Merck Patent Gmbh

Merck Patent Gesellschaft MIT Beschrankter Haftung

Fovea Pharmaceuticals

Sanofi

Merck Patent Gesellschaft MIT Beschraenkter Haftung

Merk Patent Gmbh

Caroline Leriche

Denis Carniato

Christine G Charon

Didier Roche

Liliane Doare

David Middlemiss

Gérard Moinet

Micheline R Kergoat

John Thomas Feutrill

Johannes Gleitz

Annick Audet

Annick Arbellot De Vacqueur

Eric Auclair

Jacques Le Roux

John Feutrill

The present invention relates to therapeutic applications of aniline derivatives of formula (I), for example in treating glaucoma: Formula (I), R1a represents H, an halogen, a (C-C)alkyl or a CN; R1b represents H, an halogen or a (C-C)alkyl; R1c represents H or a (C-C)alkyl; R2 represents H, an halogen, an OH, an O&#x2014;(C-C)alkyl or (C-C)alkyl; R3 represents H, an halogen, a (C-C)alkyl, an OH, an O&#x2014;(C-C)alkyl, a CONHor CN; R4 represents H, an halogen or a (C-C)alkyl; R5 represents H or F: R7 represents H or F; R8 represents H or F; R9 represents H or (C-C)alkyl, or one of its enantiomers. 

Aniline derivatives, their preparation and their therapeutic application

The present invention relates to aniline derivatives of formula (I), to their preparation and to their therapeutic application, for example in treating glaucoma: Formula (I), R1a represents H, an halogen, a (C-C)alkyl or a CN; R1b represents H, an halogen or a (C-C)alkyl; R1c represents H or a (C-C)alkyl; R2 represents H, an halogen, an OH, an O&#x2014;(C-C)alkyl or (C-C)alkyl; R3 represents H, an halogen, a (C-C)alkyl, an OH, an O&#x2014;(C-C)alkyl, a CONHor CN; R4 represents H, an halogen or a (C-C)alkyl; R5 represents H or F: R7 represents H or F; R8 represents H or F; R9 represents H or (C-C)alkyl, or one of its enantiomers. 

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

The present invention relates to NIP thiazole 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. 

NIP thiazole derivatives as inhibitors of 11-beta-hydroxysteroid dehydroge-nase-1

The invention is directed to certain novel compounds, methods for producing them and methods for treating or ameliorating a kinase-mediated disorder. More particularly, this invention is directed to substituted quinazoline compounds useful as selective kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase-mediated disorder, In particular, the methods relate to treating or ameliorating a kinase-mediated disorder including cardiovascular diseases, diabetes, diabetes-associated disorders, inflammatory diseases, immunological disorders, cancer and diseases of the eye such as retinopathies or macular degeneration or other vitreoretinal diseases, and the like.

Substituted quinazoline compounds

Diazepane-acetamide derivatives as selective 11&#x3b2;-HSD1 inhibitors

The present invention relates to novel benzimidazole-dihydrothiadiazinone derivatives as fructose-1,6-bisphosphatase inhibitors, to processes for the preparation thereof and to the use thereof in therapy, especially for the treatment of diabetes.

Benzimidazoledihydrothiadiazinone derivatives as fructose-1,6-bisphosphatase inhibitors, and pharmaceutical compositions comprising same

The present invention relates to 2-adamantyl-butyramide 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. 

2-adamantyl-butyramide derivatives as selective 11&#x3b2;-HSD1 inhibitors

The invention relates to compounds of the general formula (I) below: in which R1, R2, R3, R4, R5, R6 and X are as defined in claim These compounds can be used in the treatment of pathologies associated with insulin resistance syndrome.

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Paris, France

Caroline Leriche