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公开(公告)号：US20120302599A1
公开(公告)日：2012-11-29
申请号：US13307636
申请日：2011-11-30
IPC分类号： A61K31/437 , A61P25/00 , A61P9/10 , A61P9/04 , A61P25/28 , A61P21/02 , A61P25/08 , A61P25/06 , A61P13/02 , A61P25/30 , A61P25/16 , A61P27/02 , A61P25/18 , A61P25/24 , A61P25/22 , A61P31/00 , A61P37/00 , A61P1/16 , A61P35/00 , A61P27/16 , A61P1/08 , A61P25/14 , C07D471/04
CPC分类号： C07D471/04 , C07D487/04
摘要： Compounds of Formula I: wherein X, Y, Z, R1, R2, R3, R4 are as defined herein, and pharmaceutically acceptable salts thereof, are described as useful for the treatment of cognitive deficits associated with schizophrenia and other psychiatric, neurodegenerative and/or neurological disorders in mammals, including humans.
摘要翻译： 式I化合物：其中X，Y，Z，R 1，R 2，R 3，R 4如本文所定义，及其药学上可接受的盐被描述为可用于治疗与精神分裂症和其他精神病学，神经变性和/ 或哺乳动物包括人类的神经障碍。
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公开(公告)号：US08183238B2
公开(公告)日：2012-05-22
申请号：US12816612
申请日：2010-06-16
申请人： Michelle M. Claffey , Amy B. Dounay , Matthew M. Hayward , Suobao Rong , Patrick R. Verhoest , Jamison B. Tuttle , Xinmin Gan
发明人： Michelle M. Claffey , Amy B. Dounay , Matthew M. Hayward , Suobao Rong , Patrick R. Verhoest , Jamison B. Tuttle , Xinmin Gan
IPC分类号： A61K31/52 , A61K31/519 , A61K31/5377 , A61K31/4375 , A61K31/473 , A61K31/4741 , A61K31/506 , A61K31/501 , A61K31/517 , C07D473/30 , C07D473/20 , C07D413/12 , C07D405/10 , C07D401/10 , C07D401/04 , C07D471/04 , C07D215/58 , C07D221/10 , C07D413/10 , C07D491/048 , C07D487/04
CPC分类号： C07D215/60 , C07D401/04 , C07D401/12 , C07D405/04 , C07D471/04 , C07D491/04
摘要： Compounds of Formula X: wherein A, X, Y, Z, R5, R6a, and R6b are as defined herein, and pharmaceutically acceptable salts thereof, are described as useful for the treatment of cognitive deficits associated with schizophrenia and other neurodegenerative and/or neurological disorders in mammals, including humans.
摘要翻译： 式X的化合物：其中A，X，Y，Z，R 5，R 6a和R 6b如本文所定义，及其药学上可接受的盐被描述为可用于治疗与精神分裂症和其它神经变性和/或其它神经变性相关的认知缺陷 包括人在内的哺乳动物的神经障碍。
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公开(公告)号：US20100324043A1
公开(公告)日：2010-12-23
申请号：US12816612
申请日：2010-06-16
申请人： Michelle M. Claffey , Amy B. Dounay , Matthew M. Hayward , Suobao Rong , Patrick R. Verhoest , Jamison B. Tuttle , Xinmin Gan
发明人： Michelle M. Claffey , Amy B. Dounay , Matthew M. Hayward , Suobao Rong , Patrick R. Verhoest , Jamison B. Tuttle , Xinmin Gan
IPC分类号： A61K31/5377 , C07D471/04 , A61K31/4375 , C07D215/58 , A61K31/4704 , C07D221/10 , A61K31/473 , C07D413/10 , C07D491/048 , A61K31/4741 , C07D401/12 , C07D401/10 , C07D405/10 , A61K31/506 , A61K31/501 , C07D413/12 , A61K31/517 , C07D487/04 , A61K31/519 , C07D473/30 , A61K31/52 , A61P25/00 , A61P25/18 , A61P25/16 , A61P9/10 , A61P25/30 , A61P25/28 , A61P25/24 , A61P27/02 , A61P29/00 , A61P35/00 , A61P13/00
CPC分类号： C07D215/60 , C07D401/04 , C07D401/12 , C07D405/04 , C07D471/04 , C07D491/04
摘要： Compounds of Formula X: wherein A, X, Y, Z, R5, R6a, and R6b are as defined herein, and pharmaceutically acceptable salts thereof, are described as useful for the treatment of cognitive deficits associated with schizophrenia and other neurodegenerative and/or neurological disorders in mammals, including humans.
