WO1996032403A3 - Novel cytosine and cytidine derivatives - Google Patents

Novel cytosine and cytidine derivatives Download PDF

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Publication number
WO1996032403A3
WO1996032403A3 PCT/EP1996/001595 EP9601595W WO9632403A3 WO 1996032403 A3 WO1996032403 A3 WO 1996032403A3 EP 9601595 W EP9601595 W EP 9601595W WO 9632403 A3 WO9632403 A3 WO 9632403A3
Authority
WO
WIPO (PCT)
Prior art keywords
cytidine derivatives
cytosine
novel
novel cytosine
cytidine
Prior art date
Application number
PCT/EP1996/001595
Other languages
German (de)
French (fr)
Other versions
WO1996032403A2 (en
Inventor
Helmut Vorbrueggen
Konrad Krolikiewicz
Michael Schirner
Martin Schneider
Herbert Wiesinger
Original Assignee
Schering Ag
Helmut Vorbrueggen
Konrad Krolikiewicz
Michael Schirner
Martin Schneider
Herbert Wiesinger
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 Schering Ag, Helmut Vorbrueggen, Konrad Krolikiewicz, Michael Schirner, Martin Schneider, Herbert Wiesinger filed Critical Schering Ag
Priority to AU54000/96A priority Critical patent/AU5400096A/en
Publication of WO1996032403A2 publication Critical patent/WO1996032403A2/en
Publication of WO1996032403A3 publication Critical patent/WO1996032403A3/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • 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
    • C07H19/14—Pyrrolo-pyrimidine radicals

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biochemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)

Abstract

The invention concerns cytosine and cytidine derivatives of general formula (1) and their production and use in medicaments.
PCT/EP1996/001595 1995-04-12 1996-04-12 Novel cytosine and cytidine derivatives WO1996032403A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU54000/96A AU5400096A (en) 1995-04-12 1996-04-12 Novel cytosine and cytidine derivatives

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19514523.2 1995-04-12
DE1995114523 DE19514523A1 (en) 1995-04-12 1995-04-12 New cytosine and cytidine derivatives

Publications (2)

Publication Number Publication Date
WO1996032403A2 WO1996032403A2 (en) 1996-10-17
WO1996032403A3 true WO1996032403A3 (en) 1996-11-28

Family

ID=7759937

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP1996/001595 WO1996032403A2 (en) 1995-04-12 1996-04-12 Novel cytosine and cytidine derivatives

Country Status (3)

Country Link
AU (1) AU5400096A (en)
DE (1) DE19514523A1 (en)
WO (1) WO1996032403A2 (en)

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8841275B2 (en) 2010-11-30 2014-09-23 Gilead Pharmasset Llc 2′-spiro-nucleosides and derivatives thereof useful for treating hepatitis C virus and dengue virus infections
US8957046B2 (en) 2007-03-30 2015-02-17 Gilead Pharmasset Llc Nucleoside phosphoramidate prodrugs
US9045520B2 (en) 2008-12-23 2015-06-02 Gilead Pharmasset Llc Synthesis of purine nucleosides
US9393256B2 (en) 2011-09-16 2016-07-19 Gilead Pharmasset Llc Methods for treating HCV
US9549941B2 (en) 2011-11-29 2017-01-24 Gilead Pharmasset Llc Compositions and methods for treating hepatitis C virus

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SI1633766T1 (en) 2003-05-30 2019-06-28 Gilead Pharmasset Llc Modified fluorinated nucleoside analogues
NZ554442A (en) 2004-09-14 2011-05-27 Pharmasset Inc Preparation of 2'fluoro-2'-alkyl-substituted or other optionally substituted ribofuranosyl pyrimidines and purines and their derivatives
MX2011006891A (en) 2008-12-23 2011-10-06 Pharmasset Inc Nucleoside phosphoramidates.
EA201100851A1 (en) 2008-12-23 2012-04-30 Фармассет, Инк. NUCLEOSIDE ANALOGUES
US8618076B2 (en) 2009-05-20 2013-12-31 Gilead Pharmasset Llc Nucleoside phosphoramidates
TWI583692B (en) 2009-05-20 2017-05-21 基利法瑪席特有限責任公司 Nucleoside phosphoramidates
EP2552931B1 (en) 2010-03-31 2014-07-23 Gilead Pharmasset LLC Stereoselective synthesis of phosphorus containing actives
MY172166A (en) 2013-01-31 2019-11-15 Gilead Pharmasset Llc Combination formulation of two antiviral compounds
PT3038601T (en) 2013-08-27 2020-06-30 Gilead Pharmasset Llc Combination formulation of two antiviral compounds

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS62255499A (en) * 1986-04-28 1987-11-07 Teijin Ltd Fluorescent nucleoside or nucleotide
WO1991011186A1 (en) * 1990-02-01 1991-08-08 Emory University Method and compositions for the synthesis of bch-189 and related compounds

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS62255499A (en) * 1986-04-28 1987-11-07 Teijin Ltd Fluorescent nucleoside or nucleotide
WO1991011186A1 (en) * 1990-02-01 1991-08-08 Emory University Method and compositions for the synthesis of bch-189 and related compounds

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
BRODFUEHRER P.R. ET AL: "A Practical Synthesis of (S)-HPMPC", TETRAHEDRON LETTERS, vol. 35, no. 20, 1994, OXFORD GB, pages 3243 - 3246, XP002012084 *
ELEVENTH INTERNATIONAL ROUND TABLE ON NUCLEOSIDES, NUCLEOTIDES AND THEIR BIOLOGICAL APPLICATIONS, 7 September 1994 (1994-09-07) - 11 September 1994 (1994-09-11), LEUVEN, BE *
HARNDEN M.R. ET AL: "Novel Acyclonucleotides: Synthesis and Antiviral Activity of Alkenylphosponic Acid Derivatives of Purines and a Pyrimidine", JOURNAL OF MEDICINAL CHEMISTRY, vol. 36, 1993, WASHINGTON US, pages 1343 - 1355, XP002012083 *
LOAKES, D. ET AL: "The synthesis of bicyclic N4-amino-2'-deoxycytidine derivatives", NUCLEOSIDES NUCLEOTIDES, vol. 14, no. 3-5, May 1995 (1995-05-01), pages 291 - 293, XP002013445 *
PATENT ABSTRACTS OF JAPAN vol. 012, no. 139 (C - 491) 27 April 1988 (1988-04-27) *

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8957046B2 (en) 2007-03-30 2015-02-17 Gilead Pharmasset Llc Nucleoside phosphoramidate prodrugs
US9045520B2 (en) 2008-12-23 2015-06-02 Gilead Pharmasset Llc Synthesis of purine nucleosides
US8841275B2 (en) 2010-11-30 2014-09-23 Gilead Pharmasset Llc 2′-spiro-nucleosides and derivatives thereof useful for treating hepatitis C virus and dengue virus infections
US9394331B2 (en) 2010-11-30 2016-07-19 Gilead Pharmasset Llc 2′-spiro-nucleosides and derivatives thereof useful for treating hepatitis C virus and dengue virus infections
US9393256B2 (en) 2011-09-16 2016-07-19 Gilead Pharmasset Llc Methods for treating HCV
US9549941B2 (en) 2011-11-29 2017-01-24 Gilead Pharmasset Llc Compositions and methods for treating hepatitis C virus

Also Published As

Publication number Publication date
AU5400096A (en) 1996-10-30
DE19514523A1 (en) 1996-10-17
WO1996032403A2 (en) 1996-10-17

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