公开(公告)号：EP4219465A3

公开(公告)日：2023-09-27

申请号：EP23156656.3

申请日：2013-12-20

申请人： Epizyme, Inc.

发明人： DUNCAN, Kenneth W. ,  CHESWORTH, Richard ,  BORIACK-SJODIN, Paula Ann ,  MUNCHHOF, Michael John ,  JIN, Lei

IPC分类号： C07D401/14 ,  C07D405/14 ,  C07D217/04 ,  C07D401/12 ,  C07D413/12 ,  C07D405/12 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/498 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538

摘要： Described herein are compounds of Formula (A), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.

公开(公告)号：EP2970266B1

公开(公告)日：2018-01-31

申请号：EP14717046.8

申请日：2014-03-14

申请人： Epizyme, Inc.

发明人： CHESWORTH, Richard ,  MORADEL, Oscar Miguel ,  SHAPIRO, Gideon ,  DUNCAN, Kenneth W. ,  MITCHELL, Lorna Helen ,  JIN, Lei ,  BABINE, Robert E.

IPC分类号： C07D471/04 ,  C07D487/04 ,  A61P35/00 ,  A61K31/519 ,  A61K31/437

CPC分类号： C07D471/04 ,  C07D487/04 ,  C07D498/08

摘要： Provided herein are compounds of Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein X, R1, R2a, R2b, R2c, R2d, are as defined herein, and Ring HET is an optionally substituted 6,5-bicyclic heteroaryl ring system comprising 2 to 5 nitrogen atoms, inclusive, wherein the point of attachment is provided on the 6-membered ring of the 6,5-bicyclic heteroaryl ring system, and wherein the 6-membered ring is further substituted with a group of formula -L1-R3, wherein L1 and R3 are as defined herein. Compounds of the present invention are useful for inhibiting CARM1 activity. Methods of using the compounds for treating CARM1-mediated disorders are also described.

公开(公告)号：EP3406607A1

公开(公告)日：2018-11-28

申请号：EP18161573.3

申请日：2013-12-20

申请人： Epizyme, Inc.

发明人： DUNCAN, Kenneth W. ,  CHESWORTH, Richard ,  BORIACK-SJODIN, Paula Ann ,  MUNCHHOF, Michael John ,  JIN, Lei

IPC分类号： C07D401/14 ,  C07D405/14 ,  C07D217/16 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  A61K31/502 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/497 ,  A61K31/498 ,  A61K31/472 ,  A61K31/4725 ,  A61P35/00 ,  A61P3/10 ,  A61P3/04 ,  A61P7/06

CPC分类号： C07D413/12 ,  A61K31/472 ,  A61K31/4725 ,  A61K31/497 ,  A61K31/498 ,  A61K31/502 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/538 ,  C07D217/04 ,  C07D217/08 ,  C07D217/16 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D417/12

摘要： Described herein are compounds of Formula ( A ), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.

公开(公告)号：EP4219465A2

公开(公告)日：2023-08-02

申请号：EP23156656.3

申请日：2013-12-20

申请人： Epizyme Inc

发明人： DUNCAN, Kenneth W. ,  CHESWORTH, Richard ,  BORIACK-SJODIN, Paula Ann ,  MUNCHHOF, Michael John ,  JIN, Lei

IPC分类号： C07D401/14 ,  C07D405/14 ,  C07D217/04 ,  C07D401/12 ,  C07D413/12 ,  C07D405/12 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/498 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538

摘要： Described herein are compounds of Formula (A), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.

公开(公告)号：EP2935242A2

公开(公告)日：2015-10-28

申请号：EP13824250.8

申请日：2013-12-20

申请人： Epizyme, Inc.

