Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1999-05-06
2000-09-19
Huang, Evelyn Mei
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514337, 514339, 514342, 514369, A61K 314709, A61K 31427, A61K 31426, A61P 304
Patent
active
061212881
DESCRIPTION:
BRIEF SUMMARY
[FIELD OF THE INVENTION]
This invention relates to medicinal compositions for inhibiting visceral fat accumulation (which is now understood to cause diseases such as hypertension, diabetes, hyperlipemia, and arteriosclerosis), for decreasing visceral fat, and for improving body fat distribution. In particular, the invention relates to a visceral fat decreasing agent, a visceral fat accumulation inhibitor, and a body fat distribution improver each of which comprises a thiazolidine or oxazolidine derivative as the active ingredient.
[BACKGROUND OF THE INVENTION]
Recently, the relationship between diseases and the body fat distribution has been studied. According to the study, even in a non-obese person as well as an obese person, visceral fat accumulation in the abdominal cavity (particularly, in the mesentery and/or in the greater omentum) positively correlates with values of serum cholesterol, triglyceride, and blood glucose measured by the glucose tolerance test. Further, the visceral fat accumulation also positively correlates with the systolic and diastolic blood pressures, and accordingly it highly relates to diseases such as hypertension, diabetes, and hyperlipemia [Fujioka, S., et al. Metabolism, 36 54-59, 1987; Matsuzawa, Y., et al. Progress in Obesity Research, 309-312, 1990]. These diseases are, therefore, thought to be cured or prevented by decreasing visceral fat, by inhibiting visceral fat accumulation, or improving body fat distribution [Bray, G. A., Obesity Research, 3, Suppl. 4, 425S-434S, 1995].
For decreasing body fat, treatments such as ergo-therapy, diet, behavior therapy, and pharmacotherapy are practically employed. In the pharmacotherapy, an anorectic agent working on the central nervous system is employed, and a .beta..sub.3 -adrenergic receptor stimulant and a fat absorption inhibitor have been developed. However, these so-called "anti-obesity drugs" are not thought to be effective for decreasing visceral fat, and hence there is no effective pharmacotherapy for decreasing visceral fat.
The relationship between insulin sensitivity and body fat distribution has been also studied, and it suggests that insulin sensitivity is caused by the visceral fat accumulation. Accordingly, it is commonly understood that visceral fat accumulation causes the above-mentioned diseases accompanied by insulin sensitivity or independently thereof.
Thiazolidine derivatives which improve insulin sensitivity are already known to effectively serve as blood glucose depressors or blood lipid depressors [Japanese Patent Provisional Publications No. 61(1986)-267580 and No. 60(1985)-51189, and WO 96/12719]. On the other hand, however, some of these derivatives are reported to promote appetite and increase the body weight. Further, it is also reported that they increase brown adipocyte in rodents and promote the differentiation of preadipocyte into adipocyte in vitro. In view of those reports, the thiazolidine derivatives are generally believed to rather increase the body fat.
Accordingly, although the relationship between insulin sensitivity and visceral fat accumulation is noticed, no insulin sensitizer serving for decreasing visceral fat has been developed.
[DISCLOSURE OF THE INVENTION]
The inventors studied on thiazolidine or oxazolidine derivatives improving insulin sensitivity, and surprisingly found that some of these derivatives also decrease visceral fat, inhibit visceral fat accumlation, and improve body fat distribution.
It is an object of the present invention to provide a visceral fat decreasing agent, a visceral fat accumulation inhibitor and a body fat distribution improver each of which comprises a thiazolidine or oxazolidine derivative as an active ingredient.
The present invention resides in a visceral fat decreasing agent which comprises as an active ingredient a compound of the following formula (I): heterocyclic group; X.sup.1 represents a bond, an oxygen atom, a sulfur atom, or N(R.sup.1) in which R.sup.1 is a hydrogen atom, an alkyl or aralkyl group; B.sup.1 represents an optionally su
REFERENCES:
patent: 4572912 (1986-02-01), Yoshioka
patent: 4687777 (1987-08-01), Meguro
Yamashita S et al. Diabetes Care. 19 (3) 287-91, Mar. 1996.
Masui Seiichiro
Nakano Yoshihisa
Huang Evelyn Mei
Nippon Chemiphar Co., Ltd.
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