Patent ID: 7067505
Filing Date: 2006-06-27
Classification: A61P,C07J

Abstract:
1. A di-steroidal prodrug of estradiol having the following formula: wherein R is selected from the group consisting of wherein X and Y are independently selected from and Z is (i) an aliphatic straight chain having 1 to 10 carbon atoms which may be saturated or unsaturated and optionally may be substituted by one or more lower alkyl, hydroxy or amino groups, (ii) A-B-D wherein A and D are independently wherein f is 0 to 5, and B is —O—(CH 2 CH 2 O) p —, wherein p is 1 to 700, or (iii) a peptide linkage having 2 to 15 amino acid units derived independently from amino acids selected from the group consisting of alanine, arginine, asparagine, aspartic acid, cysteine, glutamine, glutamic acid, glycine, histidine, isoleucine, leucine, lysine, methionine, phenylalanine, proline, serine, threonine, tryptophan, tyrosine, valine, or combinations thereof wherein the end groups of the peptide are amino acid units independently derived from aspartic acid and glutamic acid.