摘要 |
The present invention is directed to compounds having a structure according formula (I), wherein: (a) R1 is alkyl; (b) R2 is selected from the group consisting of: hydrogen, alkyl, methoxy, cyano, and halo; (c) R3 is selected from the group consisting of: hydrogen, methyl, hydroxy, cyano and halo; (d) R4 is selected from the group consisting of: hydrogen, methyl, ethyl and isopropyl; (e) R5 is selected from the group consisting of: hydrogen, methyl, amino, methoxy, hydroxy, cyano an d halo; (f) provided that at least one of R2, R3, R4 or R5 is other than hydrogen or fluorine; (g) provided that when R1 is methyl and bot h R2 and R5 are hydrogen, R3 is other than methyl or halo; (h) provided that when R3 is cyano, R1 is methyl; and any tautomer of the structure or a pharmaceutically acceptable salt, or biohydrolyzable ester, amide, or imide thereof. The compounds of the present invention are peripherally acting selective alpha-2 adrenergic compounds that lower CNS activity and that resist metabolic transformation into undesirable compounds.
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申请人 |
THE PROCTER & GAMBLE COMPANY |
发明人 |
BOGDAN, SOPHIE EVA;CUPPS, THOMAS LEE;NIKOLAIDES, NICHOLAS;CRUZE, CHARLES ANDREW III;DOBSON, ROY LEE MARTIN;GAZDA, MICHAEL;GILBERT, SHERI ANN |