公开(公告)号：WO2013078254A1

公开(公告)日：2013-05-30

申请号：PCT/US2012/066153

申请日：2012-11-20

Applicant: ARRAY BIOPHARMA INC. ,  GENENTECH, INC. ,  SKELTON, Nicholas ,  GRADL, Stefan ,  BLAKE, James F. ,  GRAHAM, James M. ,  GUNAWARDANA, Indrani W. ,  HENTEMANN, Martin ,  MARLOW, Allison L. ,  TANG, Tony P.

Inventor： SKELTON, Nicholas ,  GRADL, Stefan ,  BLAKE, James F. ,  GRAHAM, James M. ,  GUNAWARDANA, Indrani W. ,  HENTEMANN, Martin ,  MARLOW, Allison L. ,  TANG, Tony P.

IPC: C07D471/04 ,  C07D487/04 ,  A61K31/4188 ,  A61P35/00

CPC classification number: C07D471/04 ,  C07D487/04

Abstract: The present invention provides compounds, including resolved enantiomers, resolved diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula 1: wherein Het, X, R 1 and R 2 are as defined herein.

Abstract translation: 本发明提供包括拆分的对映异构体，分解的非对映异构体，溶剂化物和药学上可接受的盐的化合物，其包含式1：其中Het，X，R 1和R 2如本文所定义。

公开(公告)号：WO2011123674A1

公开(公告)日：2011-10-06

申请号：PCT/US2011/030769

申请日：2011-03-31

Applicant: ARRAY BIOPHARMA INC. ,  GENENTECH, INC. ,  CLARK, Christopher, T. ,  COOK, Adam ,  GUNAWARDANA, Indrani, W. ,  HUNT, Kevin W. ,  KALLAN, Nicholas, C. ,  SIU, Michael ,  THOMAS, Allen, A. ,  VOLGRAF, Matthew

Inventor： CLARK, Christopher, T. ,  COOK, Adam ,  GUNAWARDANA, Indrani, W. ,  HUNT, Kevin W. ,  KALLAN, Nicholas, C. ,  SIU, Michael ,  THOMAS, Allen, A. ,  VOLGRAF, Matthew

IPC: C07D401/10 ,  C07D401/14 ,  C07D403/10 ,  C07D413/10 ,  C07D417/10 ,  C07D263/64 ,  A61K31/41 ,  A61P25/28

CPC classification number: C07D401/14 ,  C07D263/64 ,  C07D401/10 ,  C07D403/10 ,  C07D413/10 ,  C07D417/10

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

Abstract translation: 本发明提供新颖的抑制APP分泌​​酶切割的式（a）的四氢四氢化合物，可用作治疗神经变性疾病的治疗剂。

公开(公告)号：WO2009089359A1

公开(公告)日：2009-07-16

申请号：PCT/US2009/030450

申请日：2009-01-08

Applicant: ARRAY BIOPHARMA INC. ,  BLAKE, James ,  GUNAWARDANA, Indrani W. ,  LE HUEROU, Yvan ,  MOHR, Peter J. ,  WALLACE, Eli M. ,  WANG, Bin

Inventor： BLAKE, James ,  GUNAWARDANA, Indrani W. ,  LE HUEROU, Yvan ,  MOHR, Peter J. ,  WALLACE, Eli M. ,  WANG, Bin

IPC: C07D471/04 ,  A61K31/4162 ,  A61P35/00

CPC classification number: C07D471/04

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：WO2009089352A1

公开(公告)日：2009-07-16

申请号：PCT/US2009/030443

申请日：2009-01-08

Applicant: ARRAY BIOPHARMA INC. ,  BLAKE, James ,  GUNAWARDANA, Indrani W. ,  LE HUEROU, Yvan ,  MOHR, Peter J. ,  WALLACE, Eli M. ,  WANG, Bin

Inventor： BLAKE, James ,  GUNAWARDANA, Indrani W. ,  LE HUEROU, Yvan ,  MOHR, Peter J. ,  WALLACE, Eli M. ,  WANG, Bin

IPC: C07D471/04 ,  A61K31/496 ,  A61P35/00

CPC classification number: C07D471/04

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.Formula, (I).

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：WO2009042435A1

公开(公告)日：2009-04-02

申请号：PCT/US2008/076401

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 ,  C07D417/14 ,  A61K31/433 ,  A61P3/10

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

Abstract: Provided are compounds of Formula (I): wherein R 2 , R 3 , R 13 , L and D 2 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: 提供式（I）的化合物：其中R2，R3，R13，L和D2如说明书中所定义，其可用于治疗和/或预防由缺乏葡萄糖激酶水平的活性介导的疾病或病症，或可以 通过激活葡糖激酶，包括但不限于糖尿病，葡萄糖耐量降低，IFG（空腹血糖受损）和IFG（空腹血糖受损））以及其它疾病和病症如本文讨论的疾病和病症。

