- NOVEL COMPOUNDS
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The present invention relates to novel compounds with a variety of therapeutic uses, more particularly novel prodrugs that are particularly useful for delivering a parent compound for selective estrogen receptor modulation.
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Page/Page column 32; 40-43
(2010/02/11)
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- 1,1,2-TRIPHENYLBUT-1-ENE DERIVATIVES
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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 1 and R. sup.2 may be the same or different, provided that, when R 1 and R 2 are the same, each of them is a methyl or ethyl radical, and when R 1 and R 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 1 and R 2 may be the same or different, provided that, when R. sup.1 and R 2 are the same, each of them is a methyl or ethyl radical, and when R 1 and R 2 are different, one of them is a benzyl radical and the other is a methyl or ethyl radical; and wherein R 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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- Studies in Potential Antifertility Agents: Part XXIV - Synthesis of 2,3-Disubstituted 4'-(&β-dialkylaminoethoxy)propiophenones
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A number of 2,3-disubstituted 4'-(β-dialkylaminoethoxy)propiophenones (32-41) have been synthesized as the structural analogs of a potent antifertility agent erythro-2,3-diphenyl-4'-(β-pyrrolidinoethoxy)valerophenone (1).Compounds 34, 35, 38 and 40 show cent per cent activity at dose levels of 2.5, 10, 10, 10 and 1 mg/kg, respectively.The structure activity relationship has also been discussed.
- Rao, K. V. B.,Iyer, R. N.
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