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公开(公告)号：US07176311B2
公开(公告)日：2007-02-13
申请号：US10753199
申请日：2004-01-06
申请人： Mark Edward Bunnage , Keith Michael DeVries , Laurence James Harris , Philip Charles Levett , John Paul Mathias , Joanna Teresa Negri , Stephen Derek Albert Street , Albert Shaw Wood
发明人： Mark Edward Bunnage , Keith Michael DeVries , Laurence James Harris , Philip Charles Levett , John Paul Mathias , Joanna Teresa Negri , Stephen Derek Albert Street , Albert Shaw Wood
IPC分类号： C07D487/04 , C07D401/12
CPC分类号： C07D213/80 , A61K31/519 , C07D231/38 , C07D401/12 , C07D487/04
摘要： A process for the preparation of Compounds of the formula (1): wherein R1, R2, R4 and R13 are as defined or a pharmaceutically or veterinarily acceptable salt or polymorph thereof, or a pharmaceutically or veterinarily acceptable solvate or pro-drug thereof: are potent and selective inhibitors of type 5 cyclic guanosine 3′,5′-monophosphate phosphodiestbrase (cGMP PDE5) and have utility in the treatment of, inter alia, male erectile dysfunction (MED) and female sexual dysfunction (FSD).
摘要翻译： 制备式（1）化合物的方法：其中R 1，R 2，R 4和R 13 或其药学上或兽医学上可接受的盐或多晶型物，或其药学上或兽医学上可接受的溶剂合物或前体药物：是5型环鸟苷酸3'，5'-单磷酸磷酸二酯酶的有效和选择性抑制剂 cGMP PDE5），可用于治疗男性勃起功能障碍（MED）和女性性功能障碍（FSD）。
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公开(公告)号：US20100035891A1
公开(公告)日：2010-02-11
申请号：US12469311
申请日：2009-05-20
申请人： Mark Edward Bunnage , Keith Michael DeVries , Laurence James Harris , Philip Charles Levett , John Paul Mathias , Joanna Teresa Negri , Stephen Derek Albert Street , Albert Shaw Wood
发明人： Mark Edward Bunnage , Keith Michael DeVries , Laurence James Harris , Philip Charles Levett , John Paul Mathias , Joanna Teresa Negri , Stephen Derek Albert Street , Albert Shaw Wood
IPC分类号： A61K31/496 , A61K31/519 , A61P13/00
CPC分类号： C07D213/80 , A61K31/519 , C07D231/38 , C07D401/12 , C07D487/04
摘要： Compounds of the formula (I): wherein R1, R2, R4 and R13 are as defined or a pharmaceutically or veterinarily acceptable salt or polymorph thereof, or a pharmaceutically or veterinarily acceptable solvate or pro-drug thereof: 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（I）的化合物：其中R 1，R 2，R 4和R 13如所定义，或其药学上或兽医学上可接受的盐或多晶型物，或其药学上或兽医学上可接受的溶剂化物或前体药物：是有效和选择性的抑制剂 5环鸟苷3'，5'-单磷酸磷酸二酯酶（cGMP PDE5），具有治疗男性勃起功能障碍（MED）和女性性功能障碍（FSD）的效用。
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公开(公告)号：US06677335B1
公开(公告)日：2004-01-13
申请号：US09685080
申请日：2000-10-06
申请人： Mark Edward Bunnage , Keith Michael DeVries , Laurence James Harris , Philip Charles Levett , John Paul Mathias , Joanna Teresa Negri , Stephen Derek Albert Street , Albert Shaw Wood
发明人： Mark Edward Bunnage , Keith Michael DeVries , Laurence James Harris , Philip Charles Levett , John Paul Mathias , Joanna Teresa Negri , Stephen Derek Albert Street , Albert Shaw Wood
IPC分类号： C07D48704
CPC分类号： C07D213/80 , A61K31/519 , C07D231/38 , C07D401/12 , C07D487/04
摘要： Compounds of the formula (I): wherein R1, R2, R4 and R13 are as defined or a pharmaceutically or veterinarily acceptable salt or polymorph thereof, or a pharmaceutically or veterinarily acceptable solvate or pro-drug thereof: 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（I）的化合物：其中R 1，R 2，R 4和R 13如所定义，或其药学上或兽医学上可接受的盐或多晶型物，或药学上或兽医学上可接受的溶剂合物或 其前药：是5型环鸟苷酸3'，5'-单磷酸磷酸二酯酶（cGMP PDE5）的有效和选择性抑制剂，可用于治疗男性勃起功能障碍（MED）和女性性功能障碍（FSD） ）。
