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CO6440533A2 - Nucleósidos espiro oxetánicos uracílicos - Google Patents

Nucleósidos espiro oxetánicos uracílicos

Info

Publication number
CO6440533A2
CO6440533A2 CO11145588A CO11145588A CO6440533A2 CO 6440533 A2 CO6440533 A2 CO 6440533A2 CO 11145588 A CO11145588 A CO 11145588A CO 11145588 A CO11145588 A CO 11145588A CO 6440533 A2 CO6440533 A2 CO 6440533A2
Authority
CO
Colombia
Prior art keywords
phenyl
alkyl
optionally substituted
urpile
nucleosids
Prior art date
Application number
CO11145588A
Other languages
English (en)
Inventor
Tim Hugo Maria Jonckers
Koen Vandick
Hoof Steven Maurice Paula Van
Lili Hu
Abdellah Tahri
Pierre Jean-Marie Bernard Raboisson
Original Assignee
Jansen Products L P
Medivir Ab
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 Jansen Products L P, Medivir Ab filed Critical Jansen Products L P
Publication of CO6440533A2 publication Critical patent/CO6440533A2/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
    • 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
    • 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
    • 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)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Virology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)

Abstract

Compuestos de la fórmula I:incluyendo cualquier estereoisómero posible de los mismos, en donde: R4 es un éster monofosfato, difosfato o trifosfato; o R4 es R7 es fenilo opcionalmente sustituido, naftilo opcionalmente sustituido, o indolilo opcionalmente sustituido; R8 y R8´ es hidrógeno, alquilo C1-C6, bencilo, o fenilo; o R8 y R8' forman cicloalquilo C3-C7; R9 es alquilo C1-C10, cicloalquilo C3-C7, 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; formulaciones farmacéuticas y el uso de los compuestos I como inhibidores del VHC.
CO11145588A 2009-05-14 2011-10-27 Nucleósidos espiro oxetánicos uracílicos CO6440533A2 (es)

Applications Claiming Priority (1)

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

Publications (1)

Publication Number Publication Date
CO6440533A2 true CO6440533A2 (es) 2012-05-15

Family

ID=40823307

Family Applications (1)

Application Number Title Priority Date Filing Date
CO11145588A CO6440533A2 (es) 2009-05-14 2011-10-27 Nucleósidos espiro oxetánicos uracílicos

Country Status (38)

Country Link
US (2) US8481510B2 (es)
EP (2) EP2511282B1 (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) DK2430035T3 (es)
EA (1) EA022084B1 (es)
EC (1) ECSP11011461A (es)
ES (2) ES2411086T3 (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) PT2430035E (es)
RS (1) RS52822B (es)
SG (1) SG175981A1 (es)
SI (2) SI2430035T1 (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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Publication number Priority date Publication date Assignee Title
US8173621B2 (en) 2008-06-11 2012-05-08 Gilead Pharmasset Llc Nucleoside cyclicphosphates
TW201031675A (en) 2008-12-23 2010-09-01 Pharmasset Inc Synthesis of purine nucleosides
JO3027B1 (ar) * 2009-05-14 2016-09-05 Janssen Products Lp نيوكليوسيدات يوراسيل سبيرواوكسيتان
ES2531583T3 (es) 2010-11-10 2015-03-17 Janssen Products, L.P. Fosforamidatos de espironucleósido oxetánico uracílico
EP2638053B1 (en) * 2010-11-10 2016-08-31 Janssen Products, L.P. Uracyl spirooxetane nucleoside phosphoramidates
EP3042910B1 (en) 2010-11-30 2019-01-09 Gilead Pharmasset LLC 2'-spiro-nucleosides for use in the therapy of hepatitis c
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
WO2013096680A1 (en) 2011-12-22 2013-06-27 Alios Biopharma, Inc. Substituted phosphorothioate nucleotide analogs
PT2861611T (pt) 2012-05-25 2016-10-11 Janssen Sciences Ireland Uc Nucleósidos de espirooxetano de uracilo
AU2014225052B2 (en) 2013-03-08 2016-11-10 Nanjing Sanhome Pharmaceutical Co., Ltd. Novel nucleoside phosphoramidate compound and use thereof
AU2014250764A1 (en) 2013-04-12 2015-10-29 Achillion Pharmaceuticals, Inc. Deuterated nucleoside prodrugs useful for treating HCV
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
US20170165287A1 (en) * 2013-11-28 2017-06-15 Janssen Sciences Ireland Uc Crystal form of a nucleoside inhibitor of hcv
CN107427530B (zh) 2015-03-06 2020-09-08 阿堤亚制药公司 用于HCV治疗的β-D-2’-脱氧-2’α-氟-2’-β-C-取代的-2-改性的-N6-取代的嘌呤核苷酸
US10711029B2 (en) 2016-07-14 2020-07-14 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
CN116036114A (zh) 2016-09-07 2023-05-02 阿堤亚制药公司 用于rna病毒治疗的2’-取代的-n6-取代的嘌呤核苷酸
IL295609B2 (en) 2017-02-01 2023-11-01 Atea Pharmaceuticals Inc Nucleotide hemisulfate salt for the treatment of hepatitis C virus
WO2019139920A1 (en) 2018-01-10 2019-07-18 Nucorion Pharmaceuticals, Inc. Phosphor(n)amidatacetal and phosph(on)atalcetal compounds
TW202012001A (zh) 2018-04-10 2020-04-01 美商亞堤製藥公司 C型肝炎病毒(hcv)感染硬化之患者的治療
EP3999519A4 (en) 2019-07-17 2023-08-16 Nucorion Pharmaceuticals, Inc. CYCLIC DEOXYRIBONUCLEOTIDE COMPOUNDS
US10874687B1 (en) 2020-02-27 2020-12-29 Atea Pharmaceuticals, Inc. Highly active compounds against COVID-19
BR112022020810A2 (pt) * 2020-04-14 2022-11-29 Janssen Pharmaceuticals Inc Análogos de nucleosídeos espirocíclicos para o tratamento de hepatite e

