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31. 发明申请

US20080275067A1 Quinazolinones as Inhibitors of Human Phosphatidylinositol 3-Kinase Delta 有权
标题翻译：喹唑啉酮作为人磷脂酰肌醇3-激酶三角体抑制剂
公开(公告)号：US20080275067A1
公开(公告)日：2008-11-06
申请号：US11596092
申请日：2005-05-12
申请人： Kerry W. Fowler , Danwen Huang , Edward A. Kesicki , Hua Chee Ooi , Amy R. Oliver , Ruan Fuqiang , Jennifer Treiberg
发明人： Kerry W. Fowler , Danwen Huang , Edward A. Kesicki , Hua Chee Ooi , Amy R. Oliver , Ruan Fuqiang , Jennifer Treiberg
IPC分类号： A61K31/52 , C07D487/04 , C12N9/99 , A61P19/02 , C12N5/06 , A61K31/519
CPC分类号： C07D473/34 , A61K31/52 , C07D239/91 , C07D473/16 , C07D487/04
摘要： Compounds that inhibit PI3Kδ activity, including compounds that selectively inhibit PI3Kδ activity, are disclosed. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which PI3Kδ plays a role in leukocyte function, using the compounds also are disclosed.
摘要翻译：公开了抑制PI3Kdelta活性的化合物，包括选择性抑制PI3Kdelta活性的化合物。公开了抑制磷脂酰肌醇3-激酶δ同种型（PI3Kdelta）活性的方法，以及使用该化合物治疗诸如PI3Kdelta在白细胞功能中起作用的免疫力和炎症疾病等疾病的方法。

32. 发明授权

US06569890B2 Cyclic AMP-specific phosphodiesterase inhibitors 失效
公开(公告)号：US06569890B2
公开(公告)日：2003-05-27
申请号：US10054273
申请日：2002-01-22
申请人： Timothy J. Martins , Kerry W. Fowler , Amy Oliver , Carmen C. Hertel
发明人： Timothy J. Martins , Kerry W. Fowler , Amy Oliver , Carmen C. Hertel
IPC分类号： A61K31402
CPC分类号： C07D401/04 , C07D207/34
摘要： Pyrrole 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.

33. 发明授权

US06313156B1 Thiazole compounds as cyclic-AMP-specific phosphodiesterase inhibitors 失效
标题翻译：噻唑化合物作为环状AMP特异性磷酸二酯酶抑制剂
公开(公告)号：US06313156B1
公开(公告)日：2001-11-06
申请号：US09723091
申请日：2000-11-27
申请人： Kerry W. Fowler , Joshua Odingo
发明人： Kerry W. Fowler , Joshua Odingo
IPC分类号： A61K31427
CPC分类号： C07D417/04
摘要： Novel 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。

34. 发明授权

US06258833B1 Cyclic AMP-specific phosphodiesterase inhibitors 有权
标题翻译：环AMP特异性磷酸二酯酶抑制剂
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。

35. 发明授权

US5247119A Phenylacetonitrilehydroxyalkylaminoalkyl-ortho-substituted aryl compounds as immunosuppressives 失效
标题翻译：苯基乙腈 - 羟基烷基氨基烷基邻位取代的芳基化合物作为免疫抑制剂
公开(公告)号：US5247119A
公开(公告)日：1993-09-21
申请号：US889733
申请日：1992-05-28
申请人： Kerry W. Fowler , John M. Farah, Jr. , John P. McKearn , Richard A. Mueller , Susan A. Gregory
发明人： Kerry W. Fowler , John M. Farah, Jr. , John P. McKearn , Richard A. Mueller , Susan A. Gregory
IPC分类号： C07C255/43
CPC分类号： C07C255/43
摘要： A class of substituted phenylacetonitrilehydroxyalkylaminoalkyl-ortho-substituted aryl compounds having immunosuppressive properties is described. Compounds of this class would be useful in reducing recipient rejection of transplanted organs and for treatment of autoimmune or inflammatory diseases. Compounds of particular interest are of the formula ##STR1## wherein each of m and n is a number independently selected from one to five, inclusive; wherein R.sup.1 is selected from hydrido, alkyl, hydroxyalkyl, cycloalkyl, cycloalkylalkyl, alkoxyalkyl, alkenyl and alkynyl; wherein R.sup.6 is selected from loweralkyl; wherein each of R.sup.8, R.sup.9, R.sup.10 and R.sup.12 through R.sup.16 is independently selected from hydrido, hydroxy, alkyl, hydroxyalkyl, alkoxy, alkenyl, alkynyl, alkylcarbonyl, alkoxycarbonyl, alkylcarbonylalkenyl, alkylaminocarbonyl and alkoxyalkyl; or a tautomer thereof or a pharmaceutically-acceptable salt thereof.
摘要翻译：描述了一类具有免疫抑制特性的取代苯乙腈羟烷基氨基烷基邻位取代芳基化合物。该类化合物可用于减少移植器官的受体排斥和治疗自身免疫性或炎性疾病。特别感兴趣的化合物具有式“IMAGE”，其中m和n各自独立地选自1至5个，包括1和5; 其中R1选自氢化，烷基，羟基烷基，环烷基，环烷基烷基，烷氧基烷基，烯基和炔基; 其中R 6选自低级烷基; 其中R8，R9，R10和R12至R16各自独立地选自氢，羟基，烷基，羟基烷基，烷氧基，烯基，炔基，烷基羰基，烷氧基羰基，烷基羰基烯基，烷基氨基羰基和烷氧基烷基; 或其互变异构体或其药学上可接受的盐。

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