Superpotent calcitonin analogs having greatly increased hypocalcemic action in vivo
    1.
    发明授权
    Superpotent calcitonin analogs having greatly increased hypocalcemic action in vivo 失效
    超强降钙素类似物在体内大大增加了低钙血症作用

    公开(公告)号:US06265534B1

    公开(公告)日:2001-07-24

    申请号:US09137389

    申请日:1998-08-20

    IPC分类号: A61K3823

    CPC分类号: C07K14/585 A61K38/00

    摘要: Superpotent calcitonin analogs have greatly increased hypocalcemic action in vivo. These calcitonins and calcitonin derivatives are employed for the therapy of, for example, osteoporosis, Paget's disease or hypercalcemia. The calcitonins and calcitonin derivatives are distinguished by a bridging of the amino acids present in the positions 17 and 21. By means of suitable choice of the amino acids present in these positions an 18-membered or 19-membered ring is produced. This ring leads to an increased conformational stability and to an increased activity of the modified calcitonin. A particularly suitable hCt (human calcitonin analog) is a cyclo17,21-[Asp17, Orn21]-hCt having a 19-membered ring structure between the lactam-bridged Asp17 and Orn21.

    摘要翻译: 超强降钙素类似物在体内大大增加了低钙血症的作用。 这些降钙素和降钙素衍生物用于治疗例如骨质疏松症,佩吉特氏病或高钙血症。 降钙素和降钙素衍生物的区别在于存在于位置17和21中的氨基酸的桥接。通过适当选择存在于这些位置的氨基酸,产生18元或19元环。 该环导致增加的构象稳定性和增加的降钙素的活性。 特别合适的hCt(人降钙素类似物)是在内酰胺桥连的Asp17和Orn21之间具有19-元环结构的环17,21- [Asp17,Orn21] -hCt。

    Superpotent calcitonin analogs having greatly increased hypocalcemic action in vivo
    2.
    发明授权
    Superpotent calcitonin analogs having greatly increased hypocalcemic action in vivo 失效
    超强降钙素类似物在体内大大增加了低钙血症作用

    公开(公告)号:US06617423B1

    公开(公告)日:2003-09-09

    申请号:US09742798

    申请日:2000-12-20

    IPC分类号: A61K3823

    CPC分类号: C07K14/585 A61K38/00

    摘要: Calcitonins and calcitonin derivatives such as are employed for therapy for, for example, osteoporosis. Paget's disease or hypercalcemia. The calcitonins and calcitonin derivatives are distinguished by a bridging of the amino acids present in the positions 17 and 21. In this case, by means of a suitable choice of the amino acids present in these positions an 18- or 19-membered ring is produced. This ring leads to an increased conformational stability and to an increased activity of the modified calcitonin. A particularly suitable hCt (human Ct) analog is the cyclo17,21-[Asp17, Orn21]-hCt according to the invention having a 19-membered ring structure between the lactam-bridged Asp17 and Orn21.

    摘要翻译: 降钙素和降钙素衍生物例如用于治疗例如骨质疏松症。 佩吉特氏病或高钙血症。 降钙素和降钙素衍生物的区别在于存在于位置17和21中的氨基酸的桥接。在这种情况下,通过适当选择存在于这些位置的氨基酸,产生18-或19-元环 。 该环导致增加的构象稳定性和增加的降钙素的活性。 特别合适的hCt(人Ct)类似物是根据本发明的在内酰胺桥连的Asp17和Orn21之间具有19-元环结构的环17,21- [Asp17,Orn21] -hCt。

    Screening method for candidate drugs
    3.
    发明授权
    Screening method for candidate drugs 有权
    候选药物的筛选方法

    公开(公告)号:US07303885B1

    公开(公告)日:2007-12-04

    申请号:US10148496

    申请日:2000-11-02

    IPC分类号: C07K1/22 G01N33/566 G01N33/68

    摘要: The present invention relates to methods for screening molecules and methods to detect protein-protein interactions and means used therein. More specifically, the present invention relates to methods for screening candidate drugs for treating or detecting MIF (macrophage migration inhibitor factor) related diseases. In certain aspects, the present invention involves detecting MIF/Jab1 (c-Jun activation domain binding protein) interactions as a basis for modulating cellular regulatory pathways and for identifying candidate drugs for MIF-related diseases. The invention also provides methods for the identification of molecules which dissociate or prevent interaction or binding between MIF and Jab1.

    摘要翻译: 本发明涉及用于筛选分子的方法和检测蛋白质 - 蛋白质相互作用的方法及其中使用的方法。 更具体地,本发明涉及用于筛选用于治疗或检测MIF(巨噬细胞迁移抑制因子)相关疾病的候选药物的方法。 在某些方面,本发明涉及检测MIF / Jab1(c-Jun活化结构域结合蛋白)相互作用作为调节细胞调节途径和鉴定用于MIF相关疾病的候选药物的基础。 本发明还提供用于鉴定分解或防止MIF和Jab1之间的相互作用或结合的分子的方法。

    Peptides used as agonists and/or inhibitors of amyloid formation and cytotoxicity and also for use in alzheimer's disease, in type II diabetes mellitus and in spongiform encephalophathies
    4.
    发明授权
    Peptides used as agonists and/or inhibitors of amyloid formation and cytotoxicity and also for use in alzheimer's disease, in type II diabetes mellitus and in spongiform encephalophathies 失效
    用作激动剂和/或淀粉样蛋白形成和细胞毒性抑制剂以及用于阿尔茨海默氏病,II型糖尿病和海绵状脑病的肽

