公开(公告)号：US20150336970A1

公开(公告)日：2015-11-26

申请号：US14575663

申请日：2014-12-18

Applicant: Array BioPharma Inc.

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

IPC: C07D487/22 ,  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：US20150232442A1

公开(公告)日：2015-08-20

申请号：US14702947

申请日：2015-05-04

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 are compounds of Formula I: in which A1, A2, W, L, G, R7a, R7b, R8, R9 and R10 have the meanings given in the specification, which are DP2 receptor modulators useful in the treatment of immunologic diseases.

Abstract translation: 本文提供了式I的化合物：其中A1，A2，W，L，G，R7a，R7b，R8，R9和R10具有本说明书中给出的含义，其是可用于治疗免疫疾病的DP2受体调节剂。

公开(公告)号：US20150197496A1

公开(公告)日：2015-07-16

申请号：US14665879

申请日：2015-03-23

Applicant: Array BioPharma Inc. ,  Genentech, Inc.

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: C07D239/70 ,  C07D403/12 ,  C07D401/12 ,  C07D409/12

CPC classification number: C07D239/70 ,  A61K31/506 ,  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：US08987251B2

公开(公告)日：2015-03-24

申请号：US14057882

申请日：2013-10-18

Applicant: Array BioPharma Inc.

Inventor： Shelley Allen ,  Laura L. Celeste ,  T. Gregg Davis ,  Robert Kirk DeLisle ,  Julie Marie Hicks ,  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: A61K31/437 ,  C07D471/04 ,  C07D451/06 ,  C07D519/00

CPC classification number: C07D471/04 ,  A61K31/437 ,  C07D451/06 ,  C07D519/00

Abstract: Provided herein is a method of treating a PIM-1 and/or PIM-2 and/or PIM-3 kinase-mediated condition in a mammal, which comprises administering to said mammal a therapeutically effective amount of a compound of Formula I: in which A, B, R1, R1a, R2, R3, R4, R5, R6, and R7 have the meanings given in the specification.

Abstract translation: 本文提供了一种在哺乳动物中治疗PIM-1和/或PIM-3和/或PIM-3激酶介导的病症的方法，其包括向所述哺乳动物施用治疗有效量的式I化合物：其中 A，B，R1，R1a，R2，R3，R4，R5，R6和R7具有说明书中给出的含义。

公开(公告)号：US20140349996A1

公开(公告)日：2014-11-27

申请号：US14456670

申请日：2014-08-11

Applicant: Array BioPharma Inc. ,  Genentech, Inc.

Inventor： Ian S. Mitchell ,  James F. Blake ,  Rui Xu ,  Nicholas C. Kallan ,  Dengming Xiao ,  Keith Lee Spencer ,  Josef R. Bencsik ,  Eli M. Wallace ,  Stephen T. Schlacter ,  Anna L. Banka ,  Jun Liang ,  Brian Safina ,  Jun Li ,  Christine Chabot

IPC: C07D409/14 ,  A61K31/517 ,  A61K45/06 ,  C07D239/70 ,  C07D409/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  A61K31/5377 ,  C07D403/04 ,  C07D403/14

CPC classification number: C07D409/14 ,  A61K31/517 ,  A61K31/5377 ,  A61K45/06 ,  C07D239/70 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  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：US08883828B2

公开(公告)日：2014-11-11

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: A01N43/40 ,  C07D417/00 ,  C07D417/14 ,  C07D491/04 ,  C07D487/04 ,  C07D513/04 ,  C07D417/12 ,  C07D471/04 ,  C07D413/14 ,  C07D495/04

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：US08846683B2

公开(公告)日：2014-09-30

申请号：US13753008

申请日：2013-01-29

Applicant: Array BioPharma Inc. ,  Genentech, Inc.

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: A61P35/00

CPC classification number: C07D239/70 ,  A61K31/506 ,  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：US20140148436A1

公开(公告)日：2014-05-29

申请号：US14170272

申请日：2014-01-31

Applicant: Array BioPharma, Inc.

Inventor： Ian S. Mitchell ,  Keith L. Spencer ,  Peter Stengel ,  Yongxin Han ,  Nicolas C. Kallan ,  Mark Munson ,  Guy P.A. Vigers ,  James Blake ,  Anthony Piscopio ,  John Josey ,  Scott Miller ,  Dengming Xiao ,  Rui Xu ,  Chang Rao ,  Bing Wang ,  April L. Bernacki

IPC: C07D239/94 ,  C07D403/12 ,  C07D495/04 ,  C07D491/048 ,  C07D231/56 ,  C07D401/12 ,  C07D409/04 ,  C07D401/04 ,  C07D409/12 ,  C07D487/04

CPC classification number: C07D239/94 ,  B41M3/008 ,  B44F1/10 ,  C07D231/56 ,  C07D237/28 ,  C07D239/42 ,  C07D239/47 ,  C07D239/48 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D409/04 ,  C07D409/12 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  C07D495/04 ,  G09F13/16 ,  Y10T428/24802 ,  Y10T428/24851 ,  Y10T428/25 ,  Y10T428/31507 ,  Y10T428/31551 ,  Y10T428/31786 ,  Y10T428/31855

Abstract: The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula: A-L-CR where CR is a cyclical core group, L is a linking group and A is as defined herein. 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: 本发明提供包括分解对映异构体，非对映异构体，溶剂化物和药学上可接受的盐的化合物，其包含式为：A-L-CR，其中CR为环状核心基团，L为连接基团，A如本文所定义。 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：US20140045835A1

公开(公告)日：2014-02-13

申请号：US14054459

申请日：2013-10-15

Applicant: Array BioPharma Inc.

Inventor： Shelley Allen ,  Robert Kirk DeLisle ,  Julie Marie Hicks ,  Erik James Hicken ,  Joseph P. Lyssikatos ,  Fredrik P. Marmsater ,  Mark C. Munson ,  John E. Robinson ,  Qian Zhao

IPC: C07D471/04

CPC classification number: C07D471/04

Abstract: Provided herein are methods of treating diseases mediated by PIM-1 and/or PIM-2 and/or PIM-3 kinases by administering to a mammal in need thereof a therapeutically effective amount of a compound of Formula I: in which B, R1, R1a, R2, R3, R4, R5, R6, R7, R10 and R11 have the meanings given in the specification.

Abstract translation: 本文提供了通过向有需要的哺乳动物施用治疗有效量的式I化合物来治疗由PIM-1和/或PIM-2和/或PIM-3激酶介导的疾病的方法：其中B，R1， R1a，R2，R3，R4，R5，R6，R7，R10和R11具有说明书中给出的含义。

公开(公告)号：US20140045782A1

公开(公告)日：2014-02-13

申请号：US13913091

申请日：2013-06-07

Applicant: ARRAY BIOPHARMA INC.

Inventor： Michael J. Humphries ,  Shannon L. Winski

IPC: A61K31/437 ,  A61K31/4375 ,  A61K31/7068

CPC classification number: A61K31/437 ,  A61K31/4375 ,  A61K31/4545 ,  A61K31/4745 ,  A61K31/513 ,  A61K31/519 ,  A61K31/664 ,  A61K31/704 ,  A61K31/7068 ,  A61K31/7076 ,  A61K33/24 ,  A61K45/06 ,  A61K2300/00

Abstract: Methods of treating cancer by administering a DNA damaging agent and a CHK1 Inhibitor on a dosing regimen are provided.

Abstract translation: 提供了通过在给药方案上施用DNA损伤剂和CHK1抑制剂来治疗癌症的方法。