abstract |
PROBLEM TO BE SOLVED: To provide a VEGF receptor antagonist for treating a disease involving angiogenesis or vascular hyperpermeability. SOLUTION: The following formula (1): [R 1 is a hydrogen atom, a C 1-6 alkyl group, etc., R 2 is a hydrogen atom, a C 1-6 alkyl group, R 3 is a C 8-25 alkyl group, etc., R 4 is a hydrogen atom, OR 9 or CO 2 R 10 (where R 9 And R 10 are a hydrogen atom or a C 1-6 alkyl group), A is S (O) q R 15 (where q is 0, 1 or 2, and R 15 is a C 1-6 alkyl group, a phenyl C 1-3 alkyl group or (CH 2) such as m OR 16 (m is 2 or 3, R 16 a hydrogen atom or a methoxymethyl group), X is O, a single bond, CH = CH, CO Or NR 27 (R 27 is a hydrogen atom or a t-butoxycarbonyl group), Y is O, CONH, NHCO or NR 28 (R 28 is a hydrogen atom or a t-butoxycarbonyl group), n is an integer from 0 to 15. ] Or a pharmaceutically acceptable salt thereof as an active ingredient. |