WO2003063771A3 - N4-acylcytosine nucleosides for treatment of viral iinfections - Google Patents

N4-acylcytosine nucleosides for treatment of viral iinfections Download PDF

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Publication number
WO2003063771A3
WO2003063771A3 PCT/US2002/040081 US0240081W WO03063771A3 WO 2003063771 A3 WO2003063771 A3 WO 2003063771A3 US 0240081 W US0240081 W US 0240081W WO 03063771 A3 WO03063771 A3 WO 03063771A3
Authority
WO
WIPO (PCT)
Prior art keywords
iinfections
acylcytosine
nucleosides
viral
treatment
Prior art date
Application number
PCT/US2002/040081
Other languages
French (fr)
Other versions
WO2003063771A2 (en
Inventor
Kyoichi A Watanabe
Junxing Shi
Michael J Otto
Original Assignee
Pharmasset Ltd
Kyoichi A Watanabe
Junxing Shi
Michael J Otto
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 Pharmasset Ltd, Kyoichi A Watanabe, Junxing Shi, Michael J Otto filed Critical Pharmasset Ltd
Priority to CA2470255A priority Critical patent/CA2470255C/en
Priority to BR0214944-3A priority patent/BR0214944A/en
Priority to KR1020047009263A priority patent/KR100978904B1/en
Priority to JP2003563467A priority patent/JP2005519916A/en
Priority to MXPA04005779A priority patent/MXPA04005779A/en
Priority to AU2002365234A priority patent/AU2002365234B2/en
Priority to EP02804833A priority patent/EP1569652A4/en
Publication of WO2003063771A2 publication Critical patent/WO2003063771A2/en
Publication of WO2003063771A3 publication Critical patent/WO2003063771A3/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06—Pyrimidine radicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • 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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • 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
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
    • 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
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/18—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 one oxygen and one nitrogen atom, e.g. guanine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/16—Purine radicals

Abstract

The present invention is directed to a method and composition of treating or preventing viral infections, in particular, human immunodeficiency virus (HIV) and hepatitis B virus (HBV) infections, in human patients or other animals hosts, comprising the administration of N4-acyl-2',3'-dideoxy-5-flluorocytidine or N4-acyl-2',3'-didehydro-2',3' dideoxy-5-fluorocytidine, and pharmaceutically acceptable salts, prodrugs, and other derivatives thereof.
PCT/US2002/040081 2001-12-14 2002-12-13 N4-acylcytosine nucleosides for treatment of viral iinfections WO2003063771A2 (en)

Priority Applications (7)

Application Number Priority Date Filing Date Title
CA2470255A CA2470255C (en) 2001-12-14 2002-12-13 N4-acylcytosine nucleosides for treatment of viral infections
BR0214944-3A BR0214944A (en) 2001-12-14 2002-12-13 N4-Acylcytosine Nucleosides for the Treatment of Viral Infections
KR1020047009263A KR100978904B1 (en) 2001-12-14 2002-12-13 N4-Acylcytosine nucleosides for treatment of viral infections
JP2003563467A JP2005519916A (en) 2001-12-14 2002-12-13 N4-acylcytosine nucleosides for the treatment of viral infection
MXPA04005779A MXPA04005779A (en) 2001-12-14 2002-12-13 N4.
AU2002365234A AU2002365234B2 (en) 2001-12-14 2002-12-13 N4-acylcytosine nucleosides for treatment of viral infections
EP02804833A EP1569652A4 (en) 2001-12-14 2002-12-13 N sp 4 /sp-acylcytosine nucleosides for treatment of viral iinfections

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US34155501P 2001-12-14 2001-12-14
US60/341,555 2001-12-14

Publications (2)

Publication Number Publication Date
WO2003063771A2 WO2003063771A2 (en) 2003-08-07
WO2003063771A3 true WO2003063771A3 (en) 2005-07-07

Family

ID=23338072

Family Applications (2)

Application Number Title Priority Date Filing Date
PCT/US2002/040081 WO2003063771A2 (en) 2001-12-14 2002-12-13 N4-acylcytosine nucleosides for treatment of viral iinfections
PCT/US2002/040090 WO2003051306A2 (en) 2001-12-14 2002-12-16 N4-acylcytosine-1,3-dioxolane nucleosides for treatment of viral infections

Family Applications After (1)

Application Number Title Priority Date Filing Date
PCT/US2002/040090 WO2003051306A2 (en) 2001-12-14 2002-12-16 N4-acylcytosine-1,3-dioxolane nucleosides for treatment of viral infections

