Claims for Patent: 6,335,447

Summary for Patent: 6,335,447

Title:	Quinolonecarboxylic acid derivatives or salts thereof
Abstract:	Novel quinolonecarboxylic acid derivatives of general formula (1) or salts thereof which have potent antibacterial effects on gram-positive bacteria in particular Propionibacterium acnes(wherein R1 represents a hydrogen atom or a carboxyl-protective group; R2 represents an optionally substituted cycloalkyl group; R3 represents a hydrogen atom, a halogen atom, an optionally substituted alkyl, alkoxy or alkylthio group, an optionally protected hydroxyl or amino group, or a nitro group; R4 represents an optionally substituted alkyl or alkoxy group; and Z represents a pyridin-4-yl or pyridin-3-yl group which is optionally substituted with at least one group selected from a halogen atom, an optionally substituted alkyl, alkenyl, cycloalkyl, alkoxy, alkylthio or amino group and an optionally protected hydroxyl or amino group).
Inventor(s):	Kazuya Hayashi, Tokunori Kito, Junichi Mitsuyama, Tetsumi Yamakawa, Hiroshi Kuroda, Hiroyo Kawafuchi
Assignee:	Toyama Chemical Co Ltd
Application Number:	US09/647,763
Patent Claims:	1. Quinolonecarboxylic acid derivatives or salts thereof represented by general formula (wherein R1 represents a hydrogen atom or a carboxyl-protective group; R2 represents an optionally substituted cycloalkyl group; R3 represents a hydrogen atom, a halogen atom, an optionally substituted alkyl, alkoxy or alkylthio group, an optionally protected hydroxyl or amino group, or a nitro group; R4 represents an optionally substituted alkyl or alkoxy group; and Z represents a pyridin-4-yl or pyridin-3-yl group which is optionally substituted with at least one group selected from a halogen atom, an optionally substituted alkyl, alkenyl, cycloalkyl, alkoxy, alkylthio or amino group and an optionally protected hydroxyl or amino group). 2. The quinolonecarboxylic acid derivatives or salts thereof as claimed in claim 1, wherein R3 represents a hydrogen atom, an optionally substituted alkyl group or an optionally protected amino group; and Z represents a pyridin-4-yl or pyridin-3-yl group substituted with an optionally substituted alkyl, alkoxy or amino group. 3. The quinolonecarboxylic acid derivatives or salts thereof as claimed in claim 1 or 2, wherein R2 represents a cyclopropyl group; R3represents a hydrogen atom, an alkyl group or an amino group; and Z represents a pyridin-3-yl group substituted with an optionally substituted alkyl, alkoxy or amino group. 4. The quinolonecarboxylic acid derivatives or salts thereof as claimed in any one of claims 1 to 3, wherein R3 represents a hydrogen atom; R4 represents a methyl or methoxy group; and Z represents a pyridin-3-yl group substituted with at least one group selected from a methyl group, a hydroxymethyl group, an amino group, a methylamino group or a dimethylamino group. 5. 1-Cyclopropyl-7-(2,6-dimethyl-4-pyridyl)-8-methyl-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid or salts thereof. 6. 1-Cyclopropyl-8-methyl-7-[5-methyl-6-(methylamino)-3-pyridyl]-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid or salts thereof. 7. 7-(6-Amino-5-methyl-3-pyridyl)-1-cyclopropyl-8-methoxy-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid or salts thereof.