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HRP20130098T1 - MAKROCIKLIÄŚKE KARBOKSILNE KISELINE I ACILSULFONAMIDNI SPOJEVI KAO INHIBITORI REPLIKACIJE HCV-a - Google Patents

MAKROCIKLIÄŚKE KARBOKSILNE KISELINE I ACILSULFONAMIDNI SPOJEVI KAO INHIBITORI REPLIKACIJE HCV-a Download PDF

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Publication number
HRP20130098T1
HRP20130098T1 HRP20130098TT HRP20130098T HRP20130098T1 HR P20130098 T1 HRP20130098 T1 HR P20130098T1 HR P20130098T T HRP20130098T T HR P20130098TT HR P20130098 T HRP20130098 T HR P20130098T HR P20130098 T1 HRP20130098 T1 HR P20130098T1
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Croatia
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effective amount
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compound according
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HRP20130098TT
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English (en)
Inventor
Lawrence M. Blatt
Steven Mark Wenglowsky
Steven Wade Andrews
Yutong Jiang
April Layne Kennedy
Kevin Ronald Condroski
John Anthony Josey
Peter John Stengel
Machender R. Madduru
George Andrew Doherty
Benjamin T. Woodard
Scott D. Seiwert
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F. Hoffmann - La Roche Ag
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Publication of HRP20130098T1 publication Critical patent/HRP20130098T1/hr

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    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Virology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Biochemistry (AREA)
  • Immunology (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Claims (54)

