| 摘要 |
Multicyclic derivs. of formula (I) and their salts are new: A1 = C or N; E = 5-6 membered heteroaromatic or 6 membered aromatic ring opt. substd. by R3 or R4; X1-X2 = CHR1CH, CR1=CH, NR1CH, SOuCH or OCH; X3 = CR5R5', NR5, SOu or O; R' = H, 1-6C alkyl, 3-7C cycloalkyl-0-4C alkyl or Ar-0-4C alkyl; R" = R', COR' or CO2R5; R"' = 1-6C alkyl, 3-7C cycloalkyl-0-4C alkyl or Ar-0-4C alkyl; R1 = H, 1-6C alkyl, 3-7C cycloalkyl-0-4C alkyl or Ar-0-4C alkyl; R2 = OR', NR'R", NR'SO2R"', NR' OR', OCR'2CO2R', OCR'2OCOR', OCR'2CONR'2, CF3 or COCR'2R2'; R2' = OR', CN, SOrR', SO2NR'2, COR'CONR'2 or CO2R'; R5, R5' = H, 1-6C alkyl, 3-7C cycloalkyl-0-4C alkyl or Ar-0-4C alkyl; R6 = W(CR'2)q Z(CR'R10)r U(CR'2)5 V or W'(CR'2)qU(CR'2)s; R3, R4, R7 = H, halo, OR12, SR12, CN, NR'R12, NO2, CF3, CF3SOr, CO2R', CONR'2, R14-0-6C alkyl, R14-1-6C oxoalkyl, R14 2-6C alkenyl, R14-2-6C alkynyl, R14-0-6C alkoxy, R14-0-6C alkylamino or R14-0-6C alkyl-SOr; R8 = R', COR', CN, NO2, SO2R' or CO2R5; R9 = R', CF3, SR' or OR'; R10 = H, 1-4C alkyl or NR'R"; R12 = R', COR', CONR'2, CO2R5, SOmR' or SO2NR'2; R14 = H, 3-6C cycloalkyl, Het or Ar; R15 = H, 1-10C alkyl, 3-7C cycloalkyl-0-8 C alkyl or Ar-0-8C alkyl; U, V = absent or CO, CR'2, C(= CR15 2) (sic), SOn, O, NR15, CR15' OR15, CR'(OR")CR'2, CR'2CR'(OR"), COR'2, CR15 2 CO, CONR15, NR15CO, OC(O), CO2, C(S)O, OC(S), C(S)NR15, NR15C(S), SO2NR15, NR15SO2, N=N, NR15NR15, NR15C(R15)2, NR15C(R15)2, C(R15)2O, OC(R15)2, C?=C, CR15 = CR15, Het or Ar; provided that U and V are not both absent; W = R'R"N, R'R"NR'N, R'R"NR'NCO, (R')2NR'NC(=NR'), R'ONR'C(=NR')-, (R'2N)C(R9)=N-, (R'2N)2C=N-, R9C(=NR")NR', R"R'NC(=NR')Y, R"R'NC(=NR')NR'X-, R"R'NC(=NR8)NR' or a nitrogen contg. ring; W' = a gp. of e.g. formula (a) and (b); Q = NR', O or S; Ra = H, 1-6C alkyl, Ar-0-6C alkyl, Het-0-6C alkyl, 3-6C cycloalkyl 0-6C alkyl, halo, OR1, SR1, COR1, OH, NO2, N(R1)2, CO(NR1)2 or CH2N(R1)2; Rb, Rc = H, 1-6C alkyl, Ar-0-6C alkyl, Het-0-6C alkyl, 3-6C cycloalkyl-0-6C alkyl, halo, OR1, SR1, COR1, OH, NO2, N(R1)2, CO(NR1)2 or CH2N(R1)2; or Rb+Rc = 5-6 membered opt. aromatic ring opt. substd. by halo, 1-4C alkyl, OR1, SR1, COR1, OH, NO2, N(R1)2, CO(NR1)2, CH2N(R1)2, CN or R"R'NC(=NR'); X = NCR', CO or O; Y = absent, S or O; Z = (CH2)t, Het, Ar or 3-7C cycloalkyl; m = 1-2; q, n = 0-3; r-u = 0-2; v, w = 0-1; Ar = ph or naphthyl opt. substd. by 1-3 R7; R7 = 1-4C alkyl, 1-4C alkoxy, 1-4C alkylthio, trifluoroalkyl, OH, Cl, F, Br or I; Het = 5-6 membered monocycle or 9-10 membered bicycle contg. 1-3 N, O or S. opt. substd. by 1-3 R7. |
