KR910000628A - 디페닐우레아 유도체, 그의 제조방법 및 그를 함유하는 조성물 - Google Patents

디페닐우레아 유도체, 그의 제조방법 및 그를 함유하는 조성물 Download PDF

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KR910000628A
KR910000628A KR1019900008802A KR900008802A KR910000628A KR 910000628 A KR910000628 A KR 910000628A KR 1019900008802 A KR1019900008802 A KR 1019900008802A KR 900008802 A KR900008802 A KR 900008802A KR 910000628 A KR910000628 A KR 910000628A
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derivative
general formula
carbon atoms
diphenylurea
atom
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KR1019900008802A
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데쯔오 세끼야
신야 이노우에
마사오 다니구찌
고헤이 우메즈
가즈오 스즈끼
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에또 다께또시
미쓰비시 가세이 가부시끼가이샤
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Publication of KR910000628A publication Critical patent/KR910000628A/ko

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C335/00—Thioureas, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C335/04—Derivatives of thiourea
    • C07C335/16—Derivatives of thiourea having nitrogen atoms of thiourea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/17—Amides, e.g. hydroxamic acids having the group >N—C(O)—N< or >N—C(S)—N<, e.g. urea, thiourea, carmustine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C275/00—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C275/28—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C275/00—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C275/28—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C275/30—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by halogen atoms, or by nitro or nitroso groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C275/00—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C275/28—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C275/32—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by singly-bound oxygen atoms
    • C07C275/34—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by singly-bound oxygen atoms having nitrogen atoms of urea groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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Abstract

내용 없음

Description

디페닐우레아 유도체, 그의 제조방법 및 그를 함유하는 조성물
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (7)

  1. 하기 일반식(Ⅰ)의 디페닐우레아 유도체:
    상기식에서, R1은 탄소수 5 내지 18의 알킬기이고, R2와 R3은 각기 독립적으로 탄소수 1 내지 5의 알킬기, 탄소수 1 내지 5의 알콕시기, 또는 할로겐 원자이고, R4는 수소원자, 탄소수 1 내지 5의 알킬기, 탄소수 1 내지 5의 알콕시기, 또는 할로겐 원자이고, X는 산소 원자 또는 황 원자이다.
  2. 제1항에 있어서, R1이 탄소수 6 내지 10의 n-알킬기인 디페닐우레아 유도체.
  3. 제2항에 있어서, R1이 2- 또는 4-위치에 존재하는 디페닐우레아 유도체.
  4. 제3항에 있어서, R4가 수소 원자인 디페닐우레아 유도체.
  5. 제1항의 디페닐우레아 유도체를 활성 성분으로 포함하는 아실조효소 콜레스테롤 아실트란스퍼라제 억제제.
  6. 치료에 유효한 양만큼인 제1항의 디페닐우레아 유도체와 함께 제약학상 허용되는 담체, 희석제 또는 그의 혼합물을 포함하는 과지방혈증 및 아케롬성 동맥경화증 치료용 제약 조성물.
  7. A)하기 일반식(Ⅱ) [또는 (Ⅳ)]의 아닐린 유도체를 비활성 용매중에서 0℃ 내지 약 150℃의 온도하에 하기 일반식(Ⅲ) [또는 (Ⅴ)]의 페닐 이소시아네이트 또는 이소티오시아네이트 유도체와 반응시키거나:
    (상기식에서, R1, R2, R3및 R4와 X는 앞서 정의한 바와 같다.);B) 하기 일반식(Ⅵ) [또는 (Ⅷ)]의 벤조산 유도체를 비활성 아민 존재하에 비활성 용매중에서 실온 내지 약 150℃의 온도하에 DPPA(디페녹시포스포릴아지드)로 처리함으로써 하기 일반식(Ⅶ)[또는 (Ⅸ)]의 상응되는 페닐 이소시아네이트 유도체로 전환시키고, 일반식(Ⅵ)[또는 (Ⅱ)의 아닐린 유도체를 0℃ 내지 약 150℃의 온도하에 이소시아네이트(Ⅶ)[또는 (Ⅸ)]와 반응시키거나:
    (상기식에서, R1, R2, R3및 R4는 앞서 정의한 바와 같다.):C)일반식(Ⅱ) [또는 (Ⅳ)]의 아닐린 유도체를 포스겐 또는 페닐클로로프르메이트와 같은 카르본산의 활성화 유도체로 처리하열 아릴카르바밀클로라이드 또는 아릴카르바민산의 아릴에스테르와 같은 하기 일반식(X) [또는 (Ⅸ)]의 반응성 중간체를 얻고, 이 중간체를 비활성 유기 아민 존재하에 비활성 용매중에서 0℃ 내지 약 100℃의 온도하에 일반식(Ⅳ) [또는 (Ⅱ)]의 아닐린 유도체와 반응시킴으로써, X가 산소 원자인 본 발명의 화합물(Ⅰ)을 얻거나:
    (상기식에서, R1, R2, R3및 R4는 앞서 정의한 바와 같고, Y는 염소원자 또는 아릴옥시기와 같은 이탈기이다): 또는, D)일반식(Ⅱ) [또는 (Ⅳ)]의 아닐린 유도체를 하기 일반식(XⅡ) [또는 XⅢ)]의 반응성 중간체, 즉 아릴티오카르바민산의 알킬티오에스테르로 전환시키고, 이 중간체를 50℃ 내지 사용된 용매의 비점에 이르는 온도범위하에 비활성 용매중에서 일반식(Ⅳ) [또는 (Ⅱ)]의 아닐린 유도체와 반응시킴으로써, X가 황 원자인 본 발명의 화합물(Ⅰ)을 얻는 것을 포함하는 제1항에 정의된 바와 같은 디페닐우레아 유도체의 제조방법:
    (상기식에서, R1, R2, R3및 R4는 앞서 정의한 바와 같고, R은 탄소수 1 내지 3의 알킬기이다.)
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019900008802A 1989-06-15 1990-06-13 디페닐우레아 유도체, 그의 제조방법 및 그를 함유하는 조성물 KR910000628A (ko)

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Application Number Priority Date Filing Date Title
JP15259489 1989-06-15
JP1-152594 1989-06-15
JP2-106986 1990-04-23
JP2106986A JPH0395153A (ja) 1989-06-15 1990-04-23 ジフェニル尿素誘導体

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US (1) US5063247A (ko)
EP (1) EP0405233B1 (ko)
JP (1) JPH0395153A (ko)
KR (1) KR910000628A (ko)
AT (1) ATE96426T1 (ko)
AU (1) AU628583B2 (ko)
CA (1) CA2018848A1 (ko)
DE (1) DE69004164T2 (ko)
DK (1) DK0405233T3 (ko)
ES (1) ES2059893T3 (ko)

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JPH0395153A (ja) 1991-04-19
EP0405233A1 (en) 1991-01-02
DK0405233T3 (da) 1993-12-20
CA2018848A1 (en) 1990-12-15
ES2059893T3 (es) 1994-11-16
EP0405233B1 (en) 1993-10-27
DE69004164T2 (de) 1994-04-21
US5063247A (en) 1991-11-05
ATE96426T1 (de) 1993-11-15
DE69004164D1 (de) 1993-12-02
AU628583B2 (en) 1992-09-17
AU5700990A (en) 1990-12-20

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