KR970042518A - 트리아졸유도체,그의제조방법및이화합물을유효성분으로하는의약 - Google Patents

트리아졸유도체,그의제조방법및이화합물을유효성분으로하는의약 Download PDF

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KR970042518A
KR970042518A KR1019960067668A KR19960067668A KR970042518A KR 970042518 A KR970042518 A KR 970042518A KR 1019960067668 A KR1019960067668 A KR 1019960067668A KR 19960067668 A KR19960067668 A KR 19960067668A KR 970042518 A KR970042518 A KR 970042518A
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South Korea
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derivative
salt
formula
triazole
halogen atom
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KR1019960067668A
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KR100262442B1 (ko
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도기자와미노루
수나오 다케다
야수시 가네코
히로미치 에토
이시다가즈야
가즈로리 마에바시
마사루 마츠모토
다케미츠 아사오카
스스무 사토
히데아키 마츠다
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타이도 나오카타
에스에스세야쿠가부시키가이샤
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/081,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C07D249/101,2,4-Triazoles; Hydrogenated 1,2,4-triazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/081,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D303/00Compounds containing three-membered rings having one oxygen atom as the only ring hetero atom
    • C07D303/02Compounds containing oxirane rings
    • C07D303/34Compounds containing oxirane rings with hydrocarbon radicals, substituted by sulphur, selenium or tellurium atoms

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Epoxy Compounds (AREA)

Abstract

본 발명은 하기 화학식(1)의 트리아졸 유도체 또는 그 염, 그의 제조방법, 하기 화학식(2) 및 (3)의 제조 중간체 및 하기 화학식(1)의 화합물 또는 그염을 유효성분으로 함유하는 의약에 관한 것이다.
상기식에서, n 은 0,1 또는 2를 나타내고, X1은 수소원자 또는 불소원자를 나타내고, Y1 및 Y는 각각 독립적으로 수소원자, 할로겐원자 또는 트리플루오로메틸기를 나타낸다.

Description

트리아졸 유도체, 그의 제조방법 및 이 화합물을 유효성분으로 하는 의약
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (12)

  1. 하기 화학식(1)의 트리아졸 유도체 또는 그 염.
    상기식에서, Y1 및 Y는 같거나 상이하며, 각각 독립적으로 수소원자, 할로겐원자 또는 트리플루오로메틸기를 나타내고, n 은 0,1 또는 2를 나타낸다.
  2. 하기 화학식(2)의 2-(메틸티오)아세토페논 유도체.
    상기식에서, X1은 할로겐 또는 불소원자를 나타내고, Y1및 Y는 같거나 상이하며, 각각 독립적으로 수소원자, 할로겐원자 또는 트리플루오로메틸기를 나타낸다.
  3. 하기 화학식(3)의 화합물.
    상기식에서, Y1및 Y는 같거나 상이하며, 각각 독립적으로 수소원자, 할로겐원자 또는 트리플루오로메틸기를 나타낸다.
  4. 제 1 항에 따른 트리아졸 유도체(1) 또는 그 염의 제조방법으로서, 하기 화학식(2a)의 2-(메틸티오)아세토페논 유도체를 하기 화학식(2c)의 2,2-디플루오로-2-메틸티오아세토페논 유도체로 불소화시키고; 형성된 2,2-디르루오로-2-메틸티오세토페논 유도체를 에폭시메틸화제 및 1,2,4-트리아졸 또는 그 염과 반응시키고; 필요에 따라 산화시키는 것을 특징으로 하는 제조방법.
    상기식에서, Y1 및 Y는 같거나 상이하며, 각각 독립적으로 수소원자, 할로겐원자 또는 트리플루오로메틸기를 나타낸다.
  5. 제 1 항에 따른 트리아졸 유도체(1) 또는 그 염의 제조방법으로서, 하기 화학식(5)의 2-(할로게노)아세토페논 유도체에 메틸티오기를 도입시켜, 하기 화학식(2c)의 2,2-디플루오로-2-메틸티오아세토페논 유도체로 전환시키고; 형성된 유도체를 에폭시메틸화제 및 1,2,4-트리아졸 또는 그 염과 반응시키고; 필요에 따라 산화시키는 것을 특징으로 하는 제조방법.
    상기식에서, Y1 및 Y는 같거나 상이하며, 각각 독립적으로 수소원자, 할로겐원자 또는 트리플루오로메틸기를 나타내고, X는 할로겐원자를 나타낸다.
  6. 제 1 항에 따른 트리아졸 유도체 또는 그 염을 유효성분으로 하는 의약.
  7. 제 6 항에 있어서, 항진균제인 것을 특징으로 하는 의약.
  8. 제 1 항에 따른 트리아졸 유도체 또는 그 염 및 약제학적으로 허용가능한 담체를 포함하는 의약 조성물.
  9. 제 8 항에 있어서, 조성물이 항진균 조성물인 것을 특징으로 하는 의약 조성물.
  10. 의약으로서의 제 1 항에 따른 트리아졸 유도체 또는 그 염의 농도.
  11. 제 10 항에 있어서, 의약이 항진균제인 것을 특징으로 하는 용도.
  12. 제 1 항에 따른 트리아졸 유도체 또는 그 염의 유효량을 환자에게 투여하는 것을 특징으로 하는, 진균증의 치료방법.
KR1019960067668A 1995-12-22 1996-12-19 트리아졸유도체,그의제조방법및이화합물을유호성분으로하는의약 KR100262442B1 (ko)

