Non-peptide GnRH agents
OwnerMark Brian Anderson, Alexander Polinsky +2inventors
InventorsMark Brian Anderson, Alexander Polinsky, Yufeng Hong, Vlad Edward Gregor
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Abstract
Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are of the following general formula, where X1, X2, Y, and Z are defined variables: Such compounds and their pharmaceutically acceptable salts, multimers, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds and intermediates useful in their preparation are also described.
Claims4
A compound, salt, multimer, prodrug, or active metabolite, wherein the compound is of the following formula:
- wherein Y is a lipophilic group selected from substituted and unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, and heteroaryl, where the number of carbon atoms present in Y ranges from 6 to 20.
A compound, salt, multimer, prodrug, or active metabolite, wherein the compound is of the following formula:
- wherein Z is a group selected from substituted and unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl, heterocycle, aryl, heteroaryl, CH2OR, 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.
A compound of one of the following Formulae II, III, and IV:
- wherein
- j is 1 or 2;
- k is 1, 2, 3, 4 or 5;
- R8 is H or substituted or unsubstituted lower alkyl;
- R9 is H or substituted or unsubstituted lower alkyl, CN, NO2 or CO2R1;
- R10 is H or substituted or unsubstituted:
- lower alkyl, CH2OR1;
- (CH2)pOR1;
- CO2R1;
- or (CH2)pC(O)R2, where p is an integer from 1 to 6, and R2 is H, OR1, SR1, N(R1)2, or C(R1)3;
- R11 is H or substituted or unsubstituted lower alkyl, CH2O-phenyl, CH2O-benzyl, phenyl, or benzyl;
- or any two of R8, R9, R10, and R11 taken together form a 5- or 6-membered heterocycle;
- and where each R1 is independently selected from H and substituted or unsubstituted lower alkyl, O-lower alkyl, and S-lower alkyl.
A compound selected from the group consisting of:
Dependencies are inferred from the claim text.