EP2139883A4 - Inhibiteurs de la protéase du vih-1 - Google Patents

Inhibiteurs de la protéase du vih-1

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Withdrawn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
German (de)
English (en)
Other versions
EP2139883A2 (fr
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/fr
Publication of EP2139883A4 publication Critical patent/EP2139883A4/fr
Withdrawn legal-status Critical Current

Links

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)
EP08744245A 2007-03-23 2008-03-24 Inhibiteurs de la protéase du vih-1 Withdrawn EP2139883A4 (fr)

Applications Claiming Priority (5)

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

Publications (2)

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

Family

ID=39789249

Family Applications (1)

Application Number Title Priority Date Filing Date
EP08744245A Withdrawn EP2139883A4 (fr) 2007-03-23 2008-03-24 Inhibiteurs de la protéase du vih-1

Country Status (4)

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

Families Citing this family (17)

* 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
SI3347352T1 (sl) 2016-08-19 2019-08-30 Gilead Sciences, Inc. Terapevtske spojine uporabne za profilaktično ali terapevtsko zdravljenje okužbe z virusom HIV
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
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
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
CA3103522C (fr) * 2018-07-16 2023-11-21 Gilead Sciences, Inc. Inhibiteurs de capsides pour le traitement du vih
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
EP3938371B1 (fr) * 2019-01-15 2026-03-04 Purdue Research Foundation Inhibiteurs de la protéase du vih -1 et leurs utilisations
EP4172157B1 (fr) 2020-06-25 2025-11-19 Gilead Sciences, Inc. Inhibiteurs de capside pour le traitement du vih
US12083099B2 (en) 2020-10-28 2024-09-10 Accencio LLC Methods of treating symptoms of coronavirus infection with viral protease inhibitors
PL4445900T3 (pl) 2021-12-03 2025-09-22 Gilead Sciences, Inc. Związki terapeutyczne przeciwko zakażeniu wirusem hiv
KR20240113832A (ko) 2021-12-03 2024-07-23 길리애드 사이언시즈, 인코포레이티드 Hiv 바이러스 감염 치료용 화합물
WO2023102529A1 (fr) 2021-12-03 2023-06-08 Gilead Sciences, Inc. Composés thérapeutiques pour l'infection par le virus du vih
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 (fr) * 2002-05-17 2003-11-27 Tibotec Pharmaceuticals Ltd Inhibiteurs de la protease du vih de sulfonamide de benzisoxazole substitue a large bande
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 (fr) * 2005-03-11 2006-10-05 Smithkline Beecham Corporation Inhibiteurs de proteases du vih

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
TWI286476B (en) * 2001-12-12 2007-09-11 Tibotec Pharm Ltd Combination of cytochrome P450 dependent protease inhibitors
WO2003090691A2 (fr) * 2002-04-26 2003-11-06 Gilead Sciences, Inc. Technique et compositions permettant d'identifier des composes therapeutiques anti-vih

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 (fr) * 2002-05-17 2003-11-27 Tibotec Pharmaceuticals Ltd Inhibiteurs de la protease du vih de sulfonamide de benzisoxazole substitue a large bande
US20050209301A1 (en) * 2004-03-11 2005-09-22 Sequoia Pharmaceuticals Resistance-repellent retroviral protease inhibitors
WO2006104646A1 (fr) * 2005-03-11 2006-10-05 Smithkline Beecham Corporation Inhibiteurs de proteases du vih

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
WO2008118849A2 (fr) 2008-10-02
EP2139883A2 (fr) 2010-01-06
WO2008118849A3 (fr) 2008-12-18
CN101702908A (zh) 2010-05-05
CA2681718A1 (fr) 2008-10-02

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Legal Events

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

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Effective date: 20091019

AK Designated contracting states

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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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Effective date: 20110523

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Effective date: 20111001