-
公开(公告)号:US20050049257A1
公开(公告)日:2005-03-03
申请号:US10844004
申请日:2004-05-12
申请人: Patrick Verhoest , Jeffrey Corbett , Michael Ennis , Kristine Frank , Jian-Min Fu , Robert Hoffman
发明人: Patrick Verhoest , Jeffrey Corbett , Michael Ennis , Kristine Frank , Jian-Min Fu , Robert Hoffman
IPC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 , A61K31/4965 , C07D43/02
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 and their use in treating anxiety disorders, depression and stress related disorders are disclosed.
摘要翻译: 公开了取代的芳基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。
-
公开(公告)号:US20050101613A1
公开(公告)日:2005-05-12
申请号:US10839055
申请日:2004-05-05
申请人: Jeffrey Corbett , Michael Ennis , Kristine Frank , Jian-Min Fu , Robert Hoffman , Patrick Verhoest
发明人: Jeffrey Corbett , Michael Ennis , Kristine Frank , Jian-Min Fu , Robert Hoffman , Patrick Verhoest
IPC分类号: C07D213/72 , C07D239/42 , A61K31/506 , A61K31/4439 , C07D43/02
CPC分类号: C07D239/42 , C07D213/72
摘要: This invention relates to compounds of Formula I, a stereoisomer thereof, a pharmaceutically acceptable salt thereof, a prodrug thereof, or a pharmaceutically acceptable salt of a prodrug thereof. The compounds interact with CRF, receptors, including human CRF, 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-related disorders such as anxiety, and mood disorders such as major depression.
摘要翻译: 本发明涉及式I化合物,其立体异构体,其药学上可接受的盐,其前药或其前药的药学上可接受的盐。 该化合物与CRF,受体(包括人类CRF)受体相互作用。 本发明还涉及使用本发明化合物治疗病症或病症的方法,所述疾病或病症的治疗可以通过拮抗CRF受体如CNS疾病或疾病,特别是焦虑相关疾病例如焦虑来实现或促进 ,以及心理障碍如重度抑郁症。
-
公开(公告)号:US20050038040A1
公开(公告)日:2005-02-17
申请号:US10840485
申请日:2004-05-06
申请人: Jeffrey Corbett , Michael Ennis , Kristine Frank , Jian-Min Fu , Robert Hoffman , Patrick Verhoest
发明人: Jeffrey Corbett , Michael Ennis , Kristine Frank , Jian-Min Fu , Robert Hoffman , Patrick Verhoest
IPC分类号: A61P25/00 , C07D401/14 , C07D403/14 , C07D417/14 , A61K31/497 , C07D43/14
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CRF1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中治疗,特别是治疗与CRF或CRF1受体相关的各种疾病,或其治疗可通过拮抗作用或促进 CRF1受体。
-
公开(公告)号:US20060217398A1
公开(公告)日:2006-09-28
申请号:US11424073
申请日:2006-06-14
申请人: Jeffrey Corbett , Micheal Ennis , Kristine Frank , Jian-Min Fu , Robert Hoffman , Patrick Verhoest
发明人: Jeffrey Corbett , Micheal Ennis , Kristine Frank , Jian-Min Fu , Robert Hoffman , Patrick Verhoest
IPC分类号: A61K31/506 , A61K31/4439
CPC分类号: C07D239/42 , C07D213/72
摘要: This invention relates to compounds of Formula I, a stereoisomer thereof, a pharmaceutically acceptable salt thereof, a prodrug thereof, or a pharmaceutically acceptable salt of a prodrug thereof. The compounds interact with 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-related disorders such as anxiety, and mood disorders such as major depression.
摘要翻译: 本发明涉及式I化合物,其立体异构体,其药学上可接受的盐,其前药或其前药的药学上可接受的盐。 这些化合物与CRF1受体(包括人CRF 1受体)相互作用。 本发明还涉及使用本发明化合物治疗病症或病症的方法,所述疾病或病症的治疗可以通过拮抗CRF受体如CNS疾病或疾病,特别是焦虑相关疾病例如焦虑来实现或促进 ,以及心理障碍如重度抑郁症。
-
公开(公告)号:US20050143403A1
公开(公告)日:2005-06-30
申请号:US10827750
申请日:2004-04-20
申请人: Jian-Min Fu , Michael Ennis , Robert Hoffman , Patrick Verhoest , John Mickelson , Jeffrey Corbett
发明人: Jian-Min Fu , Michael Ennis , Robert Hoffman , Patrick Verhoest , John Mickelson , Jeffrey Corbett
IPC分类号: A61K31/513 , A61P25/00 , C07D401/14 , C07D403/04 , G01N33/76 , C07D43/04
CPC分类号: G01N33/76 , C07D401/14 , C07D403/04 , 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.
摘要翻译: 本发明涉及与CRF 1受体(包括人CRF 1受体)具有高亲和性结合的取代的嘧啶酮和嘧啶硫酮衍生物。 本发明还涉及使用本发明化合物治疗病症或病症的方法,其治疗可以通过拮抗CRF受体如CNS疾病或疾病,特别是焦虑症,抑郁和应激来实现或促进 相关疾病。
-
公开(公告)号:US20050020601A1
公开(公告)日:2005-01-27
申请号:US10840484
申请日:2004-05-06
IPC分类号: A61P25/00 , C07D241/20 , C07D401/04 , C07D401/14 , C07D403/12 , C07D403/14 , C07D417/14 , A61K31/497 , A61K31/4965
CPC分类号: C07D401/04 , C07D241/20 , C07D401/14 , C07D403/12 , C07D403/14 , C07D417/14
摘要: The present invention provides substituted pyrazinone derivatives of Formula I that are CRF1 receptor antagonists, including human CRF1 receptors. This invention also relates to use of compounds of the invention for treating a disorder or condition, the treatment of which can be effected or facilitated by antagonizing a CRF receptor, such as CNS disorders, particularly anxiety-related disorders and mood disorders.
