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公开(公告)号：US20050014679A1
公开(公告)日：2005-01-20
申请号：US10496847
申请日：2002-12-12
申请人： John Beals , Michael DeFelippis , Richard DiMarchi , Wayne Kohn , Radmila Micanovic , Sharon Myers , Kingman Ng , Lianshan Zhang
发明人： John Beals , Michael DeFelippis , Richard DiMarchi , Wayne Kohn , Radmila Micanovic , Sharon Myers , Kingman Ng , Lianshan Zhang
CPC分类号： C07K14/62
摘要： The present invention provides an insulin molecule that provides a protracted, even basal duration of action. The insulin molecule comprises a modification at the N-terminus of the A-chain, optionally a modification at the N-terminus of the B-chain, a modification at a B-chain lysine, and optionally a modification at the C-terminus of the A-chain. The present invention also provides a method of treating diabetes mellitus comprising administering the insulin molecule.
摘要翻译： 本发明提供了提供持久的，甚至基础持续时间的胰岛素分子。 胰岛素分子包含在A链的N末端的修饰，任选地在B链的N末端的修饰，B链赖氨酸的修饰，以及任选地在C末端的修饰 A链。 本发明还提供一种治疗糖尿病的方法，包括给予胰岛素分子。
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公开(公告)号：US08183340B2
公开(公告)日：2012-05-22
申请号：US11913365
申请日：2006-05-11
申请人： Wolfgang Glaesner , John Philip Mayer , Rohn Lee Millican, Jr. , Andrew Mark Vick , Lianshan Zhang
发明人： Wolfgang Glaesner , John Philip Mayer , Rohn Lee Millican, Jr. , Andrew Mark Vick , Lianshan Zhang
IPC分类号： A61K38/26 , C07K14/605 , A61P3/10
CPC分类号： C07K14/605 , A61K47/60
摘要： The invention provides GLP-1 compounds coupled to two polyethylene glycol molecule or derivative thereof, resulting in a biologically active peptide with an extended half-life and a slower clearance when compared to that of unPEGylated peptide. These PEGylated GLP-1 compounds and compositions are useful in treating conditions or disorders benefited by lowering blood glucose, decreasing food intake, decreasing gastric or intestinal emptying, increasing beta (β) cell population, or decreasing gastric or intestinal motility.
摘要翻译： 本发明提供了与两个聚乙二醇分子或其衍生物偶联的GLP-1化合物，当与未PEG化肽相比时，产生具有延长的半衰期和较慢清除率的生物活性肽。 这些聚乙二醇化GLP-1化合物和组合物可用于治疗通过降低血糖，减少食物摄取，减少胃或肠排空，增加β（β）细胞群体或减少胃或肠运动而受益的病症或病症。
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公开(公告)号：US20060014241A1
公开(公告)日：2006-01-19
申请号：US10499111
申请日：2003-01-03
申请人： Wolfgang Glaesner , Wayne Kohn , Rohn Millican , Lianshan Zhang
发明人： Wolfgang Glaesner , Wayne Kohn , Rohn Millican , Lianshan Zhang
IPC分类号： A61K38/26 , C07H21/04 , C12P21/06 , C07K14/605
CPC分类号： C07K14/605 , A61K38/00 , C07K2319/00
摘要： The invention encompasses GLP-1 peptides with modifications at various positions coupled with an extended C-terminus that provides increased stability.
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公开(公告)号：US09090568B2
公开(公告)日：2015-07-28
申请号：US14004633
申请日：2012-03-12
申请人： Dong Liu , Minsheng Zhang , Kan He , Lianshan Zhang
发明人： Dong Liu , Minsheng Zhang , Kan He , Lianshan Zhang
IPC分类号： C07D239/96 , C07D239/80 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D405/12 , C07D413/12 , C07D471/04 , C07D487/04
CPC分类号： C07D239/96 , C07D239/80 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D405/12 , C07D413/12 , C07D471/04 , C07D487/04
摘要： The present invention discloses compounds of formula (I), or pharmaceutically acceptable salts or prodrugs thereof, which inhibit the poly(ADP-ribose) polymerases (PARP) and therefore are useful for treating diseases, disorders, and conditions related to PARP. The present invention also discloses pharmaceutical compositions comprising a compound of formula (I), and methods of using such compounds to inhibit PARP enzymes, and to treat diseases, disorders, and conditions related to PARP.
