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Pyrimidine and purine derivatives and their use in treating tumour cells

  • US 5,929,046 A
  • Filed: 12/15/1995
  • Issued: 07/27/1999
  • Est. Priority Date: 06/08/1994
  • Status: Expired due to Fees
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Assignment
First Claim
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1. A pyrimidine derivative selected fromA) 6-hetarylalkyloxy pyrimidine derivatives of formula II ##STR16## wherein R is a cyclic group having at least one 5- or 6-membered heterocyclic ring, optionally with a carbocyclic or heterocyclic ring fused thereto, the or each heterocyclic ring having at least one hetero atom selected from the group consisting of O, N and S, or a substituted derivative thereof having substitution of the heterocyclic ring(s) and/or carbocyclic ring(s) by one or more substituents selected from the group consisting of alkyl, alkenyl, alkynyl, halo, haloalkyl, nitro, cyano, hydroxyalkyl, alkylenedioxy, SOn R"" where R"" is alkyl and n=0, 1 or 2, and a carboxyl or ester group of the formula --COORc where Rc is H or alkyl;

  • R2 is a member selected from the group consisting of H, C1 -C5 alkyl, halogen and NH2 ;

    R4 and R5 which are the same or different are selected from the group consisting of H, NH2 and NOn'"'"', where n'"'"'=1 or 2;

    orR4 and R5 together form a ring structure IIIa ##STR17## wherein Y is H, HOCH2 CH2 OCH2 -, ribosyl, deoxyribosyl, arabinosyl, or ##STR18## wherein X is O or S, R" and R'"'"'" are alkyl or substituted derivatives thereof having substitution by one or more substituents selected from the group consisting of hydroxy, halo, alkoxy, amino, alkylamino, amido and ureido,R3 is H or OH;

    orR4 and R5 together with the pyrimidine ring form a 5- or 6- membered ring structure containing one or more hetero atoms other than that of formula IIIa above,and pharmaceutically acceptable salts thereof, provided that if R4 and R5 form a ring structure IX ##STR19## wherein Y'"'"' is H, ribosyl, deoxyribosyl, or ##STR20## wherein X is O or S, R" and R'"'"'" are alkyl, or substituted derivatives thereof, R2 is not NH2 ; and

    B) 6-arylalkyloxy pyrimidine derivatives selected from those of formulae IIIb, IIIc, IVb, Vb, VIb, VIb and VIIb as defined below;

    ##STR21## wherein R10 is phenyl or a substituted derivative thereof having substitution by one or more substituents selected from the group consisting of alkyl, alkenyl, alkynyl, halo, haloalkyl, nitro, cyano, hydroxyalkyl, alkylenedioxy and SOn R"" where R"" and n are as defined for formula II or a carboxyl or ester group of the formula --COORc wherein Rc is as defined for formula II;

    R11 is C1 -C5 alkyl;

    Y is as defined above;

    ##STR22## wherein R10 is as defined above;

    R2 is as defined for formula II;

    R3 is H or OH;

    ##STR23## wherein R10 is as defined above;

    Y is as defined for formula IIIa ;

    X is CH or N;

    provided that if X is N and Y is H, thenR10 is not phenyl;

    ##STR24## wherein R10 is as defined above;

    X is CH or N;

    A is CH or N;

    ##STR25## wherein R10 is as defined above;

    Z is O or S or CH═

    CH;

    ##STR26## wherein R10 is as defined above;

    U is CH or N;

    V is CH or N;

    W is CH or N;

    ##STR27## wherein R10 is as defined above;

    T is H, NH2 or NOn where n=1 or 2;

    Q is H, NH2 or NOn where n=1 or 2;

    provided that;

    if Q is NH2 and T is NO or NO2, orif Q is H and T is NO2, orif Q and T are both NH2, orif Q is NH2, and T is H, thenR10 is not phenyl.

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