6-Aryl-s-triazolo-(4,3-a)-pyrido-(2,3-f)-1,4-diazepines

Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Bacterium or component thereof or substance produced by said...

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2602948B, 2602949, 260295T, 260296H, A61K 3144, C07D47104

Patent

active

041104552

ABSTRACT:
There are produced 6-aryl-s-triazolo-(4,3-a)-pyrido-(2,3-f)-(1,4)-diazepines of the formula: ##STR1## wherein R.sub.1 is hydrogen, a halogen atom, an alkyl group with 1 to 6 carbon atoms, a hydroxy group, an alkoxy group with 1 to 6 carbon atoms, a mercapto group, an alkyl mercapto group having 1 to 6 carbon atoms, an alkylsulfoxido group with 1 to 6 carbon atoms, an alkyl sulfono group with 1 to 6 carbon atoms, an amino group, an aliphatic acylamino group with 2 to 6 carbon atoms, a monoalkylamino group with 1 to 6 carb0n atoms, a dialkylamino group with 1 to 6 carbon atoms in each alkyl group or a saturated heterocyclic amino group having 5 to 7 members in the ring including 1 to 2 nitrogen atoms and 0 to 1 oxygen atoms in the ring,
R.sub.2 is hydrogen, an alkyl group with 1 to 6 carbon atoms, a hydroxy group, an acyloxy group with 2 to 6 carbon atoms, an alkoxy group with 1 to 6 carbon atoms, a mercapto group, an alkylmercapto group with 1 to 6 carbon atoms, a halogen atom, an amino group, an aliphatic acylamino group with 2 to 6 carbon atoms, a monoalkylamino group with 1 to 6 carbon atoms, a dialkylamino group with 1 to 6 carbon atoms in each alkyl group or a saturated heterocyclic amino group having 5 to 7 members in the ring including 1 to 2 nitrogen atoms and 0 to 1 oxygen atoms in the ring,
R.sub.3 is hydrogen, an alkyl group with 1 to 6 carbon atoms, an alkoxy group with 1 to 6 carbon atoms or a halogen atom,
The structural part A--B is the group --N.dbd.N--, --CH.sub.2 --NH--, --CO--NR.sub.4, --C(SR.sub.5).dbd.N--, --C(OR.sub.5).dbd.N--, --C(NR.sub.5 R.sub.5).dbd.N--, or --CR.sub.6 .dbd.N--,
wherein R.sub.4 is hydrogen, an alkenyl group with 2 to 6 carbon atoms, an alkinyl group with 2 to 6 carbon atoms, a hydroxy-alkyl group with 1 to 6 carbon atoms, a ketoalkyl group with 1 to 6 atoms in the alkyl group, a cyanoalkyl group with 1 to 6 carbon atoms, an alkyl group with 1 to 6 carbon atoms, or an alkyl group of 1 to 6 carbon atoms substituted by an alkoxy group with 1 to 6 carbon atoms, a dialkylamino group with 1 to 6 carbon atoms in each alkyl group or a saturated heterocyclic amino group having 5 to 7 members in the ring including 1 to 2 nitrogen atoms and 0 to 1 oxygen atoms,
R.sub.5 is hydrogen or an alkyl group with 1 to 6 carbon atoms,
R.sub.6 is hydrogen, an alkyl group with 1 to 6 carbon atoms or a haloalkyl group with 1 to 6 carbon atoms,
And Y--Z is the group >CH.dbd.N--, >C.dbd.N(.fwdarw.O), >CH--NH-- or >CH--N(OH)-- and wherein R.sub.6 is other than alkyl if R.sub.1 is chlorine, R.sub.2 is hydrogen, R.sub.3 is hydrogen or halogen and Y-Z is the group >C.dbd.N--, their optical isomers and their pharmaceutically acceptable salts. The compounds have anticonvulsive properties.

REFERENCES:
patent: 4039551 (1977-08-01), Hester

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