发明名称 Benzisoxazoles and phenones as alpha2-antagonists
摘要 The present invention concerns compounds of formula (I)the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Alk is C5-12alkanediyl; n is 1 or 2; p is 1 and q is 2; or p is 2 and q is 1; X is -O-, -S-, -S(=O)-, -S(=O)2- or NR2; each R1 is independently hydrogen, halogen, C1-6alkyl, nitro, hydroxy or C1-4alkyloxy; R2 is hydrogen, C1-6alkyl, aryl or C1-6alkyl substituted with aryl; aryl is phenyl or phenyl substituted with a halogen or C1-6alkyl; D is an optionally substituted benzophenone or 3-benzisoxazolyl; having central alpha2-adrenoceptor antagonist activity. It further relates to their preparation, pharmaceutical use and compositions.
申请公布号 US6576640(B1) 申请公布日期 2003.06.10
申请号 US20010868756 申请日期 2001.07.26
申请人 JANSSEN PHARMACEUTICA N.V. 发明人 KENNIS LUDO EDMOND JOSEPHINE;MERTENS JOSEPHUS CAROLUS;PIETERS SERGE MARIA ALOYSIUS
分类号 A61K31/4355;A61K31/4365;A61K31/437;A61K31/44;A61P1/00;A61P3/10;A61P15/10;A61P25/16;A61P25/24;A61P25/28;A61P27/02;A61P43/00;C07D471/04;C07D491/04;C07D491/048;C07D495/04;(IPC1-7):A61K31/437;A61K31/435;A61K31/436 主分类号 A61K31/4355
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