Sanofi-aventis

Cassella Aktiengesellschaft

Sanofi

Aventis Pharma Deutschland, Gmbh

Hoechst Aktiengesellschaft

Sanofi-a Ventis Deutschland Gmbh

Degussa Aktiengesellschaft

Hoechst Marion Roussel

Cassella Aktiengessellschaft

Gerhard Zoller

Otmar Klingler

Stefan Petry

David William Will

Melitta Just

Hubert Heuer

Norbert Tennagels

Bernd Jablonka

Jochen Knolle

Hans Matter

Paulus Wohlfart

Wolfgang Konig

Hartmut Strobel

Gerhard Breipohl

Elisabeth Defossa

Rudi Beyerle

Gunter Muller

Fahad A Al-Obeidi

Gunter Müller

Ursula Schindler

Armin Walser

Uwe Heinelt

Karl-Heinz Baringhaus

Piero A Martorana

Rolf-Eberhard Nitz

Anuschirwan Peyman

Uwe Gerlach

Manfred Schudok

Eckart Bartnik

Franz Effenberger

Christophe Philippo

Peter Wildgoose

Heinz-Werner Kleemann

Wilfried Schwab

Andreas W Herling

Hans Ulrich Stilz

Helmut Bohn

Klaus-ulrich Weithmann

James A Ostrem

Hans-Ulrich Stilz

Günter Müller

Marc Nazaré

Harmut Strobel

Frank B&uuml;ttner

Marc Dietrich Voss

Volkmar Wehner

Markus Follmann

Stefanie Keil

Marc Nazare

Pavel Safar

Guido Haschke

Ingo Focken

Claudie Namane

Manfred Schrod

Klaus Delpy

Dieter Schmoll

Hans-Peter Nestler

Manfred Seidel

Eckard Kujath

Marco Mueller

Wolfgang K Onig

Marco MÜLLER

Juan-Antonio Sanchez-Arias

The present invention relates to 5-oxoisoxazole derivatives of the formula I, the pharmaceutically usable salts thereof and the use thereof as medicinal substances. 

5-oxoisoxazoles as inhibitors of lipases and phospholipases

The invention relates to azole derivatives of the general formula I as defined in the present application as well as to their uses in treatment of conditions that would benefit from their inhibitory effect on hormone sensitive lipase, HSL, an allosteric enzyme in adipocytes which is inhibited by insulin and is responsible for the breakdown of fats in fat cells and thus for transferring fat constituents into the blood stream. Inhibition of this enzyme is therefore equivalent to an insulin-like effect of the compounds of the invention.

Azole derivatives in the form of lipase and phospholipase inhibitors

The present invention relates to imidazolidinecarboxamide derivatives of the general formula I, wherein R, R1, R2, X and Y are as defined herein, or pharmaceutically usable salts thereof and the use thereof as medicinal substances.

Imidazolidine carboxamide derivatives as lipase and phospholipase inhibitors

The invention relates to compounds of the formula (I), where the groups R1, M, A, B, D, L, and R have the specified meanings, and to the physiologically compatible salts thereof. The compounds are suitable, for example, for treating metabolic syndrome, insulin resistance, obesity, and diabetes. 

2-heteroaryl-pyrrolo [3,4-C]pyrrole derivatives, and use thereof as SCD inhibitors

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

Heterocyclic derivatives, processes for their preparation, medicaments comprising these compounds, and the use thereof. The invention relates to compounds of the formula I in which the radicals R1, R2, R3, R4, W, A, B, D, E, G, L, M, R, T and Y have the stated meanings, and to the physiologically tolerated salts thereof. The compounds are suitable for example for the treatment of the metabolic syndrome, insulin resistance, obesity and diabetes. 

Heterocyclic compounds, processes for their preparation, medicaments comprising these compounds, and the use thereof

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 invention relates to diacyl indazole derivatives of general formulae (I) or (II) and to the pharmaceutically acceptable salts thereof: Wherein X, R1 and R2 are as defined herein. The invention also relates to the use of these compounds to treat diabetes mellitus, dyslipidemia and atherosclerotic disorders.

Diacyl indazole derivatives as lipase and phospholipase inhibitors

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 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 azolopyridin-3-one derivatives of the general formula I with the meanings indicated in the description, their pharmaceutically usable salts and their use as medicinal substances. 

Azolopyridin-3-one derivatives as inhibitors of lipases and phospholipases

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

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Schöneck, Germany

Gerhard Zoller