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1.发明申请SUBSTITUTED PYRAZOLO[1,5-A]PYRIDINE COMPOUNDS AS RET KINASE INHIBITORS 审中-公开取代的吡唑并[1,5-A]吡啶化合物作为RET激酶抑制剂
公开(公告)号：WO2017011776A1
公开(公告)日：2017-01-19
申请号：PCT/US2016/042576
申请日：2016-07-15
Applicant: ARRAY BIOPHARMA, INC.
Inventor： ANDREWS, Steven W. , BLAKE, James F. , CHICARELLI, Mark J. , GOLOS, Adam , HAAS, Julia , JIANG, Yutong , KOLAKOWSKI, Gabrielle R.
IPC: C07D471/04 , A61K31/437 , A61P35/00 , A61P29/00
CPC classification number: C07D471/04 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/497 , A61K31/499 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D519/00
Abstract: Provided herein are compounds of the General Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, D, E, X 1 , X 2 , X 3 and X 4 have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including diseases or disorders mediated by a RET kinase.
Abstract translation: 本文提供了通式I的化合物及其立体异构体及其药学上可接受的盐或溶剂化物，其中A，B，D，E，X 1，X 2，X 3和X 4具有说明书中给出的含义，其为RET的抑制剂 激酶，并且可用于治疗和预防可用RET激酶抑制剂治疗的疾病，包括由RET激酶介导的疾病或病症。
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2.发明申请PYRROLIDINYL UREA AND PYRROLIDINYL THIOUREA COMPOUNDS AS TRKA KINASE INHIBITORS 审中-公开吡咯烷酮尿素和吡咯烷酮类化合物作为TRKA激酶抑制剂
公开(公告)号：WO2012158413A2
公开(公告)日：2012-11-22
申请号：PCT/US2012/037003
申请日：2012-05-09
Applicant: ARRAY BIOPHARMA INC. , ALLEN, Shelley , ANDREWS, Steven, W. , BLAKE, James, F. , CONDROSKI, Kevin, R. , HAAS, Julia , HUANG, Lily , JIANG, Yutong , KERCHER, Timothy , KOLAKOWSKI, Gabrielle R. , SEO, Jeongbeob
Inventor： ALLEN, Shelley , ANDREWS, Steven, W. , BLAKE, James, F. , CONDROSKI, Kevin, R. , HAAS, Julia , HUANG, Lily , JIANG, Yutong , KERCHER, Timothy , KOLAKOWSKI, Gabrielle R. , SEO, Jeongbeob
IPC: C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/04 , C07D495/04 , A61K31/4155 , A61K31/4162 , A61K31/4178 , A61K31/4192 , A61K31/4196 , A61K31/422 , A61K31/4245 , A61K31/427 , A61K31/4439 , A61K31/4375 , A61K31/454 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/5377 , A61P25/28 , A61P29/02 , A61P35/00 , A61P33/00
CPC classification number: C07D403/12 , A61K31/4155 , A61K31/4162 , A61K31/4178 , A61K31/4192 , A61K31/4196 , A61K31/422 , A61K31/4245 , A61K31/427 , A61K31/4375 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/5377 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/04 , C07D491/048 , C07D495/04 , Y02A50/414
Abstract: Compounds of Formula I: or stereoisomers, tautomers, or pharmaceutically acceptable salts, or solvates or prodrugs thereof, where R 1 , R 2 , R a , R b , R c , R d , X, Y, B, and Ring C are as defined herein, and wherein the Y-B moiety and the NH-C(=X)-NH moiety are in the trans configuration, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.
Abstract translation: 其中R1，R2，Ra，Rb，Rc，Rd，X，Y，B和环C如本文所定义的式I化合物或其立体异构体，互变异构体或其药学上可接受的盐或溶剂合物或前药，其中 YB部分和NH-C（= X）-NH部分是反式构型，是TrkA激酶的抑制剂，可用于治疗可用TrkA激酶抑制剂如疼痛，癌症，炎症治疗的疾病 ，神经变性疾病和某些传染病。
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公开(公告)号：WO2020055672A1
公开(公告)日：2020-03-19
申请号：PCT/US2019/049859
申请日：2019-09-06
Applicant: ARRAY BIOPHARMA INC.
