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WO2013036846A3 - N4 derivatives of deoxycytidine prodrugs - Google Patents

N4 derivatives of deoxycytidine prodrugs Download PDF

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Publication number
WO2013036846A3
WO2013036846A3 PCT/US2012/054277 US2012054277W WO2013036846A3 WO 2013036846 A3 WO2013036846 A3 WO 2013036846A3 US 2012054277 W US2012054277 W US 2012054277W WO 2013036846 A3 WO2013036846 A3 WO 2013036846A3
Authority
WO
WIPO (PCT)
Prior art keywords
prodrugs
deoxycytidine
derivatives
treatment
hypomethylation
Prior art date
Application number
PCT/US2012/054277
Other languages
French (fr)
Other versions
WO2013036846A2 (en
Inventor
Mark Fromhold
John Partridge
Original Assignee
Koronis Pharmaceuticals, Incorporated
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 Koronis Pharmaceuticals, Incorporated filed Critical Koronis Pharmaceuticals, Incorporated
Publication of WO2013036846A2 publication Critical patent/WO2013036846A2/en
Publication of WO2013036846A3 publication Critical patent/WO2013036846A3/en

Links

Classifications

    • 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
    • C07H19/12—Triazine radicals
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Virology (AREA)
  • Molecular Biology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biochemistry (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Engineering & Computer Science (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)

Abstract

The present invention provides hydrophobic prodrugs of nucleic acid bases, nucleosides, and nucleotides. The compounds of the invention have a structure according to Formula I. Methods for the hypomethylation of oligonucleotides, treatment of cancer, and treatment of HIV are also provided.
PCT/US2012/054277 2011-09-09 2012-09-07 N4 derivatives of deoxycytidine prodrugs WO2013036846A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161532975P 2011-09-09 2011-09-09
US61/532,975 2011-09-09

Publications (2)

Publication Number Publication Date
WO2013036846A2 WO2013036846A2 (en) 2013-03-14
WO2013036846A3 true WO2013036846A3 (en) 2013-05-02

Family

ID=47832796

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2012/054277 WO2013036846A2 (en) 2011-09-09 2012-09-07 N4 derivatives of deoxycytidine prodrugs

Country Status (1)

Country Link
WO (1) WO2013036846A2 (en)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6162349B1 (en) 2016-04-21 2017-07-12 大原薬品工業株式会社 Sacyl moiety silyl ether derivatives of 5-azacytidines
US10227374B2 (en) 2016-04-21 2019-03-12 Ohara Pharmaceutical Co., Ltd. Silyl etherified derivatives of 5-azacytidines in carbohydrate moiety
WO2017183215A1 (en) * 2016-04-21 2017-10-26 大原薬品工業株式会社 Sugar moiety silyl ether derivative of 5-azacytidine

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4900828A (en) * 1988-05-12 1990-02-13 Hoffmann-Laroche Inc. Intermediate compounds and an improved procedure for the synthesis of 2',3'-dideoxycytidine
US20080161548A1 (en) * 2006-12-22 2008-07-03 Roche Molecular Systems, Inc. Compounds and methods for synthesis and purification of oligonucleotides
US20080249097A1 (en) * 2003-06-20 2008-10-09 Koronis Pharmaceuticals, Incorporation Prodrugs of heteroaryl compounds
US20100075915A1 (en) * 2006-03-02 2010-03-25 Agency For Science, Technology And Research Methods for cancer therapy and stem cell modulation
US7772197B2 (en) * 2002-09-24 2010-08-10 1,3,5-Triazines for Treatment of Viral Diseases 1,3,5-triazines for treatment of viral diseases

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4900828A (en) * 1988-05-12 1990-02-13 Hoffmann-Laroche Inc. Intermediate compounds and an improved procedure for the synthesis of 2',3'-dideoxycytidine
US7772197B2 (en) * 2002-09-24 2010-08-10 1,3,5-Triazines for Treatment of Viral Diseases 1,3,5-triazines for treatment of viral diseases
US20080249097A1 (en) * 2003-06-20 2008-10-09 Koronis Pharmaceuticals, Incorporation Prodrugs of heteroaryl compounds
US20100075915A1 (en) * 2006-03-02 2010-03-25 Agency For Science, Technology And Research Methods for cancer therapy and stem cell modulation
US20080161548A1 (en) * 2006-12-22 2008-07-03 Roche Molecular Systems, Inc. Compounds and methods for synthesis and purification of oligonucleotides

Also Published As

Publication number Publication date
WO2013036846A2 (en) 2013-03-14

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