Patent ID: 6143749
Filing Date: 2000-11-07
Classification: A61P,C07D,C07F,Y02P

Abstract:
A compound of the Formula I: ##STR32## wherein X is --CR.sub.7 where R.sub.7 is hydrogen, halogen, loweralkyl, loweralkoxy or --S-- loweralkyl;Y is N or CH;R.sub.1 and R.sub.2 are each independently hydroxy, alkoxy, or acyloxy or R.sub.1 and R.sub.2 are both hydroxy protected with an individual hydroxy protecting group or with a single dihydroxy-protecting group or R.sub.1 and R.sub.2 are absent and there is a double bond between the carbon atoms to which R.sub.1 and R.sub.2 are attached;R.sub.3 is hydrogen, hydroxy or alkoxy;R.sub.4 is a) hydrogen, b) amino, c) halogen, d) hydroxy, e)sulfonamido, f) --P(O)(OH).sub.2, g) --P(O)--R.sub.8 R.sub.9 wherein R.sub.8 and R.sub.9 are each independently hydrogen, hydroxy, loweralkyl, aryl, or arylalkyl, h), --NHR.sub.10 wherein R.sub.10 is hydrogen or an amino protecting group, i) --NHC(O)NHR.sub.11 where R.sub.11 is hydrogen or loweralkyl, or j) --A--R.sub.12 wherein A is O, S(O).sub.n or --N(R.sub.13)-- wherein R.sub.13 is hydrogen or loweralkyl, n is zero, one or two, and R.sub.12 is hydrogen, loweralkyl, alkylsulfonyl, acyl which is selected from R.sub.17 CO-- wherein R.sub.17 is loweralkyl, heteroaryl or heterocyclic, alkoxycarbonyl, aryl, heteroaryl, arylalkyl, arylsulfonyl, haloalkyl, heteroarylalkyl, heteroarylalkyl, heteroarylsulfonyl, aminoalkyl or heterocyclic or k) R.sub.4 is a N-atom of a heteroaryl or heterocyclic ring; or R.sub.3 and R.sub.4 taken together are .dbd.O;R.sub.5 is hydrogen, loweralkyl, aryl, arylalkyl, heteroaryl, amino, alkylamino, alkoxy, acylamino, arylalkynyl, arylamino, arylmercapto, alkylmercapto, halogen, heterocyclic, hydrazino, --NHC(O)NH.sub.2, or --NR.sub.14 R.sub.15 wherein R.sub.14 and R.sub.15 are each independently hydrogen or an amino protecting group or --NR.sub.14 R.sub.15 is a nitrogen containing heterocycle of 5 to 7 members; andR.sub.6 is loweralkyl, cycloalkyl, alkenyl, alkynyl, alkoxy, alkoxycarbonyl, carboxy, aryl, heteroaryl, heteroarylalkyl, arylalkyl, arylalkenyl arylalkynyl, cyano, halogen, heteroarylalkynyl, or --C(O)NHR.sub.16 wherein R.sub.16 is alkyl, aryl or heterocyclic wherein heteroaryl is selected from aryl in which one and more of the ring carbon atoms is replaced by a heterocyclic atom such as N, S, O or P.