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：WO2009111278A3

公开(公告)日：2009-09-11

申请号：PCT/US2009/035380

申请日：2009-02-27

Applicant: ARRAY BIOPHARMA INC. ,  GENENTECH, INC. ,  AHRENDT, Kateri A. ,  BUCKMELTER, Alexandre J. ,  GRINA, Jonas ,  HANSEN, Joshua D. ,  LAIRD, Ellen R. ,  MORENO, David ,  NEWHOUSE, Brad ,  REN, Li ,  WENGLOWSKY, Steven Mark ,  FENG, Bainian ,  GUNZNER, Janet ,  MALESKY, Kim ,  MATHIEU, Simon ,  RUDOLPH, Joachim ,  WEN, Zhaoyang ,  YOUNG, Wendy B.

Inventor： AHRENDT, Kateri A. ,  BUCKMELTER, Alexandre J. ,  GRINA, Jonas ,  HANSEN, Joshua D. ,  LAIRD, Ellen R. ,  MORENO, David ,  NEWHOUSE, Brad ,  REN, Li ,  WENGLOWSKY, Steven Mark ,  FENG, Bainian ,  GUNZNER, Janet ,  MALESKY, Kim ,  MATHIEU, Simon ,  RUDOLPH, Joachim ,  WEN, Zhaoyang ,  YOUNG, Wendy B.

IPC: C07D471/04 ,  C07C311/08 ,  A61P35/00 ,  A61K31/437

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.

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：WO2005058808A1

公开(公告)日：2005-06-30

申请号：PCT/US2004/041851

申请日：2004-12-14

Applicant: JAPAN TOBACCO INC. ,  FRYER, Andrew, M. ,  SHIOZAKI, Makoto ,  LITTMANN, Nicole, M. ,  INABA, Takashi ,  ANDREWS, Steven, W. ,  YASUE, Katsutaka ,  LAIRD, Ellen, R. ,  YOKOTA, Masahiro ,  HAAS, Julia ,  IMAI, Hiroto ,  MAEDA, Katsuya ,  SHINOZAKI, Yuichi ,  HORI, Yoshikazu

Inventor： FRYER, Andrew, M. ,  SHIOZAKI, Makoto ,  LITTMANN, Nicole, M. ,  INABA, Takashi ,  ANDREWS, Steven, W. ,  YASUE, Katsutaka ,  LAIRD, Ellen, R. ,  YOKOTA, Masahiro ,  HAAS, Julia ,  IMAI, Hiroto ,  MAEDA, Katsuya ,  SHINOZAKI, Yuichi ,  HORI, Yoshikazu

IPC: C07C311/20

CPC classification number: C07C311/20 ,  C07C311/51 ,  C07C381/06 ,  C07C381/08 ,  C07C2601/02 ,  C07C2601/14 ,  C07D207/34 ,  C07D209/52 ,  C07D211/46 ,  C07D211/60 ,  C07D213/42 ,  C07D213/65 ,  C07D213/74 ,  C07D213/79 ,  C07D213/80 ,  C07D231/14 ,  C07D231/20 ,  C07D233/90 ,  C07D235/14 ,  C07D249/10 ,  C07D257/04 ,  C07D257/06 ,  C07D261/18 ,  C07D271/07 ,  C07D277/56 ,  C07D285/06 ,  C07D285/08 ,  C07D295/088 ,  C07D295/13 ,  C07D295/15 ,  C07D295/185 ,  C07D307/68 ,  C07D333/18 ,  C07D333/34 ,  C07D409/12 ,  C07D413/04 ,  C07D413/12

Abstract: The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a N-substituted-N-sulfonylaminocyclopropane compound of formula (1) : wherein R 1 is -W-A 1 -W 1 -A 2 , W is (CH 2 ) m -X-(CH 2 )n-, wherein W 1 is -(CH 2 ) m1 -X 1 -(CH 2 ) n1 -, m, m1, n and n1 are the same or different and each is 0 to 6, X and X1 are the same or different and each is a single bond, etc., A1 is an optionally substituted C 3-14 hydrocarbon ring group, etc. and A 2 is a substituted C 3-14 hydrocarbon ring group etc.; R 2 is -(CH 2 ) r -CO-R 8 , etc., wherein r is 0 to 6 and R 8 is a C 1-6 alkoxy group, etc.; R 3 and R 4 are the same or different and each is a hydrogen atom, a C 1-6 alkyl group, etc.; and R 5 is -CO 2 R 21 , etc.; R 30 and R 31 are the same or different and each is a hydrogen atom, etc.; or a prodrug thereof or a pharmaceutically acceptable salt thereof.

