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Last Updated: March 27, 2025

Claims for Patent: 5,053,407

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Summary for Patent: 5,053,407

Title:	Optically active pyridobenzoxazine derivatives and anti-microbial use
Abstract:	An optically action pyridobenzoxazine derivative, a process for preparing the same and a novel intermediate useful for preparing the optically active pyridobenzoxazine derivative are disclosed. The optically active pyridobenzoxazine derivative possesses increased antimicrobial activity and reduced toxicity. The intermediate is useful for preparing such optically active pyridobenzoxazine derivatives such as Ofloxacin and anolog compounds.
Inventor(s):	Hayakawa; Isao (Tokyo, JP), Atarashi; Shohgo (Tokyo, JP), Imamura; Masazumi (Tokyo, JP), Yokohama; Shuichi (Tokyo, JP), Higashihashi; Nobuyuki (Tokyo, JP), Sakano; Katsuichi (Tokyo, JP), Ohshima; Masayuki (Tokyo, JP)
Assignee:	Daiichi Pharmaceutical Co., Ltd. (Tokyo, JP)
Application Number:	06/876,623
Patent Claims:	1. An S(-)-pyridobenzoxazine compound represented by the formula (VI) ##STR9## wherein X.sub.1 represents a halogen atom, R.sub.1 represents an alkyl group having 1 to 4 carbon atoms, and R.sub.3 represents an alkyl group having 1 to 3 carbon atoms. 2. S(-)-9-Fluoro-3-methyl-10 -(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzoxa zine-6-carboxylic acid according to claim 1. 3. S(-)-9-Fluoro-3-methyl-10-(4-ethyl-1-pipe razinyl)-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzoxazine-6-carboxylic acid according to claim 1. 4. A process for treating a patient in need of an antimicrobial therapy which comprises administering to said patient an antimicrobially effective amount of an S(-)-pyridobenzoxazine compound represented by the formula (VI) ##STR10## wherein X.sub.1 represents a halogen atom, R.sub.1 represents an alkyl group having 1 to 4 carbon atoms, and R.sub.3 represents an alkyl group having 1 to 3 carbon atoms. 5. A process for treating a patient in need of an antimicrobial therapy as in claim 4 which comprises administering to said patient an antimicrobially effective amount of S(-)-9-Fluoro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H-py rido[1,2,3-de][1,4]benzoxazine-6-carboxylic acid. 6. A process for treating a patient in need of an antimicrobial therapy as in claim 4 which comprises administering to said patient an antimicrobially effective amount of S(-)-9-Fluoro-3-methyl-10-(4-ethyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H-pyr ido[1,2,3-de][1,4]benzoxazine-6-carboxylic acid.

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