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Heterocyclic carboxamides

  • US 6,602,874 B2
  • Filed: 05/22/2001
  • Issued: 08/05/2003
  • Est. Priority Date: 04/15/1998
  • Status: Expired due to Fees
First Claim
Patent Images

1. A method for treating or preventing depression in a mammal, comprising administering to mammal in need thereof:

  • a) a compound of the formula embedded image

    or the pharmaceutically acceptable salt thereof;

    wherein Z is oxygen, S(O)m wherein m is 0, 1 or 2;

    or NQ wherein Q is hydrogen, (C1-C6)alkyl or phenyl;

    X is hydrogen, chloro, fluoro, bromo, iodo, hydroxy, nitro, cyano, (C1-C6)alkyl, trifluoromethyl, (C1-C6)alkoxy, (C1-C6)alkyl S(O)a wherein a is 0, 1 or 2;

    or phenyl wherein the phenyl group is optionally substituted by hydrogen, halo, hydroxy, nitro, cyano, (C1-C6)alkyl, trifluoromethyl, (C1-C6)alkoxy, or (C1-C6)alkyl S(O)b wherein b is 0, 1 or 2;

    Y is embedded image

    wherein M is oxygen or sulfur;

    X is hydrogen, fluoro, chloro, trifluoromethyl, (C1-C6)alkyl, (C1-C6)alkoxy or (C1-C6)alkyl S(O)c wherein c is 0, 1 or 2;

    R1 is embedded imageR6 is selected from the group consisting of hydrogen, (C1-C6)alkyl optionally substituted with (C1-C6)alkoxy or one to three fluorine atoms, or [(C1-C4)alkyl] aryl wherein the aryl moiety is phenyl, naphthyl, or heteroaryl-(CH2)q

    , wherein the heteroaryl moiety is selected from the group consisting of pyridyl, pyrimidyl, benzoxazolyl, benzothiazolyl, benzisoxazolyl and benzisothiazolyl and q is zero, one, two, three or four, and wherein said aryl and heteroaryl moieties may optionally be substituted with one or more substituents independently selected from the group consisting of chioro, fluoro, bromo, iodo, (C1-C6)alkyl, (C1-C6)alkoxy, trifluoromethyl, cyano and (C1-C6)alkylS(O)e, wherein e is 0, 1 or 2;

    R10 is hydrogen or (C1-C6)alkyl;

    R2 is hydrogen, (C1-C4)alkyl, phenyl or naphthyl, wherein said phenyl or naphthyl may optionally be substituted with one or more substituents independently selected from chloro, fluoro, bromo, iodo, (C1-C6)alkyl, (C1-C6)alkoxy, trifluoromethyl, cyano and (C1-C6)alkylS(O)g wherein g is 0, 1 or 2; and

    R3 is —

    (CH2)tB, wherein t is zero, one, two or three and B is hydrogen, phenyl, naphthyl or a 5 or 6 membered heteroaryl group containing from one to four heteroatoms in the ring, and wherein each of the foregoing phenyl, naphthyl and heteroaryl groups may optionally be substituted with one or more substituents independently selected from chloro, fluoro, bromo, iodo, (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl-, trifluoromethyl, trifluoromethoxy, cyano, hydroxy, COGH and (C1-C6)alkylS(O)h wherein h is 0, 1 or 2; and

    b) sertraline or a pharmaceutically acceptable salt thereof wherein the amounts of a) and b) are such that the combination is effective in treating or preventing depression.”

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