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1. US20120264727 - Cephalosporin derivatives and pharmaceutical compositions thereof

Office
United States of America
Application Number 13467019
Application Date 08.05.2012
Publication Number 20120264727
Publication Date 18.10.2012
Grant Number 08329684
Grant Date 11.12.2012
Publication Kind B2
IPC
A61K 31/545
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
54having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame
542ortho- or peri-condensed with heterocyclic ring systems
545Compounds containing 5-thia-1-azabicyclo octane ring systems, i.e. compounds containing a ring system of the formula , e.g. cephalosporins, cefaclor, cephalexine
C07D 501/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
501Heterocyclic compounds containing 5-thia-1-azabicyclo octane ring systems, i.e. compounds containing a ring system of the formula: , e.g. cephalosporins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
14Compounds having a nitrogen atom directly attached in position 7
CPC
C07D 501/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
501Heterocyclic compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula: , e.g. cephalosporins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
02Preparation
04from compounds already containing the ring or condensed ring systems, e.g. by dehydrogenation of the ring, by introduction, elimination or modification of substituents
C07D 501/46
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
501Heterocyclic compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula: , e.g. cephalosporins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
14Compounds having a nitrogen atom directly attached in position 7
16with a double bond between positions 2 and 3
207-Acylaminocephalosporanic or substituted 7-acylaminocephalosporanic acids in which the acyl radicals are derived from carboxylic acids
24with hydrocarbon radicals, substituted by hetero atoms or hetero rings, attached in position 3
38Methylene radicals, substituted by nitrogen atoms; Lactams thereof with the 2-carboxyl group; Methylene radicals substituted by nitrogen-containing hetero rings attached by the ring nitrogen atom; Quaternary compounds thereof
46with the 7-amino radical acylated by carboxylic acids containing hetero rings
C07D 501/24
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
501Heterocyclic compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula: , e.g. cephalosporins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
14Compounds having a nitrogen atom directly attached in position 7
16with a double bond between positions 2 and 3
207-Acylaminocephalosporanic or substituted 7-acylaminocephalosporanic acids in which the acyl radicals are derived from carboxylic acids
24with hydrocarbon radicals, substituted by hetero atoms or hetero rings, attached in position 3
C07D 501/60
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
501Heterocyclic compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula: , e.g. cephalosporins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
14Compounds having a nitrogen atom directly attached in position 7
60with a double bond between positions 3 and 4
Applicants Legochem Biosciences, Inc.
Title
(EN) Cephalosporin derivatives and pharmaceutical compositions thereof
Abstract
(EN)

The present invention relates to novel cephalosporin derivatives represented by Chemical Formula 1.


Wherein, X, Y, L, R1, and R2 are as same as defined in the description of the invention. The present invention also relates to pharmaceutical antibiotic compositions comprising a novel celphalosporin derivative represented by Chemical Formula 1, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof as an effective ingredient. Compounds of the present invention are effective ingredients for the broad spectrum of antibiotic resistance, exhibit low toxicity, particularly in Gram-negative bacteria, which can be useful with strong antimicrobial activity.