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公开(公告)号：US08008481B2
公开(公告)日：2011-08-30
申请号：US11731950
申请日：2007-04-02
申请人： Anna M. Ericsson , Andrew Burchat , Kristine E. Frank , David J. Calderwood , Lily K. Abbott , Maria A. Argiriadi , David W. Borhani , Kevin P. Cusack , Richard W. Dixon , Thomas D. Gordon , Kelly D. Mullen , Robert V. Talanian , Xiaoyun Wu , Xiaolei Zhang , Lu Wang , Biqin Li , Claude E. Barberis , Neil Wishart
发明人： Anna M. Ericsson , Andrew Burchat , Kristine E. Frank , David J. Calderwood , Lily K. Abbott , Maria A. Argiriadi , David W. Borhani , Kevin P. Cusack , Richard W. Dixon , Thomas D. Gordon , Kelly D. Mullen , Robert V. Talanian , Xiaoyun Wu , Xiaolei Zhang , Lu Wang , Biqin Li , Claude E. Barberis , Neil Wishart
IPC分类号： C07D409/14 , C07D413/14
CPC分类号： C07D487/04 , C07D403/12 , C07D403/14 , C07D409/04 , C07D409/14
摘要： Novel compounds of Formula (I) or pharmaceutically acceptable salts, prodrugs and biologically active metabolites thereof of Formula (I) wherein the substituents are as defined herein, which are useful as therapeutic agents.
摘要翻译： 式（I）的新型化合物或其药学上可接受的盐，前体药物和式（I）的生物活性代谢物，其中取代基如本文所定义，其可用作治疗剂。
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公开(公告)号：US20090312338A1
公开(公告)日：2009-12-17
申请号：US12481028
申请日：2009-06-09
申请人： Neil Wishart , Maria A. Argiriadi , David J. Calderwood , Anna M. Ericsson , Bryan A. Fiamengo , Kristine E. Frank , Michael Friedman , Dawn M. George , Eric R. Goedken , Nathan S. Josephsohn , Biqin C. Li , Michael J. Morytko , Kent D. Stewart , Jeffrey W. Voss , Grier A. Wallace , Lu Wang , Kevin R. Woller
发明人： Neil Wishart , Maria A. Argiriadi , David J. Calderwood , Anna M. Ericsson , Bryan A. Fiamengo , Kristine E. Frank , Michael Friedman , Dawn M. George , Eric R. Goedken , Nathan S. Josephsohn , Biqin C. Li , Michael J. Morytko , Kent D. Stewart , Jeffrey W. Voss , Grier A. Wallace , Lu Wang , Kevin R. Woller
IPC分类号： A61K31/4985 , C07D487/14
CPC分类号： C07D487/14 , C07D498/14 , C07D513/14
摘要： The invention provides a compound of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.
摘要翻译： 本发明提供式（I）化合物的药学上可接受的盐，前药，生物活性代谢物，立体异构体和异构体，其中变量在本文中定义。 本发明的化合物可用于治疗免疫学和肿瘤学病症。
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公开(公告)号：US20080242862A1
公开(公告)日：2008-10-02
申请号：US11728919
申请日：2007-03-27
申请人： David J. Calderwood , Kristine E. Frank , Patrick Betschmann , Eric C. Breinlinger , Richard W. Dixon
发明人： David J. Calderwood , Kristine E. Frank , Patrick Betschmann , Eric C. Breinlinger , Richard W. Dixon
IPC分类号： C07D403/14
CPC分类号： C07D487/04
摘要： The present invention is directed to novel imidazopyrazine compounds useful as kinase inhibitors and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, cancers.
摘要翻译： 本发明涉及用作激酶抑制剂的新颖的咪唑并嗪化合物，因此可用于治疗某些病症和疾病，特别是炎性病症和疾病以及增殖性病症和病症，例如癌症。
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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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公开(公告)号：US06964965B2
公开(公告)日：2005-11-15
申请号：US10417867
申请日：2003-04-17
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： G01N33/50 , A61K31/4965 , A61K31/497 , A61P1/00 , A61P1/14 , A61P3/04 , A61P3/08 , A61P5/00 , A61P7/12 , A61P9/00 , A61P11/06 , A61P15/08 , A61P17/00 , A61P17/06 , A61P17/14 , A61P21/00 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/32 , A61P25/34 , A61P25/36 , A61P29/00 , A61P31/18 , A61P35/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D241/20 , C07D403/12 , C12Q1/02 , G01N33/15 , C07D401/00 , C07D403/00 , C07D405/00
CPC分类号： C07D403/12 , C07D241/20 , Y10S206/828
摘要： The present invention provides substituted pyrazine 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的取代吡嗪衍生物，其为CRF 1受体拮抗剂，包括人CRF 1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。
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![Substituted azepino[4,5b]indole derivatives](/abs-image/US/2005/06/07/US06903090B2/abs.jpg.150x150.jpg)
公开(公告)号：US06903090B2
公开(公告)日：2005-06-07
申请号：US10393968
申请日：2003-03-20
申请人： Kristine E. Frank , Brad A. Acker , Michael D. Ennis , Jed F. Fisher , Jian-min Fu , William W. McWhorter, Jr. , Jeanette K. Morris , Donald Joseph Rogier , Eric Jon Jacobsen
发明人： Kristine E. Frank , Brad A. Acker , Michael D. Ennis , Jed F. Fisher , Jian-min Fu , William W. McWhorter, Jr. , Jeanette K. Morris , Donald Joseph Rogier , Eric Jon Jacobsen
IPC分类号： A61K31/55 , A61P3/04 , A61P25/00 , A61P25/02 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P43/00 , C07D487/04 , G06T3/00
CPC分类号： C07D487/04
摘要： Disclosed are compounds of Formula (I): wherein R1-R4, p and q have any of the values described in the specification, as well as pharmaceutical salts thereof, and pharmaceutical compositions containing such compounds or salts. The compounds and salts are 5-HT ligands and are useful for treating diseases, disorders, and/or conditions in a mammal wherein activity of a 5-HT receptor is implicated. The compounds and salts are particularly useful for treating diseases of the central nervous system.
