Non-endogenous, constitutively activated human serotonin receptors and small molecule modulators thereof

A compound of formula (C) ##STR30## Wherein:

• W is Me, or Et, or halogen;
• X is either Oxygen or Sulfur;
• Y is NR.sup.2 R.sup.3, or (CH.sub.2).sub.m R.sup.4, or O(CH.sub.2).sub.n R.sup.4 ;
• Z is lower alkyl (C.sub.1-6);
• m=0-4;
• n=0-4;
• R.sup.1 is H or lower alkyl (C.sub.1-4);
• R.sup.2 is H or lower alkyl(C.sub.1-4);
• R.sup.3 is a C.sub.1-6 alkyl, or C.sub.2-6 alkenyl, or cycloalkyl, or (CH.sub.2).sub.k aryl group (k=1-4) and each said group may be optionally substituted by up to four substituents in any position independently selected from CF.sub.3, CCl.sub.3, Me, NO.sub.2, OH, OMe, OEt, CONR.sup.5 R.sup.6, NR.sup.5 R.sup.6, OCF.sub.3, SMe, COOR.sup.7, SO.sub.2 NR.sup.5 R.sup.6, SO.sub.3 R.sup.7, COMe, COEt, CO-lower alkyl, SCF.sub.3 CN, C.sub.2-6 alkenyl, H, halogens, C.sub.1-4 alkoxy, C.sub.3-6 cycloalkyl, C.sub.1-6 alkyl, aryl, and aryloxy wherein each of the C.sub.3-6 cycloalkyl, C.sub.1-6 alkyl, aryl, or aryloxy groups may be further optionally substituted by up to four substituents in any position independently selected from CF.sub.3, CCl.sub.3, Me, NO.sub.2, OH, OMe, OEt, CONR.sup.5 R.sup.6, NR.sup.5 R.sup.6, NHCOCH.sub.3, OCF3, SMe, COOR.sup.7, SO.sub.3 R.sup.7, SO.sub.2 NR.sup.5 R.sup.6, COMe, COEt, CO-lower alkyl, SCF.sub.3, CN, C.sub.2-6 alkenyl, H, halogens, C.sub.1-4 alkoxy, C.sub.3-6 cycloalkyl, C.sub.1-6 alkyl, and aryl;
• R.sup.4 is a C.sub.1-6 alkyl, or C.sub.2-6 alkenyl, or cycloalkyl, or aryl group and each said group may be optionally substituted by up to four substituents in any position independently selected from CF.sub.3, CCl.sub.3, Me, NO.sub.2, OH, OMe, OEt, CONR.sup.5 R.sup.6, NR.sup.5 R.sup.6, OCF.sub.3, SMe, COOR.sup.7, SO.sub.2 NR.sup.5 R.sup.6, SO.sub.3 R.sup.7, COMe, COEt, CO-lower alkyl, SCF.sub.3 CN, C.sub.2-6 alkenyl, H, halogens, C.sub.1-4 alkoxy, C.sub.3-6 cycloalkyl, C.sub.1-6 alkyl, aryl, and aryloxy wherein each of the C.sub.3-6 cycloalkyl, C.sub.1-6 alkyl, aryl, or aryloxy groups may be further optionally substituted by up to four substituents in any position independently selected from CF.sub.3, CCl.sub.3, Me, NO.sub.2, OH, OMe, OEt, CONR.sup.5 R.sup.6, NR.sup.5 R.sup.6, NHCOCH.sub.3, OCF3, SMe, COOR.sup.7, SO.sub.3 R.sup.7, SO.sub.2 NR.sup.5 R.sup.6, COMe, COEt, CO-lower alkyl, SCF.sub.3, CN, C.sub.2-6 alkenyl, H, halogens, C.sub.1-4 alkoxy, C.sub.3-6 cycloalkyl, C.sub.1-6 alkyl, and aryl;
• R.sup.5 and R.sup.6 are independently a H, or C.sub.1-6 alkyl, or C.sub.2-6 alkenyl, or cycloalkyl, or aryl, or CH.sub.2 aryl group and each said group may be optionally substituted by up to four substituents in any position independently selected from CF.sub.3, CCl.sub.3, Me, NO.sub.2, OH, OMe, OEt, CONR.sup.7 R.sup.8, NR.sup.7 R.sup.8, NHCOCH.sub.3, OCF.sub.3, SMe, COOR.sup.9, SO.sub.3 R.sup.7, SO.sub.2 NR.sup.7 R.sup.8, COMe, COEt, CO-lower alkyl, SCF.sub.3, CN, C.sub.2-6 alkenyl, H, halogens, C.sub.1-4 alkoxy, C.sub.3-6 cycloalkyl, C.sub.1-6 alkyl, and aryl wherein each of the C.sub.3-6 cycloalkyl, C.sub.1-6 alkyl, or aryl groups may be further optionally substituted by up to four substituents in any position independently selected from CF.sub.3, CCl.sub.3, Me, NO.sub.2, OH, OMe, OEt, CONR.sup.8 R.sup.9, NR.sup.8 R.sup.9, NHCOCH.sub.3, OCF.sub.3, SMe, COOR.sup.7, SO.sub.2 NR.sup.8 R.sup.9, SO.sub.3 R.sup.7, COMe, COEt, CO-lower alkyl, SCF.sub.3, CN, C.sub.2-6 alkenyl, H, halogens, C.sub.1-4 alkoxy, C.sub.3-6 cycloalkyl, C.sub.1-6 alkyl, and aryl,
• or R.sup.5 and R.sup.6 may form part of a 5, 6 or 7 membered cyclic structure which may be either saturated or unsaturated and that may contain up to four heteroatoms selected from O, N or S and said cyclic structure may be optionally substituted by up to four substituents in any position independently selected from CF.sub.3, CCl.sub.3, Me, NO.sub.2, OH, OMe, OEt, OCF.sub.3, SMe, COOR.sup.7, SO.sub.2 NR.sup.8 R.sup.9, SO.sub.3 R.sup.7, NHCOCH.sub.3, COEt, COMe, or halogen;
• R.sup.7 may be independently selected from H or C.sub.1-6 alkyl;
• R.sup.8 and R.sup.9 are independently a H, or C.sub.1-6 alkyl, or C.sub.2-6 alkenyl, or cycloalkyl, or aryl, or CH.sub.2 aryl group and each said group may be optionally substituted by up to four substituents in any position independently selected from halogen, CF.sub.3, OCF3, OEt, CCl.sub.3, Me, NO.sub.2, OH, OMe, SMe, COMe, CN, COOR.sup.7, SO.sub.3 R.sup.7, COEt, NHCOCH.sub.3, or aryl;
• an aryl moiety can be a 5 or 6 membered aromatic heterocyclic ring (containing up to 4 hetero atoms independently selected from N, O, or S) or a 6 membered aromatic non-heterocyclic ring or a polycycle;
• with the proviso that said compound is not:
• N-[3-(4-bromo-1-methylpyrazol-3-yl)phenyl][methylamino]carboxamide, or
• N-[3-(4-bromo-1-methylpyrazol-3-yl)phenyl][{(4-trifluoromethoxy)phenyl}amin o] carboxamide, or
• N-[3-(4-bromo-1-methylpyrazol-3-yl)phenyl][2-chlorophenyl]carboxamide, or
• N-[3-(4-bromo-1-methylpyrazol-3-yl)phenyl][2-chloro-3-pyridyl]carboxamide, or
• N-[3-(4-bromo-1-methylpyrazol-3-yl)phenyl][trichloromethyl]carboxamide.