IP Library Granted Patent US 11,731,938
Granted Patent B2
US 11,731,938 · App. 17/645,723 · Granted Aug 22, 2023

Ultra short acting anti-arrhythmic agents

Inventors: John Somberg (Lake Forest, IL); Robert J Chorvat (Chadds Ford, PA)
Assignee: Academic Pharmaceuticals Inc
C07C317/28
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Quick Facts
Patent No.
US 11,731,938
App. No.
17/645,723
Granted
Aug 22, 2023
Kind
B2
Abstract

Some aspects provide novel dofetilide derivatives and pharmaceutical compositions containing the same that are useful as pharmaceutical agents in the treatment of supraventricular and ventricular arrhythmias.

Claims (72)

1. A compound of Formula I-VI or a stereoisomer thereof:

Formula

#

Formula

I

II

III

IV

V

VI

wherein:

R is selected from H, C 1-6 alkyl, C 3-6 alkenyl, and C 3-6 alkynyl;

R′ is selected from C 1-3 alkyl and —COCH 3 ;

provided that when the compound is of formula I, R′ is also selected from —CH 2 C 6 H 5 ,

provided that when the compound is of formula VI, R′ is selected from C 1-3 alkyl;

Y, at each occurrence, is independently selected from CH 3 , CH 2 CH 3 , CH 2 CH 2 CH 3 , and CH(CH 3 ) 2 ;

Z is selected from H, C 1-6 alkyl, CH 2 OH, CH(CH 3 )OH, C(CH 3 ) 2 OH, and (CH 2 ) n -phenyl;

n, at each occurrence, is independently selected from 0 and 1,

m is selected from 0 and 1; and,

p is selected from 1 and 2;

or a pharmaceutically acceptable salt thereof.

2. A compound of claim 1 , wherein the compound is of Formula I or a stereoisomer or pharmaceutically acceptable salt thereof:

wherein:

R is selected from H, C 1-6 alkyl, C 3-6 alkenyl, and C 3-6 alkynyl;

R′ is selected from H, C 1-6 alkyl, —CH 2 C 6 H 5 , and —COCH 3 ;

Y, at each occurrence, is independently selected from CH 3 , CH 2 CH 3 , CH 2 CH 2 CH 3 , and CH(CH 3 ) 2 ; and,

p is selected from 1 and 2.

3. A compound of claim 2 , wherein the compound is of Formula I-A or a stereoisomer or pharmaceutically acceptable salt thereof:

4. A compound of claim 1 , wherein the compound is of Formula II or a stereoisomer or pharmaceutically acceptable salt thereof:

wherein:

R is selected from H, C 1-6 alkyl, C 3-6 alkenyl, and C 3-6 alkynyl;

R′ is selected from C 1-3 alkyl and —COCH 3 ;

Z is selected from H, C 1-6 alkyl, CH 2 OH, CH(CH 3 )OH, C(CH 3 ) 2 OH, and (CH 2 ) n -phenyl;

Y, at each occurrence, is independently selected from CH 3 , CH 2 CH 3 , CH 2 CH 2 CH 3 , and CH(CH 3 ) 2 ; and,

p is selected from 1 and 2.

5. A compound of claim 4 , wherein the compound is of Formula II-A or a stereoisomer or pharmaceutically acceptable salt thereof:

6. A compound of claim 1 , wherein the compound is of Formula III or a stereoisomer or pharmaceutically acceptable salt thereof:

wherein:

R is selected from H, C 1-6 alkyl, C 3-6 alkenyl, and C 3-6 alkynyl;

R′ is selected from H, C 1-3 alkyl, and —COCH 3 ;

Y, at each occurrence, is independently selected from CH 3 , CH 2 CH 3 , CH 2 CH 2 CH 3 , and CH(CH 3 ) 2 ;

m is selected from 0 and 1; and,

n, at each occurrence, is independently selected from 0 and 1.

