| abstract |
(57) [Summary]nA compound having selective agonist activity at one or both of the α2B and α2C adrenergic receptor subtypes as compared to the α2A adrenergic receptor subtype. The active compound is selected from the group of compounds represented by Formula I below:nEmbedded imagen Wherein the dashed line is any bond, provided that the two double bonds do not share a common carbon atom; R is H or lower alkyl; X is S or C (H) R 1 Where R 1 Is H or lower alkyl, but X and the following ring:nEmbedded imagen When the bond between is a double bond, 1 Does not exist; Y is O, N, S, (CR 1 Two ) y (Where y is an integer of 1 to 3), -CH = CH- or -Y 1 CH Two -(Y 1 Is O, N or S); x is an integer of 1 or 2, where R Two , R Three Or R Four Is bonded to an unsaturated carbon atom, x is 1; Two , R Three Or R Four Is 2 when is attached to a saturated carbon atom; Two Is H, lower alkyl, halogen, hydroxy or lower alkoxy, or, when attached to a saturated carbon atom, R Two May be oxo; R Three And R Four Is each H, lower alkyl, hydroxy, lower alkoxy or phenyl, or is jointly-(C (R Two ) x ) z -;-Y 1 (C (R Two ) x ) z ' -;-Y 1 (C (R Two ) x ) y Y 1 -;-( C (R Two ) x ) -Y 1 − (C (R Two ) x )-;-( C (R Two ) x ) -Y 1 − (C (R Two ) x )-(C (R Two ) x )-And -Y 1 − (C (R Two ) x ) -Y 1 − (C (R Two ) x )-(Where z is an integer of 3-5, z 'is an integer of 2-4, and x and y are defined as above), and these divalent moieties may be at either end Is R Three Or R Four To form a fused ring structure, and the ring formed may be fully unsaturated, partially unsaturated, or fully saturated. ]. The compound may be used for muscle spasms, such as hyperuria, diarrhea, increased urine output, withdrawal syndrome, pain, such as neuropathic pain, neurodegenerative diseases, memory and cognitive deficits, psychosis, such as mania, anxiety, hypertension, cardiac ischemia. , Congestive heart failure, and nasal congestion without sedation or cardiovascular side effects. |