8H-Pyrazolo[1,5-a]pyrazolo[4',3':5,6]pyrido[3,4-e]pyrimidine
AssigneeE. R. Squibb & Sons, Inc.
InventorsTheodor Denzel, Hans Hoehn
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Abstract
New derivatives of 8H-pyrazolo[1,5-a]pyrazolo[4',3':5,6]pyrido[3,4-e]pyrimidine have the general formula ##STR1## The compounds are useful as anti-inflammatory agents and central nervous system depressants.
Claims10
A compound of the formula ##STR18## wherein R.sup.1 is hydrogen, lower alkyl, phenyl, phenyl-lower alkylene, benzoyl or substituted benzoyl wherein the benzoyl substituent is one or two halogens, lower alkyl or trifluoromethyl groups;
- R.sup.2 and R.sup.3 each is hydrogen, lower alkyl or phenyl;
- R.sup.4 is hydrogen, lower alkyl, phenyl, carboxy or lower alkoxycarbonyl;
- R.sup.5 is;
- ##STR19## R.sup.6 is hydrogen or lower alkyl;
- R.sup.7 and R.sup.8 together with the nitrogen form one of the unsubstituted or substituted heterocyclics pyrrolidino, morpholino, thiamorpholino, piperidino, pyrazolyl, dihydropyridazinyl or piperazinyl wherein the heterocycle substituent is lower alkyl or hydroxy-lower alkyl;
- and acid addition salts thereof.
The compound of claim 1, 8-ethyl-2-methyl-5-(4-methyl-1-piperazinyl)-8H-pyrazolo[1,5-a]pyrazolo[4', 3':5,6]pyrido[3,4-e]-pyrimidine.
The compound of claim 1, 8-ethyl-2-methyl-5-(1-piperidinyl)-8H-pyrazolo[1,5-a]pyrazolo[4',3':5,6]py rido[3,4-e]-pyrimidine.
The compound of claim 1, 8-ethyl-2-methyl-5-(4-morpholinyl)-8H-pyrazolo[1,5-a]pyrazolo[4',3':5,6]py rido[3,4-e]pyrimidine.
The compound of claim 1, 8-ethyl-5-(4-methyl-1-piperazinyl)-8H-pyrazolo[1,5-a]pyrazolo[4',3':5,6]py rido[3,4-e]pyrimidine-3-carboxylic acid, ethyl ester.
The compound of claim 1, 8-ethyl-5-(1-piperidinyl)-8H-pyrazolo[1,5-a]pyrazolo[4',3':5,6]pyrido[3,4- e]pyrimidine-3-carboxylic acid, ethyl ester.
Dependencies are inferred from the claim text.