COMPOUNDS HAVING PEPTIDES CONJUGATED TO BONE TARGETING MOIETIES AND METHODS OF MAKING AND USING THEREOF

    公开(公告)号:EP2488208B1

    公开(公告)日:2018-11-21

    申请号:EP10823111.9

    申请日:2010-10-12

    IPC分类号: A61K38/23 A61K47/54 A61P19/08

    摘要: Described herein are compositions having a peptide sequence that includes at least one bone targeting moiety, wherein the bone targeting moiety is bonded to the peptide sequence by a linker, wherein the peptide sequence is calcitonin, and wherein the composition is neutral or a pharmaceutically acceptable salt or ester thereof. In one aspect, calcitonin inhibits or slows osteoclast mediated resorptive bone loss. The compounds described herein can be used in a number of therapeutic applications including treating or preventing conditions associated with bone loss, which include, but are not limited to, osteoporosis, Paget's disease, osteolytic tumors, Rheumatoid Arthritis, Psoriatic Arthritis, Ankylosing Spondylitis, Osteoarthritis, osteopenia, and hypercalcemia. Also described herein are the methods of making these compositions that prevent or treat conditions associated with bone loss and methods of preventing bone fractures.

    PEPTIDE ANTAGONISTS OF THE CALCITONIN CGRP FAMILY OF PEPTIDE HORMONES AND THEIR USE

    公开(公告)号:EP3272769A1

    公开(公告)日:2018-01-24

    申请号:EP17175988.9

    申请日:2013-01-25

    摘要: The embodiments provide a modified calcitonin gene-related peptide antagonist including an N-terminal fragment of modified calcitonin gene-related peptide or related protein family member where at least two residues of the N-terminal fragment are cysteine (Cys) and at least one amino acid comprises a non-threonine substitution of a threonine (Thr) residue; a central core where the central core comprises an α-helix; and a C-terminal fragment of modified calcitonin gene-related peptide or related protein family member comprising a C-terminal amide and where at least one amino acid of the C-terminal fragment is phenylalanine (Phe), proline (Pro), tyrosine (Tyr) or hydroxyproline (Hyp) or pharmaceutically acceptable salt thereof, as well as compositions, including pharmaceutical compositions, comprising a subject peptide. The embodiments further provide treatment methods, including methods of treating a migraine, the methods generally involving administering to an individual in need thereof an effective amount of a subject peptide or composition.

    CALCITONIN MIMETICS FOR TREATING DISEASES AND DISORDERS
    9.
    发明公开
    CALCITONIN MIMETICS FOR TREATING DISEASES AND DISORDERS 有权
    用于治疗疾病和病症的降钙素模拟物

    公开(公告)号:EP3095484A1

    公开(公告)日:2016-11-23

    申请号:EP16174260.6

    申请日:2012-11-02

    申请人: KeyBioscience AG

    IPC分类号: A61P3/04 A61K38/23 C07K5/00

    摘要: Use of a peptide having SEQ ID NO: 18 for the treatment of type I diabetes, Type II diabetes, metabolic syndrome, or obesity, or of apetite suppression, or for mitigating insulin resistance, or for reducing an undesirably high fasting serum glucose level, or for reducing an undesirably high peak serum glucose level, or for reducing an undesirably high peak serum insulin level, or for reducing an undesirably large response to a glucose tolerance test.

    摘要翻译: 使用具有SEQ ID NO:18的肽用于治疗I型糖尿病,II型糖尿病,代谢综合征或肥胖症或抑制性红斑狼疮,或用于缓解胰岛素抵抗或用于降低不希望的高空腹血清葡萄糖水平, 或用于降低不希望的高峰血清葡萄糖水平,或用于降低不希望的高峰血清胰岛素水平,或降低对葡萄糖耐量测试的不希望的大响应。

    CALCITONIN MIMETICS FOR TREATING DISEASES AND DISORDERS
    10.
    发明公开
    CALCITONIN MIMETICS FOR TREATING DISEASES AND DISORDERS 有权
    CALCITONIN-MIMETIKA ZUR BEHANDLUNG VON ERKRANKUNGEN UNDSTÖRUNGEN

    公开(公告)号:EP3068796A1

    公开(公告)日:2016-09-21

    申请号:EP14802345.0

    申请日:2014-11-10

    申请人: KeyBioscience AG

    IPC分类号: C07K14/585 A61K38/23

    摘要: Calcitonin mimetic peptides having an amino acid sequence in accordance with SEQ ID NO:8 or SEQ ID NO:53, each of which may be carboxylated at its N-terminal or otherwise modified to reduce the positive charge of the first amino acid and independently of that may be amidated at its C-terminal, and in each of which the 1 and 7 position cysteine residues may together be replaced by α-aminosuberic acid (Asu) are useful as medicaments for treating diabetes (Type I and/or Type II), excess bodyweight, excessive food consumption, metabolic syndrome, rheumatoid arthritis, non-alcoholic fatty liver disease, osteoporosis, or osteoarthritis, poorly regulated blood glucose levels, poorly regulated response to glucose tolerance tests, or poorly regulated of food intake.

    摘要翻译: 降钙素模拟肽具有根据SEQ ID NO:8或SEQ ID NO:53的氨基酸序列,其各自可以在其N-末端被羧化或以其它方式被修饰以减少第一氨基酸的正电荷并且独立于 其可以在其C-末端被酰胺化,并且其中每个中的1和7位半胱氨酸残基可以一起被α-氨基青霉酸(Asu)代替可用作治疗糖尿病的药物(I型和/或II型) ,过量的体重,食物过量消耗,代谢综合征,类风湿关节炎,非酒精性脂肪性肝病,骨质疏松症或骨关节炎,血糖水平调节不良,对葡萄糖耐量试验的调节反应不良或食物摄取调节不良。