公开(公告)号：EP3536692A1

公开(公告)日：2019-09-11

申请号：EP19170607.6

申请日：2013-02-14

申请人： Millennium Pharmaceuticals, Inc.

发明人： AFROZE, Roushan ,  BHARATHAN, Indu, T. ,  CIAVARRI, Jeffrey, P. ,  FLEMING, Paul, E. ,  GAULIN, Jeffrey, L. ,  GIRARD, Mario ,  LANGSTON, Steven, P. ,  SOUCY, Francois, R. ,  WONG, Tzu-Tshin ,  YE, Yingchun

IPC分类号： C07D487/04 ,  A61P35/00 ,  A61K31/519

摘要： Disclosed are chemical entities that inhibit ubiquitin-activating enzyme (UAE), each of which is a compound of Formula I :

or a pharmaceutically acceptable salt thereof, wherein Y is

and W, Z, X Y , R Y1 , R Y2 and R Y3 are defined herein; pharmaceutical compositions comprising the chemical entities; and methods of using the chemical entities. These chemical entities are useful for treating disorders, particularly cell proliferation disorders, including cancers.

公开(公告)号：EP3016934A2

公开(公告)日：2016-05-11

申请号：EP14819587.8

申请日：2014-07-01

申请人： Millennium Pharmaceuticals, Inc.

发明人： DUFFEY, Matthew, O. ,  ENGLAND, Dylan, B. ,  HU, Zhigen ,  ITO, Mitsuhiro ,  LANGSTON, Steven, P. ,  MCINTYRE, Charles ,  MIZUTANI, Hirotake ,  XU, He

IPC分类号： C07D239/48

CPC分类号： C07D403/06 ,  A61K31/505 ,  A61K31/506 ,  C07D239/28 ,  C07D401/06 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14

摘要： Disclosed are compounds of formula (I): or a pharmaceutically acceptable salt thereof; wherein Y, R
a , R
a' , R
c , R
f , X
2 , R
d , R
d' , R
e , R
e' , m, and G have the values described herein and stereochemical configurations depicted at asterisked positions indicate absolute stereochemistry, useful as inhibitors of Sumo Activating Enzyme (SAE). Further provided are pharmaceutical compositions comprising a compound of the disclosure and methods of using the compositions in the treatment of proliferative, inflammatory, cardiovascular and neurodegenerative diseases or disorders.

摘要翻译： 公开了式（I）的化合物; 或其药学上可接受的盐; 其中Y，Ra，Ra'，Rc，Rf，X2，Rd，Rd'，Re，Re'2，m和G具有本文所述的值，并且在星号位置处描绘的立体化学构型表示绝对立体化学，可用作Sumo的抑制剂 活化酶（SAE）。 还提供了包含本公开的化合物和使用该组合物治疗增殖性，炎性，心血管和神经变性疾病或病症的方法的药物组合物。

公开(公告)号：EP2814791A1

公开(公告)日：2014-12-24

申请号：EP13748707.0

申请日：2013-02-14

申请人： Millennium Pharmaceuticals, Inc.

发明人： AFROZE, Roushan ,  BHARATHAN, Indu, T. ,  CIAVARRI, Jeffrey, P. ,  FLEMING, Paul, E. ,  GAULIN, Jeffrey, L. ,  GIRARD, Mario ,  LANGSTON, Steven, P. ,  SOUCY, Francois, R. ,  WONG, Tzu-Tshin ,  YE, Yingchun

IPC分类号： C07B45/04

CPC分类号： C07D487/04

摘要： Disclosed are chemical entities that inhibit ubiquitin-activating enzyme (UAE), each of which is a compound of Formula I : or a pharmaceutically acceptable salt thereof, wherein Y is and W, Z, X Y , R Y1 , R Y2 and R Y3 are defined herein; pharmaceutical compositions comprising the chemical entities; and methods of using the chemical entities. These chemical entities are useful for treating disorders, particularly cell proliferation disorders, including cancers.

摘要翻译： 公开了抑制遍在蛋白活化酶（UAE）的化学实体，其各自为式（I）的化合物或其药学上可接受的盐，其中Y为式（II）且W，Z，XY，R Y1， 本文定义R Y2和R Y3; 包含化学实体的药物组合物; 和使用这些化学实体的方法。 这些化学实体可用于治疗疾病，特别是细胞增殖性疾病，包括癌症。

公开(公告)号：EP3173413B1

公开(公告)日：2019-05-01

申请号：EP16205139.5

申请日：2013-02-14

申请人： Millennium Pharmaceuticals, Inc.

