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公开(公告)号：WO2018136663A1
公开(公告)日：2018-07-26
申请号：PCT/US2018/014281
申请日：2018-01-18
Applicant: ARRAY BIOPHARMA, INC.
Inventor： ANDREWS, Steven W. , BLAKE, James F. , HAAS, Julia , JIANG, Yutong
IPC: C07D401/14 , C07D413/14 , C07D417/14 , A61P35/00 , A61K31/506
Abstract: Provided herein are compounds of the Formula (I): and pharmaceutically acceptable salts or solvates thereof, where A, B, Y, X 1 , X 2 , X 3 , X 4 , R 1 , R 2 , n and m are as defined 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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2.发明申请
公开(公告)号：WO2009089462A1
公开(公告)日：2009-07-16
申请号：PCT/US2009/030617
申请日：2009-01-09
Applicant: ARRAY BIOPHARMA INC. , GENENTECH, INC. , BANKA, Anna , BENCSIK, Josef R. , BLAKE, James F. , HENTEMANN, Martin F. , KALLAN, Nicholas C. , LIANG, Jun , MITCHELL, Ian S. , SCHLACHTER, Stephen T. , WALLACE, Eli M. , XU, Rui , TANG, Tony, P.
Inventor： BANKA, Anna , BENCSIK, Josef R. , BLAKE, James F. , HENTEMANN, Martin F. , KALLAN, Nicholas C. , LIANG, Jun , MITCHELL, Ian S. , SCHLACHTER, Stephen T. , WALLACE, Eli M. , XU, Rui , TANG, Tony, P.
IPC: C07D239/70 , A61K31/517 , A61P35/00 , C07D401/04 , C07D401/10 , C07D409/04 , C07D417/04 , C07D487/04
CPC classification number: C07D401/10 , C07D211/08 , C07D211/46 , C07D239/70 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/10 , C07D409/04 , C07D417/04 , C07D417/10 , C07D487/04
Abstract: Compounds of Formula I are useful for inhibiting AKT protein kinases. 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化合物可用于抑制AKT蛋白激酶。 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。 式（I）。
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3.发明申请
公开(公告)号：WO2009089459A1
公开(公告)日：2009-07-16
申请号：PCT/US2009/030610
申请日：2009-01-09
Applicant: ARRAY BIOPHARMA INC. , GENENTECH, INC. , BENCSIK, Josef R. , BLAKE, James F. , KALLAN, Nicholas C. , MITCHELL, Ian S. , SPENCER, Keith Lee , XIAO, Dengming , XU, Rui , CHABOT, Christine , DO, Steven , LIANG, Jun , SAFINA, Brian , ZHANG, Birong
Inventor： BENCSIK, Josef R. , BLAKE, James F. , KALLAN, Nicholas C. , MITCHELL, Ian S. , SPENCER, Keith Lee , XIAO, Dengming , XU, Rui , CHABOT, Christine , DO, Steven , LIANG, Jun , SAFINA, Brian , ZHANG, Birong
IPC: C07D239/70 , A61K31/517 , A61P35/00
CPC classification number: C07D239/70
Abstract: The present invention provides compounds, including pharmaceutically acceptable salts thereof, comprising the Formula (I): Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases, such as cancer.
Abstract translation: 本发明提供包含式（I）的化合物，包括其药学上可接受的盐：还提供使用本发明化合物作为AKT蛋白激酶抑制剂和治疗过度增殖性疾病如癌症的方法。
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4.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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5.发明申请N-(ARYLALKYL)-N'-PYRAZOLYL-UREA, THIOUREA, GUANIDINE AND CYANOGUANIDINE COMPOUNDS AS TRKA KINASE INHIBITORS 审中-公开作为TRKA激酶抑制剂的N-（ARYLALKYL）-N'-吡唑并 - 尿素，硫脲，胍和氰基胍化合物
公开(公告)号：WO2014078331A1
公开(公告)日：2014-05-22
申请号：PCT/US2013/069750
申请日：2013-11-12
Applicant: ARRAY BIOPHARMA INC. , BLAKE, James F. , BRANDHUBER, Barbara J. , HAAS, Julia , NEWHOUSE, Brad , THOMAS, Allen A. , WINSKI, Shannon L.
