Process for preparing pyrido-benzothiazine derivatives having high antibacterial activity and high bioavailability to tissues
US5066802A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Dec 7, 1989 |
| Grant date | Nov 19, 1991 |
| Priority date | — |
| Expiry date | Dec 7, 2009 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61P31/04
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
A process for preparing 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 C.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 process for the preparation of derivatives of formula (I) starts with a first reaction cycle starting from 2,4-difluoro-3-chloronitrobenzene. Said derivatives possess a high antibacterial activity 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.