EP2139883A4 - Hiv-1-proteasehemmer - Google Patents

Hiv-1-proteasehemmer

Info

Publication number
EP2139883A4
EP2139883A4 EP08744245A EP08744245A EP2139883A4 EP 2139883 A4 EP2139883 A4 EP 2139883A4 EP 08744245 A EP08744245 A EP 08744245A EP 08744245 A EP08744245 A EP 08744245A EP 2139883 A4 EP2139883 A4 EP 2139883A4
Authority
EP
European Patent Office
Prior art keywords
hiv
protease
inhibitors
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.)
Withdrawn
Application number
EP08744245A
Other languages
English (en)
French (fr)
Other versions
EP2139883A2 (de
Inventor
Akbar Ali
Michael D Altman
Saima Ghafoor Anjum
Hong Cao
Sripriya Chellappan
Miguel X Fernandes
Michael Gilson
Visvaldas Kairys
Nancy King
Ellen Nalivaika
Moses Prabu
Tariq M Rana
Sai Kiran Kumar Reddy Garudammagari
Celia A Schiffer
Bruce Tidor
Madhavi Naga Laxmi Nalam
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 Boston
Original Assignee
Massachusetts Institute of Technology
University of Maryland College Park
University of Massachusetts Amherst
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 Maryland College Park, University of Massachusetts Amherst filed Critical Massachusetts Institute of Technology
Publication of EP2139883A2 publication Critical patent/EP2139883A2/de
Publication of EP2139883A4 publication Critical patent/EP2139883A4/de
Withdrawn legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/10Transferases (2.)
    • C12N9/12Transferases (2.) transferring phosphorus containing groups, e.g. kinases (2.7)
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D263/00Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/08Heterocyclic 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
    • C07D263/16Heterocyclic 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
    • C07D263/18Oxygen atoms
    • C07D263/20Oxygen atoms attached in position 2
    • C07D263/24Oxygen atoms attached in position 2 with hydrocarbon radicals, substituted by oxygen atoms, attached to other ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/81Protease inhibitors

Landscapes

  • 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)
EP08744245A 2007-03-23 2008-03-24 Hiv-1-proteasehemmer Withdrawn EP2139883A4 (de)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US91981907P 2007-03-23 2007-03-23
US91989607P 2007-03-23 2007-03-23
US94178607P 2007-06-04 2007-06-04
US94182907P 2007-06-04 2007-06-04
PCT/US2008/058004 WO2008118849A2 (en) 2007-03-23 2008-03-24 Hiv-1 protease inhibitors

Publications (2)

Publication Number Publication Date
EP2139883A2 EP2139883A2 (de) 2010-01-06
EP2139883A4 true EP2139883A4 (de) 2011-06-22

Family

ID=39789249

Family Applications (1)

Application Number Title Priority Date Filing Date
EP08744245A Withdrawn EP2139883A4 (de) 2007-03-23 2008-03-24 Hiv-1-proteasehemmer

Country Status (4)

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

Families Citing this family (17)

* 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
KR102180740B1 (ko) 2016-08-19 2020-11-20 길리애드 사이언시즈, 인코포레이티드 Hiv 바이러스 감염의 예방적 또는 치유적 치료에 유용한 치료 화합물
JOP20180009A1 (ar) 2017-02-06 2019-01-30 Gilead Sciences Inc مركبات مثبط فيروس hiv
AR112412A1 (es) 2017-08-17 2019-10-23 Gilead Sciences Inc Formas de sal de colina de un inhibidor de la cápside 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
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
PL3752495T3 (pl) 2018-02-15 2024-01-15 Gilead Sciences, Inc. Pochodne pirydynowe i ich zastosowanie do leczenia infekcji hiv
CN120053445A (zh) * 2018-07-16 2025-05-30 吉利德科学公司 用于治疗hiv的衣壳抑制剂
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
WO2020150369A1 (en) 2019-01-15 2020-07-23 Ghosh Arun K Hiv-1 protease inhibitors and uses thereof
WO2021262990A1 (en) 2020-06-25 2021-12-30 Gilead Sciences, Inc. Capsid inhibitors for the treatment of hiv
US12083099B2 (en) 2020-10-28 2024-09-10 Accencio LLC Methods of treating symptoms of coronavirus infection with viral protease inhibitors
US12084467B2 (en) 2021-12-03 2024-09-10 Gilead Sciences, Inc. Therapeutic compounds for HIV virus infection
EP4440702B1 (de) 2021-12-03 2025-05-21 Gilead Sciences, Inc. Therapeutische verbindungen gegen hiv-virus-infektion
JP7736929B2 (ja) 2021-12-03 2025-09-09 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
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

