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Details for Patent: 3,976,776

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Details for Patent: 3,976,776

Title: Tranquilizer process employing N-(heteroarcyclic)piperazinylalkylazaspiroalkanediones
Abstract:The present invention concerns the class of heterocyclic carbon compounds comprised of N-(heteroarcyclic)piperazinylalkyl derivatives of azaspiroalkanediones which have potent and specific tranquilizing action and anti-emetic properties. Typical embodiments of this invention are 8-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-8-azaspiro[4.5]decane-7,9-dio ne and 8-[4-[4-(2-pyridyl)-1-piperazinyl]-butyl]-8-azaspiro[4.5]decane-7,9-dione.
Inventor(s): Wu; Yao Hua (Evansville, IN), Rayburn; James W. (Evansville, IN)
Assignee: Mead Johnson & Company (Evansville, IN)
Filing Date:Jul 14, 1975
Application Number:05/595,467
Claims:1. The process for eliciting tranquilizing effect in a mammal which comprises administering systemically to a mammal in need thereof an effective tranquilizer dose of from about 0.01 to about 40 mg./kg. of body weight of said host of a compound selected from a group consisting of compounds having the formula: ##SPC13##

wherein

n is the integer 4 or 5;

A is a divalent straight or branched alkylene chain of 2 to 6 carbon atoms inclusive and connects the nitrogen atoms as shown through at least 2 carbon atoms;

B is a heteroarcyclic represented by the symbol ##SPC14##

W and Y are independently selected from the group consisting of CH and nitrogen,

R.sup.1 and R.sup.2 are independently selected from the group consisting of hydrogen, lower alkyl from 1 to 4 carbon atoms inclusive, lower alkoxy of from 1 to 4 carbon atoms inclusive, hydroxy, amino, alkylthio of from 1 to 4 carbon atoms inclusive, halogen, trifluoromethyl, alkanoamido of 1 to 6 carbon atoms inclusive, and alkanesulfonamido of 1 to 6 carbon atoms inclusive,

and a non-toxic pharmaceutically acceptable acid addition salt thereof.

2. The process of claim 1 comprising the administration of 8-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-8-azaspiro[4.5]-decane-7,9-di one.

3. The process of claim 1 comprising the administration of 8-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-8-azaspiro[4.5]-decane-7,9-di one hydrochloride.

4. The process of claim 1 comprising the administration of 8-[4-[4-(2-pyridyl)-1-piperazinyl]butyl]-8-azaspiro[4.5]decane-7,9-dione.

5. The process of claim 1 comprising the administration of 8-[4-[4-(2-pyridyl)-1-piperazinyl]butyl]-8-azaspiro[4.5]decane-7,9-dione hydrochloride.

6. The process of claim 1 comprising the administration of 8-[2-[4-(2-pyridyl)-1-piperazinyl]ethyl]-8-azaspiro[4.5]decane-7,9-dione.

7. The process of claim 1 comprising the administration of 8-[2-[4-(2-pyridyl)-1-piperazinyl]ethyl]-8-azaspiro[4.5]decane-7,9-dione hydrochloride.

8. The process of claim 1 comprising the administration of 8-[2-[4-(2-pyrimidinyl-1-piperazinyl]ethyl]-8-azaspiro[4.5]-decane-7,9-dio ne.

9. The process of claim 1 comprising the administration of 8-[2-[4-(2-pyrimidinyl)-1-piperazinyl]ethyl]-8-azaspiro[4.5]-decane-7,9-di one hydrochloride.

10. The process of claim 1 comprising the administration of 8-[3-[4-(2-pyrimidinyl)-1-piperazinyl]propyl]-8-azaspiro[4.5]-decane-7,9-d ione.

11. The process of claim 1 comprising the administration of 8-[3-[4-(2-pyrimidinyl)-1-piperazinyl]propyl]-8-azaspiro[4.5]-decane-7,9-d ione hydrochloride.

12. The process of claim 1 comprising the administration of 8-[5-[4-(2-pyrimidinyl)-1-piperazinyl]pentyl]-8-azaspiro[4.5]-decane-7,9-d ione.

13. The process of claim 1 comprising the administration of 8-[5-[4-(2-pyrimidinyl)-1-piperazinyl]pentyl]-8-azaspiro[4.5]-decane-7,9-d ione hydrochloride.

14. The process of clam 1 comprising the administration of 8-[3-[4-(6-methoxy-2-pyridyl)-2-piperazinyl]propyl]-8-azaspiro-[4.5]decane -7,9-dione.

15. The process of clam 1 comprising the administration of 8-[3-[4-(6-methoxy-2-pyridyl)-1-piperazinyl]propyl]-8-azaspiro-[4.5]decane -7,9-dione hydrochloride.

16. The process of claim 1 comprising the administration of 3-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-3-azaspiro[5.5]-undecane-2,4- dione.

