首页> 外国专利> 1, 6-DISUBSTITUTED-1H- PYRAZOLO 3, 4-d - PYRIMIDIN-4 (5H) - ONE DERIVATIVES, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

1, 6-DISUBSTITUTED-1H- PYRAZOLO 3, 4-d - PYRIMIDIN-4 (5H) - ONE DERIVATIVES, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

机译:1,6-二取代-1H-吡唑并[3,4-d]-吡唑啉-4(5H)-一种衍生物,它们的制备和组成它们的药物成分

摘要

1, 5-Dihydro-pyrazolo [3, 4-d] pyridimidinone derivatives of the formula in which A and D together represent a radical of the formula 3425 ט" ז בשבט התשס" ד - February 8, 2004 where R2 represents aryl which has 6 to 10 carbon atoms and which is optionally up to trisubstituted by identical or different substituents from the series consisting of nitro, cyano, hydroxyl, trifluoromethyl, halogen, carboxyl, or by straight-chain or branched acyl, alkoxy or alkoxycarbonyl, each of which has up to 6 carbon atoms or hydrogen, trifluoromethyl, cyano, carboxyl, or straight-chain or branched alkoxy or alkoxycarbonyl, each of which has up to 8 carbon atoms, or straight-chain or branched alkyl which has up to 8 carbon atoms and which is optionally substituted by hydroxyl, R1 represents straight-chain or branched acyl having up to 4 carbon atoms, or represents straight-chain or branched alkyl having up to 10 carbon atoms, optionally subsituted by hydroxyl, azido or by a group of the formula -NR3R4 or -OSO2R5 where R3 and R4 are identical or different and represent hydrogen or straight-chain or branched alkyl having up to 6 carbon atoms, or R3 and R4 together with the nitrogen atom form a 5 or 6-membered saturated heterocycle which can optionally contain a further hetero atom selected from the series consisting of S or O or a radical -NR6 where R6 represents hydrogen or straight-chain or branched alkyl having up to 4 carbon atoms and R5 represents phenyl or straight-chain or branched alkyl having up to 5 carbon atoms, E represents a straight-chain or branched alkylene or alkenylene chain, each of which has up to 6 carbon atoms which are optionally substituted by hydroxyl, or represents the C=O group, L and V are identical or different and represent aryl having 6 to 10 carbon atoms or a 5- to 7-membered aromatic, optionally benzo-fused, heterocycle which has up to 3 hetero atoms from the series consisting of S, N and/or O which are optionally up to trisubstituted by identical or different substituents from the series consisting of halogen, hydroxyl, nitro, trifluoromethyl, carboxyl, straight-chain or branched alkyl, alkoxy or alkoxycarbonyl, each of which has up to 6 carbon atoms, or by a group of the formula- (W)a-NR7R8 where a and b are 0 or 1, W is a radical of the formula -CO or -SO2, R7 and R8 are identical or different and have the abovementioned meaning of R3 and R4, and/or the cycles are optionally substituted by aryl having 6 to 10 carbon atoms or by a 5-to 7-membered aromatic, optionally benzo-fused, heterocycle having up to 3 betero atoms from the series consisting of S, N and/or O, which, in turn, are optionally up to disubstituted by identical or different substituents from the series consisting of halogen, hydroxyl, nitro, carboxyl, trifluoromethyl or by straight- chain or branched alkyl, alkoxy or alkoxycarbonyl, each of which has up to 5 cabron atoms, or by a group of the formula -(W')b-NR9R10 where b has the abovementioned meaning of a and is identical to this meaning or different from it, R9 and R10 have the abovementioned meaning of R3 and R4 and are identical to this meaning or different from it, W' has the abovementioned meaning of W and is identical to this meaning or different from it, or L represents a radical of the formula 3426 ט" ז בשבט התשס" ד - February 8, 2004 T represents a radical of the formula -CH2-X-Y- where X represents a bond or an oxygen or sulphur atom or the -NH-group, Y represents a straight-chain or branched alkylene chain having up to 9 carbon atoms, and the tautomers and salts of these.
机译:具有下式的式1的5-二氢-吡唑并[3,4-d]嘧啶酮衍生物:其中A和D共同表示式3425的基团-2004年2月8日,其中R 2表示具有6到10个碳原子,并可选地最多被硝基,氰基,羟基,三氟甲基,卤素,羧基组成的系列中相同或不同的取代基取代,或被直链或支链的酰基,烷氧基或烷氧基羰基最多取代3个,具有最多6个碳原子或氢,三氟甲基,氰基,羧基或直链或支链的烷氧基或烷氧基羰基,每个直链或支链的烷基最多具有8个碳原子,或者具有直链或支链的烷基最多具有8个碳原子,并且(其任选地被羟基取代),R1代表具有至多4个碳原子的直链或支链的酰基,或代表具有至多10个碳原子的直链或支链的烷基,其任选地被羟基,叠氮基或由gro取代式-NR3R4或-OSO2R5的化学式,其中R3和R4相同或不同,表示氢或具有至多6个碳原子的直链或支链烷基,或R3和R4与氮原子一起形成5元或6元饱和杂环,可以任选地包含选自S或O或基团-NR6的其他杂原子,其中R6代表氢或碳原子数不超过4的直链或支链烷基,R5代表苯基或直链或具有最多5个碳原子的支链烷基,E表示直链或支链的亚烷基或亚烯基链,每个直链或支链的亚烷基或亚烯基链具有至多6个碳原子,可任选被羟基取代,或表示C = O,L和V为相同或不同,表示具有6至10个碳原子的芳基或5至7元芳族,视情况为苯并稠合的杂环,该环中最多具有3个由S,N和/或O组成的杂原子直到trisu由卤素,羟基,硝基,三氟甲基,羧基,直链或支链的烷基,烷氧基或烷氧基羰基组成的系列中相同或不同的取代基取代,或各自具有至多6个碳原子,或由下式组成的基团(W)a-NR7R8,其中a和b为0或1,W为式-CO或-SO2的基团,R7和R8相同或不同,具有R3和R4的上述含义,和/或环任选地被具有6至10个碳原子的芳基或由至多3个由S,N和/或O组成的杂原子的5至7元芳族,任选地苯并稠合的杂环所取代,其中依次被卤素,羟基,硝基,羧基,三氟甲基组成的系列中的相同或不同的取代基最多二取代,或被直链或支链烷基,烷氧基或烷氧基羰基最多取代两个,每个直链或支链烷基具有多达5个碳原子,或由一组式-(W')b-NR9R10组成,其中b具有上述形式a的同义含义与该含义相同或不同,R9和R10具有R3和R4的上述含义,且与该含义相同或不同,W'具有W的上述含义且与此相同L表示通式3426的基团-2004年2月8日T表示通式-CH2-XY-的基团,其中X表示键或氧或硫原子或-NH-基团,Y表示具有至多9个碳原子的直链或支链亚烷基链,以及它们的互变异构体和盐。

著录项

  • 公开/公告号IL131450B

    专利类型

  • 公开/公告日2004-02-08

    原文格式PDF

  • 申请/专利权人 BAYER AKTIENGESELLSCHAFT;

    申请/专利号IL131450

  • 发明设计人

    申请日1999-08-18

  • 分类号

  • 国家 IL

  • 入库时间 2022-08-21 23:10:41

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