公开(公告)号：US20170362217A1

公开(公告)日：2017-12-21

申请号：US15510588

申请日：2015-09-09

申请人： EPIZYME, INC.

发明人： Lorna Helen MITCHELL ,  Andrew Simon BELL ,  Richard CHESWORTH ,  Megan Alene Cloonan FOLEY ,  Kevin Wayne KUNTZ ,  James Edward John MILLS ,  Michael John MUNCHHOF

IPC分类号： C07D451/04 ,  C07D487/08 ,  C07D413/14 ,  C07D519/00 ,  C07D413/12

CPC分类号： C07D451/04 ,  A61P35/00 ,  C07D413/12 ,  C07D413/14 ,  C07D487/08 ,  C07D519/00

摘要： The present disclosure provides substituted piperidine compounds having Formula (I), and the pharmaceutically acceptable salts and solvates thereof, wherein R1, B, X, and Z 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.

公开(公告)号：US20200048195A1

公开(公告)日：2020-02-13

申请号：US16423618

申请日：2019-05-28

申请人： EPIZYME, INC.

发明人： Megan Alene Cloonan Foley ,  Kevin Wayne KUNTZ ,  Lorna Helen MITCHELL ,  Michael John MUNCHHOF ,  Darren Martin HARVEY

IPC分类号： C07D207/14 ,  C07D403/12 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  A61P35/00

摘要： The present disclosure provides pyrrolidine carboxamide compounds having Formula I and the pharmaceutically acceptable salts and solvates thereof, wherein A, B, X, Y, and Z 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.

公开(公告)号：US20170253601A1

公开(公告)日：2017-09-07

申请号：US15510602

申请日：2015-09-09

申请人： EPIZYME, INC.

发明人： Megan Alene Cloonan FOLEY ,  Kevin Wayne KUNTZ ,  Lorna Helen MITCHELL ,  Michael John MUNCHHOF ,  Darren Martin HARVEY

IPC分类号： C07D487/04 ,  C07D413/14 ,  C07D413/12

CPC分类号： C07D487/04 ,  A61P35/00 ,  C07D413/12 ,  C07D413/14

摘要： The present disclosure provides substituted pyrrolidine compounds having Formula (I): and the pharmaceutically acceptable salts and solvates thereof, wherein R1, B, X, and Z 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.

公开(公告)号：US20230101819A1

公开(公告)日：2023-03-30

申请号：US17532422

申请日：2021-11-22

申请人： EPIZYME, INC.

发明人： Megan Alene Cloonan FOLEY ,  Kevin Wayne KUNTZ ,  James Edward John MILLS ,  Lorna Helen MITCHELL ,  Michael John MUNCHHOF ,  Darren Martin HARVEY

IPC分类号： C07D451/04 ,  C07D213/81 ,  C07D213/82 ,  C07D231/14 ,  C07D233/90 ,  C07D401/12 ,  C07D241/26 ,  C07D249/04 ,  C07D261/10 ,  C07D263/34 ,  C07D275/03 ,  C07D209/08 ,  C07D277/56 ,  C07C271/18 ,  C07D205/04 ,  C07D211/34 ,  C07D237/24 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D413/12 ,  C07D417/14

摘要： The present disclosure provides carboxamides and sulfonamides having Formula (I); and the pharmaceutically acceptable salts and solvates thereof, wherein A, Y, B, X, and Z 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.

公开(公告)号：US20180230110A1

公开(公告)日：2018-08-16

申请号：US15510589

申请日：2015-09-09

申请人： EPIZYME, INC.

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

IPC分类号： C07D261/18 ,  A61P35/00 ,  A61P35/02 ,  A61P35/04 ,  C07D413/12

CPC分类号： C07D261/18 ,  A61P35/00 ,  A61P35/02 ,  A61P35/04 ,  C07D413/12

摘要： The present disclosure 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.

公开(公告)号：US20170362191A1

公开(公告)日：2017-12-21

申请号：US15510605

申请日：2015-09-09

申请人： EPIZYME, INC.

发明人： Megan Alene Cloonan FOLEY ,  Kevin Wayne KUNTZ ,  Lorna Helen MITCHELL ,  Michael John MUNCHHOF

IPC分类号： C07D261/08

CPC分类号： C07D261/08 ,  C07D261/18

摘要： The present disclosure provides substituted cyclohexylamine compounds having Formula (I): and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2a, R2b, R3a, R3b, R4, R5, and R7 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.

公开(公告)号：US20200148650A1

公开(公告)日：2020-05-14

申请号：US16588209

申请日：2019-09-30

申请人： EPIZYME, INC.

发明人： Megan Alene Cloonan Foley ,  Kevin Wayne KUNTZ ,  James Edward John MILLS ,  Lorna Helen MITCHELL ,  Michael John MUNCHHOF ,  Darren Martin HARVEY

IPC分类号： C07D261/18 ,  C07D413/14 ,  C07D413/12

摘要： The present disclosure provides substituted isoxazole carboxamide compounds having Formula (1) and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, A, X, and Z 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.

公开(公告)号：US20170280720A1

公开(公告)日：2017-10-05

申请号：US15511514

申请日：2015-09-17

申请人： EPIZYME, INC.

发明人： Richard CHESWORTH ,  Lorna Helen MITCHELL ,  Gideon SHAPIRO ,  Oscar Miguel MORADEI ,  Kevin Wayne KUNTZ ,  Kenneth W. DUNCAN ,  Lei JIN

IPC分类号： A01N47/10 ,  C07D277/20 ,  C07D233/54 ,  C07D209/10 ,  C07D241/02

CPC分类号： A01N47/10 ,  A61K38/45 ,  C07D209/10 ,  C07D233/54 ,  C07D241/02 ,  C07D277/20 ,  C07D471/04 ,  C07D487/04

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

公开(公告)号：US20170190676A1

公开(公告)日：2017-07-06

申请号：US15510593

申请日：2015-09-09

申请人： EPIZYME, INC.

发明人： Megan Alene Cloonan FOLEY ,  Kevin Wayne KUNTZ ,  James Edward John MILLS ,  Lorna Helen MITCHELL ,  Michael John MUNCHHOF ,  Darren Martin HARVEY

IPC分类号： C07D261/18 ,  C07D413/14 ,  C07D413/12

CPC分类号： C07D261/18 ,  C07D413/12 ,  C07D413/14

摘要： The present disclosure provides substituted isoxazole carboxamide compounds having Formula (I) and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, A, X, and Z 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.

公开(公告)号：US20210198252A1

公开(公告)日：2021-07-01

申请号：US16864891

申请日：2020-05-01

申请人： EPIZYME, INC.

发明人： Megan Alene Cloonan Foley ,  Kevin Wayne KUNTZ ,  James Edward John MILLS ,  Lorna Helen MITCHELL ,  Michael John MUNCHHOF ,  Darren Martin HARVEY

IPC分类号： C07D451/04 ,  C07D213/81 ,  C07D213/82 ,  C07D231/14 ,  C07D233/90 ,  C07D401/12 ,  C07D241/26 ,  C07D249/04 ,  C07D261/10 ,  C07D263/34 ,  C07D275/03 ,  C07D209/08 ,  C07D277/56 ,  C07C271/18 ,  C07D205/04 ,  C07D211/34 ,  C07D237/24 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D413/12 ,  C07D417/14

摘要： The present disclosure provides carboxamides and sulfonamides having Formula (I): and the pharmaceutically acceptable salts and solvates thereof, wherein A, Y, B, X, and Z 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 a SMYD3 or SMYD2. Compounds of the present disclosure are especially useful for treating cancer.