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US 5,508,392 AGranted
Use of vitamin D glycosides, vitamin D orthoester glycosides, vitamin D analog glycosides and vitamin D analog orthoester glycosides for the treatment of osteoporosis
OwnerMichael F. Holickinventor
Life of this patent
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Abstract
The present invention relates to methods for the treatment of prevention of osteoporosis by the administration of a vitamin D glycoside or vitamin D orthoester glycoside, or an analog thereof.
Claims6
A method for treating or preventing osteoporosis in an individual having osteoporosis or susceptible to osteoporosis without causing the side effects associated with the administration of 1,25-dihydroxyvitamin D.sub.3, comprising administering to said individual an effective amount of a compound having the formula:
- ##STR8## wherein the bond between C-22 and C-23 is a single bond or a double bond;
- Y.sup.2 is hydrogen, fluorine, methyl, ethyl or OR.sup.1 ;
- Z.sup.2 is F, H or X.sup.2 ;
- U is hydrogen, --OH or --O--(C.sub.2 -C.sub.4 alkyl)--OH;
- Q.sup.a is CF.sub.3 or CH.sub.2 X.sup.2 ;
- Q.sup.b is CF.sub.3 or CH.sub.3 ;
- R is a double bond or an epoxy group;
- X.sup.1 and X.sup.2 are selected from the group consisting of hydrogen and OR.sup.1 ;
- R.sup.1 is hydrogen or a straight or branched chain glycosidic residue containing 1-20 glycosidic units per residue, or R.sup.1 is an orthoester glycoside moiety of the formula:
- ##STR9## wherein A represents a glycothranosyl or glycopyranosyl ring;
- R.sup.2 is hydrogen, alkyl (C.sub.1 -C.sub.4), aralkyl (C.sub.7 -C.sub.10), or aryl, with the proviso that aryl is phenyl or phenyl substituted by chloro, fluoro, bromo, iodo, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy;
- or naphthyl;
- R.sup.3 is hydrogen or a straight or branched chain glycosidic residue containing 1-20 glycosidic units per residue;
- W is CH--CH.sub.3 or O:
- and
- V is CH.sub.2 or O;
- with the proviso that both W and V are not both O;
- and
- ".dbd..dbd..dbd." is either a single bond between Q.sup.a and Q.sup.b or a hydrogen atom on Q.sup.a and Q.sup.b,
- with the proviso that wherein ".dbd..dbd..dbd." is a single bond, then X.sup.2 is H;
- and
- with the further proviso that at least one of the R.sup.1 groups is either a .beta.-glycosidic residue or an orthoester .beta.-glycoside moiety.
19 more elements
Dependencies are inferred from the claim text.