Abstract translation: 本发明提供具有聚集蛋白聚糖蛋白聚糖酶抑制活性和MMP-13抑制活性的化合物，可用作骨关节炎，类风湿性关节炎等的治疗剂，更具体而言，可以使用式（1）所示的N-取代-N-磺酰氨基环丙烷化合物： 其中R 1是-WA 1 -W 1 -A 2，W是（CH 2）m X-（CH 2）n - ，其中W 1是 - （CH 2）m1-X 1 - （CH 2）n - ，m ，m1，n和n1相同或不同，分别为0〜6，X和X1相同或不同，均为单键等，A1为任选取代的C3-14烃环基等。 A 2是取代的C 3-14烃环基等。 R 2为 - （CH 2）r -CO-R 8等，其中r为0至6，R 8为C 1-6烷氧基等; R 3和R 4相同或不同，各自为氢原子，C 1-6烷基等; R 5为-CO 2 R 21等; R 30和R 31相同或不同，各自为氢原子等; 或其前药或其药学上可接受的盐。

公开(公告)号：WO2012118492A1

公开(公告)日：2012-09-07

申请号：PCT/US2011/026700

申请日：2011-03-01

Applicant: ARRAY BIOPHARMA INC. ,  GENENTECH, INC. ,  GRINA, Jonas ,  HANSEN, Joshua D. ,  LAIRD, Ellen ,  MATHIEU, Simon ,  MORENO, David ,  REN, Li ,  RUDOLPH, Joachim ,  WENGLOWSKY, Steven Mark

Inventor： GRINA, Jonas ,  HANSEN, Joshua D. ,  LAIRD, Ellen ,  MATHIEU, Simon ,  MORENO, David ,  REN, Li ,  RUDOLPH, Joachim ,  WENGLOWSKY, Steven Mark

IPC: C07D239/74 ,  C07D239/88 ,  C07D239/94 ,  C07D241/44 ,  C07D403/04 ,  C07D405/14 ,  A61K31/498 ,  A61K31/517 ,  A61P35/00

CPC classification number: C07D239/88 ,  C07D239/74 ,  C07D239/94 ,  C07D241/44 ,  C07D403/04 ,  C07D405/14

Abstract: Compounds of Formula (I) are useful for inhibition of Raf kinases. Methods of using compounds of Formula (I), stereoisomers, tautomers and pharmaceutically acceptable salts thereof, for i n 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。 公开了使用式（I）化合物，立体异构体，互变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。

公开(公告)号：WO2011025938A2

公开(公告)日：2011-03-03

申请号：PCT/US2010/046952

申请日：2010-08-27

Applicant: ARRAY BIOPHARMA INC. ,  GENENTECH, INC. ,  ALIAGAS, Ignacio ,  GRADL, Stefan ,  GUNZNER, Janet ,  LEE, Wendy ,  MATHIEU, Simon ,  RUDOLPH, Joachim ,  WEN, Zhaoyang ,  ZHAO, Guiling ,  BUCKMELTER, Alexandre J. ,  GRINA, Jonas ,  HANSEN, Joshua D. ,  LAIRD, Ellen ,  MORENO, David ,  REN, Li ,  WENGLOWSKY, Steven Mark

Inventor： ALIAGAS, Ignacio ,  GRADL, Stefan ,  GUNZNER, Janet ,  LEE, Wendy ,  MATHIEU, Simon ,  RUDOLPH, Joachim ,  WEN, Zhaoyang ,  ZHAO, Guiling ,  BUCKMELTER, Alexandre J. ,  GRINA, Jonas ,  HANSEN, Joshua D. ,  LAIRD, Ellen ,  MORENO, David ,  REN, Li ,  WENGLOWSKY, Steven Mark

IPC: A61K31/5377 ,  C07D487/02

CPC classification number: C07D239/94 ,  C07D403/12 ,  C07D405/12 ,  C07D471/04

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。 使用式I化合物及其立体异构体，互变异构体，前药和药学上可接受的盐用于体外，原位和体内诊断，预防或治疗的方法 披露了哺乳动物细胞中的病症或相关的病理学病症。