发明人： AFROZE, Roushan ,  BHARATHAN, Indu, T. ,  CIAVARRI, Jeffrey, P. ,  FLEMING, Paul, E. ,  GAULIN, Jeffrey, L. ,  GIRARD, Mario ,  LANGSTON, Steven, P. ,  SOUCY, Francois, R. ,  WONG, Tzu-Tshin ,  YE, Yingchun

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P35/00

公开(公告)号：EP2049491A1

公开(公告)日：2009-04-22

申请号：EP07811106.9

申请日：2007-08-06

申请人： MILLENNIUM PHARMACEUTICALS, INC.

发明人： CLAIBORNE, Christopher, F. ,  CRITCHLEY, Stephen ,  LANGSTON, Steven, P. ,  OLHAVA, Edward, J. ,  PELUSO, Stephane ,  WEATHERHEAD, Gabriel, S. ,  VYSKOCIL, Stepan ,  VISIERS, Irache ,  MIZUTANI, Hirotake ,  CULLIS, Courtney

IPC分类号： C07D213/82 ,  C07D239/48 ,  C07D251/18 ,  C07D403/04 ,  C07D403/08 ,  C07D473/32 ,  C07D498/04 ,  A61K31/505 ,  A61P35/00

CPC分类号： C07D239/48 ,  C07D213/82 ,  C07D251/18 ,  C07D403/04 ,  C07D403/08 ,  C07D473/32 ,  C07D498/04

摘要： This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.

公开(公告)号：EP2391619A1

公开(公告)日：2011-12-07

申请号：EP10703376.3

申请日：2010-01-28

申请人： Millennium Pharmaceuticals, Inc.

发明人： BANNO, Hiroshi ,  HIROSE, Masaaki ,  KURASAWA, Osamu ,  LANGSTON, Steven, P. ,  MIZUTANI, Hirotake ,  SHI, Zhan ,  VISIERS, Irache ,  VOS, Tricia, J. ,  VYSKOCIL, Stepan

IPC分类号： C07D417/04 ,  C07D419/14 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04 ,  A61K31/404 ,  A61P29/00

CPC分类号： C07D487/04 ,  C07D417/04 ,  C07D419/14 ,  C07D471/04 ,  C07D513/04

摘要： This invention provides compounds of formula (IA) or (IB): wherein R
1 , R
2 , G
1 and HY are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.

公开(公告)号：EP2178880A1

公开(公告)日：2010-04-28

申请号：EP08832973.5

申请日：2008-08-01

申请人： Millennium Pharmaceuticals, Inc.

发明人： ARMITAGE, Ian ,  ELLIOT, Eric, L. ,  LANGSTON, Marianne ,  LANGSTON, Steven, P. ,  MCCUBBIN, Quentin, J. ,  MIZUTANI, Hirotake ,  STIRLING, Matthew ,  ZHU, Lei

IPC分类号： C07D487/04 ,  C07C215/44 ,  C07C217/52 ,  C07C219/24

CPC分类号： C07D487/04 ,  C07C215/44 ,  C07C217/52 ,  C07C219/24 ,  C07C315/04 ,  C07C317/50 ,  C07C2601/08 ,  C07D211/96 ,  C07D213/89 ,  C07D241/50 ,  C07D295/22 ,  C07D305/08 ,  C07D471/08 ,  Y02P20/55

摘要： The present invention provides processes and synthetic intermediates for the synthesis of 4-substituted ((1 S , 2 S , 4 R )-2-hydroxy-4-{7H-pyrrolo[2,3-d]pyrimidin-7-yl}cyclopentyl)methyl sulfamates, which are E1 activating enzyme inhibitors, and are useful for the treatment of disorders of cell proliferation, particularly cancer, and other disorders associated with E1 activity.

