| abstract |
The invention describes compounds that selectively modulate the sphingosine-1-phosphate receptor, including compounds that modulate subtype 1 of the S1P receptor, having the following structural formula: where the dotted line indicates that a single bond or double bond may be present, provided that two double bonds and three simple bonds in the ring containing A, Au, and A; A, A, and A, each independently, are C or S or N, with the proviso that one of A, A, and Ap represents S; R3 is a disubstituted phenyl, where the phenyl substituents are each independently selected from the group consisting of halogen, nitro, cyano, perfluoromethyl, fluorinated methyl, and C-alkoxy; with the proviso that the phenyl is substituted in the para-position with a C-alkoxy group; R represents where the wavy line indicates the point of attachment; X is -NR'R "or -OR '"; R 'represents H, C-alkyl, n-hydroxy C-alkyl, -SO-R or -CO-R; R "is H, -SO-R, C-alkyl, optionally substituted with 1 or more R, or a ring group, optionally substituted with R, where the ring group is piperidinyl, cyclohexyl, morpholinyl, thiazolyl, pyrazolyl, pyrrolidinyl, imidazolyl or phenyl; R "" represents H, C-alkyl or -CO-R; or R 'and R "together with the nitrogen atom to which they are bonded form a 4-, 5- or 6-membered saturated heterocyclic ring containing 0 or 1 additional heteroatom, where such additional heteroatom is O or N, where such heterocycle optionally substituted one or more times with substituents independently selected from the group consisting of —OH, oxo group, —NH, n-hydroxy-C-alkyl, —COOH, - (CH) -COOH, - (CH) -COOR, -N (RR) and - (CH) -CO-N (RR); each R is independently C-alkyl or H; |