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Macroheterocyclic compounds as kinase inhibitors

  • US 20070088019A1
  • Filed: 09/27/2006
  • Published: 04/19/2007
  • Est. Priority Date: 09/29/2005
  • Status: Abandoned Application
First Claim
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1. A compound of Formula (I):

  • embedded image wherein A is CH or N, whereby the A-containing ring system of Formula (I) thus forms 1H-indole or 1H-pyrrolo[2,3-b]pyridine, respectively;

    Z is O, OH, or H, H;

    R1 and R3 are independently selected from the group consisting of hydrogen, C1-4alkyl, C2-4alkenyl, C2-4alkynyl, C1-4alkoxy, C1-4alkylthio, halogen, trifluoromethyl, trifluoromethoxy, hydroxy, hydroxy(C1-4)alkyl, cyano, nitro, amino, and amino(C1-4)alkyl;

    wherein amino and the amino portion of amino(C1-4)alkyl are optionally and independently substituted with one to two C1-4alkyl substituents;

    R4 and R5 are independently C2-8alkylene optionally substituted with oxo;

    R2 is —

    N(Ra)—

    C1-4alkyl-X—

    C1-4alkyl-N(Rb), wherein C1-4alkyl is optionally substituted with one to four substituents independently selected from the group consisting of C1-4alkyl, C2-4alkenyl, C2-4alkynyl, C1-4alkoxy, C1-4alkoxy(C1-4)alkyl, carboxyl, carboxyl(C1-4)alkyl, C1-4alkoxycarbonyl, C1-4alkoxycarbonyl(C1-4)alkyl, amino, amino(C1-4)alkyl, halogen, (halo)1-3(C1-4)alkyl, (halo)1-3(C1-4)alkoxy, hydroxy, hydroxy(C1-4)alkyl, and oxo;

    wherein amino and the amino portion of amino(C1-4)alkyl are optionally and independently substituted with one to two C1-4alkyl substituents;

    Ra and Rb are independently selected from the group consisting of hydrogen, C1-6alkyl, C2-6alkenyl, and C2-6alkynyl;

    wherein C1-6alkyl, C2-6alkenyl, and C2-6alkynyl are optionally substituted with fluoro;

    X is O or S;

    such that the —

    R4

    R2

    R5

    containing macrocycle does not exceed 25 atoms in size;

    and enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts thereof.

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