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LG Chemical Limited

The present invention relates to a novel quinolone compound having an excellent antibacterial activity. More specifically, the present invention relates to a novel quinoline(naphthyridine)carboxylic acid derivative represented by the following formula (I), which has an 4-aminomethyl-3-oximepyrrolidine substituent on 7-position of the quinolone nucleus and shows a superior antibacterial activity in contrast to the known quinolone antibactrial agents having a weak activity against gram-positive bacterial strains and also has a broad antibacterial spectrum and a highly improved pharmacokinetic property : wherein R, R1, R2, R3, R4 and Q are defined as described in the specification.

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Dong Wha Pharm. Ind. Co., Ltd.

The present invention relates to optically active quinoline carboxylic acid derivatives, their pharmaceutically acceptable salts, their solvates, and a process for the preparation thereof. More specifically, the present invention relates to optically active quinoline carboxylic acid derivatives containing 4-aminomethyl-4-methyl-3-(Z)-alkoxyirninopyrrolidine substituents causing optical activity at the 7-position of the quinolone nuclei. As the compounds of the present invention have superior antibacterial activity and pharmacokinetic profiles to their enantiomers, their racemates and conventional antibacterial agents, with nearly no phototoxicity, the compounds of this invention are useful for antibacterial agents.

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ORCHID CHEMICALS & PHARMACEUTICALS LIMITED

The present invention relates to an improved process for the preparation of Gemifloxacin mesylate of formula (V). The present invention further provides novel intermediates of formula (II) and (IV), which are useful intermediates for the preparation of Gemifloxacin mesylate of formula (V) wherein R1 is linear or branched chain alkyl group having 1-3 carbon atoms.

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Daiichi Seiyaku Co., Ltd.

The present invention relates to spiro compounds of general formula I: STR1 wherein the substituents are herein below defined. The present invention relates to antibacterial spiro compounds which are of value as drugs for humans, veterinary drugs or drugs for use in fish culture or as preservatives, and to antibacterial compositions containing one or more of the same compounds as active ingredients.

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LG Chemical Ltd.

The present invention relates to a novel quinolone compound having an excellent antibacterial activity. More specifically, the present invention relates to a novel quinoline(naphthyridine)carboxylic acid derivative represented by the following formula (I), which has an 4-aminomethyl-3-oximepyrrolidine substituent on 7-position of the quinolone nucleus and shows a superior antibacterial activity in contrast to the known quinolone antibacterial agents having a weak activity against gram-positive bacterial strains and also has a broad antibacterial spectrum and a highly improved pharmacokinetic property: STR1 wherein R, R1, R2, R3, R4 and Q are defined as described in the specification.

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In heterogeneous catalysis, the catalyst is in a different phase from the reactants. category: naphthyridine, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 100361-18-0, name is 7-Chloro-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic Acid. In an article£¬Which mentioned a new discovery about 100361-18-0

A series of 7-[3-(1-aminoalkyl and 1-aminocycloalkyl)-1- pyrrolidinyl]quinolones have been prepared and their biological properties evaluated. Among them, 1-(S)-aminoalkyl derivatives exhibited potent antibacterial activities against gram-positive and gram-negative organisms. They had moderate lipophilicity and high aqueous solubility compared to their aminomethyl counterparts; e.g., the 3-(1-aminoethyl)-1-pyrrolidinyl compound (83) showed superior pharmacokinetic properties to its aminomethyl counterpart (6).

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Dainippon Pharmaceutical Co., Ltd.

The present invention relates to a 1,8-naphthyridine derivative of the formula STR1 wherein X is a fluorine or chlorine atom, and R is a hydrogen atom, or a methyl or ethyl group; and esters thereof and salts thereof are processes for preparation thereof. These compounds show excellent anti-bacterial activity and are useful antibacterial agents.

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Discovery of 7-Chloro-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic Acid

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Warner-Lambert Company

Novel quinoline-, naphthyridine-, and benzoxazine-carboxylic acid derivatives with bridged sidechains useful as antibacterial agents are described. Methods for their preparation, formulation, and use in treatment of bacterial infections is also described.

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Pfizer Inc

Quinolone carboxylic acids 7-substituted by azabicyclo groups have antibacterial activity.

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100361-18-0, Name is 7-Chloro-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic Acid, belongs to naphthyridine compound, is a common compound. HPLC of Formula: C12H8ClFN2O3In an article, once mentioned the new application about 100361-18-0.

A series of novel 6-fluoro-7-diazabicycloalkylquinolonecarboxylic acids substituted with various C8 (H, F, Cl, N) and N1 (ethyl, cyclopropyl, vinyl, 2-fluoroethyl, 4-fluorophenyl, 2,4-difluorophenyl) substituents, as well as, 9-fluoro-10-diazabicycloalkylpyridobenzoxazinecarboxylic acids, were prepared and evaluated for antibacterial activity against a range of important veterinary pathogenic bacteria. The diazabicycloalkyl side chains investigated at the 7-position (benzoxazine 10-position) include (1S,4S)-5- methyl-2,5-diazabicyclo[2.2.1]heptane (2), (1S,4S)-2,5- diazabicyclo[2.2.1]heptane (3), (1R,4R)-5-methyl-2,5- diazabicyclo[2.2.1]heptane (4), 8-methyl-3,8-diazabicyclo[3.2.1]octane (5), 9-methyl-3,9-diazabicyclo[4.2.1]nonane (6), 1,4-diazabicyclo[3.2.2]nonane (7), 1,4-diazabicyclo[3.3.1]nonane (8), and 9-methyl-3,9- diazabicyclo[3.3.1]nonane (9). Among these side chains, in vitro potency was not highly variable; other properties therefore proved more critical to the selection of possible development candidates. However, the relative potencies observed for several of these compounds in mouse, swine, and cattle infection models correlated well with those seen in vitro. A combination of the N1 cyclopropyl group and the C7 (1S,4S)-5-methyl-2,5-diazabicyclo[2.2.1]hept-2- yl appendage conferred the best overall antibacterial, physiochemical, and pharmacodynamic properties. Hence, danofloxacin (Advocin, 2c) (originally CP- 76,136, 1-cyclopropyl-6-fluoro-7-[(1S,4S)-5-methyl-2,5- diazabicyclo[2.2.1]hept-2-yl]-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid) was selected as a candidate for development as a therapeutic antibacterial agent for veterinary medicine.

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