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1. 发明授权

US07176311B2 Process for preparing pharmaceutically active compounds 失效
标题翻译：制备药物活性化合物的方法
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）。

2. 发明申请

US20100035891A1 Pharmaceutically Active Compounds 审中-公开
标题翻译：药物活性化合物
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。

3. 发明授权

US06677335B1 Pharmaceutically active compounds 失效
标题翻译：药物活性化合物
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））。

4. 发明授权

US06723719B1 Pyrazolopyrimidinones which inhibit type 5 cyclic guanosine 3′,5′—monophosphate phosphodiesterase (cGMP PDE5) for the treatment of sexual dysfunction 失效
标题翻译：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。

5. 发明授权

US06458951B2 Pyrazolopyrimidinone cGMP PDE5 inhibitors for the treatment of sexual dysfunction 失效
标题翻译：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）。

6. 发明授权

US06916927B2 Pyrazolopyrimidinones which inhibit type 5 cyclic guanosine 3′,5′-monophosphate phosphodiesterase (cGMP-PDE5) for the treatment of sexual dysfunction 失效
公开(公告)号：US06916927B2
公开(公告)日：2005-07-12
申请号：US10808027
申请日：2004-03-23
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： C07D295/22 , A61K20060101 , A61K31/415 , A61K31/505 , A61K31/519 , A61K31/5377 , A61P1/00 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/02 , A61P11/06 , A61P13/08 , A61P13/10 , A61P15/00 , A61P15/10 , A61P27/06 , A61P35/00 , A61P37/08 , A61P43/00 , C07B20060101 , C07D231/40 , C07D401/06 , C07D487/04 , C07D295/26 , C07D231/02
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; 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

7. 发明授权

US06333330B1 Pyrazolopyrimidinone CGMP PDE5 inhibitors for the treatment of sexual dysfunction 失效
标题翻译：吡唑并嘧啶酮CGMP PDE5抑制剂治疗性功能障碍
公开(公告)号：US06333330B1
公开(公告)日：2001-12-25
申请号：US09426554
申请日：1999-10-22
申请人： Mark Edward Bunnage , John Paul Mathias , Graham Nigel Maw , David James Rawson , Stephen Derek Albert Street , Anthony Wood
发明人： Mark Edward Bunnage , John Paul Mathias , Graham Nigel Maw , David James Rawson , Stephen Derek Albert Street , Anthony Wood
IPC分类号： A61K31505
CPC分类号： C07D401/12 , C07D231/14 , C07D487/04
摘要： There is provided compounds of formula IA and of formula IB, wherein R1, R2, R3, R4 and A have meanings given in the description, which are useful in the curative and prophylactic treatment of medical conditions for which inhibition of a cyclic guanosine 3′,5′-monophosphate phosphodiesterase (e.g. cGMP PDE5) is desired.
摘要翻译：提供式IA和式IB的化合物，其中R 1，R 2，R 3，R 4和A具有在描述中给出的含义，其可用于治疗和预防治疗环状鸟苷3' ，需要5'-单磷酸磷酸二酯酶（例如cGMP PDE5）。

8. 发明授权

US06670366B1 Pyrazolopyrimidinone cGMP PDE5 inhibitors for the treatment of sexual dysfunction 失效
标题翻译：吡唑并嘧啶酮cGMP PDE5抑制剂治疗性功能障碍
公开(公告)号：US06670366B1
公开(公告)日：2003-12-30
申请号：US09426552
申请日：1999-10-22
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： C07D401/12 , C07D231/14 , C07D487/04
摘要： There is provided compounds of formula IA and of formula IB, wherein R1, R2, R3, R4 and A have meanings given in the description, which are useful in the curative and prophylactic treatment of a medical condition for which inhibition of a cyclic guanosine 3′,5′-monophosphate phosphodiesterase (e.g. cGMP PDE5) is desired.
摘要翻译：提供式IA和式IB的化合物，其中R 1，R 2，R 3，R 4和A具有在描述中给出的含义，其可用于治疗和预防性治疗需要抑制环鸟苷3'，5'-单磷酸磷酸二酯酶（例如cGMP PDE5）的医学病症。

9. 发明授权

US06407114B1 Pyrazolopyrimidinone CGMP PDE5 inhibitors for the treatment of sexual dysfunction 失效
标题翻译：吡唑并嘧啶酮CGMP PDE5抑制剂治疗性功能障碍
公开(公告)号：US06407114B1
公开(公告)日：2002-06-18
申请号：US09425095
申请日：1999-10-22
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： A61K31517
CPC分类号： C07D487/04
摘要： There is provided compounds of formula IA and of formula IB, wherein R1, R2, R3, R4 and A have meanings given in the description, which are useful in the curative and prophylactic treatment of a medical condition for which inhibition of a cyclic guanosine 3′,5′-monophosphate phosphodiesterase (e.g. cGMP PDE5) is desired.
摘要翻译：提供式IA和式IB的化合物，其中R1，R2，R3，R4和A具有描述中给出的含义，其可用于治疗性和预防性治疗其中抑制环鸟嘌呤3 '，5'-单磷酸磷酸二酯酶（例如cGMP PDE5）。

10. 发明授权

US06251904B1 Pyrazolopyrimidinone cGMP PDE5 inhibitors for the treatment of sexual dysfunction 失效
标题翻译：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）。

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