Benzothiazine dioxide derivatives

Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Bacterium or component thereof or substance produced by said...

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544 49, C07D27902, A61K 3154

Patent

active

043094279

ABSTRACT:
Certain novel derivatives of N-(2-pyridyl)-2-methyl-4-hydroxy-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide have been prepared, including N-(2-pyridyl)-2-methyl-4-acetoxy-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide, N-(2-pyridyl)-2-methyl-4-(n-butyryloxy)-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide, N-(6-methyl-2-pyridyl)-2-methyl-4-acetoxy-2H-1,2-benzothiazine-3-carboxami de 1,1-dioxide, N-(2-pyridyl)-2-methyl-4-benzoyloxy-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide, N-(6-methyl-2-pyridyl)-2-methyl-4-benzoyloxy-2H-1,2-benzothiazine-3-carbox amide 1,1-dioxide, N-(2-pyridyl)-2-methyl-4-methanesulfonyloxy-2H-1,2-benzothiazine-3-carboxa mide 1,1-dioxide and N-(6-methyl-2-pyridyl)-2-methyl-4-methanesulfonyloxy-2H-1,2-benzothiazine- 3-carboxamide 1,1-dioxide. All these compounds are useful in therapy as non-steroidal anti-inflammatory agents, especially when administered by the topical route of administration. Methods for preparing these compounds from known starting materials are provided.

REFERENCES:
patent: 3591584 (1971-07-01), Lombardino
patent: 3925371 (1975-11-01), Rasmussen
patent: 4116964 (1978-09-01), Zinnes et al.
J. G. Lombardino et al., "Potent Antiinflammatory N-Heterocyclic3-Carboxamides of 4-Hydroxy-2-methyl-2H-1,2-benzothiazine 1,1-Dioxide", Journal of Medicinal Chemistry, vol. 16, No. 5, p. 493, (1973).

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