KR890013028A - 세팔로스포린 유도체 및 이의 제법 - Google Patents

세팔로스포린 유도체 및 이의 제법 Download PDF

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KR890013028A
KR890013028A KR1019890001708A KR890001708A KR890013028A KR 890013028 A KR890013028 A KR 890013028A KR 1019890001708 A KR1019890001708 A KR 1019890001708A KR 890001708 A KR890001708 A KR 890001708A KR 890013028 A KR890013028 A KR 890013028A
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formula
compound
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alkenyl
alkyl
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KR1019890001708A
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KR0140886B1 (ko
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아담 프리드헬름
블룸바하 위르겐
뒤르크하이머 발터
휘셔 게르트
멘케 부르그하이트
이제르트 디터
자이베르트 게르하르트
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베른하르트 벡·하인리히 베커
훽스트 아크티엔게젤샤프트
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D501/00Heterocyclic 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
    • C07D501/14Compounds having a nitrogen atom directly attached in position 7
    • C07D501/16Compounds having a nitrogen atom directly attached in position 7 with a double bond between positions 2 and 3
    • C07D501/207-Acylaminocephalosporanic or substituted 7-acylaminocephalosporanic acids in which the acyl radicals are derived from carboxylic acids
    • C07D501/247-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
    • C07D501/26Methylene radicals, substituted by oxygen atoms; Lactones thereof with the 2-carboxyl group
    • C07D501/34Methylene radicals, substituted by oxygen atoms; Lactones thereof with the 2-carboxyl group with the 7-amino radical acylated by carboxylic acids containing hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D501/00Heterocyclic 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

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  • 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)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

내용 없음.

Description

세팔로스포린 유도체 및 이의 제법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (11)

  1. 다음 일반식(Ⅰ)의 세펨카복실산 에스테르, 또는 생리학적으로 허용되는 이의 산 부가염 및 이의 디아스테레오머.
    상기식에서, m은 0 또는 1이고; R1은 수소 또는 메틸이며; R2는 C1-6알킬, C2-6알케닐, C2-6알키닐 또는 그룹 -(CH2)n-OR3[여기에서, n은 0 또는 1이고; R3은 또한 추가로 페닐에 의해 치환될 수 있는 C1-6알킬이거나, C3-4알케닐이다]이고; HO그룹은 신(syn)-위치에 존재하며; m이 0이고 R1은 수소인 경우, R2는 메틸일 수 없다.
  2. 제1항에 있어서, R1및 m이 제1항에서 정의한 바와같고, R2는 C1-4알킬, C2-4알케닐, C3-4알키닐 또는 그룹 -(CH2)n-OR3[여기에서, n은 0 또는 1이고; R3은 또한 추가로 페닐에 의해 치환될 수 있는 C1-4알킬이거나, C3-4알케닐이다]인 세펨카복실산 에스테르.
  3. 2,2-디메틸-부타노일-옥시메틸 7-[2-(2-아미노티아졸-4-일)-2-(Z)-히드록시이미노-아세트아미도]-3-(메톡시메틸)-3-세펨-4-카복실레이트.
  4. 2,2-디메틸-3-부타노일-옥시메틸 7-[2-(2-아미노티아졸-4-일)-2-(Z)-히드록시이미노-아세트아미도]-3-(메톡시메틸)-3-세펨-4-카복실레이트.
  5. α-(2,2-디메틸-부타노일옥시)-에틸 7-[2-(2-아미노티아졸-4-일)-2-(Z)-히드록시이미노-아세트아미도]-3-(메톡시메틸)-3-세펨-4-카복실레이트.
  6. α-(2,2-디메틸-프로피오닐옥시)-에틸 7-[2-(2-아미노티아졸-4-일)-2-(Z)-히드록시이미노-아세트아미도]-3-(메톡시메틸)-3-세펨-4-카복실레이트 및 이의 디아스테레오머.
  7. (a) 다음 일반식(Ⅱ)의 화합물을 다음 일반식(Ⅲ)의 화합물과 반응시켜 다음 일반식(Ⅳ)의 에스테르를 제조하고, 그룹 R4및 R5를 공지방법으로 제거하거나, (b) 다음 일반식(Ⅴ)의 화합물을 다음 일반식(Ⅵ)의 화합물 또는 이 화합물의 염과 반응시켜 다음 일반식(Ⅳ)의 화합물을 제조하고, 그룹 R4및 R5를 공지방법으로 분할 제거하거나, (c) 다음 일반식(Ⅶ)의 화합물을 티오우레아와 반응시켜 다음 일반식(Ⅰ)의 화합물을 제조하고, 경우에 따라, 생성된 화합물을 생리학적으로 허용되는 이의 산부가염으로 전환시킴을 특징으로하여, 다음 일반식(Ⅰ)의 세펨카복실산 에스테르 및 생리학적으로 허용되는 이의 산 부가염을 제조하는 방법.
    상기식에서, m은 0 또는 1이고; R1은 수소 또는 메틸이며; R2는 C1-6알킬, C2-6알케닐, C2-6알키닐 또는 그룹 -(CH2)n-OR3[여기에서, n은 0 또는 1이고; R3은 또한 추가로 페닐에 의해 치환될 수 있는 C1-6알킬이거나, C3-4알케닐이다]이고; HO그룹은 신(syn)-위치에 존재하며; m이 0이고 R1은 수소인 경우, R2는 메틸일 수 없으며; R4는 아미노-보호그룹이고; R5는 용이하게 분할 제거될 수 있는 그룹이며; A는 양이온이고; X는 이탈기이며; Y는 활성화 그룹이고; Z는 할로겐이다.
  8. 제7항에 있어서, R1이 메틸인 경우, 디아스테레오머의 혼합물을, 경우에 따라, 공지방법으로 분리시키는 방법.
  9. 일반식(Ⅰ)의 세펨카복실산 에스테르를 함유하며, 세균감염에 대하여 활성인 약제학적 조성물.
  10. 일반식(Ⅰ)의 세펨카복실산 에스테르를, 약제학적 부형제 또는 희석제를 사용하여 약제학적으로 적합한 투여형태로 제조함을 특징으로 하여, 세균감염에 대하여 활성인 약제학적 조성물을 제조하는 방법.
  11. 세균감염을 퇴치하기 위하여 사용하는 일반식(Ⅰ)의 세펨카복실산 에스테르의 용도.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019890001708A 1988-02-17 1989-02-15 세팔로스포린 유도체 및 이의 제법 KR0140886B1 (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DEP3804841.8 1988-02-17
DE3804841A DE3804841A1 (de) 1988-02-17 1988-02-17 Cephalosporinderivate und verfahren zu ihrer herstellung

