发明名称 Isoxazolidine derivatives
摘要 PCT No. PCT/EP97/01830 Sec. 371 Date Oct. 6, 1998 Sec. 102(e) Date Oct. 6, 1998 PCT Filed Apr. 9, 1997 PCT Pub. No. WO97/39001 PCT Pub. Date Oct. 23, 1997This invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is zero to 6; p is zero to 3; q is zero to 3; r is zero to 3; R1 and R2 each independently are hydrogen; optionally substituted C1-6alkyl; C1-6alkylcarbonyl; trihalomethylcarbonyl; or R1 and R2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; each R3 and R4 independently are halo, cyano, hydroxy, trihalomethyl, trihalomethoxy, carboxyl, nitro, amino, mono- or di(C1-6alkyl)amino, C1-6alkylcarbonylamino, aminosulfonyl, mono- or di(C1-6alkyl)-aminosulfonyl, C1-6alkyl, C1-6alkyloxy, C1-6alkylcarbonyl or C1-6alkyloxycarbonyl; each R5 independently is C1-6alkyl, cyano or trihalomethyl; X is CR6R7, NR8, O, S, S(=O) or S(=O)2; each independently represents a bivalent aromatic heterocycle wherein the heterocycle may be selected from the group consisting of pyrrole, pyrrazole, imidazole, triazole, furane, thiophene, isoxazole, oxazole, isothiazole, thiazole, pyridine, pyridazine, pyrimidine, pyrazine and triazine; or one of the two bivalent aromatic heterocycles in the compounds of formula (I) may be 1,2-benzenediyl; and aryl is optionally substituted phenyl; it further relates to compositions comprising thesae compounds, as well as their use as therapeutic agents in the treatment or the prevention of CNS disorders, cardiovascular disorders or gastrointestinal disorders.
申请公布号 US6156747(A) 申请公布日期 2000.12.05
申请号 US19980155839 申请日期 1998.10.06
申请人 JANSSEN PHARMACEUTICA N.V. 发明人 ANDRES-GIL, JOSEIGNACIO;MARTINEZ-JIMENEZ, PEDRO;FERNANDEZ-GADEA, FRANCISCO JAVIER;SIPIDO, VICTOR KAREL
分类号 A61K31/00;A61K31/55;A61K31/551;A61K31/5513;A61K31/553;A61P1/00;A61P9/00;A61P9/12;A61P25/06;A61P25/18;A61P25/20;A61P25/22;A61P25/24;A61P25/28;A61P43/00;C07D237/30;C07D471/04;C07D487/04;C07D495/04;C07D498/04;C07D498/14;C07D498/16;(IPC1-7):A61K31/55;C07D223/14;C07D255/00;C07D243/00;C07D498/22 主分类号 A61K31/00
代理机构 代理人
主权项
地址