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Details for Patent: 5,723,648

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Details for Patent: 5,723,648

Title: Intermediates for anti-microbial benzoheterocyclic compounds
Abstract:Novel 4-oxoquinoline-3-carboxylic acid compounds of the formula: ##STR1## wherein R.sup.1 is cyclopropyl which may have 1 to 3 substituents of alkyl and halogen; phenyl which may be substituted by 1 to 3 substituents of alkoxy, halogen and OH; alkyl which may be substituted by halogen, alkanoyloxy or OH; alkenyl; or thienyl, R.sup.2 is 5- to 9-membered saturated or unsaturated heterocyclic ring which may be sustituted, R.sup.3 is alkyl, R is H or alkyl, and X is halogen, and pharmaceutically acceptable salts thereof, said compounds having excellent antimicrobial activity and hence being useful as an antimicrobial agent, and a pharmaceutical composition containing said compound as an active ingredient.
Inventor(s): Ueda; Hiraki (Mishima, JP), Miyamoto; Hisashi (Tokushima, JP), Yamashita; Hiroshi (Tokushima, JP), Tone; Hitoshi (Itano, JP)
Assignee: Otsuka Pharmaceutical Company, Limited (Tokyo-to, JP)
Filing Date:Jul 05, 1996
Application Number:08/676,034
Claims:1. A compound of the formula: ##STR36## wherein X is a halogen atom, R.sup.3 is a lower alkyl group; R.sup.2' is a halogen atom or a 5- to 9-membered saturated or unsaturated heterocyclic group that may be substituted; E is a halogen atom;

and

D is a group of the formula: ##STR37## wherein R.sup.5 is a group of the formula: --COR.sup.10 (R.sup.10 is a lower alkyl group) or a group of the formula: --COOR.sup.11 (R.sup.11 is a lower alkyl group), R.sup.6 is a lower alkyl group, R.sup.7 is a group of the formula: --NR.sup.12 R.sup.13 (R.sup.12 and R.sup.13 are each a lower alkyl group) or a lower alkoxy group, R.sup.1 is a cyclopropyl group that may be substituted by 1 to 3 of substituents selected from the group consisting of a lower alkyl group and a halogen atom, a phenyl group that may be substituted by 1 to 3 of substituents selected from the group consisting of a lower alkoxy group, a halogen atom and a hydroxy group, a lower alkyl group that may be substituted by a halogen atom, a lower alkanoyloxy group or a hydroxy group, a lower alkenyl group, or a thienyl group.

2. A compound according to claim 1, which is a member selected from the group consisting of

diethyl 2-methyl-3,4,6-trifluorobenzoylmalonate;

ethyl 2-(2-methyl-3,4,6-trifluorobenzoyl)-3-ethoxyacrylate;

ethyl 2-(2-methyl-3,4,6-trifluorobenzoyl)-3-cyclopropylaminoacrylate;

diethyl 4,6-dibromo-3-fluoro-2-methylbenzoylmalonate;

ethyl 2-(4,6-dibromo-3-fluoro-2-methylbenzoyl)-3-ethoxyacrylate;

ethyl 2-(4,6-dibromo-3-fluoro-2-methylbenzoyl)-3-cyclopropyl-aminoacrylate; and

ethyl 2-(2-methyl-3,4,6-trifluorobenzoyl)-3-(2,4-difluorophenyl)-aminoacrylate.

3. The compound according to claim 1, which is diethyl 4,6-dibromo-3-fluoro-2-methylbenzoylmalonate.

4. The compound according to claim 1, which is ethyl 2-(4,6-dibromo-3-fluoro-2-methylbenzoyl)-3-ethoxyacrylate.

5. The compound according to claim 1, which is ethyl 2-(4,6-dibromo-3-fluoro-2-methylbenzoyl)-3-cyclopropylaminoacrylate.
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