David J. Blythin

TL;DR: A series of novel five- and six-membered ring urea derivatives have been described as potent and selective NK1 receptor antagonists and exhibited good oral activity and brain penetration.

TL;DR: In this paper, the authors claim compounds of the: (formula I) is a 5-membered heteroaryl; X is S or O; R1 is H, alkyl, cycloalkyl, cylcoalkylalkyl-, -CH2F, -CHF2, -CF3, -C(O)alkyl or -C (O)NR18R19); R3 and R4 are H, AlkyL, alkenyl, hydroxyalkyl and aminoalkyl; R5 and R6 are H

TL;DR: In this article, pharmaceutical compositions comprising an effective amount of a compound of claim 1, at least one pharmaceutically acceptable carrier, and in combination with a selective serotonin reuptake inhibitor are defined.

TL;DR: A series of novel five-membered urea derivatives as potent NK1 receptor antagonists are described as well as several compounds with high affinity and sustained in vivo activity.