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Piperazino derivatives as neurokinin antagonists

  • US 5,968,929 A
  • Filed: 10/28/1997
  • Issued: 10/19/1999
  • Est. Priority Date: 10/30/1996
  • Status: Expired due to Fees
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First Claim
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1. A compound of the formula:

  • ##STR275## wherein u is 0 to 2;

    m is 1, and y is 1 to 3;

    or m is 2, and y is 0;

    each Rc is independently selected from the group consisting of H and C1 -C6 alkyl, with the proviso that no more than one Rc is other than H;

    Ra and Rb are independently selected from the group consisting of H, ##STR276## or Ra and Rb together are C3 -C6 alkylene and are attached to the same nitrogen so that Ra and Rb, together with the nitrogen to which they are attached, form a 4 to 7 membered ring;

    R1 and R2 are independently selected from the group consisting of H, ##STR277## or when R1 and R2 are on adjacent carbons on a ring, they can form ##STR278## wherein n'"'"' is 1 or 2;

    R3 is independently selected from the group consisting of H, C1 -C6 alkyl, --CF3, --C2 F5, Cl, Br, I, F, --ORa, --OCF3, phenyl, ##STR279## X6 is ═

    S or ═

    NR8 ;

    Rb '"'"' is Rb or --ORb ;

    R8 is Rm, --ORm, --O(CH2)n10 --Rk or --O(CH2)n11 --Rn ;

    Rm is Ra, thienyl or pyridyl;

    Rk is Rm, --ORm, --SO3 H, --PO3 H or ##STR280## and n10 is 2-4;

    Rn is CN or ##STR281## and n11 is 1-4;

    X7 is ═

    O, ═

    S, ═

    NRa or ═

    N--ORa ;

    Ar1 is ##STR282## m1 and m2 are independently 0 or 1;

    n6 is 0 to 2;

    X5b is (H, H);

    G is ##STR283## n3 is 0 to 4;

    X8 is --ORm, --SRm, halogen, --O--(CH2)n10 --Rk, --O--(CH2)n11 --Rn, --S--(CH2)n10 --Rk or --S--(CH2)n11 --Rn ;

    ##STR284## Rh is H, C1 -C6 alkyl, --C(O)Ra, --C(O)NRa Rb, --C(O)ORa, --C(O)CH(N(Ra)(Rb))--R7, --SO2 Rm, --(CH2)n10 --Rk, --(CH2)n11 --Rn, ##STR285## provided that when Rh is --C(O)ORa, Ra is not H;

    Ri is --CN or --Ra ;

    Re and Rf are independently selected from the group consisting of H, ##STR286## and when G is ##STR287## R6 can also be ##STR288## n8 is 0, 1 or 2;

    n9 is 1 or 2;

    R7 is ##STR289## provided that when X5b is (H,H), m1 is 0 or 1 and m2 is 0, G is not ##STR290## when R3 is H, C1 -C6 alkyl, --CF3, --C2 F5, Cl, Br, I, F, --ORa, --OCF3, phenyl, ##STR291## or an enantiomer or diastereomer thereof, or a pharmaceutically acceptable salt thereof.

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