公开(公告)号：EP3901159A1

公开(公告)日：2021-10-27

申请号：EP21165701.0

申请日：2015-06-30

申请人： Millennium Pharmaceuticals, Inc.

发明人： DUFFEY, Matthew ,  ENGLAND, Dylan ,  FREEZE, Scott ,  HU, Zhigen ,  LANGSTON, Steven ,  MCINTYRE, Charles ,  MIZUTANI, Hirotake ,  ONO, Koji ,  XU, He

IPC分类号： C07F9/54 ,  C07D409/06 ,  C07D409/14 ,  C07D491/052 ,  A61K31/34 ,  A61K31/505 ,  A61P43/00 ,  C07D405/06 ,  C07D471/04 ,  C07D493/04 ,  C07D495/04 ,  C07D498/04 ,  C07F9/535 ,  A61K31/506 ,  A61P35/00 ,  C07D487/04 ,  C07D513/04 ,  C07F9/6558

摘要： Disclosed are chemical entities which are compounds of formula ( I ):

or pharmaceutically acceptable salts thereof; wherein Y, R a , R a ', R b , R c , X 1 , X 2 , X 3 , R d , Z 1 , and Z 2 have the values described herein and stereochemical configurations depicted at asterisked positions indicate absolute stereochemistry. Chemical entities according to the disclosure can be 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.

公开(公告)号：EP3164130B1

公开(公告)日：2019-08-07

申请号：EP15815330.4

申请日：2015-06-30

申请人： Millennium Pharmaceuticals, Inc.

发明人： DUFFEY, Matthew O. ,  ENGLAND, Dylan ,  FREEZE, Scott ,  HU, Zhigen ,  LANGSTON, Steven P. ,  MCINTYRE, Charles ,  MIZUTANI, Hirotake ,  ONO, Koji ,  XU, He

IPC分类号： A61K31/44 ,  A61K31/506 ,  C07D239/24 ,  C07F9/535 ,  A61K31/34 ,  A61K31/505 ,  C07F9/54 ,  C07F9/655 ,  C07F9/6558 ,  C07D405/06 ,  C07D409/06 ,  C07D409/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/052 ,  C07D493/04 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04

公开(公告)号：EP3517112A1

公开(公告)日：2019-07-31

申请号：EP19153547.5

申请日：2015-06-30

申请人： Millennium Pharmaceuticals, Inc.

发明人： DUFFEY, Matthew ,  ENGLAND, Dylan ,  FREEZE, Scott ,  HU, Zhigen ,  LANGSTON, Steven ,  MCINTYRE, Charles ,  MIZUTANI, Hirotake ,  ONO, Koji ,  XU, He

IPC分类号： A61K31/44 ,  A61K31/506 ,  C07D239/24 ,  C07F9/535 ,  A61K31/34 ,  A61K31/505 ,  C07F9/54 ,  C07F9/655 ,  C07F9/6558 ,  C07D405/06 ,  C07D409/06 ,  C07D409/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/052 ,  C07D493/04 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04

摘要： Disclosed are chemical entities which are compounds of formula ( I ):

or pharmaceutically acceptable salts thereof; wherein Y, R a , R a' , R b , R c , X 1 , X 2 , X 3 , R d , Z 1 , and Z 2 have the values described herein and stereochemical configurations depicted at asterisked positions indicate absolute stereochemistry. Chemical entities according to the disclosure can be 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.

公开(公告)号：EP3164130A1

公开(公告)日：2017-05-10

申请号：EP15815330.4

申请日：2015-06-30

申请人： Millennium Pharmaceuticals, Inc.

发明人： DUFFEY, Matthew O. ,  ENGLAND, Dylan ,  FREEZE, Scott ,  HU, Zhigen ,  LANGSTON, Steven P. ,  MCINTYRE, Charles ,  MIZUTANI, Hirotake ,  ONO, Koji ,  XU, He

IPC分类号： A61K31/44 ,  A61K31/506 ,  C07D239/24

CPC分类号： A61K31/506 ,  A61K31/34 ,  A61K31/505 ,  C07D405/06 ,  C07D409/06 ,  C07D409/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/052 ,  C07D493/04 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04 ,  C07F9/5352 ,  C07F9/5442 ,  C07F9/65522 ,  C07F9/65586

摘要： Disclosed are chemical entities which are compounds of formula (I): or pharmaceutically acceptable salts thereof; wherein Y, Ra, Ra′, Rb, Rc, X1, X2, X3, Rd, Z1, and Z2 have the values described herein and stereochemical configurations depicted at asterisked positions indicate absolute stereochemistry. Chemical entities according to the disclosure can be 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： 公开了作为式（I）化合物的化学实体：或其药学上可接受的盐; 其中Y，Ra，Ra'，Rb，Rc，X 1，X 2，X 3，R d，Z 1和Z 2具有本文所述的值，并且星号位置描绘的立体化学构型表示绝对立体化学。 根据本公开的化学实体可以用作Sumo活化酶（SAE）的抑制剂。 进一步提供了包含本公开化合物的药物组合物和使用所述组合物治疗增殖性，炎症性，心血管和神经退行性疾病或病症的方法。