Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1997-12-30
1999-11-02
Powers, Fiona T.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
544353, A61K 31495, C07D40104
Patent
active
059771089
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to a heterocycle-containing carboxylic acid derivative and a drug containing said derivative.
BACKGROUND ART
Retinoic acid is an essential substance for the growth or life support of mammals including humans. It is known to have various effects, for example, upon ontogenesis, it serves as a morphogenetic factor, while in the adult body, it has effects on the differentiation and proliferation of cells. Described specifically, it is known to take part in the keratinization reaction, hair formation, sebaceous gland function or the like in the epidermis; the metabolism of bone or cartilage in the connective tissue; immunnomodulatory in the immune system; differentiation of neurocytes in the nerve system; differentiation and proliferation of hemocytes in the blood system; and lipid metabolism, mineral metabolism and basal metabolism. A wide variety of physiological effects of retinoic acid as exemplified above are exhibited by its various control mechanisms such as expression regulation of a transcription activator through an intranuclear retinoid receptor (RARs, RXRs) family, regulation of the hormone secretion or function at the target organ, regulation of growth factors such as EGF receptor or TGF.alpha., expression regulation of enzymes such as collagenase, tissue plasminogen activator or tyrosine kinase, and production regulation of cytokine such as IL-6.
In recent years, the relationship between these physiological effects of retinoic acid and various morbid conditions has come to be apparent. Particularly in some cancers typified by acute myelocytic leukemia, differentiation and induction treatment by using all-trans retinoic acid has drawn attentions as a novel therapeutic method of these cancers.
Retinoic acid, however, is found to involve various problems such as appearance of resistance caused by induction of P450 and expression of side effects due to its accumulation. Under such situations, there is accordingly a strong demand for the development of a novel retinoid-related compound, instead of retinoic acid, as a preventive and/or therapeutic for various diseases.
SUMMARY OF THE INVENTION
The present invention provides a heterocycle-containing derivative represented by the following formula ##STR2## wherein: A is a group represented by the following formula (i), (ii), (iii) or (iv): ##STR3## in which E.sup.1, F.sup.1, G.sup.1, H.sup.1, I.sup.1, E.sup.2, F.sup.2, G.sup.2, E.sup.3, F.sup.3 and G.sup.3 are the same or different and each independently represents an oxygen atom or a nitrogen, carbon or sulfur atom which may have a substituent; J represents a nitrogen atom which may have a substituent, with the proviso that the cases where in the ring (i), E.sup.1, F.sup.1, G.sup.1, H.sup.1 and I.sup.1 each represents a carbon group which may have a substituent, where in the ring (ii), E.sup.2, F.sup.2 and G.sup.2 each represents a carbon group which may have a substituent, and where in the ring (iii), E3, F.sup.3 and G.sup.2 each represents a carbon group which may have a substituent are excluded; R.sup.1, R.sup.2 and R.sup.3 are the same or different and each independently represents a hydrogen atom, a halogen atom, a lower alkyl group which may have a substituent, a cycloalkyl group which may have a substituent, a lower alkoxy group which may have a substituent, a cycloalkyloxy group which may have a substituent, an aryl group which may have a substituent, a heteroaryl group which may have a substituent, an aryloxy group which may have a substituent, a heteroaryloxy group which may have a substituent, a cycloalkylalkyl group which may have a substituent, an arylalkyl group which may have a substituent, a heteroarylalkyl group which may have a substituent, a cycloalkylalkyloxy group which may have a substituent, an arylalkyloxy group which may have a substituent, a heteroarylalkyloxy group which may have a substituent, an alkenyl group which may have a substituent or an alkynyl group which may have a substituent, or R.sup.1 and R.sup.2 are coupled to
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Abe Shinya
Hibi Shigeki
Hida Takayuki
Higashi Seiko
Kikuchi Kouichi
Eisai Co., Ltd
Powers Fiona T.
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