Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1995-04-25
1997-03-18
Glass, Margaret W.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514339, 514406, 5462757, 5462767, 546176, 546159, 546 77, 5483585, 548149, 548242, 548426, 548181, 549 42, 549457, 544331, 544372, 544131, 544140, A61K 31415
Patent
active
056123566
DESCRIPTION:
BRIEF SUMMARY
BACKGROUND OF THE INVENTION
Field of the Invention
The present invention relates to heterocycle-containing carbonic acid derivatives and intermediates used for the production of the heterocycle-containing carbonic acid derivatives. More particularly, the present invention relates to novel heterocycle-containing carbonic acid derivatives which exhibit an excellent preventive or therapeutic effect against various diseases.
Description of the Related Art
Retinoic acid (vitamin A acid) is a substance essential for the growth and life-preservation of human beings and other mammals. It is known that this acid acts as a morphogenic factor in the ontogenesis and also variously acts on the differentiation and multiplication with respect to the adults. For example, it is known that the acid participates in cornification, formation of hair or function of sebaceous gland with respect to the epidermis; in the metabolism of bone and cartilage with respect to the connective tissue; in the regulation of immune function with respect to the immune system; in the differentiation of nerve cell with respect to the nervous system; in the differentiation and multiplication of blood cell with respect to the blood system; and in the secretion of thyroid and parathyroid hormones and the function thereof in target organs. Thus, retinoic acid is a substance which much participates in the mineral and basal metabolism. These various physiological activities of retinoic acid are exhibited by directly controlling the gene expression through a retinoid receptor family (RAR.sub.S, RXR.sub.S) present in the nucleus of a cell. With respect to retinoid acid, there have been known not only hypovitaminosis but also hypervitaminosis such as cornification disorder, alopecia and metabolic disorder of bone and cartilage. Further, it has recently been reported that the disorder of retinoid receptor is found in acute promyelocytic leukemia, squamous cell carcinoma of the head and neck, pulmonary carcinoma and so on, i.e., the disorder thereof participates in the sideration and evolution of these diseases. Under these circumstances, the development of a compound antagonistic to retinoids is believed to contribute to the elucidation of detailed mechanism of these various activities of retinoids and the investigation of clinical applicability thereof. Up to this time, TD-550, TD-560 and Ro41-5253 have been known as compounds antagonistic to retinoids [see Cell Biol. Rev., 25, 209 (1991), and Proc. Natl. Acad. Sci. USA., 89, 7129 (1992)]. However, these compounds are thought to be poor in the RARs-binding power and the antagonism against retinoids.
DISCLOSURE OF THE INVENTION
Summary of the Invention
In view of the above problem, the present inventors have extensively studied and have found that the heterocycle-containing carbonic acid derivatives which will be described below have an extremely high RARs-binding power and exhibit potent antagonism against retinoids. The present invention has been accomplished on the basis of this finding.
Thus, the present invention relates to a compound, i.e., a heterocycle-containing carbonic acid derivative, represented by the following general formula (I) or a physiologically acceptable salt thereof: ##STR2## wherein
the ring D represents a group represented by the following formula: ##STR3## [wherein R.sup.1 and R.sup.2 may be the same or different from each other and each represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a cycloalkyloxy group which may have a substituent, a halogen atom, an aryl group which may have a substituent, an aryloxy group which may have a substituent or a heteroaryl group which may have a substituent, or alternatively R.sup.1 and R.sup.2 together form a 5- to 7-membered cycloalkyl ring which is substituted with one or more lower alkyl groups or a 5- to 7-membered saturated heterocycle containing S, O, SO, SO.sub.2 or NR.sup.3 (wherein R.sup.3 represents a hydrogen atom or a lower alkyl group) as the hereto atom which is substituted with one or more lower alkyl g
REFERENCES:
patent: 3119819 (1964-01-01), Robinson et al.
patent: 4874747 (1989-10-01), Shroot et al.
patent: 5004730 (1991-04-01), Philippe et al.
patent: 5061705 (1991-10-01), Wuest et al.
patent: 5397785 (1995-03-01), Ninomiya et al.
Asada Makoto
Hibi Shigeki
Hida Takayuki
Hishinuma Ieharu
Kikuchi Koichi
Eisai Co. Ltd.
Glass Margaret W.
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