KR1020120110625 NOVEL CEPHALOSPORIN DERIVATIVES AND A PHARMACEUTICAL COMPOSITION CONTAINING THE SAME

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Republic of Korea

Application Number 1020110028603

Application Date 30.03.2011

Publication Number 1020120110625

Publication Date 10.10.2012

Grant Number 1017195560000

Grant Date 24.03.2017

Publication Kind B1

IPC

CPC

Applicants LEGOCHEM BIOSCIENCE LTD.
주식회사 레고켐 바이오사이언스

Inventors CHO, YOUNG LAG
YUN, JOUNG YUL
PARK, CHUL SOON
조영락
CHAE, SANG EUN
윤정율
LEE, HYANG SOOK
박철순
OH, KYU MAN
채상은
HEO, HYE JIN
이향숙
KANG, DAE HYUCK
오규만
YANG, YOUNG JAE
허혜진
KWON, HYUN JIN
강대혁
PARK, TAE KYO
양영재
WOO, SUNG HO
권현진
KIM, YONG ZU
박태교
우성호
김용주

Agents 손창규

Title

(EN) NOVEL CEPHALOSPORIN DERIVATIVES AND A PHARMACEUTICAL COMPOSITION CONTAINING THE SAME

(KO) 신규한 세파로스포린 유도체 및 이를 함유하는 의약 조성물

Abstract

(EN) PURPOSE: A pharmaceutical composition for antibiotics, containing novel cephalosporin derivatives is provided to ensure broad antibacterial spectrum against resistant bacteria and low toxicity. CONSTITUTION: A novel cephalosporin derivative is denoted by chemical formula 1 or 2. A pharmaceutical composition for antibiotics contains: pharmacologically effective amount of novel cephalosporin derivatives, prodrugs thereof, hydrates thereof, solvate thereof, isomers thereof, of pharmaceutically acceptable salt thereof; and pharmaceutically acceptable carriers, diluents, excipients, or a mixture thereof. COPYRIGHT KIPO 2013 null

(KO) 본 발명은 하기 화학식 1로 표시되는 신규한 세파로스포린 유도체에 관한 것이다. (1) 상기 식에서, X, Y, L, R, R 는 발명의 상세한 설명에 정의된 바와 동일하다. 또한, 본 발명은 상기 화학식 1의 신규한 세파로스포린 유도체, 이의 프로드럭, 이의 수화물, 이의 용매화물, 이의 이성질체 및 이의 약제학적으로 허용되는 염을 유효성분으로 함유하는 항생제용 의약 조성물에 관한 것이다. 본 발명에 따른 신규한 세파로스포린 유도체, 이의 프로드럭, 이의 수화물, 이의 용매화물, 이의 이성질체 및 이의 약제학적으로 허용되는 염은 내성균에 대한 항균 스펙트럼이 넓고, 독성이 낮으며, 특히 그람음성균에 강한 항균효과를 나타내므로, 항생제로 유용하게 사용될 수 있다. TIFF 112011023052312-pat00173.tif 51 96 1 2

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

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

C	CHEMISTRY; METALLURGY
07	ORGANIC CHEMISTRY
D	HETEROCYCLIC COMPOUNDS
501	Heterocyclic 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
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

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1. KR1020120110625 - NOVEL CEPHALOSPORIN DERIVATIVES AND A PHARMACEUTICAL COMPOSITION CONTAINING THE SAME