公开(公告)号：WO2009111277A1

公开(公告)日：2009-09-11

申请号：PCT/US2009035379

申请日：2009-02-27

Applicant: ARRAY BIOPHARMA INC ,  GENENTECH INC ,  AHRENDT KATERI A ,  BUCKMELTER ALEXANDRE J ,  GRINA JONAS ,  HANSEN JOSHUA D ,  LAIRD ELLEN R ,  NEWHOUSE BRAD ,  REN LI ,  WENGLOWSKY STEVEN M ,  FENG BAINIAN ,  MALESKY KIM ,  MATHIEU SIMON ,  RUDOLPH JOACHIM ,  WEN ZHAOYANG ,  YOUNG WENDY B ,  MORENO DAVID A

Inventor： AHRENDT KATERI A ,  BUCKMELTER ALEXANDRE J ,  GRINA JONAS ,  HANSEN JOSHUA D ,  LAIRD ELLEN R ,  NEWHOUSE BRAD ,  REN LI ,  WENGLOWSKY STEVEN M ,  FENG BAINIAN ,  MALESKY KIM ,  MATHIEU SIMON ,  RUDOLPH JOACHIM ,  WEN ZHAOYANG ,  YOUNG WENDY B ,  MORENO DAVID A

IPC: C07D471/04 ,  A61K31/437 ,  A61P13/12 ,  A61P35/00 ,  C07C311/08

CPC classification number: C07D471/04 ,  C07C311/48

Abstract: Compounds of Formula I are useful for inhibition of Raf 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.

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。

公开(公告)号：WO2006125101A3

公开(公告)日：2006-11-23

申请号：PCT/US2006/019280

申请日：2006-05-18

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

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

IPC: C07D487/04 ,  A61K31/4985 ,  A61P35/00

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, 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.

公开(公告)号：WO2006044825A3

公开(公告)日：2006-10-05

申请号：PCT/US2005037305

申请日：2005-10-18

Applicant: ARRAY BIOPHARMA INC ,  HANS JEREMY ,  WALLACE ELI M ,  ZHAO QIAN ,  LYSSIKATOS JOSEPH P ,  AICHER TOM ,  LAIRD ELLEN ,  ROBINSON JOHN ,  ALLEN SHELLEY

Inventor： HANS JEREMY ,  WALLACE ELI M ,  ZHAO QIAN ,  LYSSIKATOS JOSEPH P ,  AICHER TOM ,  LAIRD ELLEN ,  ROBINSON JOHN ,  ALLEN SHELLEY

IPC: A61K31/4245 ,  C07D413/00 ,  C07D417/00

CPC classification number: C07D285/12 ,  C07D271/107 ,  C07D401/12 ,  C07D413/04 ,  C07D413/06 ,  C07D413/12 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07F9/201 ,  C07F9/65392

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抑制剂，特别是KSP，以及制备这些抑制剂的方法。 本发明还提供包含本发明抑制剂的药物组合物和利用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：WO2006044825A2

公开(公告)日：2006-04-27

申请号：PCT/US2005/037305

申请日：2005-10-18

Applicant: ARRAY BIOPHARMA INC. ,  HANS, Jeremy ,  WALLACE, Eli, M. ,  WALLACE, Eli, M. ,  ZHAO, Qian ,  LYSSIKATOS, Joseph, P. ,  AICHER, Tom ,  LAIRD, Ellen ,  ROBINSON, John ,  ALLEN, Shelley

Inventor： HANS, Jeremy ,  WALLACE, Eli, M. ,  WALLACE, Eli, M. ,  ZHAO, Qian ,  LYSSIKATOS, Joseph, P. ,  AICHER, Tom ,  LAIRD, Ellen ,  ROBINSON, John ,  ALLEN, Shelley

IPC: A61K38/04 ,  A61K31/675 ,  A61K31/496 ,  A61K31/4439 ,  A61K31/433 ,  A61K31/4245 ,  C07D417/04 ,  C07D413/04

CPC classification number: C07D285/12 ,  C07D271/107 ,  C07D401/12 ,  C07D413/04 ,  C07D413/06 ,  C07D413/12 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07F9/201 ,  C07F9/65392

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.