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公开(公告)号：WO2022003575A1
公开(公告)日：2022-01-06
申请号：PCT/IB2021/055832
申请日：2021-06-29
Applicant: ARRAY BIOPHARMA INC.
Inventor： BOYS, Mark Laurence , ELLIS, Bryan Daniel , GAUDINO, John Joseph , HICKEN, Erik James , LAIRD, Ellen Ruth , LAZZARA, Nicholas Charles , NEWHOUSE, Bradley Jon , PAJK, Spencer Phillip
IPC: A61P35/00 , C07D487/04 , A61K31/519
Abstract: This invention relates to compounds of Formula (I), and enantiomers thereof, and to pharmaceutically acceptable salts of Formula (I) and said enantiomers, wherein L1, L2, R1, R2, R3 and n are as defined herein. The invention further relates to pharmaceutical compositions comprising such compounds and salts, and to methods and uses of such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer, in a subject in need thereof.
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2.发明申请SUBSTITUTED N-(1H-INDAZOL-4-YL)IMIDAZO[1,2-a]PYRIDINE-3-CARBOXAMIDE COMPOUNDS AS TYPE III RECEPTOR TYROSINE KINASE INHIBITORS 审中-公开取代的N-（1H-咪唑-4-基）咪唑并[1,2-a]吡啶-3-羧酸酰胺化合物作为III型受体酪氨酸激酶抑制剂
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。
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公开(公告)号：WO2013055645A1
公开(公告)日：2013-04-18
申请号：PCT/US2012/059282
申请日：2012-10-09
Applicant: ARRAY BIOPHARMA INC. , BOYS, Mark Laurence , BURGESS, Laurence E. , EARY, C. Todd , GRONEBERG, Robert , HACHE, Bruno P. , HARVEY, Darren , HICKEN, Erik James , KRASER, Christopher F. , LAIRD, Ellen , MORENO, David A. , MUNSON, Mark C. , REN, Li , ROBINSON, John E. , SCHLACHTER, Stephen T.
Inventor： BOYS, Mark Laurence , BURGESS, Laurence E. , EARY, C. Todd , GRONEBERG, Robert , HACHE, Bruno P. , HARVEY, Darren , HICKEN, Erik James , KRASER, Christopher F. , LAIRD, Ellen , MORENO, David A. , MUNSON, Mark C. , REN, Li , ROBINSON, John E. , SCHLACHTER, Stephen T.
IPC: C07D487/04 , A61K31/519 , A61P29/00 , A61P37/00
CPC classification number: C07D487/04
Abstract: Compounds of Formula I: and stereoisomers and pharmaceutically acceptable salts and solvates thereof in which R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , X 1 and X 2 have the meanings given in the specification, are inhibitors of one or more JAK kinases and are useful in the treatment of autoimmune diseases, inflammatory diseases, rejection of transplanted organs, tissues and cells, as well as hematologic disorders and malignancies and their co-morbidities.
Abstract translation: R 1，R 2，R 3，R 4，R 5，R 6，X 1和X 2具有本说明书中给出的含义的式I化合物及其立体异构体及其药学上可接受的盐和溶剂合物是一种或多种JAK激酶的抑制剂，并且是有用的 治疗自身免疫性疾病，炎症性疾病，移植器官，组织和细胞排斥，以及血液系统疾病和恶性肿瘤及其并发症。
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4.发明申请5, 7-SUBSTITUTED-IMIDAZO [1, 2-C] PYRIMIDINES AS INHIBITORS OF JAK KINASES 审中-公开作为JAK KINASES的抑制剂的5,7-取代的咪唑并[1,2-C]吡啶
公开(公告)号：WO2011130146A1
公开(公告)日：2011-10-20
申请号：PCT/US2011/031896
申请日：2011-04-11
Applicant: ARRAY BIOPHARMA INC. , BOYS, Mark Laurence , BURGESS, Laurence, E. , GRONEBERG, Robert, D. , HARVEY, Darren, M. , HUANG, Lily , KERCHER, Timothy , KRASER, Christopher, F. , LAIRD, Ellen , TARLTON, Eugene , ZHAO, Qian
Inventor： BOYS, Mark Laurence , BURGESS, Laurence, E. , GRONEBERG, Robert, D. , HARVEY, Darren, M. , HUANG, Lily , KERCHER, Timothy , KRASER, Christopher, F. , LAIRD, Ellen , TARLTON, Eugene , ZHAO, Qian
IPC: C07D487/04 , A61P29/00 , A61P37/00 , A61K31/519
CPC classification number: C07D487/04 , C07D498/04
Abstract: Compounds of Formula I: (Formula should be inserted here) and stereoisomers and pharmaceutically acceptable salts and solvates thereof in which R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , X 1 and X 2 have the meanings given in the specification, are inhibitors of one or more JAK kinases and are useful in the treatment of 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（此处应该插入式）及其其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，X 1和X 2具有本说明书中给出的含义的立体异构体及其药学上可接受的盐和溶剂化物是抑制剂 的一种或多种JAK激酶，并且可用于治疗自身免疫性疾病，炎性疾病，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。
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公开(公告)号：WO2019113190A1
公开(公告)日：2019-06-13
申请号：PCT/US2018/064039
申请日：2018-12-05
Applicant: ARRAY BIOPHARMA INC.
