Title:
【発明の名称】新規選択性アロマターゼ抑制化合物
Document Type and Number:
Japanese Patent JP3186771
Kind Code:
B2
Abstract:
PCT No. PCT/FI93/00539 Sec. 371 Date May 19, 1995 Sec. 102(e) Date May 19, 1995 PCT Filed Dec. 14, 1993 PCT Pub. No. WO94/13645 PCT Pub. Date Jun. 23, 1994New compounds of formula (I) wherein R1 is H, CH3, OCH3, NO2, NH2, CN, CF3, CHF2, CH2F or halogen, R2 is a heterocyclyl radical selected from 1-imidazolyl, triazolyl, tetrazolyl, pyrazolyl, pyrimidinyl, oxazolyl, thiazolyl, isoxazolyl and isothiazolyl, R3 is H or OH, R4 is H, R5 is H or OH; or R4 is H and R3 and R5 combined form a bond; or R3 is H and R4 and R5 combined form -(O); R6 is methylene, ethylene, -CHOH-, -CH2-CHOH-, -CHOH-CH2-, -CH-CH- or -C(-O)-; or R4 is H and R5 and R6 combined is -CH- or -CH-CH2-; stereoisomers thereof and non-toxic pharmaceutically acceptable acid addition salts thereof exhibit selective aromatase inhibiting properties, compared with their desmolase inhibiting properties. The compounds of the invention are valuable in the treatment of estrogen dependent diseases, e.g. breast cancer or benign prostatic hyperplasia (BPH).
Inventors:
Karja Rainen, Alt Johannes
Sederval, Maruya-Lisa
Calapdas, Alya Marchetta
Perkonen, Reino Orabi
Linee, Aire Maruya
Lamin Tausta, Risto Arbo Sakari
Salonen and Yarmo Sakari
Sederval, Maruya-Lisa
Calapdas, Alya Marchetta
Perkonen, Reino Orabi
Linee, Aire Maruya
Lamin Tausta, Risto Arbo Sakari
Salonen and Yarmo Sakari
Application Number:
JP51384094A
Publication Date:
July 11, 2001
Filing Date:
December 14, 1993
Export Citation:
Assignee:
Lamin Tausta, Risto Arbo Sakari
International Classes:
C12N9/99; A61K31/41; A61K31/415; A61K31/4164; A61K31/4192; A61K31/4196; A61K31/425; A61K31/426; A61P3/06; A61P9/10; A61P13/08; A61P35/00; A61P43/00; C07D231/00; C07D233/58; C07D233/61; C07D239/00; C07D249/04; C07D249/08; C07D257/04; C07D261/00; C07D263/00; C07D275/00; C07D277/20; C07D277/22; C07D277/30; C07D521/00; C07D; (IPC1-7): C07D233/61; A61K31/41; A61P13/08; A61P35/00; C07D249/08; C07D257/04; C07D277/22
Other References:
【文献】米国特許4235620(US,A)
Attorney, Agent or Firm:
Sota Asahina (1 person outside)