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。

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.

公开(公告)号：US06716871B2

公开(公告)日：2004-04-06

申请号：US10151202

申请日：2002-05-17

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： A61K3140

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。

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.

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。

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。

公开(公告)号：US07553842B2

公开(公告)日：2009-06-30

申请号：US11334858

申请日：2006-01-19

申请人： Stephen T. Schlacter ,  John J. Gaudino ,  Laurence E. Burgess ,  Kevin W. Hunt

发明人： Stephen T. Schlacter ,  John J. Gaudino ,  Laurence E. Burgess ,  Kevin W. Hunt

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。

公开(公告)号：US06362213B1

公开(公告)日：2002-03-26

申请号：US09737987

申请日：2000-12-15

申请人： John J. Gaudino

发明人： John J. Gaudino

IPC分类号： A61K31415

CPC分类号： C07D403/04

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.

公开(公告)号：US06444671B1

公开(公告)日：2002-09-03

申请号：US10002867

申请日：2001-11-15

申请人： John J. Gaudino

发明人： John J. Gaudino

IPC分类号： C07D41314

CPC分类号： C07D403/04

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.

公开(公告)号：US09133187B2

公开(公告)日：2015-09-15

申请号：US14002079

申请日：2012-02-28

申请人： James F. Blake ,  Huifen Chen ,  Mark Joseph Chicarelli ,  Jason Demeese ,  Rustam Garrey ,  John J. Gaudino ,  Robert J. Kaus ,  Gabrielle R. Kolakowski ,  Allison L. Marlow ,  Peter J. Mohr ,  Li Ren ,  Jacob Schwarz ,  Christopher S. Siedem ,  Allen A. Thomas ,  Eli Wallace ,  Steven Mark Wenglowsky ,  Steven Boyd

发明人： James F. Blake ,  Huifen Chen ,  Mark Joseph Chicarelli ,  Jason Demeese ,  Rustam Garrey ,  John J. Gaudino ,  Robert J. Kaus ,  Gabrielle R. Kolakowski ,  Allison L. Marlow ,  Peter J. Mohr ,  Li Ren ,  Jacob Schwarz ,  Christopher S. Siedem ,  Allen A. Thomas ,  Eli Wallace ,  Steven Mark Wenglowsky ,  Steven Boyd

IPC分类号： A01N43/90 ,  A61K31/519 ,  C07D487/00 ,  C07D471/04 ,  C07D491/052 ,  A61K45/06

CPC分类号： C07D471/04 ,  A61K31/519 ,  A61K45/06 ,  C07D491/052

摘要： Compounds having the formula I wherein Z, Z1 Z2 Z3, R3a, R3b and Rb and as defined herein are inhibitors of ERK kinase. Also disclosed are compositions and methods for treating hyperproliferative disorders.

摘要翻译： 具有式I的化合物，其中Z，Z 1 Z 2 Z 3，R 3a，R 3b和R b如本文所定义是ERK激酶的抑制剂。 还公开了用于治疗过度增殖性疾病的组合物和方法。