Benzothiazine dioxide derivatives

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 417/12 (2006.01) A61K 31/54 (2006.01) A61K 31/55 (2006.01) C07C 229/38 (2006.01) C07D 213/20 (2006.01) C07D 295/155 (2006.01) C07D 417/14 (2006.01)

Patent

CA 1270485

BENZOTHIAZINE DIOXIDE DERIVATIVES Abstract Certain novel p-aminomethylbenzoyl derivatives of 4-hydroxy-2-methyl-N-(2-pyridinyl)-2H-1,2-benzo- thiazine-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-benzothiazine-3-carboxamide 1,1- dioxide, 2-methyl-4-[4-(piperidinomethyl)benzoyloxy]- N-(2-pyridinyl)-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide, 2-methyl-N-(6-methyl-2-pyridinyl)-4-[4- (piperidinomethyl)benzoyloxy]-2H-1,2-benzothiazine- 3-carboxamide 1,1-dioxide, 2-methyl-4-[4-(4-methyl- piperazinomethyl)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-benzothiazine-3-carboxamide 1,1-dioxide chloride. Methods for preparing these compounds from known starting materials are provided.

510033

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