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1. 发明申请

WO2007057775A1 SPIROPIPERIDINE DERIVATIVES 审中-公开
标题翻译：螺吡啶衍生物
公开(公告)号：WO2007057775A1
公开(公告)日：2007-05-24
申请号：PCT/IB2006/003320
申请日：2006-11-16
申请人： PFIZER LIMITED , ALLERTON, Charlotte, Moira, Norfor , OWEN, Dafydd, Rhys , RYCKMANS, Thomas , STAMMEN, Blanda, Luzia, Christa
发明人： ALLERTON, Charlotte, Moira, Norfor , OWEN, Dafydd, Rhys , RYCKMANS, Thomas , STAMMEN, Blanda, Luzia, Christa
IPC分类号： C07D401/04 , C07D491/10 , C07D401/10 , C07D471/10 , C07D519/00 , C07D413/04 , A61K31/4747 , A61P25/04
CPC分类号： C07D401/04 , C07D401/10 , C07D413/04 , C07D471/10 , C07D491/10
摘要： The invention provides compounds of formula (I): wherein the dotted line represents an optional covalent bond between X and Y, and X, Y, Z, m, R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , a and b have the meanings given in the specification, and pharmaceutically acceptable salts and solvates thereof. The compounds are delta opioid receptor agonists and have a number of therapeutic applications, particularly in the treatment of pain.
摘要翻译：本发明提供式（I）的化合物：其中虚线表示X和Y之间任选的共价键，X，Y，Z，m，R 2，R 3， R 4，R 4，R 5，R 6，R 7，R 8， a，b和b具有说明书中给出的含义及其药学上可接受的盐和溶剂化物。这些化合物是δ阿片样物质受体激动剂，并且具有许多治疗应用，特别是治疗疼痛。

2. 发明申请

WO2002074312A1 PYRAZOLO`4,3-D.PYRIMIDINONE COMPOUNDS AS CGMP PDE INHIBITORS 审中-公开
标题翻译： PYRAZOLO`4,3-D.PYRIMIDINONE化合物作为CGMP PDE抑制剂
公开(公告)号：WO2002074312A1
公开(公告)日：2002-09-26
申请号：PCT/IB2002/000679
申请日：2002-03-07
申请人： PFIZER LIMITED , PFIZER INC. , ALLERTON, Charlotte, Moira, Norfor , BARBER, Christopher, Gordon , KEMP, Mark, Ian
发明人： ALLERTON, Charlotte, Moira, Norfor , BARBER, Christopher, Gordon , KEMP, Mark, Ian
IPC分类号： A61K31/505
CPC分类号： C07D487/04
摘要： Compounds of general formula (I), or pharmaceutically or veterinarily acceptable salts, solvates, polymorphs or pro-drugs thereof wherein: wherein R 1 , R 2 , R 3 , R 4 , X and A have the meanings given herein 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：通式（I）的化合物或其药学上或兽医学上可接受的盐，溶剂合物，多晶型物或其前体药物，其中：其中R 1，R 2，R 3，R 4，X和A具有可用于治疗性和预防性治疗期望抑制环鸟嘌呤3'，5'-单磷酸磷酸二酯酶（例如cGMP PDE5）的医学病症的含义。

