JO3027B1 - نيوكليوسيدات يوراسيل سبيرواوكسيتان - Google Patents

نيوكليوسيدات يوراسيل سبيرواوكسيتان

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Publication number
JO3027B1
JO3027B1 JOP/2010/0138A JOP20100138A JO3027B1 JO 3027 B1 JO3027 B1 JO 3027B1 JO P20100138 A JOP20100138 A JO P20100138A JO 3027 B1 JO3027 B1 JO 3027B1
Authority
JO
Jordan
Prior art keywords
phenyl
optionally substituted
c6alkyl
compounds
spirooxetane nucleosides
Prior art date
Application number
JOP/2010/0138A
Other languages
English (en)
Inventor
Vandyck Koen
Jean-Marie Pierre Raboisson Bernard
Abdellah Tahri
Koen Vandyck
Hu Lili
Hugo Tim Jonckers Maria
Original Assignee
Janssen Products Lp
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 Janssen Products Lp, Medivir Ab filed Critical Janssen Products Lp
Application granted granted Critical
Publication of JO3027B1 publication Critical patent/JO3027B1/ar

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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
    • C07H19/067—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
    • 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
    • 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

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

Abstract

مركبات لها الصيغة I: بما فيها أية مشابهات هندسية حيث : R4 هي احادي فوسفات, ثنائي فوسفات أو ثلاثي فوسفات استر, أو R4 هي أو R7 هي فينيل مستبدلة اختيارياً أو نافثيل مستبدل اختيارياً, أو اندوليل مستبدل اختيارياً. R8 و R8' هما هيدروجين, الكيل ك1 – ك6 , بنزيل, أوفينيل أو R8 و R8' تشكلان الكيل حلقي ك3-ك7 R9 هي الكيل ك1- ك10, الكيل حلقي ك3- ك7, فينيل أو فينيل الكيل ك1- ك6, حيث يكون شق الفينيل في الفينيل أو الكيل ك1- ك6 فينيل مستبدل اختيارياً, أو ملحها أو تميؤها المقبول دوائياً, أو صيغها الدوائية واستعمال المركبات I بصفة مثبطات لفيروس سي الالتهاب الكبدي.
JOP/2010/0138A 2009-05-14 2010-05-04 نيوكليوسيدات يوراسيل سبيرواوكسيتان JO3027B1 (ar)

Applications Claiming Priority (1)

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

Publications (1)

Publication Number Publication Date
JO3027B1 true JO3027B1 (ar) 2016-09-05

Family

ID=40823307

Family Applications (1)

Application Number Title Priority Date Filing Date
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Country Status (38)

Country Link
US (2) US8481510B2 (ar)
EP (2) EP2511282B1 (ar)
JP (2) JP5778135B2 (ar)
KR (1) KR101806837B1 (ar)
CN (1) CN102439024B (ar)
AP (1) AP2783A (ar)
AR (1) AR076579A1 (ar)
AU (1) AU2010247439B2 (ar)
BR (1) BRPI1010579A2 (ar)
CA (1) CA2760329C (ar)
CL (1) CL2011002859A1 (ar)
CO (1) CO6440533A2 (ar)
CR (1) CR20120297A (ar)
CY (2) CY1114081T1 (ar)
DK (2) DK2430035T3 (ar)
EA (1) EA022084B1 (ar)
EC (1) ECSP11011461A (ar)
ES (2) ES2411086T3 (ar)
HN (1) HN2011003014A (ar)
HR (2) HRP20130554T1 (ar)
IL (1) IL215955A (ar)
JO (1) JO3027B1 (ar)
ME (1) ME01478B (ar)
MX (1) MX2011012027A (ar)
MY (1) MY157018A (ar)
NI (1) NI201100197A (ar)
NZ (1) NZ596073A (ar)
PL (2) PL2430035T3 (ar)
PT (2) PT2511282E (ar)
RS (1) RS52822B (ar)
SG (1) SG175981A1 (ar)
SI (2) SI2430035T1 (ar)
SM (2) SMT201300078B (ar)
TW (1) TWI461432B (ar)
UA (1) UA105790C2 (ar)
UY (1) UY32642A (ar)
WO (1) WO2010130726A1 (ar)
ZA (1) ZA201108309B (ar)

