申请人:Lau Jesper
公开号:US20070203058A1
公开(公告)日:2007-08-30
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 —(CH
2
)
l
D[(CH
2
)
n
E]
m
(CH
2
)
p
Q
q
-, wherein l, m and n independently are 1-20 and p is 0-10, Q is -Z-(CH
2
)
l
D[(CH
2
)
n
G]
m
(CH
2
)
p
—, q is an integer in the range from 0 to 5, each D, E and G independently are selected from —O—, NR
3
—, —N(COR
4
)—, —PR
5
(O)—, and —P(OR
6
)(O)—, wherein R
3
, R
4
, R
5
, and R
6
independently represent hydrogen or C
1-6
-alky, Z is selected from —C(O)NH—, —C(O)NHCH
2
—, —OC(O)NH—, —C(O)NHCH
2
CH
2
—, —C(O)CH
2
—, —C(O)CH═CH—, —(CH
2
)
s
—, —C(O)—, —C(O)O— or —NHC(O)—, wherein s is 0 or 1.