1. Spoj, naznačen time da ima formulu: [image] ili njegova farmaceutski prihvatljiva sol.
2. Farmaceutski pripravak, naznačen time da sadrži a) spoj prema zahtjevu 1; i b) farmaceutski prihvatljiv nosač
3. Spoj prema zahtjevu 1, ili pripravka prema zahtjevu 2, naznačen time da se upotrebljava kao medikament.
4. Upotreba spoja prema zahtjevu 1, ili pripravka prema zahtjevu 2, naznačena time da se koristi za proizvodnju lijeka za liječenje infekcija virusom hepatitisa C kod pojedinaca.
5. Upotreba prema zahtjevu 4, naznačena time da se postiže produljeni protuvirusni odgovor.
6. Upotreba spoja prema zahtjevu 1, ili pripravka prema zahtjevu 2, naznačena time da se koristi za proizvodnju lijeka za liječenje jetrene fibroze kod pojedinaca.
7. Upotreba spoja prema zahtjevu 1, ili pripravka prema zahtjevu 2, naznačena time da se koristi za proizvodnju lijeka za poboljšanje jetrene funkcije kod pojedinaca koji su inficirani virusom hepatitisa C.
8. Upotreba prema zahtjevu 4, 6, ili 7, naznačena time da se pojedincu administrira učinkovita količina spoja prema zahtjevu 1, ili pripravka prema zahtjevu 2 i dodatno učinkovita količina nukleozidnog analoga.
9. Upotreba prema zahtjevu 4, 6 ili 7, naznačena time da je lijek proizveden na način da se koristi u kombinaciji s učinkovitom količinom nukleozidnog analoga.
10. Upotreba prema zahtjevu 8 ili 9, naznačena time da je nukleozidni analog izabran iz skupine koju čine ribavirin, levovirin, viramidin, jednog L-nukleozida, i izatoribin.
11. Upotreba prema zahtjevima 8 ili 9, naznačena time da je nukleozidni analog ribavirin.
12. Upotreba prema zahtjevu 4, 6, ili 7, naznačena time da se pojedincu na dnevnoj bazi oralno administrira spoja prema zahtjevu 1 ili pripravka prema zahtjevu 2 i dodatno učinkovita količina pirfenidona ili analoga pirfenidona u količini od 400 mg do 3600 mg.
13. Upotreba prema zahtjevu 4, 6, ili 7, naznačena time da je lijek proizveden na način da se koristi u kombinaciji s pirfenidonom ili analogom pirfenidona te da se administrira oralno na dnevnoj bazi u količini od 400 mg do 3600 mg.
14. Upotreba prema zahtjevu 4, 6, ili 7, naznačena time da se pojedincu administrira učinkovita količina spoja prema zahtjevu 1, ili pripravka prema zahtjevu 2 i dodatno učinkovita količina inhibitora NS5B RNA-ovisne RNA-polimeraze.
15. Upotreba prema zahtjevu 4, 6, ili 7, naznačena time da je lijek proizveden na način da se koristi u kombinaciji s učinkovitom količinom inhibitora NS5B RNA-ovisne RNA-polimeraze.
16. Upotreba prema zahtjevu 4, 6, ili 7, naznačena time da se pojedincu administrira učinkovita količina spoja prema zahtjevu 1, ili pripravka prema zahtjevu 2 i dodatno učinkovita količina antagonista faktora tumorske nekroze izabranog iz skupine koju čini etanercept, infliximab, i adalimumab.
17. Upotreba prema zahtjevu 4, 6, ili 7, naznačena time da je antagonist faktora tumorske nekroze izabran iz skupine koju čini enanercept, infliximab, i adalimumab.
18. Upotreba prema zahtjevu 4, 6, ili 7, naznačena time da je lijek proizveden na način da se koristi u kombinaciji s učinkovitom količinom antagonista faktora tumorske nekroze.
19. Upotreba prema zahtjevu 4, 6, ili 7, naznačena time da je lijek proizveden na način da se koristi u kombinaciji s učinkovitom količinom timozina-α.
20. Upotreba prema zahtjevu 18, ili 19, naznačena time što je timozina-α administriran subkutano i to dva puta tjedno u količini od 1,0 mg do 1,6 mg.
21. Upotreba prema zahtjevu 4, 6, ili 7, naznačena time da se pojedincu administrira učinkovita količina spoja prema zahtjevu 1, ili pripravka prema zahtjevu 2 i dodatno učinkovita količina interferona-gama (IFN-γ).
22. Upotreba prema zahtjevu 4, 6, ili 7, naznačena time da je lijek proizveden na način da se koristi u kombinaciji s učinkovitom količinom interferona-gama (IFN-γ).
23. Upotreba prema zahtjevu 21, ili 22, naznačena time da se IFN-γ administrira subkutano u količini od 10 μg do 300 μg.
24. Upotreba prema zahtjevu 4, 6, ili 7, naznačena time da se pojedincu administrira učinkovita količina spoja prema zahtjevu 1, ili pripravka prema zahtjevu 2 i dodatno učinkovita količina interferona-alfa (IFN-α).
25. Upotreba prema zahtjevu 4, 6, ili 7, naznačena time da je lijek proizveden na način da se koristi u kombinaciji s učinkovitom količinom interferona-alfa (IFN-α).
26. Upotreba prema zahtjevu 24, ili 25, naznačena time da je IFN-α PEG-ilirani IFN-α2a.
27. Upotreba prema zahtjevu 24, naznačena time da je IFN-α PEG-ilirani IFN-α2a i da je pojedincu dodatno administrirana učinkovita količina ribavirina.
28. Upotreba prema zahtjevu 24, naznačena time da je IFN-α PEG-ilirani IFN-α2a i je lijek proizveden na način da se koristi u kombinaciji s učinkovitom količinom ribavirina.
29. Upotreba prema zahtjevu 24, ili 25, naznačena time da je IFN-α monoPEG (30 kD, linearni) – iliran konsenzus IFN-α administriran prema doznom intervalu po jedan puta svakih 8 dana do svakih 14 dana.
30. Upotreba prema zahtjevu 24, ili 25 naznačena time da je IFN-α monoPEG (30 kD, linearni) – iliran konsenzus IFN-α administriran prema doznom intervalu jedan puta svakih sedam dana.
31. Upotreba prema zahtjevu 24, ili 25, naznačena time da je IFN-α INFERGEN konsenzus IFN-α.
32. Upotreba prema zahtjevu 4, 6, ili 7, naznačena time da se pojedincu administrira učinkovita količina spoja prema zahtjevu 1, ili pripravka prema zahtjevu 2 i dodatno učinkovita količina agensa izabranog između 3'-azidotimidina, 2',3'-dideoksinozina, 2',3'-dideoksicitidina, 2-,3'-didehidro-2',3'-dideoksitimidina, combivira, abacavira, adefovira, adefovir dipoksila, cidofovira, i jednog od inhibitora inozin monofosfat dehidrogenaze.
33. Upotreba prema zahtjevu 4, 6, ili 7, naznačena time da se pojedincu administrira učinkovita količina spoja prema zahtjevu 1, ili pripravka prema zahtjevu 2 i dodatno učinkovita količina agensa izabranog između 3'-azidotimidina, 2',3'-dideoksinozina, 2',3'-dideoksicitidina, 2-,3'-didehidro-2',3'-dideoksitimidina, combivira, abacavira, adefovira, adefovir dipoksila, cidofovira, i jednog od inhibitora inozin monofosfat dehidrogenaze.
34. Spoj prema zahtjevu 1, ili pripravak prema zahtjevu 2, naznačen time da se koristi za liječenje infekcije virusom hepatitisa C kod pojedinca.
35. Spoj prema zahtjevu 34, naznačen time da se kod pojedinca postiže produljeni protuvirusni odgovor.
36. Spoj prema zahtjevu 1, ili pripravak prema zahtjevu 2, naznačen time da se koristi za liječenje jetrene fibroze kod pojedinca.
37. Spoj prema zahtjevu 1, ili pripravak prema zahtjevu 2, naznačen time da se koristi za liječenje pojedinca s virusnom infekcijom hepatitisa C.
38. Spoj prema zahtjevu 34, 36, ili 37, naznačen time da se koristi u kombinaciji s nukleozidnim analogom.
39. Spoj prema zahtjevu 38, naznačen time što je nukleozidni analog izabran između ribavirina, levovirina, viramidina, jednog L-nukleozida, i izatoribina.
40. Spoj prema zahtjevu 38, naznačen time da je nukleozidni analog ribavirin.
41. Spoj prema zahtjevu 34, 36, ili 37, naznačen time da se dnevno administrira u kombinaciji s pirfenidonom ili analogom pirfenidona u količini od 400 mg do 3600 mg.
42. Spoj prema zahtjevu 34, 36, ili 37, naznačen time da se koristi u kombinaciji s učinkovitom količinom inhibitora NS5B RNA-ovisne RNA-polimeraze.
43. Spoj prema zahtjevu 34, 36, ili 37, naznačen time da se koristi u kombinaciji s učinkovitom količinom antagonista faktora tumorske nekroze izabranog iz skupine koju čini etanercept, infliximab, i adalimumab.
44. Spoj prema zahtjevu 34, 36, ili 37, naznačen time da se koristi u kombinaciji s učinkovitom količinom timozina-α.
45. Spoj prema zahtjevu 44, naznačen time što je timozin-α administriran subkutano i to dva puta tjedno u količini od 1,0 mg do 1,6 mg.
46. Spoj prema zahtjevu 34, 36, ili 37, naznačen time da se koristi u kombinaciji s učinkovitom količinom interferona-gama (IFN-γ).
47. Spoj prema zahtjevu 46, naznačen time da se IFN-γ administrira subkutano u količini od 10 μg do 300 μg.
48. Spoj prema zahtjevu 34, 36, ili 37, naznačen time da se koristi u kombinaciji s učinkovitom količinom interferona-alfa (IFN-α).
49. Spoj prema zahtjevu 48, naznačen time da je IFN-α PEG-ilirani IFN-α2a.
50. Spoj prema zahtjevu 49, naznačen time da se nadalje koristi i u kombinaciji s učinkovitom količinom ribavirina.
51. Spoj prema zahtjevu 48, naznačen time, da je IFN-α monoPEG (30 kD, linearni) – iliran konsenzus IFN-α administriran prema doznom intervalu jedan puta svakih 8 dana do svakih 14 dana.
52. Spoj prema zahtjevu 48, naznačen time, da je IFN-α monoPEG (30 kD, linearni) – iliran konsenzus IFN-α administriran prema doznom intervalu jednokratno jedan puta svakih sedam dana.
53. Spoj prema zahtjevu 48, naznačen time, da je IFN-α INFERGEN konsenzus IFN-α.
54. Spoj prema zahtjevu 34, 36, ili 37, naznačen time da se koristi u kombinaciji s učinkovitom količinom agensa izabranog između 3'-azidotimidina, 2',3'-dideoksinozina, 2',3'-dideoksicitidina, 2-,3'-didehidro-2',3'-dideoksitimidina, combivira, abacavira, adefovira, adefovir dipoksila, cidofovira, i jednog od inhibitora inozin monofosfat dehidrogenaze.
HRP20130098TT 2003-10-14 2004-10-13 MAKROCIKLIÄŚKE KARBOKSILNE KISELINE I ACILSULFONAMIDNI SPOJEVI KAO INHIBITORI REPLIKACIJE HCV-a HRP20130098T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US51154103P 2003-10-14 2003-10-14
US61246004P 2004-09-22 2004-09-22
PCT/US2004/033970 WO2005037214A2 (en) 2003-10-14 2004-10-13 Macrocyclic carboxylic acids and acylsulfonamides as inhibitors of hcv replication

