Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1994-12-06
1996-05-28
Gerstl, Robert
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
544322, 5462697, 5462707, 5462714, 548183, C07D41712, A61K 31425
Patent
active
055212026
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/JP94/00590 filed 4/7/94.
TECHNICAL FIELD
The present invention relates to novel thiazolidine derivatives and salts thereof. More specifically, this invention relates to thiazolidine derivatives or salts thereof which have blood-sugar lowering action and blood-lipid lowering action and are useful as hypoglycemic agents and anti-hyperlipidemia agents, preparation processes thereof, pharmaceutical compositions containing one or more of the compounds and therapeutic methods for diabetes.
BACKGROUND ART
As synthetic therapeutic agents for diabetes which show blood-sugar lowering action, sulfonylurea preparations have commonly been used to date. Their use, however, requires very careful control because they may cause hypoglycemic symptoms or induce drug resistance. In recent years, development of hypoglycemic agents is therefore under way as substitutes for the above sulfonyl urea preparations. Among them, interested are those capable of enhancing the insulin sensitivity at peripheries and showing blood-sugar lowering action.,
Effects available from these agents, however, are still not satisfactory and moreover, their side effects cannot be considered to have been reduced fully. Further, as there are many diabetics who have also developed hyperlipidemia, there is an outstanding demand for the development of pharmaceuticals having both blood-sugar lowering action and blood-lipid lowering action.
DISCLOSURE OF THE INVENTION
In view of the foregoing circumstances, the present inventors have carried out an extensive investigation. As a result, it has been found that certain novel, specific thiazolidine derivatives and salts thereof have both the above actions, leading to the completion of the invention.
The present invention therefore provides a thiazolidine derivative represented by the following formula (1): ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 may be the same or different and individually represent a hydrogen atom, a halogen atom, a lower alkyl group or lower alkoxyl group which may be substituted by one or more halogen atom(s), a hydroxyl group, a nitro group, an amino group, a lower acylamino group, a mono- or di-lower alkylamino group, a carboxyl group, a lower alkoxycarbonyl group, a cyano group, a 2-oxazolyl group, a thiazolidine-2,4-dion-5-ylidene-methyl group or a thiazolidine-2,4-dion-5-ylmethyl group and R.sup.1 and R.sup.2 may be coupled together to form an alkylene chain --(CH.sub.2).sub.p -- wherein p stands for 3, 4 or 5 or an alkylenedioxy chain --O(CH.sub.2).sub.q O-- wherein q stands for 1, 2 or 3, thereby forming a ring; R.sup.4 and R.sup.5 may be the same or different and individually represent a hydrogen atom or a lower alkyl group; X represents a carbon atom or nitrogen atom; Y represents an oxygen atom or an imino group; A and B individually represent a lower alkylene group; m stands for 0 or 1; and the dashed line indicates the presence or absence of a double bond; or a salt thereof and a preparation process thereof.
In addition, the present invention provides a pharmaceutical composition which comprises an effective amount of the thiazolidine derivative (1) or a salt thereof and a pharmacologically acceptable carrier.
Further, the present invention provides a method of treatment of diabetes which comprises administering to patients an effective amount of the thiazolidine derivative (1) or a salt thereof.
Each thiazolidine derivative or a salt thereof according to the present invention has excellent blood-sugar lowering action and blood-lipid lowering action. It has good absorption into the body and has long lasting drug efficacy. In addition, it has excellent excretion and low toxicity against the human body, so that it is useful as pharmaceuticals such as a diabetes treating agent, a hyperlipidemia treating agent, an arteriosclerosis preventive and treating agent, and an obesity preventive drug.
BEST MODES FOR CARRYING OUT THE INVENTION
The thiazolidine derivatives represented by the formula (1) have optical isomers. It is to be noted t
Fukushima Masakazu
Ogawa Kazuo
Yano Shingo
Gerstl Robert
Taiho Pharmaceutical Co. Ltd.
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