首页> 外国专利> BISETHERS OF 1-OXA, AZA AND THIANAPHTHALEN-2- ONES AS PHOSPHOLAMBAN INHIBITORS

BISETHERS OF 1-OXA, AZA AND THIANAPHTHALEN-2- ONES AS PHOSPHOLAMBAN INHIBITORS

机译:1-氧杂,氮杂和噻吩-2-烯的双酚类化合物作为磷酰胺的抑制剂

摘要

Therapeutically active compounds of formula (I) or (II), in which R1 is hydrogen, alkyl, alkenyl, aryl, arylalkyl, hydroxyalkyl, halogenalkyl, alkoxy, COR10, CONR10R11, OR10, S(O)mR10, NR10COR11 or NR10R11, where R10 is hydrogen, alkyl, alkenyl, aryl, arylalkyl, hydroxyalkyl, halogenalkyl, alkoxy or hydroxy and R11 is hydrogen, alkyl, aryl, arylalkyl, alkoxy, aryloxy, hydroxy or acyl, or in case where X is NR11, R1 can also be carboxylalkyl; R6 is hydrogen, alkyl, alkenyl, aryl, arylalkyl; R2 and R7 mean hydrogen, alkyl, aryl, arylalkyl, alkenyl, COR10, CONR10R11, halogen, trifluoromethyl, nitro or cyano, where R10 and R11 are defined as above; R3 is hydrogen, alkyl, aryl or arylalkyl; A means alkyl or substituted alkyl, m is 0-2 and n is 1-3; Y means O, NR11 or S, where R11 is the same as above; X means O, NR11 or S, where R11 is the same as above, R4, R5, R8 and R9 mean independently one of the following groups (a), (b), (c), (d), (e), (f), (g), or in case where X is NR11, R4, R5, R8 and R9 can also independently mean HOOC-, R12OOC-, H2NCO- or HOHNCO-, wherein R12 means alkyl, arylalkyl or aryl, and wherein each aryl residue defined above by itself or as part of another group may be substituted, and pharmaceutically acceptable salts and esters thereof. The compounds have phospholamban inhibiting activity and are useful for treating heart failure.
机译:式(I)或(II)的治疗活性化合物,其中R 1为氢,烷基,烯基,芳基,芳基烷基,羟烷基,卤代烷基,烷氧基,COR10,CONR10R11,OR10,S(O)mR10,NR10COR11或NR10R11,其中R 10为氢,烷基,烯基,芳基,芳基烷基,羟烷基,卤代烷基,烷氧基或羟基,R 11为氢,烷基,芳基,芳基烷基,烷氧基,芳氧基,羟基或酰基,或者在X为NR11的情况下,R1也可以为羧基烷基R6是氢,烷基,烯基,芳基,芳基烷基; R2和R7是指氢,烷基,芳基,芳基烷基,烯基,COR10,CONR10R11,卤素,三氟甲基,硝基或氰基,其中R10和R11如上所定义; R3是氢,烷基,芳基或芳基烷基; A为烷基或取代的烷基,m为0-2且n为1-3; Y表示O,NR11或S,其中R11与上述相同; X表示O,NR11或S,其中R11与上述相同,R4,R5,R8和R9分别表示以下基团(a),(b),(c),(d),(e)中的一个, (f),(g),或在X为NR11的情况下,R4,R5,R8和R9还可以独立地表示HOOC-,R1200C-,H2NCO-或HOHNCO-,其中R12表示烷基,芳基烷基或芳基,并且其中上面单独定义或作为另一基团的一部分定义的每个芳基残基及其药学上可接受的盐和酯。该化合物具有磷酸lamban抑制活性,可用于治疗心力衰竭。

著录项

  • 公开/公告号IL134662D0

    专利类型

  • 公开/公告日2001-04-30

    原文格式PDF

  • 申请/专利权人 ORION CORPORATION;

    申请/专利号IL19980134662

  • 发明设计人

    申请日1998-09-24

  • 分类号7C07DA;

  • 国家 IL

  • 入库时间 2022-08-22 01:24:55

相似文献

  • 专利
  • 外文文献
  • 中文文献
获取专利

客服邮箱:kefu@zhangqiaokeyan.com

京公网安备:11010802029741号 ICP备案号:京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有
  • 客服微信

  • 服务号