EA026114B1 - Макроциклические ингибиторы вирусов flaviviridae - Google Patents

Макроциклические ингибиторы вирусов flaviviridae Download PDF

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Publication number
EA026114B1
EA026114B1 EA201390822A EA201390822A EA026114B1 EA 026114 B1 EA026114 B1 EA 026114B1 EA 201390822 A EA201390822 A EA 201390822A EA 201390822 A EA201390822 A EA 201390822A EA 026114 B1 EA026114 B1 EA 026114B1
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Eurasian Patent Office
Prior art keywords
mmol
alkyl
another aspect
possibly substituted
compound
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EA201390822A
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English (en)
Russian (ru)
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EA201390822A1 (ru
Inventor
Тодд Эплбай
Ганс Г. Флири
Эндрю Дж. Китс
Линос Лазаридс
Ричард Л. Макман
Саймон Н. Петтит
Карин Г. Пулленнек
Джонатан Санвуасин
Виктория А. Стедман
Грегори М. Ватт
Original Assignee
Джилид Сайэнс, Инк.
Селсиа Лимитед
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Publication of EA201390822A1 publication Critical patent/EA201390822A1/ru
Publication of EA026114B1 publication Critical patent/EA026114B1/ru

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/06Tripeptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/5025Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10Antimycotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06052Val-amino acid

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Molecular Biology (AREA)
  • Oncology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Epidemiology (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
EA201390822A 2010-12-10 2011-12-08 Макроциклические ингибиторы вирусов flaviviridae EA026114B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US42207110P 2010-12-10 2010-12-10
PCT/US2011/064009 WO2012078915A1 (en) 2010-12-10 2011-12-08 Macrocyclic inhibitors of flaviviridae viruses

Publications (2)

Publication Number Publication Date
EA201390822A1 EA201390822A1 (ru) 2013-12-30
EA026114B1 true EA026114B1 (ru) 2017-03-31

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EA201390822A EA026114B1 (ru) 2010-12-10 2011-12-08 Макроциклические ингибиторы вирусов flaviviridae

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US (2) US8513184B2 (2)
EP (1) EP2649076B1 (2)
JP (1) JP5847193B2 (2)
KR (1) KR20140031841A (2)
CN (1) CN103403009B (2)
AR (1) AR084217A1 (2)
AU (1) AU2011338262B2 (2)
BR (1) BR112013014063A2 (2)
CA (1) CA2819824A1 (2)
EA (1) EA026114B1 (2)
ES (1) ES2536321T3 (2)
IL (1) IL226739A (2)
MX (1) MX2013006475A (2)
NZ (1) NZ612159A (2)
PL (1) PL2649076T3 (2)
PT (1) PT2649076E (2)
PY (1) PY1153144A (2)
SI (1) SI2649076T1 (2)
TW (1) TWI520966B (2)
UY (1) UY33775A (2)
WO (1) WO2012078915A1 (2)

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ES2536321T3 (es) 2015-05-22
JP2014503516A (ja) 2014-02-13
EA201390822A1 (ru) 2013-12-30
JP5847193B2 (ja) 2016-01-20
PY1153144A (es) 2015-01-01
US8933015B2 (en) 2015-01-13
SI2649076T1 (sl) 2015-07-31
TWI520966B (zh) 2016-02-11
EP2649076B1 (en) 2015-03-04
IL226739A (en) 2017-05-29
AU2011338262B2 (en) 2016-12-15
TW201307355A (zh) 2013-02-16
CN103403009A (zh) 2013-11-20
US20130022573A1 (en) 2013-01-24
PL2649076T3 (pl) 2015-08-31
AU2011338262A1 (en) 2013-07-11
CN103403009B (zh) 2016-01-13
US8513184B2 (en) 2013-08-20
PT2649076E (pt) 2015-06-02
NZ612159A (en) 2015-07-31
HK1191000A1 (en) 2014-07-18
UY33775A (es) 2012-07-31
WO2012078915A1 (en) 2012-06-14
US20140023616A1 (en) 2014-01-23
MX2013006475A (es) 2013-11-01
AR084217A1 (es) 2013-05-02
BR112013014063A2 (pt) 2016-09-13
CA2819824A1 (en) 2012-06-14
EP2649076A1 (en) 2013-10-16
KR20140031841A (ko) 2014-03-13

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