公开(公告)号：EP2646454B1

公开(公告)日：2015-07-08

申请号：EP11844610.3

申请日：2011-12-05

申请人： Epizyme, Inc.

发明人： CHESWORTH, Richard ,  KUNTZ, Kevin, Wayne ,  OLHAVA, Edward, James ,  PATANE, Michael, A.

IPC分类号： C07H19/14 ,  C07D487/04 ,  C07D405/14 ,  A61K31/7052 ,  A61K31/519 ,  A61P35/00 ,  A61P25/28

CPC分类号： C07H19/14 ,  C07D487/04

公开(公告)号：EP2646454A2

公开(公告)日：2013-10-09

申请号：EP11844610.3

申请日：2011-12-05

申请人： Epizyme, Inc.

发明人： CHESWORTH, Richard ,  KUNTZ, Kevin, Wayne ,  OLHAVA, Edward, James ,  PATANE, Michael, A.

IPC分类号： C07H19/14 ,  C07D487/04 ,  C07D405/14 ,  A61K31/7052 ,  A61K31/519 ,  A61P35/00 ,  A61P25/28

CPC分类号： C07H19/14 ,  C07D487/04

摘要： Disclosed are compounds, pharmaceutical compositions containing the compounds, uses of the compounds and compositions as modulators of histone methyltransferases, and methods for treating diseases influenced by modulation of histone methyltransferase activity.

公开(公告)号：EP2646444A1

公开(公告)日：2013-10-09

申请号：EP11804836.2

申请日：2011-12-02

申请人： Epizyme, Inc.

发明人： OLHAVA, Edward, James ,  CHESWORTH, Richard ,  KUNTZ, Kevin, Wayne ,  RICHON, Victoria, Marie ,  POLLOCK, Roy, Macfarlane ,  DAIGLE, Scott, Richard

IPC分类号： C07D487/04 ,  A61K31/52 ,  A61K31/519 ,  A61P3/00 ,  A61P9/00 ,  A61P25/28 ,  A61P29/00 ,  A61P35/00 ,  A61P35/02

CPC分类号： A61K31/7076 ,  A61K31/519 ,  A61K31/52 ,  A61K31/7064 ,  C07D473/34 ,  C07D487/04 ,  C07H19/14 ,  C07H19/16

摘要： The present invention relates to substituted purine and 7-deazapurine compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating disorders in which DOTl -mediated protein methylation plays a part, such as cancer and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

公开(公告)号：EP4360712A3

公开(公告)日：2024-07-31

申请号：EP23217912.7

申请日：2012-04-13

申请人： Epizyme, Inc.

发明人： CHESWORTH, Richard ,  DUNCAN, Kenneth William ,  KEILHACK, Heike ,  WARHOLIC, Natalie ,  KLAUS, Christine ,  SEKI, Masashi ,  SHIROTORI, Syuji ,  KAWANO, Satoshi ,  WIGLE, Timothy James Nelson ,  KNUTSON, Sarah Kathleen ,  KUNTZ, Kevin Wayne

IPC分类号： A61K31/4412 ,  A61K31/444 ,  A61P35/00 ,  A61P35/02

CPC分类号： A61K31/4412 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/506 ,  A61K31/551 ,  A61K31/553 ,  A61K31/5377 ,  A61P35/00 ,  A61P35/02 ,  A61P43/00

摘要： The present invention relates to aryl- or heteroaryl-substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.

公开(公告)号：EP2970133B1

公开(公告)日：2018-10-24

申请号：EP14718873.4

申请日：2014-03-14

申请人： Epizyme, Inc.

发明人： MITCHELL, Lorna, Helen ,  SHAPIRO, Gideon ,  CHESWORTH, Richard ,  BORIACK-SJODIN, Paula, Ann ,  MORADEI, Oscar, Miguel ,  KUNTZ, Kevin, Wayne

IPC分类号： C07D231/12 ,  A61K31/415 ,  A61P35/00 ,  A61P3/00 ,  A61P9/00 ,  A61P21/00 ,  A61P25/00 ,  A61P37/00

CPC分类号： A61K31/4155 ,  A61K31/415 ,  A61K31/455 ,  C07D231/12 ,  C07D401/12 ,  C07D405/12

摘要： Described herein are compounds of Formula (I-a) and (I-b), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT1 activity. Methods of using the compounds for treating PRMT1-mediated disorders are also described.

