IP Library Granted Patent US 11,530,236
Granted Patent B2
US 11,530,236 · App. 17/083,871 · Granted Dec 20, 2022

CD73 inhibitors

Inventors: Xiaohui Du (Belmont, CA); John Eksterowicz (Burlingame, CA); Valeria R. Fantin (Burlingame, CA); Daqing Sun (Foster City, CA); Qiuping Ye (Foster City, CA); Jared Moore (San Rafael, CA); Tatiana Zavorotinskaya (Moraga, CA); Brian R. Blank (Daly City, CA); Yosup Rew (Foster City, CA); Kejia Wu (South San Francisco, CA); Liusheng Zhu (Foster City, CA); Johnny Pham (San Bruno, CA); Hiroyuki Kawai (Pacifica, CA); Chien-Hung Yeh (San Bruno, CA)
Assignee: ORIC PHARMACEUTICALS, INC.
C07H19/23A61P35/00
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Quick Facts
Patent No.
US 11,530,236
App. No.
17/083,871
Granted
Dec 20, 2022
Kind
B2
Abstract

Described herein are CD73 inhibitors and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of cancer, infections, and neurodegenerative diseases.

Claims (67)

1. A compound of Formula (I), or a pharmaceutically acceptable salt thereof:

wherein:

Q 1 is CW;

Q 2 is N and Q 3 is N;

W is hydrogen;

R 1 and R 2 are independently hydrogen, C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 hydroxyalkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, C 1 -C 6 alkyl(aryl), C 1 -C 6 alkyl(heteroaryl), C 1 -C 6 alkyl(cycloalkyl), or C 1 -C 6 alkyl(heterocycloalkyl); wherein each alkyl, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl is independently optionally substituted with one, two, or three R 1a ;

each R 1a is independently halogen, —CN, C 1 -C 6 alkyl, C 1 -C 6 fluoroalkyl, or C 1 -C 6 hydroxyaikyl;

R 3 is hydrogen, halogen, —CN, —OR b , —SR b , C 1 -C 6 alkyl, C 2 -C 6 alkynyl, or C 1 -C 6 hydroxyalkyl; wherein the alkyl and alkynyl is independently optionally substituted with one, two, or three R 3a ;

each R 3a is halogen, C 1 -C 6 alkyl, C 1 -C 6 fluoroalkyl, C 1 -C 6 hydroxyalkyl, or cycloalkyl;

R 4 and R 5 are OR b ;

R 6 is hydrogen, deuterium, halogen C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 deuteroalkyl, C 1 -C 6 hydroxyalkyl, C 1 -C 6 heteroalkyl, or heterocycloalkyl; wherein the alkyl is independently optionally substituted with one, two, or three R 6a ;

each R 6a is —OR 13 , C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 deuteroalkyl, C 1 -C 6 hydroxyalkyl, C 1 -C 6 heteroalkyl, cycloalkyl, or heteroaryl;

R 7 , R 8 , R 9 , and R 10 are independently hydrogen, deuterium, or C 1 -C 6 alkyl;

X is —S— or —O—;

Ring A is heterocycloalkyl or heteroaryl;

each R A is independently halogen, —CN, —OR b , —SR b , C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, or C 1 -C 6 hydroxyalkyl;

n is 0, 1, 2, 3, or 4;

each R 13 is independently hydrogen, C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, or C 1 -C 6 deuteroalkyl;

R 21 and R 22 are independently hydrogen or C 1 -C 20 alkyl; and

each R b is independently hydrogen or C 1 -C 6 alkyl;

provided that the compound is not

2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein:

R 3 is halogen, C 2 -C 6 alkynyl, or C 1 -C 6 hydroxyalkyl; wherein each alkyl and alkynyl is independently optionally substituted with one, two, or three R 3a .

3. The compound of claim 2 , or a pharmaceutically acceptable salt thereof, wherein:

R 3 is halogen.

4. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein:

R 1 is C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, cycloalkyl, heterocycloalkyl, C 1 -C 6 alkyl(aryl), C 1 -C 6 alkyl(heteroaryl), C 1 -C 6 alkyl(cycloalkyl), or C 1 -C 6 alkyl(heterocycloalkyl); wherein each alkyl, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl is independently optionally substituted with one, two, or three R 1a .

