IP Library › Granted Patent US 11,542,278
Granted Patent B1
US 11,542,278 · App. 17/514,877 · Granted Jan 3, 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.
C07D498/22A61P35/00C07D513/22
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Quick Facts
Patent No.
US 11,542,278
App. No.
17/514,877
Granted
Jan 3, 2023
Kind
B1
Abstract

Disclosed are heterocyclic heteroaromatic macrocyclic ether compounds of Formula (I): pharmaceutically acceptable salts of the compounds and pharmaceutical compositions thereof. The disclosure further relates to methods of treating or preventing cancer using the heterocyclic heteroaromatic macrocyclic ether compounds, pharmaceutically acceptable salts of the compounds and pharmaceutical compositions thereof.

Claims (72)

1. A compound of Formula (I):

or a pharmaceutically acceptable salt, enantiomer, or tautomer thereof,

wherein:

Q is CH;

Z is CR 5 ;

X is:

wherein:

* indicates the point of attachment of X to the —CH 2 — group bonded to Y;

Y is:

wherein:

* indicates the point of attachment of Y to the —CH 2 — group bonded to X;

R 1 is H, CH 3 , or CH 2 OH;

each R 2 is independently H, halo, C 1-4 alkyl, C 1-4 haloalkyl, CH 2 —C 3-4 cycloalkyl, OC 1-4 alkyl, C 3-6 cycloalkyl, or C 3-6 heterocycloalkyl;

R 3 is H, halo, CN, C 1-4 alkyl, C 1-4 haloalkyl, or OC 1-4 alkyl;

R 4 is H or F; and

R 5 is H or F.

2. A compound of Formula (I-B):

or a pharmaceutically acceptable salt thereof,

wherein:

Q is CH;

Z is CR 5 ;

X is:

wherein:

* indicates the point of attachment of X to the —CH 2 — group bonded to Y;

Y is:

wherein:

* indicates the point of attachment of Y to the —CH 2 — group bonded to X;

R 1 is H, CH 3 , or CH 2 OH;

each R 2 is independently H, halo, C 1-4 alkyl, C 1-4 haloalkyl, CH 2 —C 3-4 cycloalkyl, OC 1-4 alkyl, C 3-6 cycloalkyl, or C 3-6 heterocycloalkyl;

R 3 is H, halo, CN, C 1-4 alkyl, C 1-4 haloalkyl, or OC 1-4 alkyl;

R 4 is H or F; and

R 5 is H or F.

3. The compound of claim 2 , or a pharmaceutically acceptable salt thereof, wherein each R 2 is independently H, Cl, CH 3 , CH 2 CH 3 , CH 2 CH(CH 3 ) 2 , CHF 2 , CF 3 , CH 2 CH 2 F, CH 2 CHF 2 , CH 2 -cyclopropyl, OCH 3 , cyclopropyl, cyclobutyl, or oxetanyl.

4. The compound of claim 2 , or a pharmaceutically acceptable salt thereof, wherein R 3 is H, F, Cl, CN, CH 3 , or H 2 CH 3 .

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

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

7. The compound of claim 2 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

8. The compound of claim 2 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

9. The compound of claim 2 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

10. The compound of claim 2 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

11. The compound of claim 2 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

12. The compound of claim 2 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

13. The compound of claim 2 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

14. The compound of claim 2 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

15. The compound of claim 2 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

16. The compound of claim 2 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

17. The compound of claim 2 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

18. The compound of claim 2 , wherein the compound is:

or a pharmaceutically acceptable salt thereof.

19. A pharmaceutical composition comprising (i) a pharmaceutically acceptable carrier or excipient, and (ii) the compound of claim 7 , or a pharmaceutically acceptable salt thereof.

20. A pharmaceutical composition comprising (i) a pharmaceutically acceptable carrier or excipient, and (ii) the compound of claim 8 , or a pharmaceutically acceptable salt thereof.

21. A pharmaceutical composition comprising (i) a pharmaceutically acceptable carrier or excipient, and (ii) the compound of claim 9 , or a pharmaceutically acceptable salt thereof.

22. A pharmaceutical composition comprising (i) a pharmaceutically acceptable carrier or excipient, and (ii) the compound of claim 10 , or a pharmaceutically acceptable salt thereof.

23. A pharmaceutical composition comprising (i) a pharmaceutically acceptable carrier or excipient, and (ii) the compound of claim 11 , or a pharmaceutically acceptable salt thereof.

24. A pharmaceutical composition comprising (i) a pharmaceutically acceptable carrier or excipient, and (ii) the compound of claim 12 , or a pharmaceutically acceptable salt thereof.

25. A pharmaceutical composition comprising (i) a pharmaceutically acceptable carrier or excipient, and (ii) the compound of claim 13 , or a pharmaceutically acceptable salt thereof.

26. A pharmaceutical composition comprising (i) a pharmaceutically acceptable carrier or excipient, and (ii) the compound of claim 14 , or a pharmaceutically acceptable salt thereof.

27. A pharmaceutical composition comprising (i) a pharmaceutically acceptable carrier or excipient, and (ii) the compound of claim 15 , or a pharmaceutically acceptable salt thereof.

28. A pharmaceutical composition comprising (i) a pharmaceutically acceptable carrier or excipient, and (ii) the compound of claim 16 , or a pharmaceutically acceptable salt thereof.

29. A pharmaceutical composition comprising (i) a pharmaceutically acceptable carrier or excipient, and (ii) the compound of claim 17 , or a pharmaceutically acceptable salt thereof.

30. A pharmaceutical composition comprising (i) a pharmaceutically acceptable carrier or excipient, and (ii) the compound of claim 18 , or a pharmaceutically acceptable salt thereof.

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 12, 2022
From: TANG, XINXING
To: PHARMARESOURCES CO., LTD.
Reel/Frame 061402/0244 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 12, 2022
From: PHARMARESOURCES CO., LTD.
To: NUVALENT, INC.
Reel/Frame 061402/0248 →
CORRECTIVE ASSIGNMENT TO CORRECT THE REMOVE INVENTOR XINXING TANG PREVIOUSLY RECORDED AT REEL: 059813 FRAME: 0545. 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 061664/0718 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 4, 2022
From: TANG, XINXING; HORAN, JOSHUA COURTNEY; MENTE, SCOT RICHARD; PELISH, HENRY EFREM; SHAIR, MATTHEW D.; TANGPEERACHAIKUL, ANUPONG
To: NUVALENT, INC.
Reel/Frame 059813/0545 →
Priority Claims (1)
CN PCT/CN20/88590 · May 5, 2020 · national
Continuity (2)
Continuation PCTUS2021030842 · May 5, 2021
Provisional Application 63125733 · Dec 15, 2020
Cited By (2)
US 12,275,742 US 12,630,560