发明名称 Substituted [1,2,4]triazolo[1,5-a]pyrazines as phosphodiesterase inhibitors
摘要 Provided herein are substituted triazolopyrazine phosphodiesterase inhibitors, and pharmaceutical compositions thereof, useful for the treatment of, for example, central nervous system and metabolic diseases and disorder.
申请公布号 US9505751(B2) 申请公布日期 2016.11.29
申请号 US201314409866 申请日期 2013.06.19
申请人 Sunovion Pharmaceuticals Inc. 发明人 Campbell John Emmerson;Jones Phillip G.;Malcolm Scott
分类号 A61K31/4985;C07D241/38;C07D487/04;C07D471/04;A61K31/437;A61K31/4709;C07D519/00 主分类号 A61K31/4985
代理机构 代理人
主权项 1. A compound of formula (I): or a pharmaceutically acceptable salt or stereoisomer thereof, wherein n is 1, 2, or 3;m is 0, 1, 2, 3, 4, 5, 6, 7, or 8; provided that (i) when n is 1, m is 0, 1, 2, 3, or 4; (ii) when n is 2, m is 0, 1, 2, 3, 4, 5, or 6; and (iii) when n is 3, m is 0, 1, 2, 3, 4, 5, 6, 7, or 8;each R is independently halo or (C1-C4) alkyl;each Y is CR3;each R3 is independently hydrogen, halo, cyano, alkyl, alkenyl, alkoxy, aminoalkyl, heteroalkyl, cycloalkyl, aryl, heteroaryl, heterocyclyl, amino, amido or thiol;B is (i) R4 and R5 together with the atoms to which they are attached form a monocyclic or multicyclic aryl, heteroaryl, cycloalkyl, or heterocyclyl ring; or (ii) R4 and R5 are each independently hydrogen, cyano, halo, alkyl, alkenyl, alkoxy, aminoalkyl, heteroalkyl, cycloalkyl, aralkyl, heteroaralkyl, heteroaryl, heterocyclyl, hydroxy, amino, imino, amido or thiol; B1 is O, S, or NR8;B2 is CR9 or N;R6 is hydrogen, halo, cyano, alkyl, alkenyl, alkoxy, aminoalkyl, heteroalkyl, cycloalkyl, aralkyl, heteroaralkyl, aryl, heteroaryl, heterocyclyl, amino, amido or thiol;R7 is hydrogen, alkyl, alkenyl, heteroalkyl, cycloalkyl, aryl, heteroaryl or heterocyclyl;R8 is hydrogen, alkyl, alkenyl, heteroalkyl, cycloalkyl, aryl, heteroaryl, or heterocyclyl; andR9 is hydrogen, halo, cyano, alkyl, alkenyl, alkoxy, aminoalkyl, heteroalkyl, cycloalkyl, aralkyl, heteroaralkyl, aryl, heteroaryl, heterocyclyl, amino, amido or thiol;provided that a compound of formula (I) is not:
地址 Marlborough MA US