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1.SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS TRK KINASE INHIBITORS 审中-公开
Title translation: 取代的吡唑并[1,5-a]吡嗪化合物作为TRK激酶抑制剂公开(公告)号:WO2011006074A1
公开(公告)日:2011-01-13
申请号:PCT/US2010/041538
申请日:2010-07-09
Applicant: ARRAY BIOPHARMA INC. , ALLEN, Shelley , ANDREWS, Steven S. , CONDROSKI, Kevin Ronald , HAAS, Julia , HUANG, Lily , JIANG, Yutong , KERCHER, Timothy , SEO, Jeongbeob
Inventor: ALLEN, Shelley , ANDREWS, Steven S. , CONDROSKI, Kevin Ronald , HAAS, Julia , HUANG, Lily , JIANG, Yutong , KERCHER, Timothy , SEO, Jeongbeob
IPC: C07D487/04 , A61K31/519 , C07D519/00
CPC classification number: C07D487/04 , A61K31/519 , A61K31/5377 , C07D453/02 , C07D471/22 , C07D498/22 , C07D519/00
Abstract: Compounds of Formula (I) and salts thereof in which R 1 , R 2 , R 3 , R 4 , X, Y and n have the meanings given in the specification, are inhibitors of Trk kinases and are useful in the treatment of diseases which can be treated with a Trk kinase inhibitor such as pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.
Abstract translation: 其中R1,R2,R3,R4,X,Y和n具有本说明书中给出的含义的式(I)化合物及其盐是Trk激酶的抑制剂,可用于治疗可用 一种Trk激酶抑制剂,如疼痛,癌症,炎症,神经变性疾病和某些传染病。
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2.BICYCLIC HETEROARYL UREA, THIOUREA, GUANIDINE AND CYANOGUANIDINE COMPOUNDS AS TRKA KINASE INHIBITORS 审中-公开
Title translation: 作为TRKA激酶抑制剂的双相异构尿素,硫脲,胍和氰基化合物公开(公告)号:WO2014078408A1
公开(公告)日:2014-05-22
申请号:PCT/US2013/069886
申请日:2013-11-13
Applicant: ARRAY BIOPHARMA INC. , ALLEN, Shelley , BRANDHUBER, Barbara J. , CONDROSKI, Kevin Ronald , HUANG, Lily , KERCHER, Timothy , WINSKI, Shannon L.
Inventor: ALLEN, Shelley , BRANDHUBER, Barbara J. , CONDROSKI, Kevin Ronald , HUANG, Lily , KERCHER, Timothy , WINSKI, Shannon L.
IPC: C07D231/56 , C07D471/04 , C07D487/04 , C07D491/048 , C07D495/04 , A61K31/4985 , A61K31/437 , A61K31/416 , A61P29/00 , A61P35/00 , A61P25/00 , A61P31/00
CPC classification number: C07D487/04 , C07D231/56 , C07D403/12 , C07D471/04 , C07D491/048 , C07D495/04 , C07D519/00
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 and pelvic pain syndrome.
Abstract translation: 其中环A,环C和X如本文所定义的式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是TrkA激酶的抑制剂,并且可用于治疗可以用 一种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,前列腺炎和骨盆疼痛综合征。
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3.PYRROLIDINYL UREA AND PYRROLIDINYL THIOUREA COMPOUNDS AS TRKA KINASE INHIBITORS 审中-公开
Title translation: 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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4.5, 7-SUBSTITUTED-IMIDAZO [1, 2-C] PYRIMIDINES AS INHIBITORS OF JAK KINASES 审中-公开
Title translation: 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:EP3299372B1
公开(公告)日:2020-01-08
申请号:EP17199899.0
申请日:2010-07-09
Applicant: Array Biopharma, Inc.
Inventor: ALLEN, Shelley , ANDREWS, Stephen, S. , CONDROSKI, Kevin Ronald , HAAS, Julia , HUANG, Lily , JIANG, Yutong , KERCHER, Timothy , SEO, Jeongbeob
IPC: C07D487/04 , A61K31/519 , C07D519/00 , C07D498/22 , C07D471/22 , C07D453/02 , A61K31/5377
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6.PYRROLIDINYL UREA, PYRROLIDINYL THIOUREA AND PYRROLIDINYL GUANIDINE COMPOUNDS AS TRKA KINASE INHIBITORS 有权
Title translation: 作为TRKA激酶抑制剂的吡咯烷基脲,吡咯烷基硫代脲和吡咯烷基胍的化合物公开(公告)号:EP2712358A2
公开(公告)日:2014-04-02
申请号:EP12743553.5
申请日:2012-05-09
Applicant: Array Biopharma, Inc.
