| 摘要 |
PROBLEM TO BE SOLVED: To provide a new compound capable of exhibiting activity as a non- peptide antagonist to gonadotropin-releasing honnone (GnRH), and useful for treating various sex hormone-related symptoms of men and women. SOLUTION: A compound of formula I [A is a 1-6C alkyl or the like; R0 is H or the like; R1 is a radical of formula II (R13 is H, OH or the like; R14 and R15 are each H or the like) or the like; R2 is H or the like; R3, R4 and R5 are each H, a 1-6C alkyl or the like; R6 is H or the like; R7 is H or a 1-6C alkyl; R8 is H or the like; R9 and R9(a) are each H, a 1-6C alkyl or the like; R10 and R10(a) are each H or the like; (m) is 0-3; X is H, a halogen or the like], for example, N-[2-[2-(3,4-dimethoxyphenyl)-1H-indol-3-yl]ethyl]-3-(4- hydroxyphenyl)propionamide. The compound of formula I is, for example, obtained by starting from tryptamine via an N-phthalimidotryptamine derivative, then via 2-bromotryptamine, and further via a 2-aryltryptamine derivative. |
