公开(公告)号：US5350761A

公开(公告)日：1994-09-27

申请号：US99873

申请日：1993-07-30

申请人： John H. Van Duzer ,  Dennis M. Roland

发明人： John H. Van Duzer ,  Dennis M. Roland

IPC分类号： C07D209/46 ,  C07D217/24 ,  C07D223/16 ,  C07D279/02 ,  C07D401/06 ,  C07D401/12 ,  C07D409/06 ,  A61K31/405 ,  C07D209/12 ,  C07D209/34

CPC分类号： C07D209/46 ,  C07D217/24 ,  C07D223/16 ,  C07D279/02 ,  C07D401/06 ,  C07D401/12 ,  C07D409/06

摘要： Disclosed are the compound of the formula ##STR1## wherein R represents hydrogen, lower alkyl, aryl, biaryl, C.sub.3 -C.sub.7 -cycloalkyl, aryl-lower alkyl, aryl-lower alkenyl, aryl-lower alkynyl, aryloxy-lower alkyl, arylthio-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl, biaryl-lower alkyl, aryl-C.sub.3 -C.sub.7 -cycloalkyl, aryl-C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl or aryloxy-aryl-lower alkyl; and aryl represents carbocyclic or heterocyclic aryl;Z represents C.sub.1 -C.sub.3 -alkylene or vinylene, each unsubstituted or substituted by lower alkyl;Y represents SO.sub.2 (sulfonyl) or CO (carbonyl);A represents O (oxygen), S (sulfur), or a direct bond;B represents lower alkylene; or B represents lower alkenylene provided that A represents a direct bond;X represents oxygen or sulfur,R.sub.1 represents hydrogen, acyl, lower alkoxycarbonyl, aminocarbonyl, mono- or di-lower alkylaminocarbonyl, lower alkenylaminocarbonyl, lower alkynylaminocarbonyl, carbocyclic or heterocyclic aryl-lower alkylaminocarbonyl, carbocyclic or heterocyclic arylaminocarbonyl, C.sub.3 -C.sub.7 -cycloalkylaminocarbonyl or C.sub.3 -C.sub.7 -cycloalkyl-lower alkylaminocarbonyl;R.sub.2 represents lower alkyl, lower alkoxycarbonyl-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl, carbocyclic or heterocyclic aryl, carbocyclic or heterocyclic aryl-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl, amino, mono- or di-lower alkylamino, lower alkenylamino, lower alkynylamino, carbocyclic or heterocyclic aryl-lower alkylamino, carbocyclic or heterocyclic arylamino, C.sub.3 -C.sub.7 -cycloalkylamino, C.sub.3 -C.sub.7 -cycloalkyl-lower alkylamino or lower alkoxycarbonyl-lower alkylamino;R.sub.3 and R.sub.4 independently represent hydrogen or lower alkyl;R.sub.a represents hydrogen, lower alkyl, halo, trifluoromethyl or lower alkoxy; and pharmaceutically acceptable salts thereof; which are useful as lipoxygenase inhibitors.

摘要翻译： 公开了式（I）的化合物，其中R表示氢，低级烷基，芳基，联芳基，C 3 -C 7 - 环烷基，芳基 - 低级烷基，芳基 - 低级烯基，芳基 - 低级炔基，芳氧基 - 低级烷基 ，芳硫基 - 低级烷基，C 3 -C 7 - 环烷基 - 低级烷基，联芳基 - 低级烷基，芳基-C 3 -C 7 - 环烷基，芳基-C 3 -C 7 - 环烷基 - 低级烷基或芳氧基 - 芳基 - 低级烷基; 芳基表示碳环或杂环芳基; Z表示C1-C3-亚烷基或亚乙烯基，各自未被取代或被低级烷基取代; Y表示SO 2（磺酰基）或CO（羰基）; A表示O（氧），S（硫）或直接键; B表示低级亚烷基; 或B表示低级亚烯基，条件是A表示直接键; X代表氧或硫，R1代表氢，酰基，低级烷氧基羰基，氨基羰基，一或二低级烷基氨基羰基，低级烯基氨基羰基，低级炔基氨基羰基，碳环或杂环芳基 - 低级烷基氨基羰基，碳环或杂环芳基氨基羰基，C3-C7-环烷基氨基羰基或 C 3 -C 7 - 环烷基 - 低级烷基氨基羰基; R 2表示低级烷基，低级烷氧基羰基 - 低级烷基，C 3 -C 7 - 环烷基，碳环或杂环芳基，碳环或杂环芳基 - 低级烷基，C 3 -C 7 - 环烷基 - 低级烷基，氨基，一或二 - 低级烷基氨基，低级 碳环或杂环芳基 - 低级烷基氨基，碳环或杂环芳基氨基，C 3 -C 7 - 环烷基氨基，C 3 -C 7 - 环烷基 - 低级烷基氨基或低级烷氧基羰基 - 低级烷基氨基; R3和R4独立地表示氢或低级烷基; R a表示氢，低级烷基，卤素，三氟甲基或低级烷氧基; 及其药学上可接受的盐; 它们可用作脂氧合酶抑制剂。