公开(公告)号：US08153622B2

公开(公告)日：2012-04-10

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: A61P37/00 ,  A61K31/55 ,  C07D223/16 ,  C07D403/10

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.

公开(公告)号：US08088766B2

公开(公告)日：2012-01-03

申请号：US12209738

申请日：2008-09-12

Applicant: Eli Wallace ,  George Topolov ,  Qian Zhao ,  Joseph P. Lyssikatos

Inventor： Eli Wallace ,  George Topolov ,  Qian Zhao ,  Joseph P. Lyssikatos

IPC: C07D239/94 ,  C07D295/125 ,  A61K31/517 ,  A61K31/422 ,  C07D215/44 ,  A61K31/4706

CPC classification number: C07D401/12 ,  C07D239/94 ,  C07D403/12 ,  C07D405/04 ,  C07D417/14

Abstract: Cyanoguanidine quinazoline and cyanoamidine quinazolamine derivatives that are useful in the treatment of hyperproliferative diseases are disclosed. Methods of treating hyperproliferative diseases in mammals are also disclosed.

Abstract translation: 公开了可用于治疗过度增生性疾病的氰氮基喹唑啉和氰基脒喹唑啉衍生物。 还公开了治疗哺乳动物过度增殖性疾病的方法。

公开(公告)号：US20110281874A1

公开(公告)日：2011-11-17

申请号：US13191994

申请日：2011-07-27

Applicant: Thomas D. AICHER ,  Steven Armen BOYD ,  Mark Joseph CHICARELLI ,  Kevin Ronald CONDROSKI ,  Ronald Jay HINKLIN ,  Ajay SINGH

Inventor： Thomas D. AICHER ,  Steven Armen BOYD ,  Mark Joseph CHICARELLI ,  Kevin Ronald CONDROSKI ,  Ronald Jay HINKLIN ,  Ajay SINGH

IPC: A61K31/5377 ,  A61K31/497 ,  A61K31/519 ,  A61K31/506 ,  A61K31/437 ,  A61P3/10 ,  A61K31/4439 ,  C07D495/04 ,  C07D471/04 ,  C07D417/14 ,  C07D498/04 ,  C07D417/12 ,  A61K31/496 ,  A61K31/4545

CPC classification number: C07D417/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04 ,  C07D513/04

Abstract: Provided are compounds that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.

Abstract translation: 提供了可用于治疗和/或预防由缺乏水平的葡糖激酶活性（例如糖尿病）介导的疾病的化合物。 还提供了治疗或预防以葡萄糖激酶不足活性为特征的疾病和病症的方法，或者可以通过激活葡糖激酶治疗。

公开(公告)号：US08017641B2

公开(公告)日：2011-09-13

申请号：US12364310

申请日：2009-02-02

Applicant: Mark Munson ,  David A. Mareska ,  Youngboo Kim ,  Robert D. Gronenberg ,  James P. Rizzi ,  Martha Rodriguez ,  Ganghyeok Kim ,  Guy Vigers ,  Chang Rao ,  Devan Balachari ,  Darren Harvey

Inventor： Mark Munson ,  David A. Mareska ,  Youngboo Kim ,  Robert D. Gronenberg ,  James P. Rizzi ,  Martha Rodriguez ,  Ganghyeok Kim ,  Guy Vigers ,  Chang Rao ,  Devan Balachari ,  Darren Harvey

IPC: A61K31/415 ,  C07D231/56

CPC classification number: C07D401/14 ,  C07D231/56 ,  C07D261/20 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D471/04

Abstract: This invention relates to inhibitors of p38 and methods of utilizing the inhibitors and pharmaceutical compositions thereof in the treatment and prevention of various disorders mediated by p38.

Abstract translation: 本发明涉及p38的抑制剂和利用该抑制剂及其药物组合物治疗和预防由p38介导的各种疾病的方法。

公开(公告)号：US20110195948A1

公开(公告)日：2011-08-11

申请号：US13125263

申请日：2009-10-21

Applicant: Julia Haas ,  Steven W. Andrews ,  Yutong Jiang ,  Gan Zhang

Inventor： Julia Haas ,  Steven W. Andrews ,  Yutong Jiang ,  Gan Zhang

IPC: A61K31/397 ,  C07D487/04 ,  A61K31/519 ,  C07D413/14 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/497 ,  A61K31/496 ,  A61P29/00 ,  A61P35/00 ,  A61P31/00 ,  A61P25/04

CPC classification number: C07D487/04 ,  A61K9/0053 ,  A61K31/519 ,  A61K31/5377 ,  A61K45/06 ,  A61P29/00 ,  C07D471/04 ,  C07D519/00

Abstract: Compounds of Formula (I) in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification, are inhibitors of Trk kinases and are useful in the treatment of diseases which can be treated with a Trk kinase inhibitor.

Abstract translation: 其中R1，R2，R3，R4，X，Y和n具有本说明书中给出的含义的式（I）化合物是Trk激酶的抑制剂，可用于治疗可用Trk激酶治疗的疾病 抑制剂。

公开(公告)号：US20110160221A1

公开(公告)日：2011-06-30

申请号：US12667850

申请日：2008-07-03

Applicant: Josef R. Bencsik ,  James F. Blake ,  Nicholas C. Kallan ,  Ian S. Mitchell ,  Keith L. Spencer ,  Dengming Xiao ,  Rui Xu ,  Christine Chabot ,  Jun Liang ,  Brian S. Safina

Inventor： Josef R. Bencsik ,  James F. Blake ,  Nicholas C. Kallan ,  Ian S. Mitchell ,  Keith L. Spencer ,  Dengming Xiao ,  Rui Xu ,  Christine Chabot ,  Jun Liang ,  Brian S. Safina

