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 and 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 both 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;CUPPS, THOMAS, LEE;BOGDAN, SOPHIE, LEE;NIKOLAIDES, NICHOLAS;GILBERT, SHERI, ANN;GAZDA, MICHAEL;DOBSON, ROY, LEE, MARTIN;CRUZE, CHARLES, ANDREW, III |
发明人 |
CUPPS, THOMAS, LEE;BOGDAN, SOPHIE, LEE;NIKOLAIDES, NICHOLAS;GILBERT, SHERI, ANN;GAZDA, MICHAEL;DOBSON, ROY, LEE, MARTIN;CRUZE, CHARLES, ANDREW, III |