Novel tri-phenyl alkane and alkene derivatives and their preparation and use

Abstract

Abstract The invention provides novel compounds of the formula: ##STR1## wherein n is 0 to 4, R 1 and R 2 , which can be the same or different are H, OH, alkoxy of 1 to 4 carbon atoms, benzyloxy or methoxymethoxy; R 3 is H, OH, halogen, alkoxy of 1 to 4 carbon atoms, benzyloxy, methoxymethoxy, 2,3-dihydroxypropoxy or ##STR2## wherein m is 1 or 2, R 6 and R 7 , which can be the same or different are H or an alkyl group of 1 to 4 carbon atoms, or ##STR3## can form an N-containing three-, four-, five- or six-membered heterocyclic ring; R 4 is OH, F, Cl, Br, I, mesyloxy, tosyloxy, alkylcarbonyloxy of 1 to 4 C-atoms, formyloxy or CH 2 R 4 is replaced by CHO; R 5 is H or OH; or R 4 and R 5 together form an --O-- bridge between the carbon atoms to which they are attached, and their non-toxic pharmaceutically acceptable salts and esters and mixtures thereof. Processes for the preparation of these compounds are described, and also novel pharmaceutical compositions containing them. These compounds exhibit valuable pharmacological properties as estrogenic, anti-estrogenic, and progestanic agents. They are also effective against oestrogen-dependent tumors. Certain compounds are useful as chemical intermediates for the preparation of pharmacologically active compounds of the invention.

Inventors

• 👤 Reijo J. Toivola
• 👤 Arto J. Karjalainen
• 👤 Kauko O. A. Kurkela
• 👤 Marja-Liisa Soderwall
• 👤 Lauri V. M. Kangas
• 👤 Guillermo L. Blanco
• 👤 Hannu K. Sunduiqst

Bibliographic Details