| 摘要 |
Compounds having adrenergic activity which are a selective agonists for one or both of the alpha2B and alpha2c adrenoceptor receptor subtypes in preference to the alpha2A adrenoceptor receptor subtype; the active compound being selected from the group consisting of compounds having the formula wherein the dotted lines represent optional bonds provided that two double bonds may not share a common carbon atom; R is H or lower alkyl; X is S or C(H)R1, wherein R1 is H or lower alkyl, but R1 is absent when the bond between X and the ring represented by is a double bond; Y is O, N, S, (CR12)y, wherein y is an integer of from 1 to 3, -CH=CH- or -Y1CH2-, wherein Y1 is O, N or S; x is an integer of 1 or 2, wherein x is 1 when R2, R3 or R4 is bound to an unsaturated carbon atom and x is 2 when R2, R3 or R4 is bonded to a saturated carbon atom; R2 is H, lower alkyl, halogen, hydroxy, lower alkoxy, lower alkenyl, acyl or lower alkynyl, or, when attached to a saturated carbon atom, R2 may be oxo; R3 and R4 are, each, H, lower alkyl, halogen, lower alkenyl, acyl, lower alkynyl, aryl, heteroaryl, or sub stituted aryl or heteroaryl, wherein said substituent is halogen, lower alkyl, lower alkoxy, lower alkenyl, acyl, lower alkynyl, nitro, cyano, trifluoromethyl, hydroxy, or phenyl or, together, are -(C(R2)x)z-; -Y1(C(R2)x)z'-; -Y1(C(R2)x)y Y1-; -(C(R2)x)-Y1-(C(R2)x)-; -(C(R2)x)-Y1-(C(R2)x)-(C(R2)x)- and -Y1-(C(R2)x)-Y1-(C(R2)x)- wherein z is an integer of from 3 to 5, z' is an integer of from 2 to 4 and x and y are as defined above, and further either end of each of these divalent moieties may attach at either R3 or R4 to form a condensed ring structure and the rings formed may be totally unsaturated, partially unsaturated, or totally saturated; and being useful for treating muscle spasticity including hyperactive micturition, diarrhea, diuresis, withdrawal syndromes, pain including neuropathic pain, neurodegenerative diseases, memory and cognition deficits, psychoses including manic disorders a
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