KR920009394A - 상승작용성 hiv 역전사 효소 억제제 - Google Patents

상승작용성 hiv 역전사 효소 억제제 Download PDF

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KR920009394A
KR920009394A KR1019910019380A KR910019380A KR920009394A KR 920009394 A KR920009394 A KR 920009394A KR 1019910019380 A KR1019910019380 A KR 1019910019380A KR 910019380 A KR910019380 A KR 910019380A KR 920009394 A KR920009394 A KR 920009394A
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methyl
ethyl
pyridinone
amino
group
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KR1019910019380A
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에이. 프리드만 폴
에이. 에미니 에밀리오
넌버그 잭
씨. 퀸터로 줄리오
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제임스 에프. 너튼
머크 앤드 캄파니, 인코포레이티드
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Publication of KR920009394A publication Critical patent/KR920009394A/ko

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • 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
    • 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
    • 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

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

Abstract

내용 없음

Description

상승작용성 HIV 역전사 효소 억제제
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (9)

  1. 3-{〔(4,7-디클로로벤즈옥사졸-2)메틸〕아미노}-5-에틸-6-메틸-2-(1H)-피리디논, 3-{〔(4,7-디메틸벤즈옥사졸-2-일)메틸〕아미노}-5-에틸-6-메틸-2-(1H)-피리디논, 3-{〔(7-클로로벤즈옥사졸-2-일)메틸〕아미노}-5-에틸-6-메틸-2-(1H)-피리디논, 3-{〔(7-메틸벤즈옥사졸-2-일)메틸〕아미노}-5-에틸-6-메틸-2-(1H)-피리디논, 3-{〔(4-플로로벤즈옥사졸-2-일)메틸〕아미노}-5-에틸-6-메틸-2-(1H)-피리디논, 3-{〔(벤즈옥사졸-2-일)메틸〕아미노}-5-에틸-6-메틸-2-(1H)-피리디논, 3-{〔(4-클로로벤즈옥사졸-2-일)메틸〕아미노}-5-에틸-6-메틸-2-(1H)-피리디논, 3-{〔(4-플루오로-7-클로로벤즈옥사졸-2-일)메틸〕아미노}-5-에틸-6-메틸-2-(1H)-피리디논,
