493036-26-3Relevant academic research and scientific papers
Lactams as EP4 prostanoid receptor agonists. 3. Discovery of N-ethylbenzoic acid 2-pyrrolidinones as subtype selective agents
Elworthy, Todd R.,Brill, Emma R.,Chiou, San-San,Chu, Frances,Harris, Jason R.,Hendricks, R. Than,Huang, Jane,Kim, Woongki,Lach, Leang K.,Mirzadegan, Tara,Yee, Calvin,Walker, Keith A. M.
, p. 6124 - 6127 (2007/10/03)
Two distinct synthetic schemes were applied to access heteroatom-containing α-chain lactams or lactams terminated as aryl acids. The latter lactams were devised using a pharmacophore for EP4 receptor activity. γ-Lactams were characterized for their prostanoid EP receptor affinities and EP 4 activity and found to be selective for the EP2 and EP4 receptors or selective for the EP4 subtype. Benzoic acid 17 displayed enhanced in vivo exposure relative to 3.
8-Aza-11-deoxy prostaglandin analogues
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, (2008/06/13)
This invention relates to compounds which are generally EP4 receptor agonists and which are represented by Formula I: wherein A is a —CH2—CH2—, or —CH═CH—; B is absent, an aryl, or heteroaryl group; R1 is alkyl, alkenyl, alkynyl, cycloalkylalkyl, heterocyclylalkyl, aryl, arylalkyl or heteroaryl, when B is aryl or heteroaryl and R3, R4, R5 and R6 are not simultaneously hydrogen, or R1 is heterocyclylalkyl, aryl, or heteroaryl when B is absent and R3, R4, R5 and R6 are simultaneously hydrogen; and the other substituents are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.
