| 摘要 |
The present invention provides a compound of formula I:;;Said compound is inhibitor of aldosterone synthase and aromatase, and thus can be employed for the treatment of a disorder or disease mediated by aldosterone synthase or aromatase. Accordingly, the compound of formula I can be used in treatment of hypokalemia, hypertension, congestive heart failure, atrial fibrillation, renal failure, in particular, chronic renal failure, restenosis, atherosclerosis, syndrome X, obesity, nephropathy, post-myocardial infarction, coronary heart diseases, inflammation, increased formation of collagen, fibrosis such as cardiac or myocardiac fibrosis and remodeling following hypertension and endothelial dysfunction, gynecomastia, osteoporosis, prostate cancer, endometriosis, uterine fibroids, dysfunctional uterine bleeding, endometrial hyperplasia, polycystic ovarian disease, infertility, fibrocystic breast disease, breast cancer and fibrocystic mastopathy. Finally, the present invention also provides a pharmaceutical composition. |
| 主权项 |
1. A compound of formula (III)wherein
R is hydrogen, (C1-C4) alkyl, (C2-C4) alkenyl, —C(O)O—R10, or —C(O)N(R11)(R12), said (C1-C4) alkyl and (C2-C4) alkenyl are optionally substituted by one to three substituents independently selected from hydroxyl, (C1-C4) alkoxy, halo, —NH2, or (C1-C4)-[(alkyl)(alkyl)N—]; wherein R10, R11 and R12 are independently hydrogen, (C1-C4) alkyl, (C6-C10) aryl-(C1-C4) alkyl-, (C3-C8) cycloalkyl, or (C2-C4) alkenyl, each of which is optionally substituted by one to three substituents independently selected from halo, hydroxyl, or (C1-C4) alkoxy; wherein R11 and R12 taken together with the nitrogen atom to which they are attached optionally form a 3-8-membered ring: R1, R2, R3, R4, and R5 are independently selected from hydrogen, halo, cyano, —NH2, (C1-C4)-[(alkyl)(alkyl)N—], (C1-C4) alkoxy, (C2-C4) alkenyl, (C1-C4) alkyl, (C1-C4) haloalkyl, (C6-C10) aryl, or (5-9)-membered heteroaryl, said (C1-C4) alkoxy, (C2-C4) alkenyl, (C1-C4) alkyl and (C6-C10) aryl being optionally substituted by one to three substituents independently selected from halo, (C1-C4) alkoxy, (C1-C4) alkyl, —NH2, cyano, nitro, (C1-C4) alkoxy-(C1-C4) alkyl-, or (C1-C4) haloalkyl, with the proviso that no more than three of R1, R2, R3, R4, and R5 are simultaneously hydrogen; R and R1 taken together optionally form a 5-6-membered ring containing 0 or 1 heteroatom selected from O, N, or S; R6 and R7 are independently hydrogen, (C1-C4) alkyl, (C3-C8) cycloalkyl, (C1-C4) alkoxy, phenyl, or benzyl, said phenyl and benzyl are optionally substituted by one to three substituents independently selected from halo, (C1-C4) alkyl, or (C1-C4) alkoxy: when R6 and R7 are attached to the same carbon atom, they optionally form a moiety (A) represented by the following structure:wherein Ra and Rb are independently hydrogen, or (C1-C4) alkyl, or Ra and Rb taken together with said carbon atom optionally form a 3-8-membered ring;or a compound selected from the group consisting of 5-(2-cyclopropylphenyl)-5,6,7,8-tetrahydroimidazo[1,5-a]pyridine, 5-(4-cyclopropylphenyl)-5,6,7,8-tetrahydroimidazo[1,5-a]pyridine, 3-cyclopropyl-4-(5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-5-yl)benzonitrile and 4-((R)-1-bromo-5,6,7,8-tetrahydroimidazo[1,5a]pyridin-5-yl)benzonitrile,or a pharmaceutically acceptable salt thereof; or an optical isomer thereof; or a mixture of optical isomers. |
