11.beta.-Substituted steroids

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United States of America Patent

PATENT NO 4292251
SERIAL NO

05873784

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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Novel and biologically active 11.beta.-substituted steroids of the oestrane series are disclosed having the formula ##STR1## wherein (a) R.sub.1 is O or (.alpha.Y)(.beta.Z), wherein Y is selected from the group consisting of H, unsaturated aliphatic hydrocarbons of two to about four carbon atoms, saturated aliphatic hydrocarbons of about one to four carbon atoms, and Z is a free, esterified, or etherified hydroxy group; (b) R.sub.2 is H and R.sub.3 is H or CH.sub.3 ; in the alternative, R.sub.2 and R.sub.3 together constitute a carbon--carbon bond; and (c) ring A has the structure ##STR2## wherein R.sub.4 in compound (II) is a free, esterified, or etherified hydroxyl group, and R.sub.5 in compound (III) is O or is two hydrogens. The new steroids possess oestrogenic, antioestrogenic, progestational, ovulation-inhibiting, uterotropic, androgenic, and anabolic properties for therapeutic administration. Administration may be accomplished via pharmaceutically acceptable compositions containing these compounds in a parenteral, oral or enternal manner (for example, liquid presentations as solutions, suspensions, emulsions, ointments, pastes and solid pharmaceutical presentations such as tablets, pills, capsules and dragees) to take advantage of the recited properties.

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Patent Owner(s)

  • AKZONA INCORPORATED

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Overbeek, Gerhard A Nijmegen, NL 1 8

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