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JP335251/1995 1995-12-22
JP33525195 1995-12-22

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KR100262442B1 KR100262442B1 (ko) 2000-08-01

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US (2) US5945438A (ko)
EP (1) EP0780380B1 (ko)
KR (1) KR100262442B1 (ko)
CN (3) CN1058005C (ko)
CA (1) CA2193182A1 (ko)
DE (1) DE69613328T2 (ko)
ES (1) ES2159676T3 (ko)
HK (1) HK1011020A1 (ko)
TW (1) TW383299B (ko)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW438784B (en) * 1997-08-29 2001-06-07 Ssp Co Ltd Triazole derivative or salt thereof and pharmaceutical composition for treating mycosis containing the same
JP3638438B2 (ja) * 1997-12-26 2005-04-13 エスエス製薬株式会社 トリアゾール誘導体またはその塩、その製造方法及び当該化合物を有効成分とする医薬
EP0933368A1 (en) 1998-02-02 1999-08-04 SSP Co., Ltd. Triazole derivative or salt thereof, preparation process thereof and pharmaceutical containing said compound as an effective ingredient (antimycotic)
JP2000226368A (ja) * 1999-02-04 2000-08-15 Ss Pharmaceut Co Ltd ジフルオロアセトフェノン誘導体の製造法
US6391903B1 (en) * 1999-09-09 2002-05-21 Sankyo Company, Limited Triazole derivatives having antifungal activity
KR20010050557A (ko) 1999-09-29 2001-06-15 타이도 나오카타 아졸 유도체 또는 그의 염
HUP0004741A2 (hu) * 2000-11-28 2002-12-28 Sanofi-Synthelabo Kémiai eljárás tiazolszármazékok előállítására és új intermedier

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* Cited by examiner, † Cited by third party
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DE3279417D1 (en) * 1981-03-18 1989-03-09 Ici Plc Triazole compounds, a process for preparing them, their use as plant fungicides and fungicidal compositions containing them
DK161382C (da) * 1982-04-01 1991-12-09 Pfizer Fremgangsmaade til fremstilling af 1,2,4-triazol-forbindelser eller farmaceutisk acceptable syreadditionssalte deraf
BG48681A3 (en) * 1982-12-14 1991-04-15 Ciba - Geigy Ag Fungicide means
GB8304282D0 (en) * 1983-02-16 1983-03-23 Pfizer Ltd Antifungal agents
EP0117100B1 (en) * 1983-02-16 1986-12-10 Pfizer Limited Triazole antifungal agents
JPH0383973A (ja) * 1989-08-28 1991-04-09 Sumitomo Pharmaceut Co Ltd エポキシ体のスレオ選択的製造法
CA2031892C (en) * 1989-12-25 2000-08-01 Minoru Tokizawa Triazole derivatives
JP2530253B2 (ja) * 1989-12-25 1996-09-04 エスエス製薬株式会社 トリアゾ―ル誘導体
JPH03284662A (ja) * 1990-03-30 1991-12-16 Asahi Glass Co Ltd α―モノフルオロスルフィド及びその製造方法
JP3471831B2 (ja) * 1991-12-09 2003-12-02 富山化学工業株式会社 新規なトリアゾール誘導体およびその塩

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EP0780380A1 (en) 1997-06-25
US5945438A (en) 1999-08-31
US5986144A (en) 1999-11-16
HK1011020A1 (en) 1999-07-02
KR100262442B1 (ko) 2000-08-01
TW383299B (en) 2000-03-01
DE69613328D1 (de) 2001-07-19
CN1058005C (zh) 2000-11-01
CA2193182A1 (en) 1997-06-23
EP0780380B1 (en) 2001-06-13
CN1286248A (zh) 2001-03-07
CN1159446A (zh) 1997-09-17
ES2159676T3 (es) 2001-10-16
DE69613328T2 (de) 2001-09-20
CN1289771A (zh) 2001-04-04

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