US 2007/0191356 A1 · Pyridobenzoxazine derivative

Abstract

A quinolone antimicrobial agent having potent antimicrobial activity against gram positive and gram negative bacteria and having high safety is provided. A compound represented by the following formula (1): [Chemical formula 1] [wherein, R1: hydrogen, alkyl, cycloalkyl, or substituted carbonyl derived from amino acid, peptide or tripeptide; R2: hydrogen, alkyl, or cycloalkyl; R3: hydrogen, amino, halogen, or alkyl; R4: hydrogen, phenyl, acetoxymethyl, pivaloyloxymethyl, ethoxycarbonyl, choline, dimethylaminoethyl, 5-indanyl, phthalidinyl, 5-alkyl-2-oxo-1,3-dioxol-4-ylmethyl, 3-acetoxy-2-oxobutyl, alkyl, alkoxymethyl, or phenylalkyl; X, X1, X2: hydrogen or halogen] or salt thereof, or a hydrate thereof; and antimicrobial agent and therapeutic agent for infections, each containing the compound, salt thereof or a hydrate thereof.

Claims37

Dependent claims

A compound represented by the following formula (1):

[wherein, R1 represents a hydrogen atom, an alkyl group having from 1 to 6 carbon atoms or a cycloalkyl group having from 3 to 6 carbon atoms, or a substituted carbonyl group derived from an amino acid, dipeptide or tripeptide, with the proviso that the alkyl group may have, as the substituent, at least one group selected from the group consisting of a hydroxyl group, an amino group, halogen atoms, alkylthio groups having from 1 to 6 carbon atoms, and alkoxy groups having from 1 to 6 carbon atoms;
R2 represents a hydrogen atom, an alkyl group having from 1 to 6 carbon atoms or a cycloalkyl group having from 3 to 6 carbon atoms, with the proviso that the alkyl group may have, as the substituent, at least one group selected from the group consisting of a hydroxyl group, an amino group, halogen atoms, alkylthio groups having from 1 to 6 carbon atoms, and alkoxy groups having from 1 to 6 carbon atoms;
R3 represents a hydrogen atom, amino group, halogen atom or alkyl group having from 1 to 6 carbon atoms, with the proviso that the amino group may have, as the substituent, one or two groups selected from the group consisting of a formyl group, alkyl groups having from 1 to 6 carbon atoms and acyl groups having from 2 to 6 carbon atoms;
R4 represents a hydrogen atom, phenyl group, acetoxymethyl group, pivaloyloxymethyl group, ethoxycarbonyl group, choline group, dimethylaminoethyl group, 5-indanyl group, phthalidinyl group, 5-alkyl-2-oxo-1,3-dioxol-4-ylmethyl group, 3-acetoxy-2-oxobutyl group, alkyl group having from 1 to 6 carbon atoms, alkoxymethyl group having from 2 to 7 carbon atoms, or a phenylakyl group composed of an alkylene group having from 1 to 6 carbon atoms and a phenyl group;
X1 and X2 each independently represents a hydrogen atom or halogen atom, and
X represents a hydrogen atom or a halogen atom], salt thereof, or a hydrate thereof.

3 more elements

A compound represented by the following formula (3):

[wherein, R11 represents a hydrogen atom, an alkyl group having from 1 to 6 carbon atoms or a cycloalkyl group having from 3 to 6 carbon atoms, or an amino-protecting group, or a substituted carbonyl group derived from an amino acid, dipeptide or peptide having an amino group which is unsubstituted or may be protected, with the proviso that the alkyl group may have, as the substituent, at least one group selected from the group consisting of a hydroxyl group, an amino group, halogen atoms, alkylthio groups having from 1 to 6 carbon atoms and alkoxy groups having from 1 to 6 carbon atoms;
R2 has the same meaning as defined in the formula (1);
and
Q′ means an amino-protecting group or hydrogen atom], salt thereof, or a hydrate thereof.

1 more element

Dependencies are inferred from the claim text.

Pyridobenzoxazine derivative

Life of this patent

Pyridobenzoxazine derivative

Life of this patent

Abstract

Claims37