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US 6,121,253 AGranted
Prostaglandin conjugates for treating or preventing bone disease
AssigneeMerck Frosst Canada, Inc.
InventorsYongxin Han, Robert N. Young, Laurent Gil, Rejean Ruel
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Abstract
This invention relates to prostaglandin-bisphosphonate conjugates. These conjugates are effective for treating or preventing bone diseases such as osteoporosis. These conjugates simultaneously deliver a prostaglandin agent for increasing bone formation and a bisphosphonate agent for inhibiting bone resorption.
Claims18
A compound selected from the group consisting of:
- ##STR21## and mixtures thereof and the pharmaceutically acceptable salts thereof, wherein:
- A is a dioxygenated cyclopentane moiety selected from the group consisting of:
- ##STR22## X is selected from the group consisting of:
- ##STR23## Y is selected from the group consisting of:
- ##STR24## R.sup.1 is selected from the group consisting of H, C1-C10 alkyl, and Si(CH.sub.3).sub.2 tBu;
- R.sup.2 is selected from the group consisting of H and C.sub.1-10 alkyl;
- R.sup.3 is selected from the group consisting of H, tetrahydropyran, and Si(CH.sub.3).sub.2 tBu;
- R.sup.4 and R.sup.5 are independently selected from the group consisting of H, C1-C10 alkyl, phenyl, benzyl, C1-C10 alkoxy, and CF.sub.3,
- and n is an integer from 0 to 5.
6 more elements
A compound of the formula:
- ##STR25## and mixtures thereof and the pharmaceutically acceptable salts thereof, wherein:
- A is a dioxygenated cyclopentane moiety selected from the group consisting of:
- ##STR26## X is selected from the group consisting of:
- ##STR27## R.sup.1 is selected from the group consisting of H, C1-C10 alkyl, and Si(CH.sub.3).sub.2 tBu;
- R.sup.2 is selected from the group consisting of H and C.sub.1-10 alkyl;
- R.sup.3 is selected from the group consisting of H, tetrahydropyran, and Si(CH.sub.3).sub.2 tBu;
- R.sup.4 and R.sup.5 are independently selected from the group consisting of H, C1-C10 alkyl, phenyl, benzyl, C1-C10 alkoxy, and CF.sub.3,
- and n is an integer from 0 to 5.
5 more elements
Dependencies are inferred from the claim text.