公开(公告)号：US20160280682A1

公开(公告)日：2016-09-29

申请号：US14442613

申请日：2013-11-12

Applicant: ARRAY BIOPHARMA INC.

Inventor： Shelley Allen ,  Barbara J. Brandhuber ,  Timothy Kercher ,  Gabrielle R. Kolakowski ,  Shannon L. Winski

IPC: C07D401/14 ,  C07D403/12 ,  C07D403/14

CPC classification number: C07D401/14 ,  A61P29/00 ,  A61P35/00 ,  C07D403/12 ,  C07D403/14

Abstract: Compounds of Formula (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts, or solvates or prodrugs thereof, where R1, R2, Ra, Rb, Rc, Rd, X, Ring B, and Ring C are as defined herein, and wherein Ring B and the NH—C(═X)—NH moiety are in the trans configuration, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis or pelvic pain syndrome.

公开(公告)号：US20160122316A1

公开(公告)日：2016-05-05

申请号：US14993985

申请日：2016-01-12

Applicant: ARRAY BIOPHARMA INC. ,  GENENTECH, INC.

Inventor： James F. Blake ,  Mark Joseph Chicarelli ,  Rustam Ferdinand Garrey ,  John Gaudino ,  Jonas Grina ,  David A. Moreno ,  Peter J. Mohr ,  Li Ren ,  Jacob Schwarz ,  Huifen Chen ,  Kirk Robarge ,  Aihe Zhou

IPC: C07D401/04 ,  C07D409/14 ,  C07D413/14 ,  C07D405/14 ,  C07D401/14

CPC classification number: C07D401/04 ,  A61K31/444 ,  A61K31/506 ,  A61K31/513 ,  A61K31/53 ,  A61K45/06 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07F9/65586

Abstract: Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative, pain and inflammatory diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt 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：US09328091B2

公开(公告)日：2016-05-03

申请号：US14523481

申请日：2014-10-24

Applicant: Array BioPharma Inc. ,  Genentech, Inc.

Inventor： Anna Leivers ,  Josef R. Bencsik ,  James F. Blake ,  Martin F. Hentemann ,  Nicholas C. Kallan ,  Jun Liang ,  Ian S. Mitchell ,  Stephen T. Schlachter ,  Eli M. Wallace ,  Rui Xu ,  Tony P. Tang

IPC: C07D239/70 ,  C07D401/10 ,  C07D401/04 ,  C07D409/04 ,  C07D417/04 ,  C07D487/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/10 ,  C07D417/10 ,  C07D211/08 ,  C07D211/46

CPC classification number: C07D401/10 ,  C07D211/08 ,  C07D211/46 ,  C07D239/70 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/10 ,  C07D409/04 ,  C07D417/04 ,  C07D417/10 ,  C07D487/04

Abstract: Compounds of Formula I are useful for inhibiting AKT protein 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化合物可用于抑制AKT蛋白激酶。 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。

公开(公告)号：US20150322061A1

公开(公告)日：2015-11-12

申请号：US14591691

申请日：2015-01-07

Applicant: Array BioPharma Inc.

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

IPC: C07D471/04

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.

Abstract translation: 式I的化合物可用于抑制CHK1和/或CHK2。 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。

公开(公告)号：US09126940B2

公开(公告)日：2015-09-08

申请号：US14180939

申请日：2014-02-14

Applicant: VentiRx Pharmaceuticals, Inc. ,  Array BioPharma, Inc.

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

IPC: A01N43/00 ,  A61K31/55 ,  C07D223/16 ,  C07D223/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D401/04 ,  C07D405/04 ,  C07D405/10

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.

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，感染性疾病，炎性疾病，移植物排斥反应和移植物宿主病。

公开(公告)号：US20150231117A1

公开(公告)日：2015-08-20

申请号：US14421766

申请日：2013-08-13

Applicant: Array BioPharma Inc.

