SG193998 NOVEL CEPHALOSPORIN DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS THEREOF

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Application Number 2013072962

Application Date 29.03.2012

Publication Number 193998

Publication Date 29.11.2013

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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

Priority Data 1020110028603 30.03.2011 KR

Title

(EN) NOVEL CEPHALOSPORIN DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS THEREOF

Abstract

(EN) 127 [Abstract] NOVEL, CEPHALOSPORIN DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS THEREOF D The present invention relates to novel cephaicaporin derivatives represented by Chemical Formula 1. W° )1144,„ ' ;. R2 (1) Wherein, X, Y, L, RI, and R2 are as same as defined in the description of the invention. 10 The bresent invent: on also reiates to pharmaceutical antibiotic compositions comprising a novel celphalosporin derivative represented by Chemical Formula I, a prbdrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a oharracentically acceptable salt thereof as an effective 15 ingredient. Abcording to the present invention, novel cephalosporin derivatives, a prodrug thereof, a hydrate thereof, a solvate therebf, an isomer thereof, or a pharmaceutically acceptable salt thereof as an effertive inoredient for the broad spectrum. of antibiotic resistant, low tozicity, particularly in. Gram-negative bacteria, which can be useful with strong antimicrobial activity. Figure 1

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
D	HETEROCYCLIC COMPOUNDS
501	Heterocyclic 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
14	Compounds having a nitrogen atom directly attached in position 7
16	with a double bond between positions 2 and 3
20	7-Acylaminocephalosporanic or substituted 7-acylaminocephalosporanic acids in which the acyl radicals are derived from carboxylic acids
24	with hydrocarbon radicals, substituted by hetero atoms or hetero rings, attached in position 3
26	Methylene radicals, substituted by oxygen atoms; Lactones thereof with the 2-carboxyl group
34	with the 7-amino radical acylated by carboxylic acids containing hetero rings

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31	Medicinal preparations containing organic active ingredients
33	Heterocyclic compounds
395	having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
54	having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame
542	ortho- or peri-condensed with heterocyclic ring systems
545	Compounds containing 5-thia-1-azabicyclo octane ring systems, i.e. compounds containing a ring system of the formula , e.g. cephalosporins, cefaclor, cephalexine
546	containing further heterocyclic rings, e.g. cephalothin

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
P	SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31	Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
D	HETEROCYCLIC COMPOUNDS
501	Heterocyclic 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
14	Compounds having a nitrogen atom directly attached in position 7
16	with a double bond between positions 2 and 3
20	7-Acylaminocephalosporanic or substituted 7-acylaminocephalosporanic acids in which the acyl radicals are derived from carboxylic acids
24	with hydrocarbon radicals, substituted by hetero atoms or hetero rings, attached in position 3
26	Methylene radicals, substituted by oxygen atoms; Lactones thereof with the 2-carboxyl group
34	with the 7-amino radical acylated by carboxylic acids containing hetero rings

A	HUMAN NECESSITIES
61	MEDICAL OR VETERINARY SCIENCE; HYGIENE
K	PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31	Medicinal preparations containing organic active ingredients
33	Heterocyclic compounds
395	having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
54	having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame
542	ortho- or peri-condensed with heterocyclic ring systems
545	Compounds containing 5-thia-1-azabicyclo octane ring systems, i.e. compounds containing a ring system of the formula , e.g. cephalosporins, cefaclor, cephalexine
546	containing further heterocyclic rings, e.g. cephalothin

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1. SG193998 - NOVEL CEPHALOSPORIN DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS THEREOF

Y	SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
02	TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
A	TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
50	in human health protection, e.g. against extreme weather
30	Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change