Pyrazolo [4',3':5,6] pyride [3,4-e] [1,2,4] triazolo-...

C - Chemistry – Metallurgy – 07 – D

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260/242.01

C07D 471/22 (2006.01)

Patent

CA 1083570

Abstract This invention describes new derivatives of pyrazolo- [4',3':5,6]pyrido[3:4-?][1,2,4]triazolo[1,5-a]pyrimidine deri- vative? having the general formula Image wherein Z is Image or Image ; R1 is hydroqen, lower alkyl, phenyl, phenyl-lower alkylene, benzoyl or substituted benzoyl wherein the benzoyl substitutent is one or two halogens, lower alkyl or trifluoromethyl groups; R2 is hydrogen, lower alkyl or phenyl; R3 is hydrogen, lower alkyl, phenyl, lower alkylthio or lower alkylsulfinyl; R4 is hydrogen, lower alkyl, phenyl-lower alkylene, benzoyl, substituted benzoyl, lower alkanoyl, lower alkoxy-lower alkylene, lower alkylthio-lower alkylene, phenyl, substituted phenyl, or Image lower alkylene, morpholine, thiamorpholine or piperazine, the substituents on said substituted phenyl and substituted benzoyl being halogen, lower alkoxy or lower alkyl. R4' is halo, Image , -S-R8, phenyl-lower alkoxy, phenyloxy, substituted phenyloxy wherein the phenyl ring bears one or two halogen, lower alkyl or tri- fluoromethyl groups; lower alkoxy or substituted lower alkoxy wherein the lower alkoxy substituent is Image ; R5 is hydrogen or lower alkyl; R6 is hydrogen, lower alkyl, sub- stituted lower alkyl wherein the lower alkyl substituent is Image , phenyl or substituted phenyl wherein the phenyl substituent is halogen, lower alkyl or trifluoromethyl, R7 is hydrogen or lower alkyl, or R6 and R7 together with the nitro- gen form one of the unsubstituted or substituted heterocyclics pyrrolidino, morpholino, thiamorpholino, piperidino, pyrazolyl, dihydropyridazinyl or piperazinyl wherein the heterocycle sub- stituent is lower alkyl or hydroxy-lower alkylene; R8, R9 and R10 each is hydrogen or lower alkyl; and acid addition salts thereof and a process for preparing these compounds which are useful as antiinflammatory agents and central nervous system depressants.

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