PE20141599A1 - Derivados de los nucleosidos sustituidos en 4'-azido, 3'-fluoro como inhibidores de la replicacion del rna del vhc - Google Patents

Derivados de los nucleosidos sustituidos en 4'-azido, 3'-fluoro como inhibidores de la replicacion del rna del vhc

Info

Publication number
PE20141599A1
PE20141599A1 PE2014000990A PE2014000990A PE20141599A1 PE 20141599 A1 PE20141599 A1 PE 20141599A1 PE 2014000990 A PE2014000990 A PE 2014000990A PE 2014000990 A PE2014000990 A PE 2014000990A PE 20141599 A1 PE20141599 A1 PE 20141599A1
Authority
PE
Peru
Prior art keywords
ilo
azide
inhibitors
fluorine
derivatives
Prior art date
Application number
PE2014000990A
Other languages
English (en)
Inventor
Mark Smith
Francisco Xavier Talamas
Jing Zhang
Zhuming Zhang
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of PE20141599A1 publication Critical patent/PE20141599A1/es

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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
    • C07H19/06—Pyrimidine radicals
    • C07H19/10—Pyrimidine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • A61K31/7072—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • 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
    • C07H19/06—Pyrimidine radicals
    • 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
    • C07H19/16—Purine radicals

Abstract

SE REFIERE A COMPUESTOS DE FORMULA (I), EN DONDE: R1 ES H, HALOALQUILO INFERIOR O ARILO; R2a Y R2b SON INDEPENDIENTEMENTE, H, CH2SH, HIDROXIALQUILO INFERIOR, (1H-INDOL-3-ILO)METILO, (1H-INDOL-4-ILO)METILO, ENTRE OTROS; R3 ES H, ALQUILO INFERIOR, HALOALQUILO INFERIOR, FENILO O FENILALQUILO INFERIOR; R4 ES H, ALQUILO INFERIOR, O R2b Y R4 JUNTOS FORMAN (CH2)3; R5 ES H, ENTRE OTROS; R6 ES a), ENTRE OTROS. SON COMPUESTOS PREFERIDOS: (S)-2-{[(2R,3S,4S,5R)-2-AZIDO-5-(2,4-DIOXO-3,4-DIHIDRO-2H-PIRIMIDIN-1-ILO)-3-FLUORO-4-HIDROXI-TETRAHIDRO-FURAN-2-ILMETOXI]-FENOXI-FOSFORILAMINO}-PROPIONATO DE ISOPROPILO; (S)-2-[[(2R,3S,4S,5R)-5-(4-AMINO-2-OXO-2H-PIRIMIDIN-1-ILO)-2-AZIDO-3-FLUORO-4-HIDROXI-TETRAHIDRO-FURAN-2-ILMETOXI]-(NAFTALEN-1-ILOXI)-FOSFORILAMINO]-PROPIONATO DE ISOPROPILO; ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTO SON UTILES PARA EL TRATAMIENTO DE LA INFECCION POR EL VIRUS DE LA HEPATITIS C (VHC)
PE2014000990A 2011-12-20 2012-12-17 Derivados de los nucleosidos sustituidos en 4'-azido, 3'-fluoro como inhibidores de la replicacion del rna del vhc PE20141599A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201161577712P 2011-12-20 2011-12-20

Publications (1)

Publication Number Publication Date
PE20141599A1 true PE20141599A1 (es) 2014-10-30

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
PE2014000990A PE20141599A1 (es) 2011-12-20 2012-12-17 Derivados de los nucleosidos sustituidos en 4'-azido, 3'-fluoro como inhibidores de la replicacion del rna del vhc

Country Status (31)

Country Link
US (1) US9708357B2 (es)
EP (1) EP2794628B1 (es)
JP (1) JP6118336B2 (es)
KR (1) KR101687084B1 (es)
CN (2) CN104011060A (es)
AU (1) AU2012357986B2 (es)
BR (1) BR112014015066A2 (es)
CA (1) CA2869317C (es)
CL (1) CL2014001599A1 (es)
CO (1) CO6990719A2 (es)
CR (1) CR20140255A (es)
CY (1) CY1119015T1 (es)
DK (1) DK2794628T3 (es)
EA (1) EA024847B1 (es)
ES (1) ES2626484T3 (es)
HK (2) HK1199037A1 (es)
HU (1) HUE033332T2 (es)
IL (1) IL232843B (es)
IN (1) IN2014CN04530A (es)
LT (1) LT2794628T (es)
MA (1) MA35749B1 (es)
MX (1) MX350810B (es)
PE (1) PE20141599A1 (es)
PH (1) PH12014501283A1 (es)
PL (1) PL2794628T3 (es)
PT (1) PT2794628T (es)
SG (1) SG11201403086YA (es)
SI (1) SI2794628T1 (es)
UA (1) UA110428C2 (es)
WO (1) WO2013092447A1 (es)
ZA (1) ZA201404444B (es)

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IN2014CN04530A (es) 2015-09-11
US20140369959A1 (en) 2014-12-18
EA201491180A1 (ru) 2014-11-28
KR20140108303A (ko) 2014-09-05
ES2626484T3 (es) 2017-07-25
PH12014501283A1 (en) 2014-09-08
CA2869317A1 (en) 2013-06-27
BR112014015066A2 (pt) 2017-06-13
CN108409820A (zh) 2018-08-17
MX2014007028A (es) 2014-09-16
CL2014001599A1 (es) 2014-11-03
CA2869317C (en) 2016-05-17
NZ625844A (en) 2016-08-26
AU2012357986B2 (en) 2017-02-02
KR101687084B1 (ko) 2016-12-15
EP2794628A1 (en) 2014-10-29
PT2794628T (pt) 2017-07-05
IL232843B (en) 2018-02-28
US9708357B2 (en) 2017-07-18
HK1199037A1 (en) 2015-06-19
IL232843A0 (en) 2014-07-31
MA35749B1 (fr) 2014-12-01
EA024847B1 (ru) 2016-10-31
CR20140255A (es) 2014-08-20
WO2013092447A1 (en) 2013-06-27
HK1200835A1 (en) 2015-08-14
JP6118336B2 (ja) 2017-04-19
UA110428C2 (uk) 2015-12-25
AU2012357986A1 (en) 2014-06-19
SG11201403086YA (en) 2014-07-30
DK2794628T3 (en) 2017-07-10
CN104011060A (zh) 2014-08-27
CY1119015T1 (el) 2018-01-10
HUE033332T2 (en) 2017-11-28
JP2015500851A (ja) 2015-01-08
MX350810B (es) 2017-09-20
PL2794628T3 (pl) 2017-09-29
LT2794628T (lt) 2017-07-10
ZA201404444B (en) 2015-08-26
EP2794628B1 (en) 2017-03-29
SI2794628T1 (sl) 2017-07-31
CO6990719A2 (es) 2014-07-10

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