abstract |
The invention relates to 5-HT6 receptor antagonists. Novel arylamine compounds having the formula: (see formula I) and pharmaceutically acceptable salts and/or esters thereof, wherein - n is 0, 1, 2, 3, or 4; - A, when present is a lower alkyl group; - R1 is hydrogen or substituted or unsubstituted alkyl or aryl; - R2 is hydrogen; halo; nitro; cyano, lower alkoxy; carboxylate salt acid or alkyl ester thereof; a sulfone; haloalkyl or haloalkoxy; acetaldehyde; carboxamide; carbomyl; alkoxyaminocarbonyl; or substituted arylalkylamino; - R3 and R4 independently are hydrogen, substituted or unsubstituted alkyl, aryl, alkylaryl, heteroaryl or alkylheteroaryl, or, taken together, R3 and R4 form one substituted or unsubstituted aryl, alkylaryl, heteroaryl or alkylheteroaryl group; - B, when present, is lower alkyl; and - X and Y are independently C or N; and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with serotonin action, such as in treating obesity, and obesity-related disorders, e.g., cardiovascular disease, digestive disease, respiratory disease, cancer and type II diabetes; and psychological disorders such as schizophrenia, are disclosed. |