154186-47-7

Upstream product

• 5617-74-3 3-oxabicyclo[3.1.0]hexane-2,4-dione 
• 140-69-2 4-methoxybenzylhydrazine 

Downstream Products

• 1346701-80-1 5-(2-benzyl-benzoxazol-6-yl)-3-(4-methoxy-benzyl)-3,4-diaza-bicyclo[4.1.0]hept-4-en-2-one 
• 1346701-79-8 3-(4-methoxy-benzyl)-5-(2-phenyl-6,7-dihydro-4H-oxazolo[5,4-c]pyridin-5-yl)-3,4-diaza-bicyclo[4.1.0]hept-4-en-2-one 
• 1346699-80-6 5-(2-phenyl-4,5,6,7-tetrahydro-4H-oxazolo[5,4-c]pyridin-5-yl)-3,4-diaza-bicyclo[4.1.0]hept-4-en-2-one 
• 1346701-78-7 4-(4-methoxy-benzyl)-5-oxo-3,4-diaza-bicyclo[4.1.0]hept-2-en-2-yl trifluoro-methanesulphonate 
• 273213-65-3 (3S,4R)-3-Hydroxy-4-[(1R,6S)-4-(4-methoxy-benzyl)-5-oxo-3,4-diaza-bicyclo[4.1.0]hept-2-en-2-yloxy]-2,2-dimethyl-chroman-6-carbonitrile 
• 273213-64-2 (3S,4R)-3-Hydroxy-4-[(1S,6R)-4-(4-methoxy-benzyl)-5-oxo-3,4-diaza-bicyclo[4.1.0]hept-2-en-2-yloxy]-2,2-dimethyl-chroman-6-carbonitrile 

Relevant academic research and scientific papers

PYRIDAZINONES AS GPR119 AGONISTS

The present invention relates to pyridazinone derivatives of general formula (I), wherein the groups A, G and R1 are as defined in the application, the tautomers thereof, stereoisomers thereof, the mixtures thereof and the salts thereof, which

Novel potassium channel opener prodrugs with a slow onset and prolonged duration of action

(-)-(3S,4R,1'R,6'S)-4-(4-Benzyl-5-oxo-3,4-diazabicyclo[4.1.0.]hept-2-en- 2-yloxy)-3,4-dihydro-3-hydroxy-2,2-dimethyl-2H-1-benzopyran-6-carbonitrile and its derivatives with a modified benzyl group were synthesized with the objective of discovering novel ATP-sensitive potassium channel openers (PCOs) with a slow onset of action and a reduced tendency to induce tachycardia. Among the compounds synthesized, 4-(2-chlorobenzyl) derivative 5bB had potent hypotensive activity in spontaneously hypertensive rats (SHRs). In addition, compound 5bB showed the desired pharmacological profile with a slow onset and long duration of action and induction of only mild tachycardia. Compound 5bB was found to be quantitatively metabolized in rats to give active des-2- chlorobenzyl derivative 6B. These results suggest that the incorporation of an N-benzyl group is a useful method for the preparation of prodrugs, the function of which is to delay the onset and prolong the duration of action of the active substance.