发明名称 1,4-DIAZEPAN-2,5-DIONE DERIVATIVES AND THEIR USE AS NK-1 RECEPTOR ANTAGONISTS
摘要 The invention relates to compounds of general formula (I) wherein R<1>, R<2> are independently from each other aryl or heteroaryl, wherein the heteroaryl group contains one or two heteroatoms, selected from N, O or S, and wherein the aryl or heteroaryl groups are optionally substituted by 1 to 3 substituents, which are independently from each other halogen, CF3, lower alkoxy or lower alykl; R<3> is hydrogen, lower alkyl, -(CH2)nN(R)2, -(CH2)n-heteroaryl or is a -(CH2)n-non aromatic heterocycle, which heterocycles are optionally substituted by halogen, CF3, lower alkoxy or lower alkyl; R<4> is =O, =N(CH2)nCH3 or =N(CH2)nN(R)2; R<3> and R<4> may be together with the N and C atoms to which they are attached the group -CR<5>=N-N=; R<5> is hydrogen, -(CH2)nN(R)2, -(CH2)n-heteroaryl or is a -(CH2)n-non aromatic heterocycle, which heterocycles are optionally substituted by halogen, CF3, lower alkoxy or lower alkyl; R is hydrogen or lower alkyl; n is 0, 1, 2 or 3; and pharmaceutically acceptable acid addition salts and enantiomeric forms thereof. The compounds are useful in the treatment of diseases, related to the NK-1 receptor.
申请公布号 WO0190083(A1) 申请公布日期 2001.11.29
申请号 WO2001EP05723 申请日期 2001.05.18
申请人 F. HOFFMANN-LA ROCHE AG 发明人 GALLEY, GUIDO;GOERGLER, ANNICK;GODEL, THIERRY;HECK, REINHARD
分类号 C07D243/08;A61K31/551;A61K31/5517;A61P1/04;A61P1/08;A61P9/00;A61P11/06;A61P13/10;A61P17/02;A61P19/02;A61P25/00;A61P25/06;A61P27/02;A61P29/00;A61P37/08;C07D243/14;C07D401/06;C07D401/14;C07D403/06;C07D409/06;C07D487/04;(IPC1-7):C07D243/08 主分类号 C07D243/08
代理机构 代理人
主权项
地址