    3-〔2-(벤즈옥사졸-2-일)에틸〕-5-에틸-6-메틸-2-(1H)-피리디논, 3-〔N-(5-에틸-2-메톡시-6-메틸-2-피리딜메틸)아미노〕-5-에틸-6-메틸-2(1H)-피리디논, 3-〔N-(5,6-디메틸-2-메톡시-3-피리딜메틸)아미노〕-5-에틸-6-메틸-2(1H)-피리디논, 3-〔N-(5-에틸-2-메톡시벤질)아미노〕-5-에틸-6-메틸-2(1H)-피리디논, 3-〔N-(2-메톡시-4,5-디메틸벤질)아미노〕-5-에틸-6-메틸-2(1H)-피리디논 또는 3-〔N-(2,6-디메톡시벤질)아미노〕-5-에틸-6-메틸-2(1H)-피리디논으로 필수적으로 구성된 그룹 A의 화합물와 3'-아지도-2,3'-디데옥시티미딘, 2',3'-디데옥시시티딘, 2',3'-디데옥시이노신, 2',3'-디데하이드로-2',3'-디데옥시티미딘, 1-〔(2-하이드록시에톡시)메틸〕-6-페닐-티오티민 또는 3'-플루오로-2',3'-디데옥시티미딘으로 필수적으로 구성된 그룹 B의 화합물을 상승작용성 배합물 및 이의 약제학적으로 허용되는 염, 수화물 또는 에스테르.
  2. 제1항에 있어서, 그룹 A가 3-{〔(4,7-디클로로벤즈옥사졸-2-일)메틸〕아미노}-5-에틸-6-메틸-2-(1H)-피리디논 또는 3-{〔(4,7-디메틸벤즈옥사졸-2-일)메틸〕아미노}-5-에틸-6-메틸-2-(1H)-피리디논으로 필수적으로 구성되고 그룹B가 3'-아지도-2',3'-디데옥시티미딘 또는 2',3'-디데옥시이노신으로 필수적으로 구성되는 배합물 및 이의 약제학적으로 허용되는 염.
  3. 제1항에 있어서, 그룹 A가 3-{〔(4,7-디클로로벤즈옥사졸-2-일)메틸〕아미노}-5-에틸-6-메틸-2-(1H)-피리디논으로 필수적으로 구성되고 그룹 B가 3'-아지도-2,3'-디데옥시티미딘으로 필수적으로 구성되는 배합물 및 이의 약제학적으로 허용되는 염, 수화물 또는 에스테르.
  4. 제1항에 있어서, 그룹 A가 3-{〔(4,7-디메틸벤즈옥사졸-2-일)메틸〕아미노}-5-에틸-6-메틸-2-(1H)-피리디논으로 필수적으로 구성되고 그룹 B가 3'-아지도-2,3'-디데옥시티미딘으로 필수적으로 구성되는 배합물 및 이의 약제학적으로 허용되는 염, 수화물 또는 에스테르.
  5. 제1항에 있어서, 그룹 A가 3-{〔(4,4-디메틸벤즈옥사졸-2-일)메틸〕아미노}-5-에틸-6-메틸-2-(1H)-피리디논으로 필수적으로 구성되고 그룹 B가 3'-아지도-2,3'-디데옥시티미딘으로 필수적으로 구성되는 배합물 및 이의 약제학적으로 허용되는 염, 수화물 또는 에스테르.
  6. 유효량의 제1항 내지 5항중 어느 한 항에 따른 배합물을 포유동물에 투여함을 특징으로 하여, HIV 역전사효소를 상승작용적으로 억제하는 방법.
  7. 유효량의 제1항 내지 5항중 어느 한 항에 따른 배합물을 포유동물에 투여함을 특징으로 하여, HIV 감염을 예방하거나, HIV 감염을 치료하거나, AIDS 또는 ARC를 치료하는 방법.
  8. 유효량의 제1항 내지 5항중 어느 한 항에 따른 배합물 및 약제학적으로 허용되는 담체를 함유함을 특징으로 하는 HIV 역전사효소를 상승작용적으로 억제시키는데 유용한 약제조성물.
  9. 유효량의 제1항 내지 5항중 어느 한 항에 따른 배합물 및 약제학적으로 허용되는 담체를 함유함을 특징으로 하는, HIV의 감염을 억제하거나 치료하거나, AIDS 또는 ARC 를 치료하는데 유용한 약제 조성물.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019910019380A 1990-11-01 1991-11-01 상승작용성 hiv 역전사 효소 억제제 KR920009394A (ko)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US60810490A 1990-11-01 1990-11-01
US07/608,104 1990-11-01
US64585791A 1991-01-25 1991-01-25
US07/645857 1991-01-25

