CN101702908A - Hiv-1蛋白酶抑制剂 - Google Patents

Hiv-1蛋白酶抑制剂 Download PDF

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Publication number
CN101702908A
CN101702908A CN200880016701A CN200880016701A CN101702908A CN 101702908 A CN101702908 A CN 101702908A CN 200880016701 A CN200880016701 A CN 200880016701A CN 200880016701 A CN200880016701 A CN 200880016701A CN 101702908 A CN101702908 A CN 101702908A
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CN
China
Prior art keywords
alkyl
compound
heterocyclyl
amino
amido
Prior art date
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Pending
Application number
CN200880016701A
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English (en)
Chinese (zh)
Inventor
A·阿利
M·D·阿尔特曼
S·G·安朱姆
H·曹
S·谢拉潘
M·X·费尔南德斯
M·吉尔森
V·凯里斯
N·金
E·纳利韦卡
M·普拉布
T·M·拉纳
K·K·R·加鲁达马加里塞
C·A·希菲尔
B·蒂多尔
M·N·L·纳拉姆
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Massachusetts Institute of Technology
University of Maryland College Park
University of Massachusetts Amherst
Original Assignee
Massachusetts Institute of Technology
University of Massachusetts Amherst
The University of Maryland Biotechnology Institute
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 Massachusetts Institute of Technology, University of Massachusetts Amherst, The University of Maryland Biotechnology Institute filed Critical Massachusetts Institute of Technology
Publication of CN101702908A publication Critical patent/CN101702908A/zh
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/10—Transferases (2.)
    • C12N9/12—Transferases (2.) transferring phosphorus containing groups, e.g. kinases (2.7)
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/08—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D263/16—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D263/18—Oxygen atoms
    • C07D263/20—Oxygen atoms attached in position 2
    • C07D263/24—Oxygen atoms attached in position 2 with hydrocarbon radicals, substituted by oxygen atoms, attached to other ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/81—Protease inhibitors

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Biochemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Engineering & Computer Science (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Biomedical Technology (AREA)
  • Biotechnology (AREA)
  • Microbiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biophysics (AREA)
  • General Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN200880016701A 2007-03-23 2008-03-24 Hiv-1蛋白酶抑制剂 Pending CN101702908A (zh)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US91981907P 2007-03-23 2007-03-23
US91989607P 2007-03-23 2007-03-23
US60/919,819 2007-03-23
US60/919,896 2007-03-23
US94182907P 2007-06-04 2007-06-04
US94178607P 2007-06-04 2007-06-04
US60/941,829 2007-06-04
US60/941,786 2007-06-04
PCT/US2008/058004 WO2008118849A2 (fr) 2007-03-23 2008-03-24 Inhibiteurs de la protéase du vih-1

Publications (1)

Publication Number Publication Date
CN101702908A true CN101702908A (zh) 2010-05-05

Family

ID=39789249

Family Applications (1)

Application Number Title Priority Date Filing Date
CN200880016701A Pending CN101702908A (zh) 2007-03-23 2008-03-24 Hiv-1蛋白酶抑制剂

Country Status (4)

Country Link
EP (1) EP2139883A4 (fr)
CN (1) CN101702908A (fr)
CA (1) CA2681718A1 (fr)
WO (1) WO2008118849A2 (fr)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108220482A (zh) * 2018-02-11 2018-06-29 广西医科大学 艾滋病治疗药物NRTIs耐药突变位点G73S的引物及其应用
CN117304129A (zh) * 2023-09-18 2023-12-29 中国医学科学院医药生物技术研究所 一种氮杂烷酮衍生物或其药学上可接受的盐及其制备方法和应用、药物组合物

