| abstract |
The present invention discloses novel 5-HT receptor binding agents of Formula 3, wherein X is -CH or -N-. Y is selected from the group consisting of -CR10R11, -NR12, -0-, -S-, -SO-, and -SO2-. R1 to R12 are various substituents selected to optimize the physicochemical and biological properties such as receptor binding, receptor selectivity, tissue penetration, lipophilicity, toxicity, bioavailability, and pharmacokinetics of compounds of Formula 3. These include hydrogen, alkyl, acyl, hydroxyl, hydroxyalkyl, aryl, amino, aminoalkyl, alkoxyl, aryloxyl, carboxyl, alkoxycarbonyl, halogen, cyano, and other suitable electron donating or electron withdrawing groups. R2 and R3, R3 and R4, or R5 and R6 may optionally be tethered together to form fused alicyclic or heterocyclic ring. R1 and R2, R4 and R5, or R6 and R7 may also optionally be tethered together to form spiro carbo- or heterocyclic ring. |