发明名称 Benzofurane compounds
摘要 The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I); wherein n, x, Y, R1, R2, R3, and R4 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as pharmaceuticals.
申请公布号 US8877778(B2) 申请公布日期 2014.11.04
申请号 US201113313045 申请日期 2011.12.07
申请人 Hoffmann-La Roche Inc. 发明人 Rodriguez Sarmiento Rosa Maria;Wichmann Juergen
分类号 A61K31/445;C07D405/14;C07D405/10 主分类号 A61K31/445
代理机构 代理人
主权项 1. A compound of formula (I) wherein n is 0, 1, 2, 3 or 4; x is a single bond or double bond; Y is —C(O)— or —S(O)2—; R1 hydrogen, cyano, alkyl, haloalkyl, alkenyl, alkynyl, hydroxy, alkoxy, cycloalkyl, heterocycloalkyl, aryl, aryl annelated to heterocycloalkyl, heteroaryl, —NR7R8, —C(O)—NR7R8, or —S(O)2—R7, wherein alkyl, haloalkyl, and alkoxy are each optionally substituted by one to three independent R5 and wherein cycloalkyl, heterocycloalkyl, aryl, and heteroaryl are each optionally substituted by one to three independent R6; R2, R3, and R4 are each independently hydrogen, halogen, alkyl, haloalkyl, hydroxy, alkoxy or haloalkoxy; R5 is cyano, hydroxy, alkoxy, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl, wherein cycloalkyl, heterocycloalkyl, aryl, and heteroaryl are each optionally substituted by one to three independent R6; R6 is halogen, cyano, alkyl, haloalkyl, hydroxy, alkoxy, haloalkoxy, oxo, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, or —S(O)2—R7, wherein cycloalkyl, heterocycloalkyl, aryl, and heteroaryl are each optionally substituted by one to three independent R9; and R7, R8, and R9 are each independently hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl, aryl, or heteroaryl; or a pharmaceutically acceptable salt or ester thereof.
地址 Nutley NJ US