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1. WO2012134184 - NOVEL CEPHALOSPORIN DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS THEREOF

Publication Number WO/2012/134184
Publication Date 04.10.2012
International Application No. PCT/KR2012/002302
International Filing Date 29.03.2012
Chapter 2 Demand Filed 29.10.2012
IPC
C07D 501/34 2006.1
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 2006.1
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 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
CPC
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
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 501/24
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 501/46
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 501/60
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
  • 주식회사 레고켐 바이오사이언스 LEGOCHEM BIOSCIENCES, INC. [KR]/[KR] (AllExceptUS)
  • 조영락 CHO, Young Lag [KR]/[KR] (UsOnly)
  • 윤정율 YUN, Joung Yul [KR]/[KR] (UsOnly)
  • 박철순 PARK, Chul Soon [KR]/[KR] (UsOnly)
  • 채상은 CHAE, Sang Eun [KR]/[KR] (UsOnly)
  • 이향숙 LEE, Hyang Sook [KR]/[KR] (UsOnly)
  • 오규만 OH, Kyuman [KR]/[KR] (UsOnly)
  • 허혜진 HEO, Hye Jin [KR]/[KR] (UsOnly)
  • 강대혁 KANG, Dae Hyuck [KR]/[KR] (UsOnly)
  • 양영재 YANG, Young Jae [KR]/[KR] (UsOnly)
  • 권현진 KWON, Hyun Jin [KR]/[KR] (UsOnly)
  • 박태교 PARK, Tae Kyo [KR]/[KR] (UsOnly)
  • 우성호 WOO, Sung Ho [KR]/[KR] (UsOnly)
  • 김용주 KIM, Yong Zu [KR]/[KR] (UsOnly)
Inventors
  • 조영락 CHO, Young Lag
  • 윤정율 YUN, Joung Yul
  • 박철순 PARK, Chul Soon
  • 채상은 CHAE, Sang Eun
  • 이향숙 LEE, Hyang Sook
  • 오규만 OH, Kyuman
  • 허혜진 HEO, Hye Jin
  • 강대혁 KANG, Dae Hyuck
  • 양영재 YANG, Young Jae
  • 권현진 KWON, Hyun Jin
  • 박태교 PARK, Tae Kyo
  • 우성호 WOO, Sung Ho
  • 김용주 KIM, Yong Zu
Agents
  • 손창규 SOHN, Chang Kyu
Priority Data
10-2011-002860330.03.2011KR
Publication Language Korean (ko)
Filing Language Korean (KO)
Designated States
Title
(EN) NOVEL CEPHALOSPORIN DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS THEREOF
(FR) NOUVEAU DÉRIVÉ DE CÉPHALOSPORINE ET COMPOSITION MÉDICALE LE CONTENANT
(KO) 신규한 세파로스포린 유도체 및 이를 함유하는 의약 조성물
Abstract
(EN) The present invention relates to a novel cephalosporin derivative indicated in chemical formula 1 of the description. In the chemical formula 1, X, Y, L, R1, R2 are identical as defined in the detailed explanation. In addition, the present invention relates an antibiotic medical composition containing the novel cephalosporin derivative of the chemical formula 1, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, and a pharmaceutically permitted salt thereof, as active ingredients. The novel cephalosporin derivative of the chemical formula 1, the prodrug thereof, the hydrate thereof, the solvate thereof, the isomer thereof, and the pharmaceutically permitted salt thereof have a wide antibacterial spectrum for resistant bacteria, have low toxicity, and in particular, show strong antibacterial effect on gram negative bacteria, and is thus useful as an antibiotic.
(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.
(KO) 본 발명은 명세서 상의 화학식 1로 표시되는 신규한 세파로스포린 유도체에 관한 것이다. 화학식 1에서, X, Y, L, R1, R2 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.
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