Patent ID: 6057323
Filing Date: 2000-05-02
Classification: A61K,C07D

Abstract:
A method for the prevention or treatment of pruritus in a patient comprising administering to said patient an effective amount of a compound of formula I or a pharmaceutically acceptable salt thereof ##STR299## wherein n=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 --;Ar=unsubstituted or mono-, or di-substituted phenyl wherein said substituents are selected from the group consisting of halogen, OC.sub.4, SO.sub.2 CH.sub.3, CF.sub.3, amino, alkyl, and 3,4-dichloro; benzothiophenyl; benzofuranyl; naphthyl diphenyl methyl; or 9-fluorene;Z is --P(O)(OBn).sub.2 ; --P(O)(OH).sub.2 ; --(CH.sub.2).sub.p C(O)NHOH; --(CH.sub.2).sub.p CO.sub.2 H; --SO.sub.2 CH.sub.3 ; --SO.sub.2 NH.sub.2 ; --CO(CH.sub.2).sub.p CH(NH.sub.2)(CO.sub.2 H); --COCH(NH.sub.2)(CH.sub.2).sub.p CO.sub.2 H; --CO.sub.2 CH.sub.3 ; --CON--H.sub.2 ; --(CH.sub.2).sub.p O(CH.sub.2).sub.p CO.sub.2 H; --(CH.sub.2).sub.p O(CH.sub.2).sub.p CONHOH; --(CH.sub.2).sub.p NHSO.sub.2 CH.sub.3 ; --(CH.sub.2).sub.p NHC(S)NHCH(CO.sub.2 H)(CH.sub.2).sub.p CO.sub.2 H; --(CH.sub.2).sub.p SO.sub.3 H; or ##STR300## or Z is ##STR301## wherein p=0-20;R.sub.3 =--H or --Ac;X.sub.2 =--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 ;X and Y are independently--CH.sub.2 NHSO.sub.2 CH.sub.3, --CH.sub.2 NHP(O)(OBn).sub.2, --CH.sub.2 NHP(O)(OH).sub.2, --CH.sub.2 OP(O)(OBn).sub.2, --CH.sub.2 OP(O)(OH).sub.2, --(CH.sub.2).sub.q O(CH.sub.2).sub.q CO.sub.2 H, --(CH.sub.2).sub.q O(CH.sub.2).sub.q SO.sub.3 H, --(CH.sub.2).sub.q O(CH.sub.2).sub.q CHNHOH, --CH.sub.2 NHC(S)NHCH(CO.sub.2 H)(CH.sub.2).sub.q CO.sub.2 H, or ##STR302## wherein q=1-20r=1-20R.sub.4 =--H or --AcX.sub.3 =--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.2in a pharmaceutically acceptable carrier.