Serotonin reuptake inhibitors as drugs having peripheral-system-restricted activity

摘要

Serotonin reuptake inhibitor compounds which are designed to exert serotonin uptake inhibitory activity in the peripheral system while being devoid of CNS activity, and a process of preparing same are disclosed. Further disclosed are pharmaceutical compositions containing same and uses thereof in the treatment of medical conditions associated with peripheral serotonin levels and/or activity, and/or platelet aggregation.

主权项

1. A method of treating a disease or disorder in which reducing or preventing platelet aggregation and/or platelet-endothelial interactions is beneficial, the method comprising administering to a subject in need thereof a therapeutically effective amount of a serotonin reuptake inhibitor (SRI) compound which comprises citalopram modified so as to comprise at least one positively charged group, said at least one positively charged group being a quaternary ammonium group, wherein said quaternary ammonium group has the formula:
—(NR1R2R3)+Z− wherein: Z is an organic or inorganic anion; R1 and R2 are each methyl; and R3 is alkyl having from 1 to 4 carbon atoms.