公开(公告)号：EP3150580B1

公开(公告)日：2018-10-17

申请号：EP16172386.1

申请日：2012-04-13

申请人： Epizyme, Inc.

发明人： KUNTZ, Kevin Wayne ,  CHESWORTH, Richard ,  DUNCAN, Kenneth William ,  KEILHACK, Heike ,  WARHOLIC, Natalie ,  KLAUS, Christine ,  SEKI, Masashi ,  SHIROTORI, Syuji ,  KAWANO, Satoshi ,  WIGLE, Timothy James Nelson ,  KNUTSON, Sarah Kathleen

IPC分类号： C07D213/64 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D491/08 ,  C07D491/107 ,  A61K31/4412 ,  A61K31/444 ,  A61P35/00

CPC分类号： A61K31/5377 ,  A61K31/4412 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/506 ,  A61K31/551 ,  A61K31/553 ,  C07D213/64 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D491/08 ,  C07D491/107 ,  C07D498/08

摘要： The present invention relates to aryl- or heteroaryl-substituted benzene compounds (I). The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.

公开(公告)号：EP2935222B1

公开(公告)日：2018-09-05

申请号：EP13821599.1

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： C07D217/12 ,  A61K31/472 ,  A61K31/4725 ,  C07D401/12 ,  C07D405/12 ,  A61P35/00 ,  A61P3/04 ,  A61P3/10 ,  A61P7/06

CPC分类号： A61K31/4725 ,  A61K31/496 ,  A61K31/498 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  A61P3/04 ,  A61P3/10 ,  A61P7/06 ,  A61P35/00 ,  C07D217/04 ,  C07D217/12 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C12N9/1007 ,  Y02A50/414

摘要： Described herein are compounds of Formula (I), 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：EP2970134B1

公开(公告)日：2018-02-28

申请号：EP14719993.9

申请日：2014-03-14

申请人： Epizyme, Inc.

发明人： MITCHELL, Lorna, Helen ,  SHAPIRO, Gideon ,  CHESWORTH, Richard ,  BORIACK-SJODIN, Paula, Ann ,  MORADEI, Oscar, Miguel

IPC分类号： C07D231/12 ,  C07D401/12 ,  A61K31/415 ,  A61K31/506 ,  A61P35/00 ,  A61P37/00 ,  A61K31/4439

CPC分类号： C07D231/12 ,  C07D401/12

摘要： Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting PRMT1 activity. Methods of using the compounds for treating PRMT1-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：EP3193606A1

公开(公告)日：2017-07-26

申请号：EP15840663.7

申请日：2015-09-09

申请人： Epizyme, Inc.

发明人： CHESWORTH, Richard ,  FOLEY, Megan Alene Cloonan ,  KUNTZ, Kevin Wayne ,  MITCHELL, Lorna Helen ,  PETTER, Russell C. ,  SCHWARTZ, Carl Eric

IPC分类号： A01N43/80

摘要： The present disclosure provides provides substituted isoxazole carboxamides having Formula (I), and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2a, R2b, R3a, R3b, X, n, and m are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of SMYD proteins such as SMYD3 or SMYD2. Compounds of the present disclosure are especially useful for treating cancer.

摘要翻译： 本公开内容提供了提供具有式（I）的取代的异恶唑甲酰胺及其药学上可接受的盐和溶剂合物，其中R 1，R 2a，R 2b，R 3a，R 3b，X，n和m如说明书中所定义。 本公开还涉及式I化合物用于治疗响应于SMYD蛋白质例如SMYD3或SMYD2的阻断的病症的用途。 本公开的化合物对于治疗癌症尤其有用。