Patent ID: 6096724
Filing Date: 2000-08-01
Classification: A61P,C07D,C07H

Abstract:
A pyrimidine derivative selected fromA) 6-hetarylalkyloxy pyrimidine derivatives of formula II ##STR22## wherein R is a cyclic group having at least one 5- or 6-membered hetercyclic ring, or a substituted 5- or 6-membered heterocyclic ring, optionally with a carbocyclic, substituted carbocyclic, heterocyclic or substituted heterocyclic ring fused thereto, the or each heterocyclic ring or substituted heterocyclic ring having at least one hetero atom chosen from O, N or S;R.sup.2 is selected from H, C.sub.1 -C.sub.5 alkyl, halogen or NH.sub.2,R.sup.4 and R.sup.5 which are the same or different are selected from H, NH--Y' or NO.sub.n whereinY' is H, ribosyl, deoxyribosyl, arabinosyl, ##STR23## wherein X is O or S, R"" is alkyl or substituted alkyl and R""' is H, alkyl, or substituted alkyl,n-1 or 2, orR.sup.4 and R.sup.5 together form a ring structure III.sup.a ##STR24## wherein Y' is as defined above,R.sup.3 is H or OH, orR.sup.4 and R.sup.5 together with the pyrimidine ring form a 5- or 6-membered ring structure containing one or more hetero atoms other than that of formula III.sup.a above; and pharmaceutically acceptable salts thereof,with the proviso that R.sup.2 is not NH.sub.2 if R.sup.4 and R.sup.5 form a ring structure IX ##STR25## wherein Y is H, ribosyl, deoxyribosyl, or ##STR26## wherein X is O or S, R"" and R""' are alkyl or substituted alkyl; and with the further proviso that R is not a cyclic group having a heterocyclic ring with more than one S atom in the ring; andB) 6-arylalkyloxy pyrimidine derivatives selected from those of formulae III.sup.b, III.sup.c, IV.sup.b, V.sup.b, VI.sup.b, VII.sup.b, and VIII.sup.b as defined below: ##STR27## wherein R.sup.10 is phenyl or substituted phenyl;R.sup.11 is C.sub.1 -C.sub.5 alkyl;Y' is as defined above;R.sup.3 is H or OH; ##STR28## wherein R.sup.10 is as defined above;R.sup.2 is as defined for formula II;R.sup.3 is H or OH; ##STR29## wherein R.sup.10 is as defined above;Y' is as defined for formula II;X is CH or N;provided that if X is N and Y is H, then R.sup.10 is not phenyl; ##STR30## wherein R.sup.10 is as defined above;X is CH or N;A is CH or N; ##STR31## wherein R.sup.10 is as defined above;Z is O or S or CH.dbd.CH; ##STR32## wherein R.sup.10 is as defined above;U is CH or N;V is CH or N;W is CH or N; ##STR33## wherein R.sup.10 is as defined above;T is H, NH.sub.2 or NO.sub.n wherein n-1 or 2;Q is H, NH.sub.2 or HO.sub.n wherein n=1 or 2;provided that: if Q is NH.sub.2 and T is NO or NO.sub.2, or: if Q is H and T is NO.sub.2, or: if Q and T are both NH.sub.2, or: if Q is NH.sub.2, and T is H, thenR.sup.10 is not phenyl.