IP Library Granted Patent US 11,576,922
Granted Patent B2
US 11,576,922 · App. 17/404,497 · Granted Feb 14, 2023

CD73 inhibitors

Inventors: Xiaohui Du (Belmont, CA); John Eksterowicz (Burlingame, CA); Valeria R. Fantin (Burlingame, CA); Erica L. Jackson (Burlingame, CA); Daqing Sun (Foster City, CA); Qiuping Ye (Foster City, CA); Jared Moore (San Rafael, CA)
Assignee: ORIC PHARMACEUTICALS, INC.
A61K31/675C07F9/6558
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Quick Facts
Patent No.
US 11,576,922
App. No.
17/404,497
Granted
Feb 14, 2023
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 (174)

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

wherein:

A is —O— or —CH 2 —;

R 1 and R 2 are each independently hydrogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, C 1 -C 6 alkyl(aryl), C 1 -C 6 alkyl(heteroaryl), C 1 -C 6 alkyl(cycloalkyl), C 1 -C 6 alkyl(heterocycloalkyl), —S(═O) 2 R 15 , —S(═O) 2 NR 16 R 17 , or —C(═O)2R 15 ; wherein each alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl is independently optionally substituted with one, two, or three R 20a ;

or R 1 and R 2 are taken together with the nitrogen atom to which they are attached to form a heterocycloalkyl optionally substituted with one, two, or three R 20a ;

R 3 is halogen, —CN, OR 15 , SR 18 , C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, C 1 -C 6 alkyl(aryl), C alkyl(heteroaryl), C 1 -C 6 alkyl(cycloalkyl), or C 1 -C 6 alkyl(heterocycloalkyl); wherein each alkyl; alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl is independently optionally substituted with one, two, or three R 20 b;

R 4 and R 7 are each independently hydrogen, halogen, —OH, —OR 15 , —NR 16 S(═O) 2 R 15 ; —NR 16 C(═O)R 15 , C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl; wherein each alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl is independently optionally substituted with one, two, or three R 20c ;

R 5 and R 6 are each independently hydrogen, halogen, —OH, —OR 15 , —NR 16 S(═O) 2 R 15 , —NR 16 (═O)R 15 , C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl; wherein each alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl is independently optionally substituted with one, two, or three R 20d ;

R 8 is hydrogen;

R 9 and R 10 are;

Y 3 is —CR 13 R 14 —;

Y 4 is —O—;

R 13 and R 14 are hydrogen;

R 15 is C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl; wherein each alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl is independently optionally substituted with one, two, or three R 20e ;

R 16 and R 17 are each independently hydrogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, cycloalkyl, or heterocycloalkyl; wherein each alkyl, alkenyl, alkynyl, cycloalkyl, and heterocycloalkyl is independently optionally substituted with one, two, or three R 20f ;

or R 16 and R 17 are taken together with the nitrogen atom to which they are attached to form a heterocycloalkyl optionally substituted with one, two, or three halogen, C 1 -C 6 alkyl, or C 1 -C 6 haloalkyl;

R 18 is C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, C 1 -C 6 alkyl(aryl), C 1 -C 6 alkyl(heteroaryl), C 1 -C 6 alkyl(cycloalkyl), C 1 -C 6 alkyl(heterocycloalkyl); wherein each alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl is independently optionally substituted with one, two, or three R 20g ;

each R 20a , R 20b , R 20c , R 20d , R 20e , R 20f , and R 20g are independently halogen, —CN, —OH, —OR a , —SH—, SR a , —S(═O)R a , —NO 2 , —NR b R c —S(═O) 2 R a , —NHS(═O) 2 R a , —S(═O) 2 NR b R c , —C(═O)R a , —OC(═O)R a , —C(═O)OR b , —OC(═O)OR b , —C(═O)NR b R c , —OC(═O)NR b R c , —NR b C(═O)NR b R c , —NR b C(═O)R a , —NR b C(═O)OR b , C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, C 1 -C 6 alkyl(aryl), C 1 -C 6 alkyl(heteroaryl), C 1 -C 6 alkyl(cycloalkyl), or Ct-Ce alkyl(heterocycloalkyl); wherein each alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl is independently optionally substituted with one, two, or three R 21 ;

