Claims for Patent: 3,674,876

Summary for Patent: 3,674,876

Title:	Benzothiazine dioxides as lipid regulating agents
Abstract:	Certain 3,4-dihydro-4-oxo-2H-1,2-benzothiazine-3-carboxamide1,1-dioxide and 3-oxo-2H-1,2-benzothiazine-4-carboxamide-1,1dioxide compounds effective as lipid regulating agents are disclosed.
Inventor(s):	Joseph G Lombardino, Gerald F Holland
Assignee:	Pfizer Corp Belgium , Pfizer Corp SRL
Application Number:	US831768A
Patent Claims:	2. The method of claim 1 wherein said compound is a 3,4-dihydro-4-oxo-2H-1,2-benzothiazine-3-carboxamide-1,1-dioxide having the first formula wherein R is -NHR2. 3. The method of claim 2 wherein said compound is a 3,4-dihydro-4-oxo-2H-1,2-benzothiazine-3-carboxamide-1,1-dioxide wherein X and Y are each hydrogen, Z is oxygen, R2 is phenyl and R3 is alkyl of from one to six carbon atoms. 4. The method of claim 2 wherein said compound is a 3,4-dihydro-4-oxo-2H-1,2benzothiazine3-carboxamide-1,1-dioxide wherein X and Y are each hydrogen, Z is sulfur, R2 is phenyl and R3 is alkyl of from one to six carbon atoms. 5. The method of claim 2 wherein said compound is a 3,4-dihydro-4-oxo-2H-1,2benzothiazine-3-carboxamide-1,1-dioxide wherein X and Y are each hydrogen, Z is oxygen, R2 is chlorophenyl and R3 is alkyl of from one to six carbon atoms. 6. The method of claim 2 wherein said compound is a 3,4-dihydro-4-oxo-2H-1,2-benzothiazine-3-carboxamide-1,1dioxide wherein X and Y are each hydrogen, Z is oxygen, R2 is phenylalkyl having up to three carbon atoms in the alkyl moiety and R3 is alkyl of from one to six carbon atoms. 7. The method of claim 2 wherein said compound is a 3,4-dihydro-4-oxo-2H-1,2-benzothiazine-3-carboxamide-1,1-dioxide wherein X and Y are each hydrogen, Z is oxygen, R2 is alkenyl having up to six carbon atoms and R3 is alkyl of from one to six carbon atoms. 8. The method of claim 2 wherein said compound is a 3,4-dihydro-4-oxo-2H-1,2-benzothiazine-3-carboxamide-1,1-dioxide wherein X and Y are each hydrogen, Z is oxygen, R2 is cycloalkyl having up to eight carbon atoms and R3 is alkyl of from one to six carbon atoms. 9. The method of claim 2 wherein said compound is a 3,4-dihydro-4-oxo-2H-1,2-benzothiazine-3-carboxamide-1,1dioxide wherein X and Y are each hydrogen, Z is oxygen, R2 is dichlorophenyl and R3 is alkyl of from one to six carbon atoms. 10. The method of claim 2 wherein said compound is a 3,4-dihydro-4-oxo-2H-1,2-benzothiazine-3-carboxamide-1,1-dioxide wherein X and Y are each hydrogen, Z is oxygen, R2 is chlorophenyl and R3 is hydrogen. 11. The method of claim 2 wherein said compound is a 3,4-dihydro-4-oxo-2H-1,2-benzothiazine-3-carboxamide-1,1-dioxide wherein X and Y are each hydrogen, Z is oxygen, R2 is 2-thiazolyl and R3 is alkyl of from one to six carbon atoms. 12. The method of claim 2 wherein said compound is a 3,4-dihydro-4-oxo-2H-1,2-benzothiazine-3-carboxamide-1,1-dioxide wherein X and Y are each hydrogen, Z is oxygen, R2 is pyridyl and R3 is alkyl of from one to six carbon atoms. 13. The method of claim 2 wherein said compound is a 3,4-dihydro-4-oxo-2H-1,2-benzothiazine-3-carboxamide-1,1-dioxide wherein X and Y are each hyDrogen, Z is oxygen, R2 is monomethyl 2-pyridyl and R3 is alkyl of from one to six carbon atoms. 14. The method of claim 1 wherein said compound is a 3,4-dihydro-4-oxo-2H-1,2-benzothiazine-3-carboxylate-1,1-dioxide having the first formula wherein R is OR1 and Z is oxygen. 15. The method of claim 14 wherein said compound is a 3,4-dihydro-4-oxo-2H-1,2-benzothiazine-3-carboxylate-1,1-dioxide wherein X and Y are each hydrogen, R1 is alkyl having from one to 12 carbon atoms and R3 is alkyl of from one to six carbon atoms. 16. The method of claim 14 wherein said compound is a 3,4-dihydro-4-oxo-2H-1,2-benzothiazine-3-carboxylate-1,1dioxide wherein X and Y are hydrogen, R1 is alkyl having from one to 12 carbon atoms and R3 is hydrogen. 17. The method of claim 1 wherein said compound is a 3,4-dihydro-3-oxo-2H-1,2-benzothiazine-4-carboxamide-1,1-dioxide having the second formula wherein R is -NHR2. 