6,7-dihydro-3-phenyl-1,2-benzisoxazol-4(5H)-ones and -ols, compo

Details 6,7-dihydro-3-phenyl-1,2-benzisoxazol-4(5H)-ones and -ols, compo 6,7-dihydro-3-phenyl-1,2-benzisoxazol-4(5H)-ones and -ols, compo

1991-04-26

1992-05-19

Ramsuer, Robert W.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

514253, 514254, 514318, 514321, 514374, 544137, 544295, 544364, 544368, 546194, 546198, 548241, A61K 3142, A61K 31535, C07D26120, C07D41306

Patent

active

051149362

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 (Y) ##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, lower alkyl or arylloweralkyl, or R.sub.2 and R.sub.3 taken together with the nitogen atom form an optionally substituted heterocycle selected from the group consisting of piperidinyl, pyrrolidinyl, morpholinyl, imidazol-1-yl, 1-piperazinyl, said substituents being hydrogen or loweralkyl; 4-substituted-1-piperazinyl of the formula ##STR3## where R.sub.6 is loweralkyl, aryl, arylloweralkyl, ##STR4## 2-pyrimidyl, ##STR5## 2-pyridinyl of the formula ##STR6## or 4-pyridinyl of the formula ##STR7## 4-substituted-1-piperidinyl of the formula ##STR8## wherein R.sub.7 is hydrogen, loweralkyl, aryl, arylloweralkyl, 2-pyridinyl of the formula ##STR9## 4-pyridinyl of the formula ##STR10## 2-pyrimidinyl of the formula ##STR11## arylcarbonyl, ##STR12## 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.

REFERENCES:
patent: 4010176 (1977-03-01), Kulsa et al.

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