New 1-aryl-4-(biarylmethylene)piperazines as potential atypical antipsychotics sharing dopamine D2-receptor and serotonin 5-HT1A-receptor affinities
This paper describes the syntheses of several 1-aryl-4-(biarylmethylene)piperazines and the results of the determination of their affinity for D2 and 5-HT1A receptors. A selection of these compounds was evaluated in vivo, resulting in the identification of a drug candidate which is being clinically evaluated as a potential atypical antipsychotic with reduced extrapyrimidal side effects.
Feenstra, Rolf W,De Moes, Janpeter,Hofma, Jos J,Kling, Henk,Kuipers, Wilma,Long, Stephen K,Tulp, Martin Th.M,Van der Heyden, Jan A.M,Kruse, Chris G
Improved synthesis of antipsychotic drug bifeprunox
A new and efficient six-step synthesis of the antipsychotic drug bifeprunox is reported. The key step is azidation of a lithiated phenol ether. Subsequent reduction of the azide, removal of phenol protecting group, and cyclization lead to the desired benzoxazolinone.
3H-BENZOOXAZOL-2-ONE MODULATORS OF D2 RECEPTOR AND/OR 5-HT1A RECEPTOR
The present invention relates to new 3H-benzooxazol-2-one modulators of D2 receptors and/or 5-HT1A receptors, pharmaceutical compositions thereof, and methods of use thereof.
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(2010/06/11)
Stable crystalline form of bifeprunox mesylate, dosage forms thereof and methods for using same
The present disclosure provides novel pharmaceutical compounds and methods for making the same, novel pharmaceutical dosage forms and methods for making the same, and methods for using said compounds and dosage forms to treat and prevent diseases and/or d
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(2008/06/13)
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