5. The compound of claim 4 , or a pharmaceutically acceptable salt thereof, wherein:

R 1 is C 1 -C 6 alkyl, cycloalkyl, C 1 -C 6 alkyl(aryl), or C 1 -C 6 alkyl(cycloalkyl); wherein each alkyl, cycloalkyl, and aryl is independently optionally substituted with one, two, or three R 1a .

6. The compound of claim 5 , or a pharmaceutically acceptable salt thereof, wherein:

R 1 is cycloalkyl optionally substituted with one, two, or three R 1a .

7. The compound of claim 6 , or a pharmaceutically acceptable salt thereof, wherein:

R 1 is cycloalkyl.

8. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein:

each R 1a is independently halogen, —CN, C 1 -C 6 alkyl, or C 1 -C 6 fluoroalkyl.

9. The compound of claim 8 , or a pharmaceutically acceptable salt thereof, wherein:

each R 1a is independently halogen or C 1 -C 6 alkyl.

10. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein:

R 2 is hydrogen or C 1 -C 6 alkyl.

11. The compound of claim 10 , or a pharmaceutically acceptable salt thereof, wherein:

R 2 is hydrogen.

12. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein:

X is —O—.

13. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein:

R 7 , R 8 , R 9 , and R 10 are independently hydrogen or C 1 -C 6 alkyl.

14. The compound of claim 13 , or a pharmaceutically acceptable salt thereof, wherein:

R 7 , R 8 , R 9 , and R 10 are hydrogen.

15. The compound of claim 1 , or pharmaceutically acceptable salt thereof, wherein:

Ring A is heteroaryl.

16. The compound of claim 15 , or a pharmaceutically acceptable salt thereof, wherein:

n is 0.

17. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein:

R 6 is hydrogen, C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 hydroxyalkyl, C 1 -C 6 heteroalkyl, or heterocycloalkyl; wherein the alkyl, and heterocycloalkyl is independently optionally substituted with one, two, or three R 6a .

18. The compound of claim 17 , or a pharmaceutically acceptable salt thereof, wherein:

R 6 is hydrogen, C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 hydroxyalkyl, or C 1 -C 6 heteroalkyl; wherein the alkyl is independently optionally substituted with one, two, or three R 6a .

19. The compound of claim 18 , or a pharmaceutically acceptable salt thereof, wherein:

R 6 is C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 hydroxyalkyl, or C 1 -C 6 heteroalkyl; wherein the alkyl is independently optionally substituted with one, two, or three R 6a .

20. The compound of claim 19 , or a pharmaceutically acceptable salt thereof, wherein:

R 6 is C 1 -C 6 hydroxyalkyl or C 1 -C 6 heteroalkyl; wherein the alkyl is independently optionally substituted with one, two, or three R 6a .

21. The compound of claim 18 , or a pharmaceutically acceptable salt thereof, wherein:

R 6 is hydrogen, C 1 -C 6 hydroxyalkyl, or C 1 -C 6 heteroalkyl; wherein the alkyl is independently optionally substituted with one, two, or three R 6a .

22. The compound of claim 21 , or a pharmaceutically acceptable salt thereof, wherein:

R 6 is C 1 -C 6 hydroxyalkyl.

23. The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein:

R 21 and R 22 are hydrogen.

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

25. A method of inhibiting, CD73 comprising contacting CD73 with a compound of claim 1 , or a pharmaceutically acceptable salt thereof.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 1, 2020
From: DU, XIAOHUI; EKSTEROWICZ, JOHN; FANTIN, VALERIA R.; SUN, DAQING; YE, QIUPING; MOORE, JARED; ZAVOROTINSKAYA, TATIANA; BLANK, BRIAN R.; REW, YOSUP; WU, KEJIA; ZHU, LIUSHENG; PHAM, JOHNNY; KAWAI, HIROYUKI; YEH, CHIEN-HUNG
To: ORIC PHARMACEUTICALS, INC.
Reel/Frame 054508/0248 →
Continuity (4)
Provisional Application 63088646 · Oct 7, 2020
Provisional Application 62987806 · Mar 10, 2020
Provisional Application 62928138 · Oct 30, 2019
Related Publication 20210130389A1 · May 6, 2021
Cited By (2)
US 12,454,544 US 12,577,272