KR940005620A - 에이즈의 치료에 유용한 에이치아이브이(hiv) 프로테아제 억제제 - Google Patents

에이즈의 치료에 유용한 에이치아이브이(hiv) 프로테아제 억제제 Download PDF

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KR940005620A
KR940005620A KR1019930011214A KR930011214A KR940005620A KR 940005620 A KR940005620 A KR 940005620A KR 1019930011214 A KR1019930011214 A KR 1019930011214A KR 930011214 A KR930011214 A KR 930011214A KR 940005620 A KR940005620 A KR 940005620A
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heterocycle
alkyl
aryl
cycloalkyl
unsaturated heterocycle
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에드윈 먼로 존
조셉 호른백 윌리암
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리로이 휘테커
일라이 릴리 앤드 캄파니
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    • 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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    • C07K5/021—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)n-C(=0)-, n being 5 or 6; for n > 6, classification in C07K5/06 - C07K5/10, according to the moiety having normal peptide bonds
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    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • D—TEXTILES; PAPER
    • D02—YARNS; MECHANICAL FINISHING OF YARNS OR ROPES; WARPING OR BEAMING
    • D02G—CRIMPING OR CURLING FIBRES, FILAMENTS, THREADS, OR YARNS; YARNS OR THREADS
    • D02G3/00—Yarns or threads, e.g. fancy yarns; Processes or apparatus for the production thereof, not otherwise provided for
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Abstract

본 발명은 하기 일반식(Ⅰ)의 화합물 또는 그의 약학적으로 허용가능한 염인 신규한 HIV 프로테아제 억제제, 상기 화합물을 함유하는 약학 조성물 및 그의 사용방법을 제공한다.
상기식에서, R은 C1-C6알킬, 사이클로알킬, 헤테로사이클, 불포화 헤테로 사이클, 아릴, 사이클로아릴(C1-C4)알킬, 헤테로사이클(C1-C4)알킬, 불포화 헤테로사이클(C1-C4)알킬, 아릴(C1-C4)알킬 또는 일반식 -A-(CH2)a-R0를 갖는 구조이고, 이때 A는 -0-, -NH- 또는 -S-이고, q는 0,1,2 또는 3이고. R0는 사이클로알킬, 아릴, 헤테로사이클 또는 불포화 헤테로사이클이고, X는이고, 여기에서 R1은 아릴, 사이클로알킬, 헤테로사이클 또는 불포화 헤테로사이클이고, R2는 수소 또는 C1-C4알킬이고, R3는 아미노산 측매 -CH2CH3, -CH2CH2CH3, -CH2(CH2)2CH3, -C(CH3)3, 시아노(C1-C4)알킬, 불포화 헤테로사이클(C1-C4)알킬, 아릴(C1-C4) 알킬 또는 -(CH2)3-AO-(CH2)r-R4또는 -CH-C(0)-NR2-(CH2)-r-R5를 갖는 구조이고, 이때 s는 1,2,3 또는 4이고, r은 0,1,2 또는 3이고, AO는 -0-, -NH- 또는 -S- 이고, R4는 C1-C8알킬, 사이클로알킬, 아릴, 헤테로사이클 또는 불포화 헤테로사이클이고, R5는 사이클로알킬, 아릴, 헤테로사이클 또는 불포화 헤테로사이클이고, j는 0, 1, 2, 3 또는 4이고, k는 0 또는 1이고, Y는 -0-, -N(R2)- 또는 -S-이다.

