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Details for Patent: 4,362,736

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Details for Patent: 4,362,736

Title: Guanidinothiazole compounds, and medical compositions containing them
Abstract:Novel guanidinothiazole compounds of the general formula ##STR1## wherein R represents a hydrogen atom or a lower alkyl group, Y represents a sulfur atom or a methylene group, m and n each represents an integer of 1-3, A represents the group shown by ##STR2## (wherein R.sub.1 represents a hydrogen atom, a cyano group, a carbamoyl group, a ureido group, a hydroxyl group, a lower alkoxy group, a lower acyl group, an acylamino group, an arylsulfamoyl group, an aralkyl group or a carboxymethyl group, an arylsulfamoyl group, an aralkyl group or a carboxymethyl group, R.sub.2 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a cyano group or a lower acyl group, and R.sub.3 represents a hydrogen atom, a lower alkyl group, a hydroxyl group or a sulfamoyl group), and the pharmacologically acceptable acid addition salts thereof; these compounds are useful as gastric acid secretion inhibitors.
Inventor(s): Hirata; Yasufumi (Omiya, JP), Yanagisawa; Isao (Tokyo, JP), Ishii; Yoshio (Omiya, JP), Takeda; Masaaki (Urawa, JP)
Assignee: Yamanouchi Pharmaceutical Co., Ltd. (Tokyo, JP)
Filing Date:Mar 06, 1980
Application Number:06/127,902
Claims:1. A guanidinothiazole compound of the formula ##STR66## wherein R represents a hydrogen atom or a lower alkyl group, Y represents a sulfur atom or a methylene group, m and n each represent an integer of 1-3, A represents the group ##STR67## wherein R.sub.1 represents a member selected from the group consisting of a hydrogen atom, a cyano group, a carbamoyl group, a ureido group, a hydroxyl group, a lower alkoxy group, a lower alkylcarbonyl group of a straight or branched carbon chain having 1-5 carbon atoms, a lower alkylcarbonylamino group of straight or branched carbon chain having 1-5 carbon atoms, a benzoylamino group, a naphthoylamino group, a --NH--SO.sub.2 -phenyl group, a --NH--SO.sub.2 -naphthyl group, a benzyl group, a phenethyl group, and a carboxymethyl group, R.sub.2 represents a member selected from the group consisting of a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a cyano group, and a lower alkylcarbonyl group of a straight or branched carbon chain having 1-5 carbon atoms, and R.sub.3 represents a member selected from the group consisting of a hydrogen atom, a lower alkyl group, a hydroxyl group, and a sulfamoyl group, and the pharmacologically acceptable acid addition salts thereof.

2. A compound as claimed in claim 1 wherein said R represents a hydrogen atom, Y represents a sulfur atom, and A represents the group shown by ##STR68## wherein R.sub.1 and R.sub.2 have the same significance as above.

3. A compound as claimed in claim 1 wherein said R.sub.2 represents a member selected from the group consisting of a hydrogen atom, a lower alkyl group, a cyano group, and a lower alkylcarbonyl group of a straight or branched carbon chain having 1-5 carbon atoms.

4. A compound as claimed in claim 1 which is N-cyano-3-[(2-guanidinothiazol-4-yl)methylthio]propionamidine.

5. A compound as claimed in claim 1 which is N-carbamoyl-3-[(2-guanidinothiazol-4-yl)methylthio]propionamidine.

6. A pharmaceutical composition comprising a gastric acid secretion inhibiting amount of a compound of claim 1 in combination with a pharmaceutically acceptable carrier or diluent.

7. A composition according to claim 6 wherein the guanidinothiazole compound is N-cyano-3-[(2-guanidinothiazol-4-yl)methylthio]propionamidine.

8. A composition according to claim 6 wherein the guanidinothiazole compound is N-carbamoyl-3-[(2-guanidinothiazol-4-yl)methylthio]propionamidine.

9. A pharmaceutical composition comprising a histamine H.sub.2 -receptor blocking amount of a compound of claim 1 in combination with a pharmaceutically acceptable carrier or diluent.
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