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

Hiv-1蛋白酶抑制剂 Download PDF

Info

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
Authority
CN
China
Prior art keywords
alkyl
compound
heterocyclic radical
amino
amido
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
CN200880016701A
Other languages
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.)
University of Massachusetts UMass
University of Maryland at Baltimore
Massachusetts Institute of Technology
Original Assignee
University of Massachusetts UMass
University of Maryland Biotechnology Institute UMBI
Massachusetts Institute of Technology
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 University of Massachusetts UMass, University of Maryland Biotechnology Institute UMBI, Massachusetts Institute of Technology filed Critical University of Massachusetts UMass
Publication of CN101702908A publication Critical patent/CN101702908A/zh
Pending legal-status Critical Current

Links

Images

Classifications

    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Genetics & Genomics (AREA)
  • General Health & Medical Sciences (AREA)
  • Biochemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • General Engineering & Computer Science (AREA)
  • Microbiology (AREA)
  • Biotechnology (AREA)
  • Biomedical Technology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Biophysics (AREA)
  • Proteomics, Peptides & Aminoacids (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
US94178607P 2007-06-04 2007-06-04
US94182907P 2007-06-04 2007-06-04
US60/941,829 2007-06-04
US60/941,786 2007-06-04
PCT/US2008/058004 WO2008118849A2 (en) 2007-03-23 2008-03-24 Hiv-1 protease inhibitors

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 (de)
CN (1) CN101702908A (de)
CA (1) CA2681718A1 (de)
WO (1) WO2008118849A2 (de)

Cited By (1)

* 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

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010135424A1 (en) * 2009-05-19 2010-11-25 Glaxosmithkline Llc Chemical compounds
WO2011061590A1 (en) 2009-11-17 2011-05-26 Hetero Research Foundation Novel carboxamide derivatives as hiv inhibitors
CN109890808B (zh) 2016-08-19 2020-08-07 吉利德科学公司 用于预防性或治疗性治疗hiv病毒感染的治疗性化合物
JOP20180009A1 (ar) 2017-02-06 2019-01-30 Gilead Sciences Inc مركبات مثبط فيروس hiv
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
JP7083398B2 (ja) 2018-02-15 2022-06-10 ギリアード サイエンシーズ， インコーポレイテッド ピリジン誘導体およびｈｉｖ感染を処置するためのその使用
KR20210033492A (ko) * 2018-07-16 2021-03-26 길리애드 사이언시즈, 인코포레이티드 Hiv의 치료를 위한 캡시드 억제제
TWI766172B (zh) 2018-07-30 2022-06-01 美商基利科學股份有限公司 抗hiv化合物
EP3938371A4 (de) * 2019-01-15 2023-01-18 Purdue Research Foundation Hiv-1-proteasehemmer und verwendungen davon
WO2023102239A1 (en) 2021-12-03 2023-06-08 Gilead Sciences, Inc. Therapeutic compounds for hiv virus infection

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 (en) * 1998-06-23 1999-12-29 The United States Of America Represented By The Secretary, Department Of Health And Human Services Multi-drug resistant retroviral protease inhibitors and use thereof
TNSN00027A1 (fr) * 1999-02-12 2005-11-10 Vertex Pharma Inhibiteurs de l'aspartyle protease
TWI286476B (en) * 2001-12-12 2007-09-11 Tibotec Pharm Ltd Combination of cytochrome P450 dependent protease inhibitors
WO2003091264A2 (en) * 2002-04-26 2003-11-06 Gilead Sciences, Inc. Non nucleoside reverse transcriptase inhibitors
US7462636B2 (en) * 2002-05-17 2008-12-09 Tibotec Pharmaceuticals Ltd Broadspectrum substituted benzisoxazole sulfonamide HIV protease inhibitors
US7807845B2 (en) * 2004-03-11 2010-10-05 Sequoia Pharmaceuticals, Inc. Resistance-repellent retroviral protease inhibitors
EP1855672A4 (de) * 2005-03-11 2011-11-30 Glaxosmithkline Llc Hiv-proteasehemmer

