公开(公告)号：WO2009061730A3

公开(公告)日：2013-04-04

申请号：PCT/US2008082350

申请日：2008-11-04

Applicant: ARRAY BIOPHARMA INC ,  DOHERTY GEORGE A

Inventor： DOHERTY GEORGE A

IPC: A61K31/04 ,  A61K31/416 ,  A61K31/4184 ,  A61P37/00 ,  C07D209/08 ,  C07D213/56 ,  C07D231/56 ,  C07D235/06 ,  C07D235/08

CPC classification number: C07D209/08 ,  C07D231/56 ,  C07D235/06 ,  C07D235/08

Abstract: Compounds of Formula I: I in which D1, D2, R1, R2, R7, R8 and A have the meanings given in the specification, are DP2 receptor modulators useful in the treatment of immunologic diseases.

Abstract translation: 其中D1，D2，R1，R2，R7，R8和A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疾病的DP2受体调节剂。

公开(公告)号：WO2012071458A1

公开(公告)日：2012-05-31

申请号：PCT/US2011/061930

申请日：2011-11-22

Applicant: ARRAY BIOPHARMA INC. ,  GENENTECH, INC. ,  COOK, Adam ,  GUNAWARDANA, Indrani, W. ,  HUESTIS, Malcolm ,  HUNT, Kevin, W. ,  KALLAN, Nicholas, C. ,  METCALF, Andrew, T. ,  NEWHOUSE, Brad ,  SIU, Michael ,  TANG, Tony, P. ,  THOMAS, Allen, A. ,  VOLGRAF, Matthew

Inventor： COOK, Adam ,  GUNAWARDANA, Indrani, W. ,  HUESTIS, Malcolm ,  HUNT, Kevin, W. ,  KALLAN, Nicholas, C. ,  METCALF, Andrew, T. ,  NEWHOUSE, Brad ,  SIU, Michael ,  TANG, Tony, P. ,  THOMAS, Allen, A. ,  VOLGRAF, Matthew

IPC: C07D491/20 ,  C07D498/20 ,  C07D491/107 ,  C07D498/10 ,  C07D513/10 ,  C07D513/20 ,  A61K31/4439 ,  A61K31/527 ,  A61K31/444 ,  A61K31/506 ,  A61K31/424 ,  A61K31/429 ,  A61K31/437 ,  A61P25/28

CPC classification number: C07D498/20 ,  C07D491/107 ,  C07D491/20 ,  C07D498/10 ,  C07D513/10 ,  C07D513/20

Abstract: The invention provides novel tricyclic compounds of Formula I' that inhibit β-secretase cleavage of APP and are useful as therapeutic agents for treating neurodegenerative diseases.

Abstract translation: 本发明提供抑制APP的β-分泌酶切割的新颖的式I'三环化合物，并且可用作治疗神经变性疾病的治疗剂。

公开(公告)号：WO2012040641A2

公开(公告)日：2012-03-29

申请号：PCT/US2011/053118

申请日：2011-09-23

Applicant: ARRAY BIOPHARMA INC. ,  HUNT, Kevin W. ,  TANG, Tony P. ,  THOMAS, Allen A.

Inventor： HUNT, Kevin W. ,  TANG, Tony P. ,  THOMAS, Allen A.

IPC: C07D491/107 ,  C07D491/20 ,  A61K31/4188 ,  A61P25/28

CPC classification number: A61K31/4188 ,  C07D491/107 ,  C07D491/20

Abstract: The invention provides novel tricyclic compounds of Formula I' that inhibit β-secretase cleavage of APP and are useful as therapeutic agents for treating neurodegenerative diseases.

Abstract translation: 本发明提供抑制APP的β-分泌酶切割的新颖的式I'三环化合物，并且可用作治疗神经变性疾病的治疗剂。

公开(公告)号：WO2011025938A3

公开(公告)日：2011-05-05

申请号：PCT/US2010046952

申请日：2010-08-27

Applicant: ARRAY BIOPHARMA INC ,  GENENTECH INC ,  ALIAGAS IGNACIO ,  GRADL STEFAN ,  GUNZNER JANET ,  LEE WENDY ,  MATHIEU SIMON ,  RUDOLPH JOACHIM ,  WEN ZHAOYANG ,  ZHAO GUILING ,  BUCKMELTER ALEXANDRE J ,  GRINA JONAS ,  HANSEN JOSHUA D ,  LAIRD ELLEN ,  MORENO DAVID ,  REN LI ,  WENGLOWSKY STEVEN MARK

Inventor： ALIAGAS IGNACIO ,  GRADL STEFAN ,  GUNZNER JANET ,  LEE WENDY ,  MATHIEU SIMON ,  RUDOLPH JOACHIM ,  WEN ZHAOYANG ,  ZHAO GUILING ,  BUCKMELTER ALEXANDRE J ,  GRINA JONAS ,  HANSEN JOSHUA D ,  LAIRD ELLEN ,  MORENO DAVID ,  REN LI ,  WENGLOWSKY STEVEN MARK

