发明名称 Heterocycle compounds and uses thereof
摘要 The invention relates to chemical compounds, or pharmaceutically acceptable salts thereof of the formula (Q) or (I), which penetrate the blood-brain barrier, inhibit the formation and accumulation of beta-amyloid, and are useful in the treatment of neurodegenerative diseases, particularly Alzheimer's disease. Further, the compounds of the present invention inhibit certain kinases, thereby being useful for the treatment of cancers of the central nervous system.;
申请公布号 US9062023(B2) 申请公布日期 2015.06.23
申请号 US200812663224 申请日期 2008.06.06
申请人 Intra-Cellular Therapies, Inc. 发明人 Li Peng
分类号 A01N43/54;A61K31/505;C07D403/00;C07D239/02;C07D401/04;C07D401/12;C07D401/14 主分类号 A01N43/54
代理机构 Hoxie & Associates, LLC 代理人 Hoxie & Associates, LLC
主权项 1. A compound of formula (Q):in free or salt form, wherein: A1 is —C(R7)— or —N—; A2 and A3 are independently —C— or —N—, wherein at least one of A2 and A3 must be N; and wherein when A2 or A3 is —C—, it is optionally substituted with R8; W is —O— or —N(C0-6alkyl)-; Y is —NHCO—, —CONH—; D is a 5 or 6 membered aryl, hetaryl or hetcyclic ring having at least one N, S, or O ring atom, or a C ring atom forming an oxo (C═O) moiety; R1 is phenyl; optionally substituted except at the ortho position of the phenyl with 1-6 halo, C1-6alkoxy, C1-6alkyl, or trifluoromethyl substituents; wherein the ortho phenyl position is unsubstituted; R2 is hetcyclyl(C0-4alkyl)-, optionally substituted with C1-6alkyl; and R3, R4, R5, R6, R7 and R8 are independently selected from hydrogen, halo, C1-4alkyl, C1-4alkoxyl, and haloC1-4alkyl.
地址 New York NY US