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KR890013028A true KR890013028A (ko) 1989-09-20
KR0140886B1 KR0140886B1 (ko) 1998-06-01

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US (2) US5100887A (ko)
EP (1) EP0329008B1 (ko)
JP (1) JP2509689B2 (ko)
KR (1) KR0140886B1 (ko)
CN (1) CN1043042C (ko)
AT (1) ATE183188T1 (ko)
AU (1) AU613152B2 (ko)
CA (1) CA1339421C (ko)
DD (1) DD283629A5 (ko)
DE (2) DE3804841A1 (ko)
DK (1) DK174730B1 (ko)
DZ (1) DZ1324A1 (ko)
ES (1) ES2136591T3 (ko)
FI (1) FI93458C (ko)
GR (1) GR3031542T3 (ko)
HU (1) HU205121B (ko)
IL (1) IL89303A0 (ko)
MY (1) MY104937A (ko)
NO (1) NO173736C (ko)
NZ (1) NZ227990A (ko)
PT (1) PT89729B (ko)
TN (1) TNSN89016A1 (ko)
ZA (1) ZA891162B (ko)

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TW212181B (ko) * 1992-02-14 1993-09-01 Hoechst Ag
DK0570849T3 (da) * 1992-05-21 1998-09-28 Hoechst Ag Fremgangsmåde til spaltning af cephalosporin-prodrugestere til dannelse af 7-amino-3-methoxymethyl-ceph-3-em-4-carboxylsyre
LT3871B (en) 1993-11-30 1996-04-25 Hoechst Ag Additive crystalline salts of pure diastereomers of 1-cefem-4-carboxylic acid 1-(2,2-dimethyl-propionyloxy)ethyl esters, process for the preparation thereof, pharmaceutical compositions and process for the preparation thereof
DE4418957A1 (de) * 1994-05-31 1995-12-07 Merck Patent Gmbh Cefixim-Zubereitung
SE524569C2 (sv) * 1998-11-20 2004-08-31 Perstorp Ab Förfarande för framställning av en allyloxikarboxylsyra, användning av allyoxikarboxylsyran framställd enligt förfarandet som komponent i oligomera och polymera bindemedel samt 6-allyloxihexansyra framställd enligt förfarandet
AT408226B (de) * 1999-05-05 2001-09-25 Biochemie Gmbh Kristalliner 7-(2-(2-formylaminothiazol-4-yl)-2
US20060009639A1 (en) * 2002-11-22 2006-01-12 Orchid Chemicals & Pharmaceuticals Limited Process for the preparation of cefpodoxime proxetil
WO2005019227A1 (en) * 2003-08-22 2005-03-03 Orchid Chemicals & Pharmaceuticals Ltd Process for the preparation of cephalosporin antibiotic
JP2010047550A (ja) * 2008-08-25 2010-03-04 Daicel Chem Ind Ltd アルコキシアルカンカルボン酸エステルの製造方法
WO2017136705A1 (en) 2016-02-04 2017-08-10 Apple Inc. Controlling electronic devices and displaying information based on wireless ranging

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Publication number Publication date
PT89729B (pt) 1994-03-31
DD283629A5 (de) 1990-10-17
CA1339421C (en) 1997-09-02
FI93458C (fi) 1995-04-10
ATE183188T1 (de) 1999-08-15
DE3804841A1 (de) 1989-08-31
EP0329008B1 (de) 1999-08-11
GR3031542T3 (en) 2000-01-31
IL89303A0 (en) 1989-09-10
DK72289D0 (da) 1989-02-16
DK72289A (da) 1989-08-18
JP2509689B2 (ja) 1996-06-26
DE58909854D1 (de) 1999-09-16
NO173736C (no) 1994-01-26
HU205121B (en) 1992-03-30
CN1035509A (zh) 1989-09-13
JPH01249778A (ja) 1989-10-05
PT89729A (pt) 1989-10-04
FI890722A0 (fi) 1989-02-15
AU613152B2 (en) 1991-07-25
DK174730B1 (da) 2003-10-06
NO890657D0 (no) 1989-02-16
DZ1324A1 (fr) 2004-09-13
ZA891162B (en) 1989-10-25
USRE34865E (en) 1995-02-21
FI93458B (fi) 1994-12-30
AU3003189A (en) 1989-08-17
NO173736B (no) 1993-10-18
TNSN89016A1 (fr) 1991-02-04
NO890657L (no) 1989-08-18
US5100887A (en) 1992-03-31
HUT49614A (en) 1989-10-30
FI890722A (fi) 1989-08-18
EP0329008A3 (de) 1991-08-28
NZ227990A (en) 1990-10-26
CN1043042C (zh) 1999-04-21
ES2136591T3 (es) 1999-12-01
MY104937A (en) 1994-07-30
KR0140886B1 (ko) 1998-06-01
EP0329008A2 (de) 1989-08-23

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