IP Library Granted Patent US 10,150,758
Granted Patent B2
US 10,150,758 · App. 15/150,759 · Granted Dec 11, 2018

PRMT5 inhibitors and uses thereof

Inventors: Kenneth W. Duncan (Westwood, MA); Richard Chesworth (Concord, MA); Michael John Munchhof (Salem, CT)
Assignee: Epizyme, Inc.
C07D405/14C07D401/06C07D401/14C07D413/06C07D413/14
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Quick Facts
Patent No.
US 10,150,758
App. No.
15/150,759
Granted
Dec 11, 2018
Kind
B2
Abstract

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.

Claims (17)

1. A compound of Formula:

or a pharmaceutically acceptable salt thereof,

wherein:

each R B is independently selected from the group consisting of hydrogen, 5-6 membered monocyclic heterocyclyl wherein said heterocyclyl has one ring heteroatom selected from nitrogen, oxygen and sulfur, and phenyl, each optionally substituted with 1, 2, 3, or 4 independent C 1-10 alkyl or halo;

each R y is independently selected from the group consisting of: a) phenyl optionally substituted with 1, 2, 3, or 4 independent C 1-10 alkyl or halo; b) —N(R B ) 2 ; and c) —C(O)N(R B ) 2 ;

m is 0, 1, 2, 3, or 4;

and

n is 0.

2. The compound of claim 1 , wherein m is 0, 1, or 2.

3. The compound of claim 1 , wherein the compound is selected from the group consisting of:

and pharmaceutically acceptable salts thereof.

4. A pharmaceutical composition comprising a compound of claim 1 or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient.

5. A kit or packaged pharmaceutical comprising a compound of claim 1 or a pharmaceutically acceptable salt thereof, and instructions for use thereof.

6. The compound of claim 1 :

or a pharmaceutically acceptable salt thereof.

7. A compound selected from

and pharmaceutically acceptable salts thereof.

Assignments (3)
TERMINATION AND RELEASE OF SECURITY INTEREST IN PATENTS AT REEL/FRAME: 051057/0848 Recorded Aug 13, 2022
From: BIOPHARMA CREDIT PLC
To: EPIZYME, INC.
Reel/Frame 061165/0501 →
SECURITY INTEREST Recorded Nov 19, 2019
From: EPIZYME, INC.
To: BIOPHARMA CREDIT PLC
Reel/Frame 051057/0848 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 16, 2016
From: DUNCAN, KENNETH W.; CHESWORTH, RICHARD; MUNCHHOF, MICHAEL JOHN
To: EPIZYME, INC.
Reel/Frame 038605/0692 →
Continuity (4)
Continuation 14136559 · Dec 20, 2013
Provisional Application 61785025 · Mar 14, 2013
Provisional Application 61745477 · Dec 21, 2012
Related Publication 20170088541A1 · Mar 30, 2017