公开(公告)号：US20140094603A1

公开(公告)日：2014-04-03

申请号：US14099276

申请日：2013-12-06

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 ,  C07D401/12

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：US20140080829A1

公开(公告)日：2014-03-20

申请号：US14086717

申请日：2013-11-21

Applicant: Genentech, Inc. ,  Array BioPharma Inc.

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: C07D403/12 ,  C07D403/14 ,  C07D409/14 ,  C07D413/12 ,  C07D401/12 ,  C07D405/14

CPC classification number: C07D403/12 ,  C07D401/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/12

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.

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：US20140018399A1

公开(公告)日：2014-01-16

申请号：US14031958

申请日：2013-09-19

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: C07D285/12 ,  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.

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：US20140005213A1

公开(公告)日：2014-01-02

申请号：US14001657

申请日：2012-02-24

Applicant: James F. Blake ,  Robert Kirk Delisle ,  Lisa A. De Meese ,  James M. Graham ,  Yvan Le Huerou ,  Michael Lyon ,  John E. Robinson ,  Eli M. Wallace ,  Bin Wang ,  Rui Xu

Inventor： James F. Blake ,  Robert Kirk Delisle ,  Lisa A. De Meese ,  James M. Graham ,  Yvan Le Huerou ,  Michael Lyon ,  John E. Robinson ,  Eli M. Wallace ,  Bin Wang ,  Rui Xu

IPC: C07D471/04 ,  C07D491/048 ,  C07D487/10 ,  C07D487/04

CPC classification number: C07D471/04 ,  C07D401/06 ,  C07D487/04 ,  C07D487/10 ,  C07D491/048 ,  C07D519/00

Abstract: Compounds of Formula I: in which R1, R2, R3, R4 and R10 have the meanings given in the specification, are receptor tyrosine inhibitors useful in the treatment of diseases mediated by PIM-1 and/or PIM-2 and/or PIM-3 kinases.

Abstract translation: R 1，R 2，R 3，R 4和R 10具有本说明书中给出的含义的式I化合物是可用于治疗由PIM-1和/或PIM-2和/或PIM-2介导的疾病的受体酪氨酸抑制剂， 3激酶。

公开(公告)号：US20130338140A1

公开(公告)日：2013-12-19

申请号：US14002079

申请日：2012-02-28

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

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

IPC: C07D471/04 ,  A61K45/06 ,  A61K31/519

CPC classification number: C07D471/04 ,  A61K31/519 ,  A61K45/06 ,  C07D491/052

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

Abstract translation: 具有式I的化合物，其中Z，Z 1 Z 2 Z，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。

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：US20130085135A1

公开(公告)日：2013-04-04

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

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：US20130072500A1

公开(公告)日：2013-03-21

申请号：US13676963

申请日：2012-11-14

Applicant: Array BioPharma Inc.

Inventor： Anna Banka ,  Josef R. Bencsik ,  James F. Blake ,  Kin Chiu Fong ,  Martin F. Hentemann ,  Ian S. Mitchell ,  Douglas McCord Sammond ,  Tony P. Tang ,  Eli M. Wallace ,  Rui Xu

IPC: C07D471/10 ,  C07D487/10

CPC classification number: C07D471/10 ,  C07D487/10

Abstract: The present invention provides compounds of Formula I including tautomers, resolved enantiomers, resolved 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 Akt-mediated diseases, for example, 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，拆分的非对映体，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Akt介导的疾病例如过度增殖性疾病如癌症的方法。

公开(公告)号：US20130065901A1

公开(公告)日：2013-03-14

申请号：US13669083

申请日：2012-11-05

Applicant: Array BioPharma Inc.

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

IPC: A61K31/4439 ,  C07D417/14 ,  A61K31/444 ,  A61K31/4545 ,  C07D471/04 ,  A61K31/506 ,  C07D495/04 ,  C07D498/04 ,  C07D487/04 ,  A61K31/519 ,  A61K31/517 ,  A61K31/497 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/5377 ,  A61P3/10 ,  C07D417/12

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。