Antagonists with position 13 modification
    2.
    发明授权
    Antagonists with position 13 modification 失效
    具有13位修饰的拮抗剂

    公开(公告)号:US5093233A

    公开(公告)日:1992-03-03

    申请号:US514394

    申请日:1990-04-25

    IPC分类号: A61K38/00 C07K14/635

    CPC分类号: C07K14/635 A61K38/00

    摘要: The present invention relates to the use of peptide hormone analogues as inhibitors of their respective naturally occurring peptide hormone. The structure of the peptide hormone analogues is exemplified by parathyroid hormone (PTH), wherein Lys.sup.13 is substituted to increase the biological activity of the PTH analogues. Thus, there are disclosed peptides having the formulae:PTH(7-34)NH.sub.2 ;[Tyr.sup.34 ]PTH(7-34)NH.sub.2 ;[D-Trp.sup.12, Tyr.sup.34 ]PTH(7-34)NH.sub.2 ;[Nle.sup.8,18, D-Trp.sup.12, Tyr.sup.34 ]PTH(7-34)NH.sub.2 ;[Nle.sup.8,18, Tyr.sup.34 ]PTH(7-34)NH.sub.2 ;desamino[Nle.sup.8,18, D-Trp.sup.12, Tyr.sup.34 ]PTH(7-34)NH.sub.2 ; and,desamino[Nle.sup.8,18, D-Trp.sup.12, Tyr.sup.34 ]PTH(8-34)NH.sub.2wherein Lys.sup.13 is modified in the epsilon-amino acid group by N,N-diisobutyl or 3-phenylpropanoyl.

    摘要翻译: 本发明涉及肽激素类似物作为其各自天然存在的肽激素的抑制剂的用途。 肽激素类似物的结构以甲状旁腺激素(PTH)为例,其中Lys13被取代以增加PTH类似物的生物学活性。 因此,公开了具有下式的肽:PTH(7-34)NH 2; [Tyr34] PTH​​(7-34)NH2; [D-Trp12,Tyr34] PTH​​(7-34)NH2; [Nle8,18,D-Trp12,Tyr34] PTH​​(7-34)NH2; [Nle8,18,Tyr34] PTH​​(7-34)NH2; 脱氨基[Nle8,18,D-Trp12,Tyr34] PTH​​(7-34)NH 2; 和脱氨基[Nle8,18,D-Trp12,Tyr34] PTH​​(8-34)NH2,其中Lys13在ε-氨基酸基团中被N,N-二异丁基或3-苯基丙酰基修饰。

    Humoral hypercalcemic factor antagonists
    5.
    发明授权
    Humoral hypercalcemic factor antagonists 失效
    体液高钙血症因子拮抗剂

    公开(公告)号:US5114843A

    公开(公告)日:1992-05-19

    申请号:US662340

    申请日:1991-02-25

    IPC分类号: A61K38/00 C07K14/635

    CPC分类号: C07K14/635 A61K38/00

    摘要: The present invention relates to the use of peptide analogues as inhibitors of their respective naturally occurring peptides. The structure of the peptide analogues is exemplified by an internal region of the N-terminus of humoral hypercalcemic factor hHCF, and truncations thereof: hHCF(14-34)NH.sub.2, hHCF(13-34)NH.sub.2, hHCF(12-34)NH.sub.2, hHCF(11-23)NH.sub.2, hHCF(10-34)NH.sub.2, hHCF(9-34)NH.sub.2, hHCF(8-34)NH.sub.2 and various amino acid substitutions.

    摘要翻译: 本发明涉及肽类似物作为其各自天然存在的肽的抑制剂的用途。 肽类似物的结构的例子是体液高钙血症因子hHCF的N末端的内部区域及其截短:hHCF(14-34)NH2,hHCF(13-34)NH2,hHCF(12-34)NH2 ,hHCF(11-23)NH2,hHCF(10-34)NH2,hHCF(9-34)NH2,hHCF(8-34)NH2和各种氨基酸取代。

    PTH2 RECEPTOR SELECTIVE COMPOUNDS
    8.
    发明申请
    PTH2 RECEPTOR SELECTIVE COMPOUNDS 审中-公开
    PTH2受体选择性化合物

    公开(公告)号:US20090226477A1

    公开(公告)日:2009-09-10

    申请号:US12413303

    申请日:2009-03-27

    IPC分类号: A61K39/00 C07K14/00 A61K38/16

    CPC分类号: C07K14/635 A61K38/00

    摘要: This invention relates to a series of PTH and PTHrP analogues that selectively bind to PTH2 receptors and as such may be useful in treating abnormal CNS functions; abnormal pancreatic functions; divergence from normal mineral metabolism and homeostasis; male infertility; regulation of abnormal blood pressure; and hypothalmic disease.

    摘要翻译: 本发明涉及一系列选择性结合PTH2受体的PTH和PTHrP类似物,因此可用于治疗异常CNS功能; 胰腺功能异常; 与正常的矿物质代谢和体内平衡的分歧; 男性不育症 调节异常血压​​; 和下丘脑疾病。