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Treatment of platelet derived growth factor related disorders such as cancers

  • US 6,331,555 B1
  • Filed: 07/27/1999
  • Issued: 12/18/2001
  • Est. Priority Date: 06/01/1995
  • Status: Expired due to Fees
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1. A method of evaluating the susceptibility of a cancer to growth inhibition by a compound comprising the steps of:

  • (a) culturing cells of said cancer in medium containing PDGF;

    (b) culturing cells of said cancer in medium containing PDGF and said compound; and

    (c) measuring and comparing the growth of said cells in (a) and (b), wherein said compound is selected from the group consisting of;

    i) a compound of Formula I;

     

    wherein R1, R2, R′

    2, R″

    2, and R″

    2 are independently selected from the group consisting of hydrogen, halogen, trihalomethyl, and NO2; and

    R3 is selected from the group consisting of hydrogen, carboxy, alkoxy, and carbalkoxy;

    ii) a compound of Formula II;

     

    wherein R4 and R5 are independently selected from the group consisting of halogen, hydrogen, trihalomethyl, and NO2; and

    R6 is selected from the group consisting of aryl, alkyl, alkenyl and alkynyl;

    iii) a compound of Formula III;

     

    wherein R7, R′

    7, and R8 are independently selected from the group consisting of halogen, OH, hydrogen, alkoxy, SH, NH2, and C(CH3)3; and

    R9 is aryl or hydrogen;

    iv) a compound of Formula IV;

     

    wherein R10 is selected from the group consisting of ═

    S, ═

    O, SH, OH, and NH2;

    R11 is selected from the group consisting of SH, OH, NH2, ═

    C(CN)2 and aryl;

    or R10 and R11 taken together are aryl; and

    R12 is selected from the group consisting of hydrogen, aryl, alkyl, alkenyl, and alkynyl;

    v) a compound of Formula V;

    wherein R13, R14, R15, R16, R17, and R18 are independently selected from the group consisting of hydrogen, halogen, alkoxy, OH, amino, alkylamino, and SH;

    vi) a compound of Formula VI;

    wherein R19 is selected from the group consisting of aryl, alkyl, alkenyl and alkynyl; and

    R20 is alkyl;

    or R19 and R20 are together aryl;

    vii) a compound of Formula VII;

    wherein b is an optional pi bond;

    Y and Z are independently carbon or nitrogen;

    R21 and R22 are independently selected from the group consisting of hydrogen, halogen, OH, SH, NH2, NO2, alkyl, alkenyl, alkynyl, alkoxy, benzoyl, COOH, and carbalkoxy;

    or R21 and R22 are together aryl;

    R23 is selected from the group consisting of hydrogen, halogen, ═

    O, OH, SH, NH2, alkoxy, COOH, and aryl;

    R24 is H or aryl; and

    R25 is selected from the group consisting of hydrogen, halogen, ═

    S, or ═

    O, wherein if R25 is ═

    O or ═

    S then b is present as a bond;

    provided that if b is not a bond, the adjacent nitrogen optionally has a substituent selected from the group consisting of hydrogen, alkyl, alkyleneamino, alkyleneaminoalkly, and alkylenecyano;

    viii) a compound of Formula VIII;

     

    wherein R26 and R28 are independently selected from the group consisting of alkyl, aryl, alkenyl, and alkynyl; and

    R27 is aryl;

    ix) a compound of Formula IX;

     

    wherein R30 is selected from the group consisting of alkyl, alkenyl, and R31 is aryl; and

    R32 is either O or S;

    x) a compound of Formula X;

     

    wherein R33 is alkyl or aryl;

    R34, R35, and R36 are independently selected from the group consisting of halogen, OH, hydrogen, alkoxy, SH, NH2, and C(CH3)3; and

    xi) a compound of any one Formula XI(a)-Formula XI(o);

    or a pharmaceutically acceptable salt of said compound.

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