Napthyridine compounds as rock inhibitors

Details Napthyridine compounds as rock inhibitors Napthyridine compounds as rock inhibitors

C - Chemistry, Metallurgy

07

D

C07D 471/04 (2006.01) A61K 31/4375 (2006.01) A61P 7/02 (2006.01) A61P 9/00 (2006.01) A61P 11/06 (2006.01) A61P 15/10 (2006.01) A61P 19/10 (2006.01) A61P 27/06 (2006.01) A61P 29/00 (2006.01) A61P 31/00 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2593718

The present invention relates to compounds having a naphthyridine scaffold, and stereoisomeric forms, prodrugs, solvates, hydrates and/or pharmaceutically acceptable salts of these compounds as well as pharmaceutical compositions containing at least one of these naphthyridine derivatives together with pharmaceutically acceptable carrier, excipient and/or diluents. Said naphthyridine compounds have been identified as inhibitors of the protein kinase ROCK2, also known as Rho-kinase, and are useful for the treatment of cancers (tumor growth and metastases), erectile dysfunction, cardiovascular diseases, hypertension, angina pectoris, cerebral ischaemia, cerebral vasospasm, myocardial ischaemia, coronary vasospasm, heart failure, myocardial hypertrophy, atherosclerosis, restenosis, spinal cord injuries, neuronal degeneration, thrombotic disorders, asthma, glaucoma, inflammation, anti-viral diseases (e.g. HIV), and osteoporosis.

Cette invention concerne des composés comportant un échafaudage de naphthyridine et des formes stéréoisomériques, des promédicaments, des solvates, des hydrates et/ou des sels pharmaceutiquement acceptables de ces composés, ainsi que des compositions pharmaceutiques contenant au moins un de ces dérivés de naphthyridine de même qu'un vecteur, un excipient et/ou des diluants pharmaceutiquement acceptables. Ces composés de naphthyridine ont été identifiés comme étant des inhibiteurs de la protéine kinase ROCK2, aussi connue sous le nom de Rho-kinase, et sont utilisés pour traiter des cancers (croissance tumorale et métastases), la dysérection, des maladies cardio-vasculaires, l'hypertension, l'angine de poitrine, l'ischémie cérébrale, le vasospasme cérébral, l'insuffisance cardiaque, l'hypertrophie du myocarde, l'athérosclérose, la resténose, des traumatismes médullaires, la dégénérescence neuronale, des troubles thrombotiques, l'asthme, le glaucome, l'inflammation, des maladies antivirales (telles que le VIH) et l'ostéoporose.

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