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1.发明授权公开(公告)号：US07332516B2
公开(公告)日：2008-02-19
申请号：US10540601
申请日：2004-01-09
IPC分类号： A61K21/421 , A61K31/41 , A61K31/403 , A61K31/404 , A61K31/4035 , A61K31/381 , A61K31/38 , A61K31/192
CPC分类号： C07D257/04 , C07C57/30 , C07C57/58 , C07C59/68 , C07D207/20 , C07D209/26 , C07D209/28 , C07D209/46 , C07D209/48 , C07D209/86 , C07D209/88 , C07D263/57 , C07D333/22 , C07D333/24 , C07D337/14
摘要： The present invention encompasses compounds of Formula I (I) or pharmaceutically acceptable salts thereof, wherein A is the base molecule of a propionic acid or acetic acid NSAID, or a derivative thereof, X is —CO2H, 1H-tetrazol-5-yl or 2H-tetrazol-5-yl and R1 and R2 are each independently selected from the group consisting of: C1-6alkyl and C3-6cycloalkyl, as well as pharmaceutical composition comprising said compounds and methods of using said compounds. The compounds of the present invention lower the level of Aβ42 and are therefore useful for preventing, delaying or reversing the progression of Alzheimer's Disease.
摘要翻译： 本发明包括式I（I）的化合物或其药学上可接受的盐，其中A是丙酸或乙酸NSAID或其衍生物的基础分子，X是-CO 2 H ，1H-四唑-5-基或2H-四唑-5-基和R 1和R 2各自独立地选自：C 1 -C 6烷基， 1-6烷基和C 3-6环烷基，以及包含所述化合物的药物组合物和使用所述化合物的方法。 本发明的化合物降低Abeta 42的水平，因此可用于预防，延缓或逆转阿尔茨海默病的进展。
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2.发明申请Geminallyl di-substituted nsaid derivatives as abeta 42 lowering agents 失效Gemallyl二取代的nsaid衍生物作为脱硫剂42降低剂公开(公告)号：US20060063937A1
公开(公告)日：2006-03-23
申请号：US10540601
申请日：2004-01-09
申请人： Benito Munoz , Petpiboon Prasit , Nicholas Stock
发明人： Benito Munoz , Petpiboon Prasit , Nicholas Stock
IPC分类号： A61K31/415 , C07D491/02 , C07D409/02
CPC分类号： C07D257/04 , C07C57/30 , C07C57/58 , C07C59/68 , C07D207/20 , C07D209/26 , C07D209/28 , C07D209/46 , C07D209/48 , C07D209/86 , C07D209/88 , C07D263/57 , C07D333/22 , C07D333/24 , C07D337/14
摘要： The present invention encompasses compounds of Formula I (I) or pharmaceutically acceptable salts thereof, wherein A is the base molecule of a propionic acid or acetic acid NSAID, or a derivative thereof, X is —CO2H, 1H-tetrazol-5-yl or 2H-tetrazol-5-yl and R1 and R2 are each independently selected from the group consisting of: C1-6alkyl and C3-6cycloalkyl, as well as pharmaceutical composition comprising said compounds and methods of using said compounds. The compounds of the present invention lower the level of Aβ42 and are therefore useful for preventing, delaying or reversing the progression of Alzheimer s Disease.
摘要翻译： 本发明包括式I（I）的化合物或其药学上可接受的盐，其中A是丙酸或乙酸NSAID或其衍生物的基础分子，X是-CO 2 H ，1H-四唑-5-基或2H-四唑-5-基和R 1和R 2各自独立地选自：C 1 -C 6烷基， 1-6烷基和C 3-6环烷基，以及包含所述化合物的药物组合物和使用所述化合物的方法。 本发明的化合物降低Abeta 42的水平，因此可用于预防，延缓或逆转阿尔茨海默病的进展。
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公开(公告)号：US07495029B2
公开(公告)日：2009-02-24
申请号：US11667814
申请日：2005-11-10
IPC分类号： A61K31/235 , C07J71/00 , C07D311/80 , C07C381/00 , C07C69/02
CPC分类号： C07C69/24 , C07C53/128 , C07C257/14 , C07C317/46 , C07D217/02 , C07D311/80
摘要： Disclosed are prodrugs of (2R)-2-propyloctanoic acid, and pharmaceutical compositions comprising them, which may be effective in modulating multiple events in the biochemical cascade of stroke. Also disclosed are methods of treating patients who have had a stroke, or are at risk of stroke, by administering the compounds or compositions of the invention.
