公开(公告)号：US09127038B2

公开(公告)日：2015-09-08

申请号：US14236694

申请日：2012-08-01

申请人： Marion Blomenrohr ,  Martin De Kort ,  Miranda Maria Cornelia Van Der Lee ,  Jeffry Abraham Jacobus Wisse

发明人： Marion Blomenrohr ,  Martin De Kort ,  Miranda Maria Cornelia Van Der Lee ,  Jeffry Abraham Jacobus Wisse

IPC分类号： C07K9/00 ,  A61K47/48

CPC分类号： C07K9/001 ,  A61K47/48092 ,  A61K47/549

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.

摘要翻译： 本发明涉及具有通式（I）的亲肽肽 - 五糖共轭物，其中Z 1是Tyr或D-Tyr; Z3是Trp，Hyp，Phe或Lys（R2）; Z5是Thr，Aib或Ala; Z7是Gly或azaGly; Z8是Leu; 或Z7和Z8一起表示; Z10是Phe或Trp; n为0或1; 或R2，当存在时，表示具有式（II）的五糖衍生物，其中R是甲基或SO 3 X; X为正电荷的抗衡离子; 条件是当R 2存在时，R 1是H或（C 1-6）烷基羰基; R3是H或（C1-3）烷基; L代表具有10-50个原子的药理学无活性接头部分; 或其药学上可接受的盐; 涉及包含该药物组合物的药物组合物以及所述亲肽肽 - 五糖共轭物在治疗女性不孕症中的用途。

公开(公告)号：US20140206627A1

公开(公告)日：2014-07-24

申请号：US14236694

申请日：2012-08-01

申请人： Marion Blomenrohr ,  Martin De Kort ,  Miranda Maria Cornelia Van Der Lee ,  Jeffry Abraham Jacobus Wisse

发明人： Marion Blomenrohr ,  Martin De Kort ,  Miranda Maria Cornelia Van Der Lee ,  Jeffry Abraham Jacobus Wisse

IPC分类号： C07K9/00

CPC分类号： C07K9/001 ,  A61K47/48092 ,  A61K47/549

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.

摘要翻译： 本发明涉及具有通式（I）的亲肽肽 - 五糖共轭物，其中Z 1是Tyr或D-Tyr; Z3是Trp，Hyp，Phe或Lys（R2）; Z5是Thr，Aib或Ala; Z7是Gly或azaGly; Z8是Leu; 或Z7和Z8一起表示; Z10是Phe或Trp; n为0或1; 或R2，当存在时，表示具有式（II）的五糖衍生物，其中R是甲基或SO 3 X; X为正电荷的抗衡离子; 条件是当R 2存在时，R 1是H或（C 1-6）烷基羰基; R3是H或（C1-3）烷基; L代表具有10-50个原子的药理学无活性接头部分; 或其药学上可接受的盐; 涉及包含该药物组合物的药物组合物以及所述亲肽肽 - 五糖共轭物在治疗女性不孕症中的用途。