C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
167/210, 260/239
C07D 487/04 (2006.01) A61K 31/55 (2006.01) C07D 495/14 (2006.01) C07D 519/00 (2006.01) C07F 7/08 (2006.01)
Patent
CA 1327570
Abstract of the Disclosure The novel compounds of the general formula Image I wherein X is -CH=CH- or S; R1 is lower alkyl, lower alkoxy or trifluoromethyl; R2 is hydrogen, lower alkyl, lower alkoxy, hydroxy or lower alkanoyloxy; R3 and R4, independently, are hydrogen, chlorine, fluorine, lower alkyl or lower alkoxy: R5 is a radical of the formula R6-(CH2)n-C?C- or R7-O-(CH2)m-C?C-, R6 and R7 are aryl or a heterocyclic radical; n is an integer from 0 to 2; m is an integer from 1 to 2 and s is an integer from 0 to 1; with the proviso that, when s is 1, R2 cannot be hydroxy, lower alkoxy or lower alkanoyloxy: that, when n is 0, R6 must be attached through a carbon to carbon bond, and that R7 is always attached through a carbon to oxygen bond, and, when at least one asymmetric centre is present, their enantiomers and racemates and pharmaceutically acceptable acid addition salts thereof 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, shocks or transplant rejections.
585981
F. Hoffmann-La Roche Ag
Gowling Lafleur Henderson Llp
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