IP Library Granted Patent US 10,351,571
Granted Patent B2
US 10,351,571 · App. 15/988,790 · Granted Jul 16, 2019

Pyrrolotriazinones and imidazotriazinones as ubiquitin-specific protease 7 inhibitors

Inventors: Stephanos Ioannidis (Natick, MA); Adam Charles Talbot (Guilford, CT); Bruce Follows (Littleton, MA); Alexandre Joseph Buckmelter (Acton, MA); Minghua Wang (Acton, MA); Ann-Marie Campbell (Monroe, CT)
Assignee: FORMA Therapeutics, Inc.
C07D487/04
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Quick Facts
Patent No.
US 10,351,571
App. No.
15/988,790
Granted
Jul 16, 2019
Kind
B2
Abstract

The invention relates to inhibitors of USP7 inhibitors useful in the treatment of cancers, neurodegenerative diseases, immunological disorders, inflammatory disorders, cardiovascular diseases, ischemic diseases, viral infections and diseases, and bacterial infections and diseases, having the Formula: where R 1 , R 2 , R 3 , R 4 , R 5 , R 5′ , R 6 , X 1 , X 2 , m, and n are described herein.

Claims (39)

1. A compound of Formula (I):

or a pharmaceutically acceptable salt thereof,

wherein:

X 1 is C;

X 2 is CR 7 or N;

R 1 is —OH;

R 2 is (C 1 -C 8 ) alkyl, (C 6 -C 14 ) aryl, cycloalkyl, or heterocycloalkyl, wherein the alkyl, aryl, cycloalkyl, and heterocycloalkyl are optionally substituted with one or more R 8 ;

R 4 is (C 1 -C 6 ) alkyl or (C 6 -C 14 ) aryl, wherein the aryl is optionally substituted with one or more R 22 ;

R 5 and R 5′ are independently H;

R 6 is H;

R 7 is H;

each R 8 is independently (C 1 -C 6 ) alkyl, —(C 0 -C 4 )-alkylene-aryl, —(C 0 -C 4 )-alkylene-heteroaryl, —(C 0 -C 4 )-alkylene-O-heteroaryl, halogen, —C(O)R 12 , wherein alkyl, alkylene, aryl, and heteroaryl are optionally substituted with one or more R 9 ;

each R 9 is independently at each occurrence (C 1 -C 6 ) alkyl, halogen, or —NR 14 S(O) q R 15 ;

each R 12 is independently (C 2 -C 6 ) alkenyl;

each R 14 and R 15 is independently H or (C 2 -C 6 ) alkenyl;

each R 22 is independently at each occurrence (C 6 -C 14 ) aryl, —O—(C 3 -C 8 )cycloalkyl, halogen, wherein aryl and cycloalkyl are optionally substituted with one or more substituents independently selected from halogen;

m is 0;

n is 1; and

q is 2.

2. The compound of claim 1 , wherein R 4 is (C 6 -C 14 ) aryl, optionally substituted with one or more R 22 .

3. The compound of claim 2 , wherein R 22 is (C 6 -C 14 ) aryl.

4. The compound of claim 3 , wherein R 2 is heterocycloalkyl, optionally substituted with one or more R 8 .

5. The compound of claim 4 , wherein R 8 is —C(O)R 12 and R 12 is (C 2 -C 6 ) alkenyl.

6. The compound of claim 2 , wherein R 22 is halogen.

7. The compound of claim 6 , wherein R 2 is (C 1 -C 8 ) alkyl, optionally substituted with one or more R 8 .

8. The compound of claim 7 , wherein R 8 is independently selected from heteroaryl and halogen, wherein heteroaryl is substituted with one or more R 9 , and wherein R 9 is halogen.

9. The compound of claim 6 , wherein R 2 is cycloalkyl, optionally substituted with one or more R 8 .

10. The compound of claim 9 , wherein R 8 is O-heteroaryl, wherein heteroaryl is substituted with one or more R 9 , and wherein R 9 is (C 1 -C 6 ) alkyl.

11. The compound of claim 2 , wherein R 22 is —O—(C 3 -C 8 )cycloalkyl, optionally substituted with one or more substituents independently selected from halogen.

12. The compound of claim 11 , wherein R 2 is cycloalkyl, optionally substituted with one or more R 8 .

13. The compound of claim 12 , wherein R 8 is (C 1 -C 6 ) alkyl.

14. The compound of claim 1 , wherein R 4 is (C 1 -C 6 ) alkyl.

15. The compound of claim 14 , wherein R 2 is (C 6 -C 14 ) aryl, optionally substituted with one or more R 8 .

16. The compound of claim 15 , wherein:

R 8 is aryl, optionally substituted with one or more R 9 ;

R 9 is —NR 14 S(O) q R 15 ;

R 14 is H; and

R 15 is (C 2 -C 6 ) alkenyl.

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

Assignments (6)
RELEASE OF SECURITY INTEREST Recorded Oct 17, 2023
From: FIRST-CITIZENS BANK & TRUST COMPANY, AS AGENT
To: VALO HEALTH, INC.; VALO HEALTH, LLC
Reel/Frame 065255/0660 →
SECURITY INTEREST Recorded Jul 6, 2023
From: VALO HEALTH, LLC; VALO HEALTH, INC.
To: FIRST-CITIZENS BANK & TRUST COMPANY, AS AGENT
Reel/Frame 064207/0957 →
MERGER Recorded Sep 8, 2021
From: VALO EARLY DISCOVERY, INC.
To: VALO HEALTH, INC.
Reel/Frame 057438/0025 →
CHANGE OF NAME Recorded Sep 16, 2020
From: INTEGRAL EARLY DISCOVERY, INC.
To: VALO EARLY DISCOVERY, INC.
Reel/Frame 053787/0138 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 5, 2020
From: FORMA THERAPEUTICS, INC.
To: INTEGRAL EARLY DISCOVERY, INC.
Reel/Frame 053402/0298 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 14, 2018
From: IOANNIDIS, STEPHANOS; TALBOT, ADAM CHARLES; FOLLOWS, BRUCE; BUCKMELTER, ALEXANDRE JOSEPH; WANG, MINGHUA; CAMPBELL, ANN-MARIE
To: FORMA THERAPEUTICS, INC.
Reel/Frame 046824/0241 →
Continuity (3)
Continuation 14982131 · Dec 29, 2015
Provisional Application 62098145 · Dec 30, 2014
Related Publication 20180339991A1 · Nov 29, 2018