KR910006303A - 피페라지니오세팔로스포린 - Google Patents

피페라지니오세팔로스포린 Download PDF

Info

Publication number
KR910006303A
KR910006303A KR1019900014162A KR900014162A KR910006303A KR 910006303 A KR910006303 A KR 910006303A KR 1019900014162 A KR1019900014162 A KR 1019900014162A KR 900014162 A KR900014162 A KR 900014162A KR 910006303 A KR910006303 A KR 910006303A
Authority
KR
South Korea
Prior art keywords
methyl
carboxy
methylpiperazinio
oxide
carboxylic acid
Prior art date
Application number
KR1019900014162A
Other languages
English (en)
Other versions
KR0158452B1 (ko
Inventor
히로시 이노우에
도시로 고노이께
히로유끼 이시또비
Original Assignee
요시또시 가즈오
시오노기세이야꾸가부시끼가이샤
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by 요시또시 가즈오, 시오노기세이야꾸가부시끼가이샤 filed Critical 요시또시 가즈오
Publication of KR910006303A publication Critical patent/KR910006303A/ko
Application granted granted Critical
Publication of KR0158452B1 publication Critical patent/KR0158452B1/ko

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D501/00—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
    • C07D501/14—Compounds having a nitrogen atom directly attached in position 7
    • C07D501/16—Compounds having a nitrogen atom directly attached in position 7 with a double bond between positions 2 and 3
    • C07D501/20—7-Acylaminocephalosporanic or substituted 7-acylaminocephalosporanic acids in which the acyl radicals are derived from carboxylic acids
    • C07D501/24—7-Acylaminocephalosporanic or substituted 7-acylaminocephalosporanic acids in which the acyl radicals are derived from carboxylic acids with hydrocarbon radicals, substituted by hetero atoms or hetero rings, attached in position 3
    • C07D501/38—Methylene 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D501/00—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D505/00—Heterocyclic compounds containing 5-oxa-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. oxacephalosporins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Communicable Diseases (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Oncology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Cephalosporin Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

내용 없음

Description

피페라지니오세팔로스포린
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (14)