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KR920009394A true KR920009394A (ko) 1992-06-25

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EP (1) EP0484071A3 (ko)
JP (1) JPH04300834A (ko)
KR (1) KR920009394A (ko)
CN (1) CN1062138A (ko)
AU (1) AU648121B2 (ko)
CA (1) CA2054529A1 (ko)
CS (1) CS331091A3 (ko)
FI (1) FI915152A (ko)
HU (1) HUT60135A (ko)
IE (1) IE913751A1 (ko)
IL (1) IL99843A0 (ko)
MX (1) MX9101880A (ko)
NZ (1) NZ240407A (ko)
PT (1) PT99394A (ko)
YU (1) YU172991A (ko)

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US6177435B1 (en) 1992-05-13 2001-01-23 Glaxo Wellcome Inc. Therapeutic combinations
GB9215176D0 (en) * 1992-07-16 1992-08-26 Glaxo Group Ltd Antiviral combinations
IL106507A (en) * 1992-08-07 1997-11-20 Merck & Co Inc Pharmaceutical compositions containing benzoxazinones and some novel compounds of this type
WO1994018963A1 (en) * 1993-02-22 1994-09-01 Janssen Pharmaceutica N.V. Method of reversing resistance of hiv-1 strains to zidovudine
US5968910A (en) * 1994-11-30 1999-10-19 Jan M. R. Balzarini Compositions containing two or three inhibitors of different HIV reverse transcriptases
EP0906756A4 (en) * 1996-04-04 2000-11-22 Shionogi & Co ANTI-HIV COMPOSITION CONTAINING IMIDAZOLE DERIVATIVE
US6469006B1 (en) * 1999-06-15 2002-10-22 Bristol-Myers Squibb Company Antiviral indoleoxoacetyl piperazine derivatives
NL1012825C2 (nl) * 1999-08-13 2001-02-23 Faculteit Geneeskunde Universi Farmaceuticum voor de behandeling van virale infecties in het bijzonder van het humane immunodeficiency virus (HIV).
US6476034B2 (en) 2000-02-22 2002-11-05 Bristol-Myers Squibb Company Antiviral azaindole derivatives
US6573262B2 (en) 2000-07-10 2003-06-03 Bristol-Myers Sqibb Company Composition and antiviral activity of substituted indoleoxoacetic piperazine derivatives
US20030207910A1 (en) 2001-02-02 2003-11-06 Tao Wang Composition and antiviral activity of substituted azaindoleoxoacetic piperazine derivatives
US20060100432A1 (en) 2004-11-09 2006-05-11 Matiskella John D Crystalline materials of 1-(4-benzoyl-piperazin-1-yl)-2-[4-methoxy-7-(3-methyl-[1,2,4]triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-ethane-1,2-dione
US7851476B2 (en) 2005-12-14 2010-12-14 Bristol-Myers Squibb Company Crystalline forms of 1-benzoyl-4-[2-[4-methoxy-7-(3-methyl-1H-1,2,4-triazol-1-YL)-1-[(phosphonooxy)methyl]-1H-pyrrolo[2,3-C]pyridin-3-YL]-1,2-dioxoethyl]-piperazine
US7807671B2 (en) 2006-04-25 2010-10-05 Bristol-Myers Squibb Company Diketo-piperazine and piperidine derivatives as antiviral agents
GB0720503D0 (en) 2007-10-22 2007-11-28 Angeletti P Ist Richerche Bio New compound
WO2012019003A1 (en) 2010-08-06 2012-02-09 Bristol-Myers Squibb Company Substituted indole and azaindole oxoacetyl piperazinamide derivatives
ES2585396T3 (es) 2010-12-02 2016-10-05 VIIV Healthcare UK (No.5) Limited Alquilamidas como inhibidores de la unión del VIH
ES2636312T3 (es) 2011-04-12 2017-10-05 VIIV Healthcare UK (No.5) Limited Derivados de tioamida, amidoxima y amidrazona como inhibidores de la fijación del VIH
ES2616268T3 (es) 2011-08-29 2017-06-12 VIIV Healthcare UK (No.5) Limited Derivados condensados de diamina bicíclica como inhibidores de la unión de VIH
EP2751118B1 (en) 2011-08-29 2016-10-12 Bristol-Myers Squibb Company Spiro bicyclic diamine derivatives as hiv attachment inhibitors
US9193725B2 (en) 2012-03-14 2015-11-24 Bristol-Meyers Squibb Company Cyclic hydrazine derivatives as HIV attachment inhibitors
CN108299428B (zh) * 2018-04-04 2019-09-27 山东大学 8-胺基-7-甲酸甲酯-吡嗪骈吡啶酮衍生物及其制备方法与应用

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IL98526A0 (en) * 1990-06-18 1992-07-15 Merck & Co Inc Pyridones,processes for their preparation and pharmaceutical compositions containing them

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AU648121B2 (en) 1994-04-14
CA2054529A1 (en) 1992-05-02
PT99394A (pt) 1992-09-30
FI915152A (fi) 1992-05-02
AU8693491A (en) 1992-05-07
EP0484071A3 (en) 1992-11-25
HU913435D0 (en) 1992-01-28
NZ240407A (en) 1994-09-27
YU172991A (sh) 1994-06-24
CS331091A3 (en) 1992-05-13
IL99843A0 (en) 1992-08-18
JPH04300834A (ja) 1992-10-23
IE913751A1 (en) 1992-05-22
CN1062138A (zh) 1992-06-24
FI915152A0 (fi) 1991-10-31
MX9101880A (es) 1992-07-08
HUT60135A (en) 1992-08-28
EP0484071A2 (en) 1992-05-06

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