Pyrido-benzothiazine derivatives having the following general formula:
in which R is H or a C1-C6 alkyl or a C1-C6 fluoroalkyl, and R1 is N-alkyl-3-pyrrolidinalkylamine with C1 to C6 alkyls or
where R2 is a C1-C6 alkyl or a C2-Cs alkenyl or an arylalkyl group, possibly substituted by halogen, hydroxy or keto-groups, both in the racemic form and in the optically active form.
The invention also comprises the process for the preparation of derivatives of formula (I) starting from 2.4-difluoro-3-chloronitrobenzene.
Said derivatives possess a high antibacterial acitvity as well as a high bioavailability to tissues; the invention also refers to pharmaceutical compositions containing them as active components.
具有以下通式的
吡啶-苯并
噻嗪衍
生物:
其中 R 是 H 或 C1-C6 烷基或 C1-C6 氟烷基,R1 是具有 C1 至 C6 烷基的 N-烷基-3-
吡咯烷基胺或
其中 R2 是 C1-C6 烷基或 C2-Cs 烯基或芳烷基,可能被卤素、羟基或酮基取代,既可以是外消旋形式,也可以是光学活性形式。
本发明还包括以 2.4-二
氟-3-
氯硝基苯为起始原料制备式 (I) 衍
生物的工艺。
上述衍
生物具有很强的抗菌能力和对组织的高
生物利用度;本发明还涉及含有这些衍
生物作为活性成分的药物组合物。