公开(公告)号：US07605171B2

公开(公告)日：2009-10-20

申请号：US10575790

申请日：2004-12-13

Applicant: Vincent J. Colandrea ,  George A. Doherty ,  Jeffrey J. Hale ,  Pei Huo ,  Irene E. Legiec ,  Leslie Toth ,  Petr Vachal ,  Lin Yan

Inventor： Vincent J. Colandrea ,  George A. Doherty ,  Jeffrey J. Hale ,  Pei Huo ,  Irene E. Legiec ,  Leslie Toth ,  Petr Vachal ,  Lin Yan

IPC: A61K31/443 ,  A61K31/4245 ,  C07D413/04 ,  C07D271/06

CPC classification number: C07D271/06 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/443 ,  A61K31/506 ,  C07D285/12 ,  C07D413/04 ,  C07D413/10 ,  C07D413/14 ,  C07D417/04

Abstract: The present invention encompasses compounds of Formula I: as well as the pharmaceutically acceptable salts thereof. The compounds are S1P1/Edg1 receptor agonists and thus have immunosuppressive, anti-inflammatory and hemostatic activities by modulating leukocyte trafficking, sequestering lymphocytes in secondary lymphoid tissues, and enhancing vascular integrity. The invention is also directed to pharmaceutical compositions containing such compounds and methods of treatment or prevention.

Abstract translation: 本发明包括式I的化合物及其药学上可接受的盐。 化合物是S1P1 / Edg1受体激动剂，因此通过调节白细胞运输，隔离淋巴细胞在次级淋巴组织中并增强血管完整性具有免疫抑制，抗炎和止血活性。 本发明还涉及含有这些化合物和治疗或预防方法的药物组合物。

公开(公告)号：US07351725B2

公开(公告)日：2008-04-01

申请号：US10500811

申请日：2003-01-14

Applicant: George A. Doherty ,  Zhen Li ,  Jeffrey J. Hale ,  Sander G. Mills

Inventor： George A. Doherty ,  Zhen Li ,  Jeffrey J. Hale ,  Sander G. Mills

IPC: A61K31/4245 ,  A61K31/38 ,  C07D333/22 ,  C07D413/04

CPC classification number: C07D413/04 ,  C07C229/14 ,  C07C229/20 ,  C07C229/22 ,  C07D333/16 ,  C07F9/301 ,  C07F9/307 ,  C07F9/3808 ,  C07F9/4816 ,  C07F9/59 ,  C07F9/655345 ,  C07F9/65586

Abstract: The present invention encompasses compounds of Formula (I) as well as the pharmaceutically acceptable salts and hydrates thereof. The compounds are useful for treating immune mediated diseases and conditions, such as bone marrow, organ and tissue transplant rejection. Pharmaceutical compositions and methods of use are included.

Abstract translation: 本发明包括式（I）的化合物及其药学上可接受的盐和水合物。 该化合物可用于治疗免疫介导的疾病和病症，例如骨髓，器官和组织移植排斥反应。 包括药物组合物和使用方法。

公开(公告)号：US08673898B2

公开(公告)日：2014-03-18

申请号：US13445749

申请日：2012-04-12

Applicant: George A. Doherty ,  Zachary Jones

Inventor： George A. Doherty ,  Zachary Jones

IPC: A61P37/02 ,  A61K31/5513 ,  C07D243/20

CPC classification number: C07D243/20

Abstract: Provided are compositions and methods useful for modulation signaling through the Toll-like receptor TLR8. The compositions and methods have use in the treatment of autoimmunity, inflammation allergy, asthma, graft rejection, graft versus host disease, infection, sepsis, cancer and immunodeficiency.

