6,7-dihydro-3-phenyl-1,2-benzisoxazol-4(5H)-one, composition and

Details 6,7-dihydro-3-phenyl-1,2-benzisoxazol-4(5H)-one, composition and 6,7-dihydro-3-phenyl-1,2-benzisoxazol-4(5H)-one, composition and

1992-12-13

1993-10-26

Ramsuer, Robert W.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

546198, A61K 31445, C07D41302

Patent

active

052566722

ABSTRACT:
This invention relates to 6,7-dihydro-3-phenyl-1,2-benzisoxazol-4(5H)-ones and -ols of the formula ##STR1## wherein X is ##STR2## or loweralkyl; Y is hydrogen, halogen, loweralkyl, loweralkoxy, trifluoromethyl, nitro or amino; R is H when the bond between the oxygen atom and the carbon atom in question is a single bond; otherwise the dotted line signifies part of a double bond to the oxygen atom; R.sub.1 is hydrogen, loweralkyl or arylloweralkyl; R.sub.2 and R.sub.3 are independently hydrogen, loweralkyl or arylloweralkyl, or R.sub.2 and R.sub.3 taken together with the nitrogen atom form an optionally substituted heterocycle selected from the group consisting of piperidinyl, pyrtolidinyl, morpholinyl, imidazol-1-yl, 1-piperazinyl, said substituents being hydrogen or loweralkyl; 4-substituted-1-piperazinyl of the formula where R.sub.6 is loweralkyl, aryl, arylloweralkyl, ##STR3## 2-pyrimidyl, ##STR4## 2-pyridinyl of the formula ##STR5## or 4-pyridinyl of the formula ##STR6## 4-substituted-1-piperidinyl of the formula ##STR7## wherein R.sub.7 is hydrogen, loweralkyl, aryl, arylloweralkyl, 2-pyridinyl of the formula ##STR8## 4-pyridinyl of the formula ##STR9## 2-pyrimidinyl of the formula arylcarbonyl, ##STR10## R.sub.8 is hydrogen or --OH; R.sub.4 is hydrogen, loweralkoxycarbonyl or aryloxycarbonyl; Z is chlorine, bromine or fluorine; m is an integer of 1 to 4; n is an integer of 1 to 4 or a pharmaceutically acceptable acid addition salt thereof and where applicable the geometric and optical isomers and racemic mixtures thereof. The compounds of this invention display utility as antipsychotic agents and analgesic agents.

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