IP Library Granted Patent US 10,329,299
Granted Patent B2
US 10,329,299 · App. 15/794,816 · Granted Jun 25, 2019

Heterocyclic compounds and uses thereof

Inventors: Alfredo C. Castro (Woburn, MA); Catherine A. Evans (Somerville, MA); Somarajannair Janardanannair (Woburn, MA); Andre Lescarbeau (Somerville, MA); Tao Liu (Wellesley, MA); Martin R. Tremblay (Melrose, MA)
Assignee: Infinity Pharmaceuticals, Inc.
C07D487/04C07D401/12C07D401/14C07D403/12C07D403/14C07D417/14C07D471/04C07D471/08
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Quick Facts
Patent No.
US 10,329,299
App. No.
15/794,816
Granted
Jun 25, 2019
Kind
B2
Abstract

Provided herein are compounds of Formula (I″) or (A″), pharmaceutical compositions comprising the compounds, and methods of use thereof. The compounds provided herein modulate kinase activity, including PI3 kinase activity, and are useful for treating diseases and conditions associated with kinase activity, including PI3 kinase activity.

Claims (54)

1. A compound of Formula (I″):

wherein:

R 1 is hydrogen, alkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, or —COR 2 ;

B is hydrogen, alkyl, cycloalkyl, or aryl;

wherein R 2 is hydrogen;

R 1c is hydrogen, alkyl, alkenyl, or alkynyl;

R 2c is hydrogen, alkyl, alkenyl, or alkynyl;

W d is:

 wherein

X 1 , X 2 and X 3 are each independently C, CR 13 , or N; and

R 10 , R 11 , R 12 , and R 13 are each independently hydrogen, unsubstituted alkyl, or amino;

X is N;

wherein each alkyl, alkenyl, or alkynyl is optionally substituted with one or more halo, OH, alkoxy, NH 2 , NH(alkyl), N(alkyl) 2 , C(O)H, CO(alkyl), COOH, COO(alkyl), CONH 2 , CONH(alkyl), CON(alkyl) 2 , S(O)(alkyl), S(O) 2 (alkyl), cycloalkyl, heterocycloalkyl, aryl or heteroaryl;

wherein each cycloalkyl, heterocycloalkyl, aryl or heteroaryl is optionally substituted with one or more halo, alkyl, alkenyl, alkynyl, OH, alkoxy, oxo, NH 2 , NH(alkyl), N(alkyl) 2 , C(O)H, CO(alkyl), COOH, COO(alkyl), CONH 2 , CONH(alkyl), CON(alkyl) 2 , S(O)(alkyl), or S(O) 2 (alkyl);

or a pharmaceutically acceptable salt, hydrate, solvate, stereoisomer, or mixture of stereoisomers thereof.

2. The compound of claim 1 , wherein the compound is a compound of Formula (I′):

or a pharmaceutically acceptable salt, hydrate, solvate, stereoisomer, or mixture of stereoisomers thereof.

3. The compound of claim 2 , wherein the compound is a compound of Formula (I):

or a pharmaceutically acceptable salt, hydrate, or solvate thereof.

4. The compound of claim 1 , wherein

R 1 is branched alkyl, 6-membered aryl, 5- or 6-membered heteroaryl, 5- or 6-membered cycloalkyl, or 5- to 6-membered heterocycloalkyl,

 cyclopropyl, or methyl,

wherein R A is OH, alkoxy, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl;

x is 1, 2, 3, 4, 5, or 6; and

R 7 , R 8 , and R 9 are each, independently, hydrogen, OH, alkoxy, NH 2 , NH(alkyl), N(alkyl) 2 , cycloalkyl, heterocycloalkyl, aryl, or heteroaryl.

5. The compound of claim 4 , wherein

R 1 is: methyl,

6. The compound of claim 1 , wherein R 1 is a 5- to 10-membered heteroaryl.

7. The compound of claim 6 , wherein R 1 is a 6-membered heteroaryl.

8. The compound of claim 7 , wherein R 1 is a pyridinyl or pyrimidinyl.

9. The compound of claim 6 , wherein R 1 is a 5-membered heteroaryl.

10. The compound of claim 9 , wherein R 1 is a thiazolyl, pyrazolyl, or imidazolyl.

11. The compound of claim 6 , wherein the heteroaryl is substituted with one or more alkyl.

12. The compound of claim 1 , wherein B is aryl or cycloalkyl.

13. The compound of claim 12 , wherein B is aryl or 3- to 6-membered cycloalkyl.

14. The compound of claim 13 , wherein B is phenyl substituted with 0, 1, 2, or 3 occurrence(s) of R Z , wherein each instance of R Z is independently halo or alkyl.

15. The compound of claim 14 , wherein B is unsubstituted phenyl.

16. The compound of claim 13 , wherein B is

17. The compound of claim 1 , wherein W d is

18. The compound of claim 1 , wherein W d is

wherein one of X 1 and X 2 is C and the other is N.

19. The compound of claim 1 , wherein W d is

wherein X 3 is N or CR 13 .

20. The compound of claim 1 , wherein W d is

wherein one of X 1 and X 2 is N and the other is CR 13 .

21. The compound of claim 1 , wherein the compound is a compound of formula IV, VII, VIII, X, or XI:

or a pharmaceutically acceptable salt, hydrate, solvate, stereoisomer, or mixture of stereoisomers thereof.

22. The compound of claim 1 , wherein the compound is in an (S)-stereochemical configuration.

23. The compound of claim 1 , wherein the compound is the S-enantiomer having an enantiomeric purity greater than 75%.

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

25. A compound, which is

or a pharmaceutically acceptable salt, hydrate, or solvate thereof.

26. A compound, which is

or a pharmaceutically acceptable salt, hydrate, or solvate thereof.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 21, 2024
From: INFINITY PHARMACEUTICALS, INC.
To: TWELVE THERAPEUTICS, INC.
Reel/Frame 069193/0925 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 8, 2018
From: CASTRO, ALFREDO C.; EVANS, CATHERINE A.; JANARDANANNAIR, SOMARAJANNAIR; LESCARBEAU, ANDRE; LIU, TAO; TREMBLAY, MARTIN R.
To: INFINITY PHARMACEUTICALS, INC.
Reel/Frame 044875/0841 →
Continuity (6)
Division 14695699 · Apr 24, 2015
Continuation 14506429 · Oct 3, 2014
Provisional Application 61938026 · Feb 10, 2014
Provisional Application 61888958 · Oct 9, 2013
Provisional Application 61887259 · Oct 4, 2013
Related Publication 20180044346A1 · Feb 15, 2018
Cited By (2)
US 12,384,792 US 12,410,170