WO2003051306A3 - N4-acylcytosine-1,3-dioxolane nucleosides for treatment of viral infections - Google Patents

N4-acylcytosine-1,3-dioxolane nucleosides for treatment of viral infections Download PDF

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Publication number
WO2003051306A3
WO2003051306A3 PCT/US2002/040090 US0240090W WO03051306A3 WO 2003051306 A3 WO2003051306 A3 WO 2003051306A3 US 0240090 W US0240090 W US 0240090W WO 03051306 A3 WO03051306 A3 WO 03051306A3
Authority
WO
WIPO (PCT)
Prior art keywords
acylcytosine
viral infections
treatment
dioxolane nucleosides
dioxolane
Prior art date
Application number
PCT/US2002/040090
Other languages
French (fr)
Other versions
WO2003051306A2 (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 AU2002364730A priority Critical patent/AU2002364730A1/en
Publication of WO2003051306A2 publication Critical patent/WO2003051306A2/en
Publication of WO2003051306A3 publication Critical patent/WO2003051306A3/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 comound, use and composition of treating or preventing viral infections, in particular, human immunodeficiency virus 8HIV) and hepatitis B virus (HBV) infections, in human patients or other animal hosts, comprising the administration of N4-acylcytosine-1,3-dioxolane and pharmaceutically acceptable salts, prodrugs, and other derivatives thereof.
PCT/US2002/040090 2001-12-14 2002-12-16 N4-acylcytosine-1,3-dioxolane nucleosides for treatment of viral infections WO2003051306A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2002364730A AU2002364730A1 (en) 2001-12-14 2002-12-16 N4-acylcytosine-1,3-dioxolane nucleosides for treatment of viral infections

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
WO2003051306A2 WO2003051306A2 (en) 2003-06-26
WO2003051306A3 true WO2003051306A3 (en) 2003-12-18

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 Before (1)

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

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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CN101172993A (en) * 2002-06-28 2008-05-07 埃迪尼克斯(开曼)有限公司 2'-c-methyl-3'-o-l-valine ester ribofuranosyl cytidine for treatment of flaviviridae infections
RS113904A (en) * 2002-06-28 2007-02-05 Idenix (Cayman) Limited 2'-c-methyl-3'-o-l-valine ester ribofuranosyl cytidine for treatment of flaviviridae infections
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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HUE033832T2 (en) 2002-11-15 2018-01-29 Idenix Pharmaceuticals Llc 2'-methyl nucleosides in combination with interferon and flaviviridae mutation
US7598373B2 (en) * 2002-12-12 2009-10-06 Idenix Pharmaceuticals, Inc. Process for the production of 2-C-methyl-D-ribonolactone
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US7741334B2 (en) * 2004-04-01 2010-06-22 Achillion Pharmaceuticals, Inc. Low dose therapy for treating viral infections
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SI3109244T1 (en) 2004-09-14 2019-06-28 Gilead Pharmasset Llc Preparation of 2'fluoro-2'-alkyl-substituted or other optionally substituted ribofuranosyl pyrimidines and purines and their derivatives
EP1802315A2 (en) * 2004-10-19 2007-07-04 Achillion Pharmaceuticals, Inc. Combination therapy for treating viral infections
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
EP2671888A1 (en) 2008-12-23 2013-12-11 Gilead Pharmasset LLC 3',5'-cyclic nucleoside phosphate analogues
NZ617066A (en) 2008-12-23 2015-02-27 Gilead Pharmasset Llc Nucleoside analogs
CA2748057C (en) 2008-12-23 2018-07-03 Pharmasset, Inc. Nucleoside phosphoramidates
TWI576352B (en) 2009-05-20 2017-04-01 基利法瑪席特有限責任公司 Nucleoside phosphoramidates
US8618076B2 (en) 2009-05-20 2013-12-31 Gilead Pharmasset Llc Nucleoside phosphoramidates
PL3290428T3 (en) 2010-03-31 2022-02-07 Gilead Pharmasset Llc Tablet comprising crystalline (s)-isopropyl 2-(((s)-(((2r,3r,4r,5r)-5-(2,4-dioxo-3,4-dihydropyrimidin-1 (2h)-yl)-4-fluoro-3-hydroxy-4-methyltetrahydrofuran-2-yl)methoxy)(phenoxy)phosphoryl)amino)propanoate
CL2011000716A1 (en) 2010-03-31 2012-04-20 Gilead Pharmasset Llc Crystalline forms 1 6 of (s) -isopropyl-2 - (((s) - (((2r.3r.4r.5r) -5- (2,4-dioxo-3,4-dihydropyrimidin-1 (2h) -yl) -4-fluoro-3-hydroxy-4-methyl tetrahydrofuran-2-yl) methoxy) (phenoxy) phosphoryl) amino) propanoate; pharmaceutical composition and combination; and its use to treat a hepatitis c virus infection.
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Also Published As

Publication number Publication date
USRE42015E1 (en) 2010-12-28
JP2005519916A (en) 2005-07-07
US20070078080A1 (en) 2007-04-05
US8114997B2 (en) 2012-02-14
US20040214844A1 (en) 2004-10-28
WO2003063771A3 (en) 2005-07-07
CA2470255A1 (en) 2003-08-07
US20030176319A1 (en) 2003-09-18
EP1569652A4 (en) 2008-07-02
AU2002364730A8 (en) 2003-06-30
KR100978904B1 (en) 2010-08-31
WO2003063771A2 (en) 2003-08-07
CN1617726A (en) 2005-05-18
CA2470255C (en) 2012-01-17
US7105527B2 (en) 2006-09-12
AU2002365234B2 (en) 2009-01-29
EP1569652A2 (en) 2005-09-07
AU2002364730A1 (en) 2003-06-30
CN100560073C (en) 2009-11-18
MXPA04005779A (en) 2005-05-16
BR0214944A (en) 2005-06-07
KR20040094398A (en) 2004-11-09
US20090176730A1 (en) 2009-07-09
US6908924B2 (en) 2005-06-21
WO2003051306A2 (en) 2003-06-26
US20120202766A1 (en) 2012-08-09

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