KR960022469A - 항 에이즈 효과를 갖는 hiv 프로테아제 억제제 - Google Patents

항 에이즈 효과를 갖는 hiv 프로테아제 억제제 Download PDF

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KR960022469A
KR960022469A KR1019940033271A KR19940033271A KR960022469A KR 960022469 A KR960022469 A KR 960022469A KR 1019940033271 A KR1019940033271 A KR 1019940033271A KR 19940033271 A KR19940033271 A KR 19940033271A KR 960022469 A KR960022469 A KR 960022469A
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South Korea
Prior art keywords
compound
formula
lower alkyl
butyl
amino
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KR1019940033271A
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English (en)
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KR0140308B1 (ko
Inventor
윤흥식
박지효
최호일
손영찬
이창선
김성천
고종성
최낙현
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성재갑
주식회사 Lg 화학
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Priority to KR1019940033271A priority Critical patent/KR0140308B1/ko
Publication of KR960022469A publication Critical patent/KR960022469A/ko
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

본 발명은 하기 일반식(Ⅰ)으로 표시되는 신규 화합물, 이의 제조방법 및 상기 화합물을 유효성분으로 포함 하는 에이즈 치료제로 유용한 약학적 주성물을 제공한다;
상기 식에서, R1은 저급일킬, 저급알킬로 치환된 방향족, NH2또는 OH이며, R2와 R3는 각각 독립적으로 수소 또는 저급 알킬이고, n은 0, 1 또는 2이며, X는 작용화된 아실이다.

Description

항 에이즈 효과를 갖는 HIV 프로테아제 억제제
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (5)

  1. 하기 일반식(Ⅰ)로 표시되는 화합물 또는 이의 약제학적으로 허용되는 염;
    상기 식에서, R1은 저급일킬, 저급알킬로 치환된 방향족, NH2또는 OH이며, R2와 R3는 각각 독립적으로 수소 또는 저급 알킬이고, n은 0, 1 또는 2이며, X는 작용화된 아실이다.
  2. 제1항에 있어서, X는 하기 일반식(Ⅱ)로 표시되는 작용화된 아실인 화합물 또는 이의 약제학적으로 허용 되는 염;
    상기 식에서, Y는 O, NH 또는 NCH3이고, R4는 저급알킬이며, R5는 저급알킬 또는 질소원자가 포함되거나 포함되지 않은 방향족이다.
  3. 제2항에 있어서, N-t-부틸-데카히드로-2-[2(R)-히드록시-4-페닐-3(S)-[[[(N-벤질옥시카르보닐)아미노-β-메탄술포닐-L-발리닐]아미노]부틸]-(4aS,8aS)-이소퀴놀린-3(S)-카복사미드; N-t-부틸-테카히드로-2-[2(R)-히드록시-4-페닐-3(S)-[[[(N-퀴놀릴카르보닐)아미노-β-메탄술포닐-L-발리닐]아미노]부틸]-(4aS,8aS)-이소퀴놀린-3(S)-카복사미드;또는 N-t-부틸-데카히드로-2-[2(R)-히드록시-4-페닐-3(S)-[[[N-(5-히드록시이소퀴놀리놀메틸카르보닐)]아미노-3(S)-카복사미드, 또는 이의 약제학적으로 허용되는 염.
  4. 하기 일반식(Ⅲ)의 화합물을 아미드 커플링 반응시켜 일반식(Ⅳ)의 화합물을 제조하고; 일반식(Ⅳ)의화합물을 산화반응시켜 일반식(Ⅴ)의 화합물을 제조하고; 일반식(Ⅴ)의화합물을 탈보호기 반응시켜 일반식(Ⅵ)의 화합물을 제조하고; 일반식(Ⅵ)의 화합물을 아미드 커플링 반응시킴을 포함하는, 하기 일반식(Ⅰ')화합물의 제조방법;
    상기 식에서, R1, R2, R3및 X는 제1항에서 정의한 바와 같고, Cbz는 벤질옥시 카르보닐을 나타낸다.
  5. 제1항 내지 제3항 중 어느 한 항의 화합물 또는 그의 약제학적으로 허용되는 염을 유효성분으로 포함하는 항 에이즈 효과를 갖는 약학적 조성물.
    ※ 참고사항:최초출원 내용에 의하여 공개하는 것임.
KR1019940033271A 1994-12-08 1994-12-08 항 에이즈 효과를 갖는 hiv 프로테아제 억제제 KR0140308B1 (ko)

Priority Applications (1)

Application Number Priority Date Filing Date Title
KR1019940033271A KR0140308B1 (ko) 1994-12-08 1994-12-08 항 에이즈 효과를 갖는 hiv 프로테아제 억제제

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
KR1019940033271A KR0140308B1 (ko) 1994-12-08 1994-12-08 항 에이즈 효과를 갖는 hiv 프로테아제 억제제

Publications (2)

Publication Number Publication Date
KR960022469A true KR960022469A (ko) 1996-07-18
KR0140308B1 KR0140308B1 (ko) 1998-06-15

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KR1019940033271A KR0140308B1 (ko) 1994-12-08 1994-12-08 항 에이즈 효과를 갖는 hiv 프로테아제 억제제

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