NOVEL THEOPHYLLINE DERIVATIVE

NEW MATERIAL:A compound shown by formula I (R is H, lower alkyl or lower alkoxymethyl; n is 1-3; when A is S or sulfinyl, B is 3-alkyl-2- cyanoguanidyl or pyridyl and when A is O or amino, B is pyridyl). EXAMPLE:7-Methyl-3-[2-(3-methyl-2-cyano-1-guadinyl)ethylthio]theophyll ine. USE:An antiulcer hav...

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Bibliographic Details
Main Author HORI MIKIO
Format Patent
LanguageEnglish
Published 01.08.1987
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Summary:NEW MATERIAL:A compound shown by formula I (R is H, lower alkyl or lower alkoxymethyl; n is 1-3; when A is S or sulfinyl, B is 3-alkyl-2- cyanoguanidyl or pyridyl and when A is O or amino, B is pyridyl). EXAMPLE:7-Methyl-3-[2-(3-methyl-2-cyano-1-guadinyl)ethylthio]theophyll ine. USE:An antiulcer having well balanced both activities of prevention of attacking factor and protecting action on gastric mucosa and low toxicity. PREPARATION:For example, a compound shown by formula II (R is lower alkyl or lower alkoxymethyl) is reacted with a compound shown by formula III (X is halogen) in a solvent such as DMF, etc., in the presence of an alkali metal hydride at 0-100 deg.C. Then the formed compound shown by formula IV is reacted with an alkylamine at room temperature-100 deg.C to give a compound shown by formula V (B1 is 3-alkyl-2-cyanoguanidyl).
Bibliography:Application Number: JP19860015403