| abstract |
Compounds having adrenergic activity which are a selective agonists for one or both of the α 2B and α 2c adrenoceptor receptor subtypes in preference to the α 2A adrenoceptor receptor subtype; the active compound being selected from the group consisting of compounds having the formula n n n 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)R 1 , wherein R 1 is H or lower alkyl, but R 1 is absent when the bond between X and the ring represented by n n n is a double bond; Y is O, N, S, (CR 1 2 ) y , wherein y is an integer of from 1 to 3, —CH═CH— or —Y 1 CH 2 —, wherein Y 1 is O, N or S; x is an integer of 1 or 2, wherein x is 1 when R 2 , R 3 or R 4 is bound to an unsaturated carbon atom and x is 2 when R 2 , R 3 or R 4 is bonded to a saturated carbon atom; R 2 is H, lower alkyl, halogen, hydroxy, lower alkoxy, lower alkenyl, acyl or lower alkynyl, or, when attached to a saturated carbon atom, R 2 may be oxo; R 3 and R 4 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(R 2 )x)z—; —Y 1 (C(R 2 )x)z′—; —Y 1 (C(R 2 )x)y Y 1 —; —(C(R 2 )x)—Y 1 —(C(R 2 )x)—; —(C(R 2 )x)—Y 1 —(C(R 2 )x)—(C(R 2 )x)— and —Y 1 —(C(R 2 )x)—Y 1 —(C(R 2 )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 and anxiety, hypertension, cardiac ischemia, congestive heart failure, and nasal congestion without sedating or cardiovascular side effects. |