C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 217/26 (2006.01) A61K 31/47 (2006.01) C07K 5/078 (2006.01) A61K 38/00 (2006.01)
Patent
CA 2250664
Substituted isoquinoline-3-carboxamides, their preparation and their use as pharmaceuticals Novel isoquinoline-3-carboxamides of the formula I Image in which R1 is hydrogen or chlorine, R2 is hydrogen, alkyl, alkoxy, chlorine, trifluoromethyl, hydroxyl, or benzyloxy which is optionally substituted, or fluoroalkoxy of the formula O-[CH2]x-C f H(2f+1-g)F g where x = O or 1, f = 1 - 5 and g = 1 to (2f+1), R3 is hydrogen, alkyl, alkoxy, fluorine, chlorine, cyano, trifluoromethyl, hydroxyl, or benzyloxy which is optionally substituted, or fluoroalkoxy of the above formula, R4 and R5 are hydrogen, alkyl, fluorine, chlorine, bromine, trifluoromethyl, cyano, alkoxy, or fluoroalkoxy of the above formula, including the physiologically active salts, are strong prolyl-4-hydroxylase inhibitors which do not cause steatosis.
Dérivés de substitution d'isoquinoline-3-carboxamides; leur préparation et leur utilisation comme produits pharmaceutiques. Nouveaux isoquinoline-3-carboxamides de formule I Image , dans laquelle R1 est un hydrogène ou un chlore, R2 est un hydrogène, un groupe alkyle, alcoxy, chlore, trifluorométhyle, hydroxyle ou benzyloxy avec substitution facultative, ou fluoroalcoxy de formule O-[CH2]x-C f H(2f+1-g)F g, dans laquelle x = O ou 1, f = 1 - 5 et g = 1 à (2f+1), R3 est de l'hydrogène, un groupe alkyle, alcoxy, fluor, chlore, cyano, trifluorométhyle, hydroxyle ou benzyloxy avec substitution facultative, ou fluoroalcoxy correspondant à la formule ci-dessus, R4 et R5 sont de l'hydrogène, un groupe alkyle, fluor, chlore, brome, trifluorométhyle, cyano, alcoxy ou fluoroalcoxy correspondant à la formule ci-dessus; sont également inclus leurs sels physiologiquement actifs; ce sont de puissants inhibiteurs de la prolyl-4-hydroxylase, et ils n'induisent pas de stéatose.
Baringhaus Karl-Heinz
Tschank Georg
Weidmann Klaus
Werner Ulrich
Bereskin & Parr Llp/s.e.n.c.r.l.,s.r.l.
Hoechst Marion Roussel Deutschland Gmbh
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