CRAMP, MICHAEL COLIN,ARIENZO, ROSA,HYND, GEORGE,CRACKETT, PETER,GRIFFON, YANN,HARRISON, TREVOR KEITH,RAY, NICHOLAS CHARLES,FINCH, HARRY,MONTANA, JOHN GARY
申请号：
CA2622000
公开号：
CA2622000C
申请日:
2006.09.29
申请国别(地区):
CA
年份:
2014
代理人:
摘要：
Compounds of formula [1] are CRTH2 antagonists, useful in the treatment ofconditions having an inflammatory component； in which: R1, R2, R3, R4 and R5are independently hydrogen, C1-C6alkyl, C1- C6fluoroalkyl, cyclopropyl, halo, -S(O)nR6, -SO2NR7R8, -NR7R8, -NR7C(O)R6, -CO2R7, -C(O)NR7R8, -C(O)R6, -NO2, -CNor a group -OR9； wherein each R6 is independently C1-C6alkyl, C1-C6fluoroalkyl, cycloalkyl, aryl, or heteroaryl； R7, R8 are independently C1-C6alkyl, C1-C6fluoroalkyl, cycloalkyl, cycloalkyl-(C1-C6alkyl)-, aryl,heteroaryl or hydrogen； R9 is hydrogen, C1-C6alkyl, C1-C6fluoroalkyl,cycloalkyl, cylcoalkyl-(C1-C6alkyl)-, or a group -SO2R6； A is -CHR10-, -C(O)-,-S(O)n-, -0-, or -NR10- wherein n is an integer from 0-2 and R10 is hydrogen,C1-C3alkyl, or C1-C6fluoroalkyl group； B is a direct bond, or a divalentradical selected from -CH2-, -CH2CH2-, -CHR11-, -CR11R12-, -CH2CHR11-, -CH2CR11R12-, -CHR11CHR12-, and divalent radicals of formula -(CR11R12)P-Z-wherein Z is attached to the ring carrying R1, R2 and R3； wherein R11 is C1-C3alkyl, cyclopropyl, C1-C6fluoroalkyl； R12 is methyl or fluoromethyl； p isindependently 1 or 2； and Z is -0-, -NH-, or -S(O)n-, wherein n is an integerfrom 0-2； X is a carboxylic acid, tetrazole, 3-hydroxyisoxazole, hydroxamicacid, phosphinate, phosphonate, phosphonamide, or sulfonic acid group, or agroup of formula C(=O)NHSO2R6or SO2NHC(=O)R6； and Y is aryl, heteroaryl, aryl-fused- heterocycloalkyl, heteroaryl-fused-cycloalkyl, heteroaryl-fused-heterocycloalkyl or aryl-fused-cycloalkyl group.