Abstract translation: 提供了可用于通过Toll样受体TLR8调节信号传导的组合物和方法。 组合物和方法用于治疗自身免疫，炎症过敏，哮喘，移植物排斥，移植物抗宿主病，感染，败血症，癌症和免疫缺陷。

公开(公告)号：US08524702B2

公开(公告)日：2013-09-03

申请号：US12859182

申请日：2010-08-18

Applicant: James Jeffry Howbert ,  Gregory Dietsch ,  Robert Hershberg ,  Laurence E. Burgess ,  George A. Doherty ,  C. Todd Eary ,  Robert D. Groneberg ,  Zachary Jones

Inventor： James Jeffry Howbert ,  Gregory Dietsch ,  Robert Hershberg ,  Laurence E. Burgess ,  George A. Doherty ,  C. Todd Eary ,  Robert D. Groneberg ,  Zachary Jones

IPC: A61P35/00 ,  A61K31/55 ,  C07D223/16

CPC classification number: C07D223/16 ,  A61K31/4025 ,  A61K31/55 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/10 ,  C07D403/14

Abstract: Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, infectious disease, inflammatory disorder, graft rejection, and graft-verses-host disease.

公开(公告)号：US20120208801A1

公开(公告)日：2012-08-16

申请号：US13445749

申请日：2012-04-12

Applicant: George A. Doherty ,  Zachary Jones

Inventor： George A. Doherty ,  Zachary Jones

IPC: A61K31/5513 ,  A61P11/06 ,  A61P37/08 ,  A61P35/00 ,  A61P35/02

CPC classification number: C07D243/20

Abstract: Provided are compositions and methods useful for modulation signaling through the Toll-like receptor TLR8. The compositions and methods have use in the treatment of autoimmunity, inflammation allergy, asthma, graft rejection, graft versus host disease, infection, sepsis, cancer and immunodeficiency.

Abstract translation: 提供了可用于通过Toll样受体TLR8调节信号传导的组合物和方法。 组合物和方法用于治疗自身免疫，炎症过敏，哮喘，移植物排斥，移植物抗宿主病，感染，败血症，癌症和免疫缺陷。

公开(公告)号：US20110124628A1

公开(公告)日：2011-05-26

申请号：US12951344

申请日：2010-11-22

Applicant: Milan Bruncko ,  Hong Ding ,  George A. Doherty ,  Steven W. Elmore ,  Lisa A. Hasvold ,  Laura Hexamer ,  Aaron R. Kunzer ,  Xiaohong Song ,  Andrew J. Souers ,  Gerard M. Sullivan ,  Zhi-Fu Tao ,  Gary T. Wang ,  Le Wang ,  Xilu Wang ,  Michael D. Wendt ,  Robert Mantei ,  Todd M. Hansen

Inventor： Milan Bruncko ,  Hong Ding ,  George A. Doherty ,  Steven W. Elmore ,  Lisa A. Hasvold ,  Laura Hexamer ,  Aaron R. Kunzer ,  Xiaohong Song ,  Andrew J. Souers ,  Gerard M. Sullivan ,  Zhi-Fu Tao ,  Gary T. Wang ,  Le Wang ,  Xilu Wang ,  Michael D. Wendt ,  Robert Mantei ,  Todd M. Hansen

IPC: A61K31/496 ,  C07D471/04 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  A61K31/5377 ,  A61K31/517 ,  A61K31/541 ,  A61P35/00 ,  A61P35/02

CPC classification number: C07D471/04 ,  C07D491/052 ,  C07D519/00

Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.

公开(公告)号：US20100273850A1

公开(公告)日：2010-10-28

申请号：US12739560

申请日：2008-11-04

Applicant: George A. Doherty

Inventor： George A. Doherty

IPC: A61K31/404 ,  C07D209/18 ,  C07D235/16 ,  A61K31/4184 ,  A61P37/00 ,  A61P29/00 ,  A61P11/06 ,  A61P17/06 ,  A61P3/10 ,  A61P9/10 ,  A61P35/00 ,  A61P31/12

CPC classification number: C07D209/08 ,  C07D231/56 ,  C07D235/06 ,  C07D235/08

Abstract: Compounds of Formula I: I in which D1, D2, R1, R2, R7, R8 and A have the meanings given in the specification, are DP2 receptor modulators useful in the treatment of immunologic diseases.

