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WO2008118849A3 - Hiv-1 protease inhibitors - Google Patents

Hiv-1 protease inhibitors Download PDF

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Publication number
WO2008118849A3
WO2008118849A3 PCT/US2008/058004 US2008058004W WO2008118849A3 WO 2008118849 A3 WO2008118849 A3 WO 2008118849A3 US 2008058004 W US2008058004 W US 2008058004W WO 2008118849 A3 WO2008118849 A3 WO 2008118849A3
Authority
WO
WIPO (PCT)
Prior art keywords
protease inhibitors
hiv
infection
treatment
methods
Prior art date
Application number
PCT/US2008/058004
Other languages
French (fr)
Other versions
WO2008118849A2 (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
Original Assignee
Univ Massachusetts
Univ Maryland Biotech Inst
Massachusetts Inst Technology
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
Garudammagari Sai Kiran Kumar
Celia A Schiffer
Bruce Tidor
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 Univ Massachusetts, Univ Maryland Biotech Inst, Massachusetts Inst Technology, 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, Garudammagari Sai Kiran Kumar, Celia A Schiffer, Bruce Tidor filed Critical Univ Massachusetts
Priority to CA002681718A priority Critical patent/CA2681718A1/en
Priority to EP08744245A priority patent/EP2139883A4/en
Priority to CN200880016701A priority patent/CN101702908A/en
Publication of WO2008118849A2 publication Critical patent/WO2008118849A2/en
Publication of WO2008118849A3 publication Critical patent/WO2008118849A3/en

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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

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)

Abstract

Described are novel protease inhibitors and methods for using said protease inhibitors in the treatment of human immunodeficiency virus (HIV) infection.
PCT/US2008/058004 2007-03-23 2008-03-24 Hiv-1 protease inhibitors WO2008118849A2 (en)

Priority Applications (3)

Application Number Priority Date Filing Date Title
CA002681718A CA2681718A1 (en) 2007-03-23 2008-03-24 Hiv-1 protease inhibitors
EP08744245A EP2139883A4 (en) 2007-03-23 2008-03-24 INHIBITORS OF HIV-1 PROTEASE
CN200880016701A CN101702908A (en) 2007-03-23 2008-03-24 HIV-1 protease inhibitors

Applications Claiming Priority (8)

Application Number Priority Date Filing Date Title
US91981907P 2007-03-23 2007-03-23
US91989607P 2007-03-23 2007-03-23
US60/919,896 2007-03-23
US60/919,819 2007-03-23
US94182907P 2007-06-04 2007-06-04
US94178607P 2007-06-04 2007-06-04
US60/941,786 2007-06-04
US60/941,829 2007-06-04

Publications (2)

Publication Number Publication Date
WO2008118849A2 WO2008118849A2 (en) 2008-10-02
WO2008118849A3 true WO2008118849A3 (en) 2008-12-18

Family

ID=39789249

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2008/058004 WO2008118849A2 (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 (15)

* 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
UY37367A (en) 2016-08-19 2018-03-23 Gilead Sciences Inc NEW COMPOUNDS FOR USE IN THE TREATMENT OF A VIRAL INFECTION AND COMPOSITIONS OF THE SAME
JOP20180009A1 (en) 2017-02-06 2019-01-30 Gilead Sciences Inc Hiv inhibitor compounds
AR112412A1 (en) 2017-08-17 2019-10-23 Gilead Sciences Inc CHOLINE SALT FORMS OF AN HIV CAPSID INHIBITOR
TW202024061A (en) 2017-08-17 2020-07-01 美商基利科學股份有限公司 Solid 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
JP7083398B2 (en) 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 Pyridine derivatives and their use for treating HIV infection
CN120053446A (en) * 2018-07-16 2025-05-30 吉利德科学公司 Capsid inhibitors for HIV treatment
TWI829205B (en) 2018-07-30 2024-01-11 美商基利科學股份有限公司 Anti-hiv compounds
US20220363688A1 (en) * 2019-01-15 2022-11-17 Purdue Research Foundarion Hiv-1 protease inhibitors and uses thereof
AU2021296607B2 (en) 2020-06-25 2024-07-25 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
TW202337439A (en) 2021-12-03 2023-10-01 美商基利科學股份有限公司 Therapeutic compounds for hiv virus infection
JP2024542541A (en) 2021-12-03 2024-11-15 ギリアード サイエンシーズ， インコーポレイテッド Therapeutic compounds for HIV viral infections - Patents.com

Citations (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
WO2003049746A2 (en) * 2001-12-12 2003-06-19 Tibotec Pharmaceuticals Ltd. Combination of cytochome p450 dependent protease inhibitors
WO2003090690A2 (en) * 2002-04-26 2003-11-06 Gilead Sciences, Inc. Cellular accumulation of phosphonate analogs of hiv protease inhibitor compounds and the compounds as such

Family Cites Families (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
TNSN00027A1 (en) * 1999-02-12 2005-11-10 Vertex Pharma ASPARTYLE PROTEASE INHIBITORS
PL373425A1 (en) * 2002-05-17 2005-08-22 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
WO2006104646A1 (en) * 2005-03-11 2006-10-05 Smithkline Beecham Corporation Hiv protease inhibitors

Patent Citations (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
WO2003049746A2 (en) * 2001-12-12 2003-06-19 Tibotec Pharmaceuticals Ltd. Combination of cytochome p450 dependent protease inhibitors
WO2003090690A2 (en) * 2002-04-26 2003-11-06 Gilead Sciences, Inc. Cellular accumulation of phosphonate analogs of hiv protease inhibitor compounds and the compounds as such

Non-Patent Citations (7)

* Cited by examiner, † Cited by third party
Title
FRECER V. ET AL.: "Interactions of ligands with macromolecules: rational design of specific inhibitors of aspartic protease of HIV-1", MACROMOLECULAR CHEMISTRY AND PHYSICS, vol. 203, no. 10/11, 2002, pages 1650 - 1657, XP008122473 *
GOHDA K.: "Structure based design of inhibitors of aspartic protease of HIV-1", LETTERS IN DRUG DESIGN & DISCOVERY, vol. 2, no. 8, 2005, pages 638 - 646, XP001525577 *
NAGARAJAN S.R. ET AL.: "Discovery of novel benzothiazolesulfonamides as potent inhibitors of HIV-1 protease", BIOORGANIC & MEDICINAL CHEMISTRY, vol. 11, no. 22, 2003, pages 4769 - 4777, XP002506280 *
See also references of EP2139883A4 *
SURLEAUX D.L.N.G. ET AL.: "Design of HIV-1 Protease Inhibitors Active on Multidrug-Resistant Virus", JOURNAL OF MEDICINAL CHEMISTRY, vol. 48, no. 6, 2005, pages 1965 - 1973, XP002414592 *
SURLEAUX D.L.N.G. ET AL.: "Discovery and Selection of TMC114, a Next Generation HIV-1 Protease Inhibitor", JOURNAL OF MEDICINAL CHEMISTRY, vol. 48, no. 6, 2005, pages 1813 - 1822, XP008122471 *
TOSSI A. ET AL.: "Small hydroxyethylene-based peptidomimetics inhibiting both HIV-1 and C. albicans aspartic proteases", BIOORGANIC & MEDICINAL CHEMISTRY, vol. 11, no. 22, 2003, pages 4719 - 4727, XP008122472 *

Also Published As

Publication number Publication date
EP2139883A4 (en) 2011-06-22
CN101702908A (en) 2010-05-05
EP2139883A2 (en) 2010-01-06
CA2681718A1 (en) 2008-10-02
WO2008118849A2 (en) 2008-10-02

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