1,1,2-triphenylbut-1-ene derivatives

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United States of America Patent

PATENT NO 5047431
SERIAL NO

07523266

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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Novel (E)-1-[4'-(2-alkylaminoethoxy)phenyl]-1-(3'-hydroxyphenyl)-2-phenylbut-1-enes of the general formula ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different, provided that, when R.sup.1 and R.sup.2 are the same, each of them is a methyl or ethyl radical, and when R.sup.1 and R.sup.2 are different, one of them is hydrogen and the other is a methyl or ethyl radical, and the therapeutically compatible salts thereof, have a marked anti-estrogenic effect and are suitable for treating hormone-dependent mammary tumors. The compounds can be prepared by dehydrating carbinols of the general formula ##STR2## wherein R.sup.1 and R.sup.2 may be the same or different, provided that, when R.sup.1 and R.sup.2 are the same, each of them is a methyl or ethyl radical, and when R.sup.1 and R.sup.2 are different, one of them is a benzyl radical and the other is a methyl or ethyl radical; and wherein R.sup.3 is hydrogen or an easily hydrolyzable protecting group, through the action of mineral acid while removing any protecting group present, isolating through crystallization the E-form from the pair of isomers obtained, and removing by hydrogenolysis any benzyl group present. Compositions comprising the subject 1,1,2-triphenylbut-1-ene derivatives are described also. The corresponding novel 1,1,2-triphenylbut-1-ene derivatives having the (Z) configuration are also disclosed.

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Patent Owner(s)

Patent OwnerAddress
KLINGE PHARMA GMBH & COMUNICH

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Grill, Helmut Vaterstetten, DE 7 95
Loser, Roland Feldafing, DE 22 233
Schickaneder, Helmut Poing, DE 40 303

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