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Phenylethylamine analogs and their use for treating glaucoma

  • US 20070072920A1
  • Filed: 09/22/2006
  • Published: 03/29/2007
  • Est. Priority Date: 09/23/2005
  • Status: Abandoned Application
First Claim
Patent Images

1. A method for lowering and controlling normal or elevated IOP, which comprises administering a composition comprising a pharmaceutically acceptable carrier and a pharmaceutically effective amount of a compound of the formula:

  • embedded image wherein R1 and R2 independently are H or C1-4alkyl;

    R3 and R4 independently are H, C1-4 alkyl, or R3, R4 and the carbon atom to which they are attached can form a cyclopropyl ring;

    Y is H, C1-4alkyl, or OR5;

    R5 is H or C1-4 alkyl;

    A and B independently are OH, C1-3alkoxy, OS(O)2W, OC(═

    O)W, or OC(═

    O)NW2W3;

    W is C1-4alkyl;

    W2 and W3 independently are H or C1-4alkyl;

    X is CH(OH)R6, C(═

    O)R6, (CH2)nZ, or (CH2)mZ′

    ;

    R6 is C1-4 alkyl, (CH2)m2SR8, or (CH2)m2OR8;

    n is 1-4;

    m is 2-4;

    m2 is 1-4;

    Z is OCF3, CN, S(O)n2R6, C(O)NR7R6, C(C═

    O)R6, CH(OH)R6, SO2NR7R8, NR6R9, CO2R6, S(O)n2CH2CH(OH)R6, S(O)n2CH2C(═

    )O)R6, S(O)n2CH2CO2R6, S(O)n2CH2C(═

    O)NR7R8, aryl, heterocyclyl, or heteroaryl;

    Z′

    is OH or OR6;

    n is 0 or 1;

    R7 is H, C1-4alkyl, OH, or OCH3; and

    R8 and R9 independently are H or C1-4alkyl.

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