|Title:||Novel tri-phenyl alkane and alkene derivatives and their preparation and use|
|Abstract:||The invention provides novel compounds of the formula: ##STR1## wherein n is 0 to 4, R.sub.1 and R.sub.2, which can be the same or different are H, OH, alkoxy of 1 to 4 carbon atoms, benzyloxy or methoxymethoxy; R.sub.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.sub.6 and R.sub.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.sub.4 is OH, F, Cl, Br, I, mesyloxy, tosyloxy, alkylcarbonyloxy of 1 to 4 C-atoms, formyloxy or CH.sub.2 R.sub.4 is replaced by CHO; R.sub.5 is H or OH; or R.sub.4 and R.sub.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.|
|Inventor(s):||Toivola; Reijo J. (Oulu, FI), Karjalainen; Arto J. (Oulu, FI), Kurkela; Kauko O. A. (Oulu, FI), Soderwall; Marja-Liisa (Oulu, FI), Kangas; Lauri V. M. (Turki, FI), Blanco; Guillermo L. (Oulu, FI), Sunduiqst; Hannu K. (Kaarina, FI)|
|Assignee:||Farmos Group Ltd. (Turku, FI)|
1. A compound of the formula: ##STR50## or a non-toxic pharmaceutically acceptable salt or N-oxides thereof.
2. A compound according to claim 1 which is 4-chloro-1,2-diphenyl-1-[4-[2-(N,N-dimethylamino)ethoxy]phenyl]-1-butene or a non-toxic pharmaceutically acceptable salt thereof.
3. A compound according to claim 1 which is the trans-isomer of 4-chloro-1,2-diphenyl-1-[4-[2-(N,N-dimethylamino)ethoxy]phenyl]-1-butene or a non-toxic pharmaceutically acceptable salt thereof.
4. A compound according to claim 1 which is the citrate of the trans-isomer of 4-chloro-1,2-diphenyl-1-[4-[2-(N,N-dimethylamino)ethoxy]phenyl]-1-butene.
5. A pharmaceutical composition suitable for treating hormone-dependent tumours comprising an anti-tumour effective amount of a compound of claim 1 or a non-toxic pharmaceutically acceptable salt thereof and a compatible pharmaceutically carrier therefor.
6. A method of producing an anti-oestrogenic effect in a subject in which such an effect is desired which comprises administering to said subject an anti-oestrogenic effective amount of a compound as defined in claim 3 or a non-toxic pharmaceutically acceptable salt thereof.
7. A method according to claim 6 in which an antioestrogenic effect is produced in a subject suffering from an oestrogen-dependent tumour.
Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.