| 摘要 |
Novel dihydro benzo furan spiroamines of formula (I), their salts, hydrates and solvates are claimed, where A = H,H, or -CH2CH2-, or -CH=CH-; Z1 = CO, SO2, (CH2)(m+1), CO(CH2)m, SO2(CH2)m, (CH2)mCO, CO(CH2)mSO2, SO2(CH2)mSO2, CO(CH2)mCO, SO2(CH2)mCO; m = 1-6; X-Y = NCH2, NCH2CH2, C=CH, CR1-CH2; R1 = H, halogen, OH, NH2, CN, NO2, R2, OR2, SR2, NHR2, COR2, CHOHR2, COOR2, NHCOR2, NHCOOR2, NHSO2R2, OCONHR2; R2 = 11-5C alkyl, aryl or alkyl aryl in which the aryl group is selected from phenyl, naphthyl or pyridyl optionally substituted by one or more of 1-5C alkyl, halogen, OH, OR3, SR3, CF3, CH2CF3, NO2, CN, COR3, COOR3, NHR3, NHCOR3, NHCOOR3, NHSO2R3, SO2R3; R3 = H or 1-5C alkyl, Z2 is either omitted or represents (CH2)n, (CH2)nCO, CO, CO(CH2)n, O(CH2)n, O(CH2)nCO, OCO, NH(CH2)n, NH(CH2)nCO, NHCO, NHCO(CH2)n, NHSO2(CH2)n, CH=CHCO, C?=C-CO, SO2, SO2(CH2)n, NH(CH2)nSO2, NHSO2(CH2)nSO2, O(CH2)nSO2; and when X-Y = CHCH2, then Z2 may further be O, NH, CONH, SO2NH, OCONH, NHCOO, NHCONH, (CH2)nNH, (CH2)nO, CO(CH2)nNH, NH(CH2)nO, NH(CH2)nNH, O(CH2)nNH, O(CH2)nO, CO(CH2)nO, SO2(CH2)nNH, SO2(CH2)nO, (CH2)nSO2NH, (CH2)nCONH, O(CH2)nSO2NH, O(CH2)nCONH, NH(CH2)nSO2NH, NH(CH2)nCONH, NHCO(CH2)nNH, NHSO2(CH2)nNH; and when X-Y = CR1-CH2 or C=CH, Z2 may further be -CH=CH- or -C?=C-; n = 1-6; Ar = phenyl, naphthyl or pyridyl, optionally substituted by 1 or more groups selected from 1-6C alkyl, CF3, CF3O, CF3CH2, phenyl, benzyl, 3-7C cycloalkyl, OH, SH, OR4, SR4, NO2, CN, NH2, NR4R4', an amine derivative, halogen, or carbonyl, a heterocycle optionally substituted, or Ar-Z2 may represent a tetrahydronaphthyl group in which the link with X is through a saturated C atom; R4 = 1-6C alkyl; and R4' = H or 1-6C alkyl.
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