Patent ID: 6197762
Filing Date: 2001-03-06
Classification: A61P,C07C,C07D,C07J

Abstract:
A compound of formula I: ##STR13##whereinA is --CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --;R.sub.1 is(1) --C(O)--CH.sub.2 --B--D;(2) --C(O)--C(O)--O--R;(3) --C(O)--B--R;(4) --C(O)--CH.sub.2 --B--C(O)--R;(5) --C(O)--CH.sub.2 --X;(6) --S--R;(7) --C(O)--CH.sub.2 --B--M;wherein B is oxygen or sulfur; X is halogen; R.sub.1 is hydrogen or lower alkyl;D is(i) --C(R.sub.d)--O--C(O)--Y--(C(R.sub.e)(R.sub.f).sub.p --T--Q;(ii) --C(O)--T.sup.1 --(C(R.sub.e)(R.sub.f)).sub.p --T.sup.2 --Q; or(iii) --C(O)--T--(C(R.sub.y)(R.sub.z)).sub.p ;wherein R.sub.d is hydrogen, lower alkyl, cycloalkyl, aryl, alkylaryl or heteroaryl; Y is oxygen, sulfur or NR.sub.i ; R.sub.i is hydrogen, lower alkyl, lower haloalkyl or heteroaryl; R.sub.e and R.sub.f are each independently hydrogen, lower alkyl, cycloalkyl, aryl, heteroaryl, arylalkyl, alkylamino, dialkylamino, or carboxy, or R.sub.e and R.sub.f taken together are carbonyl, cycloalkyl or bridged cycloalkyl; p is an integer from 1 to 6; T, T.sup.1 and T.sup.2 are each independently a covalent bond, oxygen, sulfur or nitrogen; Q is --NO or --NO.sub.2 ;R.sub.y and R.sub.z are each independently --T.sup.1 --(C(R.sub.e)(R.sub.f)).sub.p --G--(C(R.sub.e)(R.sub.f)).sub.p --T.sup.2 --Q; whereinG is a covalent bond, --T--C(O)--, --C(O)--T or Y;wherein R.sub.d, R.sub.e, R.sub.i, p, Q, T, T.sup.1, T.sup.2 and Y are as defined above; andM is(i) --C(O)--T--(C(R.sub.e)(R.sub.f)).sub.p --G--(C(R.sub.e)(R.sub.f)).sub.p --N(N--(O.sup.-).cndot.N.dbd.O)--R.sub.i or(ii) --C(R.sub.e)--O--C(O)--T--(C(R.sub.e)(R.sub.f).sub.p --G--(C(R.sub.e)(R.sub.f)).sub.p --N(N--(O.sup.-).cndot.N.dbd.O)--R.sub.i ;wherein T, R.sub.e, R.sub.f, p, G, R.sub.i, and R.sub.d are as defined herein;R.sub.2 and R.sub.3 are each independently hydrogen, hydroxyl, lower alkyl, --O(O)C--R.sub.i or --S--R.sub.i, or R.sub.2 and R.sub.3 taken together are ##STR14##wherein R.sub.i is as defined above, and R.sup.1.sub.i and R.sup.2.sub.i are each independent R.sub.i ;R.sub.4 and R.sub.5 are each independently hydrogen or halogen; andR.sub.6 is hydrogen, D or M; wherein D and M are as defined herein; with the proviso that R.sub.6 must be D or M if the substituent selected for R.sub.1 does not include D or M.