SMARCA inhibitors and uses thereof

Patent metadata

Field	Value
Publication number	US-12569485-B2
Application number	US-202017788624-A
Country	US
Kind code	B2
Filing date	Dec 23, 2020
Priority date	Dec 23, 2019
Publication date	Mar 10, 2026
Grant date	Mar 10, 2026

Abstract

The present invention provides compounds, compositions thereof, and methods of using the same.

First claim

We claim:

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.

Assignees

• Kymera Therapeutics Inc

Inventors

• Zhang Yi
• Fleming Paul R
• Zhu Xiao

Classifications

• C07D487/14

  Ortho-condensed systems · CPC title

• C07D487/04

  Ortho-condensed systems · CPC title

• C07D471/20

  Spiro-condensed systems · CPC title

• C07D471/14 Primary

  Ortho-condensed systems · CPC title

• C07D471/04

  Ortho-condensed systems · CPC title