| 摘要 |
The invention relates to compounds of the formula;
wherein R′, R1, through R7 and Ar are as defined herein. These compounds are useful as inhibitors of phosphodiesterase 10 (PDE10A) which are useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type II diabetes, metabolic syndrome, glucose intolerance, pain and ophthalmic diseases. |
| 主权项 |
1. A compound of Formula (I) a pharmaceutically acceptable salt or a tautomer form thereof; wherein: R1 is a (C1-C4)alkyl group optionally substituted with a —(C1-C4)alkoxy or a RaNH group, Ra being selected from the group consisting of (C1-C4)alkyl-C(═O)— and (C1-C4)alkyl-S(═O)2—; R2 is a hydrogen atom; R3 and R4 independently represent a (C1-C3)alkyl group; R5 is a hydrogen atom; R6 and R7 independently represent a hydrogen atom, a halogen atom, or R6 and R7 together with the carbon atom to which they are shown attached form a —C(═O)— group; R′ is —NH2 or —OR, wherein R is a hydrogen atom, a (C1-C3)alkyl group or a (C1-C3)alkyl-C(═O)— group Ar is an aryl or heteroaryl group optionally substituted with one to four substituents independently selected from the group consisting of halogen, azido, hydroxy, (C1-C4)alkyl, (C1-C4)alkoxy, —O—(C1-C4)alkyl-(C1-C6)cycloalkyl, aryl, (C1-C4)alkyl-aryl-, (C1-C4)alkoxy-aryl-, amino-substituted aryl, N((C1-C4)alkyl)2-substituted aryl, aryloxy, heteroaryl, (C1-C4)alkyl-heteroaryl-, and RbRcN, or wherein two substituents at adjacent positions of the aryl or heteroaryl together with the atoms to which they are attached form a heterocyclic ring; and Rb and Rc, are independently selected from the group consisting of hydrogen, (C1-C4)alkyl, halogeno(C1-C4)alkyl-, (C1-C4)alkoxy(C1-C4)alkyl-, aryl(C1-C4)alkyl- and acetylamino(C1-C4)alkyl-. |
