LHRH ANTAGONIST DERIVATIVE, AND PREPARATION METHOD AND APPLICATIONS THEREOF

摘要

The present invention provides an LHRH antagonist derivative, as represented by Formula (I), modified at position 5 and 6 by water soluble groups and water-soluble vitamins, the preparation method thereof, and applications thereof in preparing contraceptive medicines and medicines for treating sex hormone-related diseases. Also provided are stereoisomers, solvates, or physiologically non-toxic salts of the LHRH antagonist derivative as represented by Formula (I), and pharmaceutical compositions comprising said compounds. The LHRH antagonist derivative of the present invention maintains the activity of the original antagonist, has a low histamine-releasing activity and enhanced water solubility, and is therefore good for clinical application. R-D-Nal-D-Cpa-D-Aaa3-Ser-Aaa5-Aaa6-Leu-Aaa8-Pro-D-Ala-B Formula (I)