R-6-hydroxy-buspirone
AssigneeBristol-Myers Squibb Company
InventorsJoseph P. Yevich, Robert F. Mayol, Jianqing Li, Frank Yocca
Life of this patent
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Abstract
The R-stereoisomer of 6-hydroxy-buspirone is an effective treatment for anxiety, depression, and other psychogenic disorders. The R-isomer exhibits greater receptor specificity than the S-isomer and should have reduced potential for the adverse effects associated with the racemic mixture and with buspirone.
Claims7
R-6-hydroxy-buspirone, substantially free of its S-stereoisomer, or a pharmaceutically acceptable salt or hydrate thereof.
A method for ameliorating a clinical disorder selected from the following:
- anxiety, depression, and anxiety mixed with depression;
- the method comprising the systemic administration of an effective but non-toxic dose of R-6-hydroxy-buspirone or a pharmaceutically acceptable salt or hydrate thereof.
A pharmaceutical composition comprising R-6-hydroxy-buspirone substantially free of its S-stereoisomer and a pharmaceutically acceptable carrier.
A method of preparing R-6-hydroxy-buspirone comprising the consecutive steps of:
- a) treating buspirone with KN(SiMe3)2 prior to reacting with 2-(phenylsulfonyl)-3-phenyloxaziridine to provide racemic 6-hydroxy-buspirone (I);
- and
- b) separating the enantiomers by means of chiral HPLC chromatography to afford R-6-hydroxy-buspirone (II).
Dependencies are inferred from the claim text.