发明名称 Arlethynyl Derivatives
摘要 The present invention relates to ethynyl compounds of formula I-C1;;wherein R1, R2, R2′, R3, R3′, R6, U, V and W are as defined herein and to a pharmaceutically acceptable acid addition salts, to a racemic mixtures, or to its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof, which are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).
申请公布号 US2014155602(A1) 申请公布日期 2014.06.05
申请号 US201314085064 申请日期 2013.11.20
申请人 Hoffmann-La Roche Inc. 发明人 Green Luke;Guba Wolfgang;Jaeschke Georg;Jolidon Synese;Lindemann Lothar;Ricci Antonio;Rueher Daniel;Stadler Heinz;Vieira Eric
分类号 C07D401/04;C07D403/04;C07D471/04 主分类号 C07D401/04
代理机构 代理人
主权项 1. The compound of formula I-C1 wherein U is ═N— or ═C(R5)—; V is —CH═ or —N═; W is ═CH— or ═N—; with the proviso that only one of U, V or W is nitrogen. R5 is hydrogen, methyl or halogen; R6 is hydrogen or lower alkyl; R1 is phenyl or heteroaryl, each of which is optionally substituted by one or two substituents, selected from halogen, lower alkyl and lower alkoxy; R2 and R2′ are each independently hydrogen, lower alkyl, hydroxy, lower alkoxy, C3-C6-cycloalkyl, or CH2-lower alkoxy, or together with the carbon atom to which they are attached form a C3-C6-cycloalkyl group or a ring containing —CH2OCH2—; and R3 and R3′ are each independently hydrogen, lower alkyl, or CH2-lower alkoxy or together with the carbon atom to which they are attached form a C3-C6-cycloalkyl group; or R3 and R2 together with the carbon atom to which they are attached form a C3-6-cycloalkyl group or a ring containing —(CH2)2OCH2—; or R6 and R2 together with the carbon atom and the nitrogen atom to which they are attached form a C3-6-cycloalkyl group; or a pharmaceutically acceptable acid addition salt, a racemic mixture, an enantiomers, an optical isomer and/or stereoisomer thereof.
地址 Nutley NJ US