EP2139883A4 - Hiv-1 protease inhibitors - Google Patents

Hiv-1 protease inhibitors

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
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Withdrawn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)
French (fr)
Other versions
EP2139883A2 (en
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.)
University of Massachusetts UMass
Massachusetts Institute of Technology
University of Maryland at College Park
Original Assignee
University of Massachusetts UMass
University of Maryland at Baltimore
Massachusetts Institute of Technology
University of Maryland at College Park
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 at Baltimore, Massachusetts Institute of Technology, University of Maryland at College Park filed Critical University of Massachusetts UMass
Publication of EP2139883A2 publication Critical patent/EP2139883A2/en
Publication of EP2139883A4 publication Critical patent/EP2139883A4/en
Withdrawn legal-status Critical Current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 Hiv-1 protease inhibitors Withdrawn EP2139883A4 (en)

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 (en) 2010-01-06
EP2139883A4 true EP2139883A4 (en) 2011-06-22

Family

ID=39789249

Family Applications (1)

Application Number Title Priority Date Filing Date
EP08744245A Withdrawn EP2139883A4 (en) 2007-03-23 2008-03-24 Hiv-1 protease inhibitors

Country Status (4)

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

Families Citing this family (12)

* 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
PE20190910A1 (en) 2016-08-19 2019-06-26 Gilead Sciences Inc THERAPEUTIC COMPOUNDS USEFUL FOR THE PROPHYLACTIC OR THERAPEUTIC TREATMENT OF AN INFECTION WITH THE HIV VIRUS
JOP20180009A1 (en) 2017-02-06 2019-01-30 Gilead Sciences Inc Hiv inhibitor compounds
AR112413A1 (en) 2017-08-17 2019-10-23 Gilead Sciences Inc SOLID FORMS OF AN HIV CAPSID INHIBITOR
AR112412A1 (en) 2017-08-17 2019-10-23 Gilead Sciences Inc CHOLINE SALT FORMS OF AN HIV CAPSID INHIBITOR
CN108220482A (en) * 2018-02-11 2018-06-29 广西医科大学 The primer for the treatment of AIDS drug NRTIs resistant mutational sites G73S and its application
WO2019161017A1 (en) 2018-02-15 2019-08-22 Gilead Sciences, Inc. Pyridine derivatives and their use for treating hiv infection
WO2020018459A1 (en) * 2018-07-16 2020-01-23 Gilead Sciences, Inc. Capsid inhibitors for the treatment of hiv
TWI829205B (en) 2018-07-30 2024-01-11 美商基利科學股份有限公司 Anti-hiv compounds
EP3938371A4 (en) * 2019-01-15 2023-01-18 Purdue Research Foundation Hiv-1 protease inhibitors and uses thereof
US11787825B2 (en) 2021-12-03 2023-10-17 Gilead Sciences, Inc. Therapeutic compounds for HIV virus infection

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
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
TWI286476B (en) * 2001-12-12 2007-09-11 Tibotec Pharm Ltd Combination of cytochrome P450 dependent protease inhibitors
US7462608B2 (en) * 2002-04-26 2008-12-09 Gilead Sciences, Inc. Non nucleoside reverse transcriptase inhibitors

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

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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

A4 Supplementary search report drawn up and despatched

Effective date: 20110523

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18D Application deemed to be withdrawn

Effective date: 20111001