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2. 发明授权

US4900727A 4H-1-benzopyran-4-one compounds which have anti-inflamatory or immunodulating action 失效
标题翻译：具有抗炎或免疫调节作用的4H-1-苯并吡喃-4-酮化合物
公开(公告)号：US4900727A
公开(公告)日：1990-02-13
申请号：US302084
申请日：1989-01-26
申请人： Samba L. Kattige , Ramchandra G. Naik , Aftab D. Lakdawalla , Alihussein N. Dohadwalla , Richard H. Rupp , Noel J. de Souza
发明人： Samba L. Kattige , Ramchandra G. Naik , Aftab D. Lakdawalla , Alihussein N. Dohadwalla , Richard H. Rupp , Noel J. de Souza
IPC分类号： A61K31/445 , A61K31/443 , A61P25/04 , A61P37/06 , A61P37/08 , C07D211/42 , C07D405/04 , C07D405/14
CPC分类号： C07D405/04 , C07D211/42 , C07D405/14
摘要： The present invention relates to novel 4H-1-benzopyran-4-one derivatives, to processes for the preparation thereof and to their use as anti-inflammatory, analgesic, immuno-suppressive and anti-allergic agents. In particular, the present invention relates to novel compounds of the formula I, ##STR1## in which R.sub.1 is hydrogen, alkyl having 1 to 6 carbon atoms, arly-C.sub.1 -C.sub.4 -alkyl, substituted C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.6 -cycloalkyl, C.sub.3 -C.sub.6 -cycloalkyl-C.sub.1 -C.sub.4 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkynyl, aryl or carboxyl or an aldehyde or COO--C.sub.1 -C.sub.4 -alkyl group, R.sub.2 is hydrogen, alkyl having 1 to 6 carbon atoms, nitro, amino, di-C.sub.1 -C.sub.4 -alkylamino or a halogen, R.sub.3 is C.sub.1 -C.sub.4 -alkyl, substituted C.sub.1 -C.sub.4 -alkyl, hydroxyl, C.sub.1 -C.sub.4 -alkoxy, aryl-C.sub.1 -C.sub.4 -alkyl, nitro, amino, a C.sub.1 -C.sub.4 -alkylamino or di-C.sub.1 -C.sub.4 -alkylamino group or halogen, R.sub.4 is hydrogen, hydroxyl, C.sub.1 -C.sub.4 -alkyoxy, C.sub.1 -C.sub.4 -alkyoxycarbonyl, aryloxy, amino or a C.sub.1 -C.sub.4 -alkylamino or di-C.sub.1 -C.sub.4 -alkylamino group, R.sub.5 is hydrogen, C.sub.1 -C.sub.6 -alkyl, substituted C.sub.1 -C.sub.6 -alkyl, aryl-C.sub.1 -C.sub.4 -alkyl, C.sub.3 -C.sub.6 -cycloalkyl, C.sub.3 -C.sub.6 -cycloalkyl-C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkanoyl or aroyl, the aryl group being phenyl which is unsubstituted, monosubstituted or polysubstituted, m is an integer between 0 and 3 and n is an integer between 0 and 2, and to pharmacologically acceptable acid addition salts thereof.
摘要翻译：本发明涉及新的4H-1-苯并吡喃-4-酮衍生物，其制备方法及其作为抗炎，镇痛，免疫抑制和抗过敏剂的用途。特别地，本发明涉及式Ⅰ的新化合物，其中R 1是氢，具有1至6个碳原子的烷基，芳基-C 1 -C 4烷基，取代的C 1 -C 6烷基，C 3 -C 6 环烷基，C 3 -C 6 - 环烷基-C 1 -C 4烷基，C 2 -C 6 - 烯基，C 3 -C 6炔基，芳基或羧基或醛或COO-C 1 -C 4烷基，R 2是氢，具有1至 6个碳原子，硝基，氨基，二-C 1 -C 4烷基氨基或卤素，R 3是C 1 -C 4 - 烷基，取代的C 1 -C 4 - 烷基，羟基，C 1 -C 4 - 烷氧基，芳基-C 1 -C 4烷基，硝基，氨基，C1-C4-烷基氨基或二C1-C4-烷基氨基或卤素，R4是氢，羟基，C1-C4-烷氧基，C1-C4-烷氧基羰基，芳氧基，氨基或C1-C4烷基氨基或二-C 1 -C 4烷基氨基，R 5是氢，C 1 -C 6烷基，取代的C 1 -C 6烷基，芳基-C 1 -C 4 - 烷基，C 3 -C 6 - 环烷基，C 3 -C 6环烷基-C 1 -C 4 - 烷基，C 1 -C 4 - 烷酰基或芳酰基，所述芳基是未取代的，单取代或多取代的苯基，m是0和3之间的整数，n是整数 0和2之间，以及其药理学上可接受的酸加成盐。

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