摘要翻译： 公开了（2R）-2-丙基辛酸的前药和包含它们的药物组合物，其可有效调节中风生化级联中的多个事件。 还公开了通过施用本发明的化合物或组合物来治疗患有中风或有卒中风险的患者的方法。
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4.发明申请1-Alkyl-3-thio-substituted indole-2-alkynoic acids useful for the treatment of alzheimer's disease and related conditions 审中-公开可用于治疗阿尔茨海默病和相关病症的1-烷基-3-硫代取代的吲哚-2-炔酸公开(公告)号：US20070142453A1
公开(公告)日：2007-06-21
申请号：US10580286
申请日：2004-11-25
申请人： Dirk Beher , Michela Bettari , Ian Churcher , Benito Munoz , Petpiboon Prasit , Abdul Quddus , Nicholas Stock , Jonathan Wrigley
发明人： Dirk Beher , Michela Bettari , Ian Churcher , Benito Munoz , Petpiboon Prasit , Abdul Quddus , Nicholas Stock , Jonathan Wrigley
IPC分类号： A61K31/404 , C07D209/36
CPC分类号： C07D417/12 , A61K31/405 , C07D209/30 , C07D209/36 , C07D403/12
摘要： Compounds of formula I: modulate the activity of γ-secretase, and hence find use in treatment or prevention of Alzheimer's disease and related conditions.
摘要翻译： 式I化合物：调节γ-分泌酶的活性，因此可用于治疗或预防阿尔茨海默病和相关病症。
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5.发明授权Heteroaryl substituted pyrazole modulators of metabotropic glutamate receptor-5 有权代谢型谷氨酸受体-5的杂芳基取代的吡唑调节剂公开(公告)号：US07569592B2
公开(公告)日：2009-08-04
申请号：US10497122
申请日：2002-12-13
申请人： Nicholas D. P. Cosford , Chixu Chen , Brian W. Eastman , Dehua Huang , Benito Munoz , Petpiboon Prasit , Nicholas D. Smith
发明人： Nicholas D. P. Cosford , Chixu Chen , Brian W. Eastman , Dehua Huang , Benito Munoz , Petpiboon Prasit , Nicholas D. Smith
IPC分类号： A61K31/4439 , A61K31/4155 , C07D401/04
CPC分类号： C07D231/38 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/04 , C07D413/14 , C07D417/04
摘要： Pyrazole compounds substituted directly, or by a bridge, with a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, bipolar disorder and panic, as well as in the treatment of pain, circadian rhythm disorders, and other diseases.
摘要翻译： 直接或通过桥连与杂芳基相连接的杂芳基部分的吡唑化合物是可用于治疗精神病和情绪障碍（例如精神分裂症，焦虑症，抑郁症）的mGluR5调节剂， 双相情感障碍和恐慌，以及治疗疼痛，昼夜节律紊乱和其他疾病。
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公开(公告)号：US20080132488A1
公开(公告)日：2008-06-05
申请号：US11667814
申请日：2005-11-10
IPC分类号： A61K31/215 , C07C69/02 , A61K31/216 , A61K31/165 , A61P25/00 , A61K31/551 , C07D401/02
CPC分类号： C07C69/24 , C07C53/128 , C07C257/14 , C07C317/46 , C07D217/02 , C07D311/80
摘要： Disclosed are prodrugs of (2R)—2-propyloctanoic acid, and pharmaceutical compositions comprising them, which may be effective in modulating multiple events in the biochemical cascade of stroke. Also disclosed are methods of treating patients who have had a stroke, or are at risk of stroke, by administering the compounds or compositions of the invention.
