125030-90-2

Upstream product

• 67860-41-7 4-(2-chlorophenyl)2-iodo-9-methyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine 
• 94707-28-5 10-(prop-2-yn-1-yl)acridin-9(10H)-one 
• 67860-47-3 5-(2-chlorophenyl)-1,3-dihydro-7-iodo-2H-thieno<2,3-e><1,4>diazepin-2-thione 
• 36811-58-2 5-(2-chlorophenyl)-1,3-dihydro-2H-thieno[2,3-e][4,1]diazepin-2-one 

Relevant academic research and scientific papers

Triazolobenzo- and triazolothienodiazepines as potent antagonists of platelet activating factor

A series of [1,2,4]triazolo[4,3-α][1,4]benzodiazepines bearing an ethynyl functionality at the 8-position and the isosteric thieno[3,2-f][1,2,4]triazolo[4,3-α][1,4]diazepines were prepared and evaluated as antagonists of platelet activating factor. The effects of substitution were explored in in vitro and in vivo test systems designed to measured PAF-antagonistic activity. Results are discussed and compared with previously published data. Many of the compounds had activity superior to WEB 2086, compound 1. In general, the thieno analogues exhibited better oral activity than the corresponding benzodiazepines. The duration of activity upon oral administration was modulated by the substitution on the acetylenic side chain. Compounds 71 and 81 were selected for further pharmacological evaluation as a result of their good oral potency and exceptionally long duration of action.

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.