# US 12,162,893 B2 · Tricyclic pyridones and pyrimidones

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- Number: US 12,162,893 B2
- Document ID: US12162893B2
- Status: Granted
- Kind: B2
- Application number: 17/482,350
- Filed: 2021-09-22
- Published: 2022-04-21
- Granted: 2024-12-10
- Earliest claimed: 2020-09-23
- Assignees: Erasca, Inc.
- Applicants: Erasca, Inc.
- Inventors: Jun Feng; Jean-Michel Vernier; Marcos Gonzalez-Lopez; Benjamin Jones; Nicholas A. Isley; Ping Chen
- Web page: https://patentgrep.com/patent/US12162893B2

## CPC

- C07D 498/16: Peri-condensed systems
- A61P 35/00: Antineoplastic agents
- C07D 513/04: Ortho-condensed systems
- C07D 513/06: Peri-condensed systems
- C07D 513/14: Ortho-condensed systems
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

A compound of Formula (I) is provided: where the variables are defined herein.

## Claims

### Claim 1

A compound of Formula (XXIX) or pharmaceutically acceptable salt thereof:
wherein:
X is S(O)p, wherein p is an integer from 0 to 2;
j is an integer from 0 to 2;
G is selected from the group consisting of N, CH, and
wherein G1 and G2 are independently (CH2)q, where q is 1 or 2;
each R1 is an optional substitution independently selected from the group consisting of alkyl, cyano, cycloalkyl, halo, haloalkyl, trifluoromethyl, and alkoxy;
Ar is aryl, N-arylamino, N-aryl-N-alkylamino, aryloxy, arylthio, heteroaryl, N-heteroarylamino, N-heteroaryl-N-alkylamino, heteroaryloxy, or heteroarylthio, any of which is optionally substituted;
n is an integer from 0 to 2;
R2 is selected from the group consisting of alkyl, alkylamino, dialkylamino, alkylamidoalkyl, arylamidoalkyl, alkylsulfonamidoalkyl, arylsulfonamidoalkyl, N-alkyl aminoalkyl, N,N-dialkyl aminoalkyl, alkoxy, alkoxyalkyl, cycloalkyl, alkylcycloalkyl, hydroxyalkyl, halo, haloalkyl, aralkyl, heteroaryl, heteroarylalkyl, heterocyclyl, heterocyclylalkyl any of which are optionally substituted;
wherein when j is 1, the heterocyclylalkyl is selected from:
m is an integer from 0 to 6;
each R7 is independently selected from an alkyl group selected from methyl, ethyl, and propyl, any of which are optionally substituted with one or more fluorine atoms, —CH2(CH3)C═CF2, cyano, propargyl, —CH2C(O)V, wherein V is selected from methyl, OH, NHRi wherein Ri is hydrogen or alkyl; or any two R7 may combine to form a fused-ring, spiro or bridging bicycle, wherein any one fused-ring or bridging atom is O, S, S═O, SO2, or NRj, wherein Rj is H, methyl or trifluoromethyl;
k is an integer from 0 to 4; and,
wherein the acrylyl moiety linked to G is optionally substituted.

### Claim 2 (depends on 1)

The compound of claim 1, wherein X is S.

### Claim 3 (depends on 1)

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

### Claim 4 (depends on 1)

A pharmaceutical composition comprising a compound of claim 1 or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier or diluent.