Inventor： BLAKE, James F. , BRANDHUBER, Barbara J. , HAAS, Julia , NEWHOUSE, Brad , THOMAS, Allen A. , WINSKI, Shannon L.
IPC: C07D403/12 , C07D401/14 , C07D231/40 , C07D231/52 , C07D231/54 , C07D401/04 , C07D401/12 , C07D403/04 , C07D413/12 , C07D495/04 , A61K31/4155 , A61P35/00 , A61P29/00
CPC classification number: C07D231/52 , C07D231/38 , C07D231/40 , C07D231/54 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/12 , C07D453/02 , C07D495/04
Abstract: Compounds of Formula I or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C, X, Ra, Rb, Rc, Rd and n 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，溶剂合物或前药的化合物，其中环A，环C，X，R a，R b，R c，R d和n如本文所定义，是TrkA激酶的抑制剂，并且是有用的 治疗可用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治疗的疾病。
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Patent Agency Ranking6.发明申请DIHYDROTHIENO PYRIMIDINES AS AKT PROTEIN KINASE INHIBITORS 审中-公开DIHYDROTHIENO PYRIMIDINES作为AKT蛋白激酶抑制剂
公开(公告)号：WO2008006039A1
公开(公告)日：2008-01-10
申请号：PCT/US2007/072884
申请日：2007-07-05
Applicant: ARRAY BIOPHARMA INC. , MITCHELL, Ian S. , BLAKE, James F. , XU, Rui , KALLAN, Nicholas C. , XIAO, Dengming , SPENCER, Keith Lee , BENCSIK, Josef R.
Inventor： MITCHELL, Ian S. , BLAKE, James F. , XU, Rui , KALLAN, Nicholas C. , XIAO, Dengming , SPENCER, Keith Lee , BENCSIK, Josef R.
IPC: C07D495/04 , A61K31/519 , A61P35/00
CPC classification number: C07D495/04
Abstract: The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula (I): Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.
Abstract translation: 本发明提供包含式（I）的分解的对映体，非对映异构体，溶剂化物和药学上可接受的盐的化合物：还提供了使用本发明化合物作为AKT蛋白激酶抑制剂和用于治疗过度增殖性疾病 作为癌症。
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7.发明申请CYCLOPENTA [D] PYRIMIDINES AS AKT PROTEIN KINASE INHIBITORS 审中-公开CYCLOPENTA [D] PYRIMININES作为AKT蛋白激酶抑制剂
公开(公告)号：WO2008006032A1
公开(公告)日：2008-01-10
申请号：PCT/US2007/072876
申请日：2007-07-05
Applicant: ARRAY BIOPHARMA INC. , GENENTECH, INC. , MITCHELL, Ian S. , BLAKE, James F. , XU, Rui , KALLAN, Nicholas C. , XIAO, Dengming , SPENCER, Keith Lee , BENCSIK, Josef R. , LIANG, Jun , SAFINA, Brian , LI, Jun , CHABOT, Christine
Inventor： MITCHELL, Ian S. , BLAKE, James F. , XU, Rui , KALLAN, Nicholas C. , XIAO, Dengming , SPENCER, Keith Lee , BENCSIK, Josef R. , LIANG, Jun , SAFINA, Brian , LI, Jun , CHABOT, Christine
IPC: C07D239/70 , C07D401/12 , C07D403/04 , C07D403/12 , C07D407/12 , C07D409/12 , C07D409/14 , A61K31/517 , A61P35/00
CPC classification number: C07D409/14 , A61K31/517 , A61K31/5377 , A61K45/06 , C07D239/70 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D409/12
Abstract: The present invention provides compounds of Formula I, including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. Formula (I). Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.
Abstract translation: 本发明提供了式I化合物，包括互变异构体，拆分的对映异构体，非对映异构体，溶剂合物，代谢物，盐和药学上可接受的前药。 式（I）。 还提供了使用本发明化合物作为AKT蛋白激酶抑制剂和治疗过度增殖性疾病如癌症的方法。
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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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