Inventor： ALLEN, Shelley , BOYS, Mark Laurence , COOK, Adam , GAUDINO, John , HINKLIN, Ronald Jay , LAIRD, Ellen , MCNULTY, Oren T. , METCALF, Andrew T. , NEWHOUSE, Brad , ROBINSON, John E.
IPC: C07D471/04 , A61P35/00 , A61K31/437
Abstract: Provided herein are compounds of the Formula (I): and stereoisomers, tautomers and pharmaceutically acceptable salts thereof, wherein Ring A, X 1 , X 2 , X 3 , R 1 , R 2 and R 3 are as defined herein, which are inhibitors of one or more TAM kinases and are useful in the treatment and prevention of diseases which can be treated with a TAM kinase inhibitor.
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Patent Agency Ranking6.发明申请4,6-SUBSTITUTED-PYRAZOLO[1,5-a]PYRAZINES AS JANUS KINASE INHIBITORS 审中-公开4,6-取代的吡唑并[1,5-a]吡啶作为JANUS KINASE INHIBITORS
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。
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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.
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公开(公告)号：WO2020081848A1
公开(公告)日：2020-04-23
申请号：PCT/US2019/056786
申请日：2019-10-17
Applicant: ARRAY BIOPHARMA INC. , BLAKE, James F. , BOYS, Mark Laurence , CHICARELLI, Mark Joseph , COOK, Adam , ELSAYED, Mohamed S. A. , FELL, Jay B. , FISCHER, John P. , HINKLIN, Ronald Jay , MCNULTY, Oren T. , MEJIA, Macedonio J. , RODRIGUEZ, Martha E. , WONG, Christina E.
Inventor： BLAKE, James F. , BOYS, Mark Laurence , CHICARELLI, Mark Joseph , COOK, Adam , ELSAYED, Mohamed S. A. , FELL, Jay B. , FISCHER, John P. , HINKLIN, Ronald Jay , MCNULTY, Oren T. , MEJIA, Macedonio J. , RODRIGUEZ, Martha E. , WONG, Christina E.
IPC: C07D401/04 , C07D471/04 , C07D519/00 , A61P35/00 , A61K31/498 , A61K31/4985
Abstract: Compounds of Formula la or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative diseases in the view of their ability to inhibit SHP2. Methods of using compounds of Formula I or a stereoisomer, tautomer 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.
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9.发明申请SUBSTITUTED N-(1H-INDAZOL-4-YL)IMIDAZO[1, 2-A]PYRIDINE-3- CARBOXAMIDE COMPOUNDS AS CFMS INHIBITORS 审中-公开取代的N-（1H-吲唑-4-基）咪唑并[1,2-A]吡啶-3-羧酰胺化合物作为CFMS抑制剂
公开(公告)号：WO2011079076A1
公开(公告)日：2011-06-30
申请号：PCT/US2010/061341
申请日：2010-12-20
Applicant: ARRAY BIOPHARMA INC. , BOYS, Mark Laurence , BRADLEY, Michael , DELISLE, Robert Kirk , HENNINGS, D. David , KENNEDY, April L. , MARMSATER, Fredrik P. , MEDINA, Matthew , MUNSON, Mark C. , RAST, Bryson , RIZZI, James P. , RODRIGUEZ, Martha E. , TOPALOV, George T. , ZHAO, Qian
Inventor： BOYS, Mark Laurence , BRADLEY, Michael , DELISLE, Robert Kirk , HENNINGS, D. David , KENNEDY, April L. , MARMSATER, Fredrik P. , MEDINA, Matthew , MUNSON, Mark C. , RAST, Bryson , RIZZI, James P. , RODRIGUEZ, Martha E. , TOPALOV, George T. , ZHAO, Qian
IPC: C07D471/04 , C07D519/00 , A61K31/437 , A61K31/4985 , A61P9/00 , A61P19/08 , A61P29/00 , A61P35/00
CPC classification number: C07D471/04 , C07D519/00
Abstract: Compounds of Formula (I): and pharmaceutically acceptable salts thereof in which R 1 , R 2 , R 3 , R 4 and R 5 have the meanings given in the specification, are inhibitors of cFMS and are useful in the treatment of bone-related diseases, cancer, autoimmune disorders, inflammatory diseases, cardiovascular diseases and pain.
Abstract translation: 其中R1，R2，R3，R4和R5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cFMS的抑制剂，可用于治疗骨相关疾病，癌症，自身免疫 疾病，炎性疾病，心血管疾病和疼痛。
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10.发明公开
公开(公告)号：EP3878451A1
公开(公告)日：2021-09-15
申请号：EP21152373.3
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: A61K31/4985 , C07D487/04 , A61P29/00 , A61P37/00
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.
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