Martin De Kort;Jeffry Abraham Jacobus Wisse;Marion Blomenrohr;Miranda Maria Cornelia Van Der Lee
发明人:
Marion Blomenrohr,Martin De Kort,Miranda Maria Cornelia Van Der Lee,Jeffry Abraham Jacobus Wisse
申请号：
US14236694
公开号：
US09127038B2
申请日:
2012.08.01
申请国别(地区):
US
年份:
2015
代理人:
摘要：
The invention relates to kisspeptide-pentasaccharide conjugates having the general formula (I) wherein Z1 is Tyr or D-Tyr； Z3 is Trp, Hyp, Phe or Lys(R2)； Z5 is Thr, Aib or Ala； Z7 is Gly or azaGly； Z8 is Leu； or Z7 and Z8 together represent； Z10 is Phe or Trp； n is 0 or 1； or R2, when present, represents a pentasaccharide derivative having the formula (II) wherein R is methyl or SO3X； X is a positively charged counterion； with the proviso that when R2 is present, R1 is H or (C1-6) alkylcarbonyl； R3 is H or (C1-3)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.
