72716-92-8

Usage

InChI:InChI=1/C12H15NO3/c1-3-16-12(15)11(8-14)6-10-5-4-9(2)13-7-10/h4-5,7-8,11H,3,6H2,1-2H3

Upstream product

• 71351-48-9 3-(6-methyl-pyridin-3-yl)-propionic acid ethyl ester 
• 109-94-4 formic acid ethyl ester 
• 72716-74-6 (E)-3-(6-Methyl-pyridin-3-yl)-acrylic acid ethyl ester 
• 72716-73-5 3-(6-methyl-3-pyridyl)acrylic acid 
• 53014-84-9 2-methyl-5-formylpyridine 

Downstream Products

• 72716-93-9 2-nitroamino-5-(6-methylpyrid-3-ylmethyl)-4(1H)-pyrimidone 
• 76517-95-8 2-<2-(5-methyl-4-imidazolylmethylthio)ethylamino>-5-(6-methylpyrid-3-yl)-4-pyrimidone 

Relevant academic research and scientific papers

Isocytosine H2-receptor histamine antagonists II. Synthesis and evaluation of biological activity at histamine H1- and H2-receptors of 5-(heterocyclyl)methylisocytosines

A series of 2--4-pyrimidones was synthesized based on oxmetidine 2, in which the methylenedioxyphenyl group of 2 was replaced by a heterocyclic ring.Good H2-receptor antagonist activity was retained over a range of basic and neutral heterocyclic substituents.Replacement of the 5-methyl-4-imidazolyl ring in selected compounds with 2-thiazolyl and, particularly, 3-bromo-2-pyridyl rings gave a series of compounds which have both H1- and H2-receptor histamine antagonist activities.Some structure-activity and structure-toxicity correlations are discussed.Compound 6d, 2--5-(6-methylpyrid-3-yl)-4-pyrimidone, has the most favourable combination of properties for H2-antagonism and has been evaluated further as an anti-secretory agent.

PYRIDINE-PYRIMIDINONE DERIVATIVES, A PROCESS FOR THEIR PRODUCTION AND H2-ANTAGONIST MEDICAMENT CONTAINING THESE COMPOUNDS

The invention relates to new pyridine-pyrimidinone derivatives corresponding to the following general formula STR1 wherein R 1 represents linear C 1-6 alkyl or cycloalkyl and R 2 represents linear C 1-6 alkyl or R 1 and R 2 together with the nitrogen atom form a pyrrolidine or piperidine ring;Alk represents a linear alkylene chain C 1-6 ;Q represents a benzene ring, furan ring, thiophene ring or thiazole ring; X represents oxygen, Y is a single bond and m is 2, 3 or 4 when Q represents benzene;X represents methylene, Y represents sulfur and m is 2 or 3 when Q is furan, thiophene or thiazole; andR 3 represents a hydrogen atom or a lower alkyl group.These compounds show improved H. sub.2-antagonistic activity.

GUANIDINOTHIAZOLYL DERIVATIVES

The compounds are guanidinothiazolyl derivatives which are histamine H. sub.2-antagonists. A specific compound of the present invention is 2-2-(2-guanidino-4-thiazolylmethylthio)ethylamino!-5-(6-methyl-3-pyridylmethy l)-4-pyrimidone.

ISOUREAS AND ISOTHIOUREAS

The compounds are isoureas and isothioureas which have an O-or S-alkylpyrimidone substituent and which are histamine H 2-antagonists and antiinflammatory agents. A specific compound of this invention is 2-[5-(O-isoureido)pentylamino]-5-(6-methyl-3-pyridylmethyl)-4-pyrimidone.

Pyrimidine compounds

The compounds are substituted pyrimidine compounds which are histamine H2 -antagonists. A specific compound of the present invention is 2-[2-(5-dimethylaminomethyl)-2-furylmethylthio)ethylamino]-5-(3-pyridylmethyl)-4-pyrimidone.