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：US20200247790A1

公开(公告)日：2020-08-06

申请号：US16756565

申请日：2018-10-18

申请人： Epizyme, Inc.

发明人： John Emmerson CAMPBELL ,  Kenneth William DUNCAN ,  James Edward John MILLS ,  Michael John MUNCHHOF

IPC分类号： C07D405/14 ,  C07D401/14 ,  C07D403/12

摘要： The present disclosure relates to amine-substituted heterocyclic compounds. The present disclosure also relates to pharmaceutical compositions containing these compounds and methods of treating a disorder (e.g., cancer) by administering an amine-substituted heterocyclic compound disclosed herein or a pharmaceutical composition thereof to subjects in need thereof. The present disclosure also relates to the use of such compounds for research or other non-therapeutic purposes.

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：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：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：US20220324851A1

公开(公告)日：2022-10-13

申请号：US17703155

申请日：2022-03-24

申请人： Epizyme, Inc.

发明人： John Emmerson CAMPBELL ,  Kenneth William DUNCAN ,  James Edward John MILLS ,  Michael John MUNCHHOF

IPC分类号： C07D405/14 ,  C07D401/14 ,  C07D403/12

摘要： The present disclosure relates to amine-substituted heterocyclic compounds. The present disclosure also relates to pharmaceutical compositions containing these compounds and methods of treating a disorder (e.g., cancer) by administering an amine-substituted heterocyclic heterocyclic compound disclosed herein or a pharmaceutical composition thereof to subjects in need thereof. The present disclosure also relates to the use of such compounds for research or other non-therapeutic purposes.

公开(公告)号：US20200317642A1

公开(公告)日：2020-10-08

申请号：US16756292

申请日：2018-10-17

申请人： Epizyme, Inc.

发明人： John Emmerson CAMPBELL ,  Kenneth William DUNCAN ,  James Edward John MILLS ,  Michael John MUNCHHOF

IPC分类号： C07D401/12 ,  C07D403/14 ,  C07D471/04 ,  C07D403/04 ,  C07D403/12 ,  C07D413/12 ,  C07D487/04 ,  A61P7/06

摘要： The present disclosure relates to amine-substituted heterocyclic compounds and derivatives thereof. The present disclosure also relates to pharmaceutical compositions containing these compounds and methods of treating a disorder (e.g., cancer) by administering an amine-substituted heterocyclic compound disclosed herein or a pharmaceutical composition thereof to subjects in need thereof. The present disclosure also relates to the use of such compounds for research or other non-therapeutic purposes.

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.