Diaminomethylidene derivatives

Details Diaminomethylidene derivatives Diaminomethylidene derivatives

1996-11-07

1998-05-19

Shah, Mukund J.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

544105, 544121, 544162, A61K 31535, C07D26536, C07D41300, C07D26530

Patent

active

057536546

DESCRIPTION:

BRIEF SUMMARY
This is a 371 application of PCT/JP 95/00938 filed on May 17, 1995 published as WO95/31431 Nov. 23, 1995.
1. Technical Field
This invention relates to novel diaminomethylidene derivatives and pharmacologically acceptable acid addition salts and quaternary ammonium salts thereof.
More specifically, this invention relates to new diaminomethylidene derivatives having a promoting action of the release of acetylcholine in digestive tracts, thus being useful for the treatment of digestive tract disorders derived from chronic gastritis, diabetes mellitus, post-gastrectomy and peptic ulcer and digestive tract diseases including reflux esophagitis, irritable bowel syndrome and spurious ileus, as well as a gastrointestinal prokinetic agent which comprises as an active ingredient the said derivatives.
2. Background Art
The abnormality in function of a gastrointestinal mobility by various causes such as chronic gastritis, diabetes, post-gastrectomy, peptic ulcer and others could result in the reflux of the gastric content into the esophagus, delayed emptying of the gastric content and the depressed function of the small and large intestines.
This can lead to appearances of nausea, vomiting, heartburn, anorexia, abdominal distention, epigastric dysphoria, abdominaglia, constipation and further reflux esophagitis. One cause of the diseases such as irritable bowel syndrome and spurious ileus has been considered to be the depression in gastrointestinal motility.
The agents for the treatment of these conditions and diseases include direct cholinergic agent (e.g. Aclatonium Napadisilate) or Dopamine antagonist (e.g. Doperidone). However, it is well-known that these known agents have the problems in their effects and side-effects, which may include, for example, diarrhea and extrapyramidal syndrome.
It is well-known that acetylcholine is the neurotransmitter participating in the control of gastrointestinal motility. Accordingly, it may be considered that a compound capable of promoting the release of acetylcholine in digestive tract may be a gastrointestinal prokinetic agent showing far more effectiveness and less side effects. In view of this, it has been desired to find out such a type of compounds and develop a process for obtaining them.


DISCLOSURE OF INVENTION

The present inventors have made earnest studies to solve these problems and, as a result, have found that the diaminomethylidene derivatives as defined below can exert a remarkable promoting action of the release of acetylcholine, upon which this invention has been completed.
More particularly, this invention is concerned with a diaminomethylidene derivative represented by formula (I) ##STR3## wherein R.sup.1 is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group, a C.sub.3 -C.sub.6 cycloalkyl group, a C.sub.3 -C.sub.6 cycloalkyl C.sub.1 -C.sub.4 alkyl group, an aryl group or an aryl C.sub.1 -C.sub.4 alkyl group, in which the aryl moiety of the aryl group or aryl C.sub.1 -C.sub.4 alkyl group may be optionally substituted with a halogen atom, a C.sub.1 -C.sub.6 alkyl group, a halo C.sub.1 -C.sub.6 alkyl group, a C.sub.1 -C.sub.6 alkoxy group, a C.sub.1 -C.sub.6 alkoxycarbonyl group, a phenyl group or an amino group, in which R.sup.4 is a C.sub.1 -C.sub.6 alkyl group, a C.sub.3 -C.sub.6 cycloalkyl group, an aryl group, or an aryl C.sub.1 -C.sub.4 alkyl group, ##STR4## wherein R.sup.5 is a C.sub.1 -C.sub.6 alkyl group, an aryl C.sub.1 -C.sub.4 alkyl group, a heteroaryl C.sub.1 -C.sub.4 alkyl group, an aryloxy C.sub.2 -C.sub.6 alkyl group, or a pyrrolidinylcarbonyl C.sub.1 -C.sub.4 alkyl group, in which the aryl moiety of the said groups may be optionally substituted with a halogen atom, a C.sub.1 -C.sub.6 alkyl group, a halo C.sub.1 -C.sub.6 alkyl group, a C.sub.1 -C.sub.6 alkoxy group, a C.sub.1 -C.sub.6 alkoxycarbonyl group, a phenyl group or an amino group, or an aryl C.sub.1 -C.sub.4 alkyl group, Z.sup.3 is N or CH, l is 0-2, n is 4 when m is 0, n is 1 or 3 when m is 1, n is 2 when m is 2, p is 1-2, j is 0-3, k is 0-3, a sum of j and k is 1-6, h is 1-6, atom, a C.

REFERENCES:
patent: 3585142 (1971-06-01), Muzyczko et al.
patent: 5422373 (1995-06-01), Franzmann
patent: 5621010 (1997-04-01), Sueda et al.

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