The authors analyse the original and literature data concerning thienopyrimidine derivatives showing the activity of luteinizing hormone (LH) receptor agonists. These compounds are known to specifically interact with the allosteric site of LH receptors localized in the transmembrane channels and activate the LH-sensitive adenylate cyclase signal system. The thienopyrimidine derivatives were shown to stimulate steroidogenesis and ovulation both in vitro and in vivo by acting on the cells that have not only normal but also mutant receptors. The thienopyrimidine derivatives are believed to be efficacious inducers of ovulation in the women.