125030-56-0

Upstream product

• 87213-50-1 8-bromo-5-(2-chlorophenyl)-1-methyl-4H-s-triazolo<4,3-a>-1,4-benzodiazepine 
• 1066-54-2 trimethylsilylacetylene 

Downstream Products

• 125030-57-1 (6-(2-chlorophenyl)-8-ethynyl-1-methyl-4H-benzo [f][1,2,4]triazolo[4,3-a][1,4]diazepine) 

Relevant academic research and scientific papers

Stereospecific anxiolytic and anticonvulsant agents with reduced muscle-relaxant, sedative-hypnotic and ataxic effects

The present invention provides compositions and methods of using stereospecific benzodiazepine derivatives, their salts and prodrugs for the treatment of anxiolytic or convulsant disorders having the side effects of reduced alcohol craving in human alcoholics and a concomitant reduced sedative, hypnotic, muscle relaxant and ataxic side-effects. The invention further provides pharmaceutical compositions for treatment of anxiolytic and convulsant disorders in subjects in need thereof, comprising a compound, prodrug or a salt having a chemical structure represented by any one of Formula I-XXI and a pharmaceutically-acceptable carrier.

ANXIOLYTIC AGENTS WITH REDUCED SEDATIVE AND ATAXIC EFFECTS

Orally active benzodiazepine derivatives and their salts are disclosed. These compounds and their salts have anxiolytic and anticonvulsant activity with reduced sedative/hypnotic/muscle relaxant/ataxic effects.

Triazolo(4,3-A)(1,4)benzodiazepines and thieno (3,2-F)(1,2,4)triazolo(4,3-A)(1,4)diazepine compounds which have useful activity as platelet activating factor (PAF) antagonists

The invention relates to compounds of the formula STR1 wherein X is --CH=CH-- or S; R1 is lower alkyl, lower alkoxy or trifluoromethyl; R2 is hydrogen, lower alkyl, lower alkoxy, hydroxy or alkanoyloxy; R3 and R4, independently, are hydrogen, chlorine, fluorine, lower alkyl or lower alkoxy; s is an integer from 0 to 1, provided that when s is 1, R2 cannot be hydroxy, lower alkoxy or alkanoyloxy; R5 is a radical of the formula R6 --(CH2)n -- or R7 --O--(CH2)m -- wherein R6 and R7 are aryl or a heterocyclic radical, n is an integer of from 0 to 2 and m is an integer of from 1 to 2, provided that, when n is 0, R6 must be attached through a carbon to carbon bond, and provided that R7 is always attached through a carbon to oxygen bond, and, when at least one asymmetric carbon is present, its enantiomers and racemates, and pharmaceutically acceptable acid addition salts thereof. The compounds of formula I exhibit activity as platelet activating factor (PAF) antagonists and are, therefore, useful in disease states characterized by excess platelet activating factor or for the prevention and treatment of cardiovascular diseases, pulmonary diseases, immunological disorders, inflammatory diseases, dermatological disorders, shock or transplant rejection.