| 摘要 |
PURPOSE: Spingosin-1-phosphate derivatives and a preparation method thereof are provided. The compounds are useful as both agonist and antagonist of EDG(endothelial differentiation gene) receptor. CONSTITUTION: Spingosin-1-phosphate derivatives are represented by the formula 1, wherein R1 and R2 are independently hydrogen, C1-6 alkyl, sugars or inositols; R3 and R4 are independently hydrogen, C1-6 alkyl, (CH2)m-benzene-(R7)p or form 3 to 8-membered heterocyclic ring together with bound nitrogen; m is 0, 1, 2 or 3; p is 0, 1 or 2; R7 is hydroxy, amino, C1-6 alkyl, halogen, C1-6 alkyloxy or C1-6 alkylamino; R5 is hydrogen or OH or 0; L is O, S, CH2 or NH; R6 is -R8, X-benzene-R9, -NR10R11 or -OR12; R8 is hydrogen, C1-20 alkyl, 1 to 9 halogen-substituted C1-20 alkyl, 1 to 8-membered cyclic alkyl, 1 to 9 halogen-substituted 3 to 8-membered cyclic alkyl or (CH2)n-X-benzene-(R13)q; R9 is hydrogen, amino, hydroxy, halogen, C1-20 alkylamino, 3 to 8-membered cyclic alkylamino, C1-20 alkyloxy, 3 to 8-membered cyclic alkyloxy, 1 to 9 halogen substituted C1-20 alkyl or 1 to 9 halogen substituted 3 to 8-membered cyclic alkyl; R10, R11 and R12 are independently hydrogen, C1-20 alkyl, 3 to 8-membered cyclic alkyl or (CH2)n-X-(R13)q; R13 is the same as R9; X is N or CH; n is 0, 1, 2, 3, 4 or 5; and q is 0, 1 or 2.
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