3. 发明申请

WO2006134487A1 3-PHENYLAZETIDINE DERIVATIVES AS DOPAMINE AGONISTS 审中-公开
标题翻译： 3-苯丙氨酸衍生物作为多巴胺激动剂
公开(公告)号：WO2006134487A1
公开(公告)日：2006-12-21
申请号：PCT/IB2006/001647
申请日：2006-06-07
申请人： PFIZER LIMITED , ALLERTON, Charlotte, Moira, Norfor
发明人： ALLERTON, Charlotte, Moira, Norfor
IPC分类号： C07D305/06 , A61K31/395 , A61P15/00 , A61P25/00
CPC分类号： C07D305/06
摘要： The present invention provides for compounds of formula (I) as defined herein. These compounds are a class of dopamine agonists, more particularly a class of agonists that are selective for D3 over D2. The compounds are useful for the treatment and/or prevention of sexual dysfunction, for example female sexual dysfunction (FSD), in particular female sexual arousal disorder (FSAD), hypoactive sexual desire disorder (HSDD; lack of interest in sex), female orgasmic disorder (FOD; inability to achieve orgasm); and male sexual dysfunction, in particular male erectile dysfunction (MED). Male sexual dysfunction as referred to herein is meant to include ejaculatory disorders such as premature ejaculation, anorgasmia (inability to achieve orgasm) or desire disorders such as hypoactive sexual desire disorder (HSDD; lack of interest in sex). These compounds are also useful in treating neuropsychiatric disorders and neurodegenerative disorders.
摘要翻译：本发明提供如本文定义的式（I）化合物。这些化合物是一类多巴胺激动剂，更特别的是一类在D2上对D3有选择性的激动剂。这些化合物可用于治疗和/或预防性功能障碍，例如女性性功能障碍（FSD），特别是女性性唤起障碍（FSAD），性欲低下症（HSDD;对性不感兴趣），女性高潮无效（FOD;无法达到性高潮）; 男性性功能障碍，特别是男性勃起功能障碍（MED）。本文所提及的男性性功能障碍意在包括射精性疾病，例如早泄，无汗（无法达到性高潮）或期望障碍，如性欲低下症（HSDD;对性不感兴趣）。这些化合物也可用于治疗神经精神障碍和神经变性疾病。

4. 发明申请

WO2005115985A1 AMINOPYRIDINE DERIVATIVES AS SELECTIVE DOPAMINE D3 AGONISTS 审中-公开
标题翻译：氨基吡啶衍生物作为选择性多巴胺D3激动剂
公开(公告)号：WO2005115985A1
公开(公告)日：2005-12-08
申请号：PCT/IB2005/001554
申请日：2005-05-17
申请人： PFIZER LIMITED , PFIZER INC. , ALLERTON, Charlotte, Moira, Norfor , COOK, Andrew, Simon , HEPWORTH, David , MILLER, Duncan, Charles
发明人： ALLERTON, Charlotte, Moira, Norfor , COOK, Andrew, Simon , HEPWORTH, David , MILLER, Duncan, Charles
IPC分类号： C07D213/73
CPC分类号： C07D213/73 , C07D401/04 , C07D413/04 , C07D417/04
摘要： The present invention provides for compounds of formula (I) which are a class of dopamine agonists, more particularly a class of agonists that are selective for D3 over D2. These compounds are useful for the treatment and/or prevention of sexual dysfunction, for example female sexual dysfunction (FSD), in particular female sexual arousal disorder (FSAD), hypoactive sexual desire disorder (HSDD; lack of interest in sex), female orgasmic disorder (FOD; inability to achieve orgasm); and male sexual dysfunction, in particular male erectile dysfunction (MED). Male sexual dysfunction as referred to herein is meant to include ejaculatory disorders such as premature ejaculation, anorgasmia (inability to achieve orgasm) or desire disorders such as hypoactive sexual desire disorder (HSDD; lack of interest in sex). These compounds are also useful in treating neuropsychiatric disorders and neurodegenerative disorders.
摘要翻译：本发明提供了作为一类多巴胺激动剂的式（I）化合物，更具体地，一类在D3上对D2有选择性的一类激动剂。这些化合物可用于治疗和/或预防性功能障碍，例如女性性功能障碍（FSD），特别是女性性唤醒障碍（FSAD），性欲低下症（HSDD;对性不感兴趣），女性高潮无效（FOD;无法达到性高潮）; 男性性功能障碍，特别是男性勃起功能障碍（MED）。本文所提及的男性性功能障碍意在包括射精性疾病，例如早泄，无汗（无法达到性高潮）或期望障碍，如性欲低下症（HSDD;对性不感兴趣）。这些化合物也可用于治疗神经精神障碍和神经变性疾病。