发明人： DUNCAN, Kenneth W. ,  CHESWORTH, Richard ,  BORIACK-SJODIN, Paula Ann ,  JIN, Lei

IPC分类号： C07D401/14 ,  C07D405/14 ,  C07D217/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D471/04 ,  C07D487/04 ,  A61K31/4725 ,  A61P35/00 ,  A61P3/04 ,  A61P3/08 ,  A61P7/06

CPC分类号： C07D401/12 ,  C07D217/04 ,  C07D401/06 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  G01N33/573 ,  G01N2333/91011 ,  G06F17/50 ,  G06F19/16

摘要： Described herein are compounds of Formula (I) useful for inhibiting PRMT5 activity. The planes of Ring AA and Ring BB are between 75° and 105°. Ring AA-M-Ring BB (I)

摘要翻译： 本文描述了可用于抑制PRMT5活性的式（I）化合物。 环AA和环BB的平面在75°和105°之间。 戒指AA-M型戒指BB（I）

公开(公告)号：EP3177288A1

公开(公告)日：2017-06-14

申请号：EP15830530.0

申请日：2015-08-04

申请人： Epizyme, Inc. ,  GlaxoSmithKline Intellectual Property Management Limited

发明人： DUNCAN, Kenneth W. ,  CHESWORTH, Richard ,  BORIACK-SJODIN, Paula Ann ,  MUNCHHOF, Michael John ,  JIN, Lei ,  PENEBRE, Elayne ,  BARBASH, Olena I.

IPC分类号： A61K31/44 ,  A61K31/535 ,  A61K31/00

CPC分类号： A61K31/506 ,  A61K31/4725 ,  A61K31/513 ,  A61K45/06 ,  A61P35/00 ,  A61K31/4545 ,  A61K2300/00

摘要： Described herein are methods of treating cancer using one or more PRMT5 inhibitors, for example using one or more compounds of Formulae (1-5) or (A-F), pharmaceutically acceptable salts thereof, and/or pharmaceutical compositions thereof. Described herein are methods of treating cancer using one or more PRMT5 inhibitors, for example using one or more compounds of Formulae (1-5) or (A-F), pharmaceutically acceptable salts thereof, and/or pharmaceutical compositions thereof.

摘要翻译： 本文描述了使用一种或多种PRMT5抑制剂，例如使用一种或多种式（1-5）或（A-F）的化合物，其药学上可接受的盐和/或其药物组合物治疗癌症的方法。 本文描述了使用一种或多种PRMT5抑制剂，例如使用一种或多种式（1-5）或（A-F）的化合物，其药学上可接受的盐和/或其药物组合物治疗癌症的方法。

公开(公告)号：EP2970266A1

公开(公告)日：2016-01-20

申请号：EP14717046.8

申请日：2014-03-14

申请人： Epizyme, Inc.

发明人： CHESWORTH, Richard ,  MORADEL, Oscar Miguel ,  SHAPIRO, Gideon ,  DUNCAN, Kenneth W. ,  MITCHELL, Lorna Helen ,  JIN, Lei ,  BABINE, Robert E.

IPC分类号： C07D471/04 ,  C07D487/04 ,  A61P35/00 ,  A61K31/519 ,  A61K31/437

CPC分类号： C07D471/04 ,  C07D487/04 ,  C07D498/08

摘要： Provided herein are compounds of Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein X, R1, R2a, R2b, R2c, R2d, are as defined herein, and Ring HET is an optionally substituted 6,5-bicyclic heteroaryl ring system comprising 2 to 5 nitrogen atoms, inclusive, wherein the point of attachment is provided on the 6-membered ring of the 6,5-bicyclic heteroaryl ring system, and wherein the 6-membered ring is further substituted with a group of formula -L1-R3, wherein L1 and R3 are as defined herein. Compounds of the present invention are useful for inhibiting CARM1 activity. Methods of using the compounds for treating CARM1-mediated disorders are also described.

摘要翻译： 本文提供式（I）的化合物及其药学上可接受的盐，及其药物组合物; 其中X，R1，R2a，R2b，R2c，R2d如本文所定义，环HET是任选取代的含5至5个氮原子的6,5-双环杂芳基环系统，其中附着点设置在 6,5-双环杂芳基环系的6元环，并且其中所述6元环进一步被式-L 1 -R 3基团取代，其中L 1和R 3如本文所定义。 本发明的化合物可用于抑制CARM1活性。 还描述了使用该化合物治疗CARM1介导的病症的方法。