CL2011002859A1 - Compuestos espironucleosidos, inhibidores del virus vhc; composicion farmaceutica de dichos compuestos; uso del compuesto para tratar la hepatitis c. - Google Patents

Compuestos espironucleosidos, inhibidores del virus vhc; composicion farmaceutica de dichos compuestos; uso del compuesto para tratar la hepatitis c.

Info

Publication number
CL2011002859A1
CL2011002859A1 CL2011002859A CL2011002859A CL2011002859A1 CL 2011002859 A1 CL2011002859 A1 CL 2011002859A1 CL 2011002859 A CL2011002859 A CL 2011002859A CL 2011002859 A CL2011002859 A CL 2011002859A CL 2011002859 A1 CL2011002859 A1 CL 2011002859A1
Authority
CL
Chile
Prior art keywords
compounds
phenyl
alkyl
spironucleoside
compound
Prior art date
Application number
CL2011002859A
Other languages
English (en)
Inventor
Tim Hugo Maria Jonckers
Pierre Jean-Marie Bernard Raboisson
Koen Vandyck
Hoof Steven Maurice Paula Van
Lili Hu
Abdellah Tahri
Original Assignee
Medivir Ab
Janssen Products Lp
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 Medivir Ab, Janssen Products Lp filed Critical Medivir Ab
Publication of CL2011002859A1 publication Critical patent/CL2011002859A1/es

Links

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
    • 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
    • C07H19/067—Pyrimidine radicals with ribosyl as the saccharide radical
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/503—Pyridazines; Hydrogenated pyridazines spiro-condensed
    • 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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/02—Acyclic radicals, not substituted by cyclic structures
    • C07H15/04—Acyclic radicals, not substituted by cyclic structures attached to an oxygen atom of the saccharide radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/18—Acyclic radicals, substituted by carbocyclic rings
    • 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
    • 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
    • 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
    • C07H21/00—Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
    • C07H21/02—Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with ribosyl as saccharide radical

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Virology (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Communicable Diseases (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)

Abstract

COMPUESTO DE LA FÓRMULA 1 INCLUYENDO CUALQUIER ESTEREOISÓMERO POSIBLE DEL MISMO, EN DONDE R4 ES UN ÉSTER MONOFOSFATO, DIFOSFATO O TRIFOSFATO; O R4 ES UN GRUPO DE FÓRMULA R7 ES FENILO OPCIONALMENTE SUSTITUIDO, NAFTILO OPCIONALMENTE SUSTITUIDO, O INDOLILO OPCIONALMENTE SUSTITUIDO; R8 Y Rª' SON HIDRÓGENO, ALQUILO C1-C6, BENCILO, O FENILO; O R8 Y Rª' FORMAN CICLOALQUILO C3-C7; R9 ES ALQUILO C1-C10, CICLOALQUILO CRC7, FENILO O FENIL-ALQUILO C1-C6, EN DONDE LA PORCIÓN FENILO EN EL FENILO O EN EL FENIL-ALQUILO C1-C6 ESTÁ OPCIONALMENTE SUSTITUIDA; O UNA SAL O UN SOLVATO FARMACÉUTICAMENTE ACEPTABLE DE LOS MISMOS; COMPOSICIONES FARMACÉUTICAS Y EL USO DE LOS COMPUESTOS I COMO INHIBIDORES DEL VHC PARA EL TRATAMIENTO DE LA HEPATITIS C.
CL2011002859A 2009-05-14 2011-11-14 Compuestos espironucleosidos, inhibidores del virus vhc; composicion farmaceutica de dichos compuestos; uso del compuesto para tratar la hepatitis c. CL2011002859A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP09160215 2009-05-14

Publications (1)

Publication Number Publication Date
CL2011002859A1 true CL2011002859A1 (es) 2012-07-20

Family

ID=40823307

Family Applications (1)

Application Number Title Priority Date Filing Date
CL2011002859A CL2011002859A1 (es) 2009-05-14 2011-11-14 Compuestos espironucleosidos, inhibidores del virus vhc; composicion farmaceutica de dichos compuestos; uso del compuesto para tratar la hepatitis c.