each R is independently halogen, —CN, —OH, —OR a , —SH, —SR a , —S(═O)R a , —NO 2 , —NR b R c , —S(═O) 2 R a , —NHS(═O) 2 R a , —S(═O) 2 NR b R c , —C(═O)R a , —OC(═O)R a , —C(═O)OR b , —OC(═O)OR b , —C(═O)NR b R c , —OC(═O)NR b R c , —NR b C(═O)NR b R c , —NR b (═O)R a , —NR b R c (═O)OR b , C 1 - C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 hydroxyalkyl, C 1 -C 6 heteroalkyl, cycloalkyl, or heterocycloalkyl;

each R a is independently C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 1 -C 6 haloalkyl, C 1 -C 6 hydroxyalkyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl;

R b and R c are each independently hydrogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 1 -C 6 haloalkyl, C 1 -C 6 hydroxyalkyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl;

or R b and R c are taken together with the nitrogen atom to which they are attached to form a heterocycloalkyl optionally substituted with one, two, or three halogen, C 1 -C 6 alkyl, or C 1 -C 6 haloalkyl; and

R 30 , R 33 , and R 34 are each independently hydrogen, C 1 -C 20 alkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, C 1 -C 6 alkyl(aryl), C 1 -C 6 alkyl(heteroaryl), C 1 -C 6 alkyl(cycloalkyl), C 1 -C 6 alkyl(heterocycloalkyl), —(CR 50 R 51 ) v OC(═O) R 40 , —(CR 50 R 51 ) v SC(═O)R 40 ), —(CR 50 R 51 ) v OC(═O)OR 40 , —(CR 50 R 51 ) v OC(═O)(CR 52 R 53 ) v C (═O)(CR 52 R 53 ) v C(═O)R 41 , or —(C 1 -C 6 alkylene)[OC(═O)R 40 ] 2 ; provided that at least one of R 30 , R 33 , or R 34 is not hydrogen;

or R 34 and R 33 are taken together with the atoms to which they are attached to form a heterocycloalkyl optionally substituted with one, two, or three R 22 ;

R 40 is C 1 -C 20 alkyl, C 2 -C 20 alkenyl, C 2 -C 2 alkynyl, C 1 -C 20 heteroalkyl, 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, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl is independently optionally substituted with one, two, or three R 24 ;

R 41 is a glycerol ester derivative, C 1 -C 20 alkyl, C 2 -C 20 alkenyl, C 2 -C 20 alkynyl, C 1 -C 20 heteroalkyl, 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, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl is independently optionally substituted with one, two, or three R 24 ;

R 50 and R 51 are each independently hydrogen, halogen, C 1 -C 6 alkyl, C 1 -C 6 heteroalkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, C 1 -C 6 alkyl(aryl), C 1 -C 6 alky(heteroaryl), C 1 -C 6 alkyl(cycloalkyl), or C 1 -C 6 alkyl(heterocycloalkyl);

R 52 and R 53 are each independently hydrogen, halogen, C 1 -C 6 alkyl, C 1 -C 6 heteroalkyl, 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);

each R 22 is independently C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, C 1 -C 6 alkyl(aryl), C 1 -C 6 alkyl(heteroaryl), C 1 -C 6 alkyl(cycloalkyl), C 1 -C 6 alkyl(heterocycloalkyl); wherein each alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl is independently optionally substituted with one, two, or three R 23 ;

each R 23 is independently halogen, —CN, —OH, —OR a , —SH, —SR a , —S(═O)R a , —NO 2 , —NR b R c , S(═O) 2 R a , —NHS(═O) 2 R a , —S(═O) 2 NR b R c , —C(═O)R a , —C(═O)R a , —C(═O)OR b , —OC(═O)OR b , —C(═O)NR b R c , —OC(═O)NR b R c , —NR b C(═O)NR b R c , —NR b C(═O)R a , —NR b C(═O)OR b , C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 hydroxyalkyl, C 1 -C 6 heteroalkyl, cycloalkyl, or heterocycloalkyl;

