Patent ID: 6124341
Filing Date: 2000-09-26
Classification: A61P,C07D

Abstract:
A compound of the formula: ##STR24## wherein R is --(CH.sub.2).sub.m -W wherein m is an integer from 0 to 6 and W is(a) --C(O).sub.2 --G wherein G is hydrogen or a carboxy protecting group,(b) --PO.sub.3 H.sub.2,(c) --P(O)(OH)E wherein E is hydrogen, loweralkyl or arylalkyl,(d)--CN,(e) --C(O)NHR.sub.17 wherein R.sub.17 is loweralkyl,(f) alkylaminocarbonyl,(g) dialkylaminocarbonyl,(h) tetrazolyl,(i) hydroxy,(j) alkoxy,(k) sulfonamido,(l) --C(O)NHS(O).sub.2 R.sub.16 wherein R.sub.16 is loweralkyl, haloalkyl, aryl or dialkylamino,(m) --S(O).sub.2 NHC(O)R.sub.16 wherein R.sub.16 is defined as above, ##STR25## R.sub.1 and R.sub.2 are independently selected from hydrogen, loweralkyl, alkenyl, alkynyl, alkoxyalkyl, alkoxycarbonylalkyl, hydroxyalkyl, haloalkyl, haloalkoxyalkyl, alkoxyalkoxyalkyl, thioalkoxyalkoxyalkyl, cycloalkyl, cycloalkylalkyl, aminocarbonylalkyl, alkylaminocarbonylalkyl, dialkylaminocarbonylalkyl, aminocarbonylalkenyl, alkylaminocarbonylalkenyl, dialkylaminocarbonylalkenyl, hydroxyalkenyl, aryl, arylalkyl, aryloxyalkyl, arylalkoxyalkyl, heterocyclic, (heterocyclic)alkyl and(R.sub.aa)(R.sub.bb)N--R.sub.cc - wherein R.sub.aa is aryl or arylalkyl, R.sub.bb is hydrogen or alkanoyl and R.sub.cc is alkylene, with the proviso that one or both of R.sub.1 and R.sub.2 is other than hydrogen; with the proviso that heterocyclic is not morpholine or pyrazole R.sub.3 is R.sub.4 --C(O)--R.sub.5 -- or R.sub.6 --S(O).sub.2 --R.sub.7 --wherein R.sub.5 is (i) a covalent bond, (ii) alkylene, (iii) alkenylene, (iv) --N(R.sub.20)--R.sub.8 -- or --R.sub.8a --N(R.sub.20)--R.sub.8 --wherein R.sub.8 and R.sub.8a are independently selected from the group consisting of alkylene and alkenylene andR.sub.20 is hydrogen, loweralkyl, alkenyl, haloalkyl, alkoxyalkyl, haloalkoxyalkyl, cylcoalkyl or cycloalkylalkyl or (v) --O--R.sub.9 -- or --R.sub.9a --O--R.sub.9 --wherein R.sub.9 and R.sub.9a are independently selected from alkylene;R.sub.7 is (i) a covalent bond, (ii) alkylene, (iii) alkenylene or (iv) --N(R.sub.21)--R.sub.10 -- or --R.sub.10a --N(R.sub.21)--R.sub.10--wherein R.sub.10 and R.sub.10a are independently selected from the group consisting of alkylene and alkenylene andR.sub.21 is hydrogen, loweralkyl, alkenyl, haloalkyl, alkoxyalkyl, haloalkoxyalkyl, aryl or arylalkyl;wherein R.sub.4 and R.sub.6 are ##STR26## wherein R.sub.11 and R.sub.12 are independently selected from the group consisting of loweralkyl, cyano, alkoxy, halo, haloalkyl, and phenyl, and R.sub.13, R.sub.14, and R.sub.15 are independently selected from the group consisting of hydrogen, loweralkyl, hydroxy, amino, alkoxy, aryl, heterocyclic, halo, carboxy, nitro, alkylsulfonyl, arylsulfonyl, thioalkoxy, thioaryloxy, or cyano with the proviso that heterocyclic is not morpholine or pyrazole or(ii) heterocyclic(amino), with the proviso that when R is --C(O).sub.2 --G and G is hydrogen, then R.sub.1 is not arylalkoxyalkylor a pharmaceutically acceptable salt thereof.