# US 10,118,931 B2 · CARM1 inhibitors and uses thereof

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- Number: US 10,118,931 B2
- Document ID: US10118931B2
- Status: Granted
- Kind: B2
- Application number: 15/835,758
- Filed: 2017-12-08
- Published: 2018-10-04
- Granted: 2018-11-06
- Earliest claimed: 2013-03-15
- Assignees: Epizyme, Inc.
- Applicants: Epizyme, Inc.
- Inventors: Richard Chesworth; Oscar Miguel Moradei; Gideon Shapiro; Lei Jin; Robert E. Babine
- Web page: https://patentgrep.com/patent/US10118931B2

## CPC

- C07D 487/10: Spiro-condensed systems
- A61P 3/00: Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00)
- A61P 21/00: Drugs for disorders of the muscular or neuromuscular system
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 35/00: Antineoplastic agents
- A61P 37/02: Immunomodulators
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07D 239/42: One nitrogen atom (nitro radicals C07D239/30)
- C07D 401/04: directly linked by a ring-member-to-ring-member bond
- C07D 403/04: directly linked by a ring-member-to-ring-member bond
- C07D 403/12: linked by a chain containing hetero atoms as chain links
- C07D 405/04: directly linked by a ring-member-to-ring-member bond
- C07D 405/12: linked by a chain containing hetero atoms as chain links
- C07D 405/14: containing three or more hetero rings
- C07D 409/14: containing three or more hetero rings
- C07D 413/04: directly linked by a ring-member-to-ring-member bond
- C07D 413/12: linked by a chain containing hetero atoms as chain links
- C07D 413/14: containing three or more hetero rings
- C07D 417/14: containing three or more hetero rings
- C07D 471/04: Ortho-condensed systems
- C07D 471/10: Spiro-condensed systems
- C07D 487/04: Ortho-condensed systems
- C07D 487/08: Bridged systems
- C07D 493/04: Ortho-condensed systems
- C07D 493/10: Spiro-condensed systems
- C07D 495/04: Ortho-condensed systems
- C07D 498/04: Ortho-condensed systems
- C07D 498/10: Spiro-condensed systems
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

Provided herein are compounds of Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, wherein X, R1, R1a, R2a, R2b, R2c, R2d, are as defined herein, and Ring HET is a 6-membered monocyclic heteroaryl ring system of Formula: wherein L2, R13, G8, G10, G11, and G12 are as defined herein. Compounds of the present invention are useful for inhibiting CARM1 activity. Methods of using the compounds for treating CARM1-mediated disorders are also described.

## Claims

### Claim 1

A compound which is:
or a pharmaceutically acceptable salt thereof.

### Claim 2

A compound which is:

### Claim 3 (depends on 1)

A pharmaceutical composition comprising the compound or pharmaceutically acceptable salt according to claim 1, and a pharmaceutically acceptable excipient.

### Claim 4 (depends on 2)

A pharmaceutical composition comprising the compound according to claim 2, and a pharmaceutically acceptable excipient.