公开(公告)号：US08835434B2

公开(公告)日：2014-09-16

申请号：US12811957

申请日：2009-01-09

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

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

IPC: A61K31/517 ,  C07D403/04 ,  A61P35/00 ,  A61P25/28 ,  A61P9/00 ,  A61P29/00 ,  A61P15/00 ,  C07D239/70

CPC classification number: C07D239/70

Abstract: The present invention provides compounds, including pharmaceutically acceptable salts thereof, comprising the Formula (I): 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: 本发明提供包含式（I）的化合物，包括其药学上可接受的盐：还提供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：US20140221342A1

公开(公告)日：2014-08-07

申请号：US14231356

申请日：2014-03-31

Applicant: Array BioPharma Inc.

Inventor： Laurence E. Burgess ,  Christopher T. Clark ,  Adam Cook ,  Christopher P. Corrette ,  Robert Kirk DeLisle ,  George A. Doherty ,  Kevin W. Hunt ,  Todd T. Romoff ,  Ganghyeok Kim

IPC: C07D311/58 ,  C07D407/12 ,  C07D405/12

CPC classification number: C07D311/58 ,  C07D311/04 ,  C07D405/12 ,  C07D407/12

Abstract: Provided herein is a method of treating an allergic inflammatory disease selected from asthma, dermatitis, allergic rhinitis, urticaria, anaphylaxis, angioedemea, allergies, contact hypersensitivity, drug hypersensitivity, and allergic conjunctivitis in a mammal, comprising administering a therapeutically effective amount of a compound of Formula I or a pharmaceutically acceptable salt thereof, to said mammal in need thereof, wherein A1, A2, W, L, G, R7a, R7b, R8, R9 and R10 are as defined herein.

Abstract translation: 本文提供了一种治疗哺乳动物中选自哮喘，皮炎，过敏性鼻炎，荨麻疹，过敏反应，血管紧张素，过敏，接触超敏反应，药物过敏和过敏性结膜炎的过敏性炎性疾病的方法，包括给予治疗有效量的化合物 其中A1，A2，W，L，G，R7a，R7b，R8，R9和R10如本文所定义。

公开(公告)号：US20140142086A1

公开(公告)日：2014-05-22

申请号：US14016951

申请日：2013-09-03

Applicant: ARRAY BIOPHARMA, INC. ,  VENTIRX PHARMACEUTICALS, INC.

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

IPC: C07D403/14 ,  C07D223/16 ,  C07D401/04 ,  C07D403/04 ,  C07D403/10 ,  C07D401/14

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：US20140088085A1

公开(公告)日：2014-03-27

申请号：US13979634

申请日：2012-01-12

Applicant: Laurence E. Burgess ,  George A. Doherty ,  C. Todd Eary ,  Robert D. Groneberg ,  Zachary Jones ,  James Jeffry Howbert ,  Robert Hershberg ,  Joseph P. Lyssikatos ,  Hong Woon Yang

Inventor： Laurence E. Burgess ,  George A. Doherty ,  C. Todd Eary ,  Robert D. Groneberg ,  Zachary Jones ,  James Jeffry Howbert ,  Robert Hershberg ,  Joseph P. Lyssikatos ,  Hong Woon Yang

IPC: C07D223/16 ,  C07D243/14 ,  C07D487/04 ,  C07D401/12

CPC classification number: C07D223/16 ,  C07D243/14 ,  C07D401/12 ,  C07D487/04

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, fibrotic disease, cardiovascular disease, infectious disease, inflammatory disorder, graft rejection, or graft-versus-host disease.

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。 组合物和方法可用于治疗或预防疾病，包括癌症，自身免疫性疾病，纤维化疾病，心血管疾病，感染性疾病，炎症性疾病，移植排斥反应或移植物抗宿主病。

公开(公告)号：US20140023643A1

公开(公告)日：2014-01-23

申请号：US14034361

申请日：2013-09-23

Applicant: ARRAY BIOPHARMA, INC.

Inventor： Joseph P. LYSSIKATOS ,  Julie Marie GRESCHUK ,  Fredrik P. MARMSATER ,  Qian ZHAO ,  D. David HENNINGS ,  Weidong LIU

IPC: C07D471/04 ,  A61K39/395 ,  A61K31/337 ,  A61K31/517 ,  A61K31/513

CPC classification number: A61K31/337 ,  A61K31/513 ,  A61K31/517 ,  A61K39/3955 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07D519/00

Abstract: This invention provides compounds of Formula I wherein B, G, A, E, R1, R2, R3, m and n are as defined herein, which are useful as type I receptor tyrosine kinase inhibitors, and methods of use thereof in the treatment of hyperproliferative disorders in mammals.