摘要翻译： 公开了式（I）的化合物：其中R 1 -R 4，p和q具有说明书中描述的任何值，以及其药用盐， 和含有这些化合物或盐的药物组合物。 化合物和盐是5-HT配体，可用于治疗其中涉及5-HT受体的活性的哺乳动物的疾病，病症和/或病症。 化合物和盐特别适用于治疗中枢神经系统疾病。
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公开(公告)号：US08962629B2
公开(公告)日：2015-02-24
申请号：US12481028
申请日：2009-06-09
申请人： Neil Wishart , Maria A. Argiriadi , David J. Calderwood , Anna M. Ericsson , Bryan A. Fiamengo , Kristine E. Frank , Michael M. Friedman , Dawn M. George , Eric R. Goedken , Nathan S. Josephsohn , Biqin C. Li , Kent D. Stewart , Grier A. Wallace , Lu Wang , Kevin R. Woller
发明人： Neil Wishart , Maria A. Argiriadi , David J. Calderwood , Anna M. Ericsson , Bryan A. Fiamengo , Kristine E. Frank , Michael M. Friedman , Dawn M. George , Eric R. Goedken , Nathan S. Josephsohn , Biqin C. Li , Kent D. Stewart , Grier A. Wallace , Lu Wang , Kevin R. Woller
IPC分类号： A61K31/495 , C07D513/14 , C07D487/14 , C07D498/14
CPC分类号： C07D487/14 , C07D498/14 , C07D513/14
摘要： The invention provides a compound of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.
摘要翻译： 本发明提供式（I）化合物的药学上可接受的盐，前药，生物活性代谢物，立体异构体和异构体，其中变量在本文中定义。 本发明的化合物可用于治疗免疫学和肿瘤学病症。
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公开(公告)号：US08188083B2
公开(公告)日：2012-05-29
申请号：US12215338
申请日：2008-06-26
申请人： David J. Calderwood , Dominique F. Bonafoux , Andrew Burchat , Ping Ding , Kristine E. Frank , Michael Z. Hoemann , Kelly D. Mullen , Heather M. Davis
发明人： David J. Calderwood , Dominique F. Bonafoux , Andrew Burchat , Ping Ding , Kristine E. Frank , Michael Z. Hoemann , Kelly D. Mullen , Heather M. Davis
IPC分类号： A61K31/50 , C07D237/26
CPC分类号： C07D487/04 , C07D519/00
摘要： The present invention is directed to novel compounds of formula (I) wherein the variables are defined as herein. The compounds of formula (I) are useful as kinase inhibitors and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, cancers.
摘要翻译： 本发明涉及新的式（I）化合物，其中变量如本文所定义。 式（I）化合物可用作激酶抑制剂，因此可用于治疗某些病症和疾病，特别是炎性病症和疾病以及增殖性病症和病症，例如癌症。
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公开(公告)号：US07790741B2
公开(公告)日：2010-09-07
申请号：US11973147
申请日：2007-10-05
申请人： David J. Calderwood , Kristine E. Frank , David W. Borhani , Heather M. Davis , Nathan S. Josephsohn , Barbara S. Skinner
发明人： David J. Calderwood , Kristine E. Frank , David W. Borhani , Heather M. Davis , Nathan S. Josephsohn , Barbara S. Skinner
IPC分类号： A61K31/437 , A61K31/4184 , A61K31/424 , A61K31/429 , C07D487/04 , C07D513/04 , C07D498/04
CPC分类号： C07D498/04 , C07D513/04 , C07D519/00
摘要： The present invention is directed to novel compounds of formula (I) wherein the variables are as defined herein. The compounds of formula (I) are useful as kinase inhibitors and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, cancers.
摘要翻译： 本发明涉及新的式（I）化合物，其中变量如本文所定义。 式（I）化合物可用作激酶抑制剂，因此可用于治疗某些病症和疾病，特别是炎性病症和疾病以及增殖性病症和病症，例如癌症。
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公开(公告)号：US20090270402A1
公开(公告)日：2009-10-29
申请号：US12215338
申请日：2008-06-26
申请人： David J. Calderwood , Dominique F. Bonafoux , Andrew Burchat , Ping Ding , Kristine E. Frank , Michael Z. Hoemann , Kelly D. Mullen , Heather M. Davis
发明人： David J. Calderwood , Dominique F. Bonafoux , Andrew Burchat , Ping Ding , Kristine E. Frank , Michael Z. Hoemann , Kelly D. Mullen , Heather M. Davis
IPC分类号： A61K31/4985 , C07D487/04 , C07D513/04 , A61K31/433 , A61P25/28 , A61K31/5025
CPC分类号： C07D487/04 , C07D519/00
摘要： The present invention is directed to novel compounds of formula (I) wherein the variables are defined as herein. The compounds of formula (I) are useful as kinase inhibitors and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, cancers.
摘要翻译： 本发明涉及新的式（I）化合物，其中变量如本文所定义。 式（I）化合物可用作激酶抑制剂，因此可用于治疗某些病症和疾病，特别是炎性病症和疾病以及增殖性病症和病症，例如癌症。
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