公开(公告)号：WO2011025968A1

公开(公告)日：2011-03-03

申请号：PCT/US2010/047013

申请日：2010-08-27

Applicant: ARRAY BIOPHARMA INC. ,  GENENTECH, INC. ,  GRADL, Stefan ,  LAIRD, Ellen ,  MORENO, David ,  REN, Li ,  WENGLOWSKY, Steven Mark

Inventor： GRADL, Stefan ,  LAIRD, Ellen ,  MORENO, David ,  REN, Li ,  WENGLOWSKY, Steven Mark

IPC: C07D471/04 ,  A61K31/437 ,  A61P13/12 ,  A61P35/00

CPC classification number: C07D471/04

Abstract: Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers 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Raf激酶。 公开了使用式I化合物和其立体异构体，互变异构体和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。 [公式I]

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：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。

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。

公开(公告)号：WO2011025940A1

公开(公告)日：2011-03-03

申请号：PCT/US2010/046955

申请日：2010-08-27

Applicant: ARRAY BIOPHARMA INC. ,  GENENTECH, INC. ,  ALIAGAS, Ignacio ,  GRADL, Stefan ,  GUNZNER, Janet ,  MATHIEU, Simon ,  PULK, Rebecca ,  RUDOLPH, Joachim ,  WEN, Zhaoyang ,  GRINA, Jonas ,  HANSEN, Joshua D. ,  LAIRD, Ellen ,  MORENO, David ,  REN, Li ,  WENGLOWSKY, Steven Mark

Inventor： ALIAGAS, Ignacio ,  GRADL, Stefan ,  GUNZNER, Janet ,  MATHIEU, Simon ,  PULK, Rebecca ,  RUDOLPH, Joachim ,  WEN, Zhaoyang ,  GRINA, Jonas ,  HANSEN, Joshua D. ,  LAIRD, Ellen ,  MORENO, David ,  REN, Li ,  WENGLOWSKY, Steven Mark

IPC: C07D487/04 ,  C07D495/04 ,  C07D513/04 ,  A61K31/38 ,  A61P35/00

CPC classification number: C07D487/04 ,  C07D495/04 ,  C07D513/04

Abstract: Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers, prodrugs 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.

Abstract translation: 式I化合物可用于抑制Raf激酶。 公开了使用式I化合物和立体异构体，互变异构体，前药和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。

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.

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。

公开(公告)号：WO2007089646A1

公开(公告)日：2007-08-09

申请号：PCT/US2007/002272

申请日：2007-01-26

Applicant: ARRAY BIOPHARMA INC. ,  GRONEBERG, Robert ,  BURGESS, Laurence, E. ,  HARVEY, Darren ,  LAIRD, Ellen ,  MUNSON, Mark ,  RIZZI, James ,  RODRIGUEZ, Martha ,  EARY, Charles, Todd ,  WATSON, Daniel

Inventor： GRONEBERG, Robert ,  BURGESS, Laurence, E. ,  HARVEY, Darren ,  LAIRD, Ellen ,  MUNSON, Mark ,  RIZZI, James ,  RODRIGUEZ, Martha ,  EARY, Charles, Todd ,  WATSON, Daniel

IPC: C07D231/40 ,  C07D231/56 ,  A61K31/416 ,  A61P29/00

CPC classification number: C07D231/40 ,  C07D231/56

Abstract: The compound of Formula (I) and pharmaceutically acceptable salts and prodrugs thereof are useful in the treatment and prevention of various disorders mediated by kinases.

Abstract translation: 式（I）化合物及其药学上可接受的盐和前药可用于治疗和预防由激酶介导的各种疾病。

公开(公告)号：WO2007027855A2

公开(公告)日：2007-03-08

申请号：PCT/US2006/033976

申请日：2006-08-31

Applicant: ARRAY BIOPHARMA INC. ,  MIKNIS, Greg ,  LYSSIKATOS, Joseph P. ,  LAIRD, Ellen ,  TARLTON, Eugene ,  BUCKMELTER, Alexandre J. ,  REN, Li ,  RAST, Bryson ,  SCHLACTER, Stephen T. ,  WENGLOWSKY, Steven Mark

Inventor： MIKNIS, Greg ,  LYSSIKATOS, Joseph P. ,  LAIRD, Ellen ,  TARLTON, Eugene ,  BUCKMELTER, Alexandre J. ,  REN, Li ,  RAST, Bryson ,  SCHLACTER, Stephen T. ,  WENGLOWSKY, Steven Mark

CPC classification number: C07D491/04 ,  C07D495/04

Abstract: Compounds of Formula I are useful for inhibiting Raf kinase and for treating disorders mediated thereby. Methods of using compounds of Formula I, and stereoisomers, geometric isomers, tautomers, solvates 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.

Abstract translation: 式I的化合物可用于抑制Raf激酶和用于治疗由此介导的病症。 使用式I化合物及其立体异构体，几何异构体，互变异构体，溶剂合物及其药学上可接受的盐的方法用于在哺乳动物细胞或相关病理状况下的体外，原位和体内诊断，预防或治疗这些疾病。 披露。

公开(公告)号：WO2006084015A3

公开(公告)日：2006-08-10

申请号：PCT/US2006/003654

申请日：2006-02-02

Applicant: GENENTECH, INC. ,  ARRAY BIOPHARMA, INC. ,  LAIRD, Ellen ,  LYSSIKATOS, Joseph, P. ,  WELCH, Mike ,  GRINA, Jonas ,  HANSEN, Josh ,  NEWHOUSE, Brad ,  OLIVERO, Alan ,  TOPOLAV, George

Inventor： LAIRD, Ellen ,  LYSSIKATOS, Joseph, P. ,  WELCH, Mike ,  GRINA, Jonas ,  HANSEN, Josh ,  NEWHOUSE, Brad ,  OLIVERO, Alan ,  TOPOLAV, George

IPC: C07D401/04 ,  C07D401/14 ,  C07D471/04 ,  A61K31/415 ,  A61P35/00 ,  A61P3/10 ,  A61P9/00 ,  A61P17/06 ,  A61P37/00 ,  A61P25/00

Abstract: Pyrazolyl compounds of Formulas Ia and Ib are useful for inhibiting Raf kinase and for treating disorders mediated thereby. Methods of using pyrazolyl compounds for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.