AZA-INDOLES AND RELATED COMPOUNDS HAVING SPHINGOSINE-1-PHOSPHATE (S1P) RECEPTOR ANTAGONIST BIOLOGICAL ACTIVITY

摘要

The present invention provides compounds having the formula: (I), (II), Wherein n is I or 2; m is 0 or 1; p is 0, 1 or 2; R1 is aryl, heteroaryl or alkyl: R2 is C1-6 hydrocarbyl, alkylacyl or hydroxyalkyl; R3 is aryl, heteroaryl, or alkyl; R4 is H, OH, -O-(C1-6 alkyl), -NH-(C1-6 alkyl), or oxide; R5 is H, halogen, C1-6 alkyl, O-(C1-6 alkyl), aryl, heteroaryl, -C(=O)(C1-6 alkyl), substituted or un-substituted oxazolin-2-yl; X = 0, NH -C(=O)- or -N=CH-; and Each L is independently alkylene and carbonyl. This compounds are SI P antagonists useful for treating a disease selected from: glaucoma, dry eye, angiogenesis, cardiovascular conditions and diseases, wounds, and pain.