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1. CA2831421 - NOVEL CEPHALOSPORIN DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS THEREOF

Office
Canada
Application Number 2831421
Application Date 29.03.2012
Publication Number 2831421
Publication Date 04.10.2012
Grant Number
Grant Date 04.06.2019
Publication Kind C
IPC
C07D 501/34
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
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
26Methylene radicals, substituted by oxygen atoms; Lactones thereof with the 2-carboxyl group
34with the 7-amino radical acylated by carboxylic acids containing hetero rings
A61K 31/546
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
546containing further heterocyclic rings, e.g. cephalothin
A61P 31/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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
A61P 31/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
A61P 31/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
04Antibacterial agents
Applicants LEGOCHEM BIOSCIENCES, INC.
Inventors CHO, YOUNG LAG
YUN, JOUNG YUL
PARK, CHUL SOON
CHAE, SANG EUN
LEE, HYANG SOOK
OH, KYUMAN
HEO, HYE JIN
KANG, DAE HYUCK
YANG, YOUNG JAE
KWON, HYUN JIN
PARK, TAE KYO
WOO, SUNG HO
KIM, YONG ZU
Title
(EN) NOVEL CEPHALOSPORIN DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS THEREOF
(FR) NOUVEAU DERIVE DE CEPHALOSPORINE ET COMPOSITION MEDICALE LE CONTENANT
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.According to the present invention, novel cephalosporin derivatives, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof as an effective ingredient for the broad spectrum of antibiotic resistant, low toxicity, particularly in Gram-negative bacteria, which can be useful with strong antimicrobial activity.
(FR) La présente invention concerne un nouveau dérivé de céphalosporine indiqué dans la formule chimique 1 de la description. Dans la formule chimique 1, X, Y, L, R1, R2 sont comme définis dans l'explication détaillée. En outre, la présente invention concerne une composition médicale antibiotique contenant le nouveau dérivé de céphalosporine de formule 1, l'un de ses promédicaments, l'un de ses hydrates, l'un de ses solvats, l'un de ses isomères et l'un de ses sels pharmaceutiquement acceptables, comme ingrédients actifs. Le nouveau dérivé de céphalosporine de formule chimique 1, son promédicament, son hydrate, son solvat, son isomère et son sel pharmaceutiquement acceptable présentent un large spectre antibactérien pour les bactéries résistantes, présentent une faible toxicité, et, en particulier, présentent un effet antibactérien puissant sur les bactéries Gram-négatives, et sont par conséquent utiles comme antibiotiques.