Sanofi-a Ventis Deutschland Gmbh

Other

Sanofi

Aventis Pharma Deutschland, Gmbh

Sanofi-aventis

Aventis Pharma S.a.

Hoechst Aktiengesellschaft

Genentech, Inc.

David William Will

Hans Matter

Gerhard Zoller

Paulus Wohlfart

Eugen Uhlmann

Anuschirwan Peyman

Hartmut Strobel

Gerhard Breipohl

Thomas Gadek

Jochen Knolle

Karl Schoenafinger

Swen Hoelder

Robert S McDowell

Volkmar Wehner

Denis Carniato

Jean-Francois Gourvest

Sarah Catherine Bodary

Marc Nazare

Anke Steinmetz

Ingrid Sassoon

Martin Bossart

Robert Andrew Cuthbertson

Christine Delaisi

Uwe Gerlach

Gunter Muller

Karl-Heinz Scheunemann

Cecile Combeau

Marc Nazaré

Heinz-Werner Kleemann

Kurt Ritter

Guenter Mueller

Karl Schönafinger

Thomas Rooney

Franck Halley

Bernard Baudoin

Gilles Tiraboschi

Karlheinz Scheunemann

Didier Benard

Cécile Combeau

Thorsten Naumann

Dominique Le Suisse

Harmut Strobel

Amuschirwan Peyman

Swen Hölder

Günther Müller

Gerhard Jaehne

Wendelin Frick

Michael Wagner

Matthias Urmann

Herman Schreuder

Jean-Marie Ruxer

Andreas Lindenschmidt

Esther H Chang

Fahad A Al-Obeidi

Kathleen F Pirollo

Guenter Billen

Heiner Jendralla

Armin Bauer

Bernd Junker

Hans-Peter Nestler

Theodor Andreas Wollmann

Günter Müller

David Rigal

Antonina Rait

Melanie Essrich

Jean Francois Gourvest

Hans Mattter

Wolkmar Wehner

The present invention relates to N-alkylamides of the formula I, in which A, Het, X, R, Rand Rhave the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of the formula I, to pharmaceutical compositions comprising them, and to the use of compounds of the formula I for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.

Heteroaryl-substituted amides comprising an unsaturated or cyclic linker group, and their use as pharmaceuticals

Heteroaryl-substituted amides comprising a saturated linker group, and their use as pharmaceuticals

The present invention relates to derivatives of imidazo[1,2-a]pyridines of formula I, in which R, R1 to R4 and n have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of formula I, to pharmaceutical compositions comprising them, and to the use of compounds of formula I for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.

Imidazo[1,2-a]pyridines and their use as pharmaceuticals

The present invention relates to heteroarylacrylamides of the formula I, in which Het, X, R, R, R, Rand Rhave the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of the formula I, to pharmaceutical compositions comprising them, and to the use of compounds of the formula I for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.

Heteroarylacrylamides and their use as pharmaceuticals

The present invention relates to heteroarylcyclopropanecarboxamides of the formula I, in which Het, X, R, R, R, R, R, Rand Rhave the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of the formula I, to pharmaceutical compositions comprising them, and to the use of compounds of the formula I for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.

Heteroarylcyclopropanecarboxamides and their use as pharmaceuticals

The present invention relates to PNA derivatives which carry, at the C terminus, or at both the C and N termini of the PNA backbone, one or more phosphoryl radicals. The phosphoryl radicals carry, where appropriate, one or more labeling groups, groups for crosslinking, groups which promote intracellular uptake, or groups which increase the binding affinity of the PNA derivative for nucleic acids. The invention furthermore relates to a process for preparing the above-mentioned PNA derivatives and to their use as pharmaceuticals or diagnostic agents.

Polymide nucleic acid derivatives, and agents and processes for preparing them

The present invention relates to heteroaryl-substituted carboxamides of the formula I, in which Het, A, X, R, Rand Rhave the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of the formula I, to pharmaceutical compositions comprising them, and to the use of compounds of the formula I for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.

Heteroaryl-substituted carboxamides and their use as pharmaceuticals

The present invention relates to derivatives of 2-phenyl-benzimidazoles of the formula I, in which X, R, R1 to R3 and n have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of the formula I, to pharmaceutical compositions comprising them, and to the use of compounds of the formula I for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.

Substituted 2-phenyl-benzimidazoles and their use as pharmaceuticals

The present invention relates to derivatives of imidazo[2,1-b]thiazoles of formula I, in which R, R1 to R3 and n have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of formula I, to pharmaceutical compositions comprising them, and to the use of compounds of formula I for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.

Imidazo[2,1-b]thiazoles and their use as pharmaceuticals

The present invention relates to derivatives of imidazo[1,2-a]azines of formula I, in which R, R1 to R3, X, Y and n have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of formula I, to pharmaceutical compositions comprising them, and to the use of compounds of formula I for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.

Imidazo[1,2-a]azines and their use as pharmaceuticals

Disclosed are compounds of Formula I wherein X is and R, R, A, B, D, E, Rare as defined herein useful for treating cancers.

Pyridazinone kinase inhibitors

The present invention is directed to a compound of formula I, in which R; R; R; R; R; Q; V, G and M have the meanings indicated below. The compound of formula I is a pharmacologically active compound. It exhibits a strong anti-thrombotic effect and is suitable, for example, for the therapy and prophylaxis of a cardio-vascular disorder like a thromboembolic disease or restenosis. It is a reversible inhibitor of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore is directed to a process for the preparation of the compound of formula I, and pharmaceutical preparation comprising it.

Pyrazole-derivatives as factor Xa inhibitors

Polyamide nucleic acid derivatives and agents, and processes for preparing them

Disclosed are compounds of the general formula (I), where the definition of the substituents A, B, D, E, Rand Rare detailed in the description, and the physiologically tolerated salts thereof, a process for the preparation of these compounds and their use as pharmaceuticals.  These compounds are kinase inhibitors, in particular inhibitors of the kinase CDK2 (cyclin-dependent kinase 2).

4-benzimidazol-2-ylpyridazin-3-one derivatives

The present invention relates to kinase inhibitor compounds and derivatives thereof as well as compositions comprising them consisting of the structure of formula I: Wherein R1, R2, A, B, D and E are defined herein. These 4-benzimidazol-2-ylpyridazin-3-ones and their derivatives and compositions comprising them are useful in the treatment of neurological disorders such as Alzheimers' disease, Parkinsons' disease, obesity, hypertension and the like. These pyridazinone derivatives particularly inhibit the metabolic activity of glycogen synthase kinase-3 &#x3b2; (GSK-3&#x3b2;) which is believed to cause the neurodegeneration that results in these diseases.

4-benzimidazol-2-yl-pyridazine-3-one-derivatives, production and use thereof in medicaments

Growing community of inventors

Kriftel, Germany

David William Will