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HRP20110732T1 - Antivirusni spojevi - Google Patents

Antivirusni spojevi Download PDF

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Publication number
HRP20110732T1
HRP20110732T1 HR20110732T HRP20110732T HRP20110732T1 HR P20110732 T1 HRP20110732 T1 HR P20110732T1 HR 20110732 T HR20110732 T HR 20110732T HR P20110732 T HRP20110732 T HR P20110732T HR P20110732 T1 HRP20110732 T1 HR P20110732T1
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alkyl
alkynyl
alkenyl
aryl
cycloalkyl
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HR20110732T
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English (en)
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Chaudhary Kleem
Fleury Melissa
U. Kim Choung
J. Mcmurtrie Darren
C. Sheng Xiaoning
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Gilead Sciences
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/08Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • 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
    • C07K5/08Tripeptides
    • C07K5/0827Tripeptides containing heteroatoms different from O, S, or N
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/06Phosphorus compounds without P—C bonds
    • C07F9/08Esters of oxyacids of phosphorus
    • C07F9/141Esters of phosphorous acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/572Five-membered rings
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    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65583Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom
    • 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
    • C07K5/06191Dipeptides containing heteroatoms different from O, S, or N
    • 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
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0804Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0808Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
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  • General Health & Medical Sciences (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Engineering & Computer Science (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Spoj formule I: ili njegova farmaceutski prihvatljiva sol, enantiomer ili solvat, naznačeni time štoR1 je nezavisno izabran iz grupe koju čine H, alkil, alkenil, alkinil, aril, cikloalkil, heterociklus, halogen, haloalkil, alkilsulfonamido, arilsulfonamido, -C(O)NHS(O)2- ili -S(O)2-, izborno supstituiran sa jednim ili više A3;R2 je -C(Y1)(A3),R3 je H ili (C1-6)alkil; Y1 je nezavisno O, S, N(A3);Z je O; Z1 je -Y1-A3;Z2a je H, (C1-10)alkil, (C2-10)alkenil ili (C2-10)alkinil ili Z2a izborno formira prsten sa Q1;Z2b je H, (C1-6)alkil, (C2-8)alkenil ili (C2-8)alkinil; Q1 je (C1-8)alkil, (C2-8)alkenil ili (C2-8)alkinil; A3 je nezavisno izabran iz grupe koju čine -OH, -C(O)OH, alkil, alkenil, alkinil, amino, amido, imido, imino, halogen, CF3, CH2CF3, cikloalkil, nitro, aril, aralkil, alkoksi, ariloksi, heterociklus, heteroaril, -C(A2)3, - C(A2)2-C(O)A2, -C(O)A2, -C(O)OA2, -O(A2), -N(A2)2, -S(A2), -(CH2)m-heterociklus,- (CH2)mC(O)Oalkil, -O-(CH2)m-O-C(O)-Oalkil, -O-(CH2)m-O-C(O)-(CH2)m-alkil, -(CH2)mO-C(O)-O-alkil, -(CH2)mO-C(O)-O-cikloalkil,

Claims (11)

