摘要 |
The present invention relates to dipeptidyl peptidase resistant BNP agonists, their synthesis and therapeutic applications thereof. In particular the present invention relates to compounds of formula (I): R-Xaa1-Xaa2-Xaa3-Pep-OH ; wherein R is selected from the group comprising hydrogen, acetyl, formyl, or alkyl, wherein Xaa1 is an amino-acid selected from serine, alanine, threonine or asparagine, Xaa2 is a L-amino acid or a D-amino acid, different from L-proline, L-alanine, L-glycine or L-serine, optionally substituted by at least one substituent selected from alkyl, aryl or acyl, and Xaa3 is a L-amino acid or a D-amino acid, optionally substituted by at least one substituent selected from alkyl, acetyl, or aryl, wherein Xaa1, Xaa2, Xaa3 are linked to each other by peptide bonds or pseudo-peptide bonds, and wherein Pep is a peptide sequence comprising not more than 29 amino acid residues said sequence comprising a disulfide linked ring structure said ring comprising between 12 and 20 amino acids, wherein the disulfide bond is formed by two cysteines. |
申请人 |
AIC;LAMBEIR, ANNE-MARIE;BRANDT, INGER;SCHARPE, SIMON;DE MEESTER, INGRID |
发明人 |
LAMBEIR, ANNE-MARIE;BRANDT, INGER;SCHARPE, SIMON;DE MEESTER, INGRID |