The invention relates to kisspeptide-pentasaccharide conjugates having the general formula (I) wherein Z
1
is Tyr or D-Tyr; Z
3
is Trp, Hyp, Phe or Lys(R
2
); Z
5
is Thr, Aib or Ala; Z
7
is Gly or azaGly; Z
8
is Leu; or Z
7
and Z
8
together represent; Z
10
is Phe or Trp; n is 0 or 1; or R
2
, when present, represents a pentasaccharide derivative having the formula (II) wherein R is methyl or SO
3
X; X is a positively charged counterion; with the proviso that when R
2
is present, R
1
is H or (C
1-6
) alkylcarbonyl; R
3
is H or (C
1-3
)alkyl; and L represents a pharmacologically inactive linker moiety having 10-50 atoms; or a pharmaceutically acceptable salt thereof; to pharmaceutical compositions comprising the same as well as to the use of said kisspeptide-pentasaccharide conjugates in the treatment of female infertility.
US9127038B2
申请人:——
公开号:US9127038B2
公开(公告)日:2015-09-08
Westerduin, Pieter; Basten, Jan E. M.; Broekhoven, Marc A., Angewandte Chemie, 1996, vol. 108, # 3, p. 339 - 342
作者:Westerduin, Pieter、Basten, Jan E. M.、Broekhoven, Marc A.、Kimpe, Vera de、Kuijpers, Will H. A.、Boeckel, Constant A. A.