5. 发明申请

WO2002072586A1 PYRAZOLO'4,3-D-PYRIMIDINE FOR INHIBITING CGMP PDE 审中-公开
标题翻译： PYRAZOLO'4,3-D-PYRIMIDINE抑制CGMP PDE
公开(公告)号：WO2002072586A1
公开(公告)日：2002-09-19
申请号：PCT/IB2002/000622
申请日：2002-02-27
申请人： PFIZER LIMITED , PFIZER INC. , ALLERTON, Charlotte, Moira, Norfor
发明人： ALLERTON, Charlotte, Moira, Norfor
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： There is provided a general formula (I) or a pharmaceutically or veterinarily acceptable salt or polymorph and/or solvate thereof, wherein R 1 represents H; C(O)C 1 -C 4 alkyl; C(O) aryl; C(O)heteroaryl. And which is useful in the curative and prophylactic treatment of a medical condition for which inhibition of a cyclic guanosine 3',5'-monophosphate phosphodiesterase (and in particular cGMP PDE5) is desired.
摘要翻译：提供通式（I）或其药学上或兽医学上可接受的盐或多晶型物和/或其溶剂合物，其中R 1表示H; C（O）C 1 -C 4烷基; C（O）芳基; C（O）杂芳基。可用于治疗性和预防性治疗期望抑制环鸟嘌呤3'，5'-单磷酸磷酸二酯酶（特别是cGMP PDE5）的医疗条件。

6. 发明申请

WO2005116027A2 NEW INDAZOLE AND INDOLONE DERIVATIVES AND THEIR USE AS PHARMACEUTICALS 审中-公开
标题翻译：新的吲哚酚和吲哚酚衍生物及其作为药物的用途
公开(公告)号：WO2005116027A2
公开(公告)日：2005-12-08
申请号：PCT/IB2005/001513
申请日：2005-05-17
申请人： PFIZER LIMTED , PFIZER, INC. , ALLERTON, Charlotte, Moira, Norfor , HEPWORTH, David , MILLER, Duncan, Charles
发明人： ALLERTON, Charlotte, Moira, Norfor , HEPWORTH, David , MILLER, Duncan, Charles
IPC分类号： C07D471/04
CPC分类号： C07D401/04 , C07D413/04
摘要： The present invention provides for compounds of formula (I), which are a class of dopamine agonists, more particularly a class of agonists that are selective for D3 over D2. These compounds are useful for the treatment and/or prevention of sexual dysfunction, for example female sexual dysfunction (FSD), in particular female sexual arousal disorder (FSAD), hypoactive sexual desire disorder (HSDD; lack of interest in sex), female orgasmic disorder (FOD; inability to achieve orgasm); and male sexual dysfunction, in particular male erectile dysfunction (MED). Male sexual dysfunction as referred to herein is meant to include ejaculatory disorders such as premature ejaculation, anorgasmia (inability to achieve orgasm) or desire disorders such as hypoactive sexual desire disorder (HSDD; lack of interest in sex). These compounds are also useful in treating neuropsychiatric disorders and neurodegenerative disorders.
摘要翻译：本发明提供式（I）化合物，其是一类多巴胺激动剂，更具体地，一类在D3上对D2具有选择性的激动剂。这些化合物可用于治疗和/或预防性功能障碍，例如女性性功能障碍（FSD），特别是女性性唤醒障碍（FSAD），性欲低下症（HSDD;对性不感兴趣），女性高潮无效（FOD;无法达到性高潮）; 男性性功能障碍，特别是男性勃起功能障碍（MED）。本文所提及的男性性功能障碍意在包括射精性疾病，例如早泄，无汗（无法达到性高潮）或期望障碍，如性欲低下症（HSDD;对性不感兴趣）。这些化合物也可用于治疗神经精神障碍和神经变性疾病。

