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KR940014337A - 에이즈의 치료에 유용한 에이치아이브이(hiv) 프로테아제 억제제 - Google Patents

에이즈의 치료에 유용한 에이치아이브이(hiv) 프로테아제 억제제 Download PDF

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Publication number
KR940014337A
KR940014337A KR1019930029121A KR930029121A KR940014337A KR 940014337 A KR940014337 A KR 940014337A KR 1019930029121 A KR1019930029121 A KR 1019930029121A KR 930029121 A KR930029121 A KR 930029121A KR 940014337 A KR940014337 A KR 940014337A
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KR
South Korea
Prior art keywords
alkyl
heterocycle
aryl
hydroxy
pharmaceutically acceptable
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KR1019930029121A
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English (en)
Inventor
니콜라우스 정하임 루이스
알란 셰퍼드 티모시
Original Assignee
피터 지. 스트링거
일라이 릴리 앤드 캄파니
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from US08/134,329 external-priority patent/US5733906A/en
Application filed by 피터 지. 스트링거, 일라이 릴리 앤드 캄파니 filed Critical 피터 지. 스트링거
Publication of KR940014337A publication Critical patent/KR940014337A/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
    • C07D215/58—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems with hetero atoms directly attached to the ring nitrogen atom
    • C07D215/60—N-oxides
    • 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
    • C07D217/26—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

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Virology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Oncology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Communicable Diseases (AREA)
  • Animal Behavior & Ethology (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)

Abstract

본 발명은 신규 HIV 프로테아제 억제제, 이러한 화합물을 함유한 약학적 제형, 및 HIV 감염 및/또는 AIDS의 치료 및/또는 예방법을 제공한다.

Description

에이즈의 치료에 유용한 에이치아이브이(HIV) 프로테아제 억제제
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (4)

  1. 하기 일반식(Ⅰ)의 화합물 또는 그의 약학적으로 허용가능한 염 :
    상기식에서, R은 하기 일반식을 갖는 그룹이고 ;
    R2는 아미노산 측쇄 또는 -(CH2)y-X-R2a이고 ; y는 0, 1 또는 2이고 ; X는 결합, 이가(C2내지 C4)알케닐, 이가(C2내지 C4)알키닐, -C(O)-O-, -0-C(O)-, -C(O)-NR2b-, NR2b-C(O)-, -NR2b-, -C(O)-, -O-, -S-, -S(O)- 또는 -S(O)2- 이고 ; R2a는 아릴, 불포화 헤테로사이클, 헤테로사이클, 아릴(C1, 내지 C4)알킬, 불포화 헤테로사이클(C1내지 C4)알킬, 헤테로사이클(C1내지 C4)알킬, 테트라졸릴, N-(C1내지 C4)알킬테트라졸릴 또는 N-(아릴)테트라졸릴이고 ; R2b는 수소 또는 C1내지 C4알킬이고 ; R0는 수소, 카바모일, 포르밀, C2내지 C6알카노일, C1내지 C4알콕시카보닐, -C(O)CF3또는 -S(O)2-Z 이고 ; Z는 C1 내지 C6알킬, 아미노, C1내지 C4알킬아미노, 트리플루오로메틸 또는 디(C1내지 C4)알킬아미노이고; 비대칭 탄소 σ는 자연 발생적이 아닌 형태이고 ; R1는 아릴, C5내지 C7사이클로알킬 또는 -S-R1x(이때, R1x는 아릴 또는 C5내지 C7사이클로알킬이다)이고 ; A는 -CH2-또는이고 ; Y1은 헤테로사이클이고 ; R3은
    p는 4 또는 5이고 ; R4는 각각의 경우 독립적으로, 수소, C1내지 C6알킬 또는 하이드록시(C1내지 C4)알킬이고 ; R5및 R6은 독립적으로 수소, 하이드록시, C1내지 C6알킬, C1내지 C6알콕시, 아미노, C1내지 C4알킬아미노, 하이드록시(C1내지 C4)-알킬, 카복시, C1내지 C4알콕시카보닐, 카바모일, N-(C1내지 C4)알킬카바모일, 아릴, 헤테로사이클 또는 불포화 헤테로사이클 중에서 선택된다.
  2. 제 1 항에 있어서, R1a, Y1, R5또는 R6중 어느 하나가 헤테로사이클일 때, 헤테로사이클이 -(CH2)4-피리딜로 치환될 수 없는 화합물 또는 그의 약학적으로 허용되는 염.
  3. [2R-(2R*, 3S*, 6S*, 3'S*, 4a'S*, 8a'S*)]-N-(t-부틸)-2′-[2-하이드록시-3-페닐메틸-4-아자-5-옥소-6-N(메틸설포닐)-아미노-7-p-플루오로-페닐셜포닐]헵틸 데카하이드로이소퀴놀린-3'-카복스아미드 메탄설포네이트 ; 또는 [2R-(2R*, 3S*, 6S*, 3'S*, 4a'S*, 8a'S*)]-N-(t-부틸)-2′-[2-하이드록시-3-페닐메틸-4-아자-5-옥소-6-N(메틸설포닐9 아미노-7-나프트-2-일설포닐]헵틸 데카하이드로이소퀴놀린-3′-카복스아미드 또는 그의 약학적으로 허용되는 염.
  4. 제 1 내지 3항 중 어느 한 항에 청구된 일반식(Ⅰ)의 화합물 또는 그의 약학적으로 허용되는 염을 그에 대한 하나 이상의 약학적으로 허용되는 담체, 부형제 또는 희석제와 함께 포함하는 약학제제.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019930029121A 1992-12-22 1993-12-22 에이즈의 치료에 유용한 에이치아이브이(hiv) 프로테아제 억제제 KR940014337A (ko)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US99525692A 1992-12-22 1992-12-22
US7/995,256 1992-12-22
US08/134,329 US5733906A (en) 1993-10-12 1993-10-12 Inhibitors of HIV Protease useful for the treatment of Aids
US8/134,329 1993-10-12

