Anti-inflammatory benzo- and thieno-1,2-thiazine-3-carboxamide 1

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

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544 48, 544 49, A61K 3138, C07D27902, C07D51304

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active

046109820

ABSTRACT:
Certain novel 2-acetoxybenzoyl and ring-substituted .alpha.-arylpropionyl derivatives of 4-hydroxy-2-methyl-N-(2-pyridinyl)-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide and several other closely-related known oxicams have been prepared. These particular compounds are useful in therapy as non-steroidal anti-arthritic agents. Typical member compounds include 4-(2-acetoxybenzoyloxy)-2-methyl-N-(2-pyridinyl)-2H-1,2-benzothiazine-3-ca rboxamide 1,1-dioxide, 4-[.alpha.-(4-isobutylphenyl)propionyloxy]-2-methyl-N-(2-pyridinyl)-2H-1,2 -benzothiazine-3-carboxyamide N-(2-pyridinyl)-2H-1,2-benzothiazine-3-carboxyamide 1,1-dioxide, 4-[.alpha.-(3-benzoylphenyl)propionyloxy]-2-methyl-N-(2-pyridinyl)-2H-1,2- benzothiazine-3-carboxamide 1,1-dioxide, "d-4-[.alpha.-6-methoxynaphth-2-yl)propionyloxy]-2-methyl-N-(2-pyridinyl)- 2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide" to -- d-4-[.alpha.-(6-methoxynaphth-2-yl)propionyloxy]-2-methyl-N-(2-pyridinyl)- 2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide.

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J. G. Lombardino et al., "Potent Antiinflammatory N-Heterocyclic 3-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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