17. The process of claim 1 comprising the administration of 3-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-3-azaspiro[5.5]-undecane-2,4- dione hydrochloride.

18. The process of claim 1 comprising the administration of 8-[4-[4-(4,6-dimethyl-2-pyrimidinyl)-1-piperazinyl]butyl]-8-azaspiro[4.5]d ecane-7,9-dione.

19. The process of claim 1 comprising the administration of 8-[4-[4-(4,6-dimethyl-2-pyrimidinyl)-1-piperazinyl]butyl]-8-azaspiro[4.5]d ecane-7,9-dione hydrochloride.

20. A pharmaceutical composition in dosage unit form suitable for systemic administration to a mammalian host comprising a pharmaceutical carrier and sufficient compound to provide an effective daily dose of from 0.01 to 40 mg./kg. of body weight of said host, said compound being selected from the group consisting of compounds of the formula: ##SPC15##

wherein

n is the integer 4 or 5;

A is a divalent straight or branched alkylene chain of 2 to 6 carbon atoms inclusive and connects the nitrogen atoms as shown through at least 2 carbon atoms;

B is a heteroarcyclic represented by the symbol wherein ##SPC16##

W and Y are independently selected from the group consisting of CH and nitrogen,

R.sup.1 and R.sup.2 are independently selected from the group consisting of hydrogen, lower alkyl from 1 to 4 carbon atoms inclusive, lower alkoxy of from 1 to 4 carbon atoms inclusive, hydroxy, amino, alkylthio of 1 to 4 carbon atoms inclusive, halogen, trifluoromethyl, alkanoamido of 1 to 6 carbon atoms inclusive, and alkanesulfonamido of 1 to 6 carbon atoms inclusive,

and a non-toxic pharmaceutically acceptable acid addition salt thereof.

21. The composition of claim 20 containing 8-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-8-azaspiro[4.5]decane-7,9-dio ne.

22. The composition of claim 20 containing 8-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-8-azaspiro[4.5]decane-7,9-dio ne hydrochloride.

23. The composition of claim 20 containing 8-[4-[4-(2-pyridyl)-1-piperazinyl)]butyl]-8-azaspiro[4.5]decane-7,9-dione.

24. The composition of claim 20 containing 8-[4-[4-(2-pyridyl)-1-piperazinyl)]butyl]-8-azaspiro[4.5]decane-7,9-dione hydrochloride.

25. The composition of claim 20 containing 8-[4-[4-(2-pyridyl)-1-piperazinyl]ethyl]-8-azaspiro[4.5]decane-7,9-dione.

26. The composition of claim 20 containing 8-[2-[4-(2-pyridyl)-1-piperazinyl]ethyl]-8-azaspiro[4.5]decane-7,9-dione hydrochloride.

27. The composition of claim 20 containing 8-[2-[4-(2-pyrimidinyl)-1-piperazinyl]ethyl]-8-azaspiro[4.5]decane-7,9-dio ne.

28. The composition of claim 20 containing 8-[2-[4-(2-pyrimidinyl)-1-piperazinyl]ethyl]-8-azaspiro[4.5]decane-7,9-dio ne hydrochloride.

29. The composition of claim 20 containing 8-[3-[4-(2-pyrimidinyl)-1-piperazinyl]propyl]-8-azaspiro[4.5]decane-7,9-di one.

30. The compositon of claim 20 containing 8-[3-[4-(2-pyrimidinyl)-1-piperazinyl]propyl]-8-azaspiro[4.5]decane-7,9-di one hydrochloride.

31. The composition of claim 20 containing 8-[5-[4-(2-pyrimidinyl)-1-piperazinyl]pentyl]-8-azaspiro[4.5]decane-7,9-di one.

32. The composition of claim 20 containing 8-[5-[4-(2-pyrimidinyl)-1-piperazinyl]pentyl]-8-azaspiro[4.5]decane-7,9-di one hydrochloride.

33. The composition of claim 20 containing 8-[3-[4-(6-methoxy-2-pyridyl)-1-piperazinyl]propyl]-8-azaspiro[4.5]decane- 7.9-dione.

34. The composition of claim 20 containing 8-[3-[4-(6-methoxy-2-pyridyl)-1-piperazinyl]propyl]-8-azaspiro[4.5]decane- 7,9-dione hydrochloride.

35. The composition of claim 20 containing 3-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-3-azaspiro[5.5]undecane-2,4-d ione.

36. The composition of claim 20 containing 3-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-3-azaspiro[5.5]undecane-2,4-d ione hydrochloride.

37. The composition of claim 20 containing 8-[4-[4-(4,6-dimethyl-2-pyrimidinyl)-1-piperazinyl]butyl]-8-azaspiro[4.5]- decane-7,9-dione.

38. The composition of claim 20 containing 8-[4-[4-(4,6-dimethyl-2-pyrimidinyl)-1-piperazinyl]butyl]-8-azaspiro[4.5]- decane-7,9-done hydrochloride.
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