Highly selective 5-HT(2C) receptor agonists that show anti-psychotic effects with antagonist activity at the 5-HT(2B) receptor

摘要

Highly selective 5-HT(2C) receptor agonists receptors are disclosed. The 5-HT(2C) receptor agonists are used in the treatments of disease and conditions wherein modulation of 5-HT(2C) receptors provides a benefit, such as obesity and psychiatric disorders.

主权项

1. A composition comprising (a) compound having a structural formula: wherein R1, independently, is selected from the group consisting of C1-6alkyl, hydroxyC1-6alkyl, haloC1-6alkyl, C1-6alkenyl, —CF3, —OCF3, C1-6heteroalkyl, —ORa, —SRa, halo, —NO2,—CN, —NC, —C(═O)Ra, —C(═C)ORa, —N(Ra)(Rb), —C(═O)N(Ra)(Rb), —SO2N(Ra)(Rb), —NRcC(═O)Ra, —N═C(Ra)(Rb), —NRcC(═O)ORa, —SO2Ra, —SO3Ra, —P(O)(ORa), —P(═O)(ORa)(ORb), and —NH—P(═O)(ORa)(ORb); Ra and Rb, independently, are selected from the group consisting of H, C1-6alkyl, aryl, heteroaryl, cycloalkyl, and heterocycloalkyl; Rc is H or C1-6alkyl; and n is an integer 0, 1, 2, 3, or 4; or a pharmaceutically acceptable salt or hydrate thereof, and (b) an excipient and/or pharmaceutically acceptable carrier.