Country Status (10)

Country Link
US (6) US7105527B2 (en)
EP (1) EP1569652A4 (en)
JP (1) JP2005519916A (en)
KR (1) KR100978904B1 (en)
CN (1) CN100560073C (en)
AU (2) AU2002365234B2 (en)
BR (1) BR0214944A (en)
CA (1) CA2470255C (en)
MX (1) MXPA04005779A (en)
WO (2) WO2003063771A2 (en)

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MY164523A (en) * 2000-05-23 2017-12-29 Univ Degli Studi Cagliari Methods and compositions for treating hepatitis c virus
EP1736478B1 (en) 2000-05-26 2015-07-22 IDENIX Pharmaceuticals, Inc. Methods and compositions for treating flaviviruses and pestiviruses
EP1569652A4 (en) * 2001-12-14 2008-07-02 Pharmasset Inc N sp 4 /sp-acylcytosine nucleosides for treatment of viral iinfections
US7608600B2 (en) * 2002-06-28 2009-10-27 Idenix Pharmaceuticals, Inc. Modified 2′ and 3′-nucleoside prodrugs for treating Flaviviridae infections
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AP2005003213A0 (en) * 2002-06-28 2005-03-31 Univ Cagliari 2'-C-methyl-3'-O-L-valine ester ribofuranosyl cytidine for treatment of flaviviridae infections.
IL166640A0 (en) 2002-08-01 2006-01-15 Pharmasset Ltd Compounds with the bicyclo Ä4.2.1Ü nonane system for the treatment of flaviviridae infections
HUE033832T2 (en) 2002-11-15 2018-01-29 Idenix Pharmaceuticals Llc 2'-methyl nucleosides in combination with interferon and flaviviridae mutation
CA2509687C (en) * 2002-12-12 2012-08-14 Idenix (Cayman) Limited Process for the production of 2'-branched nucleosides
CA2425031A1 (en) * 2003-04-01 2004-10-01 Smithkline Beecham Corporation Pharmaceutical compositions
CN100503628C (en) 2003-05-30 2009-06-24 法莫赛特股份有限公司 Modified fluorinated nucleoside analogues
US7741334B2 (en) * 2004-04-01 2010-06-22 Achillion Pharmaceuticals, Inc. Low dose therapy for treating viral infections
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US7968703B2 (en) * 2005-03-07 2011-06-28 Shire Canada Inc. Process and methods for the preparation of optically active cis-2-hydroxymethyl-4- (cytosin-1'-yl)-1,3-oxathiolane or pharmaceutically acceptable salts thereof
CA2634749C (en) * 2005-12-23 2014-08-19 Idenix Pharmaceuticals, Inc. Process for preparing a synthetic intermediate for preparation of branched nucleosides
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US7964580B2 (en) 2007-03-30 2011-06-21 Pharmasset, Inc. Nucleoside phosphoramidate prodrugs
US8173621B2 (en) 2008-06-11 2012-05-08 Gilead Pharmasset Llc Nucleoside cyclicphosphates
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US8618076B2 (en) 2009-05-20 2013-12-31 Gilead Pharmasset Llc Nucleoside phosphoramidates
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Also Published As

Publication number Publication date
EP1569652A2 (en) 2005-09-07
EP1569652A4 (en) 2008-07-02
US20070078080A1 (en) 2007-04-05
KR20040094398A (en) 2004-11-09
JP2005519916A (en) 2005-07-07
US20030176319A1 (en) 2003-09-18
US8114997B2 (en) 2012-02-14
CA2470255C (en) 2012-01-17
CA2470255A1 (en) 2003-08-07
MXPA04005779A (en) 2005-05-16
WO2003063771A2 (en) 2003-08-07
US7105527B2 (en) 2006-09-12
AU2002364730A8 (en) 2003-06-30
WO2003051306A2 (en) 2003-06-26
CN100560073C (en) 2009-11-18
AU2002364730A1 (en) 2003-06-30
BR0214944A (en) 2005-06-07
US6908924B2 (en) 2005-06-21
US20090176730A1 (en) 2009-07-09
KR100978904B1 (en) 2010-08-31
US20040214844A1 (en) 2004-10-28
USRE42015E1 (en) 2010-12-28
US20120202766A1 (en) 2012-08-09
WO2003051306A3 (en) 2003-12-18
AU2002365234B2 (en) 2009-01-29
CN1617726A (en) 2005-05-18

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