Sanofi-a Ventis Deutschland Gmbh

Sanofi-aventis

Sanofi

Hanmi Pharm. Co., Ltd.

Sanfoi-aventis Deutschland Gmbh

Norbert Tennagels

Stefan Petry

Gerhard Zoller

Hubert Heuer

Gunter Muller

Karl-Heinz Baringhaus

Gunter Müller

Guenter Mueller

Ulrich Werner

Mark Sommerfeld

Georg Tschank

Paul Habermann

Gerhard Seipke

Roland Kurrle

Sung Youb Jung

Markus Follmann

Reinhard Kirsch

In Young Choi

Oliver Plettenburg

Stefan Guessregen

Aimo Kannt

Marcus Korn

Günter Müller

Werner Dittrich, I

Harald Thuering

Kathrin Heermeier

Sabine Metzger

Jurgen Eckel

Daniela Baus

The present invention relates to a novel insulin analog, use thereof, and a method for preparing the analog.

Insulin analogs with reduced affinity to insulin receptor and use thereof

The invention describes novel conjugates of formula (I) of a pharmaceutical agent and a moiety capable of binding to a glucose sensing protein allowing a reversible release of the pharmaceutical agent depending on the glucose concentration.

Conjugates of a pharmaceutical agent and a moiety capable of binding to a glucose sensing protein

The invention relates to novel insulin analogs having a basal time-action profile, which are characterized by the following features: a) the B chain end consists of an amidated basic amino acid residue such as lysine or arginine amide; b) the N-terminal amino acid residue of the insulin A chain is a lysine or arginine radical; c) the amino acid position A8 is occupied by a histidine radical; d) the amino acid position A21 is occupied by a glycine radical; and e) one or more substitutions and/or additions of negatively charged amino acid residues are carried out in the positions A5, A15, A18, B-1, B0, B1, B2, B3 and B4.

Insulin derivatives having an extremely delayed time-action profile

The present invention relates to azolopyridin-3-one derivatives of the general formula (I) with the meanings specified in the description, to their pharmaceutically usable salts and to their use as drug substances. 

Azolopyridin-3-one derivatives 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 novel insulin analogs having a basal time-action profile, which are characterized by the addition and/or substitution of negatively and positively charged amino acid residues and by an amidation of the C-terminal carboxy group of the B chain and histidine in position 8 of the insulin A chain. The invention also relates to the production and use thereof.

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 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. 

The invention relates to benzothiazol-2-one derivatives of general formula (I) with the meanings indicated in the description, the pharmaceutically usable salts thereof, and the use thereof as medicinal substances. 

Benzothiazol-2-one derivatives as lipase and phospholipase inhibitors

The invention relates to carbamoylbenzotriazole derivatives of general formula (I), which are defined as cited in the description, to their pharmaceutically applicable salts and to their use as medicaments. 

Carbamoylbenzotriazole derivatives as inhibitors of lipases and phospholipases

The present invention relates to imidazopyridin-2-one derivatives of the formula I with the definitions specified in the description, to their pharmaceutically usable salts and to their use as medicaments. 

Imidazopyridin-2-one derivatives as inhibitors of lipases and phospholipases

The present invention provides compounds which have an inhibitory effect on hormone-sensitive lipase or endothelial lipase. The compounds of the invention are azolopyridin-2-one derivatives of the general formula I wherein the substituents are as defined herein. The compounds of formula I wherein R2 is hydrogen are distinguished by favorable effects on disorders of lipid metabolism. They beneficially influence the HDL to LDL ratio and increase in particular the HDL level and are suitable for the prevention and treatment of dyslipidemias and metabolic syndrome and their diverse sequelae such as atherosclerosis, coronary heart disease, heart failure, obesity and diabetes. The compounds of formula I wherein R1 and R2 together form a ring system are distinguished by favorable effects on metabolic disorders. They beneficially influence lipid and sugar metabolism; in particular they lower the triglyceride level and are suitable for the prevention and treatment of type II diabetes and arteriosclerosis and the diverse sequelae thereof.

Azolopyridin-2-one derivatives as lipase and phospholipase inhibitors

The present invention relates to a method for the identification of an IRS protein kinase inhibitor, comprising the steps of a) bringing into contact PKC-&#x3b6; with at least one IRS peptide comprising at least one PKC-&#x3b6;-Ser-phosphorylation site in the presence of at least one possible inhibitor, and b) measuring the phosphorylation of the PKC-&#x3b6;-Ser-phosphorylation site.

Method for identifying IRS inhibitors or agonists

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.

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Frankfurt am Main, Germany

Norbert Tennagels