scheunemann

Anurschirwan Peyman

Heinrich Englert

Marcel Alasia

David William Will

Stefan Peukert

Frank Halley

Jidong Zhang

Neerja Bhatnagar

Victor Certal

Chantal Carrez

Didier Benard

Theodor Andreas Wollmann

John Bernard Weston

Hélène Goulaouic

Peter Hamley

Jacques Demassey

Stephane Hourcade

Jean Francois Gourvest

Anuschirvan Peyman

Francois Vallee

Gerhard Brejpohl

Thierry Gouyon

Stéphane Hourcade

Maria Mendez-perez

Robert Mcdowell

Jean-François Gourvest

The invention relates to the novel substances in Formula (I): wherein Het is a heterocycle optionally substituted by one or a plurality of radicals R1 or R'1; R is selected from the group comprising Formula (A&#x2032;), (B), (C), (D), or (E), with R1 and/or R&#x2032;1 selected from H, halogen, CF3, nitro, cyano, alkyl, hydroxyl, mercapto, amino, alkylamino, dialkylamino, alkoxy, phenylalcoxy, alkylhio, or carboxy that is free or esterified by an alkyl, carboxamide, CO&#x2014;NH(alkyl), CON(alkyl)2, NH&#x2014;CO-alkyl, sulfonamide, NH&#x2014;S02-alkyl, S(0)2-NHalkyl, or S(02)-N(alkyl)2 radical; all these radicals are optionally substituted; W1, W2, and W3 independently are CH or N; X is 0, S, NR2, C(O), S(O), or S(0)2; Z is optionally substituted H, Hal, -0-R2 or &#x2014;NH&#x2014;R2 with R2 being H, alkyl, cycloalkyl, or heterocycloalkyl; and these substances are all isomeric forms and salts thereof, used as drugs. 

HSP90 inhibitory carbazole derivatives, compositions containing same and use thereof

Pyrroloindoles of formula (I) are provided wherein Het is an aromatic or partially unsaturated, monocyclic or bicyclic heterocycle containing between 1 and 4 heteroatoms N, O or S, optionally substituted by R1 or R'1 which are the same or different; R is X-(A-B)n-CONH2, X-(A-B)n-O&#x2014;CONH2, X-(A-B)n-NH&#x2014;CONH2, X&#x2014;(CH2)m-heterocycloalkyl, X(CH2)m-aryl and X&#x2014;(CH2)m-heteroaryl wherein X is &#x2014;O&#x2014;C(O), &#x2014;NH&#x2014;C(O), NH&#x2014;CS, &#x2014;NH&#x2014;CO&#x2014;CH2-O&#x2014;; &#x2014;NH&#x2014;COCH2-S&#x2014;CH2-CO&#x2014;NH&#x2014;; &#x2014;NH&#x2014;CO&#x2014;(CH2)2-SO2-; and &#x2014;NH&#x2014;CO&#x2014;CH2-N(CH3)-CO&#x2014;; A and B are the same or different and are each independently a single bond, CH2, CH-alkyl, and CH-aralkyl; n=1, 2 and m=0, 1; R1 and/or R&#x2032;1 are H, halogen, CF3, nitro, cyano, alkyle, hydroxy, mercapto, amino, alkylamino, dialkylamino, alkoxy, alkylthio, and carboxy, free or esterified by an alkyl, carboxamide, CONH(alkyl), CON(alkyl)2, NH&#x2014;CO-alkyl, sulfonamide, NH&#x2014;SO2-alkyl, S(O)2-NHalkyl, and S(O2)-N(alkyl)2 group, all of said alkyl, alcoxy and alkylthio groups being optionally substituted themselves, said products being in all isomer forms and salts, as medicaments.

Derivatives of pyrroloindole which are inhibitors of Hsp90, compositions containing same, and use thereof

The present invention relates to compounds of formula (I): wherein R1, R, R', L, Het, p and p&#x2032; are as defined herein, compositions containing them, and their use as medicinal products.

Fluorene derivatives, compositions containing the same and use thereof as inhibitors of the protein chaperone HSP 90

The invention relates to compounds of formula I in which R1, R2, R3, R4, R5, R6 and X have the meanings stated in the claims. The compounds are particularly suitable as antiarrhythmic active ingredients, in particular for the treatment and prophylaxis of atrial arrhythmias, for example atrial fibrillation (AF) or atrial flutter.

Substituted heterocycles, their use as medicament, and pharmaceutical preparations comprising them

The invention relates to compounds of formula I in which A, R1, R2, R3, R4, R5, R6, R7 and n have the meanings stated in the claims. The compounds are particularly suitable as antiarrhythmic active ingredients, in particular for the treatment and prophylaxis of atrial arrhythmias, for example atrial fibrillation (AF) or atrial flutter.

A subject of the invention is the compounds of formula (I): 

Vitronectin receptor antagonist derivatives, method for preparing same, use thereof as medicines and pharmaceutical compositions containing same

This invention relates to derivatives of 4-(benzimidazol-2-yl)fluorene and 4-(azabenzimidazol-2-yl)fluorene, to pharmaceutical compositions comprising such derivatives, and to methods of treatment of disorders related to Hsp90 protein activity, comprising administering such derivatives.