摘要翻译： 本发明公开了抑制聚（ADP-核糖）聚合酶（PARP）的式（I）化合物或其药学上可接受的盐或前药，因此可用于治疗与PARP相关的疾病，病症和病症。 本发明还公开了包含式（I）化合物的药物组合物，以及使用这些化合物抑制PARP酶以及治疗与PARP有关的疾病，病症和病症的方法。
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25.发明申请GLUCAGON SUPERFAMILY PEPTIDES EXHBITING G PROTEIN COUPLED RECEPTOR ACTIVITY 有权GLUCAGON超家族蛋白表达G蛋白偶联受体活性公开(公告)号：US20130116172A1
公开(公告)日：2013-05-09
申请号：US13697017
申请日：2011-05-10
IPC分类号： C07K14/605
CPC分类号： A61K47/48023 , A61K38/26 , A61K47/54 , A61K47/60 , A61K47/64 , C07K14/605
摘要： Provided herein are glucagon superfamily peptides conjugated with GPCR ligands that are capable of acting at a G protein-coupled receptor. Also provided herein are pharmaceutical compositions and kits of the conjugates of the invention. Further provided herein are methods of treating a disease, e.g., a metabolic disorder, such as diabetes and obesity, comprising administering the conjugates of the invention.
摘要翻译： 本文提供了与能够作用于G蛋白偶联受体的GPCR配体缀合的胰高血糖素超家族肽。 本文还提供了本发明的缀合物的药物组合物和试剂盒。 本文还提供了治疗疾病，例如代谢紊乱（例如糖尿病和肥胖症）的方法，其包括施用本发明的缀合物。
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公开(公告)号：US20090312236A1
公开(公告)日：2009-12-17
申请号：US12481111
申请日：2009-06-09
申请人： John Michael Beals , Gordon Butler Cutler, JR. , Brandon Doyle , Ryan John Hansen , Shun Li , Sean Shirani , Lianshan Zhang
发明人： John Michael Beals , Gordon Butler Cutler, JR. , Brandon Doyle , Ryan John Hansen , Shun Li , Sean Shirani , Lianshan Zhang
摘要： The present invention relates to the field of diabetes. More particularly, the invention relates to PEGylated insulin lispro compounds that are PEGylated with high molecular weight poly(ethylene glycol), are highly soluble at physiological pH, have an extended duration of action, and characterized by pharmacokinetic, pharmacodynamic, and/or activity peak-trough ratios of less than 2. The invention also relates to methods of providing such molecules, to pharmaceutical compositions containing them, and to their therapeutic uses.
摘要翻译： 本发明涉及糖尿病领域。 更具体地，本发明涉及用高分子量聚（乙二醇）聚乙二醇化的聚乙二醇化的赖脯胰岛素化合物，在生理pH下是高度可溶的，具有延长的作用持续时间，并且其特征在于药代动力学，药效学和/或活性峰 通过比例小于2.本发明还涉及提供此类分子的方法，含有它们的药物组合物及其治疗用途。
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公开(公告)号：US20090215981A1
公开(公告)日：2009-08-27
申请号：US11913365
申请日：2006-05-11
申请人： Wolfgang Glaesner , John Philip Mayer , Rohn Lee Millican, JR. , Andrew Mark Vick , Lianshan Zhang
发明人： Wolfgang Glaesner , John Philip Mayer , Rohn Lee Millican, JR. , Andrew Mark Vick , Lianshan Zhang
IPC分类号： C07K14/605 , A61K38/26 , A61P3/04 , A61P3/10
CPC分类号： C07K14/605 , A61K47/60
摘要： The invention provides GLP-1 compounds coupled to two polyethylene glycol molecule or derivative thereof, resulting in a biologically active peptide with an extended half-life and a slower clearance when compared to that of unPEGylated peptide. These PEGylated GLP-1 compounds and compositions are useful in treating conditions or disorders benefited by lowering blood glucose, decreasing food intake, decreasing gastric or intestinal emptying, increasing beta (β) cell population, or decreasing gastric or intestinal motility.
