AR044566A1 - Analogos de nucleosidos fluorados modificados - Google Patents

Analogos de nucleosidos fluorados modificados

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Publication number
AR044566A1
AR044566A1 ARP040101821A ARP040101821A AR044566A1 AR 044566 A1 AR044566 A1 AR 044566A1 AR P040101821 A ARP040101821 A AR P040101821A AR P040101821 A ARP040101821 A AR P040101821A AR 044566 A1 AR044566 A1 AR 044566A1
Authority
AR
Argentina
Prior art keywords
alkyl
alkenyl
acyl
alkynyl
optionally substituted
Prior art date
Application number
ARP040101821A
Other languages
English (en)
Inventor
Jeremy Clark
Original Assignee
Pharmasset Inc
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=33563735&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR044566(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Pharmasset Inc filed Critical Pharmasset Inc
Publication of AR044566A1 publication Critical patent/AR044566A1/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
    • 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
    • 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
    • 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
    • A61P31/04—Antibacterial agents
    • 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
    • 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
    • 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
    • A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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
    • C07H19/048—Pyridine 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
    • C07H19/06—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
    • C07H19/14—Pyrrolo-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

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Biochemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)

Abstract

Se provee composiciones y métodos de tratamiento de una infección con Flaviviridae, incluyendo infección con virus de la hepatitis C, virus del Nilo Occidental, virus de la fiebre amarilla, y un rinovirus, en un hospedante, incluyendo animales y especialmente humanos, utilizando (2'R)-2'-desoxi-2'-fluoro-2'-C-metil nucleósidos, o una sal o prodroga farmacéuticamente aceptable de los mismos. Reivindicación 1: Un (2'R)-2'-desoxi-2'-fluoro-2'-metil nucleósido (b-D o b-L) de la fórmula (1), en donde Base es una base purina o pirimidina; X es O, S, CH2, Se, NH, N-alquilo, CHW (R, S, ó racémico), C(W)2, en donde W es F, Cl, Br o I; R1 y R7 son independientemente H, fosfato, incluyendo monofosfato, difosfato, trifosfato o una prodroga de fosfato estabilizada, H-fosfonato, incluyendo H-fosfonatos estabilizados, acilo, incluyendo fenilo opcionalmente sustituido y acilo inferior, alquilo, incluyendo alquilo inferior, carboxialquilamino O-sustituido o sus derivados péptidos, éster sulfonato, incluyendo alquil o arilalquil sulfonilo, incluyendo metansulfonilo y bencilo, en donde el grupo fenilo está opcionalmente sustituido, un lípido, incluyendo un fosfolípido, un L o D-aminoácido (o mezcla racémica), un hidrato de carbono, un péptido, un colesterol u otro grupo partiente farmacéuticamente aceptable que cuando se administra in vivo es capaz de proveer un compuesto en donde R1 es H o fosfato; R2 es H o fosfato; R1 y R2 o R7 pueden también estar ligados con grupo fosfato cíclico; y R2 y R2' son independientemente H, alquilo C1-4, alquenilo C1-4, alquinilo C1-4, vinilo, N3, CN, Cl, Br, F, I, NO2, C(O)O(alquilo C1-4), C(O)O(alquilo C1-4), C(O)O(alquenilo C1-4), O(acilo C1-4), O(alquilo C1-4), O(alquenilo C1-4), S(acilo C1-4), S(alquilo C1-4), S(alquinilo C1-4), S(alquenilo C1-4), SO(acilo C1-4), SO(alquilo C1-4), SO(alquinilo C1-4), SO(alquenilo C1-4), SO2(acilo C1-4), SO2(alquilo C1-4), SO2(alquinilo C1-4), SO2(alquenilo C1-4), O3S(acilo C1-4), O3S(alquilo C1-4), O3S(alquenilo C1-4), NH2, NH(alquilo C1-4), NH(alquenilo C1-4), NH(alquinilo C1-4), NH(acilo C1-4), N(alquilo C1-4)2, N(acilo C1-18)2, en donde alquilo, alquinilo, alquenilo y vinilo están opcionalmente sustituidos con N3, CN, uno a tres halógenos (Cl, Br, F, I), NO2, C(O)O(alquilo C1-4), C(O)O(alquinilo C1-4), C(O)O(alquenilo C1-4), O(acilo C1-4), O(alquilo C1-4), O(alquenilo C1-4), S(acilo C1-4), S(alquilo C1-4), S(alquinilo C1-4), S(alquenilo C1-4), SO(acilo C1-4), SO(alquilo C1-4), SO(alquinilo C1-4), SO(alquenilo C1-4), SO2(acilo C1-4), SO2(alquilo C1-4), SO2(alquinilo C1-4), SO2(alquenilo C1-4), O3S(acilo C1-4), O3S(alquilo C1-4), O3S(alquenilo C1-4), NH2, NH(alquilo C1-4), NH(alquenilo C1-4), NH(alquinilo C1-4), NH(acilo C1-4), N(alquilo C1-4)2, N(acilo C1-4)2, OR7; R2 y R2' pueden estar unidos en conjunto para formar un vinilo opcionalmente sustituido con uno o dos de N3, CN, Cl, Br, F, I, NO2; y R6 es un alquilo opcionalmente sustituido (incluyendo alquilo inferior), ciano (CN), CH3, OCH3, OCH2CH3, hidroximetilo (CH2OH), fluorometilo (CH2F), azido (N3), CHCN, CH2N3, CH2NH2, CH2NHCH3, CH2N(CH3)2, alquino (opcionalmente sustituido) o flúor; o su sal o prodroga farmacéuticamente aceptable del mismo.
ARP040101821A 2003-05-30 2004-05-27 Analogos de nucleosidos fluorados modificados AR044566A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US47436803P 2003-05-30 2003-05-30

