Merck Patent Gmbh

Merck Patent Gesellschaft MIT Beschrankter Haftung

Lipha

Merck Patent Gesellschaft

Merck Sante

Yves Bonhomme

Daniel Guerrier

Francis Contard

Valérie Guyard-Dangremont

Gérard Ferrand

Isabelle Berard

Jean-Jacques Zeiller

Jean Jacques Zeiller

Hervè Dumas

Michel Brunet

Hervé Dumas

Geoffrey Nicholson

Eric Raspe

Didier Roche

Philippe Briet

Philippe Durbin

Stéphane Yvon

Nathalie Adje

Gillian Cave

Sarah J Nicholson

Martine Daoust

Michel Duran

Marie-Laure Poulain

Gerard Pouchol

Gèrard Ferrand

The present invention relates to butenoic acid derivatives of the formula I: in which R, R, Rand Rare as defined in the description,and also to processes for the preparation thereof, to pharmaceutical compositions comprising them and to their use for the treatment of dyslipidaemia, atherosclerosis and diabetes.

Butenoic acid derivatives, processes for the preparation thereof, pharmaceutical compositions comprising them, and use for the treatment of dyslipidaemia, atherosclerosis and diabetes

Compounds of the formula (I): in which R, R, Rand Rare as defined in the description, the use thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes, pharmaceutical compositions comprising them, and processes for the preparation of these compounds. 

Hexenoic acid derivatives, processes for the preparation thereof, pharmaceutical compositions comprising them, and therapeutic applications thereof

Butenoic acid derivatives, processes for the preparation thereof, pharmaceutical compositions comprising them and use for the treatment of dyslipidaemia, atherosclerosis and diabetes

The invention relates to compounds of the formula I: and to the pharmaceutically acceptable salts thereof, to processes for the preparation of them and to pharmaceutical compositions comprising them, which are useful especially for the treatment and prevention of dyslipidaemia, atherosclerosis and diabetes.

Substituted arylhexadienoic acids and esters thereof which can be used for the treatment and prevention of diabetes, dyslipidaemia and atherosclerosis, pharmaceutical compositions comprising them and processes for the preparation of them

The present invention relates to the use of receptors of the Rev-erb family to screen substances which are useful in the treatment of lipid metabolism dysfunctions associated with apolipoprotein C-III. The invention relates more particularly to screening methods for selecting substances which are useful for the treatment of these dysfunctions. Lastly, the invention relates to the use of the substances thus identified for the preparation of therapeutic compositions which are useful for the treatment of lipid metabolism dysfunctions associated with apolipoprotein C-III. The subject of the present invention is also the use of screening tests for the characterization, justification and claim of the mechanism of action of substances possessing anti-atherosclerotic properties using the Rev-erb receptors and/or the response elements thereof, as well as their effect on apo C-III.

Use of Rev-erb family of receptors in screening

Compounds of the formula (I): in which R, Rand Rare as defined in the description, the use thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes, pharmaceutical compositions comprising them, and . processes for the preparation of these compounds. Compounds of formula (I) are activators of PPAR&#x3b1; and PPAR&#x3b1; isoforms. 

Butanoic acid derivatives, processes for the preparation thereof, pharmaceutical compositions comprising them, and therapeutic applications thereof

Disclosed are Compounds of formula I  And methods of use thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes.

Carboxylic acids and derivatives for the treatment of and preventing diabetes and dyslipidaemia

Pentenoic acid derivatives, processes for the preparation thereof, pharmaceutical compositions comprising them, and therapeutic applications thereof

The subject of the present invention is the use of the ROR receptors and/or of their response element or alternatively of a functional equivalent thereof for the screening of substances having antiatherosclerotic properties. The invention also relates to the methods of screening substances having antiatherosclerotic properties using the ROR receptors and/or their response elements. The invention also relates to the use of the methods of screening according to the present invention in order to characterize, justify and claim the mechanism of action of substances having antiatherosclerotic properties using the ROR receptors and/or their response elements as well as their effects on apo C-III.

Use of ROR for receptors for screening substances useful for the treatment of atherosclerosis

The present invention relates to a solid oral dosage form comprising a combination of metformin and glibenclamide in which the size of glibenclamide is such that the glibenclamide bioavailability is comparable to the glibenclamide bioavailability obtained with a separate administration of metformin and glibenclamide.

Solid oral dosage form comprising a combination of metformin and glibenclamide

A pharmaceutical composition for the treatment of alcohol and drug dependence, comprising a therapeutically effective amount of a combination of: (i) an opioid antagonist; and (ii) a NMDA receptor complex modulator. A pharmaceutical kit is also provided, comprising these two substances. The opioid antagonist can, for example, be naltrexone and the NMDA receptor complex modulator can be a spermidine site modulator such as acamprosate.

Combination for the treatment of alcohol and drug dependence containing an opioid antagonist and a NMDA receptor complex modulator

A pharmaceutical composition comprising: (i) metformin, optionally in the form one of its pharmaceutically acceptable salts; (ii) a fibrate selected from fenofibrate and bezafibrate; and optionally one or more pharmaceutically acceptable excipients, is suitable for use in the treatment of non-insulin-dependent diabetes.

Pharmaceutical composition comprising a combination of metformin and fibrate, and its use for the preparation of medicines intended to reduce hyperglycaemia

The invention relates to a new dosage form of hydroxocobalamin which serves in the treatment of cyanide poisoning and contains hydroxocobalamin in freeze-dried form. The hydroxocobalamin is freeze-dried in an acidic medium so as to be practically instantly redissolved in a neutral saline solution. The present invention also relates to a process for producing hydroxocobalamin-based pharmaceutical compositions as well as to first aid kits containing these compositions and methods of using such kits for the treatment of cyanide poisoning.

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Charbonnières les Bains, France

Yves Bonhomme