| 摘要 |
<p>N-(2-Pyridyl)-4- acyloxy-2-methyl -2H-1,2- benzothiazine-3- carboxamide 1,1-dioxide derivs. of formula (I) are new (where R is 2-9C alkanoyl, benzoyl, toluoyl, thenoyl, furoyl, lower alkanesulphonyl or benzenesulphonyl; and R1 is H or CH3). - 7 Cpds. (I), e.g. N-(2-pyridyl)-2 -methyl-4- acetoxy-2H-1,2- benzothiazine-3 -carboxamide 1,1-dioxide and N-(6-methyl-2-pyridyl)-2 -methyl-4- methanesulphonyloxy- 2H-1,2- benzothiazine-3-carboxamide 1,1-dioxide are specifically claimed. - (I) are antiinflammatories, esp. active topically. Pref. doses are 0.16-16 mg/kg/day, by oral, parenteral or topical routes. Higher blood levels are obtd. after topical admin. than those of the 4-hydroxy-2H-1,2-benzothiazine-3-carboxamido 1,1-dioxides of US 3591584 (including piroxicam). EPAB- EP--57059 B Pharmaceutically active cpds have formula (I), where Q is R, are pref. produced by reacting a cpd. (I), where Q is H, with an acyl halide RX. In the formula R is 2-9C alkanoyl, benzoyl, toluoyl, furoyl, thenoyl, 1-6C alkane- or benzenesulphonyl; R' is H or Me. - (I) are highly effective anti-inflammatory agents esp. suitable for topical administration. (11pp)</p> |