Inventor： Karin Brown ,  Ronald B. Franklin ,  Gary P. Hingorani ,  Kevin S. Litwiler ,  Brian J. Tunquist ,  Duncan H. Walker

IPC: A61K31/433 ,  A61K38/05 ,  G01N33/574 ,  A61K31/454 ,  A61K38/19 ,  A61K31/573 ,  A61K38/07

CPC classification number: A61K31/433 ,  A61K31/45 ,  A61K31/454 ,  A61K31/4965 ,  A61K31/5377 ,  A61K31/573 ,  A61K38/05 ,  A61K38/07 ,  A61K38/193 ,  G01N33/57488 ,  G01N2333/4728 ,  A61K2300/00

Abstract: The compound ARRY-520 for use for treating cancer in patients with low [AAG] is provided.

Abstract translation: 提供了用于治疗低[AAG]患者癌症的化合物ARRY-520。

公开(公告)号：US20150210658A1

公开(公告)日：2015-07-30

申请号：US14679866

申请日：2015-04-06

Applicant: ARRAY BIOPHARMA INC.

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

IPC: C07D285/12 ,  C07D417/12 ,  C07F9/201 ,  C07D417/06

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：US20150191490A1

公开(公告)日：2015-07-09

申请号：US14663286

申请日：2015-03-19

Applicant: Array BioPharma Inc.

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. Voegtli

IPC: C07D513/04 ,  C07D285/12 ,  C07D417/04 ,  C07D419/04 ,  C07D497/04

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.

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：US08933084B2

公开(公告)日：2015-01-13

申请号：US13698922

申请日：2011-05-13

Applicant: Steven Wade Andrews ,  Kevin Ronald Condroski ,  Julia Haas ,  Yutong Jiang ,  Gabrielle R. Kolakowski ,  Jeongbeob Seo ,  HongWoon Yang ,  Qian Zhao

Inventor： Steven Wade Andrews ,  Kevin Ronald Condroski ,  Julia Haas ,  Yutong Jiang ,  Gabrielle R. Kolakowski ,  Jeongbeob Seo ,  HongWoon Yang ,  Qian Zhao

IPC: A61K31/519 ,  C07D487/02 ,  C07D519/00 ,  C07D498/22 ,  C07D487/04 ,  C07D471/22

CPC classification number: C07D498/22 ,  A61K31/519 ,  C07D471/22 ,  C07D487/04 ,  C07D487/22 ,  C07D519/00

Abstract: Compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein ring A, ring B, W, m, D, R2, R2a, R3, R3a, and Z are as defined herein, are inhibitors of Trk kinases and are useful in the treatment of pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.

Abstract translation: 式I化合物及其药学上可接受的盐，其中环A，环B，W，m，D，R2，R2a，R3，R3a和Z如本文所定义，是Trk激酶的抑制剂，可用于治疗 疼痛，癌症，炎症，神经变性疾病和某些传染病。

公开(公告)号：US08895566B2

公开(公告)日：2014-11-25

申请号：US13678395

申请日：2012-11-15

Applicant: Array BioPharma Inc. ,  Genentech, Inc.

Inventor： Anna Banka ,  Josef R. Bencsik ,  James F. Blake ,  Martin F. Hentemann ,  Nicholas C. Kallan ,  Jun Liang ,  Ian S. Mitchell ,  Stephen T. Schlachter ,  Eli M. Wallace ,  Rui Xu ,  Tony P. Tang

IPC: A61K31/517 ,  C07D403/10 ,  C07D409/04 ,  C07D239/70 ,  C07D401/04 ,  C07D403/04 ,  C07D487/04 ,  C07D401/12 ,  C07D417/10 ,  C07D401/10 ,  C07D417/04

CPC classification number: C07D401/10 ,  C07D211/08 ,  C07D211/46 ,  C07D239/70 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/10 ,  C07D409/04 ,  C07D417/04 ,  C07D417/10 ,  C07D487/04

Abstract: Compounds of Formula I are useful for inhibiting AKT protein 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化合物可用于抑制AKT蛋白激酶。 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。