| 摘要 |
A COMPOUND OF GENERAL FORMULA (1), OR PHARMACEUTICALLY ACCEPTABLE SALTS, SOLVATES OR POLYMORPHS THEREOF WHEREIN; R AND R2, WHICH MAY BE THE SAME OR DIFFERENT, ARE HYDROGEN, C1-C6 ALKYL, (CH2)M (C3-C6 CYCLOALKYL) WHEREIN M =0, I, 2 OR 3, OR R1 AND R2 TOGETHER WITH THE NITROGEN TO WHICH THEY ARE ATTACHED FORM AN AZETIDINE RING; EACH R3 IS INDEPENDENTLY CF3, OCF3, C1-4ALKYLTHIO OR C1-C4ALKOXY; N IS 1, 2 OR 3; AND R4 AND R5, WHICH MAY BE THE SAME OR DIFFERENT, ARE: A-X, WHEREIN A= - CH=CH – OR - (CH2) - WHERE P IS 0, 1 OR 2; X IS HYDROGEN, F, C1, BR, 1, CONR6 R7, SO2 NR6R7, SO2 NHC (=O)R6, OH, C1-4ALKOXY, NR8 SO2 R9, NO2, NR6R11, CN, CO2 R10, CHO, SR10, S(O)R9 OR SO2 R10 ; R6, R7, R8 AND R10 WHICH MAY BE THE SAME OR DIFFERENT, ARE HYDROGEN OR C1-6AIKYL OPTIONALLY SUBSTITIITED INDEPENDENTLY BY ONE OR MORE R12 R9 IS C1-6ALKYL OPTIONALLY SUBSTITUTED INDEPENDENTLY BY ONE OR MORE R12 ; R11 IS HYDROGEN, C1-6ALKYJ OPTIONALLY SUBSTITUTED INDEPENDENTLY BY ONE OR MORE R12 , C(O)R6, CO2 R9, C(O)NHR6 OR SO2 NR6 R7 R12 IS F, OH, CO2 H, C3-6CYCLOALKYL, NH2, CONH2, C1-6ALKOXY, C1-6ALKOXYCARBONYL OR A 5- OR 6-MEMBERED HETEROCYCLIC RING CONTAINING 1, 2 OR 3 HETEROATOMS SELECTED FROM N, S AND 0 OPTIONALLY SUBSTITUTED INDEPENDENTLY BY ONE OR MORE R13 OR R6 AND R7, TOGETHER WITH THE NITROGEN TO WHICH THEY ARE ATTACHED, FORM A 4-, 5- OR 6-MEMBERED HETEROCYCLIC RING OPTIONALLY SUBSTITUTED INDEPENDENTLY BY ONE OR MORE ; OR A 5- OR 6-MEMBERED HETERO CYCLIC RING CONTAINING 1, 2 OR 3 HETEROATOMS SELECTED FROM N, S AND 0, OPTIONALLY SUBSTITUTED INDEPENDENTLY BY ONE OR MORE R13 ; WHEREIN R13 IS HYDROXY, C1-C4ALKOXY, F, C1-C6ALKYL, HALOALKY1, HALOALKOXY, —NH2, —NH(C1-C6ALKYL) OR N(C1 - C6ALKYL)2; WHEREIN WHEN R1 AND R2 ARE METHYL, R4 AND R5 ARE HYDROGEN AND N IS I, R3 IS NOT A —SME GROUP PARA TO THE ETHER LINKAGE LINKING RINGS A AND B. |
