Patent ID: 6172113
Filing Date: 2001-01-09
Classification: A61K,A61P,C07C,C07D,C07F

Abstract:
A method for treating a PGD.sub.2 -mediated disease selected from the group consisting of systemic mastocytosis, disorder of systemic mast cell activation, allergic rhinitis, allergic conjunctivitis, uticaria, injury due to ischemic reperfusion and nasal occlusion, comprising administering to a subject in need thereof, a PGD.sub.2 antagonist comprising a compound of the general formula (I) below or its salt or hydrate thereof as an active ingredient: ##STR775##wherein ##STR776##isA is alkylene which optionally is intervened by hetero atom or phenylene, contains oxo group, and/or has an unsaturated bond;B is hydrogen, alkyl, aralkyl or acyl;R is COOR.sub.1, CH.sub.2 OR.sub.2 or CON(R.sub.3)R.sub.4 ;R.sub.1 is hydrogen or alkyl;R.sub.2 is hydrogen or alkyl;R.sub.3 and R.sub.4 each are independently hydrogen, alkyl, hydroxy or alkylsulphonyl;X.sub.1 is a single bond, phenylene, naphtylene, thiophenediyl, indolediyl, oxazolediyl;X.sub.2 is a single bond, --N.dbd.N--, --N.dbd.CH--, --CH.dbd.N--, --CH.dbd.N--N--, --CH.dbd.N--O--, --C.dbd.NNHCSNH--, --C.dbd.NNHCONH--, --CH.dbd.CH--, --CH(OH)--, --C(Cl).dbd.C(Cl)--, --(CH.sub.2)n--, ethynylene, --N(R.sub.5)--, --N(R.sub.51)CO--, --N(R.sub.52)SO.sub.2 --, --N(R.sub.53)CON(R.sub.54)--, --CON(R.sub.55)--, --SO.sub.2 N(R.sub.56)--, O--, --SO--, --SO.sub.2 --, --CO--, oxadiazolediyl, thiadiazolediyl, tetrazolediyl;X.sub.3 is alkyl, alkenyl, alkynyl, aryl, aralkyl, heterocyclic group, cycloalkyl, cycloalkenyl, thiazolinylidenemethyl, thiazolidinylidenemethyl, --CH.dbd.NR.sub.6 or --N.dbd.C(R.sub.7)R.sub.8 ;R.sub.5, R.sub.51, R.sub.52, R.sub.53, R.sub.54, R.sub.55 and R.sub.56, each are hydrogen or alkyl;R.sub.6 is hydrogen, alkyl, hydroxy, alkoxy, or carbamoyloxy, thiocarbamoyloxy, ureido or thioureido;R.sub.7 and R.sub.8 each are independently alkyl, alkoxy, or aryl;n is 1 or 2;Z is --SO.sub.2 -- or --CO--; andM is 0 or 1;wherein a cyclic substituent may have one to three substituents selected from the group consisting of nitro, alkoxy, sulfamoyl, substituted- or unsubstituted-amino, acyl, acyloxy, hydroxy, halogen, alkyl, alkynyl, carboxy, alkoxycarbonyl, aralkoxycarbonyl, aryloxycarbonyl, mesyloxy, cyano, alkenyloxy, hydroxyalkyl, trifluoromethyl, alkylthio, --N.dbd.PPh.sub.3, oxo, thioxo, hydroxyimino, alkoxyimino, phenyl and alkylenedioxy.