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：WO2012082689A1

公开(公告)日：2012-06-21

申请号：PCT/US2011/064549

申请日：2011-12-13

Applicant: ARRAY BIOPHARMA INC. ,  BOYS, Mark Laurence ,  DELISLE, Robert Kirk ,  HICKEN, Erik James ,  KENNEDY, April L. ,  MARESKA, David A. ,  MARMSATER, Fredrik P. ,  MUNSON, Mark C. ,  NEWHOUSE, Brad ,  RAST, Bryson ,  RIZZI, James P. ,  RODRIGUEZ, Martha E. ,  TOPALOV, George T. ,  ZHAO, Qian

Inventor： BOYS, Mark Laurence ,  DELISLE, Robert Kirk ,  HICKEN, Erik James ,  KENNEDY, April L. ,  MARESKA, David A. ,  MARMSATER, Fredrik P. ,  MUNSON, Mark C. ,  NEWHOUSE, Brad ,  RAST, Bryson ,  RIZZI, James P. ,  RODRIGUEZ, Martha E. ,  TOPALOV, George T. ,  ZHAO, Qian

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

CPC classification number: C07D471/04 ,  A61K31/496 ,  A61K45/06

Abstract: Compounds of Formula I: and pharmaceutically acceptable salts thereof in which R 1 , R 2 , R 3 , R 4 , R 5 and R 6 have the meanings given in the specification, are inhibitors of cFMS and are useful in the treatment of fibrosis, bone-related diseases, cancer, autoimmune disorders, inflammatory diseases, cardiovascular diseases, pain and burns in a mammal.

Abstract translation: 式I化合物及其药学上可接受的盐，其中R 1，R 2，R 3，R 4，R 5和R 6具有说明书中给出的含义，是cFMS的抑制剂，可用于治疗纤维化，骨相关疾病，癌症 ，自身免疫性疾病，炎性疾病，心血管疾病，哺乳动物的疼痛和灼伤。

公开(公告)号：WO2006119146A1

公开(公告)日：2006-11-09

申请号：PCT/US2006/016526

申请日：2006-05-01

Applicant: ARRAY BIOPHARMA INC. ,  HANS, Jeremy ,  WALLACE, Eli M. ,  ZHAO, Qian ,  ALLEN, Shelley ,  LAIRD, Ellen ,  LYSSIKATOS, Joseph P. ,  ROBINSON, John E. ,  CORRETTE, Christopher P. ,  DELISLE, Robert Kirk

Inventor： HANS, Jeremy ,  WALLACE, Eli M. ,  ZHAO, Qian ,  ALLEN, Shelley ,  LAIRD, Ellen ,  LYSSIKATOS, Joseph P. ,  ROBINSON, John E. ,  CORRETTE, Christopher P. ,  DELISLE, Robert Kirk

IPC: C07D417/04

CPC classification number: C07D513/04 ,  C07D285/12 ,  C07D417/04 ,  C07D417/14 ,  C07D419/04 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D497/04 ,  C07F9/65395

Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.

Abstract translation: 本发明涉及有丝分裂驱动蛋白，特别是KSP的抑制剂，以及生产这些抑制剂的方法。 本发明还提供了包含本发明抑制剂的药物组合物以及使用该抑制剂和药物组合物治疗和预防各种疾病的方法。

公开(公告)号：WO2004046101A3

公开(公告)日：2004-06-03

申请号：PCT/US2003/035670

申请日：2003-11-10

Applicant: ARRAY BIOPHARMA, INC.

Inventor： WALLACE, Eli ,  TOPALOV, George ,  ZHAO, Qian

IPC: C07D239/94

Abstract: Cyanoguanidine quinazoline and cyanoamidine quinazolamine derivatives that are useful in the treatment of hyperproliferative diseases are disclosed. Use of the compounds of the invention to manufacture therapeutic compositions for the treatment of hyperproliferative diseases in mammals is also disclosed.

公开(公告)号：WO2022015375A1

公开(公告)日：2022-01-20

申请号：PCT/US2021/019678

申请日：2021-02-25

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: C07D471/04 ,  A61K31/519 ,  A61P35/00

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：WO2017075107A9

公开(公告)日：2017-05-04

申请号：PCT/US2016/058951

申请日：2016-10-26

Applicant: THE REGENTS OF THE UNIVERSITY OF COLORADO, A BODY CORPORATE ,  LOXO ONCOLOGY, INC. ,  ARRAY BIOPHARMA INC.

Inventor： ANDREWS, Steven W. ,  KOLAKOWSKI, Gabrielle R. ,  DOEBELE, Robert C. ,  NANDA, Nisha ,  BILENKER, Josh H. ,  BLAKE, James F. ,  BRANDHUBER, Barbara J. ,  ZHAO, Qian

IPC: A61K31/5025 ,  A61K31/519 ,  C12Q1/68 ,  A61P35/00 ,  G01N33/574

Abstract: Provided herein are methods of treating a subject having a cancer, methods of selecting a treatment for a subject having a cancer, methods of selecting a subject having a cancer for a treatment that does not include a Trk inhibitor, methods of determining the likelihood that a subject having a cancer will have a positive response to a treatment with a Trk inhibitor, methods of predicting the efficacy of a Trk inhibitor in a subject having cancer, methods of determining a subject's risk for developing a Trk inhibitor-resistant cancer, and methods of determining the presence of a Trk inhibitor-resistant cancer in a subject, based on the detection of a cell from a sample from the subject that has at least one of the the point mutations in NTRK1 and/or NTRK2 and/or NTRK3.

