Patent ID: 6316457
Filing Date: 2001-11-13
Classification: A61P,C07D

Abstract:
A compound having structure VI: ##STR21##whereinR.sub.15 is a hydrogen, a lower alkyl, R.sub.4, or --(CH.sub.2).sub.4 --C(CH.sub.3).sub.2 --O--D.sub.1 ;R.sub.16 is a lower alkyl; andR.sub.17 is a hydrogen, a lower alkyl, CH.sub.3 --C(O)--CH.sub.2 --, CH.sub.3 --O--CH.sub.2 --, or D, with the proviso that either R.sub.15 or R.sub.17 must contain D;D is(i) --NO,(ii) --NO.sub.2,(iii) --CH(R.sub.d)--O--C(O)--Y--Z--(C(R.sub.e)(R.sub.f)).sub.p --T--Q,wherein R.sub.d is a hydrogen, a lower alkyl, a cycloalkyl, an aryl, an arylalkyl, or a heteroaryl; Y is oxygen, sulfur, CH.sub.2 or NR.sub.i, wherein R.sub.i is a hydrogen or a lower alkyl; R.sub.e and R.sub.f are each independently a hydrogen, a lower alkyl, a haloalkyl, an alkoxy, a cycloalkyl, an aryl, a heteroaryl, an arylalkyl, an amino, an alkylamino, an amido, an alkylamido, a dialkylamino, a carboxylic acid, a carboxylic ester, a carboxamido or --T--Q, or R.sub.e and R.sub.f taken together are a carbonyl, a cycloalkyl, a heterocyclic ring or a bridged cycloalkyl; p is an integer from 1 to 10; T is independently a covalent bond, oxygen, sulfur or NH; Z is a covalent bond, a lower alkyl, a haloalkyl, a cycloalkyl, an aryl, a heteroaryl, an arylalkyl, a heteroalkyl, an arylheterocyclic ring or (C(R.sub.e)(R.sub.f)).sub.p ; and Q is --NO or --NO.sub.2 ;(iv) --C(O)--Y--Z--(G--(C(R.sub.e)(R.sub.f)).sub.q --T--Q).sub.p,wherein G is a covalent bond, --T--C(O)--, --C(O)--T-- or T, wherein q is an integer from 0 to 5, and Y, Z, R.sub.e, R.sub.f, p, T and Q are as defined above; or(v) --P--Z--(G--(C(R.sub.e)(R.sub.f)).sub.q --T--Q).sub.p,wherein P is a carbonyl, a phosphoryl or a silyl, and Z, G, p, q, T, Q, R.sub.e and R.sub.f are as defined above;R.sub.4 is (i) hydrogen, (ii) --CH(R.sub.d)--O--C(O)--Y--Z--(C(R.sub.e)(R.sub.f)).sub.p T--Q, (iii) --C(O)--T--(C(R.sub.e)(R.sub.f)).sub.p --T--Q, or (iv) --C(O)--Z--(G--(C(R.sub.e)(R.sub.f)).sub.p --T--Q).sub.p ;wherein R.sub.d, Y, Z, R.sub.e, R.sub.f, p, T, Q, Z and G are as defined above; and D.sub.1 is D or a hydrogen.