Pyrido-benzothiazine derivatives having high antibacterial activity and high bioavailability to tissues
US4923859A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Sep 30, 1988 |
| Grant date | May 8, 1990 |
| Priority date | — |
| Expiry date | Sep 30, 2008 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61P31/04
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.