125030-79-7Relevant academic research and scientific papers
Thienotriazolodiazepines as platelet-activating factor antagonists. Steric limitations for the substituent in position 2
Walser,Flynn,Mason,Crowley,Maresca,O'Donnell
, p. 1440 - 1446 (2007/10/02)
The preparations of thienotriazolodiazepines bearing a substituted ethynyl group at the 2-position, and the corresponding cis-olefins and fully saturated analogues are described. The compounds were evaluated as potential antagonists of platelet-activating
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
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, (2008/06/13)
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.
