WO1996014314A3 - Thiepane compounds inhibiting and detecting hiv protease - Google Patents

Thiepane compounds inhibiting and detecting hiv protease Download PDF

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Publication number
WO1996014314A3
WO1996014314A3 PCT/US1995/014603 US9514603W WO9614314A3 WO 1996014314 A3 WO1996014314 A3 WO 1996014314A3 US 9514603 W US9514603 W US 9514603W WO 9614314 A3 WO9614314 A3 WO 9614314A3
Authority
WO
WIPO (PCT)
Prior art keywords
thiepane
useful
enzymes
hiv protease
compounds inhibiting
Prior art date
Application number
PCT/US1995/014603
Other languages
French (fr)
Other versions
WO1996014314A2 (en
Inventor
Norbert W Bischofberger
Choung U Kim
Steven H Krawczyk
Lawrence R Mcgee
Michael J Postich
Wenjin Yang
Original Assignee
Gilead Sciences Inc
Norbert W Bischofberger
Choung U Kim
Steven H Krawczyk
Lawrence R Mcgee
Michael J Postich
Wenjin Yang
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
Priority claimed from US08/473,876 external-priority patent/US5705524A/en
Application filed by Gilead Sciences Inc, Norbert W Bischofberger, Choung U Kim, Steven H Krawczyk, Lawrence R Mcgee, Michael J Postich, Wenjin Yang filed Critical Gilead Sciences Inc
Priority to AU42342/96A priority Critical patent/AU710492B2/en
Priority to NZ297230A priority patent/NZ297230A/en
Priority to EP95940672A priority patent/EP0789695A2/en
Priority to JP51552196A priority patent/JP2002515849A/en
Publication of WO1996014314A2 publication Critical patent/WO1996014314A2/en
Publication of WO1996014314A3 publication Critical patent/WO1996014314A3/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D337/00—Heterocyclic compounds containing rings of more than six members having one sulfur atom as the only ring hetero atom
    • C07D337/02—Seven-membered rings
    • C07D337/04—Seven-membered rings not condensed with other rings

Abstract

Tri- and tetra substituted thiepane compositions having use as immunogens, therapeutics, diagnostics and for other industrial purposes are disclosed. The compositions inhibit proteolytic activity of viral enzymes and are useful for the inhibition of such enzymes as well as in assays for the detection of such enzymes. Embodiments in which antigenic polypeptides are bonded to the compositons are useful in raising antibodies against the thiepane haptens or the polypeptide. Labeled thiepanes of this invention are useful as diagnostic reagents.
PCT/US1995/014603 1994-11-02 1995-11-03 Thiepane compounds inhibiting and detecting hiv protease WO1996014314A2 (en)

Priority Applications (4)

Application Number Priority Date Filing Date Title
AU42342/96A AU710492B2 (en) 1994-11-04 1995-11-03 Thiepane compounds inhibiting and detecting HIV protease
NZ297230A NZ297230A (en) 1994-11-02 1995-11-03 Thiepane compounds for detecting HIV protease
EP95940672A EP0789695A2 (en) 1994-11-04 1995-11-03 Thiepane compounds inhibiting and detecting hiv protease
JP51552196A JP2002515849A (en) 1994-11-04 1995-11-03 Thiepane compounds that inhibit and detect HIV protease

Applications Claiming Priority (8)

Application Number Priority Date Filing Date Title
US33447194A 1994-11-04 1994-11-04
US08/334,471 1994-11-04
US47086495A 1995-06-06 1995-06-06
US08/470,864 1995-06-06
US08/473,876 US5705524A (en) 1994-11-04 1995-06-07 Thiepane compounds
US08/473,876 1995-06-07
US52204295A 1995-11-02 1995-11-02
US08/522,042 1995-11-02

Publications (2)

Publication Number Publication Date
WO1996014314A2 WO1996014314A2 (en) 1996-05-17
WO1996014314A3 true WO1996014314A3 (en) 1996-06-20

Family

ID=27502493

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1995/014603 WO1996014314A2 (en) 1994-11-02 1995-11-03 Thiepane compounds inhibiting and detecting hiv protease

