Sanofi-a Ventis Deutschland Gmbh

Sanofi-aventis

Sanofi

Asta Medica, Aktiengesellschaft

Hoechst Marion Roussel Deutschland Gmbh

Ulrich Werner

Georg Tschank

Gerhard Jaehne

Karl Schoenafinger

Christian Buning

Elisabeth Defossa

Holger Wagner

Norbert Tennagels

Jurgen Engel

Bernhard Kutscher

Christopher James Smith

Paul Habermann

Lothar Schwink

Gunter Muller

Stefan Szelenyi

Gerhard Seipke

Ilona Fleischhauer

Mark Sommerfeld

Holger Gaul

Roland Kurrle

Barbel Rotthauser

Stefan Petry

Oliver Plettenburg

Karl-Heinz Baringhaus

Klaus Weidmann

Gerhard Scheffler

Stefan Guessregen

Peter Boderke

Guenter Billen

Thomas Boehme

Laurent Bialy

Werner Mueller

Nils Rackelmann

Petra Loos

Günter Müller

Marcus Korn

Michael Podeschwa

Isabell Schoettle

Peter Metzenauer

Annke Hahn

Reinhard Becker

Katrin Tertsch

Jens Riedel

Melissa Besenius

Ana Villar Garea

Martin Will

Maria Mendez Perez

Christiane Fuerst

Christian Bunning

Elizabeth Defossa

Bärbel ROTTHÄUSER

Annke Frick

Marcus Hermann Korn

The present invention relates to a conjugate comprising a sulfonamide of formula (I) and an active pharmaceutical ingredient such as an insulin analog comprising at least one mutation relative to the parent insulin, wherein the insulin analog comprises a mutation at position B16 which is substituted with a hydrophobic amino acid and/or a mutation at position B25 which is substituted with a hydrophobic amino acid. The present invention further relates to a sulfonamide of formula (A). Moreover, the present invention relates to an insulin analog comprising at least one mutation relative to the parent insulin.

Insulin conjugates

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 a drug comprising at least one insulin and at least one GLP-1 receptor agonist.

Combination of an insulin and a GLP-1 agonist

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

Combination of an insulin and a GLP-1-agonist

The application relates to an aqueous pharmaceutical formulation comprising 200-1000 U/mL [equimolar to 200-1000 IU human insulin] of insulin glargine.

Long-acting formulations of insulin

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 8-aminothioxanthines and the derivatives of formula I wherein the various R groups and substituents are comprised of a number of different (C-C)-alkyl, cycloalkyl, aryl, alkene, alkyne, etc. groups and derivatives thereof which are hereinafter more specifically defined for the treatment of metabolic disorders such as type-2 diabetes, hyperglycemia, arteriosclerotic diseases and the like.

Substituted 8-aminoalkylthioxanthines, and their use as inhibitors of dipeptidyl peptidase IV

The present invention comprises the use of amino-substituted 8-N-benzimidazoles compounds of formula I wherein R3, R4-R5, R11 and R20-R21 are hereinafter defined which display a therapeutically utilizable blood sugar-lowering action. These compounds are intended to be particularly suitable in the treatment of diabetes.

Amide-substituted 8-N-benzimidazoles, method for the production thereof, and use of the same as medicaments

The present invention comprises the use of amino-carbonyl-substituted 8-N-benzimidazoles compounds of formula I wherein R3, R4-R5, R11 and R20-R21 are hereinafter defined which display a therapeutically utilizable blood sugar-lowering action. These compounds are intended to be particularly suitable in the treatment of diabetes, carbohydrate and lipid metabolic disorders and other blood sugar complications.

Aminocarbonyl-substituted 8-N-benzimidazoles, methods for their preparation and their use in pharmaceutical compositions

Amino-substituted 8-N-benzimidazoles and methods for their use in blood sugar disorders

The present invention involves substituted bicyclic 8-pyrrolidinoxanthines and their derivatives of formula I: wherein the various R groups are defined herein. The present invention also comprises pharmaceutical compositions comprising them as well as processes for the preparation of these compounds and methods for the treatment of metabolic disorders such as type-2 diabetes, insulin resistance, hyperglycemia, arteriosclerosis diseases and the like through the administration of said compositions.

Substituted, bicyclic 8-pyrrolidinoxanthines, and methods for their use as inhibitors of dipeptidyl peptidase

Compounds for the treatment of elevated blood glucose levels and the physiological and metabolic disorders arising therefrom are disclosed which are inhibitors of the enzyme dipeptidyl peptidase IV (DDP-IV) and comprise novel substituted bicyclic 8-pyrrolidinoxanthines of formula I and their derivatives: wherein the various R-groups are defined herein. These compounds may be combined with other secondary active compounds which also are effective in the treatment of said disorders and the disease states or physiological manifestations arising therefrom.

Substituted 8-aminoalkoxy-xanthine compounds and compositions useful in the treatment of hyperlipidemia and diabetes

Compounds for the treatment of elevated blood glucose levels and the physiological and metabolic disorders arising therefrom are disclosed and comprise novel substituted bicyclic 8-pyrrolidinoxanthines and their derivatives of formula I: wherein the various R groups are hereinafter defined. The present invention also comprises pharmaceutical compositions comprising them as well as processes for the preparation of these compounds. Particular blood glucose disorders treatable thereby include type-2 diabetes, insulin resistance, hyperglycemia, arteriosclerotic diseases and the like.

Substituted bicyclic 8-pyrrolidinoxanthines, methods for their production, pharmaceutical formulations and their use

The present invention comprises the substituted 2-aminoalkylthiobenzimidazoles of formula I wherein R1-R5 and R11-R16 are hereinafter defined. These compounds, their derivatives and the pharmaceutically acceptable salts thereof are useful in the reduction of elevated blood sugar levels and are therefore useful in the treatment of hyperglycemia, diabetes, atherosclerosis and other blood sugar disorders. These compounds are particularly suitable in the treatment of type-2 diabetes.

Substituted 2-aminoalkylthiobenzimidazole compounds, pharmaceutical compositions thereof and methods for their use

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Miehlen, Germany

Ulrich Werner