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JO3027B1 (ar) 2009-05-14 2016-09-05 Janssen Products Lp نيوكليوسيدات يوراسيل سبيرواوكسيتان
WO2012062869A1 (en) * 2010-11-10 2012-05-18 Janssen Products, Lp Uracyl spirooxetane nucleoside phosphoramidates
PL2638054T3 (pl) 2010-11-10 2015-05-29 Janssen Products Lp Fosforoamidany nukleozydów uracylo-spirooksetanowych
ES2716158T3 (es) 2010-11-30 2019-06-10 Gilead Pharmasset Llc 2'-spiro-nucleótidos para el tratamiento de hepatitis C
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JP6298532B2 (ja) * 2013-11-28 2018-03-20 ヤンセン・サイエンシズ・アイルランド・ユーシー Ｈｃｖのヌクレオシド阻害剤の結晶形
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JO3027B1 (ar) * 2009-05-14 2016-09-05 Janssen Products Lp نيوكليوسيدات يوراسيل سبيرواوكسيتان

Also Published As

Publication number Publication date
JP5778135B2 (ja) 2015-09-16
TWI461432B (zh) 2014-11-21
US20130217648A1 (en) 2013-08-22
MY157018A (en) 2016-04-15
DK2511282T3 (da) 2014-07-07
AP2783A (en) 2013-10-31
CN102439024B (zh) 2014-09-17
AP2011005958A0 (en) 2011-10-31
IL215955A (en) 2015-03-31
KR20120018355A (ko) 2012-03-02
PL2511282T3 (pl) 2014-09-30
EP2511282A1 (en) 2012-10-17
SMT201400085B (it) 2014-09-08
KR101806837B1 (ko) 2017-12-08
JP2012526764A (ja) 2012-11-01
TW201100442A (en) 2011-01-01
SMT201300078B (it) 2013-09-06
US8481510B2 (en) 2013-07-09
HRP20140605T1 (hr) 2014-09-26
ZA201108309B (en) 2013-04-24
ECSP11011461A (es) 2012-02-29
SI2430035T1 (sl) 2013-08-30
EP2430035A1 (en) 2012-03-21
CN102439024A (zh) 2012-05-02
MX2011012027A (es) 2012-02-28
EA022084B1 (ru) 2015-10-30
CR20120297A (es) 2012-10-25
CA2760329C (en) 2017-10-31
CO6440533A2 (es) 2012-05-15
ES2477598T3 (es) 2014-07-17
CY1115383T1 (el) 2017-01-04
EA201171406A1 (ru) 2012-05-30
NI201100197A (es) 2012-05-28
PT2430035E (pt) 2013-05-22
RS52822B (sr) 2013-10-31
DK2430035T3 (da) 2013-05-27
IL215955A0 (en) 2012-01-31
ME01478B (me) 2014-04-20
HN2011003014A (es) 2014-06-30
NZ596073A (en) 2013-02-22
UA105790C2 (uk) 2014-06-25
US20120065156A1 (en) 2012-03-15
CL2011002859A1 (es) 2012-07-20
US8933052B2 (en) 2015-01-13
CA2760329A1 (en) 2010-11-18
BRPI1010579A2 (pt) 2016-03-15
UY32642A (es) 2010-11-30
AU2010247439A1 (en) 2011-12-01
AR076579A1 (es) 2011-06-22
JP2015180692A (ja) 2015-10-15
WO2010130726A1 (en) 2010-11-18
PL2430035T3 (pl) 2013-08-30
AU2010247439B2 (en) 2014-09-25
CY1114081T1 (el) 2016-07-27
EP2430035B1 (en) 2013-04-03
PT2511282E (pt) 2014-07-11
HRP20130554T1 (xx) 2013-07-31
SI2511282T1 (sl) 2014-09-30
ES2411086T3 (es) 2013-07-04
HK1166326A1 (en) 2012-10-26
SG175981A1 (en) 2011-12-29
EP2511282B1 (en) 2014-04-02

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