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1.发明授权Macrocyclic analogs for the treatment of immunoregulatory disorders and respiratory diseases 失效用于治疗免疫调节性疾病和呼吸系统疾病的大环类似物公开(公告)号：US07553842B2
公开(公告)日：2009-06-30
申请号：US11334858
申请日：2006-01-19
IPC分类号： A01N43/42 , A61K31/44 , C07D498/00 , C07D221/06
CPC分类号： C07D498/18 , A61K31/435 , A61K31/436 , A61K31/4745 , A61K45/06 , A61K2300/00
摘要： Disclosed are compounds of the Formula I and diastereomers, tautomers, solvates, metabolites, and pharmaceutically acceptable salts thereof, wherein X, A, L and Y are as defined herein. Such compounds are useful in the treatment of immunoregulatory and respiratory diseases in mammals. Also disclosed are methods of using such compounds in the treatment of immunoregulatory and respiratory diseases in mammals and pharmaceutical compositions containing such compounds.
摘要翻译： 公开了式I和非对映异构体，互变异构体，溶剂合物，代谢物和其药学上可接受的盐的化合物，其中X，A，L和Y如本文所定义。 这些化合物可用于治疗哺乳动物的免疫调节和呼吸系统疾病。 还公开了使用这些化合物治疗哺乳动物免疫调节和呼吸系统疾病的方法以及含有这些化合物的药物组合物。
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公开(公告)号：US06458787B1
公开(公告)日：2002-10-01
申请号：US09847424
申请日：2001-05-02
申请人： Timothy J. Martins , Kerry W. Fowler , Joshua Odingo , Edward A. Kesicki , Amy Oliver , Laurence E. Burgess , John J. Gaudino , Zachary S. Jones , Bradley J. Newhouse , Stephen T. Schlacter
发明人： Timothy J. Martins , Kerry W. Fowler , Joshua Odingo , Edward A. Kesicki , Amy Oliver , Laurence E. Burgess , John J. Gaudino , Zachary S. Jones , Bradley J. Newhouse , Stephen T. Schlacter
IPC分类号： A61K31535
CPC分类号： C07D207/08 , A61K31/40 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/06 , C07D417/12 , Y02A50/411
摘要： Novel pyrrolidine compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.
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公开(公告)号：US06258833B1
公开(公告)日：2001-07-10
申请号：US09471846
申请日：1999-12-23
申请人： Timothy J. Martins , Kerry W. Fowler , Joshua Odingo , Edward Kesicki , Amy Oliver , Laurence E. Burgess , John J. Gaudino , Zachary S. Jones , Bradley J. Newhouse , Stephen T. Schlacter
发明人： Timothy J. Martins , Kerry W. Fowler , Joshua Odingo , Edward Kesicki , Amy Oliver , Laurence E. Burgess , John J. Gaudino , Zachary S. Jones , Bradley J. Newhouse , Stephen T. Schlacter
IPC分类号： A61K31415
CPC分类号： C07D207/08 , A61K31/40 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/06 , C07D417/12 , Y02A50/411
摘要： Novel pyrrolidine compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.
摘要翻译： 公开了作为PDE4的有效和选择性抑制剂的新型吡咯烷化合物及其制备方法。 还公开了化合物在治疗炎性疾病和涉及细胞因子水平升高的其它疾病以及中枢神经系统（CNS）病症中的用途。
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公开(公告)号：US06423710B1
公开(公告)日：2002-07-23
申请号：US09717956
申请日：2000-11-21
申请人： Timothy J. Martins , Kerry W. Fowler , Joshua Odingo , Edward A. Kesicki , Amy Oliver , Laurence E. Burgess , John J. Gaudino , Zachary S. Jones , Bradley J. Newhouse , Stephen T. Schlachter
发明人： Timothy J. Martins , Kerry W. Fowler , Joshua Odingo , Edward A. Kesicki , Amy Oliver , Laurence E. Burgess , John J. Gaudino , Zachary S. Jones , Bradley J. Newhouse , Stephen T. Schlachter
IPC分类号： A61K31535
CPC分类号： C07D207/08 , A61K31/40 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/06 , C07D417/12 , Y02A50/411
摘要： Novel pyrrolidine compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.
