Title:
【発明の名称】新規な骨作用剤
Document Type and Number:
Japanese Patent JPH0735395
Kind Code:
B2
Abstract:
Described are new agents for treating bone disorders associated with a reduction in bone mass and abnormalities in bone resorption or bone formation including osteoporosis, Paget's disease, bone metastases and malignant hypercalcemia. The agents are hydroxyl containing steroidal hormones, having bone resorption antagonist or bone formation stimulatory activity, covalently linked through the hydroxyl group via a bond hydrolyzable in the human body, e.g. carbamate or carbonate, which is further covalently linked to an amino, or hydroxy substituted alkylidene-1,1-bisphosphonate, through the respective amino or hydroxy group. The alkyl bisphosphonate moiety confers bone affinity. The agent acts by delivering the steroidal hormone directly to the bone target site where it is released for bone resorption antagonist or bone formation stimulatory action by hydrolysis of the hydrolyzable covalent bond.
Inventors:
Wolfred F. Saari
Gideon A. Rodin
Sauce ten fisher
Paul S. Anderson
Gideon A. Rodin
Sauce ten fisher
Paul S. Anderson
Application Number:
JP878692A
Publication Date:
April 19, 1995
Filing Date:
January 22, 1992
Export Citation:
Assignee:
Merck End-Campany Inc.
International Classes:
A61K31/56; A61K31/66; A61P3/00; A61P9/12; A61P19/10; A61P43/00; C07F9/40; C07J1/00; C07J51/00; (IPC1-7): C07J51/00; A61K31/56; A61K31/66; C07J1/00
Domestic Patent References:
| JP5973593A | ||||
| JP236145A | ||||
| JP58208232A | ||||
| JP6226256A | ||||
| JP2104593A | ||||
| JP63201197A | ||||
| JP5481255A | ||||
| JP6429314A | ||||
| JP1213296A |
Attorney, Agent or Firm:
Masao Okabe (5 others)
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