C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 65/24 (2006.01) A61K 31/19 (2006.01) A61K 31/215 (2006.01) A61K 31/33 (2006.01) C07C 43/23 (2006.01) C07C 45/00 (2006.01) C07C 45/60 (2006.01) C07C 45/63 (2006.01) C07C 45/67 (2006.01) C07C 45/71 (2006.01) C07C 47/565 (2006.01) C07C 47/575 (2006.01) C07C 49/813 (2006.01) C07C 49/84 (2006.01) C07C 59/68 (2006.01) C07C 59/90 (2006.01) C07C 65/26 (2006.01) C07C 65/28 (2006.01) C07C 69/736 (2006.01) C07C 69/738 (2006.01) C07C 205/34 (2006.01) C07C 205/37 (2006.01) C07C 205/38 (2006.01) C07C 217/76 (2006.01
Patent
CA 2176363
Compounds of formula (I) are described wherein R1 is hydrogen, -(lower alkyl)q(CO2R6 or OH), -CN, -C(R7)=NOR8, NO2, -O(lower alkyl)R9, -CC-R10, - CR11=C(R12)(R13), -C(=O)CH2C(=O)CO2H, -CO(R14), alkylthio, alkylsulphinyl, alkylsulphonyl, carbamoyl, thiocarbamoyl, substituted carbamoyl, substituted thiocarbamoyl, sulphamoyl or an optionally substituted nitrogen-containing ring, m, n, o and p are independently zero or 1 and R2, R3, R4 and R5 are various groups; and physiologically acceptable salts, N-oxides and prodrugs thereof. The compounds have endothelin antagonist activity and are useful as pharmaceuticals.
L'invention concerne des composés de formule (I) dans laquelle R?1¿ représente hydrogène, -(alkyle inférieur)¿q?(CO¿2?R?6¿ ou OH), -CN, -C(R?7¿)=NOR?8¿, NO¿2?, -O(alkyle inférieur)R?9¿, -C?C-R?10¿, -CR?11¿=C(R?12¿)(R?13¿), -C(=O)CH¿2?C(=O)CO¿2?H, -CO(R?14¿), alkylthio, alkylsulfinyle, alkylsulfonyle, carbamoyle, thiocarbamoyle, carbamoyle substitué, thiocarbamoyle substitué, sulfamoyle ou un cycle contenant de l'azote facultativement substitué, m, n, o et p représentent indépendamment zéro ou 1 et R?2¿, R?3¿, R?4¿, et R?5¿ représentent différents groupes. L'invention porte également sur des sels physiologiquement acceptables, des N-oxydes et des promédicaments de ces derniers. Ces composés présentent une activité d'antagonistes de l'endothéline et sont utiles en tant que produits pharmaceutiques.
Astles Peter Charles
Harper Mark Francis
Harris Neil Victor
Lewis Richard Alan
Mccarthy Clive
Macrae & Co.
Rhone-Poulenc Rorer Limited
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