Patent ID: 6218426
Filing Date: 2001-04-17
Classification: A61P,C07C,C07D

Abstract:
A pharmaceutical composition comprising:(a) a therapeutically effective amount of a GnRH agent selected from the group consisting of compounds of the Formula I: ##STR252##wherein:Z is a group selected from substituted and unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl, heterocycle, aryl, heteroaryl, CH.sub.2 OR and C(O)OR, where R is substituted or unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl or heteroaryl, and where the number of carbon atoms present in Z ranges from 1 to 12;Y is a lipophilic group selected from substituted and unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, and heteroaryl, where the number of carbons atoms present in Y ranges from 6 to 20;X.sub.1 is a structural unit connecting CH.sub.2 NC(O), X.sub.2, Y, and Z in three-dimensional space that is selected from substituted and unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, and heteroaryl such that the atom count in the chain portion of the unit linking the central nitrogen to X.sub.2 ranges from 3 to 8; andX.sub.2 is a basic group having a pK.sub.a greater than about 8 and is guanidinyl, amidinyl, or amino, unsubstituted or substituted with one or more lower alkyls; and pharmaceutically acceptable salts, multimers, prodrugs, and active metabolites thereof; and(b) a pharmaceutically acceptable carrier or diluent.