公开(公告)号：US08754226B2

公开(公告)日：2014-06-17

申请号：US13698257

申请日：2011-05-13

Applicant: Thomas Daniel Aicher ,  Josef Roland Bencsik ,  Kevin Ronald Condroski ,  Jay Bradford Fell ,  John P. Fischer ,  Ronald Jay Hinklin ,  Scott Alan Pratt ,  Ajay Singh ,  Timothy M. Turner ,  David A. Mareska ,  Steven Armen Boyd

Inventor： Thomas Daniel Aicher ,  Josef Roland Bencsik ,  Kevin Ronald Condroski ,  Jay Bradford Fell ,  John P. Fischer ,  Ronald Jay Hinklin ,  Scott Alan Pratt ,  Ajay Singh ,  Timothy M. Turner ,  David A. Mareska ,  Steven Armen Boyd

IPC: A01N43/40 ,  A61K31/445 ,  A61K31/44 ,  C07D401/00 ,  C07D405/00 ,  C07D409/00 ,  C07D411/00 ,  C07D413/00 ,  C07D417/00 ,  C07D419/00 ,  C07D421/00

CPC classification number: C07D413/14 ,  C07D401/14 ,  C07D405/14

Abstract: Compounds of Formula (I): and pharmaceutically acceptable salts thereof in which X1, X2, L, R3, R4, R5, R6, R6a, R7, R9, R9a, and n have the meanings given in the specification, are modulators of GPR119 and are useful in the treatment or prevention of diseases such as such as, but not limited to, type 2 diabetes, diabetic complications, symptoms of diabetes, metabolic syndrome, obesity, dyslipidemia, and related conditions.

Abstract translation: 其中X1，X2，L，R3，R4，R5，R6，R6a，R7，R9，R9a和n具有本说明书中给出的含义的式（I）化合物及其药学上可接受的盐是GPR119的调节剂 并且可用于治疗或预防诸如但不限于2型糖尿病，糖尿病并发症，糖尿病症状，代谢综合征，肥胖症，血脂异常和相关病症等疾病。

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：US20140066453A1

公开(公告)日：2014-03-06

申请号：US14011501

申请日：2013-08-27

Applicant: Jim Blake ,  Huifen Chen ,  Mark Chicarelli ,  John Gaudino ,  Lewis Gazzard ,  Sam Kintz ,  Pete Mohr ,  Kirk Robarge ,  Jacob Schwarz ,  Aihe Zhou

Inventor： Jim Blake ,  Huifen Chen ,  Mark Chicarelli ,  John Gaudino ,  Lewis Gazzard ,  Sam Kintz ,  Pete Mohr ,  Kirk Robarge ,  Jacob Schwarz ,  Aihe Zhou

IPC: C07D471/04 ,  C07D401/14 ,  C07D217/22 ,  C07D401/12 ,  C07D405/14 ,  C07D405/12

CPC classification number: C07D405/14 ,  C07D217/22 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D471/04

Abstract: Compounds having the formula I wherein R2, X and Z 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，其中本文定义的R2，X和Z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：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：US08569522B2

公开(公告)日：2013-10-29

申请号：US13001201

申请日：2009-06-24

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

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

IPC: C07D311/58 ,  A61K31/353

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

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

Abstract translation: 式（I）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，是可用于治疗免疫疾病的DP2受体调节剂。

公开(公告)号：US08481557B2

公开(公告)日：2013-07-09

申请号：US12757954

申请日：2010-04-09

Applicant: Michael J. Humphries ,  Shannon L. Winski

Inventor： Michael J. Humphries ,  Shannon L. Winski

IPC: A61K31/44 ,  A61K31/445 ,  A61K31/40

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.

公开(公告)号：US20130143865A1

公开(公告)日：2013-06-06

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

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.

公开(公告)号：US20130131039A1

公开(公告)日：2013-05-23

申请号：US13640099

申请日：2011-04-11

Applicant: Laurence E. Burgess ,  Mark Laurence Boys ,  Robert D. Groneberg ,  Darren M. Harvey ,  Timothy Kercher ,  Christopher F. Kraser ,  Ellen Laird ,  Eugene Tarlton ,  Qian Zhao ,  Lily Huang

Inventor： Laurence E. Burgess ,  Mark Laurence Boys ,  Robert D. Groneberg ,  Darren M. Harvey ,  Timothy Kercher ,  Christopher F. Kraser ,  Ellen Laird ,  Eugene Tarlton ,  Qian Zhao ,  Lily Huang

IPC: C07D487/04 ,  C07D498/04

CPC classification number: C07D487/04 ,  C07D498/04

Abstract: Compounds of Formula I: (Formula should be inserted here) and stereoisomers and pharmaceutically acceptable salts and solvates thereof in which R1, R2, R3, R4, R5, R6, R7, X1 and X2 have the meanings given in the specification, are inhibitors of one or more JAK kinases and are useful in the treatment of autoimmune diseases, inflammatory diseases, rejection of transplanted organs, tissues and cells, as well as hematologic disorders and malignancies and their co-morbidities.

Abstract translation: 式I化合物（此处应该插入式）及其其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，X 1和X 2具有本说明书中给出的含义的立体异构体及其药学上可接受的盐和溶剂化物是抑制剂 的一种或多种JAK激酶，并且可用于治疗自身免疫性疾病，炎性疾病，移植器官，组织和细胞的排斥，以及血液系统疾病和恶性肿瘤及其并发症。

公开(公告)号：US20130065908A1

公开(公告)日：2013-03-14

申请号：US13672546

申请日：2012-11-08

Applicant: Array BioPharma Inc.

Inventor： Ian S. Mitchell ,  James F. Blake ,  Rui Xu ,  Nicholas C. Kallan ,  Dengming Xiao ,  Keith Lee Spencer ,  Josef R. Bencsik

IPC: A61K31/519 ,  A61P29/00 ,  A61P17/00 ,  A61P9/00 ,  A61P25/28 ,  A61P15/00 ,  C07D491/048 ,  A61P35/00

CPC classification number: C07D491/048 ,  A61K31/519 ,  A61K45/06 ,  A61K2300/00

Abstract: The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula: 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：US08377937B2

公开(公告)日：2013-02-19

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: C07D239/70 ,  A61K31/517

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。