IP Library Granted Patent US 9,732,041
Granted Patent B2
US 9,732,041 · App. 15/093,103 · Granted Aug 15, 2017

Arginine methyltransferase inhibitors and uses thereof

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Quick Facts
Patent No.
US 9,732,041
App. No.
15/093,103
Granted
Aug 15, 2017
Kind
B2
Abstract

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.

Claims (11)

1. A compound selected from the group consisting of:

and pharmaceutically acceptable salts thereof.

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

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

4. A method of inhibiting an arginine methyltransferase (RMT) comprising contacting a cell with an effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof.

5. A method of modulating gene expression comprising contacting a cell with an effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof.

6. A method of modulating transcription comprising contacting a cell with an effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof.

7. A method of treating an RMT-mediated disorder, comprising administering to a subject in need thereof a therapeutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof;

wherein the RMT-mediated disorder is breast cancer, prostate cancer, lung cancer, colon cancer, bladder cancer, lymphoma, leukemia, diabetes mellitus, kidney failure, coronary heart disease, oculopharyngeal muscular dystrophy, or amyotrophic lateral sclerosis.

8. The method of claim 7 , wherein the disorder is breast cancer, prostate cancer, lung cancer, colon cancer, bladder cancer, lymphoma, or leukemia.

9. The method of claim 7 , wherein the disorder is amyotrophic lateral sclerosis.

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 Apr 13, 2016
From: CHESWORTH, RICHARD; MITCHELL, LORNA HELEN; SHAPIRO, GIDEON; BORIACK-SJODIN, PAULA ANN; MORADEI, OSCAR MIGUEL; JIN, LEI; DUNCAN, KENNETH W.
To: EPIZYME, INC.
Reel/Frame 038424/0277 →