  1. 하기 일반식의 피레라지니오셀팔로스포린
    〔상기 식중, R1은 아미노 또는 아실아미노이고; R2는 수소 또는 메톡시이며; R3는 알킬기고; R4는 -(P-C-Q)n-(여기서 P, Q는 각각 수소, 알킬, 히드록시이건, P+Q는 옥소이고, n은 0-4의 정수이다)이며; R5는 임의 치환된 히드록시아릴 또는 히드록시헤테로고리이고; R6은 음전하를 가지며, COO 또는 임의의 보호 카르복시와 결합된 음이온이며; X는 O, S 또는 O→S이다〕.
  2. 제1항에 있어서, R1이 2-(2-아미노-4-티아졸릴)-2-알콕시이미노아세트아미도 또는 2-(2-아미노-4-티아졸릴)-2-카르복시알콕시이미노아세트아미도인 피페라지니오세팔로스포린.
  3. 제1항에 있어서, R2가 수소인 피페라지니오세팔로스포린.
  4. 제1항에 있어서, R3가 메틸인 피페라지니오세팔로스포린.
  5. 제1항에 있어서, R4가 카르보닐 또는 메틸렌인 피페라지니오세팔로스포린.
  6. 제1항에 있어서, R5가 아미노, 히드록시, 보호 히드록시, 할로겐, 니트로, 시아노, 카르복시, 카르바모일, 알콕시카르보닐, 아르알콕시카르보닐, 알킬, 알케닐 또는 아릴티오로 임의 치환된 임의의 보호 히드록시아릴인 피페라지니오셀팔로스포린.
  7. 제1항에 있어서, R5가 염소로 임의 치환된 3,4-디히드록실페닐인 피페라지니오 세팔로스포린.
  8. 제1항에 있어서, R5가 메틸, 클로로 또는 알콕시로 임의 치환된 비시날 디히드록시페닐 또는 비시날 디히드록시 피리딜인 피레라지니오세팔로스포린.
  9. 제1항에 있어서, R6가 COO-; 1-산소 치환 알킬, 알케닐, 아르알킬, 아릴, N-치환 아미노 또는 히드로카르빌실릴 카르복실레이트에스테르기; 또는 경금속, 암모니오 또는 아릴리니오 카르복실산염기인 피페라지니오세팔로스포린.
  10. 제1항에 있어서, R6가 COO-인 피페라지니오세팔로스포린.
  11. 제1항에 있어서, 7β-페닐아세트아미도-3-〔4-(3,4-디히드록시벤조일)-1-메틸피페라지니오〕메틸-3-세펨-4-카르복실산 및 그의 1-옥시드, 7β-디플루오로메틸티오아세트아미도-3-〔4-(3,4-디히드록시벤조일)-1-메틸피페라지니오〕메틸-3-세펨-4-카르복실산 및 그의 1-옥시드, 7β-〔2-(2-아미노티아졸-4-일)-2-메톡시이미노아세트아미도-3-〔4-(3,4-디히드록시페랄아세틸)-1-메틸피페라지니오〕메틸-3-세펨-4-카르복실산 및 그의 1-옥시드, 7β-〔2-(2-아미노티아졸릴-4-일)-2-메톡시이미노아세트아미도-3-〔4-(3,4-디히드록시벤조일)-1-메틸피페라지니오〕메틸-3-세펨-4-카르복실산 및 그의 1-옥시드, 7β-〔2-(2-아미노티아졸릴-4-일)-2-메톡시이미노아세트아미도-3-〔4-(3,4-디히드록시벤질)-1-메틸피페라지니오〕메틸-3-세펨-4-카르복실산 및 그의 1-옥시드, 7β-〔2-(2-아미노티아졸릴-4-일)-2-(1-카르복시-1-메틸에톡시이미노_아세트아미도-3-〔4-(3,4-디히드록시벤조일)-1-메틸피페라지니오〕메틸-3-세펨-4-카르복실산 및 그의 1-옥시드, 