KR900007844A - 2-[4-(n-시아노 설파모일메틸)-1-피리디늄]에틸티오 카바페넴 - Google Patents

2-[4-(n-시아노 설파모일메틸)-1-피리디늄]에틸티오 카바페넴 Download PDF

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KR900007844A
KR900007844A KR1019890001832A KR890001832A KR900007844A KR 900007844 A KR900007844 A KR 900007844A KR 1019890001832 A KR1019890001832 A KR 1019890001832A KR 890001832 A KR890001832 A KR 890001832A KR 900007844 A KR900007844 A KR 900007844A
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South Korea
Prior art keywords
compound
formula
effective amount
dhp inhibitor
dimethylcyclopropanecarboxamide
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KR1019890001832A
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브이. 헥크 제임스
더블류. 러트클리프 로날드
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제임스 에프. 너튼
머크 앤드 캄파니, 인코포레이티드
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Publication of KR900007844A publication Critical patent/KR900007844A/ko

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D477/00—Heterocyclic compounds containing 1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbapenicillins, thienamycins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulphur-containing hetero ring
    • C07D477/10—Heterocyclic compounds containing 1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbapenicillins, thienamycins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulphur-containing hetero ring with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 4, and with a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 2
    • C07D477/12—Heterocyclic compounds containing 1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbapenicillins, thienamycins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulphur-containing hetero ring with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 4, and with a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 2 with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached in position 6
    • C07D477/16—Heterocyclic compounds containing 1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbapenicillins, thienamycins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulphur-containing hetero ring with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 4, and with a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 2 with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached in position 6 with hetero atoms or carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 3
    • C07D477/20—Sulfur atoms
    • 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

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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)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

내용 없음

Description

2-[4-(N-시아노설파모일메틸)-1-피리디늄]에틸티오 카바페넴
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (16)

  1. 하기 일반식(Ⅰ)의 화합물.
    상기식에서, R은 H 또는 CH3이고; R'는 H, F, Cl, NH2, CH3, SO2NHCH3, SO2NH2, SO2CH3, OCH3, CONH2, S(O)CH3또는 CONHCH3이며; Y는 ⅰ) COOH 또는 약제학적으로 허용되는 에스테르 또는 이의 염, ⅱ) COOR3(여기서, R3는 용이하게 제거할 수 있는 카복실 보호그룹이다), ⅲ) COOM(여기서, M은 알칼리 금속이다) 및 ⅳ) COO (단, 추가의 보충 양이온성 그룹이 구조속에 존재한다)로 이루어진 그룹으로부터 선택된다.
  2. 제1항에 있어서, R 및 R'이 모두 H인 하기 구조식의 화합물.
  3. 제1항에 있어서, R은 CH3이고 R'는 H인 하기 구조식의 화합물.
  4. 제1항에 있어서, R은 H이고, R'는 Cl인 하기 구조식의 화합물.
  5. 제1항에 있어서, R은 H이고, R'는 F인 하기 구조식의 화합물.
  6. 제1항에 있어서, R은 CH3이고, R'는 Cl인 하기 구조식의 화합물.
  7. 제1항에 있어서, R은 CH3이고, R'는 F인 하기 구조식의 화합물.
  8. 하기 구조식(Ib)의 화합물.
    상기식에서, R은 H 또는 CH3이고, 시아노설과 모일 측쇄와 임의의 치환체를 함유하는 ±N 그룹은및으로 이루어진 그룹으로부터 선택된다.
  9. 항생적 유효량의 제1항의 화합물과 약제학적으로 허용되는 이의 담체를 포함함을 특징으로 하는 항생제용 약제학적 조성물.
  10. 항생적 유효량의 제1항의 화합물을 세균에 감염된 사람 또는 동물에게 투여함을 특징으로 하여 사람 또는 동물의 세균성 감염증을 치료하는 방법.
  11. 제1항의 화합물과 DHP 억제제와의 혼합물.
  12. 제2항의 화합물과 DHP 억제제 7-(L-2-아미노-2-카복시에틸티오)-2-(2,2-디메틸사이클로프로판카복사미드)-2-헵테노산과의 혼합물.
  13. 항생적 유효량의 제1항의 화합물, 억제 유효량의 DHP억제제 및 약제학적으로 허용되는 임의의 담체를 포함함을 특징으로 하는 항생제용 약제학적 조성물.
  14. 제13항에 있어서, DHP 억제제 7-(L-2-아미노-2-카복시에틸티오)-2-(2,2-디메틸사이클로프로판카복사미드)-2-헵테노산인 약제학적 조성물.
  15. 항생적 유효량의 제1항의 화합물과 억제 유효량의 DHP 억제제를 세균에 감염된 사람 또는 동물에게 투여함을 특징으로 하여 사람 또는 동물의 세균성 감염증을 치료하는 방법.
  16. 제15항에 있어서, DHP 억제제가 7-(L-2-아미노-2-카복시에틸티오)-2-(2,2-디메틸사이클로프로판카복사미드)-2-헵테노산인 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019890001832A 1988-11-23 1989-02-17 2-[4-(n-시아노 설파모일메틸)-1-피리디늄]에틸티오 카바페넴 KR900007844A (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US07/275,811 US4952397A (en) 1985-06-17 1988-11-23 2-quaternary heteroarylalkylthio carbapenems having an acid moiety substituent
US275811 1988-11-23

