Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1997-11-18
1999-11-09
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
059815574
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to a novel aminothiazole 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 is 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 forgoing in view, the present inventors have carried out an extensive investigation. As a result, it has been found that a specific aminothiazole derivative has excellent improving effects on gastrointestinal dysmotility and also has less side effects, leading to the completion of the present invention.
The present invention therefore provides an aminothiazole derivative represented by the following formula (I): ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are the same or different and each independently represents a hydrogen atom, a hydroxy group, a lower alkyl group, a lower alkoxy group, a lower alkylcarbonyloxy group, a halogen atom, a nitro group, an amino group, a mono- or di-(lower alkyl)amino group, a mono- or di-(lower alkyl)carbonylamino group, a formylamino group, a mono- or di-(lower alkyl)aminoalkylamino group, or R.sup.1 and R.sup.2 may be coupled together to form a methylenedioxy group; R.sup.4 represents a hydrogen atom or a lower alkyl group; R.sup.5 represents a hydrogen atom, a halogen atom or a lower alkyl group; A represents a group represented by the following formula: ##STR3## wherein R.sup.6 and R.sup.7 are the same or different and each independently represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a hydroxy(lower alkyl) group, a carboxy(lower alkyl) group, a (lower alkoxy)carbonyl(lower alkyl) group, a lower alkoxyalkyl group, a mono- or di-(lower alkyl)aminoalkyl group, a phenylalkyl group which may be substituted with one or two lower alkoxy groups on the benzene ring, a saturated or unsaturated nitrogen-containing heterocyclic group which may be substituted by a lower alkyl group, or R.sup.6 and R.sup.7, together with an adjacent nitrogen atom, form a saturated or unsaturated nitrogen-containing heterocyclic group which may be substituted by an oxo group (O.dbd.) or 1 to 3 lower alkyl or hydroxy(lower alkyl) groups, or a group represented by the following formula: ##STR4## wherein R.sup.8 and R.sup.9 are the same or different and each independently represents an amino group, a mono- or di-(lower alkyl)amino group, a mercapto group or a lower alkylthio group, or R.sup.8 and R.sup.9, together with the adjacent carbon atom, form a nitrogen-containing heterocyclic group; and B represents an imino group which may be substituted by a lower alkyl group or an oxygen atom; and m stands for an integer of 0 to 4; B--(CH.sub.2).sub.m --A may form a piperidinyl, branched alkylamino or phenylamino group which may be substituted by a mono- or di-(lower alkyl)amino group, or a piperazinyl, piperidinylamino or piperidinylalkylamino group which may be substituted by a lower alkyl group, or a salt thereof.
The present invention also provides a medicament comprising as
REFERENCES:
patent: 5510478 (1996-04-01), Sabb
patent: 5712270 (1998-01-01), Sabb
Kitagawa Osamu
Kurimoto Tadashi
Murata Masakazu
Nagasawa Masaaki
Nishioka Hiroyasu
Gerstl Robert
Zeria Pharmaceutical Co. Ltd.
LandOfFree
Aminothiazole derivative, medicament containing the same, and in does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Aminothiazole derivative, medicament containing the same, and in, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Aminothiazole derivative, medicament containing the same, and in will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-1456485