摘要翻译： 本发明提供了与两个聚乙二醇分子或其衍生物偶联的GLP-1化合物，当与未PEG化肽相比时，产生具有延长的半衰期和较慢清除率的生物活性肽。 这些聚乙二醇化GLP-1化合物和组合物可用于治疗通过降低血糖，减少食物摄入，减少胃或肠排空，增加β（β）细胞群体或减少胃或肠蠕动而受益的病症或障碍。
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公开(公告)号：US07557183B2
公开(公告)日：2009-07-07
申请号：US10548328
申请日：2004-03-19
申请人： Richard Dennis DiMarchi , Wolfgang Glaesner , Rohn Lee Millican, Jr. , Andrew Mark Vick , Lianshan Zhang
发明人： Richard Dennis DiMarchi , Wolfgang Glaesner , Rohn Lee Millican, Jr. , Andrew Mark Vick , Lianshan Zhang
CPC分类号： C07K14/605 , A61K47/60
摘要： The invention provides GLP-1 compounds coupled to at least one polyethylene glycol molecule or derivative thereof, resulting in a biologically active peptide with an extended half-life and a slower clearance when compared to that of unPEGylated peptide. These PEGylated GLP-1 compounds and compositions are useful in treating diabetes, obesity, irritable bowel syndrome and other conditions that would be benefited by lowering plasma glucose, inhibiting gastric and/or intestinal motility and inhibiting gastric and/or intestinal emptying, or inhibiting food intake.
摘要翻译： 本发明提供了与至少一种聚乙二醇分子或其衍生物偶联的GLP-1化合物，当与未PEG化肽相比时，产生具有延长的半衰期和较慢清除率的生物活性肽。 这些聚乙二醇化GLP-1化合物和组合物可用于治疗糖尿病，肥胖症，肠易激综合征和其它通过降低血浆葡萄糖，抑制胃和/或肠蠕动并抑制胃和/或肠排空或抑制食物而受益的条件 摄入量
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公开(公告)号：US07482321B2
公开(公告)日：2009-01-27
申请号：US10499111
申请日：2003-01-03
IPC分类号： A61K38/26 , C07K14/605
CPC分类号： C07K14/605 , A61K38/00 , C07K2319/00
摘要： The invention encompasses GLP-1 peptides with modifications at various positions coupled with an extended C-terminus that provides increased stability.
摘要翻译： 本发明包括具有增加的稳定性的扩展C-末端的各种位置的修饰的GLP-1肽。
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公开(公告)号：US20070105759A1
公开(公告)日：2007-05-10
申请号：US10556689
申请日：2004-06-17
申请人： David Flora , Mark Heiman , JeAnne Hertel , Hansen Hsiung , John Mayer , David Smiley , Liang Yan , Lianshan Zhang
发明人： David Flora , Mark Heiman , JeAnne Hertel , Hansen Hsiung , John Mayer , David Smiley , Liang Yan , Lianshan Zhang
摘要： The present invention relates to peptide agonists of the MC4 receptor, and as such are useful in the treatment of disorders responsive to the activation of this receptor, such as obesity, diabetes mellitus and male and/or female sexual dysfunction.
摘要翻译： 本发明涉及MC4受体的肽激动剂，因此可用于治疗对该受体的活化有响应的病症，例如肥胖症，糖尿病和男性和/或女性性功能障碍。
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