Inventor： BLAKE, James F. , DAI, Donghua , HAAS, Julia , JIANG, Yutong , KAHN, Dean , KOLAKOWSKI, Gabrielle R. , MCFADDIN, Elizabeth A. , MCKENNEY, Megan L. , METCALF, Andrew T. , MORENO, David A. , PRIGARO, Brett , RAMANN, Ginelle A. , REN, Li , WALLS, Shane M. , ZHANG, Hailong
IPC: C07D487/14 , C07D487/22 , C07D498/14 , C07D498/22 , A61P35/00 , A61K31/551
Abstract: Provided herein are compounds of the Formula (I): (I) and tautomers, stereoisomers and pharmaceutically acceptable salts and solvates thereof, wherein R x , R y , W, X, Y, Z, Ring A and (AA) have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.
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公开(公告)号：WO2019143994A1
公开(公告)日：2019-07-25
申请号：PCT/US2019/014277
申请日：2019-01-18
Applicant: ARRAY BIOPHARMA INC.
Inventor： WALLS, Shane M. , REN, Li , RAMANN, Ginelle A. , MORENO, David A. , METCALF, Andrew T. , MCFADDIN, Elizabeth A. , KOLAKOWSKI, Gabrielle R. , BLAKE, James F. , DAI, Donghua , HAAS, Julia , JIANG, Yutong , KAHN, Dean
IPC: C07D471/04 , A61P35/00 , A61K31/437
Abstract: Provided herein are compounds of the Formula I: and tautomers and pharmaceutically acceptable salts and solvates thereof, wherein R 1 , R 2 and R 3 have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.
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公开(公告)号：WO2012118850A1
公开(公告)日：2012-09-07
申请号：PCT/US2012/027009
申请日：2012-02-28
Applicant: ARRAY BIOPHARMA INC. , GENENTECH, INC. , BLAKE, James F. , CHEN, Huifen , CHICARELLI, Mark Joseph , DEMEESE, Jason , GARREY, Rustam , GAUDINO, John J. , KAUS, Robert J. , KOLAKOWSKI, Gabrielle R. , MARLOW, Allison L. , MOHR, Peter J. , REN, Li , SCHWARZ, Jacob , SIEDEM, Christopher S. , THOMAS, Allen A. , WALLACE, Eli , WENGLOWSKY, Steven Mark
Inventor： BLAKE, James F. , CHEN, Huifen , CHICARELLI, Mark Joseph , DEMEESE, Jason , GARREY, Rustam , GAUDINO, John J. , KAUS, Robert J. , KOLAKOWSKI, Gabrielle R. , MARLOW, Allison L. , MOHR, Peter J. , REN, Li , SCHWARZ, Jacob , SIEDEM, Christopher S. , THOMAS, Allen A. , WALLACE, Eli , WENGLOWSKY, Steven Mark
IPC: C07D471/04 , A61K31/519 , A61P35/00
CPC classification number: C07D471/04 , A61K31/519 , A61K45/06 , C07D491/052
Abstract: Compounds having the formula I wherein Z, Z 1 Z 2 Z 3 , R 3a , R 3b and R b and 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Z，Z 1 Z 2 Z 3，R 3a，R 3b和R b如本文所定义是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。
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Patent Agency Ranking
公开(公告)号：WO2019143977A1
公开(公告)日：2019-07-25
申请号：PCT/US2019/014248
申请日：2019-01-18
Applicant: ARRAY BIOPHARMA INC.
Inventor： BLAKE, James F. , DAI, Donghua , HAAS, Julia , JIANG, Yutong , KOLAKOWSKI, Gabrielle R. , MCFADDIN, Elizabeth A. , MCKENNEY, Megan L. , METCALF, Andrew T. , MORENO, David A. , PRIGARO, Brett , RAMANN, Ginelle A. , REN, Li
IPC: C07D487/04 , A61P35/00 , A61K31/519
CPC classification number: C07D487/04 , A61P35/00
Abstract: Provided herein are compounds of the Formula I: [INSERT FORMULA I] and tautomers, stereoisomers and pharmaceutically acceptable salts and solvates thereof, wherein R1, R2 and Ry have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.
