发明名称 SUBSTITUTED 6,7-DIALKOXY-3-ISOQUINOLINOL DERIVATIVES AS INHIBITORS OF PHOSPHODIESTERASE 10 (PDE 10A)
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.
申请公布号 US2014309253(A1) 申请公布日期 2014.10.16
申请号 US201414314930 申请日期 2014.06.25
申请人 Allergan, Inc. 发明人 Leblond Bertrand;Chauvignac Cedric;Taverne Thierry;Beausoleil Eric;Casagrande Anne-Sophie;Desire Laurent;Pando Matthew P.;Donello John E.;Yang Rong
分类号 C07D491/056;C07D401/14;C07D401/06;C07D217/24;C07D405/06 主分类号 C07D491/056
代理机构 代理人
主权项 1. A compound of Formula (I) or a pharmaceutically acceptable salt thereof; wherein: R1 is a (C1-C4)alkyl group which can optionally be 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 which can optionally be 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-.
地址 Irvine CA US