Cited By (1)

* 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

Also Published As

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

Similar Documents

Publication Publication Date Title
CN101702908A (zh) Hiv-1蛋白酶抑制剂
CA3033180C (en) Pharmaceutical compositions containing substituted polycyclic pyridone derivatives and prodrug thereof
Nagarajan et al. Discovery of novel benzothiazolesulfonamides as potent inhibitors of HIV-1 protease
Ghosh et al. Syntheses of FDA approved HIV protease inhibitors
CN101355939A (zh) 用于抑制hiv复制的新物质的组合物和合成
CN101230067B (zh) 广谱的2-(取代-氨基)-苯并噻唑磺酰胺hiv蛋白酶抑制剂
CA2704645A1 (en) Non-nucleoside reverse transcriptase inhibitors
US20110178092A1 (en) HIV-1 Protease Inhibitors
Mizuguchi et al. A minimally cytotoxic CD4 mimic as an HIV entry inhibitor
CN110105348A (zh) 新型迈克尔受体类肠病毒71型抑制剂的制备及用途
HRP20050607A2 (en) Broadspectrum substituted benzisoxazole sulfonamide hiv protease inhibitors
TWI385173B (zh) 作為ｈｉｖ蛋白酶抑制劑之經取代的胺基苯基磺醯胺化合物
Trivedi et al. Discovery of 2-isoxazol-3-yl-acetamide analogues as heat shock protein 90 (HSP90) inhibitors with significant anti-HIV activity
CN101309911A (zh) Hiv-1蛋白酶抑制剂及其制备方法和使用方法
JP4578101B2 (ja) 幅広いスペクトルのｈｉｖプロテアーゼ阻害剤である複素環置換フェニル含有スルホンアミド
CN1849117B (zh) Hiv病毒的侵入抑制剂
EP1751125A1 (de) Als inhibitor von retroviraler protease geeignete ritonavir-analoge verbindung, herstellung der ritonavir-analogen verbindung und pharmazeutische zusammenetzung für die ritonavir-analoge verbindung
JP2008546790A (ja) Ｈｉｖ−１プロテアーゼ阻害剤
Zhu et al. Design, synthesis and biological evaluation of protease inhibitors containing morpholine cores with remarkable potency against both HIV-1 subtypes B and C
Oscarsson et al. Design and synthesis of HIV-1 protease inhibitors. Novel tetrahydrofuran P2/P2′-groups interacting with Asp29/30 of the HIV-1 protease. Determination of binding from X-ray crystal structure of inhibitor protease complex
CN101775007B (zh) 具有hiv拮抗活性的三环烯类化合物及其制备方法与应用
Williams Design, Synthesis, and Biological Evaluation of Potent HIV-1 Protease Inhibitors With Novel Bicyclic Oxazolidinone and Bis Squaramide Scaffolds
Belcher Lewis Acid-Catalyzed Vinyl Acetal Rearrangement of 4, 5-Dihydro-1, 3-Dioxepines: Stereoselective Synthesis of Cis-and Trans-2, 3-Disubstituted Tetrahydrofurans and Structure-Based Design and Synthesis of Novel Inhibitors of HIV-1 Protease and SARS-3CLPRO Protease
Mainkar et al. Peptidomimetics: Current and Future Perspectives on HIV Protease Inhibitors
Cheng et al. Design, synthesis and biological evaluation of sulfamethazine derivatives as potent neuraminidase inhibitors

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
ASS Succession or assignment of patent right

Owner name: COLLEGE PARK, UNIVERSITY OF MARYLAND MASSACHUSETTS

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

C41 Transfer of patent application or patent right or utility model
TA01 Transfer of patent application right

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

C02 Deemed withdrawal of patent application after publication (patent law 2001)
WD01 Invention patent application deemed withdrawn after publication

Application publication date: 20100505