Bisphosphonate derivative
AssigneeHoechst Japan Limited
InventorsTatsuo Sugioka, Mizuho Inazu
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Abstract
A compound represented by the general formula: ##STR1## wherein A-O-denotes a residue of a compound having an estrogenic activity; R.sub.1 denotes H or a C.sub.1 -C.sub.6 alkyl group; X denotes a single bond, a C.sub.1 -C.sub.10 alkylene group or a group of the formula ##STR2## wherein R.sub.2 denotes H or a C.sub.1 -C.sub.5 alkyl group; Z denotes a nitro group or a halogen; n is an integer of 3 to 12; k is an integer of 1 to 5; L is an integer of 0 to 5; and q is an integer of 1 to 3, and physiologically acceptable salts thereof are disclosed. The compounds have a high affinity to bone tissues, and the compounds per se and metabolites thereof show significant therapeutic effect on bone diseases such as osteoporosis, rheumatoid arthritis and osteoarthritis.
Claims9
A compound represented by the formula 1 ##STR10## wherein A-O denotes a residue of a compound selected from the group consisting of estrone, estradiol, estriol and their derivatives, which binds to a bisphosphonate group at the 3-position of a steroidal group,
- R.sub.1 denotes H or a C.sub.1 -C.sub.6 alkyl group,
- X denotes a single bond or a C.sub.1 -C.sub.10 -alkylene group, and
- q denotes 1, or a physiologically acceptable salt thereof.
Dependencies are inferred from the claim text.