each R 24 are independently halogen, —CN, —OH, —OR a , —SH, —SR a , —S(═O)R a , —NO 2 , —NR b R c , S(═O) 2 R a , —NHS(═O) 2 R a , —S(═O) 2 NR b R c , —C(═O)R a , —C(═O)R a , —C(═O)OR b , —OC(═O)OR b , —C(═O)NR b R c , —OC(═O)NR b R c , —NR b C(═O)NR b R c , —NR b C(═O)R a , —NR b C(═O)OR b , C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 hydroxyalkyl, C 1 -C 6 heteroalkyl, cycloalkyl, or heterocycloalkyl; and

v is 1, 2, 3, or 4.

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

R 4 and R 7 are each independently halogen, —OH, —OR 15 , —NR 16 S(═O) 2 R 15 , —NR 16 C(═O)R 15 , C 1 -C 6 alkyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl; wherein each alkyl, cycloalkyl; heterocycloalkyl, aryl, and heteroaryl is independently optionally substituted with one, two, or three R 20c ;

R 5 and R 6 are each hydrogen;

R 15 is C 1 -C 6 alkyl optionally substituted with one, two, or three halogen; and

R 16 is hydrogen or C 1 -C 6 alkyl optionally substituted with one, two, or three halogen; and

each R 20c is independently halogen or C 1 -C 6 alkyl.

3. The compound of claim 1 , or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof, wherein:

R 4 and R 7 are each independently halogen, —OH, —OR 15 , —NR 16 S(═O) 2 R 15 , or —NR 16 C(═O)R 15 ;

R 5 and R 6 are each hydrogen;

R 15 is C 1 -C 6 alkyl optionally substituted with one, two, or three halogen; and

R 16 is hydrogen or C 1 -C 6 alkyl optionally substituted with one, two, or three halogen.

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

R 4 and R 7 are each —OH: and

R 5 and R 6 are each hydrogen.

5. The compound of claim 1 , or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof, wherein:

R 1 and R 7 are each independently halogen, —OH, —OR 15 , —NR 16 S(═O) 2 R 15 , —NR 16 C(═O)R 15 , C 1 -C 6 alkyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl; wherein each alkyl, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl is independently optionally substituted with one, two; or three R 20c ;

R: 5 and R 6 are each independently hydrogen, halogen, C 1 -C 6 alkyl, or cycloalkyl; wherein each alkyl and cycloalkyl is independently optionally substituted with one, two, or three R 20d ;

R 15 is C 1 -C 6 alkyl optionally substituted with one, two, or three halogen;

R 16 is hydrogen or C 1 -C 6 alkyl optionally substituted with one, two, or three halogen;

each R 20c independently halogen or C 1 -C 6 alkyl; and

each R 20d is independently halogen or C 1 -C 6 alkyl.

6. The compound of claim 1 , or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof, wherein:

R 4 and R 7 are each —OH;

R 5 is halogen, C 1 -C 6 alkyl, or cycloalkyl; wherein each alkyl and cycloalkyl is independently optionally substituted with one, two, or three R 20d ;

R 6 is hydrogen; and

each R 20d is independently halogen or C 1 -C 6 alkyl.

7. The compound of claim 1 , or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof, wherein:

R 4 and R 7 are each —OH;

R 5 is hydrogen;

R 6 is halogen, C 1 -C 6 alkyl, or cycloalkyl; wherein each alkyl and cycloalkyl is independently optionally substituted with one, two, or three R 20d ; and

each R 20d is independently halogen or C 1 -C 6 alkyl.