Publications (1)

Publication Number Publication Date
AR044566A1 true AR044566A1 (es) 2005-09-21

Family

ID=33563735

Family Applications (6)

Application Number Title Priority Date Filing Date
ARP040101821A AR044566A1 (es) 2003-05-30 2004-05-27 Analogos de nucleosidos fluorados modificados
ARP110102358A AR082068A2 (es) 2003-05-30 2011-06-30 Analogos de nucleosidos fluorados modificados
ARP110102357A AR082067A2 (es) 2003-05-30 2011-06-30 Analogos de nucleosidos fluorados modificados
ARP110102354A AR082064A2 (es) 2003-05-30 2011-06-30 2’-fluoro-2’-metil nucleosidos, metodo para prepararlos y composiciones farmaceuticas que los contienen utiles para tratar infecciones por flaviviridae, en particular vhc
ARP110102356A AR082066A2 (es) 2003-05-30 2011-06-30 Metodo y uso de analogos de nucleosidos fluorados modificados
ARP180101768A AR114929A2 (es) 2003-05-30 2018-06-26 Análogos de nucleósidos fluorados modificados

Family Applications After (5)

Application Number Title Priority Date Filing Date
ARP110102358A AR082068A2 (es) 2003-05-30 2011-06-30 Analogos de nucleosidos fluorados modificados
ARP110102357A AR082067A2 (es) 2003-05-30 2011-06-30 Analogos de nucleosidos fluorados modificados
ARP110102354A AR082064A2 (es) 2003-05-30 2011-06-30 2’-fluoro-2’-metil nucleosidos, metodo para prepararlos y composiciones farmaceuticas que los contienen utiles para tratar infecciones por flaviviridae, en particular vhc
ARP110102356A AR082066A2 (es) 2003-05-30 2011-06-30 Metodo y uso de analogos de nucleosidos fluorados modificados
ARP180101768A AR114929A2 (es) 2003-05-30 2018-06-26 Análogos de nucleósidos fluorados modificados

Country Status (30)

Country Link
US (8) US7429572B2 (es)
EP (8) EP2345661A1 (es)
JP (5) JP4958158B2 (es)
KR (1) KR100883703B1 (es)
CN (1) CN100503628C (es)
AR (6) AR044566A1 (es)
AU (1) AU2004253860B2 (es)
BR (3) BRPI0419345B8 (es)
CA (5) CA2734055A1 (es)
CO (1) CO5660270A2 (es)
CY (2) CY1118020T1 (es)
DK (1) DK2604620T4 (es)
ES (3) ES2726998T3 (es)
FI (1) FI2604620T4 (es)
HR (1) HRP20160873T4 (es)
HU (2) HUE029877T2 (es)
IL (2) IL172259A (es)
LT (2) LT2604620T (es)
MX (1) MXPA05012788A (es)
MY (1) MY138477A (es)
NO (5) NO333700B1 (es)
NZ (1) NZ543867A (es)
PL (3) PL2604620T3 (es)
PT (3) PT3521297T (es)
RU (1) RU2358979C2 (es)
SI (3) SI3521297T1 (es)
TR (1) TR201906767T4 (es)
TW (1) TWI333956B (es)
WO (1) WO2005003147A2 (es)
ZA (1) ZA200509521B (es)

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