    公开(公告)号:US06359112B2

    公开(公告)日:2002-03-19

    申请号:US09097194

    申请日:1998-06-12

    IPC分类号: C07K412

    摘要: Certain peptide molecules can be used as the basic structures (template molecules) for inhibiting and analysing amyloid formation and cytotoxicity in amyloid illnesses. These peptides have an effect on the molecules which are responsible for the amyloid illnesses (for their part amyloid-forming peptides and proteins). The peptides are thus either inhibitors themselves or agonists of amyloid formation and cytotoxicity or can serve as a template for identifying and producing further inhibitors and agonists and can be used as molecular tools during analysis. The peptide molecules have generally 3-15 amino acids, and preferably a maximum of 10 amino acids, and at least an active peptide sequence GA, preferably GAI, and even more preferably one selected from the group consisting of GAIL, SEQ ID NO: 1; FGAIL, SEQ ID NO: 2; NFGAIL, SEQ ID NO: 3; NNFGAIL, SEQ ID NO: 4; SNNFGAIL, SEQ ID NO: 5; NFGAILSS, SEQ ID NO: 6; SNNFGAILSS, SEQ NO: 7; or the group consisting of GAII, SEQ ID NO: 8; KGAII, SEQ ID NO: 9; NKGAII, SEQ ID NO: 10; SNKGAII, SEQ ID NO: 11; GSNKGAII, SEQ ID NO: 12; NKGAIIGL, SEQ ID NO: 13; GSNKGAIIGL, SEQ ID NO: 14; or the group consisting of GAVV, SEQ ID NO: 15; AGAVV, SEQ ID NO: 16; VAAGAVV, SEQ ID NO: 17; HVAAGAVV, SEQ ID NO: 18; AAGAVVGG, SEQ ID NO: 19; HVAAGAVVGG, SEQ ID NO: 20; AAGAVV, SEQ ID NO: 21. The peptide sequence generally has at least one hydrogen molecule, and preferably every second hydrogen molecule, of an amide bond replaced by a methyl group.

    摘要翻译: 某些肽分子可用作抑制和分析淀粉样蛋白疾病中淀粉样蛋白形成和细胞毒性的基本结构(模板分子)。 这些肽对负责淀粉样蛋白病(对于其部分淀粉样蛋白形成肽和蛋白质)的分子具有影响。 因此,肽是抑制剂本身或淀粉样蛋白形成和细胞毒性的激动剂,或者可以用作鉴定和产生其它抑制剂和激动剂的模板,并且可以在分析过程中用作分子工具。 肽分子通常具有3-15个氨基酸,优选最多10个氨基酸,和至少一个活性肽序列GA,优选GAI,甚至更优选选自GAIL,SEQ ID NO:1 ; FGAIL,SEQ ID NO:2; NFGAIL,SEQ ID NO:3; NNFGAIL,SEQ ID NO:4; SNNFGAIL,SEQ ID NO:5; NFGAILSS,SEQ ID NO:6; SNNFGAILSS,SEQ NO:7; 或由GAII,SEQ ID NO:8组成的组; KGAII,SEQ ID NO:9; NKGAII,SEQ ID NO:10; SNKGAII,SEQ ID NO:11; GSNKGAII,SEQ ID NO:12; NKGAIIGL,SEQ ID NO:13; GSNKGAIIGL,SEQ ID NO:14; 或由GAVV,SEQ ID NO:15组成的组; AGAVV,SEQ ID NO:16; VAAGAVV,SEQ ID NO:17; HVAAGAVV,SEQ ID NO:18; AAGAVVGG,SEQ ID NO:19; HVAAGAVVGG,SEQ ID NO:20; AAGAVV,SEQ ID NO:21.肽序列通常具有由甲基取代的酰胺键至少一个氢分子,优选每第二个氢分子。

    Anti-MIF antibodies
    5.
    再颁专利
    Anti-MIF antibodies 失效
    抗MIF抗体

    公开(公告)号:USRE43497E1

    公开(公告)日:2012-06-26

    申请号:US12234407

    申请日:2000-11-02

    IPC分类号: C07K16/00

    摘要: The present invention relates to methods for screening molecules and methods to detect protein-protein interactions and means used therein. More specifically, the present invention relates to methods for screening candidate drugs for treating or detecting MIF (macrophage migration inhibitor factor) related diseases. In certain aspects, the present invention involves detecting MIF/Jab1 (c-Jun activation domain binding protein) interactions as a basis for modulating cellular regulatory pathways and for identifying candidate drugs for MIF-related diseases. The invention also provides methods for the identification of molecules which dissociate or prevent interaction or binding between MIF and Jab1.

    摘要翻译: 本发明涉及用于筛选分子的方法和检测蛋白质 - 蛋白质相互作用的方法及其中使用的方法。 更具体地,本发明涉及用于筛选用于治疗或检测MIF(巨噬细胞迁移抑制因子)相关疾病的候选药物的方法。 在某些方面,本发明涉及检测MIF / Jab1(c-Jun活化结构域结合蛋白)相互作用作为调节细胞调节途径和鉴定用于MIF相关疾病的候选药物的基础。 本发明还提供用于鉴定分解或防止MIF和Jab1之间的相互作用或结合的分子的方法。