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Cytostatic agents

  • US 6,495,597 B1
  • Filed: 10/05/2000
  • Issued: 12/17/2002
  • Est. Priority Date: 02/13/1998
  • Status: Expired due to Fees
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Forward Citation
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Assignments
First Claim
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1. A method for inhibiting proliferation of tumor cells in mammals, comprising administering to a mammal suffering such cell proliferation an effective amount of a compound of general formula (I):

  • embedded imagewhereinR is hydrogen or (C1-C6)alkyl;

    R1 is hydrogen;

    (C1-C6)alkyl or fluoro-substituted (C1-C6)alkyl (C2-C6)alkenyl;

    phenyl or substituted phenyl;

    phenyl(C1-C6)alkyl or substituted phenyl(C1-C6)alkyl;

    phenyl(C2-C6)alkenyl or substituted phenyl(C2-C6)alkenyl heterocyclyl or substituted heterocyclyl;

    heterocyclyl(C1-C6)alkyl or substituted heterocyclyl(C1-C6)alkyl;

    a group BSOnA—

    wherein n is 0, 1 or 2 and B is hydrogen or a (C1-C6) alkyl, phenyl, substituted phenyl, heterocyclyl substituted heterocyclyl, (C1-C6)acyl, phenacyl or substituted phenacyl group, and A represents (C1-C6)alkylene;

    amino(C1-C6)alkyl, (C1-C6)alkylamino(C1-C6)alkyl, di(C1-C6)alkylamino(C1-C6)alkyl, hydroxy(C1-C6)alkyl, mercapto(C1-C6)alkyl or carboxy(C1-C6)alkyl wherein the amino-, hydroxy-, mercapto- or carboxyl-group are optionally protected or the carboxyl-group amidated;

    lower alkyl substituted by carbamoyl, mono(lower alkyl)carbamoyl, di(lower alkyl)carbamoyl, di(lower alkyl)amino, or carbbxy-lower alkanoylamino;

    a cycloalkyl, cycloalkenyl, cycloalkyl(C1-C6alkyl)—

    , cycloalkenyl(C1-C6alkyl)—

    or non-aromatic heterocyclic ring containing up to 3 heteroatoms, any of which may be (i) substituted by one or more substituents selected from C1-C6 alkyl, C2-C6 alkenyl, halo, cyano (—

    CN), —

    CO2H, —

    CO2R, —

    CONH2, —

    CONHR, —

    CON(R)2, —

    OH, —

    OR, oxo-, —

    SH, —

    SR, —

    NHCOR, and —

    NHCO2R wherein R is C1-C6 alkyl or benzyl and/or (ii) fused to a cycloalkyl or heterocyclic ring;

    R2 is a C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, phenyl(C1-C6 alkyl)—

    , heteroaryl(C1-C6 alkyl)—

    , phenyl(C2-C6 alkenyl)—

    , heteroaryl(C2-C6 alkenyl)—

    , phenyl(C2-C6 alkynyl)—

    , heteroaryl(C2-C6 alkynyl)—

    , cycloalkyl(C1-C6 alkyl)—

    , cycloalkyl(C2-C6 alkenyl)—

    , cycloalkyl(C2-C6 alkynyl)—

    , cycloalkenyl(C1-C6 alkyl)—

    , cycloalkenyl(C2-C6 alkenyl)—

    , cycloalkenyl(C2-C6 alkynyl)—

    , phenyl(C1-C6 alkyl)O(C1-C6 alkyl)—

    , or heteroaryl(C1-C6 alkyl)O(C1-C6 alkyl)—

    group, any one of which may be optionally substituted by C1-C6 alkyl, C1-C6 alkoxy, halo, cyano(—

    CN), phenyl or heteroaryl, optionally ring-substituted by C1-C6 alkyl, C1-C6 alkoxy, halo, or cyano(—

    CN);

    R3 is a benzyl group substituted in the phenyl ring by a group of formula —

    OCH2COR8 where R8 is hydroxyl, amino, (C1-C6)alkoxy, phenyl(C1-C6)alkoxy, (C1-C6)alkylamino, di((C1-C6)alkyl)amino, phenyl(C1-C6)alkylamino, the residue of an amino acid or acid halide, ester or amide derivative thereof, said residue being linked via an amide bond, said amino acid being selected from glycine, α

    or β

    alanine, valine, leucine, isoleucine, phenylalanine, tyrosine, tryptophan, serine, threonine, cysteine, methionine, asparagine, glutamine, lysine, histidine, arginine, glutamic acid, and aspartic acid; and

    R4 is an ester or thioester group, or a pharmaceutically acceptable salt, hydrate or solvate thereof, sufficient to inhibit such proliferation.

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