abstract |
The invention includes a sphingosine-1-phosphate receptor 2 (S1P2) antagonist of formula (I), wherein R1 is —CH2CH═CH2, —CH3, or —CH2CH2CH2OH, and R2 is —H , -CH2CO2H, -CH2CH2OH, -CH2CH2CH2OH, -CH2CONH2, or -CH2CO2Et, wherein R3 is 4-substituted-2,6-dichloropyridine, 4-substituted 2-chloro-6-hydroxyethylpyridine, 4-substituted- 2-chloro-6-hydroxypropylpyridine, 4-substituted-2- (aminoethyl) -6-chloropyridine, 4-substituted-2- (aminoethylmethyl) -6-chloropyridine, or 5-substituted-2 3-dichlorothiophene. Pharmaceutical compositions comprising sphingosine-1-phosphate S1P2 receptor 2 antagonist receptors are also disclosed as being useful for the treatment of neoplastic eye disorders and blindness, and fibrotic lung, kidney, liver, and skin diseases. [Selection figure] None |