Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1995-05-18
1997-09-30
Gulakowski, Randy
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514212, 514213, 514217, 514277, 514279, 514280, 514299, 514332, 514333, 514335, 514343, 514344, 514345, 514359, 514613, 514616, 514927, 546196, 546198, 546208, 546270, 546272, 546283, 546285, 546286, A01N 4300, A61K 3155, C07D40100
Patent
active
056725973
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention, which relates to a novel acetamide derivative having both of an inhibition of gastric acid secretion and a potentiation of defensive factor, is a useful invention in the medicinal field.
BACKGROUND ART
Peptic ulcer occurs owing to ill-balance between offensive factors such as gastric acid and pepsin, and defensive factors such as gastric mucus and mucosal blood flow. In particular, gastric acid is considered to take part in it importantly. Therefore, there are now widely used offensive factor inhibitors, for example, histamine H.sub.2 -receptor blockers having particularly potent inhibition of gastric acid secretion, such as cimetidine and famotidine. However, there is a problem in the use of histamine H.sub.2 -receptor blockers such as recrudescence or relapse of the ulcer after breaking the use thereof. It is considered that such problem occurs mainly due to defensive factors such as gastric mucosa, which are weakened by the potent inhibition of gastric acid secretion. So, there has been desired the development of a medicament having both of an inhibition of gastric acid secretion and a potentiation of defensive factor. As such medicaments, there are described, for example, compounds having pyridine ring in Japanese Unexamined Patent Publication No. 225371/1988, U.S. Pat. Nos. 4,912,101 and 4,977,267. However, there has not yet been known any compound which satisfactorily possesses both of the above-mentioned inhibition of gastric acid secretion and potentiation of defensive factor.
The object of the present invention is to provide a novel compound effective for preventing and treating peptic ulcer and gastritis, which not only has both of potent inhibition of gastric acid secretion and potentiation of defensive factor, but also has an accelerating effect for curing chronic ulcer.
DISCLOSURE OF THE INVENTION
Acetamide derivatives of the present invention are an acetamide derivative having the general formula (I): ##STR2## wherein each of R.sup.1 and R.sup.2 is a C.sub.1-7 alkyl group, or R.sup.1 and R.sup.2 together form the formula --(CH.sub.2).sub.m -- wherein m is 4 to 6, C.sub.1-4 alkoxy group, nitro group, amino group, cyano group, carboxyl group or acetyl group, which may be substituted for any hydrogen atom of the ring, R.sup.5 and R.sup.6 is hydrogen atom; a C.sub.1-7 alkyl group; a C.sub.2-6 alkenyl group; a C.sub.2-6 alkynyl group; a C.sub.1-4 alkoxy C.sub.1-7 alkyl group; a C.sub.1-5 acyloxy C.sub.1-7 alkyl group; a C.sub.7-16 aralkyl group; a phenyl or a heterocyclic group which may be substituted by a C.sub.1-7 alkyl group, a halogen atom, a C.sub.1-4 alkoxy group, nitro group, trifluoromethyl group, amino group, cyano group, carboxyl group or acetyl group; a C.sub.1-7 alkyl group substituted by a heterocycle, which is a synthetic intermediate of the above-mentioned acetamide derivative, having the general formula (VIII): ##STR3## wherein each of R.sup.1 and R.sup.2 is a C.sub.1-7 alkyl group, or R.sup.1 and R.sup.2 together form the formula --(CH.sub.2).sub.m -- wherein m is 4 to 6, C.sub.1-4 alkoxy group, nitro group, amino group, cyano group, carboxyl group or acetyl group, which may be substituted for any hydrogen atom of the ring,
The present invention also relates to an aminoethanethiol derivative having the general formula (XX): ##STR4## wherein R.sup.7 is hydroxyl group, a C.sub.1-7 alkoxy group, or a phenoxy group which may be substituted, R.sup.5 and R.sup.6 is hydrogen atom; a C.sub.1-7 alkyl group; a C.sub.2-6 alkenyl group; a C.sub.2-6 alkynyl group; a C.sub.1-4 alkoxy C.sub.1-7 alkyl group; a C.sub.1-5 acyloxy C.sub.1-7 alkyl group; a C.sub.7-16 aralkyl group; a phenyl or a heterocyclic group which may be substituted by a C.sub.1-7 alkyl group, a halogen atom, a C.sub.1-4 alkoxy group, nitro group, trifluoromethyl group, amino group, cyano group, carboxyl group or acetyl group; a C.sub.1-7 alkyl group substituted by a heterocycle, of which comprises the above-mentioned compound having the general formula (I) or a salt thereof as an
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Chemical Abstracts, vol. 92, No. 12, Abstract No. 103527f, p. 636, col. R.
Fujii Masahiro
Hata Yoshiyuki
Hayashida Mitsuo
Ishiyama Nobuo
Kimura Kunio
Gulakowski Randy
Kaken Pharmaceutical Co. Ltd.
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