Serotonergic agents with long-acting in vivo effects
AssigneeWyeth
InventorsWayne E. Childers, Michael G. Kelly, Lee E. Schechter, Sharon J. Rosenzweig-Lipson
Life of this patent
Estimating the term…
Abstract
Compounds of the formula 1 have a long duration of action and are useful for the treatment of chronic diseases resulting from the dysfunction of the serotonergic 5-HT1A system, such as schizophrenia and other psychotic disorders such as paranoia and mano-depressive illness.
Claims28
A labeled compound according to formula I:
- 9
- wherein
- R1=H or lower alkyl of 1-4 carbon atoms,
- R2=H or lower alkyl or 1-4 carbon atoms;
- R3 is I and p is 0 or 1, and pharmaceutical salts thereof.
A method of treating a patient suffering from a chronic condition resulting from the dysfunction of the serotonergic 5-HT1A system comprising providing a therapeutically effective amount of compound of Formula I
- 10
- wherein
- R1=H or lower alkyl of 1-4 carbon atoms, and
- R2=H or lower alkyl or 1-4 carbon atoms, and pharmaceutical salts thereof, to a patient in need thereof, said effective dose being administered no more than once during a seven day period.
A method of potentiating the action of an inhibitor of serotonin reuptake comprising administering to a patient in need thereof in combination with a compound of Formula I
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- wherein
- R1=H or lower alkyl of 1-4 carbon atoms, and
- R2=H or lower alkyl or 1-4 carbon atoms, and pharmaceutical salts thereof, said effective dose being administered no more than once during a seven day periods, in combination with an inhibitor of serotonin reuptake.
A method of testing the effects of long term 5-HT1A receptor occupancy in a population of cells comprising contacting said cells with a labeled compound of Formula I
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- wherein
- R1=H or lower alkyl of 1-4 carbon atoms,
- R2=H or lower alkyl or 1-4 carbon atoms;
- R3 is I and p is 0 or 1, and pharmaceutical salts thereof.
A pharmaceutical composition comprising a compound of Formula I
- 13
- wherein
- R1=H or lower alkyl of 1-4 carbon atoms, and
- R2=H or lower alkyl or 1-4 carbon atoms, and pharmaceutical salts thereof, an inhibitor of serotonin reuptake, and a pharmaceutically acceptable carrier or excipient.
Dependencies are inferred from the claim text.