发明名称 Positive allosteric modulators of MGLUR2
摘要 The present invention is directed to benzimidazolone derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved, such as schizophrenia.
申请公布号 US8993779(B2) 申请公布日期 2015.03.31
申请号 US201113814870 申请日期 2011.08.05
申请人 Merck Sharp & Dohme Corp. 发明人 Dudkin Vadim Y.;Fraley Mark E.;Arrington Kenneth L.;Layton Mark E.;Reif Alexander J.;Rodzinak Kevin J.;Pero Joseph E.
分类号 C07D235/26;C07D417/14;C07D403/04;C07D403/14;C07D401/04;C07D401/14;C07D401/06;C07D401/10;C07D401/12;C07D403/10;C07D405/06;C07D453/02;C07D513/14;C07D405/10;C07D409/10;C07D413/10;C07D471/04 主分类号 C07D235/26
代理机构 代理人 MacMillan Keith D.;Todaro John C.
主权项 1. A compound according Formula Icor a pharmaceutically acceptable salt thereof, wherein E1 and E2 are independently C or N; ring B is phenyl or heteroaryl, R3 is CN, halo or C1-4alkyl, optionally substituted with 1-5 halo atoms, and each R6 is independently selected from the group consisting of: CN, halo, R5, —O—R5, —N(R)—R5, —N(R)C(O)—R5, —N(R)S(O)2—R5, —N(R)—C(O)—O—R5, —C(O)—N(R)—R5, —C(O)—O—R5, —C(O)—R5, —C(O)—C(R4)2—R5, —C(O)—C(R4)2—S(O)2—R5, —C(R4)2—N(R)—R5, —SO2—N(R)—R5, —Si(CH3)2(R5), —C(R4)2—R5 and —SO2—R5; each R is independently selected from the group consisting of: H and C1-4alkyl; each R4 is independently selected from the group consisting of: H, OH and C1-4alkyl; each R5 is independently selected from the group consisting of: H, C1-4alkyl, C2-4alkenyl, C2-4alkynyl, C3-6cycloalkyl, phenyl, benzyl, heterocycle and heteroaryl, wherein each member of the group excluding hydrogen is optionally substituted with 1 to 3 substituents independently selected from: halogen, cyano, hydroxy and methyl; Z is selected from H, halo, hydroxy, methyl, methoxy or CN; R1 is selected from the group consisting of: (1) C2-8alkyl,(2) C2-8alkenyl,(3) C2-8alkynyl,(4) C3-6cycloalkyl-(CH2)p—,(5) aryl-(CH2)p—,(6) heteroaryl-(CH2)p—, and(7) heterocycle-(CH2)p—, wherein p is 0, 1, 2, 3 or 4, and groups (1) to (7) above are optionally substituted with 1 to 4 R2 groups; and each R2 is independently selected from the group consisting of: halo, OH, —CN, C1-4alkyl, C1-4alkoxy, CF3, —OCF3, —C(O)—O—C1-4alkyl, —N(R)2, pyrimidinyl and —CN.
地址 Rahway NJ US