Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1997-05-05
1998-09-15
Berch, Mark L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
540501, 540554, C07D48704, C07D40106, C07D40912, A61K 3155
Patent
active
058078509
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to therapeutic agents for osteoporosis containing, as an active ingredient, a certain triazepine compound having superior inhibitory effect on bone resorption, novel triazepine compounds and intermediate compounds useful for producing such triazepine compounds.
BACKGROUND ART
Osteoporosis is a syndrome representing symptoms wherein bone mass per unit volume decreases abnormally without changes in chemical composition (proportion between organic substance and inorganic substance) of the bone itself, and is physiologically characterized by a decrease in the amounts of protein, calcium and phosphorus in the bone. The bone mass also decreases due to the physiological aging. Osteoporosis is defined to be a disease which shows greater degree of decrease in bone mass than that caused by physiological aging, and which is associated with clinical symptoms such as dorsolumbar pain, pathologic fracture and deformation of vertebral body.
Osteoporosis increases in number with aging and generally affects vertebra to cause dorsolumbar pain and shortened stature. In particularly advanced cases, long bone is also affected to sometimes cause fracture. The cause of the femoral fracture found in aged people is said to be mostly caused by senile osteoporosis. The cause of the osteoporosis is divergent and examples thereof include abnormal endocrine including menopause, nutritional disorder and so on.
The therapeutic agents for osteoporosis heretofor known are vitamin preparations, calcium preparations, calcitonin preparations, bisphosphonate preparations and isoflavone preparations. These therapeutic agents are not necessarily satisfactory from the aspects of side-effects and the method of use. Accordingly, there is a strong demand for the development of a therapeutic agent for osteoporosis which can exhibit ensured effects, which is highly safe and which can be used easily.
A recent report teaches the usefulness, as therapeutic agents for osteoporosis, of benzothiadiazine derivatives and benzothiadiazepine derivatives having completely different chemical structures from the above-mentioned preparations (Japanese Patent Unexamined Publication No. 183572/1989). The inventors of the present invention also found the bone resorption-inhibitory action of triazolobenzothiadiazine derivatives and triazolobenzothiadiazepine derivatives and filed the finding as a patent application (Japanese Patent Application No. 357369/1992). In addition, the present inventors have found the bone resorption-inhibitory action of the compounds having a diazepine skeleton and filed a patent application thereto (W093/07129). Yet, these compounds are not satisfactory in terms of activity and are faced with difficulties in that they cannot fully meet the above-mentioned requirements, that optical resolution is difficult due to the presence of asymmetric carbon in the compound, and that they are associated with practical problems caused by long production steps.
On the other hand, certain compounds having a triazepine skeleton have been reported to have anticonvulsive action, muscle-relaxing action, sedative action, anti-anxiety action and ataractic action. However, a bone resorption-inhibitory action thereof has not been reported (U.S. Pat. Nos. 4,144,233, 5,091,381, 3,891,666 and 3,880,878).
DISCLOSURE OF THE INVENTION
It is therefore an object of the present invention to provide a novel therapeutic agent for osteoporosis.
It is another object of the present invention to provide a novel compound useful as an active ingredient of a therapeutic agent for osteoporosis.
It is still another object of the present invention to provide an intermediate compound for producing a compound useful as an active ingredient of a therapeutic agent for osteoporosis.
It is further object of the present invention to provide a method for treating osteoporosis and use of triazepine compounds.
The present inventors have investigated and now found that a triazepine resorption, which resulted in the completion of the present inv
REFERENCES:
patent: 4094871 (1978-06-01), Trepanier
patent: 4144233 (1979-05-01), Brittan
patent: 4455307 (1984-06-01), Hester, Jr.
patent: 5593988 (1997-01-01), Tahara et al.
Richter, Pharmazie 46, 701-5 (1991).
P.H. Richter et al., "Synthese und Biologische Aktivitat von 5-phenyl-1,3,4-benzotriazepinen", Pharmazie vol. 46, No. 10, Oct. 1991, pp. 701-705.
Koga Yoshihisa
Nakamura Takeshi
Shindo Masanori
Berch Mark L.
Japan Tobacco Inc.
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