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1. WO2013013009 - 2',3'-DIDEOXY-2'-α-FLUORO-2'-β-C-METHYLNUCLEOSIDES AND PRODRUGS THEREOF

Publication Number WO/2013/013009
Publication Date 24.01.2013
International Application No. PCT/US2012/047338
International Filing Date 19.07.2012
IPC
C07D 473/18 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
473Heterocyclic compounds containing purine ring systems
02with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6
18one oxygen and one nitrogen atom, e.g. guanine
CPC
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
A61P 31/14
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
12Antivirals
14for RNA viruses
C07D 307/20
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
307Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
02not condensed with other rings
04having no double bonds between ring members or between ring members and non-ring members
18with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
20Oxygen atoms
C07D 307/33
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
307Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
02not condensed with other rings
26having one double bond between ring members or between a ring member and a non-ring member
30with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
32Oxygen atoms
33in position 2, the oxygen atom being in its keto or unsubstituted enol form
Applicants
  • NANJING MOLECULAR RESEARCH, INC. [CN]/[CN] (AllExceptUS)
  • HUANG, Qiang [CN]/[CN] (UsOnly)
  • ZHOU, Suping [CN]/[US] (UsOnly)
  • CHANG, Junbiao [CN]/[CN] (UsOnly)
Inventors
  • HUANG, Qiang
  • ZHOU, Suping
  • CHANG, Junbiao
Agents
  • LIU, Wansheng, Jerry
Priority Data
61/509,47819.07.2011US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) 2',3'-DIDEOXY-2'-α-FLUORO-2'-β-C-METHYLNUCLEOSIDES AND PRODRUGS THEREOF
(FR) 2',3'-DIDÉSOXY-2'-A-FLUORO-2'-SS-C-MÉTHYLNUCLÉOSIDES ET LEURS PROMÉDICAMENTS
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.
(FR)
La présente invention concerne des 2',3'-didésoxy-2'-fluoro-α-2'-C-méthylnucléosides, leurs promédicaments et leur utilisation thérapeutique comme agents anti-VHC. La présente invention concerne également des procédés et des intermédiaires pour la préparation des nucléosides décrits ici.
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