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    • 6. 发明申请
    • TREATMENT OF PEDIATRIC GROWTH HORMONE DEFICIENCY WITH HUMAN GROWTH HORMONE ANALOGUES
    • 人类生长激素类似物治疗小儿生长激素缺乏症
    • WO2016109823A1
    • 2016-07-07
    • PCT/US2015068328
    • 2015-12-31
    • AMUNIX OPERATION INC
    • CLELAND JEFFREY L
    • A61K38/27A61K38/16C07K14/615
    • A61K38/27C07K14/61C07K2319/00
    • The present disclosure provides a pediatric growth hormone deficiency (PGHD) therapy for pediatric subjects. In some embodiments, the therapy comprises administering to the pediatric patient with PGHD a human growth hormone -XTEN (hGH-XTEN) fusion protein in therapeutically effective doses once a month, two-times a month, three-times a month, or four-times a month, wherein the treatment continues for at least about 3 months from first administration, and wherein the pediatric patient's height velocity does not decline during the treatment. In some embodiments, methods disclosed herein achieve results that are not statistically inferior compared to the height velocity achieved with daily injections of hGH alone over the same period.
    • 本公开提供用于儿科对象的小儿生长激素缺乏症(PGHD)疗法。 在一些实施方案中,治疗包括向患有PGHD的儿科患者以治疗有效剂量每月一次,一个月二次,一个月三次或四个月一次给予人生长激素-XTEN(hGH-XTEN)融合蛋白, 每月一次,其中治疗从首次施用开始持续至少约3个月,并且其中在治疗期间儿科患者的身高速度不下降。 在一些实施方案中,本文公开的方法获得的结果与在同一时期每日单独注射hGH获得的身高相比,统计学上并不差。
    • 8. 发明申请
    • HALOGENATED INSULIN ANALOGUES OF ENHANCED BIOLOGICAL POTENCY
    • 增强的生物学功能的分离胰岛素类似物
    • WO2016064606A1
    • 2016-04-28
    • PCT/US2015/055057
    • 2015-10-12
    • CASE WESTERN RESERVE UNIVERSITY
    • WEISS, Michael A.
    • A61K38/28A61K38/27
    • A61K33/30A61K38/00A61K38/27A61K38/28A61K2300/00C07K14/00C07K14/62
    • An insulin molecule comprises an Asp substitution at position B10, Glu at one or more of positions corresponding to A8, B28, and B29, and a halogenated phenylalanine at position B24. The analogue may optionally include (i) N-terminal deletion of one, two or three residues from the B chain, (ii) a mono-peptide or dipeptide C-terminal extension of the B-chain containing at least one acidic residue, and (iii) other modifications known in the art to enhance the stability of insulin. Formulations of the above analogues at successive strengths U-100 to U-1000 in soluble solutions at at least pH value in the range 7.0-8.0 in the absence or presence of zinc ions at a molar ratio of 0.00-0.10 zinc ions per insulin analogue monomer. A method of lowering the blood sugar level of a patient comprises administering a physiologically effective amount of the insulin to a patient.
    • 胰岛素分子包含位置B10处的Asp取代,对应于A8,B28和B29的一个或多个位置的Glu和位置B24的卤代苯丙氨酸。 类似物可以任选地包括(i)来自B链的一个,两个或三个残基的N-末端缺失,(ii)含有至少一个酸性残基的B链的单肽或二肽C-末端延伸,以及 (iii)本领域已知的其他修饰以增强胰岛素的稳定性。 在不存在或存在锌离子的情况下,在0.001-10锌离子/胰岛素类似物的摩尔比下,在连续的强度U-100至U-1000的溶液中至少在7.0-8.0的pH值范围内的上述类似物的制剂 单体。 降低患者血糖水平的方法包括向患者施用生理有效量的胰岛素。