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010135424A1 (fr) * 2009-05-19 2010-11-25 Glaxosmithkline Llc Composés chimiques
WO2011061590A1 (fr) 2009-11-17 2011-05-26 Hetero Research Foundation Nouveaux dérivés carboxamides comme inhibiteurs du vih
TW202138365A (zh) 2016-08-19 2021-10-16 美商基利科學股份有限公司 治療性化合物
AR110922A1 (es) 2017-02-06 2019-05-15 Gilead Sciences Inc Compuestos inhibidores del vih
TWI687415B (zh) 2017-08-17 2020-03-11 美商基利科學股份有限公司 Hiv蛋白質膜抑制劑之固體形式
AR112412A1 (es) 2017-08-17 2019-10-23 Gilead Sciences Inc Formas de sal de colina de un inhibidor de la cápside del vih
CN111836805B (zh) 2018-02-15 2023-07-14 吉利德科学公司 吡啶衍生物及其用于治疗hiv感染的用途
US11944611B2 (en) * 2018-07-16 2024-04-02 Gilead Sciences, Inc. Capsid inhibitors for the treatment of HIV
TWI829205B (zh) 2018-07-30 2024-01-11 美商基利科學股份有限公司 抗hiv化合物
US12454537B2 (en) 2019-01-15 2025-10-28 Purdue Research Foundation HIV-1 protease inhibitors and uses thereof
JP7520162B2 (ja) 2020-06-25 2024-07-22 ギリアード サイエンシーズ， インコーポレイテッド Ｈｉｖの治療のためのカプシド阻害剤
US12083099B2 (en) 2020-10-28 2024-09-10 Accencio LLC Methods of treating symptoms of coronavirus infection with viral protease inhibitors
WO2023102523A1 (fr) 2021-12-03 2023-06-08 Gilead Sciences, Inc. Composés thérapeutiques pour l'infection par le virus du vih
PT4440702T (pt) 2021-12-03 2025-08-13 Gilead Sciences Inc Compostos terapêuticos para a infecção pelo vírus do hiv
JP7765637B2 (ja) 2021-12-03 2025-11-06 ギリアード サイエンシーズ， インコーポレイテッド Ｈｉｖウイルス感染症のための治療化合物

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040122000A1 (en) * 1981-01-07 2004-06-24 Vertex Pharmaceuticals Incorporated. Inhibitors of aspartyl protease
US5877334A (en) * 1996-07-23 1999-03-02 Abbott Laboratories Intermediates useful in solid phase synthesis method
WO1999067254A2 (fr) * 1998-06-23 1999-12-29 The United States Of America Represented By The Secretary, Department Of Health And Human Services Inhibiteurs de protease retrovirale resistant a l'action de plusieurs medicaments et procedes associes
TWI260322B (en) * 1999-02-12 2006-08-21 Vertex Pharma Inhibitors of aspartyl protease
AR037797A1 (es) * 2001-12-12 2004-12-01 Tibotec Pharm Ltd Combinacion de inhibidores de proteasa dependientes del citocromo p450
AU2003231765B9 (en) * 2002-04-26 2010-01-28 Gilead Sciences, Inc. Cellular accumulation of phosphonate analogs of HIV protease inhibitor compounds and the compounds as such
ATE371652T1 (de) * 2002-05-17 2007-09-15 Tibotec Pharm Ltd Substituierte benzisoxazolsulfonamide mit breitbändiger hiv-protease hemmender wirkung
CA2559328A1 (fr) * 2004-03-11 2005-09-22 Sequoia Pharmaceuticals, Inc. Inhibiteurs de la protease retrovirale inhibant la resistance
JP2008533017A (ja) * 2005-03-11 2008-08-21 スミスクライン ビーチャム コーポレーション Ｈｉｖプロテアーゼ阻害薬

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108220482A (zh) * 2018-02-11 2018-06-29 广西医科大学 艾滋病治疗药物NRTIs耐药突变位点G73S的引物及其应用
CN117304129A (zh) * 2023-09-18 2023-12-29 中国医学科学院医药生物技术研究所 一种氮杂烷酮衍生物或其药学上可接受的盐及其制备方法和应用、药物组合物

Also Published As

Publication number Publication date
WO2008118849A2 (fr) 2008-10-02
EP2139883A2 (fr) 2010-01-06
CA2681718A1 (fr) 2008-10-02
EP2139883A4 (fr) 2011-06-22
WO2008118849A3 (fr) 2008-12-18

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Owner name: COLLEGE PARK, UNIVERSITY OF MARYLAND MASSACHUSETTS

Free format text: FORMER OWNER: UNIVERSITY OF MARYLAND BIOTECHNOLOGY INSTITUTE MASSACHUSETTS INSTITUTE OF TECHNOLOGY

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Effective date of registration: 20110418

Address after: Massachusetts

Applicant after: Univ Massachusetts

Co-applicant after: Univ Maryland

Co-applicant after: Massachusetts Institute of Technology

Address before: Massachusetts

Applicant before: Univ Massachusetts

Co-applicant before: Univ Maryland Biotech Inst

Co-applicant before: Massachusetts Institute of Technology

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Application publication date: 20100505