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Quinazolinone derivatives as cholyecystokinin (CCK) ligands

  • US 5,756,502 A
  • Filed: 07/10/1995
  • Issued: 05/26/1998
  • Est. Priority Date: 08/08/1994
  • Status: Expired due to Fees
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First Claim
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1. A pharmaceutical composition comprising an effective therapeutic amount of the compound of Formula I and a pharmaceutically acceptable salt thereof with a pharmaceutically acceptable carrier in unit dosage form wherein the therapeutic indication is selected from the group consisting of an appetite suppressant, a gastric acid secretion reducing agent, an anxiety reducing agent, a gastrointestinal ulcer treating agent, a psychosis treating agent, a withdrawal reaction blocking agent, a pain treatment agent, an agent for treating or preventing panic and an agent for treating gastrin-dependent tumors ##STR36## wherein W, X, Y, and Z are each independently selected from C--R3, C--R4, C--R5, C--R6, and N (nitrogen) and that no more than two of W, X, Y, and Z are N;

  • wherein R3, R4, R5 and R6 are each independently hydrogen, hydroxy, sulfhydryl, lower alkoxy (1-4 carbon atoms), lower thioalkoxy (1-4 carbon atoms), lower alkyl (1-4 carbon atoms), halo, CN, CF3, NO2, COOR7 or NR7 R8 ;

    wherein R7 and R8 are independently hydrogen or lower alkyl (1-4 carbon atoms);

    M is oxygen or sulfur;

    B is defined as a direct bond or, ##STR37## wherein i and j are independently 0 or 1;

    R9 and R10 are independently hydrogen, lower alkyl (1-4 carbon atoms), or lower alkoxy (1-4 carbon atoms);

    A is selected from the group consisting of;

    ##STR38## wherein R11 and R12 are independently hydrogen or lower alkyl (1-4 carbon atoms);

    n=0 or 1;

    R1 is;

    an alkyl of 1 to 6 carbon atoms,unsubstituted, mono- or polysubstituted phenyl or polyaromatic,unsubstituted, mono- or polysubstituted heteroaromatic, with hetero atom(s) N (nitrogen), O (oxygen), and/or S (sulfur) or,unsubstituted, mono- or polysubstituted aralkyl,unsubstituted, mono- or polysubstituted cyclo or polycycloalkyl hydrocarbon, ormono- or polyheterocycle (3 to 8 atoms per ring) with 1 to 4 hetero atoms as N (nitrogen), O (oxygen), or S (sulfur); and

    wherein the substitutions are selected from hydrogen, methyl, methoxy, fluorine, bromine, chlorine, iodine, trifluoromethyl, cyano, acetyl, carboxy, carbmethoxy, carbethoxy, amino, N,N-dimethylamino, amido, acetyl, methylene carboxy, tetrazole, nitro, cyclohexyl, and adamantyl;

    R2 is;

    an alkyl of 1 to 6 carbon atoms,unsubstituted, mono- or polysubstituted phenyl or polyaromatic,unsubstituted, mono- or polysubstituted heteroaromatic with hetero atom(s) N (nitrogen), O (oxygen), and/or S (sulfur) or,unsubstituted, mono- or polysubstituted aralkyl,unsubstituted, mono- or polysubstituted cyclo or polycycloalkyl hydrocarbon, ormono- or polyheterocycle (3-8 atoms per ring) with 1 to 4 hetero atoms as N (nitrogen), O (oxygen), or S (sulfur);

    wherein substitutions are selected from hydrogen, methyl, methoxy, fluorine, chlorine, bromine, iodine, hydroxy, ethoxy, propoxy, i-propoxy, t-butoxy, ethyl, propyl, i-propyl, trifluoromethyl, cyclopropoxy, thioisopropyl, cyano, N,N-dimethylamino, N,N-dimethylamino methyl, carboxy, carbmethoxy, and tetrazole.

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