Albumin-binding derivatives of therapeutic peptides

Details Albumin-binding derivatives of therapeutic peptides Albumin-binding derivatives of therapeutic peptides

A - Human Necessities

61

K

A61K 47/48 (2006.01)

Patent

CA 2539253

Novel polypeptide derivatives having protracted profile of action. The present invention relates to a compound which comprises a therapeutic polypeptide linked to an albumin binding residue via a hydrophilic spacer. The present invention also relates to a compound which comprises a therapeutic polypeptide linked to an albumin binding residue via a hydrophilic spacer that separates the polypeptide and the albumin binding residue with a chemical moiety comprising at least 5 non-hydrogen atoms where 30-50% of these atoms are either N or O. In one embodiment of this invention the spacer is defined as - (CH2)lD[(CH2)nE]m(CH2)pQq-, wherein l, m and n independently are 1-20 and p is 0-10, Q is -Z-(CH2)lD[(CH2)nG]m(CH2)p-, q is an integer in the range from 0 to 5, each D, E and G independently are selected from -O-, NR3-, -N(COR4)-, - PR5(O)-, and -P(OR6)(O)-, wherein R3, R4, R5, and R6 independently represent hydrogen or C1-6-alky, Z is selected from -C(O)NH-, -C(O)NHCH2-, -OC(O)NH-, - C(O)NHCH2CH2-, -C(O)CH2-, -C(O)CH=CH-, -(CH2)s-, -C(O)-, -C(O)O- or -NHC(O)-, wherein s is 0 or 1.

Nouveaux dérivés de polypeptides présentant un profil d'action prolongée.

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