摘要翻译： 公开了（2R）-2-丙基辛酸的前药和包含它们的药物组合物，其可有效调节中风生化级联中的多个事件。 还公开了通过施用本发明的化合物或组合物来治疗患有中风或有卒中风险的患者的方法。
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7.发明申请Heteroaryl substituted pyrazole modulators of metabotropic glutamate receptor-5 有权代谢型谷氨酸受体-5的杂芳基取代的吡唑调节剂公开(公告)号：US20050026963A1
公开(公告)日：2005-02-03
申请号：US10497122
申请日：2002-12-13
申请人： Nicholas Cosford , Chixu Chen , Brian Eastman , Dehua Huang , Benito Munoz , Petpiboon Prasit , Nicholas Smith
发明人： Nicholas Cosford , Chixu Chen , Brian Eastman , Dehua Huang , Benito Munoz , Petpiboon Prasit , Nicholas Smith
IPC分类号： A61K31/4155 , A61K31/424 , A61K31/427 , A61K31/4439 , A61K31/444 , A61K31/4709 , A61K31/497 , A61K31/498 , A61K31/506 , A61K45/00 , A61P3/04 , A61P17/06 , A61P21/00 , A61P25/04 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/34 , A61P29/00 , A61P43/00 , C07D231/38 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/04 , C07D413/14 , C07D417/04
CPC分类号： C07D231/38 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/04 , C07D413/14 , C07D417/04
摘要： Pyrazole compounds substituted directly, or by a bridge, with a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, bipolar disorder and panic, as well as in the treatment of pain, circadian rhythm disorders, and other diseases.
摘要翻译： 直接或通过桥连与杂芳基相连接的杂芳基部分的吡唑化合物是可用于治疗精神病和情绪障碍（例如精神分裂症，焦虑症，抑郁症）的mGluR5调节剂， 双相情感障碍和恐慌，以及治疗疼痛，昼夜节律紊乱和其他疾病。
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![Treatment of neuropathic pain with 6H-pyrrolo[3,4-d]pyridazine compounds](/abs-image/US/2008/12/16/US07465730B2/abs.jpg.150x150.jpg)
8.发明授权Treatment of neuropathic pain with 6H-pyrrolo[3,4-d]pyridazine compounds 失效用6H-吡咯并[3,4-d]哒嗪化合物治疗神经性疼痛公开(公告)号：US07465730B2
公开(公告)日：2008-12-16
申请号：US10520962
申请日：2003-07-08
申请人： Naomi Burke Anker , Jeannie M. Arruda , Brian Thomas Campbell , Benito Munoz , Petpiboon Prasit , Brian A. Stearns , Tao Hu
发明人： Naomi Burke Anker , Jeannie M. Arruda , Brian Thomas Campbell , Benito Munoz , Petpiboon Prasit , Brian A. Stearns , Tao Hu
IPC分类号： A01N43/58 , A61K31/5025 , C07D487/06
CPC分类号： C07D487/04 , A61K31/045 , A61K31/05 , A61K31/435 , A61K31/495 , A61K31/50 , A61K31/503
摘要： 6H-pyrrolo[3,4-d]pyridazine compounds and methods of their use of as ligands of voltage gated calcium channels (VGCC), useful in the treatment of neuropathic pain, and psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, panic, and bipolar disorder, as well as in the treatment of pain, Parkinson's disease, cognitive dysfunction, epilepsy, circadian rhythm disorders, drug addiction, drug abuse, drug withdrawal and other.