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6319946B1 (en) * 1999-02-12 2001-11-20 Vertex Pharmaceuticals Incorporated Inhibitors of aspartyl protease
WO2003097616A1 (en) * 2002-05-17 2003-11-27 Tibotec Pharmaceuticals Ltd Broadspectrum substituted benzisoxazole sulfonamide hiv protease inhibitors
US20040122000A1 (en) * 1981-01-07 2004-06-24 Vertex Pharmaceuticals Incorporated. Inhibitors of aspartyl protease
US20050209301A1 (en) * 2004-03-11 2005-09-22 Sequoia Pharmaceuticals Resistance-repellent retroviral protease inhibitors
WO2006104646A1 (en) * 2005-03-11 2006-10-05 Smithkline Beecham Corporation Hiv protease inhibitors

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5877334A (en) * 1996-07-23 1999-03-02 Abbott Laboratories Intermediates useful in solid phase synthesis method
AU4828199A (en) * 1998-06-23 2000-01-10 Board Of Trustees Of The University Of Illinois, The Multi-drug resistant retroviral protease inhibitors and associated methods
AR037797A1 (es) * 2001-12-12 2004-12-01 Tibotec Pharm Ltd Combinacion de inhibidores de proteasa dependientes del citocromo p450
EP1509537B9 (de) * 2002-04-26 2007-11-14 Gilead Sciences, Inc. Anreicherung in der zelle an phosphonat analoga von hiv protease inhibitor verbindungen und die verbindungen selbst

Patent Citations (5)

* 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
US6319946B1 (en) * 1999-02-12 2001-11-20 Vertex Pharmaceuticals Incorporated Inhibitors of aspartyl protease
WO2003097616A1 (en) * 2002-05-17 2003-11-27 Tibotec Pharmaceuticals Ltd Broadspectrum substituted benzisoxazole sulfonamide hiv protease inhibitors
US20050209301A1 (en) * 2004-03-11 2005-09-22 Sequoia Pharmaceuticals Resistance-repellent retroviral protease inhibitors
WO2006104646A1 (en) * 2005-03-11 2006-10-05 Smithkline Beecham Corporation Hiv protease inhibitors

Non-Patent Citations (6)