1. Spoj formule I: [image] ili njegova farmaceutski prihvatljiva sol, enantiomer ili solvat, naznačeni time što R1 je nezavisno izabran iz grupe koju čine H, alkil, alkenil, alkinil, aril, cikloalkil, heterociklus, halogen, haloalkil, alkilsulfonamido, arilsulfonamido, -C(O)NHS(O)2- ili -S(O)2-, izborno supstituiran sa jednim ili više A3; R2 je -C(Y1)(A3), R3 je H ili (C1-6)alkil; Y1 je nezavisno O, S, N(A3); Z je O; Z1 je -Y1-A3; Z2a je H, (C1-10)alkil, (C2-10)alkenil ili (C2-10)alkinil ili Z2a izborno formira prsten sa Q1; Z2b je H, (C1-6)alkil, (C2-8)alkenil ili (C2-8)alkinil; Q1 je (C1-8)alkil, (C2-8)alkenil ili (C2-8)alkinil; A3 je nezavisno izabran iz grupe koju čine -OH, -C(O)OH, alkil, alkenil, alkinil, amino, amido, imido, imino, halogen, CF3, CH2CF3, cikloalkil, nitro, aril, aralkil, alkoksi, ariloksi, heterociklus, heteroaril, -C(A2)3, - C(A2)2-C(O)A2, -C(O)A2, -C(O)OA2, -O(A2), -N(A2)2, -S(A2), -(CH2)m-heterociklus,- (CH2)mC(O)Oalkil, -O-(CH2)m-O-C(O)-Oalkil, -O-(CH2)m-O-C(O)-(CH2)m-alkil, -(CH2)mO-C(O)-O-alkil, -(CH2)mO-C(O)-O-cikloalkil, -N(H)C(Me)C(O)O-alkil ili alkoksi arilsulfonamid, pri čemu svako A3 može biti izborno supstituiran sa 1 do 4 -R1, halogen, alkil, alkenil, alkinil, aril, carbocycle, heterociklus, aralkil, aril sulfonamid, aril alkilsulfonamid, ariloksi sulfonamid, ariloksi alkilsulfonamid, ariloksi arilsulfonamid, alkil sulfonamid, alkiloksi sulfonamid, alkiloksi alkilsulfonamid, -(CH2)mheterociklus, -(CH2)m-C(O)O-alkil, -O(CH2)mOC(O)Oalkil, -O-(CH2)m-O-C(O)-(CH2)m-alkil, -(CH2)m-O-C(O)-O-alkil, -(CH2)m-O-C(O)-O-cikloalkil, -N(H)C(CH3)C(O)O-alkil ili alkoksi arilsulfonamid grupe, izborno supstituirane sa R1; A2 je nezavisno izabran iz grupe koju čine H, alkil, alkenil, alkinil, amino, aminokiselina, alkoksi, ariloksi, cijano, haloalkil, cikloalkil, aril, heteroaril, alkilsulfonamid ili arilsulfonamid; i m je 0 do 6, pri čemu, ako nije drugačije naznačeno, alkil je (C1-18)alkil; alkenil je (C2-18)alkenil; alkinil je (C2-18)alkinil; cikloalkil je (C3-7)cikloalkil; aril je (C6-20)aril; aralkil je (C6-20)aralkil; alkoksi je (C1-18)alkoksi; karbociklus je zasićeni, nezasićeni ili aromatični (C3-7)monociklus, (C7-12)biciklus ili policiklus sa do 20 atoma ugljika; heterociklus je karbociklus kao što je prethodno definirano, u kojem su 1, 2, 3 ili 4 atoma ugljika zamijenjeni sa O, N ili S.
2. Spoj prema patentnom zahtjevu 1 koji ima formulu XI: [image] ili njegova farmaceutski prihvatljiva sol, enantiomer ili solvat, naznačeni time što: svako R1, R2, R3, Z, Z1, Z2b, m, A3, i A2 su kao što su definirani u patentnom zahtjevu 1; i Z2a formira prsten sa Q1.
3. Spoj prema patentnom zahtjevu 2, naznačen time što je Z1 jednako O-A3.
4. Spoj patentnom zahtjevu 2 koji ima formulu XXVI: [image] ili njegova farmaceutski prihvatljiva sol, enantiomer ili solvat, naznačeni time što: svako R1, R2, R3, Z, Z2a, Z2b, Q1, m, A3, i A2 su kao što su definirani u patentnom zahtjevu 2; i L je nezavisno izabran iz grupe koju čine C ili N, uz uvjet da nema više od tri uzastopna N, pri čemu je svaki izborno supstituiran sa jednim ili više A3.
5. Farmaceutska kompozicija koja sadrži spoj prema bilo kojem od patentnih zahtjeva 1 do 4, naznačena time što sadrži i najmanje jedan farmaceutski prihvatljiv nosač.
6. Farmaceutska kompozicija prema patentnom zahtjevu 5, naznačena time što se koristi za primjenu u liječenju poremećaja povezanih sa HCV-om.
7. Farmaceutska kompozicija prema patentnom zahtjevu 5 ili 6, naznačena time što dodatno sadrži nukleozidni analog.
8. Farmaceutska kompozicija prema patentnom zahtjevu 5 ili 6, naznačena time što dodatno sadrži interferon ili pegilirani interferon.
9. Farmaceutska kompozicija prema patentnom zahtjevu 7, naznačena time što je navedeni nukleozidni analog izabran iz grupe koju čine ribavirin, viramidin, levovirin, L-nukleozid i izatoribin i navedeni interferon je α-interferon ili pegilirani interferon.
10. Uporaba spoja prema bilo kojem od patentnih zahtjeva 1 do 4, naznačena time što se koristi za pripremu lijeka za liječenje hepatitisa C ili poremećaja povezanog sa hepatitisom C.
11. Spoj prema bilo kojem od patentnih zahtjeva 1 do 4, naznačena time što se koristi za primjenu u postupku za liječenje hepatitisa C ili poremećaja povezanog sa hepatitisom C.
HR20110732T 2004-07-16 2011-10-11 Antivirusni spojevi HRP20110732T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US58863304P 2004-07-16 2004-07-16
US59163504P 2004-07-27 2004-07-27
PCT/US2005/025503 WO2006020276A2 (en) 2004-07-16 2005-07-18 Antiviral compounds

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HRP20110732T1 true HRP20110732T1 (hr) 2011-11-30

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HR20070043A HRP20070043A2 (hr) 2004-07-16 2007-02-09 Antivirusna sredstva
HR20110732T HRP20110732T1 (hr) 2004-07-16 2011-10-11 Antivirusni spojevi

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US (2) US20080311077A1 (hr)
EP (2) EP1778702B1 (hr)
JP (2) JP5676839B2 (hr)
KR (1) KR20070034119A (hr)
AP (1) AP2461A (hr)
AR (1) AR050174A1 (hr)
AT (1) ATE516293T1 (hr)
AU (1) AU2005274700B2 (hr)
BR (1) BRPI0513426A (hr)
CA (1) CA2571984C (hr)
CY (1) CY1112453T1 (hr)
DK (1) DK1778702T3 (hr)
EA (1) EA200700336A1 (hr)
ES (1) ES2468441T3 (hr)
HK (1) HK1103089A1 (hr)
HR (2) HRP20070043A2 (hr)
IL (1) IL180288A0 (hr)
MX (1) MX2007000584A (hr)
NO (1) NO20070866L (hr)
NZ (1) NZ552405A (hr)
PL (2) PL382845A1 (hr)
PT (1) PT1778702E (hr)
RS (1) RS51974B (hr)
TW (2) TW201228665A (hr)
WO (1) WO2006020276A2 (hr)

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