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1. EA201391325 - ПРОИЗВОДНЫЕ ЦЕФАЛОСПОРИНА И ИХ ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ

Office
Eurasian Patent Organization
Application Number 201391325
Application Date 29.03.2012
Publication Number 201391325
Publication Date 30.04.2014
Grant Number 024709
Grant Date 31.10.2016
Publication Kind B1
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
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 ЛЕГОКЕМ БАЙОСАЙЕНСИЗ, ИНК.
LEGOCHEM BIOSCIENCES, INC.
Inventors Чо Юн Лаг
Йоун Джоун Йуль
Парк Чуль Сун
Чае Сан Еунь
Ли Ньян Сук
Ох Кьюман
Хео Хье Джинь
Кан Дае Хьюк
Ян Юн Джае
Квон Хьюнь Джинь
Парк Тае Кью
Ву Сун Хо
Ким Йон Зу
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
Agents Поликарпов Александр Викторович
Polikarpov Aleksandr, V.
Title
(RU) ПРОИЗВОДНЫЕ ЦЕФАЛОСПОРИНА И ИХ ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ
Abstract
(RU)

Изобретение относится к новым производным цефалоспорина, представленным химической формулой (1)

где X, Y, L, R1, R2 и R3 являются такими, как определено в описании изобретения. Изобретение также относится к фармацевтическим антибиотическим композициям, содержащим новое производное цефалоспорина, представленное химической формулой (1), его пролекарство, его гидрат, его сольват, его изомер или его фармацевтически приемлемую соль в качестве эффективного ингредиента. Согласно изобретению предложены новые производные цефалоспорина, их пролекарство, их гидрат, их сольват, их изомер или их фармацевтически приемлемая соль в качестве ингредиента с низкой токсичностью, эффективного в отношении широкого спектра устойчивых к антибиотикам бактерий, в частности грамотрицательных, который может быть полезен сильной антимикробной активностью.