Furylthiazoles and their use as H.sub.2 - receptor antagonists a

Details Furylthiazoles and their use as H.sub.2 - receptor antagonists a Furylthiazoles and their use as H.sub.2 - receptor antagonists a

1994-01-28

1996-04-30

Gerstl, Robert

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514342, 546280, 548139, 548193, 548194, G07D41704, A61K 31425

Patent

active

055125883

DESCRIPTION:

BRIEF SUMMARY
This application is a 371 of PCT/JP92/00986 filed Aug. 3, 1992.


TECHNICAL FIELD

This invention relates to new furylthiazole derivatives and pharmaceutically acceptable salts thereof.
More particularly, it relates to furylthiazole derivatives and pharmaceutically acceptable salts thereof which have antiulcer activity, H.sub.2 -receptor antagonism and antimicrobial activity, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the treatment of ulcer and infectious diseases in human being or animals.


BACKGROUND ART

In European Patent Application Publication No. 355,612, there are disclosed furylthiazole derivatives having antiulcer activity and H.sub.2 -receptor antagonism.


DISCLOSURE OF THE INVENTION

One object of this invention is to provide new furylthiazole derivatives and pharmaceutically acceptable salts thereof which possess antiulcer activity, H.sub.2 -receptor antagonism and antimicrobial activity.
Another object of this invention is to provide processes for the preparation of said furylthiazole derivatives and salt thereof.
A further object of this invention is to provide a pharmaceutical composition comprising, as an active ingredient, said furylthiazole derivatives or pharmaceutically acceptable salts thereof.
Still further object of this invention is to provide a therapeutical method for the treatment of ulcer and infectious diseases in human being or animals.
The furylthiazole derivatives of this invention are new and can be represented by the following general formula (I): ##STR2## wherein R.sup.1 is methyl, ethyl, propyl, butyl, hexyl, lower alkoxy(lower)alkyl, lower alkenyl, lower alkynyl, cyclo(lower)alkyl, heterocyclic(lower)alkyl or hydroxy(lower)alkyl, amino, heterocyclic group, or a group of the formula: ##STR3## in which n is 0 or 1, X is .dbd.CH-- or .dbd.N--, which may have suitable substituent(s), and ##STR4## in which n, X, R.sup.5 and R.sup.6 are each as defined above.
The object compound (I) or a salt thereof can be prepared by processes as illustrated in the following reaction schemes. ##STR5## wherein as defined above, alkyl,
In the above and subsequent descriptions of the present specification, suitable examples of the various definitions to be included within the scope of the invention are explained in detail in the following.
The term "lower" is intended to mean a group having 1 to 6 carbon atom(s) preferably 1 to 4 carbon atom(s), unless otherwise provided.
Suitable "lower alkyl" and lower alkyl moiety in the term "lower alkylthio" may be a straight or branched one such as methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tert-butyl, pentyl, hexyl or the like, in which the preferable one is C.sub.1 -C.sub.4 alkyl and the more preferable one is methyl or ethyl.
Suitable "lower alkoxy" may be methoxy, ethoxy, propoxy, isopropoxy, butoxy, isobutoxy, tert-butoxy, pentyloxy, hexyloxy or the like, in which the preferable one is C.sub.1 -C.sub.4 alkoxy, the more preferable one is C.sub.1 -C.sub.2 alkoxy and the most preferable one is methoxy.
Suitable "acyl" and the acyl moiety in the term "acylamino" may include carbamoyl, thiocarbamoyl, sulfamoyl, an aliphatic acyl, an aromatic acyl, a heterocyclic acyl and an aliphatic acyl substituted with aromatic or heterocyclic group(s) derived from carbamic, sulfonic, carboxylic or carbonic acids and their thio acids.
The aliphatic acyl may include saturated or unsaturated, acyclic or cyclic ones, such as lower alkanoyl (e.g. formyl, acetyl, propionyl, butyryl, isobutyryl, valeryl, isovaleryl, pivaloyl, hexanoyl, etc.), lower alkanesulfonyl (e.g. mesyl, ethanesulfonyl, propanesulfonyl, etc.), lower alkoxycarbonyl (e.g. methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, isopropoxycarbonyl, butoxycarbonyl, tert-butoxycarbonyl, etc.), lower alkenoyl (e.g. acryloyl, methacryloyl, crotonoyl, etc.), (C.sub.3 -C.sub.7)cycloalkanecarbonyl (e.g. cyclohexanecarbonyl, etc.), lower alkoxalyl (e.g. methoxalyl, ethoxalyl, etc.), lower alkanoylcarbonyl (e.g. pyruvoyl, etc.), lower alkan

REFERENCES:
patent: 5308857 (1994-05-01), Takasugi

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