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

R 4 is halogen, —OH, —NR 16 S(═O) 2 R 15 ,NR 16 C(═O)R 15 , C 1 -C 6 , alkyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl; wherein each alkyl, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl is independently optionally substituted with one, two, or three R 20c ;

R 7 is hydrogen;

R 5 and R 6 are each hydrogen;

R 15 is C 1 -C 6 alkyl optionally substituted with one, two, or three halogen;

R 16 is hydrogen or C 1 -C 6 alkyl optionally substituted with one, two, or three halogen; and

each R 20c is independently halogen or C 1 -C 6 alkyl.

9. The compound of claim 1 , or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof, wherein:

R 4 is —OH;

R 7 is hydrogen; and

R 5 and R 6 are each hydrogen.

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

R 7 is halogen, —OH, —NR 16 S(═O) 2 R 15 , —NR 16 C(═O)R 15 , C 1 -C 6 alkyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl; wherein each alkyl, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl is independently optionally substituted with one, two, or three R 20c ;

R 4 is hydrogen;

R 5 and R 6 are each hydrogen;

R 15 is C 1 -C 6 alkyl optionally substituted with one, two; or three halogen;

R 16 is hydrogen or C 1 -C 6 alkyl optionally substituted with one, two, or three halogen; and

each R 20c is independently halogen or C 1 -C 6 alkyl.

11. The compound of claim 1 , or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof, wherein:

R 7 is —OH;

R 4 is hydrogen; and

R 5 and R 6 are each hydrogen.

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

R 1 is C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, C 1 -C 6 alkyl(aryl), C 1 -C 6 alkyltheteroaryl), C 1 -C 6 alkyl(cycloalkyl), C 1 -Co alkyl(heterocycloalkyl), —S(═O)2R 15 , —S(═O) 2 NR 16 R 17 , or —C(═O) 2 R 15 ; wherein each alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl is independently optionally substituted with one, two, or three R 20a ;

R 2 is hydrogen;

R 15 is C 1 -C 6 alkyl, aryl; or C 1 -C 6 alkyl(aryl); wherein each alkyl and aryl is optionally substituted with one, two, or three halogen;

R 16 and R 17 are each independently hydrogen or C 1 -C 6 alkyl; wherein each alkyl is optionally substituted with one, two, or three halogen; and

each R 20a is independently halogen, —CN, —OH, —OC 1 -C 6 alkyl, C 1 -C 6 alkyl, or C 1 -C 6 haloalkyl.

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

R 1 is C 1 -C 6 alkyl, 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 20a ;

R 2 is hydrogen; and

each R 20a is independently halogen, —CN, —OH, —OC 1 -C 6 alkyl, C 1 -C 6 alkyl, or C 1 -C 6 haloalkyl.

14. The compound of claim 1 , or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof; wherein:

R 1 is C 1 -C 6 alkyl or C 1 -C 6 alkyl(aryl); wherein each alkyl and aryl is independently optionally substituted with one, two, or three R 20a ;

R 2 is hydrogen; and

each R 20a is independently halogen, —CN; —OH, —OC 1 -C 6 alkyl, C 1 -C 6 alkyl, or C 1 -C 6 haloalkyl.

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

R 1 is C 1 -C 6 alkyl or C 1 -C 6 alkyl(aryl); wherein aryl is optionally substituted with one R 20a ;

R 2 is hydrogen; and

each R 20a is independently halogen, —CN, —OH, —OC 1 -C 6 alkyl, C 1 -C 6 alkyl, or C 1 -C 6 haloalkyl.

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

each R 20a is independently halogen.

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

R 1 and R 2 are taken together with the nitrogen atom to which they are attached to form a heterocycloalkyl optionally substituted with one, two, or three R 20a ;

each R 20a is independently aryl optionally substituted with one, two, or three R 21 ; and

each R 21 is independently halogen, C 1 -C 6 alkyl or C 1 -C 6 haloalkyl.

18. The compound of claim 1 , or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof, wherein:

R 1 and R 2 are taken together with the nitrogen atom to which they are attached to form a piperidine or a pyrrolidine optionally substituted with one, two, or three R 20a ;

each R 20a is independently aryl optionally substituted with one, two, or three R 21 ; and

each R 21 is independently halogen, C 1 -C 6 alkyl, or C 1 -C 6 haloalkyl.

