KR960705809A - HIV 프로테아제 억제제의 프로드러그(Prodrugs of an inhibitor of HIV protease) - Google Patents

HIV 프로테아제 억제제의 프로드러그(Prodrugs of an inhibitor of HIV protease)

Info

Publication number
KR960705809A
KR960705809A KR1019960702721A KR19960702721A KR960705809A KR 960705809 A KR960705809 A KR 960705809A KR 1019960702721 A KR1019960702721 A KR 1019960702721A KR 19960702721 A KR19960702721 A KR 19960702721A KR 960705809 A KR960705809 A KR 960705809A
Authority
KR
South Korea
Prior art keywords
treatment
hiv
prodrug
alkyl
infection
Prior art date
Application number
KR1019960702721A
Other languages
English (en)
Inventor
알렉산더 조스
빈드라 딜버
디. 도르시 브루스
제이. 렙타 아놀드
피. 백카 조셉
Original Assignee
도나 엘. 폴락
머크 앤드 캄파니, 인코포레이티드
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
Application filed by 도나 엘. 폴락, 머크 앤드 캄파니, 인코포레이티드 filed Critical 도나 엘. 폴락
Publication of KR960705809A publication Critical patent/KR960705809A/ko

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Classifications

    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
    • C07D213/38—Radicals substituted by singly-bound nitrogen atoms having only hydrogen or hydrocarbon radicals attached to the substituent nitrogen atom
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/04—Immunostimulants

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Immunology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Plant Substances (AREA)

Abstract

아래 일반식(I)의 프로드러그는 다른 항균제, 면역 조절제, 항생제 또는 백신과의 배합과는 무관하게 희석제 중의 화합물, 약제학적으로 허용가능한 염, 약제학적 조성물 중의 한 형태로서 HIV 프로테아제 억제, HIV에 의한 감염의 예방 또는 치료 및 AIDS 치료에 유용하다. AIDS 의 치료 방법 및 HIV 에 의한 감염의 예방 또는 치료 방법이 또한 기술된다.

Description

HIV 프로테아제 억제제의 프로드러그(Prodrugs of an inhibitor of HIV protease)
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (8)

  1. 아래 일반식의 프로드러그 또는 약제학적으로 허용 가능한 이의 염.
    상기 식에서, Y 및 Z는 모두 H가 아니며, 독립적으로 (a) H; (b); (c)(단, Z는알킬-NH2가 아니다) 또는 (d)이며; n 은 0 내지 16이고; R1및 R2는 독립적으로 H ; 하이드록시; 아미노; 페닐; 헤테로사이클; 또는 치환되지 않거나 하이드록시, -COOH, 아미노, 아릴, 케토 또는 헤테로사이클에 의해 치환된 C1-4알킬이며; R3은 H; 또는 치환되지 않거나 아릴, 아미노, -COOH, 케토,알킬 또는알킬에 의해 치환된 C1-4알킬이고; R4는 H, -NR1R2또는 헤테로사이클이다.
  2. 제1항에 있어서, 케토코나졸과 배합된 프로드러그.
  3. 제1항에 있어서, 시메티딘과 배합된 프로드러그.
  4. 제1항에 있어서, 약제학적으로 허용가능한 염이, Y및 Z중의 하나 이상이 숙시네이트, 글루타레이트 또는 아디페이트 에스테르를 형성하도록, 나트륨, 칼륨, 하이드로클로라이드 또는 설페이트 염인 프로드로그.
  5. HIV 프로테아제 억제를 요하는 포유동물에게 제1항의 프로드러그 유효량을 투여함을 포함하여, HIV 프로테아제를 억제하는 방법.
  6. HIV 감염의 예방 또는 HIV에 의한 감염의 치료 또는 AIDS 또는 ARC의 치료를 요하는 포유동물에게 제1항의 프로드로그 유효량을 투여함을 포함하는, HIV 감염의 예방 또는 HIV 에 의한 감염의 치료 또는 AIDS 또는 ARC의 치료 방법.
  7. 제1항의 프로드러그 유효량과 약제학적으로 허용가능한 담체를 포함하는, HIV 프로테아제 억제에 유용한 약제학적 조성물.
  8. 제1항의 프로드러그 유효량과 약제학적으로 허용가능한 담체를 포함하는, HIV 감염의 예방 또는 치료 또는 AIDS 또는 ARC 치료에 유용한 약제학적 조성물.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019960702721A 1993-11-18 1994-11-14 HIV 프로테아제 억제제의 프로드러그(Prodrugs of an inhibitor of HIV protease) KR960705809A (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US15420493A 1993-11-18 1993-11-18
US08/154,204 1993-11-18
PCT/US1994/013085 WO1995014016A1 (en) 1993-11-18 1994-11-14 Prodrugs of an inhibitor of hiv protease

Publications (1)

Publication Number Publication Date
KR960705809A true KR960705809A (ko) 1996-11-08

