Chemistry of carbon compounds – Miscellaneous organic carbon compounds – C-metal
Patent
1981-03-12
1982-09-14
Daus, Donald G.
Chemistry of carbon compounds
Miscellaneous organic carbon compounds
C-metal
260239BC, 260239BD, 2602456, C07D48704, C07D48714
Patent
active
043494757
ABSTRACT:
This invention is directed toward pharmacologically active compound of the formula ##STR1## wherein A is ##STR2## R.sub.1 is selected from the group consisting of hydrogen, lower alkyl, hydroxy lower alkyl, acyloxy lower alkyl, phenyl, alkoxy lower alkyl, halo lower alkyl, amino lower alkyl, substituted amino lower alkyl, substituted phenyl, pyridyl, aralkyl and the groups ##STR3## wherein R is hydrogen or lower alkyl and ROOC where R is lower alkyl; R.sub.2 is selected from the group consisting of hydrogen, lower alkyl, hydroxy lower alkyl, acyloxy lower alkyl, alkoxy lower alkyl, halo lower alkyl, amino or substituted amino lower alkyl, amino, cyano, cyano lower alkyl, substituted amino, chloro, bromo and iodo, the group --COOR where R is hydrogen or lower alkyl, the group ##STR4## where R is hydrogen or lower alkyl, or derivatives thereof, e.g., the group R--C.dbd.N--R' wherein R' is hydrogen, lower alkyl, hydroxy, phenyl, alkoxy, amino, mono or di-alkylamino and arylamino and R is hydrogen or lower alkyl, the group ##STR5## (where R and R' are individually hydrogen, lower alkyl, hydroxy lower alkyl, lower alkenyl, aryl or together R and R' form a part of a heterocyclic ring and the group (CH.sub.2).sub.n NRR' where R and R' are hydrogen, lower alkyl, hydroxy lower alkyl, lower alkenyl or together R and R' form a part of a heterocyclic ring and n is 1 to 4); the group ##STR6## where R.sup.10, R.sup.11, R.sup.12 are hydrogen or lower alkyl and the group (CH.sub.2).sub.n NR.sup.13 R.sup.14 where n is 1 to 4 and R.sup.13, R.sup.14 are hydrogen, lower alkyl, hydroxy lower alkyl, lower alkenyl or R.sup.13 and R.sup.14 together form part of a heterocyclic ring, with the limitation that where R.sup.10, R.sup.11 or R.sup.12 is a basic side chain, then the remaining substituents are hydrogen or lower alkyl; R.sub.3 is selected from the group consisting of hydrogen and lower alkyl; R.sub.5 is selected from the group consisting of hydrogen, lower alkanoyloxy and hydroxy; R.sub.4 is selected from the group consisting of hydrogen, halogen, nitro, cyano, trifluoromethyl, lower alkyl, substituted amino, amino, hydroxy lower alkyl and lower alkanoyl; R.sub.6 is selected from the group consisting of phenyl, mono-substituted phenyl, di-substituted phenyl, pyridyl and mono-substituted pyridyl; and ##STR7## is selected from the group consisting of ##STR8## and the pharmaceutically acceptable salts thereof. Also provided are methods for the preparation of these compounds as well as pharmaceutical formulations which contain the active compounds of this invention. The compounds of the formulas illustrated above and their analogs are useful as anticonvulsants, muscle relaxants, anxiolytic and sedative agents.
REFERENCES:
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Fryer, et al., J. Heterocyclic Chemistry, vol. 15, pp. 619-624 (6/78).
Fryer Rodney I.
Walser Armin
Daus Donald G.
Hoffman Frank P.
Hoffmann-La Roche Inc.
Leon Bernard S.
Rivers Diana G.
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