发明名称 1,4 DIAZEPAN 2,5 DIONE DERIVATIVES AND THEIR USE AS NK 1 RECEPTOR ANTAGONISTS.
摘要 <p>The invention relates to compounds of general formula (I) wherein R1, R2 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; R3 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; R4 is =O, =N(CH2)nCH3 or =N(CH2)nN(R)2; R3 and R4 may be together with the N and C atoms to which they are attached the group CR5=N N=; R5 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.</p>
申请公布号 MXPA02011464(A) 申请公布日期 2003.04.25
申请号 MX2002PA11464 申请日期 2001.05.18
申请人 F. HOFFMANN LA ROCHE AG 发明人 GALLEY, GUIDO
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 主分类号 C07D243/08
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