Acylated indanyl amines and their use as pharmaceuticals

Details Acylated indanyl amines and their use as pharmaceuticals Acylated indanyl amines and their use as pharmaceuticals

C - Chemistry, Metallurgy

07

C

C07C 233/64 (2006.01) A61K 31/165 (2006.01) A61K 31/36 (2006.01) A61K 31/38 (2006.01) A61K 31/435 (2006.01) A61P 9/00 (2006.01) C07C 233/58 (2006.01) C07C 233/65 (2006.01) C07C 233/66 (2006.01) C07C 233/74 (2006.01) C07C 233/76 (2006.01) C07C 235/42 (2006.01) C07C 235/44 (2006.01) C07C 235/54 (2006.01) C07C 235/84 (2006.01) C07C 237/38 (2006.01) C07C 237/42 (2006.01) C07C 255/57 (2006.01) C07C 255/60 (2006.01) C07C 309/66 (2006.01) C07C 309/73 (2006.01) C07C 311/08 (2006.01) C07C 311/16 (2006.01) C07C 311/2

Patent

CA 2437944

The present invention relates to acylated indanyl amines according to the general formula (I) where R1-R4 have the meanings given in the description, A is CH2 CHOH or CH-(C1-C3-alkyl), B is CH2 or CH-(C1-C3-alkyl), and R5 is an aryl or heteroaryl group, possibly substituted by the substituents listed in the description. These compounds are useful in the upregulation of endothelial nitric oxide synthase (eNOS), and may therefore be useful for the manufacture of medicaments for the treatment of cardiovascular diseases, stable or unstable angina pectoris, coronary heart disease, Prinymetal angina, actue coronary syndrome, heart failure, myocardial infarction, stroke, thrombosis, peripheral artery occlusive disease, endothelial dysfunction, atherosclerosis, restenosis, endothel damage after PTCA, hypertension, essential hypertension, pulmonary hypertension, secondary hypertension, renovascular hypertension, chronic glomerulonephritis, erectile dysfunction, ventricular arrhythmia, diabetes or diabetes complications, nephropathy or retinopathy, angiogenesis, asthma bronchiale, chronic renal failure, cirrhosis of the liver, osteoporosis, restricted memory performance, a restricted ability to learn, or for the lowering of cardiovascular risk of postmenopausal women or after intake of contraceptives.

La présente invention porte sur des amines indanyle acylés de la formule générale (I) dans laquelle R?1¿-R?4¿ sont tels que définis dans la demande ; A représente CH¿2? CHOH ou CH-(C¿1?-C¿3?-alkyl), B représente CH¿2? ou CH-(C¿1?-C¿3?-alkyl), et R?5¿ représente un groupe aryle ou hétéroaryle, éventuellement substitué par les substituants listés dans la demande. ?es composés sont utiles dans la régulation de la synthase endothéliale de l'oxyde nitrique (eNOS), et peuvent, par conséquent, être utiles dans la fabrication de médicaments prévus pour traiter les maladies cardio-vasculaires, l'angine de poitrine stable ou instable, la coronaropathie, l'angor de Prinzmetal, le syndrome coronaire aigu, l'insuffisance cardiaque, l'infarctus du myocarde, l'ictus, la thrombose, l'artérite oblitérante, le dysfonctionnement endothélial, l'athérosclérose, la resténose, les lésions endothéliales après angioplastie coronarienne transluminale percutanée (ACTP), l'hypertension, l'hypertension artérielle essentielle, l'hypertension pulmonaire, l'hypertension secondaire, l'hypertension rénovasculaire, la glomérulonéphrite chronique, la dysérection, l'arythmie ventriculaire, les diabètes ou complications de diabètes, la néphropathie ou la rétinopathie, l'angiogenèse, l'asthme bronchique, l'insuffisance rénale chronique, la cirrhose du foie, l'ostéoporose, les troubles de la mémoire, les troubles d'apprentissage, ce médicament permettant également de réduire les risques cardio-vasculaires des femmes postménopausées ou après une prise de contraceptifs.

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