C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 209/42 (2006.01) A61K 31/404 (2006.01)
Patent
CA 2552781
The present invention relates to agonists of the S1P4 receptor, which are selective for the S1P4 receptor over one or more of the S1P1, S1P2, S1P3 or S1P5 receptors of at least 10 fold, in particular new indol-alanine derivatives of structure (I), process for their production, their uses, in particular in transplantation, and pharmaceutical compositions containing them (I) wherein R1 is phenyl or naphthyl, wherein phenyl is substituted by one or two of halogen, C1-6alkyl, C1-6alkoxy or phenylC1-6alkyl; and R2 is hydrogen or C1-6alkyl; in free or salt form.
La présente invention concerne des agonistes du récepteur S1P4 qui sont sélectifs du récepteur S1P4 sur un ou plusieurs des récepteurs S1P1, S1P2, S1P3 ou S1P5 d'au moins 10 replis. L'invention concerne en particulier de nouveaux dérivés d'indol-alanine de structure (I), un procédé pour les produire, leurs utilisations, en particulier pour la transplantation, et des compositions pharmaceutiques qui les contiennent. Dans la formule (I) : R¿1? est phényle ou naphthyle, phényle étant substitué par un ou deux halogène, alkyle en C¿1-6?, alcoxy en C¿1-6 ?ou phényl-C¿1-6?-alkyle ; et R¿2? est hydrogène ou alkyle en C¿1-6?; sous forme libre ou sous forme de sel.
Azzaoui Kamal
Bouhelal Rochdi
Buehlmayer Peter
Guerini Danilo
Koller Manuel
Fetherstonhaugh & Co.
Novartis Ag
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