abstract |
The present invention comprises sphingosine-1-phosphate receptor 2 (S1P2 ) antagonists of the formula (I) wherein R1 is -CH2CH=CH2, -CH3, or -CH2CH2CH2OH, R2 is -H, -CH2C02H, -CH2CH2OH, -CH2CH2CH2OH, -CH2CONH2, or -CH2C02Et and R3 is 4-substituted-2,6-dichloropyridine, 4-substituted 2-chloro-6-hydroxyethyl pyridine, 4-substituted-2-chloro-6-hydroxypropyl pyridine, 4-substituted-2-(aminoethyl)-6- chloro pyridine, 4-substituted-2-(aminoethylmethyl)-6-chloro pyridine or 5-substituted-2,3-dichloro thiophene. Pharmaceutical compositions comprising the sphingosine-1-phosphate S1P2 receptor 2 antagonist receptors are also disclosed as being useful in the treatment of neoplastic ocular disorders and blindness as well as fibrotic lung, kidney, liver and skin diseases. |