IP Library Granted Patent US 10,934,299
Granted Patent B2
US 10,934,299 · App. 16/517,149 · Granted Mar 2, 2021

Pyrrolo and pyrazolopyrimidines as ubiquitin-specific protease 7 inhibitors

Inventors: Stephanos Ioannidis (Natick, MA); Adam Charles Talbot (Watertown, MA); Bruce Follows (Littleton, MA); Alexandre Joseph Buckmelter (Acton, MA); Minghua Wang (Acton, MA); Ann-Marie Campbell (Monroe, CT); Darby Rye Schmidt (Arlington, MA); David Joseph Guerin (Natick, MA); Justin Andrew Caravella (Cambridge, MA); R. Bruce Diebold (Waltham, MA); Anna Ericsson (Shrewsbury, MA); David R. Lancia, Jr. (Boston, MA)
Assignee: Valo Early Discovery, Inc.
C07D487/04A61K31/519C07D519/00
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Quick Facts
Patent No.
US 10,934,299
App. No.
16/517,149
Granted
Mar 2, 2021
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 m, n, X 1 , X 2 , R 1 -R 5 , R 5′ and R 6 are described herein.

Claims (28)

1. A compound of Formula (Ig):

or pharmaceutically acceptable salts thereof,

wherein

R 2 is (C 1 -C 8 ) alkyl, (C 3 -C 8 ) cycloalkyl, or heterocyclyl, wherein alkyl, cycloalkyl, and heterocyclyl are optionally substituted with one or more R 8 ;

each R 8 is, independently at each occurrence, selected from —(C 0 -C 4 )-alkylene-heteroaryl, —(C 0 -C 4 )-alkylene-O-heteroaryl, or halogen, wherein heteroaryl is optionally substituted with one or more R 9 ;

each R 9 is, independently at each occurrence, halogen;

R 4 is —(C 0 -C 3 ) alkylene-aryl, wherein aryl is optionally substituted with one or more R 12 ;

each R 12 is, independently at each occurrence, selected from halogen or aryl optionally substituted with one or more R 13 ; and

each R 13 is, independently at each occurrence, (C 1 -C 6 ) haloalkyl.

2. The compound of claim 1 , wherein R 4 is —(C 0 -C 3 ) alkylene-phenyl, wherein phenyl is optionally substituted with one or more R 12 .

3. The compound of claim 2 , wherein R 4 is —(C 0 -C 3 ) alkylene-phenyl, wherein phenyl is substituted with one R 12 .

4. The compound of claim 3 , wherein R 12 is halogen.

5. The compound of claim 4 , wherein R 12 is fluorine.

6. The compound of claim 5 , wherein R 2 is (C 3 -C 8 ) cycloalkyl optionally substituted with one or more R 8 .

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

8. The compound of claim 7 , wherein R 2 is cyclohexyl substituted with one R 8 .

9. The compound of claim 8 , wherein R 8 is —(C 0 -C 4 )-alkylene-O-heteroaryl.

10. The compound of claim 9 , wherein R 8 is O-pyridyl.

11. The compound of claim 3 , wherein R 12 is aryl optionally substituted with one or more R 13 .

12. The compound of claim 11 , wherein R 12 is phenyl optionally substituted with one or more R 13 .

13. The compound of claim 12 , wherein R 12 is phenyl substituted with one R 13 .

14. The compound of claim 13 , wherein R 13 is trifluoromethyl.

15. The compound of claim 14 , wherein R 2 is heterocyclyl.

16. The compound of claim 15 , wherein R 2 is piperazinyl.

17. The compound of claim 1 , wherein the compound is 5-({1-[(3 S)-4,4-difluoro-3-(4-fluoro-1H-pyrazol-1-yl)butanoyl]-4-hydroxypiperidin-4-yl}methyl)-1-(4-fluorophenyl)-1H,4H,5H-pyrazolo[3,4-d]pyrimidin-4-one, or a pharmaceutically acceptable salt thereof.

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

19. A pharmaceutical composition comprising a compound of claim 10 , or a pharmaceutically accepted salt thereof, and a pharmaceutically accepted carrier.

20. A pharmaceutical composition comprising a compound of claim 16 , or a pharmaceutically accepted salt thereof, and a pharmaceutically accepted 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 Dec 26, 2019
From: IOANNIDIS, STEPHANOS; TALBOT, ADAM CHARLES; FOLLOWS, BRUCE; BUCKMELTER, ALEXANDRE JOSEPH; WANG, MINGHUA; CAMPBELL, ANN-MARIE; SCHMIDT, DARBY RYE; GUERIN, DAVID JOSEPH; CARAVELLA, JUSTIN A.; DIEBOLD, R. BRUCE; ERICSSON, ANNA; LANCIA, DAVID R., JR.
To: FORMA THERAPEUTICS, INC.
Reel/Frame 051372/0388 →
Continuity (4)
Continuation 15874163 · Jan 18, 2018
Continuation 14982127 · Dec 29, 2015
Provisional Application 62098141 · Dec 30, 2014
Related Publication 20190367525A1 · Dec 5, 2019
Cited By (3)
US 12,319,668 US 12,595,244 US 12,703,692