Aventis Pharmaceuticals Inc.

Sanofi-a Ventis Deutschland Gmbh

Aventis Pharma Deutschland, Gmbh

Sanofi

Selectide Corporation

Pavel Safar

Armin Walser

Siegfried Stengelin

Matthias Gossel

Thomas Klabunde

Martin Smrcina

Stephen J Shimshock

James Spoonamore

Stefanie Flohr

Kenneth J Bordeau

Uwe Heinelt

Gregory H Merriman

Brian K Whiteley

Michal Lebl

Carolina Lanter

James A Ostrem

Peter Strop

Zhaoxia Yang

Volkmar Wehner

Gerhard Zoller

Karl Schoenafinger

Fahad A Al-Obeidi

Joseph T Klein

Alena Stierandova

Elisabeth Defossa

Hans Matter

Manfred Schudok

Otmar Klingler

Henning Steinhagen

Jacques Mauger

Matthias Herrmann

Alena Safarova

Petra Lennig

Bodo Scheiper

Petra Stahl

Peter Wildgoose

Karl Schoenafinager

The disclosure relates to compounds of formula I: wherein the groups R1, R2, R3, R4, R5 and X are as defined in the disclosure, having antithrombotic activity, which in particular inhibits the protease-activated receptor 1 (PAR1). The disclosure further relates to methods for producing the same and to the use thereof as a pharmaceutical product.

Pyridylvinylpyrazoloquinolines as PAR1 inhibitors

The invention relates to substituted hexahydropyrazino[1,2-a]pyrimidine-4,7-dione derivatives substituted with amino acids, and to the physiologically tolerated salts thereof, processes for their preparation and their use as medicaments.

Hexahydro-pyrazino[1,2-A]pyrimidine-4,7-dione derivatives substituted with amino acids

The invention relates to substituted hexahydropyrazino[1,2-a]pyrimidine-4,7-dione derivatives and to the physiologically tolerated salts and physiologically functional derivatives thereof. Compounds of the formula I in which the radicals have the stated meanings, and the physiologically tolerated salts thereof and processes for preparing them are described. The compounds are suitable for example as anorectic agents.

Substituted hexahydropyrazino [1,2-A] pyrimidine-4,7-dione derivatives, process for their preparation and their use as medicaments

Nitrogen-substituted hexahydropyrazino[1,2-a]pyrimidine-4,7-dione derivatives, processes for the preparation and their use as medicaments The invention relates to substituted hexahydropyrazino[1,2-a]pyrimidine-4,7-dione derivatives and to the physiologically tolerated salts and physiologically functional derivatives thereof. Compounds of the formula I in which the radicals have the stated meanings, and the physiologically tolerated salts thereof and processes for preparing them are described. The compounds are suitable for example as anorectic agents.

Nitrogen-substituted hexahydropyrazino[1,2-A]pyrimidine-4,7-dione derivatives, processes for their preparation and their use as medicaments

Sulfonamide and urea compounds having an inhibitory effect on Src kinase including enantiomers, stereoisomers and tautomers thereof, as well as pharmaceutically acceptable salts or solvates of said compound, said compound having the general structure shown in Formula II are disclosed and claimed: 

Substituted sulfonamides and ureas useful for inhibiting kinase activity

Substituted hexahydropyrazino[1,2-a]pyrimidine-4,7-dione derivatives, processes for their preparation and their use as medicaments The invention relates to substituted hexahydropyrazino[1,2-a]pyrimidine-4,7-dione derivatives and to the physiologically tolerated salts and physiologically functional derivatives thereof. Compounds of the formula I in which the radicals have the stated meanings, and the physiologically tolerated salts thereof and processes for preparing them are described. The compounds are suitable for example as anorectic agents.

Substituted hexahydropyrazino [1,2-a] pyrimidine-4,7-dione derivatives, process for their preparation and their use as medicaments

Amide, sulfonamide and urea compounds having an inhibitory effect on Src kinase including enantiomers, stereoisomers and tautomers thereof, as well as pharmaceutically acceptable salts or solvates of said compound, said compound having the general structure shown in Formulae I and II:

Substituted amides, sulfonamides and ureas useful for inhibiting kinase activity

The invention provides compounds which specifically inhibit factor Xa activity having the structure A &mdash;A &mdash;(A ) &mdash;B, where m is 0 or 1. A compound of the invention is characterized, in part, in that it exhibits a specific inhibition of factor Xa activity with a K &lE;100 &mgr;M, preferably &lE;2 nM, and does not substantially inhibit the activity of other proteases involved in the coagulation cascade. The invention further provides methods of specifically inhibiting the activity of factor Xa and of inhibiting blood clotting in vitro and in an individual and methods of detecting factor Xa levels or activity.

Factor Xa inhibitors

Factor VIIa inhibitors

The present invention relates to novel compounds and pharmaceutical composition, their preparation, and their use, having a antithrombotic effect through reversible inhibition of activated blood coagulation factor VIIa &ldquo;FVIIa&rdquo;.

Factor Vlla inhibitors

The invention provides compounds which specifically inhibit factor Xa activity. The compounds consist of the structure X.sub.1 -YIR-X.sub.2, wherein X.sub.1 is H, acyl, alkyl, acylalkyl, arylalkyl or one or more amino acids, and X.sub.2 is a modified C-terminal group, one or more carboxy-protecting groups or one or more amino acids or other substituent, and Y, I and R are tyrosine, isoleucine and arginine, respectively, or peptidomimetic or organic structures that possess the same functional activity as Y, I and R, respectively. In addition, the present invention provides a compound having the structure A1-A2-(A3).sub.m --B, where m is 0 or 1. A compound of the invention can be linear or cyclic and can be about 2 and 43 residues in length. A compound of the invention is characterized, in part, in that it exhibits a specific inhibition of factor Xa activity with a K.sub.i of .ltoreq.100 .mu.M, preferably .ltoreq.2 nM, and does not substantially inhibit the activity of other proteases involved in the coagulation cascade. The invention further provides methods of specifically inhibiting the activity of factor Xa and of inhibiting blood clotting in vitro and in an individual and methods of detecting factor Xa levels or activity.

Growing community of inventors

Tucson, AZ, United States of America

Pavel Safar