摘要翻译： 本发明提供了合成4-取代的（（1S，2S，4R）-2-羟基-4- {7H-吡咯并[2,3-d]嘧啶-7-基} 环戊基）甲基磺酸盐，其是E1活化酶抑制剂，并且可用于治疗细胞增殖，特别是癌症和与E1活性相关的其它病症的病症。

公开(公告)号：EP1848718A1

公开(公告)日：2007-10-31

申请号：EP06734691.6

申请日：2006-02-02

申请人： MILLENNIUM PHARMACEUTICALS, INC.

发明人： CRITCHLEY, Stephen ,  GANT, Thomas, G. ,  LANGSTON, Steven, P. ,  OLHAVA, Edward, J. ,  PELUSO, Stephane

IPC分类号： C07D473/34 ,  A61K31/52 ,  A61P35/00

CPC分类号： C07H19/16 ,  C07D405/04 ,  C07D471/04 ,  C07D473/00 ,  C07D473/34 ,  C07D487/04 ,  C07H19/048 ,  C07H19/14 ,  C07H19/23

摘要： This invention relates to compounds of formula (I-A) wherein Ring A and the variables X, Y, R3a, R3b, R3c, R3d, R4, R5, R5′, and m are defined herein. The compounds of formula (I-A) inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds of the invention are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.

公开(公告)号：EP2178880B1

公开(公告)日：2017-10-04

申请号：EP08832973.5

申请日：2008-08-01

申请人： Millennium Pharmaceuticals, Inc.

发明人： ARMITAGE, Ian ,  ELLIOT, Eric, L. ,  LANGSTON, Marianne ,  LANGSTON, Steven, P. ,  MCCUBBIN, Quentin, J. ,  MIZUTANI, Hirotake ,  STIRLING, Matthew ,  ZHU, Lei

IPC分类号： C07D487/04 ,  C07C215/44 ,  C07C217/52 ,  C07C219/24

CPC分类号： C07D487/04 ,  C07C215/44 ,  C07C217/52 ,  C07C219/24 ,  C07C315/04 ,  C07C317/50 ,  C07C2601/08 ,  C07D211/96 ,  C07D213/89 ,  C07D241/50 ,  C07D295/22 ,  C07D305/08 ,  C07D471/08 ,  Y02P20/55

摘要： The present invention provides processes and synthetic intermediates for the synthesis of 4-substituted ((1 S , 2 S , 4 R )-2-hydroxy-4-{7H-pyrrolo[2,3-d]pyrimidin-7-yl}cyclopentyl)methyl sulfamates, which are E1 activating enzyme inhibitors, and are useful for the treatment of disorders of cell proliferation, particularly cancer, and other disorders associated with E1 activity.

摘要翻译： 本发明提供了合成4-取代的（（1S，2S，4R）-2-羟基-4- {7H-吡咯并[2,3-d]嘧啶-7-基} 环戊基）甲基氨基磺酸酯，其为E1激活酶抑制剂，并且可用于治疗细胞增殖障碍，特别是癌症以及与E1活性相关的其他障碍。

公开(公告)号：EP3173413A1

公开(公告)日：2017-05-31

申请号：EP16205139.5

申请日：2013-02-14

申请人： Millennium Pharmaceuticals, Inc.

发明人： AFROZE, Roushan ,  BHARATHAN, Indu, T. ,  CIAVARRI, Jeffrey, P. ,  FLEMING, Paul, E. ,  GAULIN, Jeffrey, L. ,  GIRARD, Mario ,  LANGSTON, Steven, P. ,  SOUCY, Francois, R. ,  WONG, Tzu-Tshin ,  YE, Yingchun

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P35/00

CPC分类号： C07D487/04

摘要： Disclosed are chemical entities that inhibit ubiquitin-activating enzyme (UAE), each of which is a compound of Formula I :

or a pharmaceutically acceptable salt thereof, wherein Y is

and W, Z, X Y , R Y1 , R Y2 and R Y3 are defined herein; pharmaceutical compositions comprising the chemical entities; and methods of using the chemical entities. These chemical entities are useful for treating disorders, particularly cell proliferation disorders, including cancers.

摘要翻译： 公开了抑制泛素活化酶（UAE）的化学物质，其各自为式I化合物或其药学上可接受的盐，其中Y为和W，Z，XY，R Y1，R Y2和R Y3为 本文定义; 包含化学实体的药物组合物; 以及使用化学实体的方法。 这些化学实体可用于治疗疾病，特别是细胞增殖障碍，包括癌症。