7. 发明申请

WO2003061653A1 3-(IMIDAZOLYL)-2-AMINOPROPANOIC ACIDS FOR USE AS TAFI-A INHIBITORS FOR THE TREATMENT OF THROMBOTIC DISEASES 审中-公开
标题翻译： 3-（咪唑烷基）-2-氨基壬酸用于治疗感染性疾病的TAFI-A抑制剂
公开(公告)号：WO2003061653A1
公开(公告)日：2003-07-31
申请号：PCT/IB2003/000058
申请日：2003-01-13
申请人： PFIZER LIMITED , PFIZER INC. , ALLERTON, Charlotte, Moira, Norfor , BUNNAGE, Mark, Edward , STEELE, John
发明人： ALLERTON, Charlotte, Moira, Norfor , BUNNAGE, Mark, Edward , STEELE, John
IPC分类号： A61K31/4178
CPC分类号： C07D401/06 , C07D403/06
摘要： Compounds according to formula (I) wherein n is 1-4, R 1 is optionally substituted C 1-6 alkyl, C 2-6 alkenyl, or C 2-6 alkynyl, Heterocycle, Aromatic heterocycle, Aryl or hydrogen and R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and R8 are each independently selected from hydrogen and optionally substituted C 1-6 alkyl are novel. They are useful in the treatment of thrombotic conditions and other pathologies associated with fibrin deposition. (1).
摘要翻译：根据式（I）的化合物，其中n为1-4，R 1为任选取代的C 1-6烷基，C 2-6烷基，烯基或C 2-6烯基炔基，杂环，芳族杂环，芳基或氢和R 2，R 3，R 4， R 6，R 6，R 7和R 8各自独立地选自氢和任选取代的C 1〜 -6-C烷基是新的。它们可用于治疗与血纤维蛋白沉积相关的血栓形成状况和其他病理。（1）。

8. 发明申请

WO2003061652A1 3-(IMIDAZOLYL)-2-ALKOXYPROPANOIC ACIDS AS TAFIA INHIBITORS 审中-公开
标题翻译： 3-（咪唑烷基）-2-烷氧基丙酸作为TAFIA抑制剂
公开(公告)号：WO2003061652A1
公开(公告)日：2003-07-31
申请号：PCT/IB2003/000060
申请日：2003-01-10
申请人： PFIZER LIMITED , PFIZER INC. , ALLERTON, Charlotte, Moira, Norfor , BULL, David, John , BUNNAGE, Mark, Edward , MAGUIRE, Robert, John , STEELE, John
发明人： ALLERTON, Charlotte, Moira, Norfor , BULL, David, John , BUNNAGE, Mark, Edward , MAGUIRE, Robert, John , STEELE, John
IPC分类号： A61K31/4172
CPC分类号： C07D233/64 , C07D401/04 , C07D403/12
摘要： Compounds according to formula (I) wherein n is 0-3, R 1 is optionally substituted C 1-6 alkyl, C 2-6 alkenyl, or C 2-6 alkynyl, Heterocycle, Aromatic heterocycle, Aryl or hydrogen and R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 and R 9 are each independently selected from hydrogen and optionally substituted C 1-6 alkyl, or R 5 and R 8 are an alkylene chain, are novel. They are useful in the treatment of thrombotic conditions and other pathologies associated with fibrin deposition.
摘要翻译：根据式（I）的化合物，其中n为0-3，R 1为任选取代的C 1-6烷基，C 2-6烷基，烯基或C 2-6烯基炔基，杂环，芳族杂环，芳基或氢和R 2，R 3，R 4，，R 5，R 6，R 7，R 8和R 9，各自独立地选自氢和任选取代的C 1-6烷基，或者R 5和R 8是亚烷基链，是小说。它们可用于治疗与血纤维蛋白沉积相关的血栓形成状况和其他病理。

9. 发明申请

WO2002079203A1 PHARMACEUTICALLY ACTIVE COMPOUNDS 审中-公开
标题翻译：药物活性化合物
公开(公告)号：WO2002079203A1
公开(公告)日：2002-10-10
申请号：PCT/IB2002/000854
申请日：2002-03-19
申请人： PFIZER LIMITED , PFIZER INC. , ALLERTON, Charlotte, Moira, Norfor , DACK, Kevin, Neil , KEMP, Mark, Ian
发明人： ALLERTON, Charlotte, Moira, Norfor , DACK, Kevin, Neil , KEMP, Mark, Ian
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： Compounds of general formula (1): wherein R 1 , R 2 , R 3 , R 4 , X, Y and A have the meanings given herein 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：通式（1）的化合物：其中R 1，R 2，R 3，R 4，R 5，R 5， X，Y和A具有本文给出的含义，其可用于治疗性和预防性治疗抑制环鸟苷3'，5'-单磷酸磷酸二酯酶（例如cGMP PDE5）的医学病症，是期望的。

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