* Cited by examiner, † Cited by third party
Title
DOMINIQUE L N G SURLERAUX ET AL: "Discovery and selection of TMC114, a next generation HIV-1 protease inhibitor", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY, WASHINGTON, US, vol. 48, no. 6, 24 March 2005 (2005-03-24), pages 1813 - 1822, XP002621636, ISSN: 0022-2623, [retrieved on 20041005], DOI: 10.1021/JM049560P *
GHOSH A K ET AL: "Potent HIV protease inhibitors incorporating high-affinity P2-ligands and (R)-[(hydroxyethyl)amino]sulfonamide isostere", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, PERGAMON, ELSEVIER SCIENCE, GB, vol. 8, no. 6, 1 January 1998 (1998-01-01), pages 687 - 690, XP002156428, ISSN: 0960-894X, DOI: 10.1016/S0960-894X(98)00098-5 *
GHOSH A K ET AL: "STRUCTURE-BASED DESIGN OF NON-PEPTIDE HIV PROTEASE INHIBITORS", FARMACO, SOCIETA CHIMICA ITALIANA, PAVIA, IT, vol. 50, no. 1/02, 1 January 2001 (2001-01-01), pages 29 - 32, XP001057865, ISSN: 0014-827X, DOI: 10.1016/S0014-827X(01)01025-4 *
MILLER J F ET AL: "Novel arylsulfonamides possessing sub-picomolar HIV protease activities and potent anti-HIV activity against wild-type and drug-resistant viral strains", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, PERGAMON, ELSEVIER SCIENCE, GB, vol. 14, no. 4, 23 February 2000 (2000-02-23), pages 959 - 963, XP002984326, ISSN: 0960-894X, DOI: 10.1016/J.BMCL.2003.12.008 *
MILLER J F ET AL: "Novel P1 chain-extended HIV protease inhibitors possessing potent anti-HIV activity and remarkable inverse antiviral resistance profiles", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, PERGAMON, ELSEVIER SCIENCE, GB, vol. 15, no. 15, 1 August 2005 (2005-08-01), pages 3496 - 3500, XP004969879, ISSN: 0960-894X, DOI: 10.1016/J.BMCL.2005.05.129 *
SURLERAUX D L N G ET AL: "Design of HIV-1 Protease Inhibitors Active on Multidrug-Resistant Virus", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY, WASHINGTON, US, vol. 48, no. 6, 1 January 2005 (2005-01-01), pages 1965 - 1973, XP002414592, ISSN: 0022-2623, DOI: 10.1021/JM049454N *

Also Published As

Publication number Publication date
CN101702908A (zh) 2010-05-05
WO2008118849A3 (en) 2008-12-18
CA2681718A1 (en) 2008-10-02
WO2008118849A2 (en) 2008-10-02
EP2139883A2 (de) 2010-01-06

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Legal Events

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PUAI Public reference made under article 153(3) epc to a published international application that has entered the european phase

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Designated state(s): AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MT NL NO PL PT RO SE SI SK TR

RIN1 Information on inventor provided before grant (corrected)

Inventor name: ALI, AKBAR

Inventor name: KING, NANCY

Inventor name: ANJUM, SAIMA, GHAFOOR

Inventor name: NALAM, MADHAVI, NAGA, LAXMI

Inventor name: TIDOR, BRUCE

Inventor name: SCHIFFER, CELIA, A.

Inventor name: NALIVAIKA, ELLEN

Inventor name: KAIRYS, VISVALDAS

Inventor name: CHELLAPPAN, SRIPRIYA

Inventor name: CAO, HONG

Inventor name: FERNANDES, MIGUEL, X.

Inventor name: RANA, TARIQ, M.

Inventor name: GILSON, MICHAEL

Inventor name: PRABU, MOSES

Inventor name: GARUDAMMAGARI SAI, KIRAN KUMAR, REDDY

Inventor name: ALTMAN, MICHAEL, D.

RIN1 Information on inventor provided before grant (corrected)

Inventor name: NALIVAIKA, ELLEN

Inventor name: CHELLAPPAN, SRIPRIYA

Inventor name: SCHIFFER, CELIA, A.

Inventor name: ANJUM, SAIMA, GHAFOOR

Inventor name: CAO, HONG

Inventor name: TIDOR, BRUCE

Inventor name: KING, NANCY

Inventor name: FERNANDES, MIGUEL, X.

Inventor name: GARUDAMMAGARI SAI, KIRAN KUMAR, REDDY

Inventor name: ALTMAN, MICHAEL, D.

Inventor name: PRABU, MOSES

Inventor name: ALI, AKBAR

Inventor name: GILSON, MICHAEL

Inventor name: NALAM, MADHAVI, NAGA, LAXMI

Inventor name: RANA, TARIQ, M.

Inventor name: KAIRYS, VISVALDAS

RAP1 Party data changed (applicant data changed or rights of an application transferred)

Owner name: MASSACHUSETTS INSTITUTE OF TECHNOLOGY

Owner name: UNIVERSITY OF MARYLAND, COLLEGE PARK

Owner name: UNIVERSITY OF MASSACHUSETTS

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