122957-33-9

Upstream product

• 13091-23-1 4-chloro-3-nitropyridine 
• 873-74-5 4-Aminobenzonitrile 

Downstream Products

• 122957-34-0 3-amino-4-[N-(4-cyanophenyl)amino]pyridine 
• 122957-32-8 4-(2-methylimidazo[4,5-c]pyrid-1-yl)benzonitrile 
• 132504-92-8 4-(2-Methyl-imidazo[4,5-c]pyridin-1-yl)-benzoyl chloride 
• 170499-29-3 methyl 4-(1H-2-methylimidazo[4,5-c]pyrid-1-yl)benzoate 
• 142161-56-6 1-(4-cyanophenyl)-2,3-dihydroimidazo<4,5-c>pyridin-2-one 
• 122957-37-3 1-(4-cyanophenyl)-2-ethylimidazo<4,5-c>pyridine 
• 122957-36-2 2-butyl-1-(4-cyanophenyl)imidazo<4,5-c>pyridine 
• 122957-35-1 1-(4-cyanophenyl)-2-(trifluoromethyl)imidazo<4,5-c>pyridine 
• 122957-08-8 ethyl 4'-(2-methylimidazo[4,5-c]pyridin-1-yl)benzoylacetate 
• 142161-52-2 3-Oxo-3-[4-(2-oxo-2,3-dihydro-imidazo[4,5-c]pyridin-1-yl)-phenyl]-propionic acid ethyl ester 
• 122957-13-5 3-[4-(2-Ethyl-imidazo[4,5-c]pyridin-1-yl)-phenyl]-3-oxo-propionic acid ethyl ester 
• 122957-10-2 3-[4-(2-Butyl-imidazo[4,5-c]pyridin-1-yl)-phenyl]-3-oxo-propionic acid ethyl ester 
• 122957-09-9 3-Oxo-3-[4-(2-trifluoromethyl-imidazo[4,5-c]pyridin-1-yl)-phenyl]-propionic acid ethyl ester 
• 142161-40-8 4-(2-chlorophenyl)-1,4-dihydro-3-(ethoxycarbonyl)-6-methyl-2-<4-(2-methylimidazo<4,5-c>pyrid-1-yl)phenyl>-pyridine-5-carboxylic acid 

Relevant academic research and scientific papers

Discovery and evaluation of a series of 3-acylindole imidazopyridine platelet-activating factor antagonists

Studies conducted with the goal of discovering a second-generation platelet-activating factor (PAF) antagonist have identified a novel class of potent and orally active antagonists which have high aqueous solubility and long duration of action in animal m

1,4-dihydropyridines useful as pharmaceuticals

The invention provides compounds of the formula: STR1 The variables are defined in the specification. The compounds are useful e.g. for the curative or prophylactic treatment of allergic conditions.

1,4-Dihydropyridines as Antagonists of Platelet Activating Factor. 1. Synthesis and Structure-Activity Relationships of 2-(4-Heterocyclyl)phenyl Derivatives

A novel class of 2-(4-heterocyclylphenyl)-1,4-dihydropyridines (2-38) possessing antagonist activity against platelet activating factor (PAF) was prepared by the Hantzsch synthesis from a variety of ethyl 4'-heterocyclic-substituted benzoylacetates, aryl or heteroaryl aldehydes, and substituted 3-aminocrotonamides or 3-aminocrotonate esters.Structure-activity relationships were evaluated where PAF antagonist activity was measured in vitro by determining the concentration of compound (IC50) required to inhibit the PAF-induced aggregation of rabbit washed platelets,and in vivo by determining the oral dose (ED50) which protected mice from a lethal injection of PAF.The nature of the substituent at the dihydropyridine 2-position was found to be important for both in vitro and in vivo activity, whereas there was greater flexibility for structural variation at the 4- and 5-positions.The most potent compound was 4-(2-chlorophenyl)-1,4-dihydro-3-(ethoxycarbonyl)-6-methyl-2-pyrid-1-yl)phenyl>-5-pyridine (17, UK-74,505), IC50 = 4.3 nM, ED50 = 0.26 mg/kg po, which was found to be approximately 33 times more potent in vitro (rabbit platelet aggregation) and about 8 times more potent in vivo (murine lethality) than WEB2086.Compound 17 also exhibited a long duration of action in the dog (inhibition of PAF-induced whole blood aggregation ex vivo was maintained for > 24 h following a single oral dose of 75 μg/kg) and was highly selective as a PAF antagonist, showing only weak affinity (IC50 = 6600 nM) for the nitrendipine binding site.As a result of its high oral potency, selectivity, and duration of action, UK-74,505 has been selected for clinical evaluation.

1,4-dihydropyridine derivatives

The invention provides compounds of the formula STR1 and pharmaceutically acceptable salts thereof, wherein R is phenyl substituted by halo; R1 is C1 -C4 alkyl; is hydrogen, C5 -C7 cycloalkyl, benzyl