摘要翻译： 式X的化合物：其中A，X，Y，Z，R 5，R 6a和R 6b如本文所定义，及其药学上可接受的盐被描述为可用于治疗与精神分裂症和其它神经变性和/或其它神经变性相关的认知缺陷 包括人在内的哺乳动物的神经障碍。
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公开(公告)号：US20120142729A1
公开(公告)日：2012-06-07
申请号：US13307140
申请日：2011-11-30
IPC分类号： A61K31/4704 , A61P25/00 , A61P25/18 , A61P25/28 , A61P9/04 , A61P9/10 , A61P25/14 , A61P27/02 , A61P25/16 , A61P25/08 , A61P25/06 , A61P13/00 , A61P25/30 , A61P25/24 , A61P25/22 , A61P29/00 , A61P37/00 , A61P1/16 , A61P35/00 , A61P27/16 , A61P1/08 , C07D215/58
CPC分类号： C07D215/58
摘要： The present invention relates to compounds 3-amino-1-hydroxy-2-oxo-1,2,3,4-tetrahydroquinoline-7-carbonitrile, 3-amino-1-hydroxy-7-(2-methoxyethoxy)-3,4-dihydroquinolin-2(1H)-one, and 3-amino-1-hydroxy-7-[(1S)-2-methoxy-1-methylethoxy]-3,4-dihydroquinolin-2(1H)-one, including racemic mixtures and resolved enantiomers thereof, to pharmaceutically acceptable salts thereof, and to the treatment of cognitive deficits associated with schizophrenia and other psychiatric, neurodegenerative and/or neurological disorders in mammals, including humans.
摘要翻译： 本发明涉及3-氨基-1-羟基-2-氧代-1,2,3,4-四氢喹啉-7-腈，3-氨基-1-羟基-7-（2-甲氧基乙氧基） （1H） - 酮和3-氨基-1-羟基-7 - [（1S）-2-甲氧基-1-甲基乙氧基] -3,4-二氢喹啉-2（1H） - 酮，包括 外消旋混合物及其拆分的对映异构体，其药学上可接受的盐，以及治疗与哺乳动物（包括人）中的精神分裂症和其它精神病，神经变性和/或神经障碍有关的认知缺陷。
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公开(公告)号：US06992087B2
公开(公告)日：2006-01-31
申请号：US10298193
申请日：2002-11-15
申请人： Patrick R. Verhoest , Robert Louis Hoffman , Jeffrey W. Corbett , Michael Dalton Ennis , Kristine E. Frank , Jian-Min Fu
发明人： Patrick R. Verhoest , Robert Louis Hoffman , Jeffrey W. Corbett , Michael Dalton Ennis , Kristine E. Frank , Jian-Min Fu
IPC分类号： A61K31/4965 , C07D241/00 , C07D241/02 , B65D75/80
CPC分类号： C07D241/18 , C07D241/20 , C07D241/26 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D491/04 , G01N33/74 , G01N2333/5751 , G01N2500/02 , Y10S206/828
摘要： Substituted aryl 1,4-pyrazine derivatives of formula I as defined herein and their use in treating anxiety disorders, depression and stress related disorders are disclosed.
摘要翻译： 公开了本文定义的式I的取代的芳基1,4-吡嗪衍生物及其在治疗焦虑症，抑郁症和应激相关疾病中的用途。
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公开(公告)号：US07250418B2
公开(公告)日：2007-07-31
申请号：US10840485
申请日：2004-05-06
申请人： Jeffrey W. Corbett , Michael Dalton Ennis , Kristine E. Frank , Jian-Min Fu , Robert Louis Hoffman , Patrick R. Verhoest
发明人： Jeffrey W. Corbett , Michael Dalton Ennis , Kristine E. Frank , Jian-Min Fu , Robert Louis Hoffman , Patrick R. Verhoest
IPC分类号： A61K31/4965 , C07D239/02 , C07D401/00 , C07D403/00 , C07D405/00
CPC分类号： C07D401/14 , C07D403/14 , C07D417/14
摘要： The present invention relates to compounds of Formula I, or a stereoisomer thereof, a pharmaceutically acceptable salt thereof, or a prodrug thereof. The compounds of the inventions are CRF1 receptor antagonists. Compounds of the invention are useful for treating, in a warm-blooded animal, particularly a mammal, and more particularly a human, various disorders that are associated with CRF or CRF1 receptors, or disorders the treatment of which can be effected or facilitated by antagonizing CRF1 receptors.