IPC: A61K31/497 ,  C07D239/70 ,  A61P35/00

CPC classification number: C07D239/70 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12

Abstract: The present invention provides compounds of Formula I, including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

Abstract translation: 本发明提供了式I化合物，包括互变异构体，拆分的对映异构体，非对映异构体，溶剂合物，代谢物，盐和药学上可接受的前药。 还提供了使用本发明化合物作为AKT蛋白激酶抑制剂和治疗过度增殖性疾病如癌症的方法。

公开(公告)号：US20110144085A1

公开(公告)日：2011-06-16

申请号：US13059902

申请日：2009-08-18

Applicant: Shelley Allen ,  Laura L. Celeste ,  T. Gregg Davis ,  Robert Kirk DeLisle ,  Julie Marie Greschuk ,  Stefan D. Gross ,  Erik James Hicken ,  Leila J. Jackson ,  Nicholas C. Kallan ,  Joseph P. Lyssikatos ,  Fredrik P. Marmsater ,  Mark C. Munson ,  Jed Pheneger ,  Bryson Rast ,  John E. Robinson ,  Stephen T. Schlachter ,  George T. Topalov ,  A. Dale Wright ,  Qian Zhao

Inventor： Shelley Allen ,  Laura L. Celeste ,  T. Gregg Davis ,  Robert Kirk DeLisle ,  Julie Marie Greschuk ,  Stefan D. Gross ,  Erik James Hicken ,  Leila J. Jackson ,  Nicholas C. Kallan ,  Joseph P. Lyssikatos ,  Fredrik P. Marmsater ,  Mark C. Munson ,  Jed Pheneger ,  Bryson Rast ,  John E. Robinson ,  Stephen T. Schlachter ,  George T. Topalov ,  A. Dale Wright ,  Qian Zhao

IPC: A61K31/55 ,  C07D471/04 ,  A61K31/437 ,  A61K31/513 ,  A61K31/5377 ,  A61P35/00 ,  A61P25/00 ,  A61P29/00

CPC classification number: C07D471/04

Abstract: Compounds of Formula (I), in which A, B, R1, R1a, R2, R3, R4, R5, R6, and R7 have the meanings given in the specification, are receptor tyrosine inhibitors useful in the treatment of immune cell-associated diseases and disorders, such as inflammatory and autoimmune diseases.

Abstract translation: 其中A，B，R1，R1a，R2，R3，R4，R5，R6和R7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细胞相关的受体酪氨酸抑制剂 疾病和病症，例如炎性和自身免疫性疾病。

公开(公告)号：US20110092485A1

公开(公告)日：2011-04-21

申请号：US12859178

申请日：2010-08-18

Applicant: James Jeffry Howbert ,  Gregory Dietsch ,  Robert Hershberg ,  Laurence E. Burgess ,  Joseph P. Lyssikatos ,  Brad Newhouse ,  Hong Woon Yang

Inventor： James Jeffry Howbert ,  Gregory Dietsch ,  Robert Hershberg ,  Laurence E. Burgess ,  Joseph P. Lyssikatos ,  Brad Newhouse ,  Hong Woon Yang

IPC: A61K31/55 ,  C07D223/16 ,  A61P11/06 ,  A61P37/02 ,  A61P35/00

CPC classification number: A61K31/55 ,  C07D223/14 ,  C07D223/16 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D405/04 ,  C07D405/10

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：US20110015204A1

公开(公告)日：2011-01-20

申请号：US12667848

申请日：2008-07-03

Applicant: Josef Bencsik ,  James F. Blake ,  James M. Graham ,  Martin F. Hentemann ,  Nicholas C. Kallan ,  Ian S. Mitchell ,  Stephen T. Schlachter ,  Keith L. Spencer ,  Dengming Xiao ,  Rui Xu ,  Mike Welch ,  Jun Liang ,  Brian S. Safina

Inventor： Josef Bencsik ,  James F. Blake ,  James M. Graham ,  Martin F. Hentemann ,  Nicholas C. Kallan ,  Ian S. Mitchell ,  Stephen T. Schlachter ,  Keith L. Spencer ,  Dengming Xiao ,  Rui Xu ,  Mike Welch ,  Jun Liang ,  Brian S. Safina

IPC: A61K31/497 ,  C07D239/70 ,  A61P35/00

CPC classification number: C07D403/12 ,  C07D401/12

Abstract: The present invention provides compounds of Formula (I), including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

Abstract translation: 本发明提供式（I）化合物，其包括互变异构体，拆分的对映异构体，非对映异构体，溶剂合物，代谢物，盐和药学上可接受的前药。 还提供了使用本发明化合物作为AKT蛋白激酶抑制剂和治疗过度增殖性疾病如癌症的方法。

公开(公告)号：US20110003859A1

公开(公告)日：2011-01-06

申请号：US12919972

申请日：2009-02-27

Applicant: Kateri A. Ahrendt

Inventor： Kateri A. Ahrendt

IPC: A61K31/444 ,  C07D213/02 ,  C07D401/04 ,  C07D213/04 ,  C07D417/04 ,  C07D405/04 ,  A61K31/4439 ,  A61K31/443 ,  A61K31/4427 ,  A61K31/44 ,  A61P35/00 ,  A61P35/02

CPC classification number: C07D213/75 ,  C07C311/48 ,  C07D213/80 ,  C07D213/82 ,  C07D213/85 ,  C07D401/04 ,  C07D401/06 ,  C07D405/04 ,  C07D417/04

Abstract: Compounds of Formula (I) are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

Abstract translation: 式（I）的化合物可用于抑制Raf激酶。 公开了使用式I化合物及其立体异构体及其药学上可接受的盐在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。