19. The compound of claim 1 ,

or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof, wherein:

R 1 and R 2 are taken together with the nitrogen atom to which they are attached to form a piperidine or a pyrrolidine optionally substituted with one R 20a ; and

each R 20a is independently aryl optionally substituted with one, two, or three R 21 ; and

each R 21 is independently halogen, C 1 -C 6 alkyl, or C 1 -C 6 haloalkyl.

20. The compound of claim 1 , or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof, wherein:

R 3 is halogen, —CN, SR 18 , C 1 -C 6 alkyl, 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 20b ;

R 18 is C 1 -C 6 alkyl, cycloalkyl or C alkyl(cycloalkyl); each independently optionally substituted with one, two, or three R 20g ;

each R 20b is independently halogen or C 1 -C 6 alkyl; and

each R 20g is independently halogen or C 1 -C 6 alkyl.

21. The compound of claim 1 , or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof, wherein:

R 3 is halogen, —CN, SR 18 , C 1 -C 6 alkyl, or C 1 -C 6 alkyl(cycloalkyl); wherein each alkyl, and cycloalkyl is independently optionally substituted with one, two, or three R 20b ;

R 18 is C 1 -C 6 alkyl, cycloalkyl or C 1 -C 6 alkyl(cycloalkyl); each independently optionally substituted with one, two, or three R 20g , each R 20b is independently halogen or C 1 -C 6 alkyl; and

each R 20g is independently halogen or C 1 -C 6 alkyl.

22. The compound of claim 1 , or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof, wherein:

R 3 is halogen.

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

A is —O—.

24. The compound of claim 1 , or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof, wherein:

A is —CH 2 —.

25. The compound of claim 1 , or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof, wherein:

R 30 , R 33 , and R 34 are each independently hydrogen, C 1 -C 20 alkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, C 1 -C 6 alkyl(aryl), C 1 -C 6 , alkyl(heteroaryl), C 1 -C 6 alkyl(cycloalkyl), C 1 -C 6 alkyl(heterocycloalkyl), —(CR 50 R 51 ) v OC(═O)R 40 , or —(CR 50 R 51 ) v OC(═O)OR 40 ); provided that at least one of R 30 , R 33 , or R 34 is not hydrogen.

26. The compound of claim 1 , or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof, wherein:

R 30 , R 33 , and R 34 are each independently hydrogen, C 1 -C 20 alkyl, aryl, C 1 -C 6 alkyl(aryl), C 1 -C 6 alkyl(cycloalkyl), —(CR 50 R 51 ) v OC(═O)R 40 , or —(CR 50 R 51 ) v OC(═O)OR 40 ;

provided that at least one of R 30 , R 33 , or R 34 is not hydrogen.

27. The compound of claim 1 , or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof, wherein:

R 30 , R 33 , and R 34 are each independently hydrogen, C 1 -C 20 alkyl, aryl, C 1 -C 6 alkyl(aryl), or C 1 -C 6 alkyl(cycloalkyl); provided that at least one of R 30 , R 33 , or R 34 is not hydrogen.

28. The compound of claim 1 , or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof, wherein:

R 30 is C 1 -C 6 alkyl, aryl, C 1 -C 6 alkyl(aryl), C 1 -C 6 alkyl(cycloalkyl), —(CR 50 R 51 ) v OC(═O)R 40 , or —(CR 50 R 51 ) v OC(═O)OR 40 ; and

R 33 and R 34 are each independently hydrogen, C 1 -C 6 alkyl, aryl, C 1 -C 6 alkyl(aryl), C 1 -C 6 alkyl(cycloalkyl), —(CR 50 R 51 ) v OC(═O)R 40 , or —(CR 50 R 51 ) v OC(═O)OR 40 .