Abstract translation: 其中D1，D2，R1，R2，R7，R8和A具有本说明书中给出的含义的式I化合物是可用于治疗免疫疾病的DP2受体调节剂。

公开(公告)号：US20100160322A1

公开(公告)日：2010-06-24

申请号：US12631367

申请日：2009-12-04

Applicant: Milan Bruncko ,  Yujia Dai ,  Hong Ding ,  George A. Doherty ,  Steven W. Elmore ,  Lisa Hasvold ,  Laura Hexamer ,  Aaron Kunzer ,  Robert A. Mantei ,  William J. McClellan ,  Chang H. Park ,  Cheol-Min Park ,  Andrew M. Petros ,  Xiaohong Song ,  Andrew J. Souers ,  Gerard M. Sullivan ,  Zhi-Fu Tao ,  Gary T. Wang ,  Le Wang ,  Xilu Wang ,  Michael D. Wendt

Inventor： Milan Bruncko ,  Yujia Dai ,  Hong Ding ,  George A. Doherty ,  Steven W. Elmore ,  Lisa Hasvold ,  Laura Hexamer ,  Aaron Kunzer ,  Robert A. Mantei ,  William J. McClellan ,  Chang H. Park ,  Cheol-Min Park ,  Andrew M. Petros ,  Xiaohong Song ,  Andrew J. Souers ,  Gerard M. Sullivan ,  Zhi-Fu Tao ,  Gary T. Wang ,  Le Wang ,  Xilu Wang ,  Michael D. Wendt

IPC: A61K31/5377 ,  C07D405/02 ,  A61K31/496 ,  C07D403/02 ,  C07D401/02 ,  C07D413/02 ,  A61P35/00

CPC classification number: C07D209/08 ,  A61K31/635 ,  C07D211/58 ,  C07D213/74 ,  C07D213/84 ,  C07D231/56 ,  C07D235/06 ,  C07D277/24 ,  C07D295/30 ,  C07D309/04 ,  C07D309/08 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  Y02A50/401 ,  Y02A50/409 ,  Y02A50/411

Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.

公开(公告)号：US07479504B2

公开(公告)日：2009-01-20

申请号：US10500895

申请日：2003-01-15

Applicant: Robert L. Bugianesi ,  George A. Doherty ,  Amy Gentry ,  Jeffrey J. Hale ,  Christopher L. Lynch ,  Sander G. Mills ,  William E. Neway, III

Inventor： Robert L. Bugianesi ,  George A. Doherty ,  Amy Gentry ,  Jeffrey J. Hale ,  Christopher L. Lynch ,  Sander G. Mills ,  William E. Neway, III

IPC: A61K31/4025 ,  C07D205/04 ,  C07D409/12

CPC classification number: C07D403/04 ,  C07D205/04 ,  C07D207/16 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/10 ,  C07D413/14 ,  C07F9/572 ,  C07F9/65586

Abstract: The present invention encompasses compounds of Formula 1: as well as the pharmaceutically acceptable salts and hydrates thereof. The compounds are useful for treating immune mediated diseases and conditions, such as bone marrow, organ and tissue transplant rejection. Pharmaceutical compositions and methods of use are included.

Abstract translation: 本发明包括式1的化合物及其药学上可接受的盐和水合物。 该化合物可用于治疗免疫介导的疾病和病症，例如骨髓，器官和组织移植排斥反应。 包括药物组合物和使用方法。

公开(公告)号：US20080234251A1

公开(公告)日：2008-09-25

申请号：US12064193

申请日：2006-08-17

Applicant: George A. Doherty ,  C. Todd Eary ,  Robert D. Groneberg ,  Zachary Jones

Inventor： George A. Doherty ,  C. Todd Eary ,  Robert D. Groneberg ,  Zachary Jones

IPC: A61K31/55 ,  C07D223/16 ,  A61P37/00

CPC classification number: C07D223/16

Abstract: Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in the treatment of autoimmunity, inflammation allergy, asthma, graft rejection, graft versus host disease, infection, sepsis, cancer and immunodeficiency.

Abstract translation: 提供了可用于通过Toll样受体TLR7和/或TLR8调节信号传导的组合物和方法。 组合物和方法用于治疗自身免疫，炎症过敏，哮喘，移植物排斥，移植物抗宿主病，感染，败血症，癌症和免疫缺陷。