Description

에이지의 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 C1-C6알킬, 사이클로알킬, 헤테로사이클, 불포화 헤테로 사이클, 아릴, 사이클로아릴(C1-C4)알킬, 헤테로사이클(C1-C4)알킬, 불포화 헤테로사이클(C1-C4)알킬, 아릴(C1-C4)알킬 또는 일반식 -A-(CH2)q-R0를 갖는 구조이고, 이때 A는 -0-, -NH- 또는 -S-이고, q는 0,1,2 또는 3이고, R0는 사이클 로알킬, 아릴, 헤테로사이클 또는 불포화 헤테로사이클이고, X는
    이고, 여기에서 R1은 아릴, 사이클로알킬, 헤테로사이클 또는 불포화 헤테로사이클이고, R2는 수소 또는 C1-C4알킬이고, R3는 아미노산 촉매 -CH2CH3, -CH2CH2CH2, -CH2(CH2)2CH3, -C(CH3)3, 시아노(C1-C1)알킬, 불포화 헤테로사이클(C1-C4)알킬, 아릴(C1-C4) 알킬 또는 -(CH2)3-A0-(CH2)r-R4또는 -CH-C(0)-NR2-(CH2)-r-R5를 갖는 구조이고, 이때 s는 1,2,3 또는 4이고, r은 0,1,2 또는 3이고, A0는 -0-, -NH- 또는 -S- 이고, R4는 C1-C8알킬, 사이클로알킬, 아릴, 헤테로사이클 또는 불포화 헤테로사이클이고, R5는 사이클로알킬, 아릴, 헤테로사이클 또는 불포화 헤테로사이클이고, j는 0,1,2,3 또는 4이고, k는 0또는 1이고, Y는 -0-, -N(R2)- 또는 -S-이다.
  2. 제1항에 있어서, X가이고, 상기식에서, R1은 아릴 또는 불포화 헤테로사이클이고, j는 0.1 또는 2이고, Y는 -0- 또는 -N(R2)-이고, k는 1이고, R2는 수소 또는 메틸이고, R3는 아미노산 측쇄 -CH2CH3, -CH2CH2CH2, -CH2(CH2)2CH3, -C(CH3)3또는 일반식 -CH2-C(O)-NR2-(CH2)r-R5이고, 이때, r은 0,1,2 또는 2이고, R5는 사이클로알킬 아릴 헤테로사이클 또는 불포화 헤테로사이클이고, R이 아릴, 아릴(C1-C4)알킬 또는 일반식 -A-(CH2)q-R0이고, 이때 A는 -S-이고, q는 0이고, R0는 아릴인 화합물 또는 그의 약학적으로 허용가능한 염.
  3. 1,6-디페닐-2(S),5(S)-디(N-[2(S)-N[(퀴놀린-2-일메특시)가보닐]아미노부다노일]아미노]-3,4-시스-에폭시헥산, 1,6-디페닐-2(S),5(S)-디[N-[2(S)-N[[N(메틸)-N(퀴놀린-2-일메틸)아미노]카보닐]아미노부타노일]아미노]3,4-시스-에폭시헥산, 1,6-디페닐-2(S),5(S)-디[N-[2(S)-N[8-플루오로퀴놀린-2-일메톡시)카보닐]아미노-3-메틸부타노일]아미노]-3,4-시스-에폭시헥산, 1,10-디페닐-4(S),7(S)-디[N-2(S)-N[[N(메틸)-N(퀴놀린-2-일메틸)아미노]카보닐]아미노부타노일]아미노]-5,6-시스-에폭시데칸, 또는 그의 약학적으로 허용가능한 염.
  4. 하나 이상의 약학적으로 허용가능한 담체, 부형제 또는 희석제와 함께 제1항 내지 제3항중 어느 한 항에 청구된 일반적(I)의 화합물 또는 그의 약학적으로 허용가능한 염을 포함하는 약학 조성물.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019930011214A 1992-06-19 1993-06-18 에이즈의 치료에 유용한 에이치아이브이(hiv) 프로테아제 억제제 KR940005620A (ko)

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KR1019930011216A KR940000634A (ko) 1992-06-18 1993-06-18 폴리아미드 기재 연속 필라멘트의 토우 및 이의 제조방법

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US6071895A (en) 1992-03-11 2000-06-06 Narhex Limited Polar-substituted hydrocarbons
BR9306058A (pt) 1992-03-11 1997-11-18 Narhex Ltd Derivados de amina de hidrocarbonetos oxo- e hidroxi- substituidos
CZ184194A3 (en) * 1993-08-09 1995-03-15 Lilly Co Eli Aspartylprotease inhibitor and method of identifying thereof
KR0159652B1 (ko) * 1995-10-26 1998-12-01 성재갑 항 에이즈 효과를 갖는 비가역적 인간 면역 결핍 바이러스 프로테아제 저해제 및 그의 제조방법
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FI932847A (fi) 1993-12-20
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AU4135493A (en) 1993-12-23
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CZ113393A3 (en) 1994-03-16
HU9301795D0 (en) 1993-09-28
US5578608A (en) 1996-11-26
EP0575097A1 (en) 1993-12-22
EP0575097B1 (en) 2000-11-02
MX9303572A (es) 1994-01-31
DE69329606D1 (de) 2000-12-07
ES2152241T3 (es) 2001-02-01
NO932130D0 (no) 1993-06-10
PL299369A1 (en) 1993-12-27
HUT67571A (en) 1995-04-28
IL105973A0 (en) 1993-10-20
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AU663958B2 (en) 1995-10-26
BR9302389A (pt) 1994-01-11
CO4130200A1 (es) 1995-02-13
FI932847A0 (fi) 1993-06-18
JPH0656812A (ja) 1994-03-01
CA2098165A1 (en) 1993-12-20
YU42893A (sh) 1996-07-24
CN1082035A (zh) 1994-02-16
TW218873B (ko) 1994-01-11
NO932130L (no) 1993-12-20

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