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Piperazino derivatives as neurokinin antagonists

  • US 5,869,488 A
  • Filed: 08/29/1996
  • Issued: 02/09/1999
  • Est. Priority Date: 05/01/1996
  • Status: Expired due to Fees
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First Claim
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1. A compound of the formula:

  • ##STR181## wherein u is 0 to 2;

    m is 1, and y is 1 to 3;

    or m is 2, and y is 0;

    and with the further proviso that no more than one Rc is other than H in the ##STR182## moiety;

    each Rc is independently selected from the group consisting of H and C1 -C6 alkyl;

    each Ra and Rb is independently selected from the group consisting of H, C1 -C6 alkyl, phenyl, substituted phenyl, benzyl, substituted benzyl and allyl;

    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 member ring;

    each R1 and R2 is independently selected from the group consisting of H, C1 -C6 alkyl, CF3, C2 F5, Cl, Br, I, F, NO2, ORa, CN, NRa Rb, ##STR183## and where Ra is not H in ##STR184## or when R1 and R2 are on adjacent carbons on a ring, they can form ##STR185## wherein n'"'"' is 1 or 2;

    each R3 is independently selected from the group consisting of H, C1 -C6 alkyl, CF3, C2 F5, ##STR186## Cl, Br, I, F, ORa, OCF3, and phenyl;

    Ar1 is ##STR187## Ar2 is ##STR188## Z is ##STR189## n is independently 0-2;

    m2 =1-2;

    n3 is 0-4;

    each Re and Rf is independently selected from the group consisting of H, C1 -C6 alkyl, phenyl, substituted phenyl, benzyl, substituted benzyl and allyl;

    or Re and Rf taken together with the carbon to which they are attached can also form a carbonyl group with the proviso that no more than one carbonyl group is in the ##STR190## moiety;

    n5 is 1;

    R5 is H or C1 -C6 alkyl;

    R6 is H, C1 -C6 alkyl, C3 -C6 cycloalkyl, thienyl, pyridyl, isoxazoyl, ##STR191## or when Re,Rf taken together with the carbon atom to which they are attached form a carbonyl group and n3 is 1, R6 can also be --ORa wherein Ra is not H;

    and wherein substituted means 1 to 3 substituents independently selected from the group consisting of H, C1 -C6 alkyl, CF3, C2 F5, OH, OC1 -C6 alkyl, Cl, Br, I and F;

    or any enantiomer thereof,or a pharmaceutically acceptable salt thereof.

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