摘要翻译： 本发明涉及式I化合物或其立体异构体，其药学上可接受的盐或其前药。 本发明的化合物是CRF 1受体拮抗剂。 本发明的化合物可用于在温血动物，特别是哺乳动物，特别是人类与CRF或CRF 1受体相关的各种疾病中治疗，或治疗失调 其可以通过拮抗CRF 1受体来实现或促进。
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公开(公告)号：US08278295B2
公开(公告)日：2012-10-02
申请号：US12693480
申请日：2010-01-26
IPC分类号： A01N43/00 , A01N43/90 , A61K31/00 , A61K31/519 , C07D487/00
CPC分类号： C07D487/04 , A61K31/13 , A61K31/27 , A61K31/444 , A61K31/445 , A61K31/473 , A61K31/519 , A61K31/55
摘要： The invention provides PDE9-inhibiting compounds of Formula (I), and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, A, and n are as defined herein. Pharmaceutical compositions containing the compounds of Formula I, and uses thereof in treating neurodegenerative and cognitive disorders, such as Alzheimer's disease and schizophrenia, are also provided.
摘要翻译： 本发明提供抑制PDE9的式（I）化合物及其药学上可接受的盐，其中R 1，R 2，R 3，A和n如本文所定义。 还提供了含有式I化合物的药物组合物及其用于治疗神经变性和认知障碍如阿尔茨海默病和精神分裂症的用途。
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公开(公告)号：US20100190771A1
公开(公告)日：2010-07-29
申请号：US12693480
申请日：2010-01-26
IPC分类号： A61K31/519 , A61P25/00 , A61P25/28 , C07D487/04
CPC分类号： C07D487/04 , A61K31/13 , A61K31/27 , A61K31/444 , A61K31/445 , A61K31/473 , A61K31/519 , A61K31/55
摘要： The invention provides PDE9-inhibiting compounds of Formula (I), and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, A, and n are as defined herein. Pharmaceutical compositions containing the compounds of Formula I, and uses thereof in treating neurodegenerative and cognitive disorders, such as Alzheimer's disease and schizophrenia, are also provided.
摘要翻译： 本发明提供抑制PDE9的式（I）化合物及其药学上可接受的盐，其中R 1，R 2，R 3，A和n如本文所定义。 还提供了含有式I化合物的药物组合物及其用于治疗神经变性和认知障碍如阿尔茨海默病和精神分裂症的用途。
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公开(公告)号：US20090030003A1
公开(公告)日：2009-01-29
申请号：US12118062
申请日：2008-05-09
IPC分类号： A61K31/519 , C07D487/04 , A61P25/28
CPC分类号： C07D487/04
摘要： The invention provides PDE9-inhibiting compounds of Formula (I), and pharmaceutically acceptable salts thereof, wherein R, R1, R2 and R3 are as defined herein. Pharmaceutical compositions containing the compounds of Formula I, and uses thereof in treating neurodegenerative and cognitive disorders, such as Alzheimer's disease and schizophrenia, are also provided.
摘要翻译： 本发明提供抑制PDE9的式（I）化合物及其药学上可接受的盐，其中R，R 1，R 2和R 3如本文所定义。 还提供了含有式I化合物的药物组合物及其用于治疗神经变性和认知障碍如阿尔茨海默病和精神分裂症的用途。
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公开(公告)号：US07015229B2
公开(公告)日：2006-03-21
申请号：US10370259
申请日：2003-02-20
申请人： Jian-Min Fu , Jeffrey W. Corbett , Michael Dalton Ennis , Kristine E. Frank , Robert Louis Hoffman , Patrick R. Verhoest
发明人： Jian-Min Fu , Jeffrey W. Corbett , Michael Dalton Ennis , Kristine E. Frank , Robert Louis Hoffman , Patrick R. Verhoest
IPC分类号： C07D239/46 , C07D401/04 , C07D403/12 , A61K31/506
CPC分类号： C07D239/47 , C07D401/04 , C07D401/14 , C07D403/12 , C07D417/14 , G01N2333/726
摘要： This invention relates to substituted pyrimidinone and pyrimidithione derivatives that bind with high affifnity to CRF1 receptors, including human CRF1 receptors. This invention also relates to methods of using the compounds of the invention to treat a disorder or condition, the treatment of which can be effected or facilitated by antagonizing a CRF receptor, such as CNS disorders or diseases, particularly anxiety disorders, and depression and stress related disorders.
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