Country Status (39)

Country Link
US (2) US8481510B2 (es)
EP (2) EP2430035B1 (es)
JP (2) JP5778135B2 (es)
KR (1) KR101806837B1 (es)
CN (1) CN102439024B (es)
AP (1) AP2783A (es)
AR (1) AR076579A1 (es)
AU (1) AU2010247439B2 (es)
BR (1) BRPI1010579A2 (es)
CA (1) CA2760329C (es)
CL (1) CL2011002859A1 (es)
CO (1) CO6440533A2 (es)
CR (1) CR20120297A (es)
CY (2) CY1114081T1 (es)
DK (2) DK2511282T3 (es)
EA (1) EA022084B1 (es)
EC (1) ECSP11011461A (es)
ES (2) ES2477598T3 (es)
HK (1) HK1166326A1 (es)
HN (1) HN2011003014A (es)
HR (2) HRP20130554T1 (es)
IL (1) IL215955A (es)
JO (1) JO3027B1 (es)
ME (1) ME01478B (es)
MX (1) MX2011012027A (es)
MY (1) MY157018A (es)
NI (1) NI201100197A (es)
NZ (1) NZ596073A (es)
PL (2) PL2511282T3 (es)
PT (2) PT2511282E (es)
RS (1) RS52822B (es)
SG (1) SG175981A1 (es)
SI (2) SI2511282T1 (es)
SM (2) SMT201300078B (es)
TW (1) TWI461432B (es)
UA (1) UA105790C2 (es)
UY (1) UY32642A (es)
WO (1) WO2010130726A1 (es)
ZA (1) ZA201108309B (es)

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US8173621B2 (en) 2008-06-11 2012-05-08 Gilead Pharmasset Llc Nucleoside cyclicphosphates
SG194404A1 (en) 2008-12-23 2013-11-29 Gilead Pharmasset Llc Synthesis of purine nucleosides
JO3027B1 (ar) 2009-05-14 2016-09-05 Janssen Products Lp نيوكليوسيدات يوراسيل سبيرواوكسيتان
DK2638054T3 (en) 2010-11-10 2015-03-09 Janssen Products Lp URACYLSPIROOXETANNUCLEOSIDE PHOSPHORAMIDATES
US9006209B2 (en) 2010-11-10 2015-04-14 Janssen Products, Lp Uracyl spirooxetane nucleoside phosphoramidates
WO2012075140A1 (en) * 2010-11-30 2012-06-07 Pharmasset, Inc. Compounds
AU2015252113B2 (en) * 2010-11-30 2017-05-04 Gilead Pharmasset Llc Compounds
WO2012142523A2 (en) * 2011-04-13 2012-10-18 Gilead Sciences, Inc. 1'-substituted pyrimidine n-nucleoside analogs for antiviral treatment
US8980865B2 (en) 2011-12-22 2015-03-17 Alios Biopharma, Inc. Substituted nucleotide analogs
CA2871547C (en) 2012-05-25 2021-05-25 Janssen R&D Ireland Uracyl spirooxetane nucleosides
EP2940031B1 (en) * 2013-03-08 2017-09-27 Nanjing Sanhome Pharmaceutical Co., Ltd. Nucleoside phosphoramidate compounds for use in the treatment of hcv
CN105377868A (zh) 2013-04-12 2016-03-02 艾其林医药公司 用于治疗hcv的高活性核苷衍生物
CN104231023B (zh) * 2013-06-06 2019-02-05 南京汇诚制药有限公司 三环稠杂环类核苷氨基磷酸酯化合物、其制备方法及应用
RU2016125445A (ru) * 2013-11-28 2018-01-10 Янссен Сайенсиз Айрлэнд Юси Кристаллическая форма нуклеозидного ингибитора hcv
EP3265102A4 (en) 2015-03-06 2018-12-05 ATEA Pharmaceuticals, Inc. Beta-d-2'-deoxy-2'alpha-fluoro-2'-beta-c-substituted-2-modified-n6-substituted purine nucleotides for hcv treatment
LU100724B1 (en) 2016-07-14 2018-07-31 Atea Pharmaceuticals Inc Beta-d-2'-deoxy-2'-alpha-fluoro-2'-beta-c-substituted-4'-fluoro-n6-substituted-6-amino-2-substituted purine nucleotides for the treatment of hepatitis c virus infection
MY197236A (en) 2016-09-07 2023-06-07 Atea Pharmaceuticals Inc 2'-substituted-n6-substituted purine nucleotides for rna virus treatment
SG10202012214WA (en) 2017-02-01 2021-01-28 Atea Pharmaceuticals Inc Nucleotide hemi-sulfate salt for the treatment of hepatitis c virus
CN112351799A (zh) 2018-04-10 2021-02-09 阿堤亚制药公司 具有硬化的hcv感染患者的治疗
US10874687B1 (en) 2020-02-27 2020-12-29 Atea Pharmaceuticals, Inc. Highly active compounds against COVID-19
WO2021209427A1 (en) * 2020-04-14 2021-10-21 Janssen Sciences Ireland Unlimited Company Spirocyclic nucleoside analogues for the treatment of hepatitis e

