To obtain a new compound exhibiting steroid sulfatase inhibitory activity and useful for the therapy or prophylaxis for hormone dependent diseases.
This compound is represented by formula I (R1 is OH, an alkoxy or group NR2R3; R2 are each H, a 1-3C straight-chain alkyl or 3-8C branched alkyl), e.g. 3-hydroxyestra-1,3,5(10),16-tetraene-17, carboxylic acid. The compound of formula I is obtained, for instance, by hydrolyzing the nitrile of a compound of formula II (R4a is acetyl, benzoyl, methanesulfonyl or the like) [e.g. 17- cyano-3-hydroxyestra-1,3,5(10)-16-tetraene 3-methanesulfonate] in the presence of an acid such as hydrochloric acid or base such as sodium hydroxide, in a solvent such as ethylene glycol, preferably at 20-160°C for 5 m. to 140 h.
| JP2010505960 | Composition for reducing nicotine withdrawal and / or tobacco use |
| WO/1998/045285 | SOMATOSTATIN AGONISTS |
| WO/2003/050099 | PHENYLALKYNES |
AMISHIRO NOBUYOSHI
NAKADA TAISUKE
ISHIDA HIROYUKI
AKINAGA SHIRO
MURAGATA TSUTOMU
RII PYUI KAI
DYUUKUENSU UNIV OF THE HOLY GH