Patent ID: 6180623
Filing Date: 2001-01-30
Classification: A61K,A61P,C07D,Y02A

Abstract:
A method for prevention or treatment of pruritus in a patient comprising administering to said patient an effective amount of a composition comprising a compound of the formula IV or a pharmaceutically acceptable salt thereof ##STR160##whereinn=1-3;R.sub.1 and R.sub.2 are independently --CH.sub.3 ; --(CH.sub.2).sub.m, where m=4-8;--CH.sub.2 CH(OH)(CH.sub.2).sub.2 --; --CH.sub.2 CH(F)(CH.sub.2).sub.2 --; --(CH.sub.2).sub.2 O(CH.sub.2).sub.2 --; or--(CH.sub.2).sub.2 CH.dbd.CHCH.sub.2 --:R.sub.3 and R.sub.4 are independently H; OCH.sub.3 ; alkyl or --O(CH.sub.2).sub.2 ;X.sub.9 =1-4 substituents selected from the group consisting of -halogen; --CF.sub.3 ; --OCH.sub.3 ; --SO.sub.2 NH(CH.sub.2).sub.q CO.sub.2 H; --NH.sub.2 ; --NHSO.sub.2 CH.sub.3 ; --NHP(O)(OBn).sub.2 ; --NHP(O)(OH).sub.2 ; --NH(CH.sub.2).sub.q CO.sub.2 H; --SO.sub.2 CH.sub.3 ; --OP(O)(OBn).sub.2 ; --OP(O)(OH).sub.2 ; --CO.sub.2 H; --O(CH.sub.2).sub.q CO.sub.2 H; --O(CH.sub.2)qSO.sub.3 H; --O(CH.sub.2).sub.q OPO.sub.3 H.sub.2 ; wherein q=1-20;or X.sub.9 is ##STR161##whereint=1-20;R.sub.5 =--H or --Ac;X.sub.6 =--CO.sub.2 H; --NHSO.sub.2 CH.sub.3 ; --NHP(O)(OBn).sub.2 ; --NHP(O)(OH).sub.2 ; --OP(O)(OBn).sub.2 ; or --OP(O)(OH).sub.2 ; andwherein said compound of formula IV is not (.+-.)-trans-3,4-dichloro-N-methyl-N-[2-(dimethylamino)cyclohexyl]-phenyla cetamido Hydrochloride; (.+-.)-trans-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl]-phenyl acetamido Hydrochloride, or a pharmaceutically acceptable salt thereof:in a pharmaceutically acceptable vehicle.