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1. 发明授权

US07939496B2 Modified human growth horomone polypeptides and their uses 有权
标题翻译：改良人类生长horomone多肽及其用途
公开(公告)号：US07939496B2
公开(公告)日：2011-05-10
申请号：US11316534
申请日：2005-12-21
申请人： Ho Sung Cho , Thomas O. Daniel , Richard D. DiMarchi , Anna-Maria Hays , Troy E. Wilson , Bee-Cheng Sim , David C. Litzinger
发明人： Ho Sung Cho , Thomas O. Daniel , Richard D. DiMarchi , Anna-Maria Hays , Troy E. Wilson , Bee-Cheng Sim , David C. Litzinger
IPC分类号： A61K38/27 , C07K14/61
CPC分类号： A61K38/27 , A61K9/0019 , A61K9/19 , A61K47/02 , A61K47/183 , A61K47/26 , C07K14/61 , C08G65/33396
摘要： Modified growth hormone polypeptide and uses thereof are provided.
摘要翻译：提供了改良的生长激素多肽及其用途。

2. 发明授权

US08907064B2 Modified human four helical bundle polypeptides and their uses 有权
标题翻译：改良人类四螺旋束多肽及其用途
公开(公告)号：US08907064B2
公开(公告)日：2014-12-09
申请号：US11874713
申请日：2007-10-18
申请人： Ho Sung Cho , Thomas O. Daniel , Richard D. DiMarchi , Anna-Maria Hays , Troy E. Wilson , Bee-Cheng Sim , David C. Litzinger
发明人： Ho Sung Cho , Thomas O. Daniel , Richard D. DiMarchi , Anna-Maria Hays , Troy E. Wilson , Bee-Cheng Sim , David C. Litzinger
IPC分类号： C07K1/00 , A61K38/24 , C07K14/00 , C07H21/04 , A61K38/21 , C07K14/61 , C07K14/575 , G01N33/68 , C08G65/333 , A61K38/27 , A61K47/48 , C07K14/52
CPC分类号： C07H21/04 , A61K38/21 , A61K38/27 , A61K47/60 , C07K14/475 , C07K14/52 , C07K14/575 , C07K14/61 , C08G65/33396 , G01N33/6875 , G01N2500/00
摘要： Modified human four helical bundle (4HB) polypeptides and uses thereof are provided.
摘要翻译：提供了修饰的人类四螺旋束（4HB）多肽及其用途。

3. 发明授权

US08906676B2 Modified human four helical bundle polypeptides and their uses 有权
公开(公告)号：US08906676B2
公开(公告)日：2014-12-09
申请号：US10587371
申请日：2005-01-28
申请人： Ho Sung Cho , Thomas O. Daniel , Richard D. DiMarchi , Anna-Maria Hays , Troy E. Wilson , Bee-Cheng Sim , David C. Litzinger
发明人： Ho Sung Cho , Thomas O. Daniel , Richard D. DiMarchi , Anna-Maria Hays , Troy E. Wilson , Bee-Cheng Sim , David C. Litzinger
IPC分类号： C12N5/00 , C07H21/04 , C07K14/61 , A61K38/27 , C08G65/333 , A61K38/21 , C07K14/475 , G01N33/68 , A61K47/48 , C07K14/52
CPC分类号： C07H21/04 , A61K38/21 , A61K38/27 , A61K47/60 , C07K14/475 , C07K14/52 , C07K14/575 , C07K14/61 , C08G65/33396 , G01N33/6875 , G01N2500/00
摘要： Modified human four helical bundle (4HB) polypeptides and uses thereof are provided.

4. 发明申请

US20080300163A1 Modified Human Four Helical Bundle Polypeptides And Their Uses 有权
标题翻译：改良人类四螺旋束多肽及其用途
公开(公告)号：US20080300163A1
公开(公告)日：2008-12-04
申请号：US10587371
申请日：2005-01-28
申请人： Ho Sung Cho , Thomas O. Daniel , Richard D. DiMarchi , Anna-Maria Hays , Troy E. Wilson , Bee-Cheng Sim , David C. Litzinger
发明人： Ho Sung Cho , Thomas O. Daniel , Richard D. DiMarchi , Anna-Maria Hays , Troy E. Wilson , Bee-Cheng Sim , David C. Litzinger
IPC分类号： A61K38/02 , C07K2/00 , C07K14/535 , C07K14/555 , C12N9/00 , C12P21/00 , C12N1/19 , C07K14/505 , C07H21/04
CPC分类号： C07H21/04 , A61K38/21 , A61K38/27 , A61K47/60 , C07K14/475 , C07K14/52 , C07K14/575 , C07K14/61 , C08G65/33396 , G01N33/6875 , G01N2500/00
摘要： Modified human four helical bundle (4HB) polypeptides and uses thereof are provided.
摘要翻译：提供了修饰的人类四螺旋束（4HB）多肽及其用途。