Abstract translation: 本发明提供式I化合物，其中B，G，A，E，R 1，R 2，R 3，m和n如本文所定义，其可用作I型受体酪氨酸激酶抑制剂，及其用于治疗 哺乳动物过度增生性疾病。

公开(公告)号：US08623895B2

公开(公告)日：2014-01-07

申请号：US13538698

申请日：2012-06-29

Applicant: Jeremy Hans ,  Eli M. Wallace ,  Qian Zhao ,  Joseph P. Lyssikatos ,  Thomas D. Aicher ,  Ellen R Laird ,  John Robinson ,  Shelley Allen

Inventor： Jeremy Hans ,  Eli M. Wallace ,  Qian Zhao ,  Joseph P. Lyssikatos ,  Thomas D. Aicher ,  Ellen R Laird ,  John Robinson ,  Shelley Allen

IPC: A61K31/433 ,  A61K31/4439 ,  C07D417/12 ,  C07D285/12

CPC classification number: C07D285/12 ,  C07D271/107 ,  C07D401/12 ,  C07D413/04 ,  C07D413/06 ,  C07D413/12 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07F9/201 ,  C07F9/65392

Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.

Abstract translation: 本发明涉及有丝分裂驱动蛋白抑制剂，特别是KSP，以及制备这些抑制剂的方法。 本发明还提供包含本发明抑制剂的药物组合物和利用抑制剂和药物组合物治疗和预防各种疾病的方法。

公开(公告)号：US08580828B2

公开(公告)日：2013-11-12

申请号：US13586355

申请日：2012-08-15

Applicant: Jeremy Hans ,  Eli M. Wallace ,  Qian Zhao ,  Shelley Allen ,  Ellen Laird ,  Joseph P. Lyssikatos ,  John E. Robinson ,  Christopher P. Corrette ,  Robert Kirk DeLisle ,  Walter C. Voegtil

Inventor： Jeremy Hans ,  Eli M. Wallace ,  Qian Zhao ,  Shelley Allen ,  Ellen Laird ,  Joseph P. Lyssikatos ,  John E. Robinson ,  Christopher P. Corrette ,  Robert Kirk DeLisle ,  Walter C. Voegtil

IPC: A61K31/41 ,  C07D417/04

CPC classification number: C07D513/04 ,  C07D285/12 ,  C07D417/04 ,  C07D417/14 ,  C07D419/04 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D497/04 ,  C07F9/65395

Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.

公开(公告)号：US08575145B2

公开(公告)日：2013-11-05

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 ,  A61K31/437 ,  A61K31/513 ,  A61K31/5377 ,  C07D471/04 ,  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：US08545897B2

公开(公告)日：2013-10-01

申请号：US13425186

申请日：2012-03-20

Applicant: Yvan Le Huerou ,  James F. Blake ,  Indrani W. Gunwardana ,  Pete Mohr ,  Eli M. Wallace ,  Bin Wang ,  Mark Joseph Chicarelli ,  Michael Lyon

Inventor： Yvan Le Huerou ,  James F. Blake ,  Indrani W. Gunwardana ,  Pete Mohr ,  Eli M. Wallace ,  Bin Wang ,  Mark Joseph Chicarelli ,  Michael Lyon

IPC: A61K31/4545 ,  A61K31/437 ,  A61K31/497 ,  A61K31/506 ,  A61K33/24 ,  A61K31/513 ,  A61K31/444 ,  A61K31/501 ,  A61P35/00

CPC classification number: C07D471/04 ,  C07D401/06 ,  C07D519/00

Abstract: Compounds of Formula I are useful for inhibition of CHK1 and/or CHK2. 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.

公开(公告)号：US20130231301A1

公开(公告)日：2013-09-05

申请号：US13885644

申请日：2011-11-16

Applicant: Kurtis D. Davies ,  Stefan Gross

Inventor： Kurtis D. Davies ,  Stefan Gross

IPC: A61K45/06 ,  A61K31/437 ,  A61K31/7068

CPC classification number: A61K31/4545 ,  A61K31/437 ,  A61K31/4745 ,  A61K31/495 ,  A61K31/519 ,  A61K31/551 ,  A61K31/7068 ,  A61K45/06 ,  A61K2300/00

Abstract: A combination of a CHK1 inhibitor and a WEE1 inhibitor are provided.

Abstract translation: 提供CHK1抑制剂和WEE1抑制剂的组合。