Publications (1)

Publication Number Publication Date
KR900007844A true KR900007844A (ko) 1990-06-02

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KR1019890001832A KR900007844A (ko) 1988-11-23 1989-02-17 2-[4-(n-시아노 설파모일메틸)-1-피리디늄]에틸티오 카바페넴

Country Status (10)

Country Link
US (1) US4952397A (ko)
EP (1) EP0376355A1 (ko)
JP (1) JPH02145585A (ko)
KR (1) KR900007844A (ko)
AU (1) AU2967189A (ko)
DK (1) DK41889A (ko)
IE (1) IE890307L (ko)
IL (1) IL89130A0 (ko)
PT (1) PT89807A (ko)
ZA (1) ZA89971B (ko)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1993016080A1 (en) * 1992-02-06 1993-08-19 Yamanouchi Pharmaceutical Co., Ltd. Novel carbapenem derivative
US5496816A (en) * 1994-03-14 1996-03-05 Merck & Co., Inc. Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment
AU3215395A (en) * 1994-07-29 1996-03-04 Merck & Co., Inc. Carbapenem compounds, compositions and methods of treatment
AU2003300447B2 (en) * 2002-12-30 2009-09-03 Vertex Pharmaceuticals Incorporated Sulfhydantoins as phosphate isosteres for use as phosphatase inhibitors in the treatment of cancer and autoimmune disorders

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ201471A (en) * 1981-08-10 1985-09-13 Merck & Co Inc Antibacterial compositions containing penems and dipeptidase inhibitors
ZA832412B (en) * 1982-04-09 1983-12-28 Bristol Myers Co Carbapenem antibiotics
US4552696A (en) * 1982-04-09 1985-11-12 Bristol-Myers Company Carbapenem antibiotics
IE851586L (en) * 1984-07-02 1986-01-02 Interchem Internat S A I methylcarbapenems having a 2-quaternary¹heteroarylalkylthio substituent
CA1285940C (en) * 1984-07-02 1991-07-09 Merck & Co., Inc. Carbapenems having a 2-quaternary heteroarylalkylthio substituent
US4680292A (en) * 1984-12-13 1987-07-14 Merck & Co., Inc. Carbapenems and 1-methylcarbapenems having a 2-heteroaryliumaliphatic substituent

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EP0376355A1 (en) 1990-07-04
US4952397A (en) 1990-08-28
AU2967189A (en) 1990-05-31
PT89807A (pt) 1990-05-31
IE890307L (en) 1990-05-23
IL89130A0 (en) 1989-08-15
DK41889A (da) 1990-05-24
ZA89971B (en) 1990-03-28
DK41889D0 (da) 1989-01-31
JPH02145585A (ja) 1990-06-05

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