首页> 外国专利> INDENO2,1-CQUINOLINONE AND INDENO2,1-B-ISOQUINOLINONE DERIVATIVES AND PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, PREPARATION AND USE THEREOF

INDENO2,1-CQUINOLINONE AND INDENO2,1-B-ISOQUINOLINONE DERIVATIVES AND PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, PREPARATION AND USE THEREOF

机译:茚并[2,1-C]喹啉酮和茚并[2,1-B]-异喹啉酮衍生物及其药物可接受的盐的制备,制备和使用

摘要

The present invention relates to indeno [2,1-c] quinolinone and indeno [2,1-b] isoquinolinone derivatives represented by the general formula (1), wherein A is optionally substituted with up to two hydroxyl groups or halogen atoms, or an alkoxy or C1-4 alkoxy group. - a C2-C2 alkylenedioxy-substituted benzene or naphthalene ring; B is optionally halogen, up to two hydroxyl, nitro, amino, C 1-4 alkyl, C 1-4 alkoxy or C 1-4 alkylcarbonylamino groups, or a benzyloxy group ( A C 1-4 alkylcarbonyloxy or C 1-2 alkylenedioxy substituted benzene ring; Y is -N = CR- or -CR = N-, wherein R is -NR1R2 or -OR3, wherein R1 is hydrogen, C1-6 alkyl or phenyl, optionally amino, di (1) C 1-6 alkyl monosubstituted with C 1-4 alkylamino or C 1-4 alkylamino, or di (C 1-4 alkyl) azinoyl, hydroxyl, hydroxy (C 1-4) alkyl) amino, [di (C 1-4 alkyl) amino- (C 1-4 alkyl) (C 1-2 alkyl) amino, pyrrolidinyl, pyridinyl, piperidinyl, morpholinyl or (benzyl) -oxy) carbonylamino, monosubstituted C 1-6 alkyl, R 2 is hydrogen or C 1-4 alkyl, or R 1 and R 2 together with the intervening nitrogen atom are (C 1-4 alkyl) piperazinyl, pyrrolidinyl or 1, 2,4-triazolyl, where R3 is di (C1-C4) alkylamino a mono-substituted C 1-4 alkyl group, provided that when R is a nitrogen-containing heterocyclic group as defined above, Ring A and Ring B are unsubstituted benzene rings. The invention also provides pharmaceutically acceptable salts of the compounds. The compounds of the invention are used as antitumor drugs. ŕ
机译:本发明涉及由通式(1)表示的茚并[2,1-c]喹啉酮和茚并[2,1-b]异喹啉酮衍生物,其中A任选被至多两个羟基或卤素原子取代,或烷氧基或C 1-4烷氧基。 -C2-C2亚烷基二氧基取代的苯或萘环; B任选地为卤素,至多两个羟基,硝基,氨基,C 1-4烷基,C 1-4烷氧基或C 1-4烷基羰基氨基或苄氧基(被AC 1-4烷基羰氧基或C 1-2亚烷基二氧基取代)苯环; Y为-N = CR-或-CR = N-,其中R为-NR1R2或-OR3,其中R1为氢,C1-6烷基或苯基,任选为氨基,二(1)C 1-6烷基用C 1-4烷基氨基或C 1-4烷基氨基或二(C 1-4烷基)叠氮酰基,羟基,羟基(C 1-4烷基)烷基)氨基,[二(C 1-4烷基)氨基-( C 1-4烷基)(C 1-2烷基)氨基,吡咯烷基,吡啶基,哌啶基,吗啉基或(苄基-氧基)羰基氨基,单取代的C 1-6烷基,R 2是氢或C 1-4烷基,或R 1和R 2与插入的氮原子一起是(C 1-4烷基)哌嗪基,吡咯烷基或1,2,4-三唑基,其中R3是二(C1-C4)烷基氨基单取代的C 1-4烷基前提是当R是如上定义的含氮杂环基时,环A和环B是未被取代的ted苯环。本发明还提供了化合物的药学上可接受的盐。本发明的化合物用作抗肿瘤药。 ŕ

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