5. 发明授权

US08778880B2 Human growth hormone modified at position 35 有权
标题翻译：在35位修饰的人生长激素
公开(公告)号：US08778880B2
公开(公告)日：2014-07-15
申请号：US11046432
申请日：2005-01-28
申请人： Ho Sung Cho , Thomas O. Daniel , Richard D. DiMarchi , Anna-Maria Hays , Troy E. Wilson , Bee-Cheng Sim , David C. Litzinger
发明人： Ho Sung Cho , Thomas O. Daniel , Richard D. DiMarchi , Anna-Maria Hays , Troy E. Wilson , Bee-Cheng Sim , David C. Litzinger
IPC分类号： A61K38/27 , C07K14/61
CPC分类号： C07H21/04 , A61K38/21 , A61K38/27 , A61K47/60 , C07K14/475 , C07K14/52 , C07K14/575 , C07K14/61 , C08G65/33396 , G01N33/6875 , G01N2500/00
摘要： Modified human growth hormone polypeptides and uses thereof are provided.
摘要翻译：提供了修饰的人生长激素多肽及其用途。

6. 发明授权

US08143216B2 Modified human growth hormone 有权
标题翻译：改良人生长激素
公开(公告)号：US08143216B2
公开(公告)日：2012-03-27
申请号：US11924101
申请日：2007-10-25
申请人： Ho Sung Cho , Thomas O. Daniel , Richard D. DiMarchi , Anna-Maria A. Hays , Troy E. Wilson , Bee-Cheng Sim , David C. Litzinger
发明人： Ho Sung Cho , Thomas O. Daniel , Richard D. DiMarchi , Anna-Maria A. Hays , Troy E. Wilson , Bee-Cheng Sim , David C. Litzinger
IPC分类号： A61K38/27 , A61P5/06
CPC分类号： A61K38/27 , A61K9/0019 , A61K9/19 , A61K47/02 , A61K47/183 , A61K47/26 , C07K14/61 , C08G65/33396
摘要： Modified growth hormone polypeptide and uses thereof are provided.
摘要翻译：提供了改良的生长激素多肽及其用途。

7. 发明授权

US08975223B2 Methods for treating metabolic disorders and obesity with a peptide comprising the amino acid sequence of SEQ ID No. 146 有权
标题翻译：用包含SEQ ID No.146的氨基酸序列的肽治疗代谢紊乱和肥胖症的方法
公开(公告)号：US08975223B2
公开(公告)日：2015-03-10
申请号：US13996937
申请日：2011-12-22
申请人： Louis Vignati , Richard D. DiMarchi
发明人： Louis Vignati , Richard D. DiMarchi
IPC分类号： A61K38/26 , A61P3/10 , A61K31/195 , A61K31/198 , A61K45/06
CPC分类号： A61K38/26 , A61K9/0019 , A61K31/195 , A61K31/198 , A61K38/17 , A61K45/06 , A61K47/60 , A61K2300/00
摘要： Methods are provided for administering an extended half-life GLP-1/GIP coagonist peptide to a patient in need thereof for reducing weight gain, inducing weight loss, treating hyperglycemia, reducing blood glucose levels, or normalizing blood glucose levels in said patient.
摘要翻译：提供了向有需要的患者施用延长的半衰期GLP-1 / GIP拮抗肽的方法，用于减轻体重增加，引起体重减轻，治疗高血糖，降低血糖水平或使所述患者的血糖水平正常化。

8. 发明授权

US08703701B2 Glucagon/GLP-1 receptor co-agonists 有权
标题翻译：胰高血糖素/ GLP-1受体共激动剂
公开(公告)号：US08703701B2
公开(公告)日：2014-04-22
申请号：US13515977
申请日：2010-12-09
申请人： Richard D. DiMarchi
发明人： Richard D. DiMarchi
IPC分类号： A61K38/26 , A61P3/10
CPC分类号： C07K14/605 , A61K38/00
摘要： Provided herein are glucagon analogs comprising a modified amino acid sequence of native human glucagon (SEQ ID NO: 2) that exhibit activity at the glucagon receptor, activity at the GLP-1 receptor, or activity at each of the glucagon receptor and the GLP-1 receptor. In some embodiments, the glucagon analog exhibits at least 100% or more of the activity of native glucagon at the glucagon receptor and/or at least 100% or more of the activity of native GLP-1 at the GLP-1 receptor. In some embodiments, the glucagon analog has an EC50 at the GLP-1 receptor which is within 50-fold or less than the EC50 at the glucagon receptor. In some embodiments, the glucagon analog has an EC50 at the GLP-1 receptor which is two- to ten-fold greater than the EC50 at the glucagon receptor. Related conjugates, dimers and multimers, and pharmaceutical compositions, and uses thereof, are further provided.
摘要翻译：本文提供的是包含显示胰高血糖素受体活性，GLP-1受体活性或每种胰高血糖素受体和GLP-1受体活性的天然人胰高血糖素（SEQ ID NO：2）的修饰氨基酸序列的胰高血糖素类似物， 1受体。在一些实施方案中，胰高血糖素类似物在胰高血糖素受体上表现出至少100％或更多的天然胰高血糖素的活性和/或天然GLP-1在GLP-1受体的至少100％或更多的活性。在一些实施方案中，胰高血糖素类似物在GLP-1受体处具有在胰高血糖素受体的50倍或更小的EC 50内的EC 50。在一些实施方案中，胰高血糖素类似物具有GLP-1受体的EC 50，其比胰高血糖素受体的EC50大2至10倍。还提供了相关的缀合物，二聚体和多聚体，以及药物组合物及其用途。

