| 摘要 |
A composition for treating pain comprises an analgesic dose of a muscarinic compound of formula (I)-(III) or (3R,4R)-3-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)-1-azabicyclo[2.2.1]heptane or their salts or solvates; and one or more synergistic analgesics (SA) in a weight ratio of compound to SA of 1 to 1000. R1 = H, 1-6C alkyl or phenyl(1-4C alkyl) optionally Ph-substituted by halo, 1-4C alkyl or 1-4C alkoxy; R2 = 1-6C alkyl, 3-6C alkenyl, 3-6C alkynyl, branched or unbranched with 1-6 C atoms inclusive (sic), and optionally substituted by F, OH, or Ph optionally substituted by F, CF3, lower alkyl, OH or lower alkoxy; R3, R4 = H, 1-6C alkyl, 3-6C cycloalkyl, Ph optionally substituted by halo, CF3, 1-4C alkyl, OH or 1-4C alkoxy, or phenyl(1-4C alkyl) optionally Ph-substituted by halo, 1-4C alkyl or 1-4C alkoxy; R5 = a benzene ring substituted at any position by R6; or naphthyl optionally substituted by R6'; R6, R6' = optionally cyclic 1-8C alkyl, 2-8C alkenyl or 2-8C alkynyl , or NR7R8; R7, R8 = H, linear 1-8C alkyl, 2-8C alkenyl or 2-8C alkynyl; or NR7R8 = carbonaceous heterocyclic group optionally containing another heteroatom, or OR9; R9 = H, optionally cyclic 1-8C alkyl, 2-8C alkenyl or 2-8C alkynyl, or up to 14C aryl, or SR10 or S(O)R11; R10, R11 = optionally cyclic 1-8C alkyl, 2-8C alkenyl or 2-8C alkynyl; R12 = a benzene ring substituted at any position by R13; or naphthyl optionally substituted by R13'; R13, R13' = optionally cyclic 1-8C alkyl, 2-8C alkenyl or 2-8C alkynyl, or NR14R15; R14, R15 = H, linear 1-8C alkyl, 2-8C alkenyl or 2-8C alkynyl; or NR14R15 = carbonaceous heterocyclic group optionally containing another heteroatom, or NO2 or OR12'; R12' = H, optionally cyclic 1-8C alkyl, 2-8C alkenyl or 2-8C alkynyl, or up to 14C aryl, or SR16 or S(O)R17; R16, R17 = as R10, R11. MORE SPECIFICALLY - SA is one or more of NSAID's, acetaminophen, opioids and ~a-adrenergic cpds. |