7β-〔2-(2-아미노티아졸릴-4-일)-2-(1-카르복시-1-메틸에톡시이미노)아세트 아미도-3-〔4-(2-클로로-3,4-디히드록시벤조일)-1-메틸피페라지니오〕메틸-3-세펨-4-카르복실산 및 그의 1-옥시드, 7β-〔2-(2-아미노티아졸릴-4-일)-2-(1-카르복시-1-메틸에톡시이미노)아세트아미도-3-〔4-(5-클로로-3,4-디히드록시벤조일)-1-메틸피페라지니오〕메틸-3-세펨-4-카르복실산 및 그의 1-옥시드, 7β-〔2-(2-아미노티아졸릴-4-일)-2-(1-카르복시-1-메틸에톡시이미노)아세트아미도-3-〔4-(6-클로로-3,4-디히드록시벤조일)-1-메틸피페라지니오〕메틸-3-세펨-4-카르복실산 및 그의 1-옥시드, 7β-〔2-(2-아미노티아졸릴-4-일)-2-(1-카르복시-1-메틸에톡시이미노)아세트아미도-3-〔4-(2,5-디클로로-3,4-디히드록시벤조일)-1-메틸피페라지니오〕메틸-3-세펨-4-카르복실산 및 그의 1-옥시드, 7β-〔2-(2-아미노티아졸릴-4-일)-2-(1-카르복시-1-메틸에톡시이미노)아세트아미도-3-〔4-(3-메톡시-4-디히드록시벤조일)-1-메틸피페라지니오〕메틸-3-세펨-4-카르복실산 및 그의 1-옥시드, 7β-〔2-(2-아미노티아졸릴-4-일)-2-(1-카르복시-1-메틸에톡시이미노)아세트아미도-3-〔4-(3,4-디히드록시벤질)-1-메틸피페라지니오〕메틸-3-세펨-4-카르복실산 및 그의 1-옥시드, 7β-〔2-(2-아미노티아졸-4-일)-2-(1-카르복시-1-메틸에톡시이미노)아세트아미도-3-〔4-(3,4,5-트리히드록시벤질)-1-메틸피페라지니오〕메틸-3-세펨-4-카르복실산 및 그의 1-옥시드, 7-〔2-(2-아미노티아졸릴-4-일)-2-(1-카르복시-1-비닐옥시이미노)아세트아미도-3-〔4-(3,4-디히드록시벤조일)-1-메틸피페라지니오〕메틸-3-세펨-4-카르복실산 및 그의 1-옥시드, 또는 그의 보호유도체인 피페라지니오세팔로스포린.
  12. 실시예 및 명세서 내에 기재되어 있는 바와 같은 아미드화, 아미드의 절단, 1-알킬-4-R4-R5-피페라진의 도입, R4-R5의 피페라진으로의 도입, 카르복시의 보호, 보호 카르복시의 탈보호, 카르복실산염 형성, 술폭시드로의 산화, 술폭시드의 환원, 히드록시의 보호, 보호 히드록시의 탈보호, 아미노-보호기의 도입, 보호 아미노의 탈보호 단계들로 구성된, 제1 내지 11항중 어느 한 항 기재의 피페라지니오세팔로스포린의 제조방법.
  13. 제1항 기재의 피페라지니오세팔로스포린 유효량을 세균에 접촉시킴을 특징으로 하는 살균방법.
  14. 제1항 기재의 피페라지니오세팔로스포린 유효량과 약학적 담체를 함유하는 항균조성물.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019900014162A 1989-09-07 1990-09-07 피페라지니오 세팔로스포린 KR0158452B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
JP232631/89 1989-09-07
JP1-232631 1989-09-07
JP23263189 1989-09-07

