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Benzoxazine derivatives

Assignee: Daiichi Pharmaceutical Co Ltd
•
Filing: 1981-09-02
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Granted: 1983-05-10
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Expires: 2001-09-02
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Abstract

Abstract Pyrido[1,2,3-de][1,4]benzoxazine derivatives are described having the formula (I) ##STR1## wherein X is a halogen atom, R is a hydrogen atom or an alkyl group of 1 to 6 carbon atoms and Z represents mono-substituted, di-substituted or cyclic-substituted amino group which may contain a hetero atom and may have a substituent such as hydroxyl, alkyl having 1 to 6 carbon atoms, amino, hydroxyalkyl having 1 to 6 carbon atoms or mono- or di-alkylamino having 1 to 6 carbon atoms in each alkyl moiety and the pharmaceutically acceptable salt thereof, having antibacterial activity.

Inventors

  • 👤 Isao Hayakawa
  • 👤 Tokiyuki Hiramitsu
  • 👤 Yoshiaki Tanaka

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-04 05:49
CPC Classifications
C; C07; C07D; C07D498/00; C07D498/02; C07D498/04; C07C; C07C205/00; C07C205/27; C07C205/35; C07C205/36; C07C205/37; A; A61; A61P; A61P31/00; A61P31/04; C07D265/00; C07D265/28; C07D265/34; C07D265/36; C07D498/06

Claims Analysis

Total Claims: 11
Claim 1
Independent Claim 107 words
A compound having the formula (I) ##STR7## wherein X is a halogen atom, R is a hydrogen atom or an alkyl group having from 1 to 6 carbon atoms and Z represents (1) a mono-alkylamino or di-alkylamino group or (2) a cyclicamino group selected from the group consisting of azetidinyl, pyrrolidinyl, piperdinyl, morpholinyl, piperidinyl, homopiperazinyl, thiamorpholinyl and pyrazolidinyl, each of which amino groups may be substituted with a hydroxyl group, an alkyl group having 1 to 6 carbon atoms, an amino group, a hydroxyalkyl group having 1 to 6 carbon atoms or a mono- or di-alkylamino group having 1 to 6 carbon atoms in each alkyl group.
Claim 2
Dependent Claim 107 words
A compound having the formula (I) ##STR7## wherein X is a halogen atom, R is a hydrogen atom or an alkyl group having from 1 to 6 carbon atoms and Z represents (1) a mono-alkylamino or di-alkylamino group or (2) a cyclicamino group selected from the group consisting of azetidinyl, pyrrolidinyl, piperdinyl, morpholinyl, piperidinyl, homopiperazinyl, thiamorpholinyl and pyrazolidinyl, each of which amino groups may be substituted with a hydroxyl group, an alkyl group having 1 to 6 carbon atoms, an amino group, a hydroxyalkyl group having 1 to 6 carbon atoms or a mono- or di-alkylamino group having 1 to 6 carbon atoms in each alkyl group.
Claim 3
Dependent Claim 130 words
A compound having the formula (I) ##STR8## wherein X is a halogen atom, R is a hydrogen atom or an alkyl group having from 1 to 6 carbon atoms and Z represents (1) a mono-alkylamino or di-alkylamino group having 1 to 6 carbon atoms in each alkyl group which may be substituted with a hydroxyl group or an amino (-NH 2 ) group, or (2) a cyclicamino group selected from the group consisting of azetidinyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, homopiperazinyl, thiamorpholinyl and pyrazolidinyl, each of which cyclic-amino group may be substituted with a hydroxyl group, an alkyl group having 1 to 6 carbon atoms, an amino group, a hydroxyalkyl group having 1 to 6 carbon atoms or a di-alkylamino group having 1 to 6 carbon atoms in each alkyl group.
Claim 4
Dependent Claim 130 words
A compound having the formula (I) ##STR8## wherein X is a halogen atom, R is a hydrogen atom or an alkyl group having from 1 to 6 carbon atoms and Z represents (1) a mono-alkylamino or di-alkylamino group having 1 to 6 carbon atoms in each alkyl group which may be substituted with a hydroxyl group or an amino (-NH 2 ) group, or (2) a cyclicamino group selected from the group consisting of azetidinyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, homopiperazinyl, thiamorpholinyl and pyrazolidinyl, each of which cyclic-amino group may be substituted with a hydroxyl group, an alkyl group having 1 to 6 carbon atoms, an amino group, a hydroxyalkyl group having 1 to 6 carbon atoms or a di-alkylamino group having 1 to 6 carbon atoms in each alkyl group.
Claim 5
Dependent Claim 47 words
A compound as in claim 1, wherein Z represents a mono-substituted amino group selected from monoethylamino and monomethylamino, a di-substituted amino group selected from diethylamino and dimethylamino, and a cyclic-substituted amino group comprising a 4- to 7-membered ring selected from azetidinyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl and homopiperazinyl.
Claim 6
Dependent Claim 14 words
A compound as in claim 1, wherein R is methyl and Z is 4-methyl-1-piperazinyl.
Claim 7
Dependent Claim 14 words
A compound as in claim 1, wherein R is methyl and Z is 4-hydroxy-1-piperazinyl.
Claim 8
Dependent Claim 14 words
A compound as in claim 1, wherein R is methyl and Z is 3-hydroxy-1-pyrrolidinyl.
Claim 9
Dependent Claim 14 words
A compound as in claim 1, wherein R is methyl and Z is homopiperazinyl.
Claim 10
Dependent Claim 4 words
The compound 9-fluoro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzoxazine-6-carboxylic acid.
Claim 11
Dependent Claim 4 words
The compound 9-fluoro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzoxazine-6-carboxylic acid.

References Cited (Backward Citations)

US3883522A Cited
US3984548A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1986-05-09 1986-11-08 1987-05-10 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1990-05-09 1990-11-08 1991-05-10 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1994-05-09 1994-11-08 1995-05-10 $7700.00 Window Closed / Lapsed

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