Sphingosine-1-phosphate receptor agonists, methods of preparing the same, and pharmaceutical compositions containing the same as an active agent

摘要

The present invention relates to novel compounds of Formula 1 as sphingosine-1-phosphate receptor agonists which can be effectively used for the treatment of autoimmune diseases, a method for preparing the same, and a pharmaceutical composition comprising the same as an active component. The compounds according to the present invention are effective on extensive autoimmune diseases and chronic inflammatory diseases including relapsing-remitting multiple sclerosis, and can also be used for treating or preventing immunoregulation disorders.

主权项

1. A compound of Formula 1, or a pharmaceutically acceptable salt or stereoisomer thereof: wherein X represents C or N, R1 represents optionally substituted alkyl,
wherein the optional substituent of the optionally substituted alkyl is one or more selected from halo(gen), cyano, hydroxyl, C1-C6-alkyloxy, oxo or sulfonyl unsubstituted or substituted by alkyl, R2 represents H, optionally substituted alkyl, halogen, CN, CF3 or COCF3,
wherein the optional substituent of the optionally substituted alkyl is one or more selected from halo(gen), cyano, hydroxyl, C1-C6-alkyloxy, oxo or sulfonyl unsubstituted or substituted by alkyl, W represents C, N, C-alkoxy, C-halogen or C—CN, Q represents CH2O or  and S is selected from the following residues: wherein m and n represent independently 0, 1, 2 or 3, R3-R10 represent independently H, alkyl, halogen, halogenoalkyl or alkoxyalkyl, R11 represents H,  and R12 represents OH, NH2,