9. 发明申请

US20110245164A1 YL-BASED INSULIN-LIKE GROWTH FACTORS EXHIBITING HIGH ACTIVITY AT THE INSULIN RECEPTOR 审中-公开
标题翻译：基于YL的胰岛素样生长因子在胰岛素受体中展示高活性
公开(公告)号：US20110245164A1
公开(公告)日：2011-10-06
申请号：US13130960
申请日：2009-12-18
申请人： Richard D. DiMarchi , Shujiang Cheng , Binbin Kou , Jie Han
发明人： Richard D. DiMarchi , Shujiang Cheng , Binbin Kou , Jie Han
IPC分类号： A61K38/28 , C07K14/62 , A61K38/30 , A61P3/10 , C07K14/65
CPC分类号： C07K14/65 , A61K38/00
摘要： Insulin-like growth factor analogs are disclosed wherein substitution of the IGF native amino acids, at positions corresponding to positions B16 and B17 of native insulin, with tyrosine and leucine, respectively, increases potency of the resulting analog at the insulin receptor by tenfold. Also disclosed are prodrug and depot formulations of the IGF analogs, wherein the IGF analog has been modified by the linkage of a dipeptide to the analog through an amide bond linkage. The prodrug and depot formulations disclosed herein have extended half lives of at least 2 hours, 10 hours, and more typically greater than 2 are converted to the active form at physiological conditions through a non-enzymatic reaction driven by chemical instability.
摘要翻译：公开了胰岛素样生长因子类似物，其中分别用酪氨酸和亮氨酸取代天然胰岛素的位置B16和B17处的IGF天然氨基酸将胰岛素受体上得到的类似物的效力增加十倍。还公开了IGF类似物的前药和贮库制剂，其中IGF类似物已经通过二肽与类似物通过酰胺键连接而被修饰。本文公开的前药和贮库制剂具有至少2小时，10小时，更典型地大于2的半衰期在生理条件下通过由化学不稳定性驱动的非酶反应而转化为活性形式。

10. 发明申请

US20110190200A1 GLUCAGON ANALOGS EXHIBITING ENHANCED SOLUBILITY AND STABILITY IN PHYSIOLOGICAL pH BUFFERS 有权
标题翻译： GLUCAGON ANALOGS展示增强的生理pH缓冲液中的溶解性和稳定性
公开(公告)号：US20110190200A1
公开(公告)日：2011-08-04
申请号：US12999284
申请日：2009-06-16
申请人： Richard D. DiMarchi , David L. Smiley , Maria Dimarchi , Joseph Chabenne , Jonathan Day
发明人： Richard D. DiMarchi , David L. Smiley , Maria Dimarchi , Joseph Chabenne , Jonathan Day
IPC分类号： A61K38/26 , C07K14/605 , A61P3/08
CPC分类号： C07K14/605 , A61K38/00
摘要： Modified glucagon peptides are disclosed having improved solubility and/or half-life while retaining glucagon agonist activity. The glycogen peptides have been modified by substitution of native amino acids with, and/or addition of, charged amino acids to the carboxy terminus of the peptide. The modified glucagon agonists can be further modified by pegylation, or the addition of a carboxy terminal peptide selected from the group consisting of SEQ ID NO: 20, SEQ ID NO: 21, SEQ ID NO: 23, or both to further enhance the solubility of the glucagon agonist analogs.
摘要翻译：公开了具有改善的溶解度和/或半衰期同时保留胰高血糖素激动剂活性的改良的胰高血糖素肽。糖原肽已经通过用带氨基酸的氨基酸取代天然氨基酸和/或添加到肽的羧基末端而被修饰。修饰的胰高血糖素激动剂可以通过聚乙二醇化，或加入选自SEQ ID NO：20，SEQ ID NO：21，SEQ ID NO：23或两者的羧基末端肽进一步修饰，以进一步增强溶解度的胰高血糖素激动剂类似物。

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