公开(公告)号：WO2022066646A1

公开(公告)日：2022-03-31

申请号：PCT/US2021/051315

申请日：2021-09-21

Applicant: MIRATI THERAPEUTICS, INC. ,  ARRAY BIOPHARMA INC.

Inventor： WANG, Xiaolun ,  MARX, Matthew Arnold ,  ALLEN, Shelley ,  CHICARELLI, Mark Joseph ,  DAHLKE, Joshua Ryan ,  DAI, Donghua ,  FELL, Jay Bradford ,  FISCHER John, Peter ,  HILTON, Michael Christopher ,  KAHN, Dean Russell ,  MEJIA, Macedonio Junior ,  NGUYEN, Phong ,  PAJK, Spencer ,  RODRIGUEZ, Martha E. ,  SAVECHENKOV, Pavel Yu ,  TANG, Tony Pisal

IPC: A61K31/4353 ,  A61K31/519 ,  C07D471/04

Abstract: The present invention relates to compounds that inhibit KRas G12D. In particular, the present invention relates to compounds that inhibit the activity of KRas G12D, pharmaceutical compositions comprising the compounds and methods of use therefor.

公开(公告)号：WO2013074641A1

公开(公告)日：2013-05-23

申请号：PCT/US2012/065036

申请日：2012-11-14

Applicant: ARRAY BIOPHARMA INC. ,  FELL, Jay Bradford ,  FISCHER, John P. ,  HINKLIN, Ronald J.

Inventor： FELL, Jay Bradford ,  FISCHER, John P. ,  HINKLIN, Ronald J.

IPC: C07D401/04 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  A61K31/454 ,  A61K31/4545 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10

CPC classification number: C07D417/14 ,  C07D401/04 ,  C07D401/14 ,  C07D413/14

Abstract: Compounds of Formula I: and pharmaceutically acceptable salts thereof, in which X 1 , X 2 , R 3 , R 4 , R 5 , R x , R 7 , R 9 , R 10 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，R3，R4，R5，Rx，R7，R9，R10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，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：WO2016090285A1

公开(公告)日：2016-06-09

申请号：PCT/US2015/064062

申请日：2015-12-04

Applicant: ARRAY BIOPHARMA INC. ,  CELGENE CORPORATION

Inventor： ALLEN, Shelley ,  BOYS, Mark Laurence ,  CHICARELLI, Mark J. ,  FELL, Jay Bradford ,  FISCHER, John P. ,  GAUDINO, John ,  HICKEN, Erik James ,  HINKLIN, Ronald Jay ,  KRASER, Christopher F. ,  LAIRD, Ellen ,  ROBINSON, John E. ,  TANG, Tony P. ,  BURGESS, Laurence E. ,  RIEGER, Robert Andrew ,  PHENEGER, Jed ,  SATOH, Yoshitaka ,  LEFTHERIS, Katerina ,  RAHEJA, Raj K. ,  BENNETT, Brydon L.

IPC: C07D487/04 ,  A61K31/4985 ,  A61P29/00 ,  A61P37/00

CPC classification number: C07D487/04 ,  A61K31/4985 ,  A61K31/5377 ,  A61K45/06

Abstract: Compounds of Formula I: and stereoisomers and pharmaceutically acceptable salts and solvates thereof in which R 1 , R 2 , R 3 and R 4 have the meanings given in the specification, are inhibitors of one or more JAK kinases and are useful in the treatment of JAK kinase-associated diseases and disorders, such as 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化合物及其立体异构体及其药学上可接受的盐和溶剂化物，其中R1，R2，R3和R4具有说明书中给出的含义，是一种或多种JAK激酶的抑制剂，并且可用于治疗JAK激酶相关 疾病和病症，例如自身免疫性疾病，炎症性疾病，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：WO2022031678A1

公开(公告)日：2022-02-10

申请号：PCT/US2021/044308

申请日：2021-08-03

Applicant: MIRATI THERAPEUTICS, INC. ,  ARRAY BIOPHARMA INC.

Inventor： WANG, Xiaolun ,  LAWSON, John David ,  MARX, Matthew Arnold ,  ALLEN, Shelley ,  BARBOUR, Patrick Michael ,  BLAKE, James Francis ,  DAHLKE, Joshua Ryan ,  DAI, Donghua ,  FELL, Jay Bradford ,  FISCHER, John Peter ,  HASSANIEN, Sherif Hosam ,  HILTON, Michael Christopher ,  MEJIA, Macedonio, Junior ,  O'LEARY, Jacob Matthew ,  TANG, Tony Pisal

IPC: A61P35/00 ,  C07D417/14 ,  A61K31/517

Abstract: The present invention relates to compounds that inhibit KRas G12D. In particular, the present invention relates to compounds that inhibit the activity of KRas G12D, pharmaceutical compositions comprising the compounds and methods of use therefor.

公开(公告)号：WO2020201991A1

公开(公告)日：2020-10-08

申请号：PCT/IB2020/053019

申请日：2020-03-30

Applicant: ARRAY BIOPHARMA INC.

Inventor： BLAKE, James F. ,  BOYS, Mark Laurence ,  CHICARELLI, Mark Joseph ,  COOK, Adam W. ,  ELSAYED, Mohamed S. A. ,  FELL, Jay Bradford ,  FISCHER, John P. ,  HINKLIN, Ronald Jay ,  JIANG, Yutong ,  MCNULTY, Oren T. ,  MEJIA, Macedonio J. ,  RODRIGUEZ, Martha E. ,  WONG, Christina E.

