Reference

Preparation and use of aromatase inhibitors as contraceptives for female primates which leave the menstrual cycle unaffected

All Rights Reserved. Preparation and use of aromatase inhibitors as contraceptives for female primates which leave the menstrual cycle unaffected. Bhatnagar, Ajay (Ciba-Geigy A.-G.; Novartis A.-G., Switz.). Ger. Offen. DE 4213005 A1 29 Oct 1992, 24pp. (German). (Germany). CODEN: GWXXBX. CLASS: ICM: A61K045-00. 4595-59-9 and 288-88-0 are cas registry numbers of chemicals which are used as reagents here. ICS: A61K031-44; A61K031-275. APPLICATION: DE 1992-4213005 21 Apr 1992. PRIORITY: CH 1991-1227 24 Apr 1991. DOCUMENT TYPE: Patent CA Section: 28 (Heterocyclic Compounds (More Than One Hetero Atom)) Section cross-reference(s): 1 Use of aromatase inhibitors for prepn. of pharmaceuticals which prevent conception in female primates without affecting the menstrual cycle is claimed. Thus, 4-[a-(4-cyanophenyl)-1-(1,2,4-triazolyl)methyl]benzonitrile was stirred 1 h with KN(SiMe3)2 in THF/PhMe at -78°; N-fluorodimethylsaccharinsultam in THF was added followed by stirring for 1.5 h to give 4-[a-(4-cyanophenyl)-a-fluoro-1-(1,2,4-triazolyl)methyl]benzonitrile. A continuous infusion of Fadrozole hydrochloride [4-(5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-5-yl)benzonitrile hydrochloride] at 500 mg/day in female bonnet monkeys from days 13-26 of their ovarian cycle completely prevented pregnancy, vs. 80% pregnancy for untreated controls. .