Publications (1)

Publication Number Publication Date
KR940014337A true KR940014337A (ko) 1994-07-18

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Country Status (21)

Country Link
US (1) US5905077A (ko)
EP (1) EP0604185B1 (ko)
JP (1) JPH06271534A (ko)
KR (1) KR940014337A (ko)
CN (1) CN1044117C (ko)
AT (1) ATE178055T1 (ko)
AU (1) AU667146B2 (ko)
BR (1) BR9305162A (ko)
CA (1) CA2112042A1 (ko)
CZ (1) CZ281493A3 (ko)
DE (1) DE69324120T2 (ko)
ES (1) ES2132201T3 (ko)
FI (1) FI935778A (ko)
HU (1) HUT69693A (ko)
IL (1) IL108092A (ko)
MX (1) MX9308016A (ko)
MY (1) MY131388A (ko)
NO (1) NO934719L (ko)
NZ (1) NZ250491A (ko)
PL (1) PL301581A1 (ko)
TW (1) TW262468B (ko)

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MX9308016A (es) 1994-08-31
NZ250491A (en) 1995-08-28
IL108092A0 (en) 1994-04-12
JPH06271534A (ja) 1994-09-27
FI935778A0 (fi) 1993-12-21
NO934719L (no) 1994-06-23
ES2132201T3 (es) 1999-08-16
CA2112042A1 (en) 1994-06-23
EP0604185A1 (en) 1994-06-29
CZ281493A3 (en) 1994-07-13
NO934719D0 (no) 1993-12-20
DE69324120T2 (de) 1999-11-25
TW262468B (ko) 1995-11-11
ATE178055T1 (de) 1999-04-15
EP0604185B1 (en) 1999-03-24
BR9305162A (pt) 1994-11-01
US5905077A (en) 1999-05-18
HUT69693A (en) 1995-09-28
AU667146B2 (en) 1996-03-07
FI935778A (fi) 1994-06-23
MY131388A (en) 2007-08-30
AU5252893A (en) 1994-07-07
PL301581A1 (en) 1994-06-27
DE69324120D1 (de) 1999-04-29
CN1044117C (zh) 1999-07-14
IL108092A (en) 1998-06-15
CN1094399A (zh) 1994-11-02

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