KR950702561A - 퀴놀린 및 나프티리딘 약물 전구체(quinoline and naphthyridine prodrugs) - Google Patents

퀴놀린 및 나프티리딘 약물 전구체(quinoline and naphthyridine prodrugs) Download PDF

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Publication number
KR950702561A
KR950702561A KR1019950700158A KR19950700158A KR950702561A KR 950702561 A KR950702561 A KR 950702561A KR 1019950700158 A KR1019950700158 A KR 1019950700158A KR 19950700158 A KR19950700158 A KR 19950700158A KR 950702561 A KR950702561 A KR 950702561A
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KR
South Korea
Prior art keywords
compound
hydrogen
diazabicyclo
methyl
naphthyridine
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KR1019950700158A
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English (en)
Inventor
마틴 알. 제프슨
Original Assignee
알렌 제이. 스피겔
화이자 인코포레이티드
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Application filed by 알렌 제이. 스피겔, 화이자 인코포레이티드 filed Critical 알렌 제이. 스피겔
Publication of KR950702561A publication Critical patent/KR950702561A/ko

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/08Bridged systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • 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
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/08Bridged systems

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

Abstract

하기 일반식 (I)의 3-카복스알데하이드 퀴놀린 및 나프티리딘은 항균활성을 갖는다 :
상기 식에서, A, Y, R1및 R2는 본원에 정의된 바와 같이, 이러한 화합물은 주사에 의해서 투여하기에 특히 적합하다. 이러한 화합물의 특정한 예는 1-사이클로프로필-6-플루오로-7-[(1S,4S)-5-메틸-2,5-디아자비사이클로[2.2.1]헵트-2-일]-4-옥소-1,4-디하이드로퀴놀린-3-카복스알데하이드이다.

Description

퀴놀린 및 나프티리딘 약물 전구체(QUINOLINE AND NAPHTHYRIDINE PRODRUGS)
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (7)

  1. 하기 일반식의 화합물, 및 하기 일반식에서 R2가 수소가 아닌 경우 그의 약학적으로 허용가능한 산 부가염 :
    상기 식에서, A는 CH, CF 또는 N이고; Y는 에틸, 사이클로프로필, 4-플루오로페닐 또는 2,4-디플루오로페닐이거나; 또는 A 및 Y는 함께이고; R1은 수소 또는 메틸이고; R2는 수소, 5-메틸-2,5-디아자비사이클로[2.2.1]헵트-2-일, 8-메틸-3,8-디아자비사이클로[3.2.1]옥트-3-일, 1,4-디아자비사이클로[3.2.2]논-4-일이고; 단, R2가 수소일 경우, A 및 Y는 함께이다.
  2. 제1항에 있어서, 상기 화합물이 빈플록사신 또는 플루메퀸의 3-카복스알데하이드 유도체인 화합물.
  3. 제1항에 있어서, 상기 화합물이 다노플록사신의 3-카복스알데하이드 유도체인 화합물.
  4. 제1항 내지 제3항중 어느 한 항에 따른 화합물 및 약학적으로 허용가능한 담체를 포함하는 항균성 조성물.
  5. 제4항에 있어서, 상기 담체가 주사액인 조성물.
  6. 제1항 내지 제3항중 어느 한 항에 따른 화합물의 항균 효과량을 세균에 감염된 숙주에게 투여함을 포함하는, 세균에 감염된 숙주의 치료방법.
  7. 제6항에 있어서, 주사에 의해서 투여하는 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019950700158A 1992-07-15 1993-04-23 퀴놀린 및 나프티리딘 약물 전구체(quinoline and naphthyridine prodrugs) KR950702561A (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US07/914188 1992-07-15
US07/914,188 US5235054A (en) 1992-07-15 1992-07-15 3-carboxaldehyde substituted quinolines and naphthyridines
PCT/US1993/003624 WO1994002480A1 (en) 1992-07-15 1993-04-23 Quinoline and naphthyridine prodrugs

Publications (1)

Publication Number Publication Date
KR950702561A true KR950702561A (ko) 1995-07-29

Family

ID=25434020

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1019950700158A KR950702561A (ko) 1992-07-15 1993-04-23 퀴놀린 및 나프티리딘 약물 전구체(quinoline and naphthyridine prodrugs)

Country Status (20)

Country Link
US (1) US5235054A (ko)
EP (1) EP0650488A1 (ko)
JP (1) JPH07504684A (ko)
KR (1) KR950702561A (ko)
CN (1) CN1083053A (ko)
AU (1) AU669958B2 (ko)
BR (1) BR9306733A (ko)
CA (1) CA2140135A1 (ko)
CZ (1) CZ280603B6 (ko)
FI (1) FI933203A (ko)
HU (1) HUT68745A (ko)
IL (1) IL106264A0 (ko)
MX (1) MX9304266A (ko)
NO (1) NO950142L (ko)
NZ (1) NZ252847A (ko)
PL (1) PL307135A1 (ko)
RU (1) RU2097379C1 (ko)
SK (1) SK4695A3 (ko)
WO (1) WO1994002480A1 (ko)
ZA (1) ZA935076B (ko)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU8448491A (en) * 1990-09-07 1992-03-30 Schering Corporation Antiviral compounds and antihypertensive compounds
IL124454A (en) * 1995-12-21 2003-10-31 Pfizer Injectable danofloxacin formulations
JO3077B1 (ar) * 2005-07-28 2017-03-15 Janssen Pharmaceutica Nv مشتقات كوينولين مضادة للبكتيريا
MX2011012134A (es) 2009-05-15 2012-02-08 Redx Pharma Ltd Derivados de farmaco de oxido-reduccion.
WO2020184578A1 (ja) * 2019-03-11 2020-09-17 小胞体ストレス研究所株式会社 新規なeIF2αのリン酸化促進剤

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2509728A1 (fr) * 1981-07-17 1983-01-21 Roussel Uclaf Nouveaux derives de la quinoleine, leurs sels, procede de preparation, application a titre de medicaments et compositions les renfermant
IN166416B (ko) * 1985-09-18 1990-05-05 Pfizer
JP2777661B2 (ja) * 1988-10-20 1998-07-23 大塚製薬株式会社 ベンゾヘテロ環化合物

Also Published As

Publication number Publication date
AU669958B2 (en) 1996-06-27
US5235054A (en) 1993-08-10
HUT68745A (en) 1995-07-28
NZ252847A (en) 1996-07-26
IL106264A0 (en) 1993-11-15
CZ280603B6 (cs) 1996-03-13
AU5574694A (en) 1994-02-14
FI933203A0 (fi) 1993-07-14
NO950142D0 (no) 1995-01-13
ZA935076B (en) 1995-01-16
RU95105159A (ru) 1997-02-10
RU2097379C1 (ru) 1997-11-27
FI933203A (fi) 1994-01-16
SK4695A3 (en) 1995-07-11
CN1083053A (zh) 1994-03-02
MX9304266A (es) 1994-01-31
CZ10195A3 (en) 1995-09-13
WO1994002480A1 (en) 1994-02-03
NO950142L (no) 1995-01-13
EP0650488A1 (en) 1995-05-03
CA2140135A1 (en) 1994-02-03
PL307135A1 (en) 1995-05-02
HU9302018D0 (en) 1993-10-28
JPH07504684A (ja) 1995-05-25
BR9306733A (pt) 1999-01-12

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