公开(公告)号：WO2011146336A1

公开(公告)日：2011-11-24

申请号：PCT/US2011/036452

申请日：2011-05-13

Applicant: ARRAY BIOPHARMA INC. ,  ANDREWS, Steven, Wade ,  CONDROSKI, Kevin, Ronald ,  HAAS, Julia ,  JIANG, Yutong ,  KOLAKOWSKI, Gabrielle, R. ,  SEO, Jeongbeob ,  YANG, Hong-Woon ,  ZHAO, Qian

Inventor： ANDREWS, Steven, Wade ,  CONDROSKI, Kevin, Ronald ,  HAAS, Julia ,  JIANG, Yutong ,  KOLAKOWSKI, Gabrielle, R. ,  SEO, Jeongbeob ,  YANG, Hong-Woon ,  ZHAO, Qian

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

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, R 2 , R 2a , R 3 , R 3a , 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：WO2010022076A1

公开(公告)日：2010-02-25

申请号：PCT/US2009/054193

申请日：2009-08-18

Applicant: ARRAY BIOPHARMA INC. ,  ALLEN, Shelley ,  CELESTE, Laura L. ,  DAVIS, T. Gregg ,  DELISLE, Robert Kirk ,  GRESCHUK, Julie Marie ,  GROSS, Stefan, D. ,  HICKEN, Erik, James ,  JACKSON, Leila, J. ,  LYSSIKATOS, Joseph, P. ,  KALLAN, Nicholas C. ,  MARMSATER, Fredrik, P. ,  MUNSON, Mark, C. ,  PHENEGER, Jed ,  RAST, Bryson ,  ROBINSON, John, E. ,  SCHLACHTER, Stephen T. ,  TOPALOV, George T. ,  WRIGHT, A. Dale ,  ZHAO, Qian

Inventor： ALLEN, Shelley ,  CELESTE, Laura L. ,  DAVIS, T. Gregg ,  DELISLE, Robert Kirk ,  GRESCHUK, Julie Marie ,  GROSS, Stefan, D. ,  HICKEN, Erik, James ,  JACKSON, Leila, J. ,  LYSSIKATOS, Joseph, P. ,  KALLAN, Nicholas C. ,  MARMSATER, Fredrik, P. ,  MUNSON, Mark, C. ,  PHENEGER, Jed ,  RAST, Bryson ,  ROBINSON, John, E. ,  SCHLACHTER, Stephen T. ,  TOPALOV, George T. ,  WRIGHT, A. Dale ,  ZHAO, Qian

IPC: C07D471/04 ,  A61K31/47

CPC classification number: C07D471/04

Abstract: Compounds of Formula (I), in which A, B, R 1 , R 1a , R 2 , R 3 , R 4 , R 5 , R 6 , and R 7 have the meanings given in the specification, are receptor tyrosine inhibitors useful in the treatment of immune cell-associated diseases and disorders, such as inflammatory and autoimmune diseases.

Abstract translation: 其中A，B，R1，R1a，R2，R3，R4，R5，R6和R7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细胞相关的受体酪氨酸抑制剂 疾病和病症，如炎性和自身免疫性疾病。

公开(公告)号：WO2008042928A2

公开(公告)日：2008-04-10

申请号：PCT/US2007/080246

申请日：2007-10-03

Applicant: ARRAY BIOPHARMA, INC. ,  AHRENDT, Kateri ,  DELISLE, Robert, Kirk ,  HANS, Jeremy ,  LYSSIKATOS, Joseph, P. ,  ROBINSON, John, E. ,  WALLACE, Eli, M. ,  ZHAO, Qian

Inventor： AHRENDT, Kateri ,  DELISLE, Robert, Kirk ,  HANS, Jeremy ,  LYSSIKATOS, Joseph, P. ,  ROBINSON, John, E. ,  WALLACE, Eli, M. ,  ZHAO, Qian

IPC: C07D285/12 ,  C07D413/06 ,  C07D413/12 ,  A61K31/433 ,  A61P35/00

CPC classification number: C07D285/12 ,  C07D413/06 ,  C07D413/12

Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment of various disorders.

Abstract translation: 本发明涉及有丝分裂驱动蛋白抑制剂，特别是KSP，以及制备这些抑制剂的方法。 本发明还提供包含本发明抑制剂的药物组合物和利用抑制剂和药物组合物治疗各种疾病的方法。

公开(公告)号：WO2007059257A3

公开(公告)日：2007-05-24

申请号：PCT/US2006/044431

申请日：2006-11-15

Applicant: ARRAY BIOPHARMA, INC. ,  LYSSIKATOS, Joseph, P. ,  MARMSATER, Fredrik, P. ,  ZHAO, Qian ,  GRESCHUK, Julie, Marie

Inventor： LYSSIKATOS, Joseph, P. ,  MARMSATER, Fredrik, P. ,  ZHAO, Qian ,  GRESCHUK, Julie, Marie

IPC: C07D413/14 ,  C07D417/14 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D495/04 ,  A61K31/517 ,  A61P35/00

Abstract: This invention provides compounds of Formula (I), wherein B, G, A, E, R 1 , R 2 , R 3 , m and n are as defined herein, which are useful as type I receptor tyrosine kinase inhibitors, and methods of use thereof in the treatment of hyperproliferative disorders in mammals.