Country Status (5)

Country Link
EP (1) EP0789695A2 (en)
JP (1) JP2002515849A (en)
AU (1) AU710492B2 (en)
CA (1) CA2203570A1 (en)
WO (1) WO1996014314A2 (en)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9579332B2 (en) 2004-07-27 2017-02-28 Gilead Sciences, Inc. Phosphonate analogs of HIV inhibitor compounds

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5610294A (en) 1991-10-11 1997-03-11 The Du Pont Merck Pharmaceutical Company Substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors
DE10299052I1 (en) 1995-02-27 2003-05-22 Gilead Sciences Inc New selective inhibitors of viral or bacterial neuraminidases
US5763483A (en) * 1995-12-29 1998-06-09 Gilead Sciences, Inc. Carbocyclic compounds
US5859284A (en) 1996-08-23 1999-01-12 Gilead Sciences, Inc. Preparation of carbocyclic compounds
US6518438B2 (en) 1996-08-23 2003-02-11 Gilead Sciences, Inc. Preparation of cyclohexene carboxylate derivatives
US5994377A (en) 1996-10-21 1999-11-30 Gilead Sciences, Inc. Piperidine compounds
TW480247B (en) * 1997-12-12 2002-03-21 Gilead Sciences Inc Novel compounds useful as neuraminidase inhibitors and pharmaceutical compositions containing same
CA2481449A1 (en) 2002-04-26 2003-11-06 Gilead Sciences, Inc. Method and compositions for identifying anti-hiv therapeutic compounds
US7452901B2 (en) 2003-04-25 2008-11-18 Gilead Sciences, Inc. Anti-cancer phosphonate analogs
US7427636B2 (en) 2003-04-25 2008-09-23 Gilead Sciences, Inc. Inosine monophosphate dehydrogenase inhibitory phosphonate compounds
US7432261B2 (en) 2003-04-25 2008-10-07 Gilead Sciences, Inc. Anti-inflammatory phosphonate compounds
NZ542342A (en) 2003-04-25 2009-05-31 Gilead Sciences Inc Antiviral phosphonate analogs
EP1620109A2 (en) 2003-04-25 2006-02-01 Gilead Sciences, Inc. Kinase inhibitor phosphonate conjugates
WO2005002626A2 (en) 2003-04-25 2005-01-13 Gilead Sciences, Inc. Therapeutic phosphonate compounds
WO2004096285A2 (en) 2003-04-25 2004-11-11 Gilead Sciences, Inc. Anti-infective phosphonate conjugates
US7470724B2 (en) 2003-04-25 2008-12-30 Gilead Sciences, Inc. Phosphonate compounds having immuno-modulatory activity
US7273716B2 (en) 2003-04-25 2007-09-25 Gilead Sciences, Inc. Methods and compositions for identifying therapeutic compounds with GS-7340 ester hydrolase
US7407965B2 (en) 2003-04-25 2008-08-05 Gilead Sciences, Inc. Phosphonate analogs for treating metabolic diseases
WO2005044308A1 (en) 2003-10-24 2005-05-19 Gilead Sciences, Inc. Phosphonate analogs of antimetabolites
WO2005044279A1 (en) 2003-10-24 2005-05-19 Gilead Sciences, Inc. Purine nucleoside phosphonate conjugates
WO2005063751A1 (en) 2003-12-22 2005-07-14 Gilead Sciences, Inc. 4’-substituted carbovir-and abacavir-derivatives as well as related compounds with hiv and hcv antiviral activity
WO2010005986A1 (en) 2008-07-08 2010-01-14 Gilead Sciences, Inc. Salts of hiv inhibitor compounds
SI3661937T1 (en) 2017-08-01 2021-11-30 Gilead Sciences, Inc. Crystalline forms of ethyl ((s)-((((2r,5r)-5-(6-amino-9h-purin-9-yl)-4-fluoro-2,5-dihydrofuran-2-yl)oxy)methyl)(phenoxy)phosphoryl)-l-alaninate (gs-9131) for treating viral infections

