C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 275/42 (2006.01) A61K 31/17 (2006.01) A61K 31/40 (2006.01) C07D 207/27 (2006.01)
Patent
CA 2316235
The invention is directed to physiologically active compounds of general formula (I), wherein R1 is hydrogen, halogen, lower alkyl or lower alkoxy; X1, X2 and X6 independently represent N or CR2; and one of X3, X4 and X5 represents CR3 and the others independently represents N or CR2 [where R2 is hydrogen, halogen, lower alkyl or lower alkoxy; and R3 represents a group -L1- (CH2)n-C(=O)-N(R4)-CH2-CH2-Y]; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs. Such compounds have valuable pharmaceutical properties, in particular the ability to regulate the interaction of VCAM-1 and fibronectin with the integrin VLA- 4(.alpha.4.beta.1).
L'invention concerne des composés physiologiquement actifs de la formule générale (I) dans laquelle R?1¿ représente hydrogène, halogène, alkyle inférieur ou alcoxy inférieur, X?1¿, X?2¿ et X?6¿ représentent indépendamment N ou CR?2¿; et X?3¿, X?4¿ ou X?5¿ représente CR?3¿ et les autres représentent indépendamment N ou CR?2¿[où R?2¿ représente hydrogène, halogène, alkyle inférieur ou alcoxy inférieur; et R?3¿ représente un groupe -L?1¿-(CH¿2?)¿n?-C(=O)-N(R?4¿)-CH¿2?-CH¿2?-Y]; et leurs promédicaments, ainsi que des sels et solvates acceptables pharmaceutiquement de ces composés et leurs promédicaments. Ces composés présentent des propriétés pharmaceutiques de valeur, notamment la capacité de réguler l'interaction de VCAM -1 et la fibronectine avec l'intégrine VAL-4(.alpha.4.beta.1).
Astles Peter Charles
Harris Neil Victor
Morley Andrew David
Aventis Pharma Limited
Macrae & Co.
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