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Composition and method for treating allergic diseases

  • US 6,221,880 B1
  • Filed: 10/06/1999
  • Issued: 04/24/2001
  • Est. Priority Date: 10/09/1998
  • Status: Expired due to Fees
First Claim
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1. A pharmaceutical composition comprising, in combination, a therapeutically effective amount of at least one neurokinin antagonist or a pharmaceutically acceptable derivative thereof, and a therapeutically effective amount of at least one leukotriene antagonist or a pharmaceutically acceptable derivative thereof, wherein said neurokinin antagonist is a compound having the general formula:

  • where B is OR2;

    NR6COR2, CONR6R7 or NR2CONR6R7,m=0 or 1, P is R5-aryl;

    or R5-heteroaryl; and

    Y is H, CR2R3CO2R6;

    CR2R3CONR6R7 or CR2R3NR6COR2, a═

    b═

    0, 1 or 2;

    Q has the same definitions as P above, with the proviso that P and Q may be the same or different;

    A is=N—

    OR1;

    =N—

    NR2R3;

    or=CR1R2;

    X is —

    O—

    ;



    NR6

    ;



    N(R6)CO—

    ;

    or —

    CO—

    NR6

    ;

    T is R4-aryl;

    R4-heteroaryl;

    R4-cycloalkyl;

    or R2-bridged cycloalkyl;

    R1 is H, C1-C6 alkyl;

    or (CH2),-G where n═

    1-6, G is H;

    R4-aryl;

    R4-heteroaryl;

    COR6;

    CO2R6;

    CONR6R7;

    CN;

    OCOR6;

    SO3R2;

    C(═

    NOR2)NR6R7;

    C(=NR2)NR6R7, with the proviso that when n≠

    1, G can additionally be OR6, NR6R7 or NR6(CO)R7;

    R2 and R3 are independently H or C1-C6 alkyl;

    R4 and R5 are independently 1, 2 or 3 substituents independently selected from OR2, OC(O)R2, OC(O)NR6R7, C1-C6 alkyl, H, halogen, CF3, C2F5, or OCF3; and

    R6 and R7 are independently selected from H or C1-C6 alkyl, with the proviso that when R6 and R7 are part of NR6R7 then said NR6R7 may form part of a C5-C6 ring wherein 0-2 ring members are selected from the group consisting of —

    O—

    , —

    S—

    and —

    NR2

    , with the further proviso that said C5-C6 ring may contain substituents on said ring, with said substituents being selected from the group consisting of hydrogen, halogen, —

    OR6 and —

    COOR6.

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