IPC: C07D239/94 ,  A61K31/517 ,  A61K31/519 ,  A61P35/00 ,  C07D403/12 ,  C07D405/12 ,  C07D471/04

CPC classification number: C07D239/94 ,  C07D403/12 ,  C07D405/12 ,  C07D471/04

Abstract: Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers, prodrugs 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Raf激酶。 公开了使用式I化合物及其立体异构体，互变异构体，前药和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中的这些病症或相关病理学病症的方法。

公开(公告)号：WO2011006074A1

公开(公告)日：2011-01-13

申请号：PCT/US2010/041538

申请日：2010-07-09

Applicant: ARRAY BIOPHARMA INC. ,  ALLEN, Shelley ,  ANDREWS, Steven S. ,  CONDROSKI, Kevin Ronald ,  HAAS, Julia ,  HUANG, Lily ,  JIANG, Yutong ,  KERCHER, Timothy ,  SEO, Jeongbeob

Inventor： ALLEN, Shelley ,  ANDREWS, Steven S. ,  CONDROSKI, Kevin Ronald ,  HAAS, Julia ,  HUANG, Lily ,  JIANG, Yutong ,  KERCHER, Timothy ,  SEO, Jeongbeob

IPC: C07D487/04 ,  A61K31/519 ,  C07D519/00

CPC classification number: C07D487/04 ,  A61K31/519 ,  A61K31/5377 ,  C07D453/02 ,  C07D471/22 ,  C07D498/22 ,  C07D519/00

Abstract: Compounds of Formula (I) and salts thereof in which R 1 , R 2 , R 3 , R 4 , X, Y and n have the meanings given in the specification, are inhibitors of Trk kinases and are useful in the treatment of diseases which can be treated with a Trk kinase inhibitor such as pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.

Abstract translation: 其中R1，R2，R3，R4，X，Y和n具有本说明书中给出的含义的式（I）化合物及其盐是Trk激酶的抑制剂，可用于治疗可用 一种Trk激酶抑制剂，如疼痛，癌症，炎症，神经变性疾病和某些传染病。

公开(公告)号：WO2010118390A1

公开(公告)日：2010-10-14

申请号：PCT/US2010/030634

申请日：2010-04-09

Applicant: ARRAY BIOPHARMA INC. ,  HUMPHRIES, Michael J. ,  WINSKI, Shannon L.

Inventor： HUMPHRIES, Michael J. ,  WINSKI, Shannon L.

IPC: A61K31/437 ,  A61K31/4745 ,  A61K31/7068 ,  A61K45/06 ,  A61P35/00

CPC classification number: A61K31/437 ,  A61K31/4745 ,  A61K31/7068 ,  A61K45/06 ,  A61K2300/00

Abstract: A CHK1 inhibitor for administration to a patient with cancer for potentiating a DNA damaging agent is provided.

Abstract translation: 提供了一种用于给患有恶性肿瘤加强DNA损伤剂的患者施用的CHK1抑制剂。

公开(公告)号：WO2010039825A3

公开(公告)日：2010-10-07

申请号：PCT/US2009059017

申请日：2009-09-30

Applicant: ARRAY BIOPHARMA INC ,  ALLEN SHELLEY ,  MARMSATER FREDRIK P ,  ROBINSON JOHN E ,  SCHLACHTER STEPHEN T ,  LYSSIKATOS JOSEPH P

Inventor： ALLEN SHELLEY ,  MARMSATER FREDRIK P ,  ROBINSON JOHN E ,  SCHLACHTER STEPHEN T ,  LYSSIKATOS JOSEPH P

IPC: C07D487/04 ,  A61K31/4375 ,  A61P35/00

CPC classification number: C07D487/04 ,  C07D471/04

Abstract: Compounds of Formula I and II: I II having the chemical names cis-6-fluoro-8-(3-fluoropiperidin-4-yloxy)-2-(7-(2-methoxyethoxy)imidazo[1,2-a]pyridin-3-yl)quinoline and 6-fluoro-8-(trans-3-fluoropiperidin-4-yloxy)-2-(7-(2-methoxyethoxy)imidazo[1,2-a]pyridin-3-yl)quinoline, respectively, and enantiomers and pharmaceutically acceptable salts thereof, are receptor tyrosine inhibitors useful in the treatment of diseases mediated by class 3 and class 5 receptor tyrosine kinases. The compounds of this invention have also been found to be inhibitors of Pim-1.

