| 摘要 |
<p>Compounds of formula (I): wherein:R1 represents C3-8 cycloalkyl-Y1-, aryl-Y1-, heteroaryl-Y1-, aryl- G-Y1-, heteroaryl-G-Y1-, C1-6 alkyl-G-Y1-, J1-Y1-, R22R23N-Y1-, R22R23N-CO-Y1- or R24-CONR22-Y1-; Q represents -(CR19R20)(CR19aR20a)t-, wherein t represents an integer from 0 to 3;R2 and R3 independently represent hydrogen or C1-6 alkyl;X represents ethylene or a group of formula CReRf wherein Re and Rf independently represent hydrogen or C1-4 alkyl or Re and Rf may together with the carbon atom to which they are attached form a C3-8 cycloalkyl group; R4 and R5 independently represent hydrogen or C1-4 alkyl; Z represents a bond, CO, SO2, CR10R7(CH2)n, (CH2)nCR10R7, CR10R7(CH2)nO, CR10R7(CH2)nS, CR10R7(CH2)nCO, COCR10R7(CH2)n or SO2CR10R7(CH2)n; R6 represents aryl, heteroaryl or aryl-C2-6 alkenyl-; R7 represents hydrogen, C1-4 alkyl, CONR8R9 or COOC1-6 alkyl;a and b represent 1 or 2, such that a+b represents 2 or 3;G represents -S-, -SO2-, -SO2NR21, -NR21SO2 or -NR21-; n represents an integer from 0 to 4; J1 independently represents a moiety of formula (K): wherein X1 represents oxygen, NR11 or sulphur, X2 represents CH2, oxygen, NR12 or sulphur, m1 represents an integer from 1 to 3, m2 represents an integer from 1 to 3, provided that m1+m2 is in the range from 3 to 5, also provided that when both X1 and X2 represent oxygen, NR11, NR12 or sulphur, m1 and m2 must both not equal less than 2, wherein K is optionally substituted by one or more (eg. 1 or 2) -Y3-aryl, -Y3-heteroaryl, -Y3-CO-aryl, -Y3-CO-heteroaryl, -C1-6 alkyl, -Y3-COOC1-6 alkyl, -Y3-COC1-6 alkyl, -Y3-W, -Y3-CO-W, -Y3-NR15R16, -Y3-CONR15R16, hydroxy, oxo, -Y3-SO2NR15R16, -Y3-SO2C1-6 alkyl, -Y3-SO2aryl, -Y3-SO2heteroaryl, -Y3-NR13C1-6 alkyl, -Y3-NR13SO2C1-6 alkyl, -Y3-NR13CONR15R16, -Y3-NR13COOR14 or -Y3-OCONR15R16 groups, and is optionally fused to a monocyclic aryl or heteroaryl ring;R8, R9, R10, R11, R12, R13 and R14 independently represent hydrogen or C1-6 alkyl; R15 and R16 independently represent hydrogen or C1-6 alkyl or R15 and R16 together with the nitrogen atom to which they are attached may form a morpholine, piperidine or pyrrolidine ring; R17, R18, R19, R20, R19a, R20a, and R21 independently represent hydrogen or C1-4 alkyl; R22 and R23 independently represent hydrogen, C1-6 alkyl, C3-8 cycloalkyl or C3-8cycloalkylC1-6alkyl; R24 represents C1-6 alkyl, C3-8 cycloalkyl, aryl or heteroaryl; W represents a saturated or unsaturated, non-aromatic 5-7 membered ring containing between 1 and 3 heteroatoms selected from nitrogen, oxygen or sulphur, optionally substituted with one or more C1-6 alkyl, halogen or hydroxy groups; Y1 and Y3 independently represent a bond or a group of formula - (CH2)pCRcRd(CH2)q- wherein Rc and Rd independently represent hydrogen or C1-4alkyl or Rc and Rd may together with the carbon atom to which they are attached form a C3-8cycloalkyl group, and p and q independently represent an integer from 0 to 5 wherein p + q is an integer from 0 to 5; and salts and solvates thereof are CCR3 receptor antagonists and thus are indicated to be useful in therapy. </p> |
