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    Therapeutic agents for reducing parathyroid hormone levels
    1.
    发明授权
    Therapeutic agents for reducing parathyroid hormone levels 有权
    降低甲状旁腺激素水平的治疗剂

    公开(公告)号：US08377880B2

    公开(公告)日：2013-02-19

    申请号：US13365213

    申请日：2012-02-02

    申请人： Felix Karim ,  Amos Baruch ,  Derek MacLean ,  Kanad Das ,  Qun Yin

    发明人： Felix Karim ,  Amos Baruch ,  Derek MacLean ,  Kanad Das ,  Qun Yin

    IPC分类号： A61K38/08 ,  A61P13/12 ,  A61P5/18 ,  C07K7/06

    CPC分类号： C07K7/06 ,  A61K9/0019 ,  A61K9/08 ,  A61K38/00 ,  A61K47/60 ,  C07K5/1013 ,  C07K7/08

    摘要： Compounds having activity for lowering parathyroid hormone levels are described. In one embodiment, the compounds are comprised of a contiguous sequence of subunits, X1—X2—X3—X4—X5—X6—X7, wherein the X1 subunit comprises a thiol-containing moiety and the distribution of charge on the X2—X7 subunits provides the desired activity. Methods of using the compounds for treating hyperparathyroidism, bone disease and/or hypercalcemic disorders are also described, and in particular, methods for lowering plasma PTH and serum calcium are provided. The compounds can be used to treat subjects having, for example: primary, secondary or tertiary hyperparathyroidism; hypercalcemia of malignancy; metastatic bone disease; or osteoporosis.

    摘要翻译： 描述了具有降低甲状旁腺激素水平的活性的化合物。 在一个实施方案中，化合物由亚单位X1-X2-X3-X4-X5-X6-X7的连续序列组成，其中X1亚基包含含巯基的部分，并且X2-X7亚基上的电荷分布 提供所需的活动。 还描述了使用该化合物治疗甲状旁腺功能亢进，骨疾病和/或高钙血症的方法，特别是提供降低血浆PTH和血清钙的方法。 这些化合物可用于治疗患有例如：原发性，继发性或甲状腺功能亢进的受试者; 恶性高钙血症; 转移性骨病; 或骨质疏松。

    Modifications of peptide compositions to increase stability and delivery efficiency
    6.
    发明授权
    Modifications of peptide compositions to increase stability and delivery efficiency 有权
    改进肽组合物以增加稳定性和递送效率

    公开(公告)号：US08067532B2

    公开(公告)日：2011-11-29

    申请号：US12017985

    申请日：2008-01-22

    申请人： Derek MacLean

    发明人： Derek MacLean

    IPC分类号： A61K38/16

    CPC分类号： C12N9/96 ,  A61K38/10 ,  A61K47/64 ,  A61K47/645 ,  C07K7/00 ,  C12N9/12 ,  C12Y207/11013

    摘要： The disclosed invention relates to methods of modifying peptide compositions to increase stability and delivery efficiency. Specifically, the disclosed invention relates to methods to increase the stability and delivery efficiency of protein kinase C (PKC) modulatory peptide compositions. A “therapeutic peptide composition” comprises a “carrier peptide” and a “cargo peptide.” A “carrier peptide” is a peptide or amino acid sequence within a peptide that facilitates the cellular uptake of the therapeutic peptide composition. The “cargo peptide” is a PKC modulatory peptide. Peptide modifications to either the carrier peptide, the cargo peptide, or both, which are described herein increase the stability and delivery efficiency of therapeutic peptide compositions by reducing disulfide bond exchange, physical stability, reducing proteolytic degradation, and increasing efficiency of cellular uptake.

    摘要翻译： 所公开的发明涉及修饰肽组合物以提高稳定性和递送效率的方法。 具体地，所公开的发明涉及增加蛋白激酶C（PKC）调节肽组合物的稳定性和递送效率的方法。 “治疗性肽组合物”包含“载体肽”和“货物肽”。“载体肽”是促进细胞摄取治疗性肽组合物的肽内的肽或氨基酸序列。 “货物肽”是PKC调节肽。 通过减少二硫键交换，物理稳定性，减少蛋白水解降解和增加细胞摄取的效率，本文所述的载体肽，载体肽或两者的肽修饰增加了治疗性肽组合物的稳定性和递送效率。

    Protein kinase C peptide modulators of angiogenesis
    7.
    发明申请
    Protein kinase C peptide modulators of angiogenesis 审中-公开
    蛋白激酶C肽调节剂的血管发生

    公开(公告)号：US20070141040A1

    公开(公告)日：2007-06-21

    申请号：US11524350

    申请日：2006-09-19

    申请人： Leon Chen ,  Derek MacLean ,  Sarah Walter

    发明人： Leon Chen ,  Derek MacLean ,  Sarah Walter

    IPC分类号： A61K38/54 ,  C07H21/04 ,  C12P21/06 ,  C12N9/12

    CPC分类号： C12Y207/11013 ,  A61K9/0048 ,  A61K9/08 ,  A61K38/00 ,  A61K47/645 ,  C12N9/1205

    摘要： The present invention provides peptides for inhibiting various protein kinase C isozymes. The peptide can be directed to any region of the protein kinase C isozyme, and in one embodiment, is directed to the V5 domain. The peptide can be conjugated to a carrier, in a releasable or non-releasable manner. The peptides can be used to inhibit angiogenesis and/or vascular permeability. The peptides can be used to treat subjects having, for example, cancer, diabetic blindness, macular degeneration, rheumatoid arthritis, or psoriasis.

    摘要翻译： 本发明提供用于抑制各种蛋白激酶C同功酶的肽。 肽可以被引导到蛋白激酶C同功酶的任何区域，并且在一个实施方案中，涉及V 5结构域。 肽可以以可释放或不可释放的方式与载体缀合。 肽可以用于抑制血管发生和/或血管通透性。 肽可用于治疗患有例如癌症，糖尿病性失明，黄斑变性，类风湿性关节炎或牛皮癣的受试者。