Abstract translation: 具有化学名称的顺式-6-氟-8-（3-氟哌啶-4-基氧基）-2-（7-（2-甲氧基乙氧基）咪唑并[1,2-a]吡啶的式I和II化合物： 吡啶-3-基）喹啉和6-氟-8-（反式-3-氟哌啶-4-基氧基）-2-（7-（2-甲氧基乙氧基）咪唑并[1,2-a]吡啶-3-基）喹啉 和对映异构体及其药学上可接受的盐是可用于治疗由3类和5类受体酪氨酸激酶介导的疾病的受体酪氨酸抑制剂。 本发明的化合物也被发现是Pim-1的抑制剂。

公开(公告)号：WO2009140320A1

公开(公告)日：2009-11-19

申请号：PCT/US2009/043691

申请日：2009-05-13

Applicant: ARRAY BIOPHARMA INC. ,  LE HUEROU, Yvan ,  BLAKE, James, F. ,  GUNWARDANA, Indrani, W. ,  MOHR, Pete ,  WALLACE, Eli, M. ,  WANG, Bin ,  CHICARELLI, Mark ,  LYON, Michael

Inventor： LE HUEROU, Yvan ,  BLAKE, James, F. ,  GUNWARDANA, Indrani, W. ,  MOHR, Pete ,  WALLACE, Eli, M. ,  WANG, Bin ,  CHICARELLI, Mark ,  LYON, Michael

IPC: C07D471/04 ,  A61K31/437 ,  A61P35/00

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

Abstract: Compounds of Formula (I) are useful for inhibition of CHKl 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：WO2009042435A8

公开(公告)日：2009-10-08

申请号：PCT/US2008076401

申请日：2008-09-15

Applicant: ARRAY BIOPHARMA INC ,  AICHER THOMAS DANIEL ,  BOYD STEVEN ARMEN ,  CHICARELLI MARK JOSEPH ,  CONDROSKI KEVIN RONALD ,  FELL JAY BRADFORD ,  FISCHER JOHN P ,  GUNAWARDANA INDRANI W ,  HINKLIN RONALD JAY ,  SINGH AJAY ,  TURNER TIMOTHY M ,  WALLACE ELI M

Inventor： AICHER THOMAS DANIEL ,  BOYD STEVEN ARMEN ,  CHICARELLI MARK JOSEPH ,  CONDROSKI KEVIN RONALD ,  FELL JAY BRADFORD ,  FISCHER JOHN P ,  GUNAWARDANA INDRANI W ,  HINKLIN RONALD JAY ,  SINGH AJAY ,  TURNER TIMOTHY M ,  WALLACE ELI M

IPC: C07D417/12 ,  A61K31/433 ,  A61P3/10 ,  C07D417/14

CPC classification number: C07D401/14 ,  C07D213/75 ,  C07D401/12 ,  C07D417/12 ,  C07D417/14

Abstract: Provided are compounds of Formula (I): wherein R2, R3, R13, L and D2 are as defined in the specification, which are useful in the treatment and/or prevention of diseases or disorders mediated by deficient levels of glucokinase activity or which can be treated by activating glucokinase including, but not limited to, diabetes mellitus, impaired glucose tolerance, IFG (impaired fasting glucose) and IFG (impaired fasting glycemia), as well as other diseases and disorders such as those discussed herein.

Abstract translation: 提供了式（I）的化合物：其中R 2，R 3，R 13，L和D 2如说明书中所定义，其可用于治疗和/或预防由葡萄糖激酶活性水平不足所介导的疾病或病症， 通过激活包括但不限于糖尿病，葡萄糖耐量降低，IFG（空腹葡萄糖受损）和IFG（空腹血糖受损）以及其他疾病和病症（例如本文讨论的那些）的葡萄糖激酶来治疗。

公开(公告)号：WO2009111278A2

公开(公告)日：2009-09-11

申请号：PCT/US2009035380

申请日：2009-02-27

Applicant: ARRAY BIOPHARMA INC ,  GENENTECH INC ,  AHRENDT KATERI A ,  BUCKMELTER ALEXANDRE J ,  GRINA JONAS ,  HANSEN JOSHUA D ,  LAIRD ELLEN R ,  MORENO DAVID ,  NEWHOUSE BRAD ,  REN LI ,  WENGLOWSKY STEVEN MARK ,  FENG BAINIAN ,  GUNZNER JANET ,  MALESKY KIM ,  MATHIEU SIMON ,  RUDOLPH JOACHIM ,  WEN ZHAOYANG ,  YOUNG WENDY B

Inventor： AHRENDT KATERI A ,  BUCKMELTER ALEXANDRE J ,  GRINA JONAS ,  HANSEN JOSHUA D ,  LAIRD ELLEN R ,  MORENO DAVID ,  NEWHOUSE BRAD ,  REN LI ,  WENGLOWSKY STEVEN MARK ,  FENG BAINIAN ,  GUNZNER JANET ,  MALESKY KIM ,  MATHIEU SIMON ,  RUDOLPH JOACHIM ,  WEN ZHAOYANG ,  YOUNG WENDY B

IPC: A61K31/4745

CPC classification number: C07D471/04 ,  C07C311/08

Abstract: Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers, prodrugs 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Raf激酶。 公开了使用式I化合物和立体异构体，互变异构体，前药和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。