公开(公告)号：WO2014074940A9

公开(公告)日：2014-08-07

申请号：PCT/US2013069331

申请日：2013-11-08

Applicant: ARRAY BIOPHARMA INC ,  ASSELIN SYLVIE ,  BRETT LISA ,  CHEN YING ,  CORSON DONALD T ,  COSBIE ANDREW ,  FARRELL ROBERT ,  GUNAWARDANA INDRANI W ,  HUANG JINKUN ,  LANE JONATHAN W ,  LEI DENNIS ,  LINDEMANN CHRISTOPHER M ,  LUU VAN ,  MANNILA CORALEE G ,  MILBURN ROBERT ,  MORRISON HENRY ,  TAN HELMING ,  TEDROW JASON ,  WATSON DANIEL J

Inventor： ASSELIN SYLVIE ,  BRETT LISA ,  CHEN YING ,  CORSON DONALD T ,  COSBIE ANDREW ,  FARRELL ROBERT ,  GUNAWARDANA INDRANI W ,  HUANG JINKUN ,  LANE JONATHAN W ,  LEI DENNIS ,  LINDEMANN CHRISTOPHER M ,  LUU VAN ,  MANNILA CORALEE G ,  MILBURN ROBERT ,  MORRISON HENRY ,  TAN HELMING ,  TEDROW JASON ,  WATSON DANIEL J

IPC: C07D417/14 ,  A61K31/444 ,  A61P3/10

CPC classification number: C07D417/14 ,  C07B2200/13

Abstract: The present invention relates to crystalline polymorph forms of (1S)-1-[5-({3-[(2-methylpyridin-3-yl)oxy]-5-(pyridin-2-ylsulfanyl)pyridin-2-yl}amino)-1,2,4-thiadiazol-3-yl]ethane-1,2-diol, to pharmaceutical compositions comprising such crystalline polymorph forms, and to processes for preparing them. The invention further relates to methods of treatment of diabetes related disorders comprising administering such solid-state forms or compositions thereof to a subject, and to use of such crystalline polymorph forms in the manufacture of medicaments.

Abstract translation: 本发明涉及（1S）-1- [5 - （{3 - [（2-甲基吡啶-3-基）氧基] -5-（吡啶-2-基硫烷基）吡啶-2-基} 氨基）-1,2,4-噻二唑-3-基]乙-1,2-二醇，涉及包含此类结晶多晶型物的药物组合物，并涉及制备它们的方法。 本发明进一步涉及治疗糖尿病相关病症的方法，包括将所述固态形式或其组合物施用于受试者，并且涉及这种结晶多晶型物在制造药物中的用途。

公开(公告)号：WO2014074940A1

公开(公告)日：2014-05-15

申请号：PCT/US2013/069331

申请日：2013-11-08

Applicant: ARRAY BIOPHARMA INC. ,  ASSELIN, Sylvie ,  BRETT, Lisa ,  CHEN, Ying ,  CORSON, Donald T. ,  COSBIE, Andrew ,  FARRELL, Robert ,  GUNAWARDANA, Indrani W. ,  HUANG, Jinkun ,  LANE, Jonathan W. ,  LEI, Dennis ,  LINDEMANN, Christopher M ,  LUU, Van ,  MANNILA, Coralee G. ,  MILBURN, Robert ,  MORRISON, Henry ,  TAN, Helming ,  TEDROW, Jason ,  WATSON, Daniel J.

Inventor： ASSELIN, Sylvie ,  BRETT, Lisa ,  CHEN, Ying ,  CORSON, Donald T. ,  COSBIE, Andrew ,  FARRELL, Robert ,  GUNAWARDANA, Indrani W. ,  HUANG, Jinkun ,  LANE, Jonathan W. ,  LEI, Dennis ,  LINDEMANN, Christopher M ,  LUU, Van ,  MANNILA, Coralee G. ,  MILBURN, Robert ,  MORRISON, Henry ,  TAN, Helming ,  TEDROW, Jason ,  WATSON, Daniel J.

IPC: C07D417/14 ,  A61K31/444 ,  A61P3/10

CPC classification number: C07D417/14 ,  C07B2200/13

Abstract: The present invention relates to crystalline polymorph forms of (1S)-1-[5-({3-[(2-methylpyridin-3-yl)oxy]-5-(pyridin-2-ylsulfanyl)pyridin-2-yl}amino)-1,2,4-thiadiazol-3-yl]ethane-1,2-diol, to pharmaceutical compositions comprising such crystalline polymorph forms, and to processes for preparing them. The invention further relates to methods of treatment of diabetes related disorders comprising administering such solid-state forms or compositions thereof to a subject, and to use of such crystalline polymorph forms in the manufacture of medicaments.

Abstract translation: 本发明涉及（1S）-1- [5 - （{3 - [（2-甲基吡啶-3-基）氧基] -5-（吡啶-2-基硫烷基）吡啶-2-基} 氨基）-1,2,4-噻二唑-3-基]乙烷-1,2-二醇，包括这种结晶多晶型物的药物组合物及其制备方法。 本发明还涉及治疗糖尿病相关病症的方法，包括将这种固态形式或其组合物施用于受试者，以及在制备药物中使用这种结晶多晶型物。

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：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。