7. A compound of claim 6 , wherein the compound is of Formula III-A or a stereoisomer or pharmaceutically acceptable salt thereof:

8. A compound of claim 1 , wherein the compound is of Formula IV or a stereoisomer or pharmaceutically acceptable salt thereof:

wherein:

R is selected from H, C 1-6 alkyl, C 3-6 alkenyl, and C 3-6 alkynyl;

R′ is selected from H, C 1-3 alkyl, and —COCH 3 ; and, Y, at each occurrence, is independently selected from CH 3 , CH 2 CH 3 , CH 2 CH 2 CH 3 , and CH(CH 3 ) 2 .

9. A compound of claim 8 , wherein the compound is of Formula IV-A or a stereoisomer or pharmaceutically acceptable salt thereof:

10. A compound of claim 8 , wherein the compound is of Formula IV-B or a stereoisomer or pharmaceutically acceptable salt thereof:

11. A compound of claim 8 , wherein the compound is of Formula IV-C or a stereoisomer or pharmaceutically acceptable salt thereof:

12. A compound of claim 1 , wherein the compound is of Formula V or a stereoisomer or pharmaceutically acceptable salt thereof:

wherein:

R is selected from H, C 1-6 alkyl, C 3-6 alkenyl, and C 3-6 alkynyl;

R′ is selected from H, C 1-3 alkyl, and —COCH 3 ;

Z is selected from H, C 1-6 alkyl, CH 2 OH, CH(CH 3 )OH C(CH 3 ) 2 OH, and (CH 2 ) n -phenyl;

Y, at each occurrence, is independently selected from CH 3 , CH 2 CH 3 , CH 2 CH 2 CH 3 , and CH(CH 3 ) 2 .

13. A compound of claim 12 , wherein the compound is of Formula V-A or a stereoisomer or pharmaceutically acceptable salt thereof:

14. A compound of claim 12 , wherein the compound is of Formula V-B or a stereoisomer or pharmaceutically acceptable salt thereof:

15. A compound of claim 12 , wherein the compound is of Formula V-C or a stereoisomer or pharmaceutically acceptable salt thereof:

16. A compound of claim 1 , wherein the compound is of Formula VI or a stereoisomer or pharmaceutically acceptable salt thereof:

wherein:

R is selected from H, C 1-6 alkyl, C 3-6 alkenyl, and C 3-6 alkynyl;

R′ is selected from C 1-3 alkyl;

Y, at each occurrence, is independently selected from CH 3 , CH 2 CH 3 , CH 2 CH 2 CH 3 , and CH(CH 3 ) 2 ;

m is selected from 0 and 1; and,

n is selected from 0 and 1.

17. A compound of claim 16 , wherein the compound is of Formula VI-A or a stereoisomer or pharmaceutically acceptable salt thereof:

18. A compound of claim 16 , wherein the compound is of Formula VI-B or a stereoisomer or pharmaceutically acceptable salt thereof:

19. A compound of claim 16 , wherein the compound is of Formula VI-C or a stereoisomer or pharmaceutically acceptable salt thereof:

20. A pharmaceutical composition, comprising: a therapeutically effective amount of a compound of claim 1 or a stereoisomer or pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.

21. A method of terminating or blocking the occurrence of an arrhythmia, comprising: administering to a patient in need thereof a therapeutically effective amount of a compound of claim 1 or a stereoisomer or pharmaceutically acceptable salt thereof, wherein the arrhythmia is selected from: paroxysmal atrial tachycardia, junctional ectopic tachycardia, atrial flutter, atrial fibrillation, atrial tachycardia, ventricular tachycardia, junctional tachycardia, and ventricular fibrillation.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 15, 2022
From: SOMBERG, JOHN; CHORVAT, ROBERT J
To: ACADEMIC PHARMACEUTICALS INC
Reel/Frame 058666/0900 →
Continuity (2)
Provisional Application 63199436 · Dec 28, 2020
Related Publication 20220213032A1 · Jul 7, 2022
Cited By (1)
US 12,258,309