摘要翻译： 公开了作为PDE4的有效和选择性抑制剂的新型吡咯烷化合物及其制备方法。 还公开了化合物在治疗炎性疾病和涉及细胞因子水平升高的其它疾病以及中枢神经系统（CNS）病症中的用途。
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公开(公告)号：US06586467B2
公开(公告)日：2003-07-01
申请号：US09899654
申请日：2001-07-05
申请人： Laurence E. Burgess , John J. Gaudino , Robert D. Groneberg , Mark H. Norman , Martha E. Rodriguez , Xicheng Sun , Eli M. Wallace
发明人： Laurence E. Burgess , John J. Gaudino , Robert D. Groneberg , Mark H. Norman , Martha E. Rodriguez , Xicheng Sun , Eli M. Wallace
IPC分类号： C07C25500
CPC分类号： C07D213/40 , C07C237/22 , C07C311/13 , C07C311/19 , C07C311/29 , C07D209/14 , C07D209/16 , C07D257/04 , C07D307/52
摘要： Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein A, B; R1, R2, R3, R4 and R5 are as defined in the specification. Such compounds are tyrosine phosphatase inhibitors and useful in the treatment or prevention of Type II Diabetes Mellitus. Also encompassed by the invention are formulations comprising the noted compounds, processes for preparing such compounds, a method for treating or preventing Type II Diabetes Mellitus.
摘要翻译： 公开了式I化合物及其药学上可接受的盐和前药，其中A，B; R1，R2，R3，R4和R5如本说明书中所定义。这些化合物是酪氨酸磷酸酶抑制剂，可用于治疗或预防II型糖尿病。 本发明还包括包含所述化合物的制剂，制备这些化合物的方法，治疗或预防II型糖尿病的方法。
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公开(公告)号：US06998416B2
公开(公告)日：2006-02-14
申请号：US10758675
申请日：2004-01-15
申请人： Timothy J. Martins , Kerry W. Fowler , Joshua Odingo , Edward A. Kesicki , Amy Oliver , Laurence E. Burgess , John J. Gaudino , Zachary S. Jones , Bradley J. Newhouse , Stephen T. Schlachter
发明人： Timothy J. Martins , Kerry W. Fowler , Joshua Odingo , Edward A. Kesicki , Amy Oliver , Laurence E. Burgess , John J. Gaudino , Zachary S. Jones , Bradley J. Newhouse , Stephen T. Schlachter
IPC分类号： A61K31/40
CPC分类号： C07D207/08 , A61K31/40 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/06 , C07D417/12 , Y02A50/411
摘要： Novel pyrrolidine compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.
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公开(公告)号：US08026233B2
公开(公告)日：2011-09-27
申请号：US12294550
申请日：2007-03-27
申请人： Mark C. Munson , Kevin W. Hunt , Christopher T. Clark , Ganghyeok Kim , Laurence E. Burgess , James P. Rizzi
发明人： Mark C. Munson , Kevin W. Hunt , Christopher T. Clark , Ganghyeok Kim , Laurence E. Burgess , James P. Rizzi
IPC分类号： C07D403/12 , C07D401/12 , A61K31/416
CPC分类号： C07D403/12 , C07D401/12
摘要： Compounds of formula (I): in which A, B, X, Ar1, R8 and R4 have any of the meanings given in the specification, are inhibitors of p38 useful in the treatment and prevention of various disorders mediated by p38.
摘要翻译： 式（I）化合物：其中A，B，X，Ar 1，R 8和R 4具有本说明书中给出的任何含义，是可用于治疗和预防由p38介导的各种疾病的p38的抑制剂。
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公开(公告)号：US20120101103A1
公开(公告)日：2012-04-26
申请号：US13141675
申请日：2009-12-18
申请人： Adam Cook , Kevin W. Hunt , Robert Kirk Delisle , Todd Romoff , Christopher T. Clark , Ganghyeok Kim , Christopher P. Corrette , George A. Doherty , Laurence E. Burgess
发明人： Adam Cook , Kevin W. Hunt , Robert Kirk Delisle , Todd Romoff , Christopher T. Clark , Ganghyeok Kim , Christopher P. Corrette , George A. Doherty , Laurence E. Burgess
IPC分类号： A61K31/498 , A61K31/497 , A61K31/506 , A61K31/4709 , A61K31/453 , A61K31/444 , A61K31/4433 , A61K31/433 , A61K31/427 , A61K31/428 , A61K31/423 , A61K31/4155 , A61K31/4025 , C07D405/14 , C07D405/12 , C07D417/12 , A61K31/501
CPC分类号： C07D405/12 , C07D405/14 , C07D413/12 , C07D417/12
摘要： Compounds of Formula I: (I) in which A, A1, R1, R7a, R7b, R8 and R10 have the meanings given in the specification, are DP2 receptor inhibitors useful in the treatment of useful in the treatment and prevention of immunologic diseases, allergic diseases such as asthma, allergic rhinitis and atopic dermatitis, and other inflammatory diseases mediated by prostaglandin D2 (PGD2). The compounds of Formula I may also be useful in treating diseases or medical conditions involving the Th2 T cell via production of IL-4, IL-5 and/or IL-13.