Family

ID=22550424

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1019960702721A KR960705809A (ko) 1993-11-18 1994-11-14 HIV 프로테아제 억제제의 프로드러그(Prodrugs of an inhibitor of HIV protease)

Country Status (17)

Country Link
US (1) US5733907A (ko)
EP (1) EP0729467A1 (ko)
JP (1) JPH09505303A (ko)
KR (1) KR960705809A (ko)
CN (1) CN1139432A (ko)
AU (1) AU687128B2 (ko)
CA (1) CA2174649A1 (ko)
CZ (1) CZ140696A3 (ko)
FI (1) FI962073A0 (ko)
HU (1) HUT76270A (ko)
IL (1) IL111584A0 (ko)
NO (1) NO962000D0 (ko)
NZ (1) NZ276622A (ko)
PL (1) PL314486A1 (ko)
SK (1) SK61496A3 (ko)
WO (1) WO1995014016A1 (ko)
ZA (1) ZA949127B (ko)

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US6458772B1 (en) 1909-10-07 2002-10-01 Medivir Ab Prodrugs
US6878728B1 (en) 1999-06-11 2005-04-12 Vertex Pharmaceutical Incorporated Inhibitors of aspartyl protease
US20040122000A1 (en) 1981-01-07 2004-06-24 Vertex Pharmaceuticals Incorporated. Inhibitors of aspartyl protease
MY126358A (en) * 1996-03-22 2006-09-29 Glaxo Group Ltd Compositions comprising vx478 and a water soluble tocopherol derivative such as vitamin e-tpgs
AU2012199A (en) * 1997-12-24 1999-07-19 Vertex Pharmaceuticals Incorporated Prodrugs of aspartyl protease inhibitors
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FR2773994B1 (fr) * 1998-01-23 2002-10-11 Univ Nice Sophia Antipolis Prodrogues issues d'anti-proteases inhibitrices du virus de l'immunodeficience humaine (vih) pour l'amelioration de leur biodisponibilite, de leur tropisme vers et/ou de leur delivrance dans le systeme nerveux central
EP1086076B1 (en) 1998-06-19 2004-12-22 Vertex Pharmaceuticals Incorporated Sulfonamide inhibitors of aspartyl protease
TWI260322B (en) 1999-02-12 2006-08-21 Vertex Pharma Inhibitors of aspartyl protease
CN1441790A (zh) * 2000-01-28 2003-09-10 罗姆和哈斯公司 增强性质的药物
US6818787B2 (en) 2001-06-11 2004-11-16 Xenoport, Inc. Prodrugs of GABA analogs, compositions and uses thereof
US7202092B2 (en) * 2001-07-13 2007-04-10 Roche Diagnostics Operations, Inc. Indinavir derivatives useful in immunoassay
EP1485082A4 (en) 2002-02-19 2009-12-30 Xenoport Inc PROCESS FOR THE SYNTHESIS OF PROMEDICAMENTS FROM 1-ACYL-ALKYL DERIVATIVES AND CORRESPONDING COMPOSITIONS
US8603949B2 (en) * 2003-06-17 2013-12-10 California Institute Of Technology Libraries of optimized cytochrome P450 enzymes and the optimized P450 enzymes
US7662987B2 (en) * 2003-07-15 2010-02-16 Xenoport, Inc. Methods for synthesis of acyloxyalkyl compounds
WO2005019163A2 (en) * 2003-08-20 2005-03-03 Xenoport, Inc. Acyloxyalkyl carbamate prodrugs, methods of synthesis and use
EP2371815A1 (en) 2003-12-30 2011-10-05 XenoPort, Inc. Sythesis of acyloxyalkyl carbamate prodrugs and intermediates thereof

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US541168A (en) * 1895-06-18 Frank e
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US4144346A (en) * 1977-01-31 1979-03-13 Janssen Pharmaceutica N.V. Novel 1-(1,3-dioxolan-2-ylmethyl)-1H-imidazoles
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Also Published As

Publication number Publication date
FI962073A (fi) 1996-05-15
JPH09505303A (ja) 1997-05-27
NZ276622A (en) 1997-09-22
FI962073A0 (fi) 1996-05-15
ZA949127B (en) 1996-05-17
HU9601340D0 (en) 1996-07-29
IL111584A0 (en) 1995-01-24
EP0729467A1 (en) 1996-09-04
NO962000L (no) 1996-05-15
CZ140696A3 (en) 1996-12-11
PL314486A1 (en) 1996-09-16
CA2174649A1 (en) 1995-05-26
WO1995014016A1 (en) 1995-05-26
NO962000D0 (no) 1996-05-15
AU687128B2 (en) 1998-02-19
AU1096095A (en) 1995-06-06
SK61496A3 (en) 1996-11-06
US5733907A (en) 1998-03-31
HUT76270A (en) 1997-07-28
CN1139432A (zh) 1997-01-01

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