Publications (2)

Publication Number Publication Date
KR910006303A true KR910006303A (ko) 1991-04-29
KR0158452B1 KR0158452B1 (ko) 1998-12-01

Family

ID=16942341

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1019900014162A KR0158452B1 (ko) 1989-09-07 1990-09-07 피페라지니오 세팔로스포린

Country Status (7)

Country Link
US (1) US5143910A (ko)
EP (1) EP0416410B1 (ko)
JP (1) JP2969283B2 (ko)
KR (1) KR0158452B1 (ko)
AT (1) ATE114658T1 (ko)
DE (1) DE69014490T2 (ko)
DK (1) DK0416410T3 (ko)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0492277A3 (en) * 1990-12-20 1992-10-14 F. Hoffmann-La Roche Ag Cephalosporin derivatives
EP0550775A1 (en) * 1992-01-07 1993-07-14 F. Hoffmann-La Roche Ag Cephalosporin derivatives
JP3081773B2 (ja) * 1995-03-31 2000-08-28 株式会社資生堂 Ｎ−アシルピペラジン誘導体及び抗菌剤、抗潰瘍剤
JP4189043B2 (ja) * 1996-09-30 2008-12-03 株式会社資生堂 Ｎ−アシルピペラジン誘導体及び抗菌剤、抗潰瘍剤
EP1032559B1 (en) * 1997-09-29 2006-11-29 Aventis Pharmaceuticals Inc. Aminoalkylphenol derivatives for treating depression and memory dysfunction
US6479495B1 (en) 1997-09-29 2002-11-12 Aventis Pharmaceuticals Inc. Aminoalkylphenol derivatives and related compounds
US20060247248A1 (en) * 2003-08-05 2006-11-02 Vassilios Papadopoulos Sigma-1 receptor ligand with acetylcholinesterase
JP2007501254A (ja) * 2003-08-05 2007-01-25 サマリタン，ファーマスーティカルス，インク． アセチルコリンエステラーゼ阻害特性を有する、シグマ‐１受容体配位子
EP1993613A2 (en) * 2006-03-15 2008-11-26 Mallinckrodt, Inc. Chelating conjugates having a substituted aromatic moiety and derivatives thereof
US8883772B2 (en) 2007-10-09 2014-11-11 Sopharmia, Inc. Broad spectrum beta-lactamase inhibitors
RS55365B1 (sr) 2008-10-31 2017-03-31 Shionogi & Co Cefalosporin sa kateholskom grupom
KR20130018845A (ko) 2010-04-05 2013-02-25 시오노기세야쿠 가부시키가이샤 카테콜기를 갖는 세펨 화합물
WO2011125966A1 (ja) * 2010-04-05 2011-10-13 塩野義製薬株式会社 擬似カテコール基を有するセフェム化合物
US9085589B2 (en) 2010-04-28 2015-07-21 Shionogi & Co., Ltd. Cephem derivative
CA2833121A1 (en) * 2011-04-28 2012-11-01 Shionogi & Co., Ltd. Novel cephem compound having catechol or pseudo-catechol structure
JP2014513116A (ja) 2011-05-02 2014-05-29 ゾエティス・エルエルシー 抗菌剤として有用な新規セファロスポリン
US9242999B2 (en) 2011-06-27 2016-01-26 Shionogi & Co., Ltd. Cephem compound having pyridinium group
WO2013051597A1 (ja) 2011-10-04 2013-04-11 塩野義製薬株式会社 カテコール基を有するセフェム誘導体
UY35103A (es) 2012-10-29 2014-05-30 Glaxo Group Ltd Compuestos de cefem 2-sustituidos
CA2888543A1 (en) 2012-10-29 2014-05-08 Shionogi & Co., Ltd. Processes for production of intermediates for 2-alkyl cephem compounds
WO2021043973A1 (en) 2019-09-06 2021-03-11 Nabriva Therapeutics GmbH Siderophore cephalosporin conjugates and uses thereof
AU2021210472A1 (en) 2020-01-22 2022-07-21 Jiangsu Hengrui Medicine Co., Ltd. Cephalosporin antibacterial compound and pharmaceutical application thereof
CN116528874A (zh) 2021-01-12 2023-08-01 上海森辉医药有限公司 一种头孢类抗菌化合物及其制备方法

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5285187A (en) * 1976-01-08 1977-07-15 Shionogi & Co Ltd Antibacterials against pseudomonas aeruginosa
US4525473A (en) * 1983-03-30 1985-06-25 Bristol-Myers Company Cephalosporins
JPS6117589A (ja) * 1984-07-03 1986-01-25 Meiji Seika Kaisha Ltd 新規セフアロスポリン誘導体及びその製造法
US4785090A (en) * 1984-02-23 1988-11-15 Meiji Seika Kaisha, Ltd. Cephalosporin derivatives
US4880795A (en) * 1984-05-22 1989-11-14 Bayer Aktiengesellschaft Cephalosporins
IL77458A (en) * 1985-01-14 1990-07-26 Eisai Co Ltd Cephem derivatives,their production and antibacterial compositions containing them and certain novel intermediates therefor
ZA86405B (en) * 1985-01-31 1986-09-24 Yamanouchi Pharma Co Ltd Cephalosporin compounds and slats thereof,and their production
DE3506159A1 (de) * 1985-02-22 1986-08-28 Bayer Ag, 5090 Leverkusen Neue cephalosporine, verfahren zu ihrer herstellung und ihre verwendung in arzneimitteln
JPS6230786A (ja) * 1985-04-11 1987-02-09 Eisai Co Ltd ３−（キヌクリジニオ）メチル−３−セフエム誘導体
JPS625961A (ja) * 1985-07-01 1987-01-12 Meiji Seika Kaisha Ltd 酸性基を有するピリドチオン類化合物および該化合物より誘導される新規なセフアロスポリン誘導体
DE3541095A1 (de) * 1985-11-21 1987-05-27 Bayer Ag Neue cephalosporine, verfahren zu deren herstellung sowie ihre verwendung als arzneimittel
JPS62209082A (ja) * 1986-03-11 1987-09-14 Banyu Pharmaceut Co Ltd セフアロスポリン誘導体
US4814328A (en) * 1986-03-19 1989-03-21 Banyu Pharmaceutical Co., Ltd. Cephalosporin derivatives, and antibacterial agents
DE3775798D1 (de) * 1986-03-19 1992-02-20 Banyu Pharma Co Ltd Cephalosporinverbindungen, verfahren zu ihrer herstellung und antibakterielle mittel.
US4782155A (en) * 1986-03-19 1988-11-01 Banyu Pharmaceutical Co., Ltd. Cephalosporin derivatives, processes for their preparation and antibacterial agents
EP0272827A3 (en) * 1986-12-23 1990-02-07 ZENECA Pharma S.A. 3-heterocyclicthiomethyl cephalosphorins
DE3711343A1 (de) * 1987-04-03 1988-10-20 Bayer Ag Cephalosporinderivate, verfahren zu ihrer herstellung und ihre verwendung in arzneimitteln
PH25965A (en) * 1988-06-06 1992-01-13 Fujisawa Pharmaceutical Co New cephem compounds which have antimicrobial activities

