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1. US20140315850 - 2',3'-Dideoxy-2'-alpha-Fluoro-2'-beta-C-Methylnucleosides and Prodrugs Thereof

Office
United States of America
Application Number 14233641
Application Date 19.07.2012
Publication Number 20140315850
Publication Date 23.10.2014
Publication Kind A1
IPC
C07H 19/20
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
19Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro derivatives thereof
02sharing nitrogen
04Heterocyclic radicals containing only nitrogen as ring hetero atom
16Purine radicals
20with the saccharide radical being esterified by phosphoric or polyphosphoric acids
A61K 31/708
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
70Carbohydrates; Sugars; Derivatives thereof
7042Compounds having saccharide radicals and heterocyclic rings
7052having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
706containing six-membered rings with nitrogen as a ring hetero atom
7064containing condensed or non-condensed pyrimidines
7076containing purines, e.g. adenosine, adenylic acid
708having oxo groups directly attached to the purine ring system, e.g. guanosine, guanylic acid
A61K 45/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/-A61K41/132
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 31/7076
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
70Carbohydrates; Sugars; Derivatives thereof
7042Compounds having saccharide radicals and heterocyclic rings
7052having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
706containing six-membered rings with nitrogen as a ring hetero atom
7064containing condensed or non-condensed pyrimidines
7076containing purines, e.g. adenosine, adenylic acid
CPC
C07H 19/20
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
19Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides ; Anhydro-derivatives thereof
02sharing nitrogen
04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
16Purine radicals
20with the saccharide radical esterified by phosphoric or polyphosphoric acids
A61K 31/7076
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
70Carbohydrates; Sugars; Derivatives thereof
7042Compounds having saccharide radicals and heterocyclic rings
7052having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
706containing six-membered rings with nitrogen as a ring hetero atom
7064containing condensed or non-condensed pyrimidines
7076containing purines, e.g. adenosine, adenylic acid
A61K 31/708
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
70Carbohydrates; Sugars; Derivatives thereof
7042Compounds having saccharide radicals and heterocyclic rings
7052having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
706containing six-membered rings with nitrogen as a ring hetero atom
7064containing condensed or non-condensed pyrimidines
7076containing purines, e.g. adenosine, adenylic acid
708having oxo groups directly attached to the purine ring system, e.g. guanosine, guanylic acid
A61K 45/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
Applicants Huang Qiang
Nanjing Molecular Research, Inc.
Zhou Suping
Chang Junbiao
Inventors Huang Qiang
Zhou Suping
Chang Junbiao
Title
(EN) 2',3'-Dideoxy-2'-alpha-Fluoro-2'-beta-C-Methylnucleosides and Prodrugs Thereof
Abstract
(EN)

The present invention is made to fulfill the foregoing need. Since most of antiHN nucleosides are 2′,3′-dideoxynucleosides that have been proved to be excellent substrates of kinases for the phosphorylations. 2′,3′-Dideoxy-2,-a-fluoro-2′-{3-C-methyl-nucleosides can be considered as one unique class of 2′,3′-dideoxynucleosides to be good substrate of kinases because fluorine mimics hydrogen. It also can be considered as ribo-nucleosides to incorporate into RNA of HCV because 2′-fluorine-a mimics 2′-a-OH group.