Pyrido-benzothiazine derivatives having high antibacterial activ

Details Pyrido-benzothiazine derivatives having high antibacterial activ Pyrido-benzothiazine derivatives having high antibacterial activ

1988-09-30

1990-05-08

Raymond, Richard L.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

544 32, A61K 3154, C07D51306

Patent

active

049238590

ABSTRACT:
Pyrido-benzothiazine derivatives having the following general formula: ##STR1## in which R is H or a C.sub.1 -C.sub.6 alkyl or a C.sub.1 -C.sub.6 fluoroalkyl, and R.sub.1 is N-alkyl-3-pyrrolidinalkylamine with C.sub.1 to C.sub.6 alkyls or ##STR2## where R.sub.2 is a S.sub.1 -C.sub.6 alkyl or a C.sub.2 -C.sub.6 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.

REFERENCES:
patent: 4571396 (1986-02-01), Hutt et al.
patent: 4684647 (1987-08-01), Mascellani et al.
Dauchi Seiyaku Co. Chemical Abstracts, vol. 98(1983) 198294p.
Otsuka Pharm. Co., Chemical Abstracts, vol. 101(1984) 151868u.
Cecchetti et al., Chemical Abstracts, vol. 106(1987) 102235e.
Terni et al., Chemical Abstracts, vol. 109(1988) 129034.

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