1055306-76-7

Upstream product

• 102503-23-1 1-(2,4-dimethoxyphenyl)-N-methylmethanamine 
• 1055306-65-4 (2RS)-3,3-difluoro-2-(2-fluoropyridin-3-yl)-2-hydroxy-4-methylidenepyrrolidine-1-carboxylate 
• 1055306-64-3 tert-butyl 3,3-difluoro-4-methylidene-2-oxopyrrolidine-1-carboxylate 
• 1055306-63-2 tert-butyl (4RS)-4-(bromomethyl)-3,3-difluoro-2-oxopyrrolidine-1-carboxylate 
• 1055306-62-1 tert-butyl [bromo(difluoro)acetyl]prop-2-en-1-ylcarbamate 
• 198547-62-5 2-bromo-2,2-difluoro-N-(prop-2-en-1-yl)acetamide 
• 16133-25-8 Pyridine-3-sulfonyl chloride 

Downstream Products

• 1055305-44-6 1-(4-fluoro-5-(2-fluoropyridin-3-yl)-1-{[3-(5-methyl-1,3,4-oxadiazol-2-yl)phenyl]sulfonyl}-1H-pyrrol-3-yl)-N-methylmethanamine fumarate 
• 1055305-39-9 3-({3-fluoro-2-(2-fluoropyridin-3-yl)-4-[(methylamino)methyl]-1H-pyrrol-1-yl}sulfonyl)benzyl acetate fumarate 
• 1055305-35-5 3-({3-fluoro-2-(2-fluoropyridin-3-yl)-4-[(methylamino)methyl]-1H-pyrrol-1-yl}sulfonyl)-N-(2-hydroxyethyl)benzamide hydrochloride 
• 1055305-42-4 1-[4-fluoro-5-(2-fluoropyridin-3-yl)-1-({3-[(methylsulfonyl)methyl]phenyl}sulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine hydrochloride 
• 1055305-34-4 1-(4-fluoro-5-(2-fluoropyridin-3-yl)-1-{[3-(methylsulfonyl)phenyl]sulfonyl}-1H-pyrrol-3-yl)-N-methylmethanamine hydrochloride 
• 1055305-49-1 1-{1-[(2,6-difluorophenyl)sulfonyl]-4-fluoro-5-(2-fluoropyridin-3-yl)-1H-pyrrol-3-yl}-N-methylmethanamine hydrochloride 
• 1055305-47-9 1-[1-(cyclohexylsulfonyl)-4-fluoro-5-(2-fluoropyridin-3-yl)-1H-pyrrol-3-yl]-N-methylmethanamine hydrochloride 
• 1055305-33-3 3-({3-fluoro-2-(2-fluoropyridin-3-yl)-4-[(methylamino)methyl]-1H-pyrrol-1-yl}sulfonyl)benzonitrile hydrochloride 
• 1055305-93-5 2-({3-fluoro-2-(2-fluoropyridin-3-yl)-4-[(methylamino)methyl]-1H-pyrrol-1-yl}sulfonyl)benzonitrile hydrochloride 
• 1055305-95-7 1-[4-fluoro-5-(2-fluoropyridin-3-yl)-1-(morpholin-4-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine hydrochloride 
• 1055305-20-8 1-{4-fluoro-5-(2-fluoropyridin-3-yl)-1-[(3-methoxyphenyl)sulfonyl]-1H-pyrrol-3-yl}-N-methylmethanamine hydrochloride 
• 1055305-21-9 1-{4-fluoro-1-[(3-fluorophenyl)sulfonyl]-5-(2-fluoropyridin-3-yl)-1H-pyrrol-3-yl}-N-methylmethanamine hydrochloride 
• 1055305-94-6 4-({3-fluoro-2-(2-fluoropyridin-3-yl)-4-[(methylamino)methyl]-1H-pyrrol-1-yl}sulfonyl)phenol hydrochloride 
• 1055307-01-1 benzyl 3-{[4-{[(tert-butoxycarbonyl)(methyl)amino]methyl}-3-fluoro-2-(2-fluoropyridin-3-yl)-1H-pyrrol-1-yl]sulfonyl}benzoate 

Relevant academic research and scientific papers

Exploration of pyrrole derivatives to find an effective potassium-competitive acid blocker with moderately long-lasting suppression of gastric acid secretion

With the aim to discover a novel excellent potassium-competitive acid blocker (P-CAB) that could perfectly overcome the limitations of proton pump inhibitors (PPIs), we tested various approaches based on pyrrole derivative 1 as a lead compound. As part of a comprehensive approach to identify a new effective drug, we tried to optimize the duration of action of the pyrrole derivative. Among the compounds synthesized, fluoropyrrole derivative 20j, which has a 2-F-3-Py group at position 5, fluorine atom at position 4, and a 4-Me-2-Py sulfonyl group at the first position of the pyrrole ring, showed potent gastric acid-suppressive action and moderate duration of action in animal models. On the basis of structural properties including a slightly larger C?log?P value (1.95), larger log?D value (0.48) at pH 7.4, and fairly similar pKa value (8.73) compared to those of the previously optimized compound 2a, compound 20j was assumed to undergo rapid transfer to the stomach and have a moderate retention time there after single administration. Therefore, compound 20j was selected as a new promising P-CAB with moderately long duration of action.

PYRROLE COMPOUNDS

The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity, which is represented by the formula (I) wherein R1 is an optionally substituted cyclic group, R2 is a substituent, R3 is an optionally substituted alkyl group, an acyl group, an optionally substituted hydroxy group, an optionally substituted amino group, a halogen atom, a cyano group or a nitro group, R4 and R5 are each a hydrogen atom, an optionally substituted alkyl group, an acyl group, an optionally substituted hydroxy group, an optionally substituted amino group, a halogen atom, a cyano group or a nitro group, R6 and R6' are each a hydrogen atom or an alkyl group, and n is an integer of 0 - 3, or a salt thereof.