SI9620136B - Substituted n-/(aminoiminomethyl or aminomethyl)phenyl/-propyl amides - Google Patents

Substituted n-/(aminoiminomethyl or aminomethyl)phenyl/-propyl amides Download PDF

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SI9620136B
SI9620136B SI9620136A SI9620136A SI9620136B SI 9620136 B SI9620136 B SI 9620136B SI 9620136 A SI9620136 A SI 9620136A SI 9620136 A SI9620136 A SI 9620136A SI 9620136 B SI9620136 B SI 9620136B
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compound according
pharmaceutically acceptable
acceptable salt
optionally substituted
alkyl
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SI9620136A
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SI9620136A (sl
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Kevin R Guertin
Scott I Klein
Alfred P Spada
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Aventis Pharma Inc
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Publication of SI9620136B publication Critical patent/SI9620136B/sl

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    • C07D207/30Heterocyclic 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 two double bonds between ring members or between ring members and non-ring members
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Claims (24)

  1. Λ Patentni zahtevki 1. Spojina s formulo
    Ri in R2 sta vodik ali skupaj =NRg; R3 je -C02R6, -C(0)R6, -CONR^R*, -CH2OR7 ali -CH2SR7; R4 je skupina s formulo:
    ali je R4 vodik, alkil, cikloalkil ali cikloalkilalkil; R5 je alkil, alkenil, po izbiri substituiran aril ali po izbiri substituiran heteroaril; R<5 je vodik ali C^alkil; R7 je vodik, C^alkil, Ci.7acil, aroil ali heteroaril; R8 je vodik ali Ci_6alkil; Roje Ri0O2C-, R10O-, HO-, ciano, Ri0CO-, HCO-, Ci^alkil, nitro ali Υ^Ν-, kjer je Rio po izbiri substituiran alkil, po izbiri substituiran aralkil ali po izbiri substituiran heteroaralkil in kjer sta Υ1 in Y2 neodvisno vodik ali alkil; A in B sta vodik ali skupaj vez; Ar je po izbiri substituiran aril ali po izbiri substituiran heteroaril in n je 0, 1 ali 2, ali njena farmacevtsko sprejemljiva sol, njen N-oksid, njen hidrat ali njen solvat. 2-
  2. 2. Spojina po zahtevku 1, označena s tem, da sta Rj in R2 skupaj =NH.
  3. 3. Spojina po zahtevku 2, označena s tem, da sta Ri in R2 skupaj =NH in tvorita aminoiminometil na fenilnem delu, ki je v meta položaju glede na položaj vezave fenilnega dela na propilnem delu.
  4. 4. Spojina po zahtevku 1, označena s tem, daje R3 -C02R$, -CH2OR7 ali -CH2SR7.
  5. 5. Spojina po zahtevku 4, označena s tem, daje R3 -C02R$ in je R$ Ci^alkil.
  6. 6. Spojina po zahtevku 4, označena s tem, da je R3 -CH2OR7 ali -CH2SR7 in je R7 vodik ali Ci.6alkil.
  7. 7. Spojina po zahtevku 1, označena s tem, daje n 1.
  8. 8. Spojina po zahtevku 1, označena s tem, daje Ar po izbiri substituiran aril.
  9. 9. Spojina po zahtevku 1, označena s tem, daje Ar fenil.
  10. 10. Spojina po zahtevku 1, označena s tem, da je R5 po izbiri substituiran fenil, po izbiri substituiran bifenil, po izbiri substituiran naftil ali po izbiri substituiran heterobifenil.
  11. 11. Spojina po zahtevku 1, označena s tem, daje: 3
    η2ν
    ^ COOMe Η2Ν P*» ΝΗ ΗΝ /=\ >oc
    η2νγ^νη. F
    8
    ο2ν η2ν
    5
    NHAc
    Η2ΝΓ ^NH. H2N^NH. 40
    ΓΛ
    ιΓΛ
    ο ΝΗ ΟΑΑ OMe ΝΗ ΝΗ2
    43 0-0^° '—' ΝΗ Ο \* Ν-λ * ο
    Ph' °Μβ ΝΗ ΝΗ, ΝΗ Ο Ph-~^-^v*A V' £ °Me ΝΗ "Ό^ b-Oi ali ΝΗ Ο Ph '0H ΝΗ ali njena farmacevtsko sprejemljiva sol.
  12. 12. Farmacevtski sestavek, označen s tem, da obsega farmacevtsko sprejemljivo količino spojine po zahtevku 1 in farmacevtsko sprejemljiv nosilec.
  13. 13. Uporaba farmacevtsko učinkovite količine spojine po zahtevku 1 ali njene farmacevtsko sprejemljive soli za izdelavo zdravila za zdravljenje patološkega učinka trombina.
  14. 14. Uporaba farmacevtsko učinkovite količine spojine po zahtevku 1 ali njene farmacevtsko sprejemljive soli za izdelavo zdravila za zdravljenje venske ali arterijske tromboze pri pacientu.
  15. 15. Uporaba farmacevtsko učinkovite količine spojine po zahtevku 1 ali njene farmacevtsko sprejemljive soli v kombinaciji s heparinom ali heparinom z nizko molekulsko maso za izdelavo zdravila za zdravljenje venske ali arterijske tromboze.
  16. 16. Uporaba farmacevtsko učinkovite količine spojine po zahtevku 1 ali njene farmacevtsko sprejemljive soli za izdelavo zdravila za zdravljenje restenoze pri pacientu.
  17. 17. Spojina po zahtevku 11, označena s tem, daje:
    ali
    COOMe ΎΟΟ H2N^-NH ali njena farmacevtsko sprejemljiva sol. AS
  18. 18. Spojina po zahtevku 11, označena s tem, daje:
    ali njena farmacevtsko sprejemljiva sol.
  19. 19. Spojina po zahtevku 11, označena s tem, daje:
    ali
    ali njena farmacevtsko sprejemljiva sol.
  20. 20. Spojina po zahtevku 11, označena s tem, daje:
    ali ali njena farmacevtsko sprejemljiva sol.
  21. 21. Spojina po zahtevku 11, označena s tem, daje:
    ali njena farmacevtsko sprejemljiva sol.
  22. 22. Spojina po zahtevku 11, označena s tem, da je: O
    ali njena farmacevtsko sprejemljiva sol.
  23. 23. Spojina po zahtevku 11, označena s tem, daje: 9
    ali njena farmacevtsko sprejemljiva sol.
  24. 24. Spojina po zahtevku 11, označena s tem, daje:
    ali njena farmacevtsko sprejemljiva sol.
SI9620136A 1996-01-02 1996-12-23 Substituted n-/(aminoiminomethyl or aminomethyl)phenyl/-propyl amides SI9620136B (en)

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