DK2049506T5 - Modulatorer af terapeutikas farmakokinetiske egenskaber - Google Patents

Modulatorer af terapeutikas farmakokinetiske egenskaber Download PDF

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DK2049506T5
DK2049506T5 DK07836007.0T DK07836007T DK2049506T5 DK 2049506 T5 DK2049506 T5 DK 2049506T5 DK 07836007 T DK07836007 T DK 07836007T DK 2049506 T5 DK2049506 T5 DK 2049506T5
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Manoj C Desai
Allen Yu Hong
Hongtao Liu
Lianhong Xu
Randall W Vivian
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Gilead Sciences Inc
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Claims (12)

  1. MODULATORER AF TERAPEUTIKAS FARMAKOKINETISKE EGENSKABER PATENTKRAV
    1. Forbindelse med formlen IIB:
    eller et/en farmaceutisk acceptabell/acceptabel salt, solvat, stereoisomer og/eller ester deraf, hvor: R10a og R10b hver uafhængigt er FI eller -C'i^-alkyl; R12 er H eller -CH3; R13 er H, -C^-alkyl, -(CH2)0.iCR17R18OR19, -(CH2)0.3CR17R18NR20R21, -(CH2)0. 3CR17R18NR17C(O)NR20R21, -(CH2)1.3C(0)R22, -(CH2)i_3S(0)2R22 eller -(CH2)1.3-R23; R14 og R15 hver uafhængigt er H, -C^-alkyl eller arylalkyl; R17 og R18 hver uafhængigt er FI eller -Cj^-alkyl; R19 er H, -CV4-alkyl eller-arylalkyl; R20 og R21 hver uafhængigt er FI, -Ci.3-alkyl, -C(0)R17 eller -S(0)2R17; eller R20 og R21, sammen med det nitrogenatom, hvortil de er bundet, danner en ikke-substitueret eller substitueret 5-6-leddet heterocyclylring indeholdende 1-2 heteroatomer udvalgt fra gmppen bestående af N og O; R22 er H, -C^-alkyl, -OR19 eller -NR20R21; og R23 er en ikke-substitueret eller substitueret 5-6-leddet heterocyclylring indeholdende 1-2 heteroatomer udvalgt fra gruppen bestående af N og O; hvor den ikke-substituerede eller substituerede 5-6-leddede heterocyclylring dannet af R20 og R21 og den ikke-substituerede eller substituerede 5-6-leddede heterocyclylring af R23 hver uafhængigt er ikke-substitueret eller substitueret med en Ci_2-alkyl.
  2. 2. Forbindelse ifølge krav 1, hvor: R13 er -(CH2y3CR17R18NR20R21, -(CH2)0_3CR17R18NR17C(O)NR20R21 eller -(CH2)k;-R23.
  3. 3. Forbindelse ifølge krav 2, hvor: R13 er -(CH2)o_3CR17R18NR20R21 eller -(CH2y3CR17R18NR17C(O)-NR20R21.
  4. 4. Forbindelse ifølge krav 1 med formlen IIC:
    Formel IIC eller et/en farmaceutisk acceptabelt/acceptabel salt, solvat, stereoisomer og/eller ester deraf, hvor: R13 er H, -C14-alkyl, -(CH2)0.|CR17RISOR19, -(CH2V3CR17R18NR20R21, -(CH2)0. 3CR17R18NR17C(O)NR20R21, -(CH2)1.3C(0)R22 eller -(CH2)I4-R2i; R17 og R18 hver uafhængigt er H eller Ci_3-alkyl; R19 er H, -C14-alkyl eller -arylalkyl; R20 og R21 hver uafhængigt er H, -Ci.3-alkyl, -C(0)R17 eller -S(0)2R17; eller R20 og R21, sammen med det nitrogenatom, hvortil de er bundet, danner en 5-6-leddet heterocyclylring indeholdende 1-2 heteroatomer udvalgt fra gruppen bestående af N og O; R22 er H, -C^alkyl, -OR19 eller -NR20R21; og R23 er en ikke-substitueret eller substitueret 5-6-leddet heterocyclylring indeholdende 1-2 heteroatomer udvalgt fra gruppen bestående af N og O.
  5. 5. Forbindelse ifølge krav 1 med formlen
    eller et/en farmaceutisk acceptabelt/acceptabel salt, stereoisomer og/eller solvat deraf.
  6. 6. Forbindelse ifølge krav 5, der er:
    eller et farmaceutisk acceptabelt salt deraf.
  7. 7. Forbindelse ifølge krav 1, der udvalgt fra gruppen bestående af:
    eller farmaceutisk acceptable salte, solvater, estere og/eller stereoisomerer deraf.
  8. 8. Forbindelse ifølge krav 1, hvilken forbindelse er udvalgt fra gruppen bestående af
    Og
    eller farmaceutisk acceptable salte, solvater, estere og/eller stereoisomerer deraf.
  9. 9. Farmaceutisk sammensætning omfattende en forbindelse ifølge et hvilket som helst af kravene 1 til 8, eller et/en farmaceutisk acceptabelt/acceptabel salt, solvat og/eller ester deraf og et farmaceutisk acceptabelt bærestof eller excipiens.
  10. 10. Forbindelse ifølge et hvilket som helst af kravene 1 til 8 til anvendelse i terapi.
  11. 11. Forbindelse ifølge et hvilket som helst af kravene 1 til 8 til anvendelse ved forbedring af farmakokinetik for et lægemiddel, der metaboliseres ved cytochrom P450 monooxygenase, øgning af blodplasmaniveauet for et lægemiddel, der metaboliseres ved cytochrom P450 monooxygenase, hæmning af cytochrom P450 monooxygenase, behandling af en HIV-infektion eller behandling af en HCV-infektion hos en patient.
  12. 12. Forbindelse til anvendelse ifølge krav 11, hvor den cytochrome P450 monooxygenase er cytochrom P450 monooxygenase 3A.
DK07836007.0T 2006-07-07 2007-07-06 Modulatorer af terapeutikas farmakokinetiske egenskaber DK2049506T5 (da)

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