Also Published As

Publication number Publication date
KR0158452B1 (ko) 1998-12-01
DE69014490D1 (de) 1995-01-12
EP0416410B1 (en) 1994-11-30
US5143910A (en) 1992-09-01
EP0416410A1 (en) 1991-03-13
JPH03173893A (ja) 1991-07-29
DK0416410T3 (da) 1995-05-15
DE69014490T2 (de) 1995-04-20
ATE114658T1 (de) 1994-12-15
JP2969283B2 (ja) 1999-11-02

Similar Documents

Publication Publication Date Title
KR910006303A (ko) 피페라지니오세팔로스포린
PE128799A1 (es) Quinolinas antimicrobianas y sus composiciones
ES8101596A1 (es) Metodo para producir compuestos de beta-lactama
SE7612053L (sv) Forfarande for framstellning av enolderivat
RU94030236A (ru) Производные 3 бета-алкенил-пенама, способ их получения, лекарственные средства и их применение для борьбы и предупреждения болезней
AU564150B2 (en) 1-sulfo-2-azetidinone derivatives
RU94039539A (ru) N,n'-замещенные имидокарбонимидные диамиды, получаемые из гидроксиламинов, имеющие антимикробную и антипаразитическую активность, профилактическая композиция, композиция для снижения уровня инфекций
KR840005816A (ko) 세팜로스포틴 화합물의 제조방법
CA1246583A (en) 4-ISOXAZOLYL)-THIAZOLE-2-OXAMIC ACIDS AND THEIR DERIVATIVES
JPS6485A (en) Novel cephalosporin derivative
GB1358027A (en) Alpha-amino-rho-hydroxyphenylacetamidocephalosporins
JPS5799592A (en) Novel cephalosporins
ES499915A1 (es) Procedimiento para la obtencion de derivados del aminotia- diazolilo
GB1472174A (en) Dihydroxy amino cephalosporins
ES441744A1 (es) Procedimiento para la preparacion de un nuevo derivado de lacefalosporina.
DE2408905A1 (de) Aminoacylthiocephalosporine
KR950032220A (ko) 세팔로스포린 화합물 및 그 제조방법
SE8105628L (sv) Cefalosporinderivat
AU4878479A (en) Clavulanic acid derivatives
KR960000894A (ko) 세팔로스포린 유도체 및 이의 염의 제조방법

Legal Events

Date Code Title Description
A201 Request for examination
E902 Notification of reason for refusal
E701 Decision to grant or registration of patent right
GRNT Written decision to grant
LAPS Lapse due to unpaid annual fee