Fluorene derivatives, composition containing said derivatives and the use thereof

The invention relates particularly to 2-alkoxy-3,4,5-trihydroxy-alkylamides, preparation thereof, compositions containing them and use thereof as a medicament, particularly as anti-cancer agents.

2-alkoxy-3,4,5-trihydroxy-alkylamides, preparation thereof, compositions containing them and use thereof

The present invention relates to acylguanidino derivatives of formula (I), in which R, R, R, A, B, X, Y and n have the meanings indicated in claim, their physiologically tolerable salts and their prodrugs. The compounds of the formula (I) are valuable pharmaceutically active compounds. They are vitronectin receptor antagonists and inhibitors of cell adhesion and bone resorption by osteoclasts. This renders them suitable, for example, for the therapy and prophylaxis of illness which are based on the interaction between vitronectin receptors and their ligands in cell-cell or cell-matrix interaction processes or which can be prevented, alleviated or cured by influencing such interactions. For example, they can be applied for treating and preventing osteoporosis, or for inhibiting undesired angiogenesis or proliferation of cells of the vascular smooth muscles. The invention furthermore relates to processes for the preparation of compounds of the formula (I), their use, in particular as pharmaceutical active ingredients, and pharmaceutical compositions comprising them 

Guanidino derivatives as inhibitors of cell adhesion

(2S)-2-(Adamantan-1-ylmethoxycarbonylamino)-3-(4-(2-(1,4,5,6-tetrahydropyrimidin-2-ylcarbamoyl)ethyl)benzoylamino)propionic acid isopropyl ester, its preparation and its use The present invention relates to (2S)-2-(adamantan-1-ylmethoxycarbonylamino)-3-(4-(2-(1,4,5,6-tetrahydropyrimidin-2-ylcarbamoyl)ethyl)benzoylamino)propionic acid isopropyl ester of the formula Iand its physiologically tolerable salts, their preparation, their use as pharmaceuticals and to pharmaceutical compositions comprising them. The compound of the formula I and its physiologically tolerable salts are valuable pharmacologically active compounds which can be used, for example, in the treatment or prophylaxis of diseases which can be influenced by inhibiting the vitronectin receptor, for example of bone diseases such as osteoporosis.

(2S)-2-(adamantan-1-ylmethoxycarbonylamino)-3-(4-(2-(1,4,5,6-tetrhydropyrimidin-2-ylcarbamoyl)ethyl)benzoylamino)propionic acid isopropyl ester, its preparation and its use

The present invention relates to compounds of the formula IA&#x2014;B&#x2014;D&#x2014;E&#x2014;F&#x2014;G&#x2003;&#x2003;(I)in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.

Vitronectin receptor antagonists, their preparation and their use

The invention concerns vitronectin receptor antagonist compounds of formula (3): R&#x2014;Y&#x2014;A&#x2014;B&#x2014;D&#x2014;E&#x2014;F&#x2014;G wherein R, Y, A, B, D, E, F, and G are as defined in the description, their physiologically acceptable salts and their prodrugs, methods for preparing compounds of formula (I), their use, in particular as medicine and pharmaceutical compositions containing them.

Antagonist derivatives of the vitronectin receptor

The present invention relates to compounds of formula (I), in which A, B, X, Y, R , R , R and n have the meanings indicated in the claims. The compounds of formula (I) are valuable pharmacologically active compounds. They are vitronectin receptor antagonists and inhibitors of cell adhesion and are suitable for the therapy and prophylaxis of illnesses which are based on the interaction between vitronectin receptors and their ligands in cell-cell or cell-matrix interaction processes or which can be prevented, alleviated or cured by influencing such interactions. For example, they can be applied for inhibiting bone resorption by osteoclasts and thus for treating and preventing osteoporosis, or for inhibiting undesired angiogenesis or proliferation of cells of the vascular smooth musculature. The invention furthermore relates to processes for the preparation of compounds of formula (I), their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.

Thienylalanine derivatives as inhibitors of cell adhesion

The present invention relates to compounds of formula (I), in which B, D, E, G, X, Y, Z, R , R and s have the meanings indicated in the claims, their physiologically tolerable salts and their prodrugs. The compounds of formula (I) are valuable pharmacologically active compounds. They are vitronectin receptor antagonist and inhibitors of cell adhesion and are suitable for the therapy and prophylaxis of illnesses which are based on the interaction between vitronectin receptors and their ligands in cell-cell or cell-matrix interaction processes or which can be prevented, alleviated or cured by influencing such interactions. For example, they can be applied for inhibiting bone resorption by osteoclasts and thus for treating and preventing osteoporosis, or for inhibiting undesired angiogenesis or prolifertion of cells of the vascular smooth musculature. The invention furthermore relates to processes for the preparation of compounds of formula (I), their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.

Substituted purine derivatives as inhibitors of cell adhesion

Growing community of inventors

Issy les Moulineaux, France

Jean-Marie Ruxer