KR960034178A - 벤자제핀- 벤즈옥사제핀- 및 벤조티아제핀-n- 아세트산 유도체와 그 제조방법 및 그들을 함유한 약제학적 조성물 - Google Patents

벤자제핀- 벤즈옥사제핀- 및 벤조티아제핀-n- 아세트산 유도체와 그 제조방법 및 그들을 함유한 약제학적 조성물 Download PDF

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KR960034178A
KR960034178A KR1019960007794A KR19960007794A KR960034178A KR 960034178 A KR960034178 A KR 960034178A KR 1019960007794 A KR1019960007794 A KR 1019960007794A KR 19960007794 A KR19960007794 A KR 19960007794A KR 960034178 A KR960034178 A KR 960034178A
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hydrogen
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발데크 하랄드
휠트제 다크마르
메싱거 요제프
안텔 요헨
부를 미하일
토르멜렌 딜크
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디터 라우어
칼리-케미 파마 게엠베하
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/14—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D223/16—Benzazepines; Hydrogenated benzazepines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10—Antioedematous agents; Diuretics
    • 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
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
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Abstract

NEP-억제효과를 갖는 하기 일반식(Ⅰ)의 화합물 및 생리적으로 내성을 갖는 그의 염.
여기에서 R1은 저급알콕시라디칼이 저급알콕시기로 치환되는 저급 알콕시-저급-알킬기이거나, 페닐고리에서 저급알킬, 저급알콕시 또는 할로겐으로 선택적 치환이 가능한 페닐-저급-알킬기 또는 페닐옥시-저급 알킬기이거나, 또는 나프틸-저급-알킬기이며, A는 CH2, O 또는 S이며, R2는 수소 또는 할로겐이며, R3는 수소 또는 할로겐이며, R4는 수소 또는 생체내 가변성 에스테르를 형성하는 기이고, R5는 수소 또는 생체내 가변성 에스테르를 형성하는 기이다.

Description

벤자제핀- 벤즈옥사제핀- 및 벤조티아제핀-N-아세트산 유도체와 그 제조방법 및 그들을 함유한 약제학적 조성물
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (8)

  1. 하기 일반식(Ⅰ)로 표시되는 화합물 및 생리학적으로 내성을 갖는 그의 염
    여기에서 R1은 저급알콕시라디칼이 저급알콕시기로 치환되는 저급 알콕시-저급-알킬기이거나, 페닐고리에서 저급알킬, 저급알콕시 또는 할로겐으로 선택적 치환이 가능한 페닐-저급-알킬기 또는 페닐옥시-저급-알킬기이거나, 또는 나프틸-저급-알킬기이며, A는 CH2, O 또는 S이며, R2는 수소 또는 할로겐이며, R3는 수소 또는 할로겐이며, R4는 수소 또는 생체내 가변성 에스테르를 형성하는 기이고, R5는 수소 또는 생체내 가변성 에스테르를 형성하는 기이다.
  2. 제1항에 있어서, R4및/또는 R5가 생체내 가변성 에스테르를 형성하는 기인 것을 특징으로 하는 화합물.
  3. 상기 전 청구항 중 어느 한 항에서, 생체내 가변성 에스테를 형성하는 기는 저급알킬기, 페닐고리에서 저급알킬기 또는 인접한 두 탄소원자들과 결합한 저급 알킬렌 사슬로 선택적으로 치환되는 페닐 또는 페닐-저급-알킬기 특히, 페닐, 벤질 또는 인도닐, 디옥솔란 고리에서 저급알킬로 선택적으로 치환되는 디옥솔라닐메틸기 특히, (2,2-디메틸-1,3-디옥솔란-4-일)메틸 또는 옥시메틸기상에서 저급알킬로 선택적으로 치환되는 C2-C6-알카노일옥시메틸기인 것을 특징으로 하는 화합물.
  4. 상기 전 청구항 중 어느 한 항에 있어서, R4는 생체내 가변성 에스테르를 형성하는 기이고, R5는 수소인 것을 특징으로 하는 화합물.
  5. 상기 전 청구항 중 어느 한 항에 있어서, A는 CH2인 것을 특징으로 하는 화합물.
  6. 제5항에 있어서, R1은 펜에틸기 또는 나프틸에틸기이고 R2는 수소인 것을 특징으로 하는 화합물.
  7. 약리학적 유효량의 제1항에 따른 화합물 및 통상의 약제학적 보조물질 및/또는 부형제들을 함유하는 약제.
  8. 하기 일반식(Ⅱ)의 산 또는 그의 반응성산유도체와 하기 일반식(Ⅲ)의 아민이 반응하여 하기 일반식(Ⅳ)의 아미드가 생성되며, 하기 일반식(Ⅳ)의 화합물에 있는 산보호기 R4aR5a가 생체내 가변성 에스테르를 형성하는 기가 아니면 이들은 적당한 순서에서 동시에 또는 연속적으로 제거되며, 필요하다면 비보호 산성기는 하기 일반식(Ⅴ)의 알코올 또는 상응하는 하기 일반식(Ⅴ)의 반응성유도체와 에스테르화반응하며, 필요하다면 생성된 하기 일반식(Ⅰ)의 산이 생리학적으로 내성인 그의 염으로 전환되거나 하기 일반식(Ⅰ)의산의 염이 유리 산으로 전환되는 것을 특징으로 하는 하기 일반식(Ⅰ)의 화합물 및 생리학적으로 내성을 갖는 그의 염의 제조방법.
    여기에서 R1은 저급 알콕시 라디칼이 저급알콕시기로 치환되는 저급 알콕시-저급-알킬기이거나, 페닐고리에서 저급알킬, 저급알콕시 또는 할로겐으로 선택적 치환이 가능한 페닐-저급-알킬기 또는 페닐옥시-저급 알킬기이거나, 또는 나프틸-저급-알킬기이며, A는 CH2, O 또는 S이며, R2는 수소 또는 할로겐이며, R3는 수소 또는 할로겐이며, R4는 수소 또는 생체내 가변성 에스테르를 형성하는 기이고, R5는 수소 또는 생체내 가변성 에스테르를 형성하는 기이며,
    여기에서 R1은 상기한 바와 같고 R4a는 산보호기이며,
    여기에서 R2, R3및 A는 상기한 바와 같고 R5a는 산보호기이며,
    여기에서 R1, R2, R3, R4a, R5a및 A는 상기한 바와 같고,
    여기에서 R6은 생체내 가변성 에스테르를 형성하는 기이고 X는 제거될 수 있는 반응성기이다.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019960007794A 1995-03-23 1996-03-21 벤자제핀-,벤즈옥사제핀-및벤조티아제핀-n-아세트산유도체와그제조방법및그들을함유한약제학적조성물 KR100482499B1 (ko)

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DE19510566A DE19510566A1 (de) 1995-03-23 1995-03-23 Benzazepin-, Benzoxazepin- und Benzothiazepin-N-essigsäurederivate sowie Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel
DE19510566.4 1995-03-23

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KR100710548B1 (ko) * 2002-12-26 2007-04-24 에스케이 주식회사 (ｓ)-3-아미노-2,3,4,5-테트라히드로-2-옥소-1Ｈ-1-벤자제핀-1-아세트산 및 이의 에스테르 화합물의 제조방법
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