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CA2434386C (en) * 2001-01-22 2006-12-05 Merck & Co., Inc. Nucleoside derivatives as inhibitors of rna-dependent rna viral polymerase
US20070265222A1 (en) * 2004-06-24 2007-11-15 Maccoss Malcolm Nucleoside Aryl Phosphoramidates for the Treatment of Rna-Dependent Rna Viral Infection
JP2009504704A (ja) * 2005-08-15 2009-02-05 エフ．ホフマン−ラ ロシュ アーゲー 抗ウイルス４′−置換プロヌクレオチドホスホルアミダート
US7879815B2 (en) * 2006-02-14 2011-02-01 Merck Sharp & Dohme Corp. Nucleoside aryl phosphoramidates for the treatment of RNA-dependent RNA viral infection
PA8852101A1 (es) * 2008-12-08 2010-07-27 Medivir Ab Nucleótidos uracil ciclopropílicos
JO3027B1 (ar) 2009-05-14 2016-09-05 Janssen Products Lp نيوكليوسيدات يوراسيل سبيرواوكسيتان

Also Published As

Publication number Publication date
NZ596073A (en) 2013-02-22
IL215955A0 (en) 2012-01-31
KR20120018355A (ko) 2012-03-02
WO2010130726A1 (en) 2010-11-18
ECSP11011461A (es) 2012-02-29
JO3027B1 (ar) 2016-09-05
US20130217648A1 (en) 2013-08-22
CY1114081T1 (el) 2016-07-27
SI2511282T1 (sl) 2014-09-30
PL2511282T3 (pl) 2014-09-30
US20120065156A1 (en) 2012-03-15
CO6440533A2 (es) 2012-05-15
ES2477598T3 (es) 2014-07-17
EP2511282A1 (en) 2012-10-17
EP2430035A1 (en) 2012-03-21
ZA201108309B (en) 2013-04-24
NI201100197A (es) 2012-05-28
US8481510B2 (en) 2013-07-09
PL2430035T3 (pl) 2013-08-30
DK2511282T3 (da) 2014-07-07
IL215955A (en) 2015-03-31
PT2511282E (pt) 2014-07-11
CR20120297A (es) 2012-10-25
PT2430035E (pt) 2013-05-22
MX2011012027A (es) 2012-02-28
SI2430035T1 (sl) 2013-08-30
HN2011003014A (es) 2014-06-30
US8933052B2 (en) 2015-01-13
EA022084B1 (ru) 2015-10-30
SMT201400085B (it) 2014-09-08
TWI461432B (zh) 2014-11-21
BRPI1010579A2 (pt) 2016-03-15
KR101806837B1 (ko) 2017-12-08
CY1115383T1 (el) 2017-01-04
TW201100442A (en) 2011-01-01
CN102439024A (zh) 2012-05-02
HRP20140605T1 (hr) 2014-09-26
EA201171406A1 (ru) 2012-05-30
JP2015180692A (ja) 2015-10-15
JP5778135B2 (ja) 2015-09-16
HK1166326A1 (en) 2012-10-26
AU2010247439A1 (en) 2011-12-01
AR076579A1 (es) 2011-06-22
MY157018A (en) 2016-04-15
EP2511282B1 (en) 2014-04-02
UA105790C2 (uk) 2014-06-25
AP2783A (en) 2013-10-31
RS52822B (en) 2013-10-31
HRP20130554T1 (en) 2013-07-31
CA2760329C (en) 2017-10-31
AP2011005958A0 (en) 2011-10-31
DK2430035T3 (da) 2013-05-27
ES2411086T3 (es) 2013-07-04
SG175981A1 (en) 2011-12-29
EP2430035B1 (en) 2013-04-03
CA2760329A1 (en) 2010-11-18
JP2012526764A (ja) 2012-11-01
SMT201300078B (it) 2013-09-06
CN102439024B (zh) 2014-09-17
ME01478B (me) 2014-04-20
AU2010247439B2 (en) 2014-09-25
UY32642A (es) 2010-11-30

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