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1992009297A1 (en) * 1990-11-30 1992-06-11 Smithkline Beecham Corporation Hiv protease inhibitors
WO1993007128A1 (en) * 1991-10-11 1993-04-15 The Du Pont Merck Pharmaceutical Company Cyclic ureas and analogues useful as retroviral protease inhibitiors
WO1994014793A1 (en) * 1992-12-29 1994-07-07 G. D. Searle & Co. Cyclic sulfone containing retroviral protease inhibitors
WO1994019329A1 (en) * 1993-02-26 1994-09-01 The Du Pont Merck Pharmaceutical Company Substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors
WO1995002582A1 (en) * 1993-07-14 1995-01-26 Ciba-Geigy Ag Cyclic hydrazine compounds

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1992009297A1 (en) * 1990-11-30 1992-06-11 Smithkline Beecham Corporation Hiv protease inhibitors
WO1993007128A1 (en) * 1991-10-11 1993-04-15 The Du Pont Merck Pharmaceutical Company Cyclic ureas and analogues useful as retroviral protease inhibitiors
WO1994014793A1 (en) * 1992-12-29 1994-07-07 G. D. Searle & Co. Cyclic sulfone containing retroviral protease inhibitors
WO1994019329A1 (en) * 1993-02-26 1994-09-01 The Du Pont Merck Pharmaceutical Company Substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors
WO1995002582A1 (en) * 1993-07-14 1995-01-26 Ciba-Geigy Ag Cyclic hydrazine compounds

Non-Patent Citations (7)

* Cited by examiner, † Cited by third party
Title
ABBENANTE,G. ET AL.: "Regioselective Structural and Functional Mimicry of Peptides. Design of Hydrolytically-Stable Cyclic Peptidomimetic Inhibitors of HIV-Protease", J.AM.CHEM.SOC., vol. 117, no. 41, 18 October 1995 (1995-10-18), WASHINGTON, pages 10220 - 10226 *
CHENERA,B. ET AL.: "Nonpetitde HIV Protease Inhibitors Designed to Replace a Bound Water", BIOORG.&MED.CHEM.LETT., vol. 3, no. 12, OXFORD, pages 2717 - 2722 *
GHOSH,A.K. ET AL.: "Cyclic Sulfone-3-Carboxamides as Novel P2-Ligands for RO 31-8959 Based HIV-1 Protease Inhibitors", BIOORG.&MED.CHEM.LETT., vol. 5, no. 1, OXFORD, pages 83 - 88 *
JADHAV,P.K. ET AL: "Synthesis of 8-Membered Cyclic Sulfamides : Novel HIV-1 Protease Inhibitors", TETRAHEDRON LETT., vol. 36, no. 36, 4 September 1995 (1995-09-04), OXFORD, pages 6383 - 6386 *
LAM,P.Y.S. ET AL.: "Rational Design of Potent, Bioavailable, Nonpeptide Cyclic Ureas as HIV Protease Inhibitors", SCIENCE, vol. 263, 21 January 1994 (1994-01-21), WASHINGTON, pages 380 - 384 *
RANDAD,R. ET AL.: "De Novo Design of Nonpeptidic HIV-1-Protease Inhibitors : Incorporation of Structural Water", BIOORG.&MED.CHEM.LETT., vol. 4, no. 10, OXFORD, pages 1247 - 1252 *
WONG,Y.N. ET AL.: "A Pharmacokinetic Evaluation of HIV Protease Inhibitors, Cyclic Ureas, in Rats and Dogs", BIOPHARM.&DRUG DISPOSITION, vol. 15, pages 535 - 544 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9579332B2 (en) 2004-07-27 2017-02-28 Gilead Sciences, Inc. Phosphonate analogs of HIV inhibitor compounds

Also Published As

Publication number Publication date
WO1996014314A2 (en) 1996-05-17
EP0789695A2 (en) 1997-08-20
AU710492B2 (en) 1999-09-23
JP2002515849A (en) 2002-05-28
CA2203570A1 (en) 1996-05-17
AU4234296A (en) 1996-05-31

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