IPC: C07D401/14 ,  C07D403/04 ,  C07D451/04 ,  C07D471/10 ,  C07D491/107 ,  C07D519/00 ,  A61K31/53 ,  A61P35/00 ,  C07D513/10

Abstract: Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt 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.

公开(公告)号：WO2022098625A1

公开(公告)日：2022-05-12

申请号：PCT/US2021/057672

申请日：2021-11-02

Applicant: MIRATI THERAPEUTICS, INC. ,  ARRAY BIOPHARMA INC.

Inventor： MARX, Matthew Arnold ,  LAWSON, John David ,  DOERNER BARBAUR, Patrick Michael ,  BLAKE, James Francis ,  FELL, Jay Bradford ,  FISCHER, John, Peter ,  NEWHOUSE, Bradley J. ,  NGUYEN, Phong ,  O'LEARY, Jacob M. ,  PAJK, Spencer ,  RODRIGUEZ, Martha E. ,  TANG, Tony Pisal

IPC: A61P35/00 ,  C07D417/14 ,  A61K31/517

Abstract: The present invention relates to compounds that inhibit KRas G12D. In particular, the present invention relates to compounds that inhibit the activity of KRas G12D, pharmaceutical compositions comprising the compounds and methods of use therefor.

公开(公告)号：WO2021041671A1

公开(公告)日：2021-03-04

申请号：PCT/US2020/048194

申请日：2020-08-27

Applicant: MIRATI THERAPEUTICS, INC. ,  ARRAY BIOPHARMA INC.

Inventor： WANG, Xiaolun ,  BURNS, Aaron Craig ,  CHRISTENSEN, James Gail ,  KETCHAM, John Michael ,  LAWSON, John David ,  MARX, Matthew Arnold ,  SMITH, Christopher Ronald ,  ALLEN, Shelley ,  BLAKE, James Francis ,  CHICARELLI, Mark Joseph ,  DAHLKE, Joshua Ryan ,  DAI, Donghua ,  FELL, Jay Bradford ,  FISCHER, John Peter ,  MEJIA, Macedonio J. ,  NEWHOUSE, Brad ,  NGUYEN, Phong ,  O'LEARY, Jacob Matthew ,  PAJK, Spencer ,  RODRIGUEZ, Martha E. ,  SAVECHENKOV, Pavel ,  TANG, Tony P. ,  VIGERS, Guy P. A. ,  ZHAO, Qian

IPC: A61K31/435 ,  A61K31/4375 ,  A61K31/517 ,  C07D471/00 ,  C07D471/02 ,  C07D471/04

Abstract: The present invention relates to compounds that inhibit KRas G12D. In particular, the present invention relates to compounds that inhibit the activity of KRas G12D, pharmaceutical compositions comprising the compounds and methods of use therefor.

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：WO2013066869A1

公开(公告)日：2013-05-10

申请号：PCT/US2012/062576

申请日：2012-10-30

Applicant: ARRAY BIOPHARMA INC. ,  AICHER, Thomas Daniel ,  BENSCIK, Josef Roland ,  BOYD, Steven Armen ,  CONDROSKI, Kevin Ronald ,  FELL, Jay Bradford ,  FISCHER, John Peter ,  HINKLIN, Ronald Jay ,  PRATT, Scott ,  SINGH, Ajay ,  TURNER, Timothy M.

Inventor： AICHER, Thomas Daniel ,  BENSCIK, Josef Roland ,  BOYD, Steven Armen ,  CONDROSKI, Kevin Ronald ,  FELL, Jay Bradford ,  FISCHER, John Peter ,  HINKLIN, Ronald Jay ,  PRATT, Scott ,  SINGH, Ajay ,  TURNER, Timothy M.

IPC: C07D413/14 ,  C07D417/14 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/433 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P9/12 ,  A61P9/00 ,  A61P25/28 ,  A61P25/18

CPC classification number: C07D417/14 ,  C07D413/14

Abstract: Compounds of Formula (I) and pharmaceutically acceptable salts thereof in which X 1 , X 2 , X 3 , L, R 3 , R 4 , R 5 , R 7 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，X3，L，R3，R4，R5，R7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，可用于治疗或预防 的疾病，例如但不限于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。

公开(公告)号：WO2012037393A1

公开(公告)日：2012-03-22

申请号：PCT/US2011/051821

申请日：2011-09-15

Applicant: ARRAY BIOPHARMA INC. ,  AICHER, Thomas Daniel ,  BENCSIK, Josef R. ,  BOYD, Steven Armen ,  CONDROSKI, Kevin Ronald ,  FELL, Jay Bradford ,  FISCHER, John P. ,  HINKLIN, Ronald Jay ,  PRATT, Scott Alan ,  SINGH, Ajay ,  TURNER, Timothy M.

Inventor： AICHER, Thomas Daniel ,  BENCSIK, Josef R. ,  BOYD, Steven Armen ,  CONDROSKI, Kevin Ronald ,  FELL, Jay Bradford ,  FISCHER, John P. ,  HINKLIN, Ronald Jay ,  PRATT, Scott Alan ,  SINGH, Ajay ,  TURNER, Timothy M.

IPC: A61K31/4468 ,  A61K31/454 ,  A61P3/04 ,  C07D413/14

CPC classification number: C07D413/14 ,  A61K31/4468 ,  A61K31/454 ,  C07D211/76 ,  C07D401/04 ,  C07D401/14

Abstract: Compounds of Formula (I) and pharmaceutically acceptable salts thereof in which X 1 , X 2 , L, R 3 , R 4 , R 5 , R 7 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，R7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，可用于治疗或预防疾病 例如但不限于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。