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
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 R1, R2, Ra, Rb, Rc, Rd, 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: 式I化合物或其立体异构体,互变异构体或药学上可接受的盐或溶剂合物或前药:其中R 1,R 2,R a,R b,R c,R d,X,Y,B和环C为 如本文所定义,并且其中YB部分和NH-C(= X)-NH部分处于反式构型,是TrkA激酶的抑制剂并且可用于治疗可用TrkA激酶抑制剂治疗的疾病, 如疼痛,癌症,炎症,神经退行性疾病和某些传染病。
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7.5, 7-SUBSTITUTED-IMIDAZO [1, 2-C]PYRIMIDINES AS INHIBITORS OF JAK KINASES 有权
Title translation: 5,7-取代的咪唑并[1,2-C]嘧啶类AS JAK激酶的抑制剂公开(公告)号:EP2558468A1
公开(公告)日:2013-02-20
申请号:EP11715818.8
申请日:2011-04-11
Applicant: Array Biopharma, Inc.
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.-
8.5, 7-SUBSTITUTED-IMIDAZO [1,2-C] PYRIMIDINES AS INHIBITORS OF JAK KINASES 有权
Title translation: 5,7-取代的咪唑并[1,2-C]嘧啶类AS JAK激酶的抑制剂公开(公告)号:EP2558468B1
公开(公告)日:2015-04-01
申请号:EP11715818.8
申请日:2011-04-11
Applicant: Array Biopharma, Inc.
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
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9.SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS TRK KINASE INHIBITORS 有权
Title translation: 替米沙米汀 - [1,5-A] -PYRIMIDINVERBINDUNGEN ALS TRK-KINASEHEMMER公开(公告)号:EP2451812A1
公开(公告)日:2012-05-16
申请号:EP10732606.8
申请日:2010-07-09
Applicant: Array Biopharma, Inc.
Inventor: ALLEN, Shelley , ANDREWS, Steven S. , CONDROSKI, Kevin Ronald , HAAS, Julia , HUANG, Lily , JIANG, Yutong , KERCHER, Timothy , SEO, Jeongbeob
IPC: C07D487/04 , A61K31/519 , C07D519/00
CPC classification number: C07D487/04 , A61K31/519 , A61K31/5377 , C07D453/02 , C07D471/22 , C07D498/22 , C07D519/00
Abstract: Compounds of Formula II, III and IV, wherein R 3 , R 4 , Y and n are defined in the claims.
Abstract translation: 及其盐,其中R1,R2,R3,R4,X,Y和n具有本说明书中给出的含义,是Trk激酶的抑制剂,可用于治疗可用Trk激酶抑制剂如 疼痛,癌症,炎症,神经变性疾病和某些传染病。
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10.INTERMEDIATE COMPOUNDS FOR THE PREPARATION OFSUBSTITUTED PYRAZOLO[1,5-A]PYRIMIDINE COMPOUNDS AS TRK KINASE INHIBITORS 审中-公开
Title translation: 用于制备作为TRK激酶抑制剂的取代的吡唑并[1,5-A]嘧啶化合物的中间体化合物公开(公告)号:EP3299372A1
公开(公告)日:2018-03-28
申请号:EP17199899.0
申请日:2010-07-09
Applicant: Array Biopharma, Inc.
Inventor: ALLEN, Shelley , ANDREWS, Stephen, S. , CONDROSKI, Kevin Ronald , HAAS, Julia , HUANG, Lily , JIANG, Yutong , KERCHER, Timothy , SEO, Jeongbeob
IPC: C07D487/04 , A61K31/519 , C07D519/00 , C07D498/22 , C07D471/22 , C07D453/02 , A61K31/5377
Abstract: Compounds of Formula II, III and IV, wherein R 3 , R 4 , Y and n are defined in the claims.
Abstract translation: 式II,III和IV化合物,其中R3,R4,Y和n如权利要求中所定义。
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