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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.
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8.发明申请PYRAZOLYL UREA, THIOUREA, GUANIDINE AND CYANOGUANIDINE COMPOUNDS AS TRKA KINASE INHIBITORS 审中-公开作为TRKA激酶抑制剂的吡咯烷酮，硫脲，胍和氰基化合物
公开(公告)号：WO2014078417A1
公开(公告)日：2014-05-22
申请号：PCT/US2013/069897
申请日：2013-11-13
Applicant: ARRAY BIOPHARMA INC. , BRANDHUBER, Barbara J. , JIANG, Yutong , KOLAKOWSKI, Gabrielle R. , WINSKI, Shannon L.
IPC: C07D403/12 , C07D401/14 , C07D403/14 , A61K31/4155 , A61K31/4412 , A61P29/00
CPC classification number: C07D403/14 , C07D401/14 , C07D403/12
Abstract: Compounds of Formula I: or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis or pelvic pain syndrome.
Abstract translation: 式I化合物或其立体异构体，互变异构体或其药学上可接受的盐，溶剂合物或前药，其中环A，环C和X如本文所定义，是TrkA激酶的抑制剂，并且可用于治疗可治疗的疾病 具有TrkA激酶抑制剂如疼痛，癌症，炎症/炎性疾病，神经变性疾病，某些感染性疾病，干燥综合征，子宫内膜异位症，糖尿病性周围神经病变，前列腺炎或骨盆疼痛综合征。
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9.发明申请N-BICYCLIC ARYL,N'-PYRAZOLYL UREA, THIOUREA, GUANIDINE AND CYANOGUANIDINE COMPOUNDS AS TRKA KINASE INHIBITORS 审中-公开N-BICYCLIC ARYL，N'-PYRAZOLYL UREA，THIOUREA，GUANIDINE AND CYANOGUANIDINE COMPOUNDS as TRKA KINASE INHIBITORS
公开(公告)号：WO2014078328A1
公开(公告)日：2014-05-22
申请号：PCT/US2013/069747
申请日：2013-11-12
Applicant: ARRAY BIOPHARMA INC. , ALLEN, Shelley , BLAKE, James F. , BRANDHUBER, Barbara J. , JIANG, Yutong , KOLAKOWSKI, Gabrielle R. , XU, Rui , WINSKI, Shannon L.
Inventor： ALLEN, Shelley , BLAKE, James F. , BRANDHUBER, Barbara J. , JIANG, Yutong , KOLAKOWSKI, Gabrielle R. , XU, Rui , WINSKI, Shannon L.
IPC: C07D401/14 , C07D231/40 , C07D231/44 , C07D231/56 , C07D401/04 , C07D401/12 , A61K31/415 , A61P29/00 , A61P35/00 , A61P25/28
CPC classification number: C07D401/14 , C07D231/40 , C07D231/44 , C07D231/52 , C07D231/56 , C07D401/04 , C07D401/12 , C07D403/04
Abstract: Compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis or pelvic pain syndrome.
Abstract translation: 式（I）的化合物或其立体异构体，互变异构体或其药学上可接受的盐，溶剂合物或前药，其中环A，环C和X如本文所定义，是TrkA激酶的抑制剂，并且可用于治疗可以 用TrkA激酶抑制剂治疗，如疼痛，癌症，炎症/炎性疾病，神经变性疾病，某些传染病，干燥综合征，子宫内膜异位症，糖尿病性周围神经病变，前列腺炎或骨盆疼痛综合征。
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公开(公告)号：EP3523301B1
公开(公告)日：2020-05-27
申请号：EP17787843.6
申请日：2017-10-10
Applicant: Array Biopharma Inc.
Inventor： ANDREWS, Steven W. , ARONOW, Sean , BLAKE, James F. , BRANDHUBER, Barbara J. , COOK, Adam , HAAS, Julia , JIANG, Yutong , KOLAKOWSKI, Gabrielle R. , MCFADDIN, Elizabeth A. , MCKENNEY, Megan L. , MCNULTY, Oren T. , METCALF, Andrew T. , MORENO, David A. , TANG, Tony P. , REN, Li
IPC: C07D471/04 , A61K31/437 , A61P35/00
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