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Non-peptide GnRH agents

  • US 6,218,426 B1
  • Filed: 03/01/1999
  • Issued: 04/17/2001
  • Est. Priority Date: 03/05/1998
  • Status: Expired due to Fees
First Claim
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1. A pharmaceutical composition comprising:

  • (a) a therapeutically effective amount of a GnRH agent selected from the group consisting of compounds of the Formula I;

    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;

    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;

    X1 is a structural unit connecting CH2NC(O), X2, 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 X2 ranges from 3 to 8; and

    X2 is a basic group having a pKa 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.

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