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    Pyrazolopyrimidinone cGMP PDE5 inhibitors for the treatment of sexual dysfunction
    5.
    发明授权
    Pyrazolopyrimidinone cGMP PDE5 inhibitors for the treatment of sexual dysfunction 失效
    吡唑并嘧啶酮cGMP PDE5抑制剂治疗性功能障碍

    公开(公告)号：US06251904B1

    公开(公告)日：2001-06-26

    申请号：US09402242

    申请日：1999-09-29

    申请人： Mark Edward Bunnage ,  John Paul Mathias ,  Stephen Derek Albert Street ,  Anthony Wood

    发明人： Mark Edward Bunnage ,  John Paul Mathias ,  Stephen Derek Albert Street ,  Anthony Wood

    IPC分类号： C07D48704

    CPC分类号： C07D213/80 ,  C07D401/12 ,  C07D405/12 ,  C07D487/04

    摘要： Compounds of the formulae (IA) and (IB): wherein R1 is C1 to C3 alkyl optionally substituted with phenyl, Het or a N-linked heterocyclic group selected from piperidinyl and morpholinyl; wherein said phenyl group is optionally substituted by one or more substitutents selected from C1 to C4 alkoxy; halo; CN; CF3; OCF3 or C1 to C4 alkyl wherein said C1 to C4 alkyl group is optionally substituted by C1 to C4 haloalkyl or haloalkoxy either of which is substituted by one or more halo atoms; R2 is C1 to C6 alkyl and R13 is OR3 or NR5R6, or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity are potent and selective inhibitors of type 5 cyclic guanosine 3′,5′-monophosphate phosphodiesterase (cGMP PDE5) and have utility in the treatment of, inter alia, male erectile dysfunction (MED) and female sexual dysfunction (FSD).

    摘要翻译： 式（IA）和（IB）的化合物：其中R 1为任选被苯基，Het或选自哌啶基和吗啉基的N-连接的杂环基取代的C 1至C 3烷基; 其中所述苯基任选被一个或多个选自C 1至C 4烷氧基的取代基取代; 光环; CN; CF3; OCF 3或C 1至C 4烷基，其中所述C 1至C 4烷基任选被被一个或多个卤素原子取代的C 1至C 4卤代烷基或卤代烷氧基取代; R2是C1至C6烷基，R13是OR3或NR5R6，或其药学或兽医学上可接受的盐，或任何一个实体的药学上或兽医学上可接受的溶剂合物是5型环鸟嘌呤3'，5'-单磷酸磷酸二酯酶（cGMP）的有效和选择性抑制剂 PDE5），并且可用于治疗男性勃起功能障碍（MED）和女性性功能障碍（FSD）。

    Pyrazolopyrimidinones which inhibit type 5 cyclic guanosine 3′,5′—monophosphate phosphodiesterase (cGMP PDE5) for the treatment of sexual dysfunction
    6.
    发明授权
    Pyrazolopyrimidinones which inhibit type 5 cyclic guanosine 3′,5′—monophosphate phosphodiesterase (cGMP PDE5) for the treatment of sexual dysfunction 失效
    抑制5型环鸟嘌呤3'，5'-单磷酸磷酸二酯酶（cGMP PDE5）治疗性功能障碍的吡唑并嘧啶酮

    公开(公告)号：US06723719B1

    公开(公告)日：2004-04-20

    申请号：US09402229

    申请日：1999-09-29

    申请人： Mark Edward Bunnage ,  John Paul Mathias ,  Stephen Derek Albert Street ,  Anthony Wood

    发明人： Mark Edward Bunnage ,  John Paul Mathias ,  Stephen Derek Albert Street ,  Anthony Wood

    IPC分类号： C07D48704

    CPC分类号： C07D487/04 ,  C07D231/40

    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; (CH2)nHet or (CH2)nAr; R2 is C1 to C6 alkyl; R3 is C1 to C6 alkyl optionally substituted with C1 to C4 alkoxy; R4 is SO2NR7R8; R5 and R6 are each independently selected from H and C1 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; R7 and R8, together with the nitrogen atom to which they are attached, form a 4-R10-piperazinyl group; R10 is H or C1 to C4 alkyl optionally substituted with OH, C1 to C4 alkoxy or CONH2; H 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.

