Phenyl and heterocyclic piperazinyl alkoxy-benzheterocyclic compounds as antipsychotic agents
First Claim
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1. A compound of the formula ##STR9## in which Het is selected from the group consisting of ##STR10## n is an integer from two to five;
- A is phenyl or phenyl substituted by loer alkyl, lower alkoxy, lower thioalkoxy, halogen or trifluoromethyl;
2-, 3- or 4-pyridinyl or 2-, 3- or 4-pyridinyl substituted by lower alkyl, lower alkoxy or halogen;
2-, 4- or 5-pyrimidinyl, or 2-, 4- or 5-pyrimidinyl substituted by lower alkyl, lower alkoxy or halogen;
2-pyrazinyl or 2-pyrazinyl substituted by lower alkyl, lower alkoxy or halogen;
2- or 3-thienyl or 2- or 3-thienyl substituted by lower alkyl or halogen;
2- or 3-furanyl or 2- or 3-furanyl substituted by lower alkyl or halogen, or 2- or 5-thiazolyl or 2- or 5-thiazolyl substituted by lower alkyl or halogen, or a pharmaceutically acceptable acid addition salt thereof, with the exclusion of the compound wherein Het is ##STR11## and A is phenyl or substituted phenyl.
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Abstract
Novel phenyl and heterocyclic tetrahydropyridyl and piperazinyl alkoxy benzheterocyclic compounds are described which have valuable neuroleptic properties by virture of their dopamine autoreceptor agonist activity. Methods of preparation, pharmeceutical compositions, and methods for treating psychoses, such a schizophrenia, are also described.
30 Citations
22 Claims
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1. A compound of the formula ##STR9## in which Het is selected from the group consisting of ##STR10## n is an integer from two to five;
- A is phenyl or phenyl substituted by loer alkyl, lower alkoxy, lower thioalkoxy, halogen or trifluoromethyl;
2-, 3- or 4-pyridinyl or 2-, 3- or 4-pyridinyl substituted by lower alkyl, lower alkoxy or halogen;
2-, 4- or 5-pyrimidinyl, or 2-, 4- or 5-pyrimidinyl substituted by lower alkyl, lower alkoxy or halogen;
2-pyrazinyl or 2-pyrazinyl substituted by lower alkyl, lower alkoxy or halogen;
2- or 3-thienyl or 2- or 3-thienyl substituted by lower alkyl or halogen;
2- or 3-furanyl or 2- or 3-furanyl substituted by lower alkyl or halogen, or 2- or 5-thiazolyl or 2- or 5-thiazolyl substituted by lower alkyl or halogen, or a pharmaceutically acceptable acid addition salt thereof, with the exclusion of the compound wherein Het is ##STR11## and A is phenyl or substituted phenyl. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22)
- A is phenyl or phenyl substituted by loer alkyl, lower alkoxy, lower thioalkoxy, halogen or trifluoromethyl;
Specification
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Current AssigneeWarner-Lambert Company (Pfizer Inc.)
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Original AssigneeWarner-Lambert Company (Pfizer Inc.)
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InventorsDeWald, Horace A., Jaen, Juan C., Caprathe, Bradley W., Wise, Lawrence D.
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Primary Examiner(s)Raymond, Richard L.
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Application NumberUS07/062,752Time in Patent Office602 DaysField of Search544/105, 544/295, 544/357, 544/360, 544/363, 544/369, 544/370, 544/373, 544/376, 514/234, 514/239, 514/253, 514/230.5US Class Current514/230.5CPC Class CodesC07D 209/34 in position 2C07D 215/20 Oxygen atomsC07D 217/02 with only hydrogen atoms or...C07D 235/06 with only hydrogen atoms, h...C07D 307/79 with only hydrogen atoms, h...C07D 307/83 Oxygen atomsC07D 311/22 with oxygen or sulfur atoms...C07D 401/12 linked by a chain containin...C07D 403/12 linked by a chain containin...C07D 405/12 linked by a chain containin...C07D 413/12 linked by a chain containin...
