Granted Patent B2

US 12,569,485 · App. 17/788,624 · Granted Mar 10, 2026

Inventors: Yi Zhang (Belmont, MA); Paul R. Fleming (Lexington, MA); Xiao Zhu (Winchester, MA)

Assignee: Kymera Therapeutics, Inc.

A61K31/506A61K31/437A61K31/496A61K31/501A61K31/5025C07D217/22C07D237/20C07D401/12C07D401/14C07D405/12C07D471/04C07D471/14C07D471/20C07D487/04C07D487/14

Abstract

Claims (20)

1 . A SMARCA2 inhibitor compound of formula II-a-3:

or a pharmaceutically acceptable salt thereof, wherein:

each of Ring B and Ring D is independently a fused ring selected from 6-membered aryl, 5 to 6-membered heteroaryl containing 1-4 heteroatoms independently selected from nitrogen, oxygen, and sulfur, and a 4 to 9-membered saturated or partially unsaturated monocyclic, bicyclic, or bridged bicyclic carbocyclyl or heterocyclyl with 1-4 heteroatoms independently selected from boron, nitrogen, oxygen, silicon, and sulfur;

each R 2 is independently hydrogen, R 4 , halogen, —CN, —OR, —NR 2 , —CFR 2 , —CF 2 R, —CF 3 , —C(O)R, —C(O)OR, or —C(O)NR 2 ;

each R 3 is independently fluoro or chloro;

each R is independently hydrogen, or an optionally substituted group selected from C 1-6 aliphatic, phenyl, a 4-7 membered saturated or partially unsaturated heterocyclic having 1-2 heteroatoms independently selected from nitrogen, oxygen, and sulfur, and a 5-6 membered heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, and sulfur, or:

two R groups on the same atom are taken together with their intervening atoms to form a 4-7 membered saturated, partially unsaturated, or heteroaryl ring having 0-3 heteroatoms, in addition to the atom to which they are attached, independently selected from nitrogen, oxygen, and sulfur;

each R 4 is independently an optionally substituted group selected from C 1-6 aliphatic, phenyl, a 4-7 membered saturated or partially unsaturated heterocyclic ring having 1-2 heteroatoms independently selected from nitrogen, oxygen, and sulfur, and a 5-6 membered heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, and sulfur;

n is 0, 1, 2, 3, 4, or 5; and

m is 0, 1, or 2.

2 . The compound of claim 1 , wherein said compound is any one of the following formulae:

or a pharmaceutically acceptable salt thereof.

3 . The compound of claim 1 , wherein said compound is selected from:

or a pharmaceutically acceptable salt thereof.

4 . The compound of claim 1 , wherein Ring B is a fused ring selected from a 5 to 6-membered heteroaryl containing 1-4 heteroatoms independently selected from nitrogen, oxygen, and sulfur, and a 4 to 9-membered saturated or partially unsaturated monocyclic, bicyclic, or bridged bicyclic heterocyclyl with 1-4 heteroatoms independently selected from nitrogen, oxygen, and sulfur.

5 . The compound of claim 1 , wherein Ring B is

6 . The compound of claim 1 , wherein Ring D is a fused ring selected from 5 to 6-membered heteroaryl containing 1-4 heteroatoms independently selected from nitrogen, oxygen, and sulfur, and a 4 to 9-membered saturated or partially unsaturated monocyclic, bicyclic, or bridged bicyclic carbocyclyl or heterocyclyl with 1-4 heteroatoms independently selected from nitrogen, oxygen, and sulfur.

7 . The compound of claim 1 , wherein Ring D is

8 . A pharmaceutical composition comprising a compound of claim 1 , and a pharmaceutically acceptable carrier, adjuvant, or vehicle.

9 . The pharmaceutical composition according to claim 8 , further comprising an additional therapeutic agent.

Assignments (1)

Continuity (2)

References Cited (141)