Patent ID: 6294668
Filing Date: 2001-09-25
Classification: A61P,C07D,Y02P

Abstract:
A compound of the formula ##STR79##whereinR.sup.1 is halogen, lower alkyl, phenyl, benzyl, styryl, naphthyl or heterocyclyl; the lower alkyl, phenyl, benzyl, styryl, naphthyl and heterocyclyl being optionally substituted by at least one of halogen, hydroxy, optionally substituted lower alkyl, optionally substituted lower alkoxy, optionally substituted phenyl, amino, lower alkylamino, di-lower alkylamino, carboxy, carbamoyl, or lower alkylcarbamoyl;R.sup.4, R.sup.5 independently are hydrogen, lower alkyl or phenyl;X is S, NH or CH.sub.2 ;n is 0, 1 or 2;m is 0 or 1;s is 0 or 1;R.sup.2 is hydrogen, hydroxy, --CH.sub.2 --CONHR.sup.6, lower alkyl-Q.sub.r, cycloalkyl-Q.sub.r, lower alkoxy, lower alkenyl, cycloalkenyl-Q.sub.r, lower alkynyl, aralkyl-Q.sub.r, aryl-Q.sub.r, aryloxy, aralkoxy, a heterocyclic ring or a heterocyclyl-Q.sub.r, the lower alkyl, cycloalkyl, lower alkoxy, lower alkenyl, cycloalkenyl, lower alkynyl, aralkyl, aryl, aryloxy, aralkoxy and the heterocyclic ring is optionally substituted with at least one group selected from carboxy, amino, nitro, cyano, SO.sub.2 NHR.sup.6, optionally fluoro substituted lower alkyl, lower alkoxy, hydroxy, halogen, --CONR.sup.6 R.sup.7, --CH.sub.2 CONR.sup.6 R.sup.7, --N(R.sup.7)COOR.sup.8, R.sup.7 CO--, R.sup.7 OCO--, R.sup.7 COO--, --C(R.sup.7 R.sup.9)CO.sub.2 R.sup.8, --C(R.sup.7 R.sup.9)CONR.sup.7 R.sup.10, wherein R.sup.6 is hydrogen, lower alkyl, cycloalkyl or aryl;R.sup.7 and R.sup.9 are independently hydrogen or lower alkyl;R.sup.8 is hydrogen, lower alkyl or a lower alkenyl group; andR.sup.10 is hydrogen, .omega.-hydroxy-alkyl, phenyl, naphthyl or heterocyclyl, the phenyl, naphthyl or heterocyclyl being unsubstituted or substituted with hydroxy, halogen, optionally substituted lower alkyl or .omega.-hydroxyalkyl, optionally substituted lower alkoxy and/or cyano, or R.sup.7 and R.sup.10 form together group of formula ##STR80##Q is --CHR--, --CO-- or --SO.sub.2 --;r is 0 or 1;R is hydrogen or lower alkyl; andR.sup.3 is hydroxy, --O.sup.-, lower-alkoxy, or --OM and M is an alkali metal;wherein when R.sup.2 is positively charged R.sup.3 is --O.sup.- and when R.sup.3 is --O.sup.- R.sup.2 is positively charged,wherein each heterocyclyl is independently an unsaturated or saturated, unsubstituted or substituted 4-, 5-, 6-, or 7-membered heterocyclic ring containing at least one atom selected from the group consisting of oxygen, nitrogen and sulfur;an ester thereof which is readily hydrolyzable in vivo, a pharmaceutically acceptable salt thereof, or a hydrate thereof, or a hydrate of said ester or said salt.