29. The compound of claim 1 , or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof, wherein:

R 30 is C 1 -C 6 alkyl, aryl, C 1 -C 6 alky(aryl), or C 1 -C 6 alkyl(cycloalkyl), and

R 33 and R 34 are hydrogen or C 1 -C 6 alkyl.

30. The compound of claim 1 , or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof, wherein:

R 30 is C 1 -C 6 alkyl, aryl, C 1 -C 6 alkyl(aryl), or C 1 -C 6 alkyl(cycloalkyl); and

R 33 and R 34 are hydrogen.

31. The compound of claim 1 , or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof, wherein:

R 33 is C 1 -C 6 alkyl, aryl, C 1 -C 6 alkyl(aryl), C 1 -C 6 alkyl(cycloalkyl), —(CR 50 R 51 ) v OC(═O)R 40 , or —(CR 50 R 51 ) v OC(═O)OR 40 ; and

R 30 and R 34 are each independently hydrogen, C 1 -C 20 alkyl, aryl, C 1 -C 6 alkyl(aryl), C 1 -C 6 alkyl(cycloalkyl), —(CR 50 R 51 ) v OC(═O), or —(CR 50 R 51 ) v OC(═O)OR 40 .

32. The compound of claim 1 , or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof, wherein:

R 33 is C 1 -C 6 alkyl, aryl, C 1 -C 6 alky(aryl), or C 1 -C 6 alkyl(cycloalkyl), and

R 30 and R 34 are hydrogen or C 1 -C 6 alkyl.

33. The compound of claim 1 , or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof, wherein:

R 33 is C 1 -C 6 alkyl, aryl, C 1 -C 6 alkyl(aryl), or C 1 -C 6 alkyl(cycloalkyl); and

R 30 and R 34 are hydrogen.

34. The compound of claim 1 , or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof, wherein:

R 34 is C 1 -C 6 alkyl, aryl, C 1 -C 6 alkyl(aryl), C 1 -C 6 alkyl(cycloalkyl), —(CR 50 R 51 ) v OC(═O)R 40 , or —(CR 50 R 51 ) v OC(═O)OR 40 , and

R 33 and R 30 are each independently hydrogen, C 1 -C 20 alkyl, aryl, C 1 -C 6 alkyl(aryl), C 1 -C 6 alkyl(cycloalkyl), —(CR 50 R 51 ) v OC(═O)R 40 , or —(CR 50 R 51 ) v OC(═O)OR 40 .

35. The compound of claim 1 , or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof, wherein:

R 34 is C 1 -C 6 alkyl, aryl, C 1 -C 6 alkyl(aryl), or C 1 -C 6 alkyl(cycloalkyl); and

R 33 and R 30 are hydrogen or C 1 -C 6 alkyl.

36. The compound of claim 1 , or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof; wherein:

R 34 is C 1 -C 6 alkyl, aryl, C 1 -C 6 alkyl(aryl), or C 1 -C 6 alkyl(cycloalkyl); and

R 33 and R 30 are hydrogen.

37. The compound of claim 1 , or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof, wherein:

R 30 , R 33 , and R 34 are each independently —(CR 50 R 51 ) v OC(═O)R 40 or —(CR 50 R 51 ) v OC(═O)OR 40 .

38. A compound or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof selected from:

wherein A is —O— or —CH 2 —.

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

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

41. A method of treating cancer in a subject, comprising administering to the subject a compound of claim 1 , or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 17, 2021
From: DU, XIAOHUI; EKSTEROWICZ, JOHN; FANTIN, VALERIA R.; JACKSON, ERICA L.; SUN, DAQING; YE, QIUPING; MOORE, JARED
To: ORIC PHARMACEUTICALS, INC.
Reel/Frame 057206/0585 →
Continuity (5)
Continuation 16612108
Provisional Application 62574140 · Oct 18, 2017
Provisional Application 62504440 · May 10, 2017
Provisional Application 62504446 · May 10, 2017
Related Publication 20220054512A1 · Feb 24, 2022
Cited By (1)
US 12,454,544