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Claims for Patent: 4,283,408

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Claims for Patent: 4,283,408

Title: Guanidinothiazole compounds, process for preparation and gastric inhibiting compositions containing them
Abstract:Novel guanidinothiazole compounds of the general formula ##STR1## wherein R represents a hydrogen atom or a lower alkyl group, R.sub.1 represents an amino group, a lower alkyl group, a halogeno lower alkyl group, a substituted- or unsubstituted-aryl group, a mono- or di-lower alkylamino group, an arylamino group or an aralkylamino group, R.sub.2 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, Y represents a sulfur atom or a methylene group, m and n, each represents an integer of 1-3, and the pharmacologically acceptable acid addition salts thereof, they are useful as gastric acid secretion inhibitors.
Inventor(s): Hirata; Yasufumi (Omiya, JP), Yanagisawa; Isao (Tokyo, JP), Ishii; Yoshio (Omiya, JP), Tsukamoto; Shinichi (Tokyo, JP), Ito; Noriki (Twatsuki, JP), Isomura; Yasuo (Yokohama, JP), Takeda; Masaaki (Urawa, JP)
Assignee: Yamanouchi Pharmaceutical Co., Ltd. (Tokyo, JP)
Application Number:06/107,629
Patent Claims: 1. Guanidinothiazole compounds of the formula ##STR34## wherein R represents a hydrogen atom or a lower alkyl group, R.sub.1 represents an amino group, a lower alkyl group, a halogeno lower alkyl group, a phenyl or naphthyl group which is unsubstituted or substituted by halogen, hydroxyl, amino, or alkoxy, a mono- or di-lower alkylamino group, an arylamino group or an aralkylamino group, R.sub.2 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, Y represents a sulfur atom or a methylene group, m and n, each represents an integer of 1-3, and the pharmacologically acceptable acid addition salts thereof.

2. The compounds as claimed in claim 1 wherein R and R.sub.2 are hydrogen atoms, R.sub.1 is an amino group and Y is a sulfur atom.

3. The compounds as claimed in claim 1 wherein R.sub.2 is a hydrogen atom or a lower alkyl group.

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

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

6. Medical composition containing a gastric acid secretion inhibiting amount of a guanidinothiazole compound of the formula ##STR35## wherein R represents a hydrogen atom or a lower alkyl group, R.sub.1 represents an amino group, a lower alkyl group, a halogeno lower alkyl group, a phenyl or naphthyl group which is unsubstituted or substituted by halogen, hydroxyl, amino, or akoxy, a mono- or di-lower alkylamino group, an arylamino group or an aralkylamino group, R.sub.2 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, Y represents a sulfur atom or a methylene group, m and n, each represent an integer of 1-3, or a non-toxic acid addition salt thereof and pharmaceutically acceptable carriers or diluents.
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