EP0047005B1
Expired / Lapsed
EP
⏱️ 0.0 years remaining
Benzoxazine derivatives
Assignee: Daiichi Pharmaceutical Co Ltd
•
Filing: 1981-08-28
•
Granted: 1984-11-14
•
Expires: 2001-08-28
Abstract
Abstract Pyrido[1,2,3-de][1,4]benzoxazine derivatives are described having the formula (I) <IMAGE> (I) 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 C/O Daiichi Seiyaku Laboratories Hayakawa
- 👤 Tokiyuki Daiichi Seiyaku Laboratories Hiramitsu
- 👤 Yoshiaki C/O Daiichi Seiyaku Laboratories Tanaka
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-31 19:57
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
118 words
Benzoxazine derivatives of the general formula I 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 monoethylamino, monomethylamino, diethylamino, dimethylamino, hydrazyl, methylhydrazyl, azetidinyl, pyrrolidinyl, piperidinyl, morpholinyl, pyrazolidinyl, piperazinyl and homopiperazinyl, in which the alkyl radicals and heterocycles may be further substituted by one or more substituents selected from the group consisting of a hydroxy group, an alkyl group having from 1 to 6 carbon atoms, an amino group, a hydroxyalkyl group having from 1 to 6 carbon atoms, and a monoalkylamino and a dialkylamino group having from 1 to 6 carbon atoms in each alkyl moiety and the pharmaceutically acceptable salts thereof.
Claim 2
Dependent Claim
118 words
Benzoxazine derivatives of the general formula I 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 monoethylamino, monomethylamino, diethylamino, dimethylamino, hydrazyl, methylhydrazyl, azetidinyl, pyrrolidinyl, piperidinyl, morpholinyl, pyrazolidinyl, piperazinyl and homopiperazinyl, in which the alkyl radicals and heterocycles may be further substituted by one or more substituents selected from the group consisting of a hydroxy group, an alkyl group having from 1 to 6 carbon atoms, an amino group, a hydroxyalkyl group having from 1 to 6 carbon atoms, and a monoalkylamino and a dialkylamino group having from 1 to 6 carbon atoms in each alkyl moiety and the pharmaceutically acceptable salts thereof.
Claim 3
Dependent Claim
37 words
A benzoxazine derivative which is 9 - fluoro - 3 - methyl - 7 - oxo - 10 - (4 - thiamorpholinyl) - 2,3 - dihydro - 7H - pyrido[1,2,3 - de][1,4]benzoxazine - 6 - carboxylic acid.
Claim 4
Dependent Claim
37 words
A benzoxazine derivative which is 9 - fluoro - 3 - methyl - 7 - oxo - 10 - (4 - thiamorpholinyl) - 2,3 - dihydro - 7H - pyrido[1,2,3 - de][1,4]benzoxazine - 6 - carboxylic acid.
Claim 5
Dependent Claim
14 words
A compound according to claim 1, wherein R is methyl and Z is 4-methyl-1-piperazinyl.
Claim 6
Dependent Claim
15 words
A compound according to claim 1, wherein R is methyl and Z is 4-hydroxy-1 -piperazinyl.
Claim 7
Dependent Claim
14 words
A compound according to claim 1, wherein R is methyl and Z is 3-hydroxy-1-pyrrolidinyl.
Claim 8
Dependent Claim
14 words
A compound according to claim 1, wherein R is methyl and Z is homopiperazinyl.
Claim 9
Dependent Claim
39 words
Process for preparing the compounds of claim 1 to 6 charracterized in that a 9,1 0-dihalo-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de] [1,4]benzoxazine-6-carboxylic acid or its 3-alkyl derivative is reacted with an amine corresponding to the substituent Z at a temperature from 30°C to 200°C.
Claim 10
Dependent Claim
21 words
Process according to claim 7, characterized in that the reaction is carried out at a temperature of from 70°C to 150°C.
Claim 11
Dependent Claim
12 words
Pharmaceutical composition comprising at least one compound of claims 1 to 6.
References Cited (Backward Citations)
No citation records indexed.
USPTO Annuity & Maintenance Windows
Maintenance schedule is calculated for granted US utility patents.