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PL207405B1 (pl) * 2001-01-22 2010-12-31 Isis Pharmaceuticals Inc Pochodne nukleozydów, zawierająca je kompozycja farmaceutyczna i ich zastosowanie
CN1972696B (zh) * 2004-06-24 2010-08-11 默沙东公司 用于治疗rna依赖性rna病毒感染的核苷氨基磷酸芳基酯
CA2618335C (en) * 2005-08-15 2015-03-31 F.Hoffmann-La Roche Ag Antiviral phosphoramidates of 4'-substituted pronucleotides
EP1987050A2 (en) * 2006-02-14 2008-11-05 Merck & Co., Inc. 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
AR076579A1 (es) 2011-06-22
HK1166326A1 (en) 2012-10-26
UY32642A (es) 2010-11-30
CY1115383T1 (el) 2017-01-04
EP2430035B1 (en) 2013-04-03
SI2430035T1 (sl) 2013-08-30
DK2511282T3 (da) 2014-07-07
MX2011012027A (es) 2012-02-28
MY157018A (en) 2016-04-15
JP2015180692A (ja) 2015-10-15
ECSP11011461A (es) 2012-02-29
PL2511282T3 (pl) 2014-09-30
SMT201400085B (it) 2014-09-08
KR101806837B1 (ko) 2017-12-08
HRP20130554T1 (xx) 2013-07-31
WO2010130726A1 (en) 2010-11-18
AP2011005958A0 (en) 2011-10-31
HN2011003014A (es) 2014-06-30
US20120065156A1 (en) 2012-03-15
EP2511282A1 (en) 2012-10-17
SI2511282T1 (sl) 2014-09-30
PT2511282E (pt) 2014-07-11
CN102439024B (zh) 2014-09-17
CA2760329C (en) 2017-10-31
EP2511282B1 (en) 2014-04-02
SMT201300078B (it) 2013-09-06
TW201100442A (en) 2011-01-01
EP2430035A1 (en) 2012-03-21
SG175981A1 (en) 2011-12-29
IL215955A0 (en) 2012-01-31
AP2783A (en) 2013-10-31
RS52822B (en) 2013-10-31
ME01478B (me) 2014-04-20
PL2430035T3 (pl) 2013-08-30
US8481510B2 (en) 2013-07-09
JP5778135B2 (ja) 2015-09-16
DK2430035T3 (da) 2013-05-27
IL215955A (en) 2015-03-31
EA022084B1 (ru) 2015-10-30
CY1114081T1 (el) 2016-07-27
EA201171406A1 (ru) 2012-05-30
KR20120018355A (ko) 2012-03-02
ES2477598T3 (es) 2014-07-17
NZ596073A (en) 2013-02-22
HRP20140605T1 (hr) 2014-09-26
AU2010247439B2 (en) 2014-09-25
US20130217648A1 (en) 2013-08-22
CR20120297A (es) 2012-10-25
AU2010247439A1 (en) 2011-12-01
JO3027B1 (ar) 2016-09-05
PT2430035E (pt) 2013-05-22
US8933052B2 (en) 2015-01-13
NI201100197A (es) 2012-05-28
JP2012526764A (ja) 2012-11-01
TWI461432B (zh) 2014-11-21
ZA201108309B (en) 2013-04-24
BRPI1010579A2 (pt) 2016-03-15
CA2760329A1 (en) 2010-11-18
CN102439024A (zh) 2012-05-02
ES2411086T3 (es) 2013-07-04
UA105790C2 (uk) 2014-06-25
CL2011002859A1 (es) 2012-07-20

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