Quinoline carboxylic acid derivatives having 7-(4-amino-methyl-3

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Patent

Rate now

  [ 0.00 ] – not rated yet Voters 0   Comments 0

Details

546156, A61K 3147, C07D40102

Patent

active

056985703

ABSTRACT:
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: ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and Q are defined as described in the specification.

REFERENCES:
patent: 4897489 (1990-01-01), Yoshioka
Lesher et al., "1, 8-Naphthyridine Derivatives. A New Class of Chemotherapeutic Agents", J. Med. Chem., vol. 5, pp. 1063-1065, 1962.
Koga et al., "Structure-Activity Relationships of Antibacterial 6,7-and 7,8-Disubstituted 1-Alkyl-1,4-dihydro-4-oixouquinoline-3-carboxylic Acids", J. Med. Chem.,vol. 23, pp. 1358-1363, 1980.
Wise et al., "In Vitro Activity of Bay 09867, a New Quinoline Derivative, Compared with Those of Other Antimicrobial Agents", J. Antimicrob. Agents Chemother, vol. 23, pp. 559-564, 1983.
Sato et al., "In Vitro and In Vivo Activity of DL-8280, a New Oxazine Derivative", J. Antimicrob. Agents Chemother, vol. 23, pp. 548-553, 1982.
Rosen et al., "Design, Synthesis, and Properties of (4S)-7-(4-Amino-2-substituted-pyrrolidin-1-yl)quinolone-3-carboxylic Acids", J. Med. Chem., vol. 31, pp. 1598-1611, 1988.
Matsumoto et al., "AT-3295, a New Pyridonecarboxylic Acid Derivative with Potent Antibacterial Activity: Synthesis and Structure-activity Relationships", Proceedings of the 14th International Congress of Chemotheraphy, pp. 1519-1520, 1985.
Cooper et al., "Preparation and in Vitro and in Vivo Evaluation of Quinolones with Selective Activity against Gram-Positive Organisms", J. Med. Chem., vol. 35, pp. 1392-1398, 1992.
Domagala et al., "Synthesis and Biological Activity of 5-Amino-and 5-Hydroxyquinolones, and the Overwhelming Influence of the Remote N-Substituent in Determining the Structure-Activity Relationship", J. Med. Chem., vol. 34, pp. 1142-1154, 1991.
Domagala et al., "1-Substituted, 3-quinolinecarboxylic Acids. New Quantitative Structure-Activity Relationships at N for the Quinolone Antibacterials", J. Med. Chem., vol. 31, pp. 991-1001, 1988.
Bouzard et al., "Fluoronaphthyridines as Antibacterial Agents. 4. Synthesis and Structure-Activity Relationships of 5-Substituted-6-fluoro-7-(cycloalkylamino)-1,4-dihydro-4-oxo-1,8-naphthyri dine-3-carboxylic Acids", J. Med. Chem., vol. 35, pp. 518-525, 1992.
Parikh et al., "Sulfur Trioxide in the Oxidation of Alcohols by Dimethyl Sulfoxide", JACS, vol. 89, pp. 5505-5507, 1967.
CA 114: 164195r, p.775, 1991.
CA119: 203318h, p. 884, 1993.

LandOfFree

Say what you really think

Search LandOfFree.com for the USA inventors and patents. Rate them and share your experience with other people.

Rating

Quinoline carboxylic acid derivatives having 7-(4-amino-methyl-3 does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Quinoline carboxylic acid derivatives having 7-(4-amino-methyl-3, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Quinoline carboxylic acid derivatives having 7-(4-amino-methyl-3 will most certainly appreciate the feedback.

Rate now

     

Profile ID: LFUS-PAI-O-206560

  Search
All data on this website is collected from public sources. Our data reflects the most accurate information available at the time of publication.