Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1999-04-21
2000-09-19
Gerstl, Robert
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
548195, C07D27756, A61K 31425
Patent
active
061213012
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to a novel benzoylaminothiazole derivative having improving effects on the dysmotility in the gastrointestinal tract, a medicament containing the derivative and an intermediate for preparing said compound.
BACKGROUND ART
As a therapeutic agent for gastrointestinal dysmotility, dopamine antagonists such as domperidone and metoclopramide, opioate agonists such as trimebutine maleate, 5-HT.sub.3 antagonists 5-HT.sub.4 agonists such as cisapride, acetylcholine agonists such as acetylcholine chloride and the like have conventionally been provided for clinical use. In addition to them, a number of prokinetics have been studied with a view to treating gastrointestinal dysmotility (Japanese Patent Applications Laid-Open Nos. HEI 1-313424, HEI 3-163074 and HEI 4-279581).
These agents, however, do not always bring about sufficient effects for the improvement of dysmotility. There is a potential problem that side effects may possibly occur owing to the acting mechanism of the agent even if it has sufficient effects. So, the above-described agents are not completely satisfactory. Accordingly, there has been a demand for the development of a medicament having excellent improving effects on gastrointestinal dysmotility and having less side effects.
DISCLOSURE OF THE INVENTION
With the foregoing in view, the present inventors have carried out an extensive investigation. As a result, it has been found that a specific benzoylaminothiazole derivative has excellent improving effects on gastrointestinal dysmotility, has less side effects and is therefore useful as a medicament, leading to the completion of the present invention.
The present invention therefore provides a substituted benzoylaminothiazole derivative represented by the following formula (I): ##STR2## wherein X represents an imino group which may be substituted by a lower alkyl group, or an oxygen atom, R.sup.1 represents a cyano group, a lower alkoxycarbonyl group, a lower alkoxycarbonylamino group, a lower alkylsulfonylamino group, a lower alkanoyl or lower alkylsulfonyl group which may be substituted by a halogen atom, a 1-ureido group, a halo-substituted lower alkyl group or a 2-pyrrolylimino group, R.sup.2 and R.sup.3 are the same or different and each independently represents a hydrogen atom or a lower alkyl group and m stands for an integer of 2 to 4; or a salt thereof.
The present invention also provides a medicament comprising as an effective ingredient the above-described substituted benzoylaminothiazole derivative (I) or salt thereof.
The present invention further provides a preventive and therapeutic agent for gastrointestinal dysmotility, which comprises as an effective ingredient the above-described substituted benzoylaminothiazole derivative (I) or salt thereof.
The present invention still further provides a preventive and therapeutic agent for epigastric dyscomfort, nausea, vomiting, heart burn, anorexia, bellyache, abdominal flatulence, chronic gastritis, reflux esophagitis, postgastrectomy syndrome or the like, which comprises as an effective ingredient the above-described substituted benzoylaminothiazole derivative (I) or salt thereof.
The present invention still further provides a pharmaceutical composition comprising the above-described substituted benzoylaminothiazole derivative (I) or salt thereof and a pharmaceutically acceptable carrier.
The present invention still further provides the use of the above-described substituted benzoylaminothiazole derivative (I) or salt thereof as a medicament.
The present invention still further provides a method for preventing or treating gastrointestinal dysmotility, which comprises administering an effective amount of the above-described substituted benzoylaminothiazole derivative (I) or salt thereof to mammals including human.
The present invention still further provides a thiazole derivative represented by the following formula (II): ##STR3## wherein R.sup.1 has the same meanings as described above, and Y represents a hydroxy or a lower alkoxy group
REFERENCES:
patent: 4829073 (1989-05-01), Gidda et al.
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patent: 5510478 (1996-04-01), Sabb
patent: 5712270 (1998-01-01), Sabb
patent: 5981557 (1999-09-01), Nagasawa
Kurimoto Tadashi
Nagasawa Masaaki
Sato Kenji
Ueki Shigeru
Gerstl Robert
Zeria Pharmaceutical Co. Ltd.
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