18. The method of claim 17 wherein said compound is a 3,4-dihydro-3-oxo-2H-1,2-benzothiazine-4-carboxamide-1,1-dioxide wherein X and Y are each hydrogen, Z is oxygen, R2is phenyl and R3 is alkyl of from one to six carbon atoms. 19. The method of claim 17 wherein said compound is a 3,4-dihydro-3-oxo-2H-1,2-benzothiazine-4-carboxamide-1,1-dioxide wherein X and Y are each hydrogen, Z is oxygen, R2 is chlorophenyl and R3 is alkyl of from one to six carbon atoms. 20. The method of claim 17 wherein said compound is a 3,4-dihydro-3-oxo-2H-1,2-benzothiazine-4-carboxamide-1,1-dioxide wherein X and Y are each hydrogen, Z is oxygen, R2 is pyridyl and R3 is alkyl of from one to six carbon atoms. 21. The method of claim 17 wherein said compound is a 3,4-dihydro-3-oxo-2H-1,2-benzothiazine-4-carboxamide-1,1-dioxide wherein X and Y are each hydrogen, Z is oxygen, R2 is dichlorophenyl and R3 is alkyl having from one to six carbon atoms. 22. The method of claim 17 wherein said compound is a 3,4-dihydro-3-oxo-2H-1,2-benzothiazine-4-carboxamide-1,1-dioxide wherein X and Y are each hydrogen, Z is oxygen, R2 is bromophenyl and R3 is alkyl of from one to six carbon atoms. 23. The method of claim 17 wherein said compound is a 3,4-dihydro-3-oxo-2H-1,2-benzothiazine-4-carboxamide-1,1-dioxide wherein X and Y are each hydrogen, Z is oxygen, R2 is naphthyl and R3 is alkyl of from one to six carbon atoms. 24. The method of claim 17 wherein said compound is a 3,4-dihydro-3-oxo-2H-1,2-benzothiazine-4-carboxamide-1,1-dioxide wherein X and Y are each hydrogen, Z is oxygen, R2 is alkyl having from one to eight carbon atoms and R3 is alkyl of from one to six carbon atoms. 25. The method of claim 17 wherein said compound is a 3,4-dihydro-3-oxo-2H-1,2-benzothiazine-4-carboxamide-1,1-dioxide wherein X is hydrogen, Y is alkyl having from one to five carbon atoms, Z is oxygen, R2 is dichlorophenyl and R3 is alkyl of from one to six carbon atoms. 26. The method of claim 17 wherein said compound is a 3,4-dihydro-3-oxo-2H-1,2-benzothiazine-4-carboxamide-1,1-dioxide wherein X is hydrogen, Y is alkyl having from one to five carbon atoms, Z is oxygen, R2 is bromophenyl and R3 is alkyl of from one to six carbon atoms. 27. The method of claim 17 wherein said compound is a 3,4-dihydro-3-oxo-2H-1,2-benzothiazine-4-carboxamide-1,1-dioxide wherein X and Y are each hydrogen, Z is oxygen, R2 is phenyl and R3 is phenylalkyl having up to three carbon atoms in the alkyl moiety. 28. The method of claim 17 wherein said compound is a 3,4-dihydro-3oxo-2H-1,2-benzothiazine-4-carboxamide-1,1-dioxide wherein X and Y are each hydrogen, Z is oxygen, R2 is 2-thiazolyl and R3 is alkyl of from one to six carbon atoms. 29. The method of claim 1 wherein said compound is a 3,4-dihydro-3-oxo-2H-1,2-benzothiazine-4-carboxylate-1,1-dioxide having the second formula wherein R is OR1 and Z is oxygen. 30. The method of claim 29 wherein said compound is a 3,4-dihydro-3-oxo-2H-1,2-benzothiazine-4-carboxylate-1,1-dioxide wherein X and Y are each hydrogen, R1 is alkyl having from one to 12 carbon atoms and R3 is alkyl of from one to six carbon atoms. 31. The method of claim 17 wherein said compound is 3,4-dihydro-4''-ethoxy-2-methyl-3-oxo-2H-1,2-benzothiazine-4-carboxanilide -1, 1-dioxide. 32. The method of claim 17 wherein said compound is 2-benzyl-4''-chloro-3,4-dihydro-3-oxo-2H-1,2-benzothiazine-4-carboxanilide-1, 1-dioxide. 33. The method of claim 2 wherein said compound is 2,2'',5''-trimethyl-4''-nitro-4-hydroxy-2H-1,2-benzothiazine-3-carboxanilide -1,1-dioxide. 34. The method of claim 17 wherein said compound is 2-benzyl-2'', 4''-dichloro-3,4-dihydro-3-oxo-2H-1,2-benzothiazine-4-carboxanilide-1,1 -dioxide. 35. The method of claim 2 wherein said compound is 4-hydroxy-2-methyl-N-(6-methyl-2-benzothiazolyl)-2H-1,2-benzothiazine-3 -carboxamide-1,1-dioxide. 36. The method of claim 2 wherein said compound is N-(6-bromo-2-benzothiazolyl)-4-hydroxy-2-methyl-2H-1,2-benzothiazine-3 -carboxamide-1,1-dioxide.