Yamanouchi Pharmaceutical Company Ltd.

Yoshio Ishii

Isao Yanagisawa

Masuo Murakami

Kenichi Tomioka

Toshinari Tamura

Hidenori Iwamoto

Noriyoshi Inukai

Yasufumi Hirata

Masaaki Takeda

Tetsuya Shiozaki, Deceased

Yasuo Isomura

Noriki Ito

Osamu Hasegawa

Hideya Matsuda

Tetsuya Shizaoki

Shinichi Tsukamoto

Tokuichi Takagi

Tetsuya Shiozaki

A process is provided for producing a guanidinothiazole compound represented by the formula: ##STR1## wherein, R.sup.1 and R.sup.2, which may be the same or different, each represents a hydrogen or an alkyl group having 1 to 3 carbon atoms; m represents 1 or 2; and n represents 2, 3 or 4. The process comprises reacting an aminothiazole compound of the formula: ##STR2## with a cyanamide or an amidinopyrazole, the compounds are useful as intermediates in the preparation of a gastric acid secretion inhibitor.

Process of producing guanidinothiazole derivatives

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.

Guanidinothiazole compounds, and medical compositions containing them

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.

Guanidinothiazole compounds, process for preparation and gastric

There are disclosed 20-alkoxy-16-alkyl-prostadienoic acid derivatives of the formula: ##STR1## wherein A represents ##STR2## R and R.sup.5, which may be the same or different, each represents a hydrogen atom or a lower alkyl group; and R.sup.1 and R.sup.4, which may be the same or different, each represents a lower alkyl group, and the pharmaceutically acceptable non-toxic salts thereof. These compounds have excellent pharmacological effects as prostaglandin E.sub.2 and prostaglandin F.sub.2.alpha..

20-Alkoxy-16-alkyl-prostadienoic acid derivatives

3,15-Dilower alkyl prostaglandin E.sub.2 derivatives and 3,15-dilower alkyl prostaglandin D.sub.2 derivatives are disclosed. These compounds have antigastric ulcer activity without undesirable side effects to intestinal organs.

Novel 3,15-dilower alkyl PGE.sub.2 derivatives

A 20-alkoxy-16-alkyl-prostadienoic acid derivative shown by the formula ##STR1## wherein A represents ##STR2## R and R.sup.5, which may be the same or different, each represents a hydrogen atom or a lower alkyl group; and R.sup.1 and R.sup.4, which may be the same or different, each represents a lower alkyl group, And the pharmacologically acceptable nontoxic salts thereof. The compounds have excellent effects as prostaglandin E.sub.2 and prostaglandin F.sub.2.alpha..

20-Alkoxy-16-alkyl prostadienoic acid derivatives

Novel prostaglandin derivatives are provided having the formula: ##STR1## wherein A represents ##STR2## one of R.sub.3 and R.sub.4 represents a hydrogen atom and the other of them represents a lower alkyl group; one of R.sub.5 and R.sub.6 represents a hydrogen atom and the other of them represents a hydroxyl group; and one of R.sub.7 and R.sub.8 represents a hydrogen atom and the other of them represents a lower alkyl group. The compounds of this invention have excellent effects as prostaglandin E.sub.2 and prostaglandin F.sub.2.sub..alpha..

Growing community of inventors

Omiya, Japan

Yoshio Ishii