摘要翻译： 6H-吡咯并[3,4-d]哒嗪化合物及其用作电压门控钙通道（VGCC）配体的方法，可用于治疗神经性疼痛，以及精神和心境障碍，例如精神分裂症， 焦虑，抑郁，恐慌和双相情感障碍，以及治疗疼痛，帕金森病，认知功能障碍，癫痫，昼夜节律紊乱，药物成瘾，药物滥用，戒毒等。
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![Treatment of neuropathic pain with 6h-pyrrolo[3,4-d]pyridazine compounds](/abs-image/US/2006/07/13/US20060154929A1/abs.jpg.150x150.jpg)
9.发明申请Treatment of neuropathic pain with 6h-pyrrolo[3,4-d]pyridazine compounds 失效用6h-吡咯并[3,4-d]哒嗪化合物治疗神经性疼痛公开(公告)号：US20060154929A1
公开(公告)日：2006-07-13
申请号：US10520962
申请日：2003-07-08
申请人： Naomi Anker , Jeannie Arruda , Brian Campbell , Benito Munoz , Petpiboon Prasit , Brian Stearns , Tao Hu
发明人： Naomi Anker , Jeannie Arruda , Brian Campbell , Benito Munoz , Petpiboon Prasit , Brian Stearns , Tao Hu
IPC分类号： A61K31/503
CPC分类号： C07D487/04 , A61K31/045 , A61K31/05 , A61K31/435 , A61K31/495 , A61K31/50 , A61K31/503
摘要： 6H-pyrrolo[3,4-d]pyridazine compounds and methods of their use of as ligands of voltage gated calcium channels (VGCC), useful in the treatment of neuropathic pain, and psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, panic, and bipolar disorder, as well as in the treatment of pain, Parkinson's disease, cognitive dysfunction, epilepsy, circadian rhythm disorders, drug addiction, drug abuse, drug withdrawal and other.
摘要翻译： 6H-吡咯并[3,4-d]哒嗪化合物及其用作电压门控钙通道（VGCC）配体的方法，可用于治疗神经性疼痛，以及精神和心境障碍，例如精神分裂症， 焦虑，抑郁，恐慌和双相情感障碍，以及治疗疼痛，帕金森病，认知功能障碍，癫痫，昼夜节律紊乱，药物成瘾，药物滥用，戒毒等。
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10.发明申请Heteroaryl substituted triazole modulators of metabotropic glutamate receptor-5 失效代谢型谷氨酸受体-5的杂芳基取代三唑调节剂公开(公告)号：US20050020585A1
公开(公告)日：2005-01-27
申请号：US10499391
申请日：2002-12-13
IPC分类号： A61K31/135 , A61K31/145 , A61K31/185 , A61K31/19 , A61K31/195 , A61K31/4439 , A61K31/485 , A61K31/506 , A61K31/5513 , A61K45/00 , A61K45/06 , A61P3/04 , A61P3/12 , A61P3/14 , A61P21/00 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P29/00 , C07D401/04 , C07D401/14 , A61K31/54 , A61K31/4178 , A61K31/4196 , A61K31/454 , A61K31/496 , A61K31/5377
CPC分类号： C07D401/04 , C07D401/14
摘要： Triazole compounds substituted directly, or by a bridge, with a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl which are metabotropic glutamate receptor—subtype 5 (“mGluR5”) modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, bipolar disorder and panic, as well as in the treatment of pain, Parkinson's disease, cognitive dysfunction, epilepsy, circadian rhythm disorders, drug addiction, drug abuse, drug withdrawal and other diseases.
摘要翻译： 直接或桥接的三唑化合物与杂芳基部分相邻的杂芳基部分，杂芳基部分与杂芳基的连接点相邻，杂芳基是代谢型谷氨酸受体 - 亚型5（“mGluR5”）调节剂，可用于治疗精神病和情绪障碍，例如 例如精神分裂症，焦虑症，抑郁症，双相情感障碍和恐慌，以及治疗疼痛，帕金森病，认知功能障碍，癫痫，昼夜节律紊乱，药物成瘾，药物滥用，戒毒等疾病。
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