摘要翻译: 本发明提供式I的取代的吡嗪酮衍生物,其为CRF1受体拮抗剂,包括人CRF1受体。 本发明还涉及本发明化合物用于治疗病症或病症的用途,所述疾病或病症的治疗可以通过拮抗CRF受体(例如CNS病症,特别是焦虑相关疾病和情绪障碍)来实现或促进。
-
公开(公告)号:US20060211710A1
公开(公告)日:2006-09-21
申请号:US11363009
申请日:2006-02-27
申请人: Patrick Verhoest , Robert Hoffmann
发明人: Patrick Verhoest , Robert Hoffmann
IPC分类号: A61K31/496 , C07D403/02
CPC分类号: C07D401/04
摘要: The invention is directed to compounds of Formula I, described herein, as well as pharmaceutically acceptable salts thereof, which act as CRF1 antagonists and are useful in the treatment of disorders and diseases associated with CRF1 receptors, including CNS-related disorders and diseases.
摘要翻译: 本发明涉及本文所述的式I化合物及其药学上可接受的盐,其作为CRF 1拮抗剂,并且可用于治疗与CRF u> 1受体,包括CNS相关疾病和疾病。
-
公开(公告)号:US20060154931A1
公开(公告)日:2006-07-13
申请号:US11326221
申请日:2006-01-05
IPC分类号: A61K31/506 , A61K31/498 , A61K31/4709 , C07D403/14 , C07D401/14
CPC分类号: C07D401/14 , C07D413/14
摘要: The invention pertains to heteroaromatic compounds that serve as effective phosphodiesterase (PDE) inhibitors. In particular, the invention relates to said compounds which are selective inhibitors of PDE10. The invention also relates to intermediates for preparation of said compounds; pharmaceutical compositions comprising said compounds; and the use of said compounds in a method for treating certain central nervous system (CNS) or other disorders.
摘要翻译: 本发明涉及用作有效磷酸二酯酶(PDE)抑制剂的杂芳族化合物。 特别地,本发明涉及作为PDE10的选择性抑制剂的所述化合物。 本发明还涉及制备所述化合物的中间体; 包含所述化合物的药物组合物; 以及所述化合物在治疗某些中枢神经系统(CNS)或其它疾病的方法中的用途。
-
公开(公告)号:US20070155779A1
公开(公告)日:2007-07-05
申请号:US11619218
申请日:2007-01-03
IPC分类号: A61K31/4745 , A61K31/4439 , C07D471/02 , C07D403/14
CPC分类号: C07D401/14 , C07D403/14 , C07D417/14 , C07D471/04 , C07D471/06 , C07D513/04
摘要: The invention pertains to bicyclic heteroaryl compounds that serve as effective phosphodiesterase (PDE) inhibitors The invention also relates to compounds which are selective inhibitors of PDE-10. The invention further relates to intermediates for preparation of such compounds; pharmaceutical compositions comprising such compounds; and the use of such compounds in methods for treating certain central nervous system (CNS) or other disorders. The invention relates also to methods for treating neurodegenerative and psychiatric disorders, for example psychosis and disorders comprising deficient cognition as a symptom.
摘要翻译: 本发明涉及用作有效磷酸二酯酶(PDE)抑制剂的双环杂芳基化合物本发明还涉及作为PDE-10的选择性抑制剂的化合物。 本发明还涉及制备这些化合物的中间体; 包含这些化合物的药物组合物; 以及这些化合物在治疗某些中枢神经系统(CNS)或其他疾病的方法中的应用。 本发明还涉及用于治疗神经变性和精神疾病的方法,例如包括缺乏认知作为症状的精神病和病症。
-
公开(公告)号:US20100035873A1
公开(公告)日:2010-02-11
申请号:US12489902
申请日:2009-06-23
申请人: Patrick Verhoest , Matthew Merrill Hayward , Vinod Parikh , Stanton Furst McHardy , Stafford McLean
发明人: Patrick Verhoest , Matthew Merrill Hayward , Vinod Parikh , Stanton Furst McHardy , Stafford McLean
IPC分类号: A61K31/535 , C07D401/02 , A61K31/4439 , C07D265/30
CPC分类号: C07D207/48 , C07D209/02 , C07D209/52 , C07D211/14 , C07D211/48 , C07D213/71 , C07D265/30 , C07D295/26 , C07D305/06 , C07D307/22 , C07D309/14 , C07D401/12
摘要: The invention relates to derivatives of a compound of formula I: wherein R1 to R7 and X1 to X6 are as defined herein.The invention relates to the uses thereof for treating diseases, conditions and/or disorders mediated by kappa opioid receptors (KORs). Specifically, the compounds are selective antagonists of KORs and are highly selective to KORs relative to mu and delta opioid receptors.
摘要翻译: 本发明涉及式I化合物的衍生物:其中R 1至R 7和X 1至X 6如本文所定义。 本发明涉及其用于治疗由κ阿片受体介导的疾病,病症和/或病症(KOR)的用途。 具体地说,这些化合物是KORs的选择性拮抗剂,相对于mu和δ阿片样物质受体,对KORs具有高选择性。
-
-
-
-
-
-
-
-
-