公开(公告)号：US10428029B2

公开(公告)日：2019-10-01

申请号：US15510593

申请日：2015-09-09

Applicant: EPIZYME, INC.

Inventor： Megan Alene Cloonan Foley ,  Kevin Wayne Kuntz ,  James Edward John Mills ,  Lorna Helen Mitchell ,  Michael John Munchhof ,  Darren Martin Harvey

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

Abstract: 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

Applicant: EPIZYME, INC.

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

IPC: 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

Abstract: 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.

公开(公告)号：US12116358B2

公开(公告)日：2024-10-15

申请号：US17268151

申请日：2019-08-14

Applicant: EPIZYME, INC.

Inventor： John Lampe ,  John Campbell ,  Kenneth Duncan ,  Megan Alene Cloonan Foley ,  Darren Martin Harvey ,  Michael John Munchhof ,  Michael Thomenius ,  Lawrence Alan Reiter

IPC: C07D403/12 ,  A61P35/00 ,  C07D209/42 ,  C07D209/96 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10 ,  C07D491/08 ,  C07D491/107 ,  C07D498/04 ,  C07D498/08 ,  C07D498/10 ,  C07D513/10

CPC classification number: C07D403/12 ,  A61P35/00 ,  C07D209/42 ,  C07D209/96 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10 ,  C07D491/08 ,  C07D491/107 ,  C07D498/04 ,  C07D498/08 ,  C07D498/10 ,  C07D513/10

Abstract: Compounds of Formula I: (I) and the pharmaceutically acceptable salts and solvates thereof, wherein R1a, R1e, G1, G2, Q1, Q2, Q3, and (II) are defined as set forth in the specification, as are uses of compounds of Formula I to treat a disease, disorder, or condition such as cancer in a subject.

公开(公告)号：US10266526B2

公开(公告)日：2019-04-23

申请号：US15510586

申请日：2015-09-09

Applicant: EPIZYME, INC.

Inventor： Megan Alene Cloonan Foley ,  Kevin Wayne Kuntz ,  James Edward John Mills ,  Lorna Helen Mitchell ,  Michael John Munchhof ,  Darren Martin Harvey

IPC: A61K31/4192 ,  C07D249/04 ,  C07D451/04 ,  C07D213/81 ,  C07D213/82 ,  C07D231/14 ,  C07D233/90 ,  C07D401/12 ,  C07D241/26 ,  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

Abstract: 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：US20200148650A1

公开(公告)日：2020-05-14

申请号：US16588209

申请日：2019-09-30

Applicant: EPIZYME, INC.

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

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

Abstract: 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：US10179773B2

公开(公告)日：2019-01-15

申请号：US15510589

申请日：2015-09-09

Applicant: EPIZYME, INC.

Inventor： Richard Chesworth ,  Megan Alene Cloonan Foley ,  Kevin Wayne Kuntz ,  Lorna Helen Mitchell ,  Jennifer C. Petter ,  Carl Eric Schwartz

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

Abstract: 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：US10106510B2

公开(公告)日：2018-10-23

申请号：US15510605

申请日：2015-09-09

Applicant: EPIZYME, INC.

Inventor： Megan Alene Cloonan Foley ,  Kevin Wayne Kuntz ,  Lorna Helen Mitchell ,  Michael John Munchhof

IPC: A61K31/42 ,  C07D261/18 ,  C07D261/08

Abstract: 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：US10669243B2

公开(公告)日：2020-06-02

申请号：US16245986

申请日：2019-01-11

Applicant: EPIZYME, INC.

Inventor： Richard Chesworth ,  Megan Alene Cloonan Foley ,  Kevin Wayne Kuntz ,  Lorna Helen Mitchell ,  Jennifer C. Petter ,  Carl Eric Schwartz

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

Abstract: 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.

公开(公告)号：US10577363B2

公开(公告)日：2020-03-03

申请号：US15510588

申请日：2015-09-09

Applicant: EPIZYME, INC.

Inventor： Lorna Helen Mitchell ,  Andrew Simon Bell ,  Richard Chesworth ,  Megan Alene Cloonan Foley ,  Kevin Wayne Kuntz ,  James Edward John Mills ,  Michael John Munchhof

IPC: C07D451/04 ,  C07D413/14 ,  C07D413/12 ,  C07D487/08 ,  C07D519/00 ,  A61P35/00

Abstract: 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

Applicant: EPIZYME, INC.

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

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

Abstract: 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.