Merck Patent Gmbh

Merck Patent Gesellschaft MIT Beschrankter Haftung

Metabrain Research

Poxel

Merck Patent Gesellschaft MIT Beschraenkter Haftung

Merk Patent Gmbh

Christine G Charon

Micheline R Kergoat

Samer Elbawab

Denis Carniato

Franck F Lepifre

Eric Valeur

Johannes Gleitz

Didier Roche

Norbert Beier

Gérard Moinet

Daniel Cravo

Sophie Hallakou-Bozec

Lars Thore Burgdorf

Gérard Botton

Liliane Doare

Caroline Leriche

Annick Audet

Jean-Denis Durand

Sophie N Raynal

Ulrich Emde

Valerie Autier

Bjoern Hock

Sébastien Bolze

Gersande R Lena

Laurent Faveriel

Christoph Saal

Oliver Poeschke

Dominique Marais

Sophie Hallakou-bozec

Lauren R Faveriel

Stefan Bender

Valérie Autier

Caroline Lerich

Franck Lepifre

Annick M Audet

Sebastien Bolze

Gerard Botton

Micheline Kergoat

The present invention concerns a tryptophan metabolite chosen from kynurenic acid, anthranilic acid, quinolinic acid, picolinic acid, quinaldic acid and the mixtures of same or an enantiomer, diastereoisomer, hydrate, solvate, tautomer, racemic mixture or pharmaceutically acceptable salt of same, for use as a drug intended for increasing and/or maintaining muscle mass and/or strength in a mammal, and in particular intended for treating and/or preventing muscle atrophy in mammals and/or for promoting muscle growth in mammals doing exercise and aiming to increase muscle mass and/or quality and/or strength, for preventing the appearance of symptoms of sarcopenia or for rehabilitation following muscle loss and/or for improving recovery time after an intense physical effort.

Use of tryptophan metabolites for treating muscle atrophy

This invention relates to oxime and alkoxy derivatives of the general formula (I), or an enantiomer, diastereoisomer, hydrate, solvate, tautomer, racemic mixture or pharmaceutically acceptable salt thereof for use as a medicament for the treatment and/or prevention of muscle atrophy in mammals and/or for limiting muscular atrophy in mammals and/or to promote muscle growth in exercising mammals aimed at increasing muscle mass and quality, preventing the occurrence of symptoms of sarcopenia related to age or rehabilitation after a muscle loss, age-related muscle atrophy and/or the consequences of drug therapy and/or immobilization and/or cachexia.

Derivatives used in the treatment of muscle atrophy

The present invention relates to a thiophene derivative of the following general formula I or an enantiomer, diastereoisomer, hydrate, solvate, tautomer, racemic mixture or pharmaceutically acceptable salt thereof or to its use as a drug in particular intended for treating and/or preventing diabetes, its complications and/or associated pathologies, advantageously diabetes of type II and hyperglycemia.

Useful thiophene derivatives in the treatment of diabetes

The present invention relates to imidazopyridine derivatives of the following general formula I: and to their use as a drug, in particular in treating and/or preventing diabetes, its complications and/or associated pathologies.

Imidazopyridine derivatives useful in treating diabetes

The invention relates to compounds that are direct activators of AMPK (AMP-activated protein kinase) and their use in the treatment of disorders regulated by activation of AMPK. For instance, compounds according to the invention are useful for the treatment of diabetes, metabolic syndrome, obesity, inflammation, cancer and cardiovascular diseases. 

Thieno [2,3-B] pyridinedione activators of AMPK and therapeutic uses thereof

Activators of AMPK and therapeutic uses thereof The invention relates to compounds that are direct activators of AMPK (AMP-activated protein kinase) and their use in the treatment of disorders regulated by activation of AMPK. For instance, compounds according to the invention are useful for the treatment of diabetes, metabolic syndrome, obesity, liver disease, hepatic steatosis, non alcoholic fatty liver disease (NAFLD), non alcoholic steato-hepatitis (NASH), liver fibrosis, dyslipidemia, hypertriglyceridemia, hypercholesterolemia, inflammation, cancer, cardiovascular diseases, atherosclerosis, high blood pressure, retinopathies or neuropathies. 

Thienopyridone derivatives useful as activators of AMPK

Arylpyrazinone derivatives of formula (I), as insulin secretion stimulators, the preparation and use of these pyrazinone derivatives for the prophylaxis and/or treatment of diabetes and pathologies associated.

Method of stimulating insulin secretion and/or modulating INS-1 kinase with substituted pyrazinones and/or substituted tetrahydroquinoxalinones

The treatment of diabetes and associated pathologies is achieved by administering the pyrazinone compounds of formula (I) 

Pyrazinone derivatives as insulin secretion stimulators, methods for obtaining them and use thereof for the treatment of diabetes

The present invention relates to methods for the treatment of a pathology associated with hyperglycaemia, particularly diabetes, by administering quinoxalinone compounds of formula (I), wherein R1, R2, R3, R4, R5 and R6 are as defined in the claims. The compounds have activity as insulin secretion stimulators. The invention also relates to the preparation and use of these quinoxalinone compounds for modulating insulin secretion in insulin-1 cells by contacting the cells with the compounds.

Quinoxalinone derivatives as insulin secretion stimulators, methods for obtaining them and use thereof for the treatment of diabetes

Substituted pyrazin-2-ones and substituted 5,6,7,8-tetrahydroquinoxalin-2-ones and methods of use thereof

The present invention relates to pyridopyrazinone derivatives of formula (I), wherein X, Y, Z1 W, A and R1 are as defined in claim, as insulin secretion stimulators. The invention also relates to the preparation and use of these pyridopyrazinone derivatives for the prophylaxis and/or treatment of diabetes and pathologies associated. 

Pyridopyrazinones derivatives insulin secretion stimulators, methods for obtaining them and use thereof for the treatment of diabetes

The present invention relates to pyrazinone derivatives of formula (I), wherein n, R1, R2, R3 and R4 are as defined in claim, as insulin secretion stimulators. The invention also relates to the preparation and use of these pyrazinone derivatives for the prophylaxis and/or treatment of diabetes and pathologies associated.

The present invention relates to compounds of formula (I) wherein R, Rand B, Bare as defined in claim, including pharmaceutical compositions thereof and for their use in the treatment and/or prevention of diseases and disorders modulated by AMP agonists. The invention is also directed to intermediates and to a method of preparation of compounds of formula (I). 

Thienopyridone derivatives as AMP-activated protein kinase (AMPK) activators

The present invention relates to diazepane-acetamide derivatives of formula I as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11&#x3b2;-HSD-1) and the use of such compounds for the treatment and prevention of metabolic syndrome, diabetes, insulin resistance, obesity, lipid disorders, glaucoma, osteoporosis, cognitive disorders, anxiety, depression, immune disorders, hypertension and other diseases and conditions. 

Diazepane acetamide derivatives as selective 11B-HSD1 inhibitors

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Gometz le Chatel, France

Christine G Charon