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Pyrazolopyrimidinones which inhibit type 5 cyclic guanosine 3',5'-monophosphate phosphodiesterase (cGMP PDE5) for the treatment of sexual dysfunction

机译:抑制5型环鸟苷3',5'-单磷酸磷酸二酯酶(cGMP PDE5)的吡唑并嘧啶酮治疗性功能障碍

摘要

Compounds of formulae (IA) and (IB) or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein R1 is C1 to C3 alkyl substituted with C3 to C6 cycloalkyl, CONR5R6 or a N-linked heterocyclic group; (CH¿2?)nHet or (CH2)nAr; R?2 is C¿1 to C6 alkyl; R3 is C1 to C6 alkyl optionally substituted with C1 to C4 alkoxy; R4 is SO¿2?NR?7R8; R5 and R6¿ are each independently selected from H and C¿1? to C4 alkyl optionally substituted with C1 to C4 alkoxy, or, together with the nitrogen atom to which they are attached, form a 5- or 6-membered heterocyclic group; R?7 and R8¿, together with the nitrogen atom to which they are attached, form a 4-R10-piperazinyl group; R10 is H or C¿1? to C4 alkyl optionally substituted with OH, C1 to C4 alkoxy or CONH2; Het is an optionally substituted C-linked 5- or 6-membered heterocyclic group; Ar is optionally substituted phenyl; and n is 0 or 1; are potent and selective cGMP PDE5 inhibitors useful in the treatment of, inter alia, male erectile dysfunction and female sexual dysfunction.
机译:式(IA)和(IB)的化合物或其药学上或兽医学上可接受的盐,或任一实体的药学上或兽医学上可接受的溶剂化物,其中R 1为被C 3至C 6环烷基,CONR 5 R 6或N-连接的杂环基取代的C 1至C 3烷基; (CH 2?)nHet或(CH2)nAr; R 2是C 1至C 6烷基。 R3是任选地被C1-C4烷氧基取代的C1-C6烷基; R4是SO¿2?NR?7R8; R5和R6¿各自独立地选自H和C?1? -任选地被C1-C4烷氧基取代的C4烷基,或与它们所连接的氮原子一起形成5或6元杂环基; R 7和R 8与它们所连接的氮原子一起形成一个4-R 10哌嗪基; R10是H还是C?1? -任选地被OH,C1-C4烷氧基或CONH2取代的C4烷基; Het是任选取代的C-连接的5-或6-元杂环基; Ar是任选取代的苯基; n为0或1;是有效的选择性cGMP PDE5抑制剂,可用于治疗男性勃起功能障碍和女性性功能障碍。

著录项

  • 公开/公告号IL165411D0

    专利类型

  • 公开/公告日2006-01-15

    原文格式PDF

  • 申请/专利权人 PFIZER INC.;

    申请/专利号IL20040165411

  • 发明设计人

    申请日2004-11-25

  • 分类号7C07DA;

  • 国家 IL

  • 入库时间 2022-08-21 21:39:14

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