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Compositions and Methods for Treatment of Cancer

  • US 20100221251A1
  • Filed: 03/11/2010
  • Published: 09/02/2010
  • Est. Priority Date: 02/09/2005
  • Status: Active Grant
First Claim
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1. A pyrroloquinolinyl-pyrrolidine-2,5-dione compound of formula IVa, IVb, Va, or Vb, or pharmaceutically acceptable salts thereof:

  • where;

    R1, R2 and R3 are independently selected from the group consisting of hydrogen, F, Cl, Br, I, —

    NR5R6, —

    (C1-C6) alkyl, —

    (C1-C6) substituted alkyl, —

    (C3-C9) cycloalkyl, —

    (C3-C9) substituted cycloalkyl, —

    O—

    (C1-C6) alkyl, —

    O—

    (C1-C6) substituted alkyl, —

    O—

    (C3-C9) cycloalkyl, and —

    O—

    (C3-C9) substituted cycloalkyl, aryl, heteroaryl, heterocyclyl;

    R4 is independently selected from the group consisting of hydrogen, —

    (C1-C6) alkyl, —

    CH2R7;

    R5, R6 are independently selected from the group consisting of hydrogen, and —

    (C1-C6) alkyl;

    R7 is independently selected from the group consisting of —

    O—

    P(═

    O)(OH)2, —

    O—

    P(═

    O)(—

    OH)(—

    O—

    (C1-C6) alkyl), —

    O—

    P(═

    O)(—

    O—

    (C1-C6) alkyl)2, —

    O—

    P(═

    O)(—

    OH) (—

    O—

    (CH2)-phenyl), —

    O—

    P(═

    O)(—

    O—

    (CH2)-phenyl)2, a carboxylic acid group, an amino carboxylic acid group and a peptide;

    Q is selected from the group consisting of aryl, heteroaryl, —

    O-aryl, —

    S-aryl, —

    O-heteroaryl, and —

    S-heteroaryl;

    X is —

    (NR8)-;

    R8 is independently selected from the group consisting of hydrogen, —

    (C1-C6) alkyl, —

    (C1-C6) substituted alkyl, —

    (C3-C9) cycloalkyl, —

    (C3-C9) substituted cycloalkyl, and —

    O—

    (C1-C6) alkyl, —

    C(═

    O)—

    O—

    (C1-C6) alkyl and —

    C(═

    O)—

    O—

    (C1-C6) substituted alkyl;

    Y is (CH2)—

    ;

    wherein said aryl, heteroaryl, —

    O-aryl, —

    S-aryl, —

    O-heteroaryl, and —

    S-heteroaryl groups may be substituted with one or more substituents independently selected from the group consisting of F, Cl, Br, I, —

    NR5R6, —

    (C1-C6) alkyl, —

    (C1-C6) substituted alkyl, —

    (C3-C9) cycloalkyl, —

    (C3-C9) substituted cycloalkyl, —

    O—

    (C1-C6) alkyl, —

    O—

    (C1-C6) substituted alkyl, —

    O—

    (C3-C9) cycloalkyl, —

    O—

    (C3-C9) substituted cycloalkyl, -aryl, -aryl-(C1-C6) alkyl, -aryl-O—

    (C1-C6) alkyl, —

    O-aryl, —

    O—

    (C1-C4) alkyl-aryl, heteroaryl, heterocyclyl, —

    O—

    (C1-C4) alkyl-heterocycle, and —

    (S(═

    O)2)—

    (C1-C6) alkyl; and

    m is 1.

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