Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai
Patent
1995-11-13
1996-10-15
Henley, III, Raymond
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Cyclopentanohydrophenanthrene ring system doai
A61K 3156
Patent
active
055654444
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/JP94/00798 filed May 18, 1994.
TECHNICAL FIELD
The present invention relates to a novel osteogenesis promoter and also to an osteoporosis remedy.
Background Art
In recent years, the incidence of osteoporosis has shown a drastic increase keeping step with the aging of population and accordingly, fractures of the femoral neck or the like caused by osteoporosis have increased, posing an increasing threat to our health.
Osteoporosis is a condition in which the bone mass decreases while the components of the bone are kept normal, and is distinguished from a normal phenomenon of aging. What is troublesome is, however, that when osteoporosis advances to a certain extent or further, it becomes difficult for the patient to support his or her own weight, developing problems such as lower back pains, the vertebral column deformation and moreover, susceptibility to fractures at various body parts by light impact.
The condition called "osteoporosis" refers to a condition or syndrome caused by various causes and appears as one of symptoms of various diseases.
It is said that particularly, women tend to suffer from osteoporosis because a drastic decrease occurs in their bone quantities after menopause. Specifically, osteoporosis is considered to be induced by the deficiency of estrogen.
Bones protect the human body from external force and support the body as fulcrums for muscles, so that they are always exposed to physical forces such as pressure, tension and the like. To bear such physical forces is the significance of the existence of bones. It is accordingly presumed that without such physical stimuli, bones lose even their strength in addition to a drastic decrease in mass, resulting in the occurrence of osteoporosis. In short, a reduction in the bone mass is caused when physical stimuli to bones are lost. Osteoporosis characterized by such a cause is called immobilized osteoporosis.
Osteoporosis is, on the other hand, considered to be a representation of calcium dysbolism as one aspect of aging phenomena. Bones amount to 99% of the calcium in the whole body, which means that a decrease in the bone mass leads to a decrease in the calcium of the whole body. The continued deficiency of calcium with aging exasperates the secretion of parathyroid hormones, reduces the bone mass owing to an advance in the bone resorption and causes deposition of bone-released calcium in soft tissues, especially, in blood vessels and the cerebrum, which in turn induces osteoporosis, hypertension, arteriosclerosis, or senile dementia. Osteoporosis is therefore not only a disease of bones but also a representation of aging of the human body and of calcium dysbolism accompanied therewith and is also said to be an index showing in vivo abnormal calcium distribution.
Accordingly, the importance of osteoporosis lies in that because it becomes an index of various diseases of old age and represents the extent of calcium deficiency, the prevention of osteoporosis and the normalization of calcium metabolism conversely lead to the prevention of aging and also diseases of old age.
Examples of osteoporosis remedies clinically used now include calcium preparations, vitamin D derivatives, calcitonin, ipriflavone and the like. These preparations have as their principal effect the control of bone resorption. For postmenopausal osteoporosis, estrogen preparations are administered. Their effect is based on the acting mechanism of controlling an exasperation in bone resorption which is accompanied with a high bone turnover.
In senile osteoporosis, immobilized osteoporosis and glucocorticoid-induced osteoporosis, on the other hand, lowered bone formation is a serious morbid condition. In Europe and America, sodium fluoride was administered as an ostogenesis promoter for such lowered bone formation. It has, however, many adverse effects and therefore is not be used frequently these days.
An anabolic steroid was once used for osteoporosis in view of the report that it promotes bone formation. The above steroid, however, has
REFERENCES:
patent: 3741990 (1973-06-01), Nelson
patent: 5183815 (1993-02-01), Saari et al.
Derwent abstract of NL 6407296. 1964.
Mizushima Yutaka
Suzuki Yasuo
Henley III Raymond
LTT Institute Co., Ltd.
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