| 摘要 |
Carboxamide derivatives (I) are new. Carboxamide derivatives of formula D-NH-CO-X-CH(R1)-CO-NH-W-Y-T (I) and their derivatives, solvates and stereoisomers are new. D = phenyl or pyridyl (both optionally substituted by halo, A, OR, NRR, NO2, CN, COOR or CONRR); R1 = A optionally substituted with 1-3 of SOmR, SO2NRR, SO3R, S(O)(NR)R, NRSO2R, OSO2R, OSO2NRR or PO(OR)2 and with 1-2 of OR', NR'R', CN, COOR' or CONR'R'; R = H, A or (CR'R')nQ; Q = Ar', Het'., cycloalkyl, NR'R' or OR'; R' = H or A; W = (CR'R')n; X = NR' or O; Y = alkylene, cycloalkylene, Het-diyl or Ar-diyl; T = mono- or bi-cyclic ring system optionally containing 1-4 N, O and/or S heteroatoms (optionally substituted by 1-3 oxo, R, halo, A, (CR'R')n-Ar, (CR'R')n-Het, (CR'R')n-cycloalkyl, OR, NRR, NO2, CN, COOR, CONRR, NRCOA, NRCONRR, NRSO2A, COR, SO2NRR and/or SOnA), or NRR, or R or cycloalkyl if Y is piperidine-1,4-diyl; A = 1-10C alkyl in which 1 or 2 CH2 groups are optionally replaced by O, S or CH=CH (optionally substitutred by 1-7 F); Ar = phenyl, naphthyl or biphenylyl (all optionally substituted by 1-3 halo, A, OR, NRR, NO2, CN, COOR, CONRR, NRCOA, NRCONRR, NRSO2A, COR, SO2NRR, (CR'R')nCOOR, O(CR'R')oCOOR, SO3H or SOnA); Ar' = phenyl optionally substituted by 1-3 halo, A, OR', NR'R', NO2, CN, COOR', CONR'R', NR'COA, NR'CONR'R', NR'SO2A, COR', SO2NR'R', (CR'R')nCOOR', O(CR'R')oCOOR' or SOnA; Het = mono- or bi-cyclic ring system containing 1-4 N, O and/or S heteroatoms (optionally substituted by 1-3 oxo, thioxo, NRR, halo, A, (CR'R')nQ', NO2, CN, NRCONRR, COR, SO2NRR and/or SOnA); Q' = Ar, Het', cycloalkyl, OR, NRR, COOR, CONRR, NRCOA or NRSO2A; Het' = mono- or bi-cyclic ring system containing 1-4 N, O and/or S heteroatoms (optionally substituted by 1-3 oxo, thioxo, NRR, halo, A, OR', NR'R', NO2, CN, COOR', CONR'R', NR'COA, NR'CONR'R', NR'SO2A, COR', SO2NR'R' and/or SOnA); m = 1 or 2; n = 0-2, and o = 1-3. Independent claims are also included for: (1) preparation of (I); (2) medicament comprising at least one compound (I) and optionally another drug, and (3) a kit comprising a compound (I) and another drug in separate packaging.
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