Last Updated: May 10, 2026

Claims for Patent: 4,959,366


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Summary for Patent: 4,959,366
Title:Anti-arrhythmic agents
Abstract:A series of [N-alkyl-N-(nitro-, alkylsulphonamido, or amino-phenalkyl)amino]-alkyl, alkoxy or alkylthio phenyl derivatives having utility as anti-arrhythmic agents.
Inventor(s):Peter E. Cross, Geoffrey N. Thomas, John E. Arrowsmith
Assignee: Pfizer Corp SRL , Pfizer Inc
Application Number:US07/044,086
Patent Claims: 1. A compound of the formula: ##STR73## or a pharmaceutically acceptable salt thereof; whereinRa is --NO2, --NH2 or --NHSO2 R1 where R1 is a C1 -C4 alkyl group; Rb is --NO2, --NH2 or R3 where R3 is --NHSO2 (C1 -C4 alkyl) or --CONR4 R5 where R4 and R5 are each independently H or C1 -C4 alkyl or together with the nitrogen atom to which they are attached represent a 1-pyrrolidinyl, piperidino, morpholino or N-methylpiperazin-1-yl group; with the proviso that when one of Ra and Rb is --NO2, then the other is not --NH2 ; X is O or S absent; Y is an ethylene group optionally substituted by a methyl group; "alk" is an ethylene, trimethylene or tetramethylene group, "alk" being optionally substituted by a methyl group; R is C1 -C4 alkyl; and R2 is H, halo, CF3 or C1 -C4 alkyl.

2. A compound of the formula: ##STR74## or a pharmaceutically acceptable salt thereof; whereR and R1 are each independently C1 -C4 alkyl; X is O or S absent; Y is an ethylene group optionally substituted by a methyl group; "alk" is an ethylene, trimethylene and tetramethylene group, "alk" being optionally substituted by a methyl group; R2 is H, halo, CF or C1 -C4 alkyl; and R3 is a group of the formula --NHSO2 (C1 -C4 alkyl) or --CONR4 R5 where R4 and R5 are each independently H or C1 -C4 alkyl or together with the nitrogen atom to which they are attached represent a 1-pyrrolidinyl, piperidino, morpholino or N-methylpiperazin-1-yl group.

3. A compound according to claim 2 wherein R1 is methyl.

4. A compound according to claim 2 wherein R is methyl or ethyl.

5. A compound according to claim 3 wherein R is methyl or ethyl.

6. A compound according to claim 5 wherein R is methyl.

7. A compound according to claim 2 wherein X is O.

8. A compound according to claim 3 wherein X is O.

9. A compound according to claim 4 wherein X is O.

10. A compound according to claim 5 wherein X is O.

11. A compound according to claim 6 wherein X is O.

12. A compound according to claim 2 wherein Y is --(CH2)2 --.

13. A compound according to claim 3 wherein Y is --(CH2)2 --.

14. A compound according to claim 4 wherein Y is --(CH2)2 --.

15. A compound according to claim 5 wherein Y is --(CH2)2 --.

16. A compound according to claim 6 wherein Y is --(CH2)2 --.

17. A compound according to claim 7 wherein Y is --(CH2)2 --.

18. A compound according to claim 8 wherein Y is --(CH2)2 --.

19. A compound according to claim 9 wherein Y is --(CH2)2 --.

20. A compound according to claim 10 wherein Y is --(CH2)2 --.

21. A compound according to claim 11 wherein Y is --(CH2)2 --.

22. A compound according to claim 2 wherein R2 is H, Cl or CH3.

23. A compound according to claim 3 wherein R2 is H, Cl or CH3.

24. A compound according to claim 4 wherein R2 is H, Cl or CH3.

25. A compound according to claim 5 wherein R2 is H, Cl or CH3.

26. A compound according to claim 6 wherein R2 is H, Cl or CH3.

27. A compound according to claim 7 wherein R2 is H, Cl or CH3.

28. A compound according to claim 8 wherein R2 is H, Cl or CH3.

29. A compound according to claim 9 wherein R2 is H, Cl or CH3.

30. A compound according to claim 10 wherein R2 is H, Cl or CH3.

31. A compound according to claim 11 wherein R2 is H, Cl or CH3.

32. A compound according to claim 12 wherein R2 is H, Cl or CH3.

33. A compound according to claim 13 wherein R2 is H, Cl or CH3.

34. A compound according to claim 14 wherein R2 is H, Cl or CH3.

35. A compound according to claim 15 wherein R2 is H, Cl or CH3.

36. A compound according to claim 16 wherein R2 is H, Cl or CH3.

37. A compound according to claim 17 wherein R2 is H, Cl or CH3.

38. A compound according to claim 18 wherein R2 is H, Cl or CH3.

39. A compound according to claim 19 wherein R2 is H, Cl or CH3.

40. A compound according to claim 20 wherein R2 is H, Cl or CH3.

41. A compound according to claim 21 wherein R2 is H, Cl or CH3.

42. A compound according to claim 2 wherein R2 is H.

43. A compound according to claim 2 wherein R3 is NHSO2 CH3, --CONH2, CON(C2 H5)2 or ##STR75##

44. A compound according to claim 43 wherein R3 is --NHSO2 CH3.

45. A compound of the formula: ##STR76##

46. A compound according to claim 2 wherein Y is --(CH2)2 --and X is O or S.

47. A pharmaceutical composition comprising an anti-arrhythmic effective amount of a compound of claim 2 in combination with a pharmaceutically acceptable diluent or carrier.

48. A method of treating cardiac arrhythmia comprising administering to an arrhythmic host in need of such treatment an anti-arrhythmic effective dose of a compound of claim 2 in combination with a pharmaceutically acceptable diluent or carrier.

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