| 摘要 |
Certain novel p-aminomethylbenzoyl 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 prodrug forms of the known anti-inflammatory and analgesic oxicams. Preferred member compounds include 2-methyl-4-[4-(morpholinomethyl)benzoyloxy]-N-(2-pyridinyl)-2H-1,2-ben zothiazine-3-carboxamide 1,1-dioxide, 2-methyl-4-[4-(piperidinomethyl)benzoyloxy]-N-(2-pyridinyl)-2H-1,2-ben zothiazine-3-carboxamide 1,1-dioxide, 2-methyl-N-(6-methyl-2-pyridinyl)-4-[4-(piperidinomethyl)benzoyloxy]-2 H-1,2-benzothiazine-3-carboxamide 1,1-dioxide, 2-methyl-4-[4-(4-methylpiperazinomethyl)benzoyloxy]-N-(2-pyridinyl)-2H -1,2-benzothiazine-3-carboxamide 1,1-dioxide and 2-methyl-4-[4-(pyridiniummethyl)benzoyloxy]-N-(2-pyridinyl)-2H-1,2-ben zothiazine-3-carboxamide 1,1-dioxide chloride. Methods for preparing these compounds from known starting materials are provided.
|