摘要翻译： 其中A，A1，R1，R7a，R7b，R8和R10具有本说明书中给出的含义的式I化合物：（I）是可用于治疗和预防免疫疾病的DP2受体抑制剂， 过敏性疾病如哮喘，过敏性鼻炎和特应性皮炎，以及由前列腺素D2（PGD2）介导的其他炎性疾病。 式I化合物还可用于通过产生IL-4，IL-5和/或IL-13来治疗涉及Th2T细胞的疾病或医学病症。
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公开(公告)号：US08785445B2
公开(公告)日：2014-07-22
申请号：US13141675
申请日：2009-12-18
申请人： Adam Cook , Kevin W. Hunt , Robert Kirk Delisle , Todd Romoff , Christopher T. Clark , Ganghyeok Kim , Christopher P. Corrette , George A. Doherty , Laurence E. Burgess
发明人： Adam Cook , Kevin W. Hunt , Robert Kirk Delisle , Todd Romoff , Christopher T. Clark , Ganghyeok Kim , Christopher P. Corrette , George A. Doherty , Laurence E. Burgess
IPC分类号： C07D405/12 , A61K31/4433 , C07D241/20 , A61K31/497 , A61K31/501 , A61P11/06 , A61P27/14 , A61P17/00 , A61P29/00
CPC分类号： C07D405/12 , C07D405/14 , C07D413/12 , C07D417/12
摘要： Compounds of Formula I: (I) in which A, A1, R1, R7a, R7b, R8 and R10 have the meanings given in the specification, are DP2 receptor inhibitors useful in the treatment of useful in the treatment and prevention of immunologic diseases, allergic diseases such as asthma, allergic rhinitis and atopic dermatitis, and other inflammatory diseases mediated by prostaglandin D2 (PGD2). The compounds of Formula I may also be useful in treating diseases or medical conditions involving the Th2 T cell via production of IL-4, IL-5 and/or IL-13.
摘要翻译： 其中A，A1，R1，R7a，R7b，R8和R10具有本说明书中给出的含义的式I化合物：（I）是可用于治疗和预防免疫疾病的DP2受体抑制剂， 过敏性疾病如哮喘，过敏性鼻炎和特应性皮炎，以及由前列腺素D2（PGD2）介导的其他炎性疾病。 式I化合物还可用于通过产生IL-4，IL-5和/或IL-13来治疗涉及Th2T细胞的疾病或医学病症。
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公开(公告)号：US08569522B2
公开(公告)日：2013-10-29
申请号：US13001201
申请日：2009-06-24
申请人： Laurence E. Burgess , Christopher T. Clark , Adam Cook , Christopher P. Corrette , Robert Kirk DeLisle , George A. Doherty , Kevin W. Hunt , Todd T. Romoff
发明人： Laurence E. Burgess , Christopher T. Clark , Adam Cook , Christopher P. Corrette , Robert Kirk DeLisle , George A. Doherty , Kevin W. Hunt , Todd T. Romoff
IPC分类号： C07D311/58 , A61K31/353
CPC分类号： C07D311/58 , C07D311/04 , C07D405/12 , C07D407/12
摘要： Compounds of Formula (I): in which A1, A2, W, L, G, R7a, R7b, R8, R9 and R10 have the meanings given in the specification, are DP2 receptor modulators useful in the treatment of immunologic diseases.
摘要翻译： 式（I）化合物：其中A1，A2，W，L，G，R7a，R7b，R8，R9和R10具有本说明书中给出的含义，是可用于治疗免疫疾病的DP2受体调节剂。
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