118420-35-2

Upstream product

• 541-41-3 chloroformic acid ethyl ester 
• 101620-10-4 4-(4-diphenyl-methyl-1-piperazinyl)butylamine 
• 118419-96-8 (E)-3-(5-fluoropyridin-3-yl)acrylic acid 
• 107756-01-4 C₁₃H₁₂FN₃O₃S 
• 22620-29-7 Ethyl 5-fluoronicotinate 
• 701-40-6 5-fluoropyridine-3-carbohydrazide 
• 39891-04-8 5-fluoropyridine-3-carboxaldehyde 

Relevant academic research and scientific papers

Pyridine compounds, process for the preparation thereof and pharmaceutical composition containing the same

The present invention relates to novel pyridine compounds having antiallergic activity mainly through 5-lipoxygenase inhibitory activity, antihistamine activity and/or inhibiting activity against chemical mediator release

Acrylamide derivatives as antiallergic agents. 2. Synthesis and structure-activity relationships of N-[4-[4-(diphenylmethyl)-1-piperazinyl]butyl]-3-(3-pyridyl)acrylamides

A new series of 3-(3-pyridyl)acrylamides 16, 17, 19, and 26, and 5-(3-pyridyl)-2,4-pentadienamides 20-25 were prepared and evaluated for their antiallergic activity. Several of these compounds exhibited more potent inhibitory activities than the parent compounds 1a [(E)-N-[4 [4-(diphenylmethyl)-1-piperazinyl]butyl]-3-(3-pyridyl)acrylamide] against the rat passive cutaneous anaphylaxis (PCA) reaction and the enzyme 5-lipoxygenase. Particularly, 4-[4-(diphenylmethyl)-1-piperazinyl]butyl]-3-(6-methyl-3-pyridyl)acrylamide (17p) showed an ED50 value of 3.3 mg/kg po in the rat PCA test, which was one-fifth of ketotifen and oxatomide. As compared with ketotifen and oxatomide, compound 17p (AL-3264) possessed a better balance of antiallergic properties due to inhibition of chemical mediator release, inhibition of 5-lipoxygenase, and antagonism of histamine.

ω-(3-pyridyl)alkenamide derivatives and anti-allergenic pharmaceutical compositions containing same

Compounds of the formula: STR1 wherein X is alkylene or --(CR6 =CR7)r -- wherein R6 is H, alkyl or phenyl, R7 is H, alkyl, cyano or phenyl, and r is 1 or 2; A is alkylene or alkylene interrupted by at least one double bond; R1 is H, halogen, alkyl, alkoxy, alkylthio, cycloalkyloxy, cycloalkylthio, alkoxycarbonyl, carboxy, phenyl, phenoxy, phenylthio, 3-pyridyloxy or 3-pyridylthio; R2 is H, hydroxy, alkanoyloxy or alkoxycarbonyloxy, or adjacent R1 and R2 may combine to form tetramethylene or --CH2 OCR8 R9 O-- (R8 and R9 are alkyl); R3 is H, alkyl or hydroxyalkyl; R4 is H or alkyl; R5 is phenyl, heteroaryl or --(CH2)m --CHR10 R11 (R10 is H or phenyl, R11 is phenyl or pyridyl and m is 0 to 2); p is 0 or 1; and q is 2 or 3; the phenyl group or moiety being optionally substituted, and a salt thereof, process for the preparation thereof, and pharmaceutical composition containing the same. Said compounds and salts thereof show excellent antiallergic activity mainly through 5-lipoxygenase inhibiting activity, antihistamine activity and/or inhibitory activity against chemical mediator release and useful for treatment of allergic diseases.