| 摘要 |
Certain disubstituted 3,8-diaza-bicyclo[4.2.0]octane and 3,6-diazabicyclo[3.2.0]heptane are described, which are useful as orexin inhibitors. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia. |
| 主权项 |
1. A chemical entity that is a compound of Formula (I): wherein n is 0-1; R1 is a member selected from the group consisting of:
A) phenyl substituted or unsubstituted with Ra, and substituted in the ortho position with Rb;Ra is a member independently selected from the group consisting of: halo, —C1-4alkyl, and —C1-4alkoxy;Rb is a member selected from the group consisting of:
a) halo or —C1-4alkoxy,b) thiophen-2-yl, 2H-1,2,3-triazole, 1H-1,2,3-triazol-1-yl, 1H-pyrazol-1-yl, 1H-pyrazol-5-yl, pyrimidin-2-yl, isoxazol-5-yl, 3-methylisoxazol-5-yl or 3-methyl-1,2,4-oxadiazol-5-yl, andc) phenyl;B) pyridine substituted or unsubstituted with one or two members independently selected from the group consisting of: C1-4alkyl and 1H-1,2,3-triazol-1-yl, wherein the substituents are positioned adjacent to the point of attachment by R1; andC) methylthiazole substituted with 2-fluorophenyl; R2 is a member selected from the group consisting of:
A) 6-membered heteroaryl ring containing two nitrogen members substituted or unsubstituted with one or more members selected from the group consisting of: —C1-4 alkyl, —C1-4alkoxy, —CF3, halo, —N(C1-4alkyl)2, —NH2, and phenyl;B) pyridine substituted or unsubstituted with one or more members independently selected from the group consisting of: —CF3 and —C1-4alkyl;C) quinoxalin-2-yl or quinoline substituted or unsubstituted with —C1-4alkyl;D) benzooxazol-2-yl substituted or unsubstituted with halo; andE) 4-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidine; and pharmaceutically acceptable salts of compounds of Formula (I). |
