IP Library › Granted Patent US 12,662,481
Granted Patent B2
US 12,662,481 · App. 17/580,207 · Granted Jun 23, 2026

Substituted 2-morpholinopyridine derivatives as ATR kinase inhibitors

Inventors: Sheldon N. Crane (Notre Dame de I'lle Perrot, CA); Vouy-linh Truong (Pierrefonds, CA); Abbas Abdoli (Montreal, CA); Jean-François Truchon (Saint-Laurent, CA); Cameron Black (Baie-D'Urfé, CA); Stéphane Dorich (Point-Claire, CA); Lee Fader (Hawkesbury, CA); Stéphanie Lanoix (Mansfield, CA); Paul Jones (Verdun, CA); Miguel St-Onge (Vaudreuil-Dorion, CA); Audrey Picard (Mirabel, CA); Cyrus M. Lacbay (Montreal, CA)
Assignee: Repare Therapeutics Inc.
C07D471/04A61P35/00C07D519/00
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Quick Facts
Patent No.
US 12,662,481
App. No.
17/580,207
Filed
Jan 20, 2022
Granted
Jun 23, 2026
Kind
B2
Art Unit
1624
USPC
514/234.2
Abstract

Disclosed are compounds and pharmaceutically acceptable salts thereof that may be used in the treatment of subjects in need thereof. The compounds disclosed herein may be inhibitors of Ataxia-telangiectasia and RAD-3-related protein kinase (ATR). Also disclosed are pharmaceutical compositions containing the compounds or pharmaceutically acceptable salts thereof and methods of their preparation and use.

Claims (31)

1 . A compound of formula (I):

or a pharmaceutically acceptable salt thereof,

wherein

is a double bond, and each Y is independently N or CR 4 ; or is a single bond, and each Y is independently NR Y , carbonyl, or C(R Y ) 2 ; wherein each R Y is independently H or optionally substituted C 1-6 alkyl;

R 1 is methyl;

R 3 is optionally substituted C 1-9 heteroaryl or optionally substituted C 1-9 heteroaryl C 1-6 alkyl;

each R 4 is independently hydrogen, halogen, optionally substituted C 1-6 alkyl, optionally substituted C 2-6 alkenyl, or optionally substituted C 2-6 alkynyl; and

X is hydrogen or halogen.

2 . The compound of claim 1 , wherein the compound is a compound of formula (II):

or a pharmaceutically acceptable salt thereof.

3 . The compound of claim 1 , wherein the compound is a compound of formula (IB):

or a pharmaceutically acceptable salt thereof.

4 . The compound of claim 1 , wherein the compound is a compound of formula (IB-a):

or a pharmaceutically acceptable salt thereof.

5 . The compound of claim 1 , wherein R 3 is optionally substituted, monocyclic C 1-9 heteroaryl comprising at least one nitrogen atom.

6 . The compound of claim 1 , wherein R 3 is:

7 . The compound of claim 1 , wherein R 4 is hydrogen.

8 . The compound of claim 1 , wherein X is hydrogen.

9 . A compound selected from the group consisting of:

and pharmaceutically acceptable salts thereof.

10 . The compound of claim 9 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

11 . The compound of claim 9 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

12 . The compound of claim 9 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

13 . The compound of claim 9 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

14 . The compound of claim 9 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

15 . A pharmaceutical composition comprising the compound of claim 1 and a pharmaceutically acceptable excipient.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 1, 2022
From: CRANE, SHELDON N.; TRUONG, VOUY-LINH; ABDOLI, ABBAS; TRUCHON, JEAN-FRANÇOIS; BLACK, CAMERON; DORICH, STÉPHANE; FADER, LEE; LANOIX, STÉPHANIE; JONES, PAUL; ST-ONGE, MIGUEL; PICARD, AUDREY; LACBAY, CYRUS M.
To: REPARE THERAPEUTICS INC.
Reel/Frame 058841/0689 →
Priority Claims (1)
WO PCT/CA2019/051539 · Oct 30, 2019 · international
Continuity (3)
Continuation PCTCA2020051014 · Jul 22, 2020
Provisional Application 62877177 · Jul 22, 2019
Related Publication 20220185809A1 · Jun 16, 2022
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