    摘要翻译： 式（IA）和（IB）化合物或其药学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环烷基取代的C 1至C 3烷基，CONR 5 R 6或N-连接的杂环基; （CH2）nHet或（CH2）nAr; R 2是C 1至C 6烷基; R 3是任选被C 1至C 4烷氧基取代的C 1至C 6烷基; R 4是SO 2 NR 7 R 8; R 5和R 6各自独立地选自H和任选被C 1至C 4烷氧基取代的C 1至C 4烷基，或与它们所连接的氮原子一起形成5-或6-元杂环 组; R 7和R 8与它们所连接的氮原子一起形成4-R 10 - 哌嗪基; R 10是H或任选被OH，C 1至C 4烷氧基或CONH 2取代的C 1至C 4烷基; H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; 并且n为0或1; 是用于治疗男性勃起功能障碍和女性性功能障碍的有效和选择性的cGMP PDE5抑制剂。

    Pyrazolopyrimidinone cGMP PDE5 inhibitors for the treatment of sexual dysfunction
    8.
    发明授权
    Pyrazolopyrimidinone cGMP PDE5 inhibitors for the treatment of sexual dysfunction 失效
    吡唑并嘧啶酮cGMP PDE5抑制剂治疗性功能障碍

    公开(公告)号：US06458951B2

    公开(公告)日：2002-10-01

    申请号：US09845420

    申请日：2001-04-30

    申请人： Mark Edward Bunnage ,  John Paul Mathias ,  Stephen Derek Albert Street ,  Anthony Wood

    发明人： Mark Edward Bunnage ,  John Paul Mathias ,  Stephen Derek Albert Street ,  Anthony Wood

    IPC分类号： C07D40112

    CPC分类号： C07D213/80 ,  C07D401/12 ,  C07D405/12 ,  C07D487/04

    摘要： Compounds of the formulae (IA) and (IB): wherein R1 is C1 to C3 alkyl optionally substituted with phenyl, Het or a N-linked heterocyclic group selected from piperidinyl and morpholinyl; wherein said phenyl group is optionally substituted by one or more substitutents selected from C1 to C4 alkoxy; halo; CN; CF3; OCF3 or C1 to C4 alkyl wherein said C1 to C4 alkyl group is optionally substituted by C1 to C4 haloalkyl or haloalkoxy either of which is substituted by one or more halo atoms; R2 is C1 to C6 alkyl and R13 is OR3 or NR5R6, or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity are potent and selective inhibitors of type 5 cyclic guanosine 3′,5′-monophosphate phosphodiesterase (cGMP PDE5) and have utility in the treatment of, inter alia, male erectile dysfunction (MED) and female sexual dysfunction (FSD).

    摘要翻译： 式（IA）和（IB）的化合物：其中R 1为任选被苯基，Het或选自哌啶基和吗啉基的N-连接的杂环基取代的C 1至C 3烷基; 其中所述苯基任选被一个或多个选自C 1至C 4烷氧基的取代基取代; 光环; CN; CF3; OCF 3或C 1至C 4烷基，其中所述C 1至C 4烷基任选被被一个或多个卤素原子取代的C 1至C 4卤代烷基或卤代烷氧基取代; R2是C1至C6烷基，R13是OR3或NR5R6，或其药学或兽医学上可接受的盐，或任何一个实体的药学上或兽医学上可接受的溶剂合物是5型环鸟嘌呤3'，5'-单磷酸磷酸二酯酶（cGMP）的有效和选择性抑制剂 PDE5），并且可用于治疗男性勃起功能障碍（MED）和女性性功能障碍（FSD）。