Publications (1)

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HRP20130098T1 true HRP20130098T1 (hr) 2013-02-28

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EP (2) EP1680137B1 (hr)
JP (3) JP4584260B2 (hr)
KR (1) KR100853579B1 (hr)
CN (2) CN103145715B (hr)
AP (2) AP2287A (hr)
AR (2) AR046422A1 (hr)
AU (1) AU2004281780B2 (hr)
BR (1) BRPI0415373A (hr)
CA (1) CA2540858C (hr)
CY (1) CY1113809T1 (hr)
DK (1) DK1680137T3 (hr)
EA (1) EA011857B8 (hr)
EC (2) ECSP066570A (hr)
ES (1) ES2398912T3 (hr)
GE (1) GEP20084560B (hr)
HR (1) HRP20130098T1 (hr)
IL (3) IL174704A (hr)
IS (1) IS2876B (hr)
MA (1) MA28152A1 (hr)
MX (1) MXPA06003963A (hr)
MY (1) MY144593A (hr)
NO (1) NO343231B1 (hr)
NZ (1) NZ546347A (hr)
OA (1) OA13315A (hr)
PL (1) PL1680137T3 (hr)
PT (1) PT1680137E (hr)
RS (3) RS20110578A3 (hr)
TW (2) TWI375679B (hr)
WO (1) WO2005037214A2 (hr)

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