PURPOSE: To obtain a new urea derivative and its pharmacologically permissible salt having steroid 5α-reductase inhibiting action and useful as an agent for the treatment of prostatomegaly, prostatic cancer, alopecia and acne.
CONSTITUTION: This urea derivative is a compound of formula I [R1 is H or a lower alkyl; R2 is H or a halogen; A is group of formula V [Y1-Y2-Y3 is R4C=CH-NR3, N=CH-NR3 or R3N-CH=N [R3 is CHR5R6 (R5 and R6 each is H, an alkyl or an aryl); R4 is H or CHR7R8 (R7 and R8 each is H, an alkyl or an aryl)]] or formula VI (R9 is H or CHR5R6); X is O or s(O)n (n is 0-2)] or its pharmacologically permissible salt, e.g. 4-[2-[3-[1-(4,4'-difluorobenzhydryl) indol-5-yl]ureido]phenoxy]butyric acid ethyl ester. The compound of formula I, the compound of formula Ia (the compound of formula I wherein R1 is an alkyl) and the compound of formula Ib (the compound of formula I wherein R1 is H) can be produced from a compound of formula IV and a compound of formula III derived from a compound of formula II.
TAKAMI HITOSHI
KUMAZAWA TOSHIAKI
TAKASAKI KOTARO
KISHIBAYASHI NOBUYUKI
ISHII AKIO
NONAKA HIROMI
KASE HIROSHI
