Patent ID: 6492351
Filing Date: 2002-12-10
Classification: A61K,C07D

Abstract:
A method for the treatment of pruritus in a patient comprising administering to said patient an effective amount of a compound of formula IIA or a pharmaceutically acceptable salt thereof whereinn=1-3, R1 and R2 are independently &boxH;CH3; â€”(CH2)m, where m=4-8, â€”CH2CH(OR)(CH2)2â€” wherein R is H, alkyl, acyl or aroyl; CH2CH(F)(CH2)2â€”; â€”(CH2)2O(CH2)2â€”; or â€”(CH2)2CH&boxH;CHCH2â€”; Ar=mono- or di-substituted phenyl; wherein said substituents are selected from the group consisting of halogen, OCH3, OH, SO2CH3, CF3, NH2, alkyl, CN, unsubstituted and substituted sulfamoyl groups; or Ar substituted with â€”NH(CH2)uCO2Râ€²; â€”NH(CH2)u(CH&boxH;CH)u(CH2)CO2Râ€²; â€”NHCO(CH2)u(CH&boxH;CH)u(CH2)uCO2Râ€²; â€”NHP(O)(OBn)2; â€”NHP(O)(ORâ€²)2; â€”(CH2)uNHSO2CH3; â€”(CH2)uNHC(S)NHCH(CO2Râ€²)(CH2)uCO2Râ€²; â€”CONHOH; or â€”(CH2)uCONHOH; â€ƒwherein u=0-5; Râ€²=H or lower alkyl; or Ar is R6=â€”H or â€”Ac X8=â€”CO2H; â€”NHSO2CH3; â€”NHP(O)(OBn)2; â€”NHP(O)(OH)2; â€”OP(O)(OBn)2; or â€”OP(O)(OH)2; R7=â€”NH(CH2)vCO2H; â€”NH(CH2)vCH(NH2)(CO2H); â€”NHCH(CO2H)(CH2)vNH2; â€”NH(CH2)vSO3H; â€”NH(CH2)vPO3H2; â€”NH(CH2)vNHC(NH)NH2; or â€”NHCH(CO2H)(CH2)vCO2H; and v=1-20; X4 and X5 are independently H; halogen; OH; OCH3; CF3; NO2; NH2; amino substituted with acyl, carbamate, alkyl or aryl sulfonates; CORâ€² where Râ€² is OH, amide, alkoxy, aryloxy or heteroaryloxy, in a pharmaceutically acceptable carrier.