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US 5,700,791 AGranted
Vitamin D derivatives modified in the 20-position and pharmaceutical compositions thereof
AssigneeSchering Corporation
InventorsAndreas Steinmeyer, Gunter Neef, Gerald Kirsch, Katica Schwarz, Ruth Thieroff-Ekerdt, Herbert Wiesinger, Martin Haberey
Life of this patent
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Abstract
The invention relates to vitamin D derivatives, modified in 20-position, of general formula I ##STR1## in which X, Y, Z, R.sub.1, R.sub.2 as well as R.sub.3 have the meaning indicated in the description, process for their production and their use as agents for treatment of hyperproliferative diseases of the skin.
Claims10
A vitamin D compound of the formula ##STR51## in which Y means a hydrogen atom, an alkanoyl group of 1 to 9 carbon atoms, or an aroyl group, wherein each Y is chosen independently;
- Z means a hydrogen atom, a hydroxyl group or an alkanoyloxy group of 1 to 9 carbon atoms,
- X means a hydrogen atom or both X's together mean an exocyclic methylene group,
- R.sub.1 and R.sub.2, independent of one another, mean an alkyl group of 1 to 4 carbon atoms,
- R.sub.3 means a linear or branched alkyl group of 1 to 5 carbon atoms or a trifluoromethyl group, or the two R.sub.3 groups together with carbon atom 25 form a cyclopropyl or cyclopentyl ring,
- L means the grouping ##STR52## in which A represents an oxygen atom, and B represents an alkylene group --(CH.sub.2).sub.n --, in which n=1, 2, 3, 4, 5 or 6, or
- L means grouping ##STR53## in which D represents a direct bond, a methylene bridge or a 1,2-ethenediyl bridge (E-double bond) between carbon atoms 20 and 22,
- E and F respectively represent a hydrogen atom, or together a second bond (E-double bond), and
- G represents a direct bond or an alkylene group --(CH.sub.2).sub.n -, in which n=1, 2, 3, 4, 5 or 6 or a corresponding alkylene group in which a methylene group is replaced by an oxygen atom with the proviso that when the two X's together mean a methylene group, at least one of R.sub.1 and R.sub.2 is not a methyl group.
5 more elements
Dependencies are inferred from the claim text.