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Phenylindole derivatives as 5-HT2A receptor ligands

  • US 6,486,153 B1
  • Filed: 03/03/2000
  • Issued: 11/26/2002
  • Est. Priority Date: 09/04/1997
  • Status: Expired due to Fees
First Claim
Patent Images

1. A compound having formula I, or a pharmaceutically acceptable salt thereof;

  • embedded imagewhereinA represents hydrogen, halogen, cyano, nitro, trifluoromethyl, trifluoromethoxy, C1-6 alkyl or C1-6 alkoxy;

    B represents trifluoromethyl or trifluoromethoxy,;

    X and Y independently represent hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy or phenyl;

    R1 represents hydrogen or C1-6 alkyl;

    R2 represents hydrogen, methyl, ethyl, 2-methoxyethyl, n-propyl, isopropyl, n-butyl, 2-methylpropyl, tert-butyl or n-pentyl; and

    R3 represents C1-6 alkyl, C2-6 alkenyl, C3-9 cycloalkyl, aryl, C3-7 heterocycloalkyl, C3-7 heterocycloalkyl(C1-6)alkyl, heteroaryl or heteroaryl(C1-6)alkyl, any of which groups may be optionally substituted by one or more substituents;

    or R2 and R3 taken together with the intervening nitrogen atom represent a group of formula (a), (b), (c), (d), (e), (f), (g), (h), (i), (j), (k), (l) or (m);

    embedded imageembedded imagein which the broken line represents an optional chemical bond;

    Z represents oxygen, sulphur, N—

    R6 or CR7R8;

    R4 represents hydrogen, C1-6 alkyl, C1-6 alkoxy(C1-6)alkyl, C3-7 heterocycloalkyl(C1-6)alkyl or aryloxy;

    R5 represents hydrogen, C1-6 alkyl or C1-6 alkoxy(C1-6)alkyl;

    R6 represents hydrogen, —

    COR9 or —

    CO2R9;

    or C1-6 alkyl, C2-6 alkenyl, C3-9 cycloalkyl, aryl(C1-6)alkyl, aryl(C2-6)alkenyl, C3-7 heterocycloalkyl(C1-6)alkyl or heteroaryl, any of which groups may be optionally substituted by one or more substituents;

    R7 represents hydrogen, hydrocarbon, a heterocyclic group, —

    COR9 or —

    CO2R9, R8 represents hydrogen, phenyl or acetoxy; and

    R9 represents C1-6 alkyl.

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