IP Library › Granted Patent US 11,667,649
Granted Patent B2
US 11,667,649 · App. 17/524,169 · Granted Jun 6, 2023

Heteroaromatic macrocyclic ether chemotherapeutic agents

Inventors: Joshua Courtney Horan (Somerville, MA); Xinxing Tang (Pudong, CN); Scot Richard Mente (Arlington, MA); Henry Efrem Pelish (Newton, MA); Matthew D. Shair (Lexington, MA); Anupong Tangpeerachaikul (Quincy, MA)
Assignee: Nuvalent, Inc.
C07D491/22
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Quick Facts
Patent No.
US 11,667,649
App. No.
17/524,169
Granted
Jun 6, 2023
Kind
B2
Abstract

Disclosed are heterocyclic heteroaromatic macrocyclic ether compounds, pharmaceutically acceptable salts of the compounds and pharmaceutical compositions thereof. Also disclosed are methods of treating or preventing cancer using the heterocyclic heteroaromatic macrocyclic ether compounds, pharmaceutically acceptable salts of the compounds, and pharmaceutical compositions thereof.

Claims (55)

1. A compound of Formula (I), or an enantiomer, a mixture of enantiomers, or a tautomer thereof, or a pharmaceutically acceptable salt thereof:

wherein

Q is CH;

Z is CR 5 ;

X is a 5-membered heteroarylene selected from the group consisting of

wherein * indicates the point of attachment of X to the methylene group bonded to X and Y;

Y is a 5- membered heteroarylene selected from the group consisting of

wherein * indicates the point of attachment of Y to the methylene group bonded to X and Y;

R 1 is selected from the group consisting of H, methyl, and hydroxymethyl;

each instance of R 2 is independently selected from the group consisting of H, CN, halo, C 1-4 alkoxy, C 1-4 alkyl, halo-C 1-4 alkyl, C 3-4 cycloalkylmethyl, C 3-6 cycloalkyl, and C 3-6 heterocyclyl;

each instance of R 3 is independently selected from the group consisting of H, halo, CN, C 1-4 alkoxy, halo-C 1-4 alkyl, and C 1-4 alkyl; and

each of R 4 and R 5 is independently H or F.

2. The compound of claim 1 , which is a compound of Formula (I-B):

or a pharmaceutically acceptable salt thereof.

3. The compound of claim 2 or a pharmaceutically acceptable salt thereof, wherein each instance of R 2 is independently selected from the group consisting of H, chloro, fluoro, CN, methyl, ethyl, isopropyl, methoxy, trifluoromethyl, 2-fluoroethyl, difluoromethyl, 2,2-difluoroethyl, 2,2,2-trifluoroethyl, cyclopropylmethyl, cyclopropyl, cyclobutyl, and oxetanyl.

4. The compound of claim 2 or a pharmaceutically acceptable salt thereof, wherein each instance of R 3 is independently selected from the group consisting of H, fluoro, chloro, bromo, CN, methoxy, difluoromethyl, trifluoromethyl, methyl, and ethyl.

5. The compound of claim 4 or a pharmaceutically acceptable salt thereof, wherein R 4 is F.

6. The compound of claim 2 , which is:

or a pharmaceutically acceptable salt thereof.

7. The compound of claim 2 , which is:

or a pharmaceutically acceptable salt thereof.

8. The compound of claim 2 , which is:

or a pharmaceutically acceptable salt thereof.

9. The compound of claim 2 , which is:

or a pharmaceutically acceptable salt thereof.

10. The compound of claim 2 , which is:

or a pharmaceutically acceptable salt thereof.

11. The compound of claim 2 , which is:

or a pharmaceutically acceptable salt thereof.

12. The compound of claim 2 , which is:

or a pharmaceutically acceptable salt thereof.

13. The compound of claim 2 , which is:

or a pharmaceutically acceptable salt thereof.

14. The compound of claim 2 , which is:

or a pharmaceutically acceptable salt thereof.

15. The compound of claim 2 , which is:

or a pharmaceutically acceptable salt thereof.

16. The compound of claim 2 , which is:

or a pharmaceutically acceptable salt thereof.

17. The compound of claim 2 , which is:

or a pharmaceutically acceptable salt thereof.

18. A pharmaceutical composition, comprising the compound of claim 1 or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier or excipient.

19. A pharmaceutical composition, comprising the compound of claim 6 or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier or excipient.

20. A pharmaceutical composition, comprising the compound of claim 7 or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier or excipient.

21. A pharmaceutical composition, comprising the compound of claim 8 or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier or excipient.

22. A pharmaceutical composition, comprising the compound of claim 9 or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier or excipient.

23. A pharmaceutical composition, comprising the compound of claim 10 or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier or excipient.

24. A pharmaceutical composition, comprising the compound of claim 11 or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier or excipient.

25. A pharmaceutical composition, comprising the compound of claim 12 or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier or excipient.

26. A pharmaceutical composition, comprising the compound of claim 13 or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier or excipient.

27. A pharmaceutical composition, comprising the compound of claim 14 or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier or excipient.

28. A pharmaceutical composition, comprising the compound of claim 15 or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier or excipient.

29. A pharmaceutical composition, comprising the compound of claim 16 or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier or excipient.

30. A pharmaceutical composition, comprising the compound of claim 17 or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier or excipient.

31. The compound of claim 4 or a pharmaceutically acceptable salt thereof, wherein R 5 is H.

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 12, 2022
From: TANG, XINXING
To: PHARMARESOURCES CO., LTD.
Reel/Frame 061402/0279 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 12, 2022
From: PHARMARESOURCES CO., LTD.
To: NUVALENT, INC.
Reel/Frame 061402/0288 →
CORRECTIVE ASSIGNMENT TO CORRECT THE REMOVE ASSIGNOR XINXING TAN INTHE ASSIGNMENT DOCUMENT PREVIOUSLY RECORDED AT REEL: 059235 FRAME: 0922. ASSIGNOR(S) HEREBY CONFIRMS THE ASSIGNMENT. Recorded Oct 12, 2022
From: HORAN, JOSHUA COURTNEY; MENTE, SCOT RICHARD; PELISH, HENRY EFREM; SHAIR, MATTHEW D.; TANGPEERACHAIKUL, ANUPONG
To: NUVALENT, INC.
Reel/Frame 061664/0733 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 11, 2022
From: HORAN, JOSHUA COURTNEY; MENTE, SCOT RICHARD; PELISH, HENRY EFREM; SHAIR, MATTHEW D.; TANG, XINXING; TANGPEERACHAIKUL, ANUPONG
To: NUVALENT, INC.
Reel/Frame 059235/0922 →
Priority Claims (1)
WO PCT/CN2020/088589 · May 5, 2020 · international
Continuity (5)
Continuation PCTUS2021030940 · May 5, 2021
Provisional Application 63125747 · Dec 15, 2020
Provisional Application 63060331 · Aug 3, 2020
Related Publication 20220098212A1 · Mar 31, 2022
Related Publication 20220340586A9 · Oct 27, 2022
Cited By (2)
US 12,275,742 US 12,630,560