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![Process for the preparation of pyrazolo[4,3-d]pyrimidin-7-one compounds and intermediates thereof](/abs-image/US/2004/10/26/US06809200B2/abs.jpg.150x150.jpg)
4.发明授权Process for the preparation of pyrazolo[4,3-d]pyrimidin-7-one compounds and intermediates thereof 失效吡唑并[4,3-d]嘧啶-7-酮化合物及其中间体的制备方法公开(公告)号：US06809200B2
公开(公告)日：2004-10-26
申请号：US09916099
申请日：2001-07-26
申请人： Charlotte Moira Norfor Allerton , Christopher Gordon Barber , Keith Michael DeVries , Laurence James Harris , Philip Charles Levett , Joanna Teresa Negri , David James Rawson , Albert Shaw Wood
发明人： Charlotte Moira Norfor Allerton , Christopher Gordon Barber , Keith Michael DeVries , Laurence James Harris , Philip Charles Levett , Joanna Teresa Negri , David James Rawson , Albert Shaw Wood
IPC分类号： C07D48704
CPC分类号： C07D487/04
摘要： A process is provide for the preparation of compounds of formula (I) herein comprising reacting a compound of formula (III), (IV) or (V) wherein the variables are as defined in the specification. The reaction is conducted in the presence of −OR3 and a hydroxide trapping agent or in the case of compounds of formula (IV) reacting in the presence of an auxiliary base and a hydroxide trapping agent.
摘要翻译： 一种制备式（I）化合物的方法，其包括使式（III），（IV）或（V）化合物与变量如说明书中所定义的反应。 反应在< - > OR 3和氢氧化物捕获剂的存在下进行，或在式（Ⅳ）化合物的情况下，在辅助碱和氢氧化物捕获剂的存在下反应。
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公开(公告)号：US06420557B1
公开(公告)日：2002-07-16
申请号：US09915705
申请日：2001-07-26
IPC分类号： C07D48704
CPC分类号： C07D213/80 , A61K31/519 , C07D231/38 , C07D401/12 , C07D487/04
摘要： A polymorph of 1-{6-ethoxy-5-[3-ethyl-6,7-dihydro-2-(2-methoxyethyl)-7-oxo-2H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-pyridylsulfonyl}-4-ethylpiperazine.
摘要翻译： 1- {6-乙氧基-5- [3-乙基-6,7-二氢-2-（2-甲氧基乙基）-7-氧代-2H-吡唑并[4,3-d]嘧啶-5-基的多晶型物 -3-吡啶基磺酰基} -4-乙基哌嗪。
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公开(公告)号：US6066735A
公开(公告)日：2000-05-23
申请号：US360128
申请日：1999-07-23
申请人： Peter James Dunn , Albert Shaw Wood
发明人： Peter James Dunn , Albert Shaw Wood
IPC分类号： C07D295/22 , A61K31/00 , A61K31/505 , A61K31/519 , A61K31/635 , A61P13/02 , A61P15/00 , A61P15/10 , C07B61/00 , C07D20060101 , C07D231/14 , C07D231/40 , C07D295/26 , C07D403/12 , C07D487/04
CPC分类号： C07D295/26 , C07D231/14 , C07D487/04
摘要： A process for the preparation of a compound of formula (I): ##STR1## which comprises cyclization of a compound of formula (II): ##STR2##
摘要翻译： 一种制备式（I）化合物的方法：其包括式（II）化合物的环化：
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公开(公告)号：US5955611A
公开(公告)日：1999-09-21
申请号：US869532
申请日：1997-06-06
申请人： Peter James Dunn , Albert Shaw Wood
发明人： Peter James Dunn , Albert Shaw Wood
IPC分类号： C07D295/22 , A61K31/00 , A61K31/505 , A61K31/519 , A61K31/635 , A61P13/02 , A61P15/00 , A61P15/10 , C07B61/00 , C07D20060101 , C07D231/14 , C07D231/40 , C07D295/26 , C07D403/12 , C07D487/04 , C07D247/02 , C07D247/00
CPC分类号： C07D295/26 , C07D231/14 , C07D487/04
摘要： A process for the preparation of a compound of formula (I): ##STR1## which comprises cyclization of a compound of formula (II): ##STR2##
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