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1. EP2734535 - 2',3'-DIDEOXY-2'-alpha-FLUORO-2'-beta-C-METHYLNUCLEOSIDES AND PRODRUGS THEREOF

Office
European Patent Office
Application Number 12814614
Application Date 19.07.2012
Publication Number 2734535
Publication Date 28.05.2014
Publication Kind A4
IPC
C07H 19/16
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
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
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 307/33
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
C07H 15/18
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
15Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
18Acyclic radicals, substituted by carbocyclic rings
C07H 19/207
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
207the phosphoric or polyphosphoric acids being esterified by a further hydroxylic compound, e.g. flavine-adenine dinucleotide or nicotinamide-adenine dinucleotide
CPC
C07F 7/1804
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
7Compounds containing elements of Groups 4 or 14 of the Periodic System
02Silicon compounds
08Compounds having one or more C—Si linkages
18Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
1804Compounds having Si-O-C linkages
C07H 1/00
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
1Processes for the preparation of sugar derivatives
C07H 13/00
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
13Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids
C07H 19/207
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
207the phosphoric or polyphosphoric acids being esterified by a further hydroxylic compound, e.g. flavine adenine dinucleotide or nicotinamide-adenine dinucleotide
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
Applicants NANJING MOLECULAR RES INC
Inventors CHANG JUNBIAO
HUANG QIANG
ZHOU SUPING
Designated States
Priority Data 201161509478 19.07.2011 US
Title
(DE) 2 ', 3'-DIDEOXY-2 '-ALPHA-FLUOR-2'-BETA-C-METHYLNUCLEOSIDE UND PRODRUGS DAVON
(EN) 2',3'-DIDEOXY-2'-alpha-FLUORO-2'-beta-C-METHYLNUCLEOSIDES AND PRODRUGS THEREOF
(FR) 2',3'-DIDÉSOXY-2'-alpha-FLUORO-2'-beta-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.