C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 261/20 (2006.01) A61K 31/33 (2006.01) C07D 413/06 (2006.01) C07D 413/08 (2006.01) C07D 413/12 (2006.01) C07D 413/14 (2006.01) C07D 417/12 (2006.01) C07D 417/14 (2006.01)
Patent
CA 2049733
This invention relates to 6,7-dihydro-3-phenyl-1,2-benzisoxazol-4(5H)-ones and -ols of the formula (see Formula I) wherein X is (see Formula II) 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; R1 is hydrogen, loweralkyl or arylloweralkyl; R2 and R3 are independently hydrogen, loweralkyl or arylloweralkyl, or R2 and R3 taken together with the nitrogen 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 (see Formula III) 9 where R6 is loweralkyl, aryl, arylloweralkyl, (see Formula IV, V) 2-pyrimidyl, 2 Image , 2-pyridinyl of the formula Image or 4-pyridinyl of the formula Image ; 4-substituted-1-piperidinyl of the formula Image , wherein R7 is hydrogen, loweralkyl, aryl, arylloweralkyl, 2-pyridinyl of the formula Image , 4-pyridinyl of the formula Image , 2-pyimidinyl of the formula Image arylcarbonyl, Image ; R8 is hydrogen or -OH; R4 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.
Nemoto Peter Allen
Shutske Gregory Michael
Wettlaufer David Gordon
Aventis Pharmaceuticals Inc.
Bereskin & Parr Llp/s.e.n.c.r.l.,s.r.l.
Hoechst-Roussel Pharmaceuticals Inc.
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