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1. 发明授权

US09062124B2 GIP-based mixed agonists for treatment of metabolic disorders and obesity 有权
标题翻译：用于治疗代谢紊乱和肥胖的基于GIP的混合激动剂
公开(公告)号：US09062124B2
公开(公告)日：2015-06-23
申请号：US12999285
申请日：2009-06-16
申请人： Richard D. Dimarchi , Tao Ma
发明人： Richard D. Dimarchi , Tao Ma
IPC分类号： A61K38/26 , C07K14/605
CPC分类号： C07K14/605 , A61K38/00 , A61K38/26 , A61K47/60
摘要： Glucagon peptides that exhibit GIP agonist activity in addition to glucagon and/or GLP-I activity are provided. Pharmaceutical compositions comprising such glucagon peptides and therapeutic methods of using such peptides are also provided.
摘要翻译：提供了除胰高血糖素和/或GLP-1活性外还显示GIP激动剂活性的胰高血糖素肽。还提供了包含这种胰高血糖素肽的药物组合物和使用这些肽的治疗方法。

2. 发明申请

US20120322725A1 GLUCAGON ANTAGONIST-GIP AGONIST CONJUGATES AND COMPOSITIONS FOR THE TREATMENT OF METABOLIC DISORDERS AND OBESITY 有权
标题翻译： GLUCAGON ANTAGONIST-GIP激动剂联合用药和组合物治疗代谢障碍和肥胖
公开(公告)号：US20120322725A1
公开(公告)日：2012-12-20
申请号：US13575363
申请日：2011-01-26
申请人： Richard D. Dimarchi , Tao Ma
发明人： Richard D. Dimarchi , Tao Ma
IPC分类号： A61K38/00 , A61P3/10 , C07K14/00 , A61P3/04
CPC分类号： C07K14/605 , A61K38/26 , A61K2300/00
摘要： Provided herein are peptide combinations comprising a GIP agonist peptide and a glucagon antagonist peptide. In some embodiments, the peptide combination is provided as a composition, e.g., a pharmaceutical composition, while in other embodiments, the peptide combination is provided as a kit. In yet other embodiments, the peptide combination is provided as a conjugate, e.g., a fusion peptide, a heterodimer. In specific aspects, the GIP agonist peptide is an analog of native human glucagon. In specific aspects, the glucagon antagonist peptide is an analog of native human glucagon. In some embodiments, the GIP agonist peptide is covalently attached to the glucagon antagonist peptide via a linker. Methods of treating a disease, e.g., a metabolic disorder, such as diabetes and obesity, comprising administering the peptide compositions described herein are further provided.
摘要翻译：本文提供了包含GIP激动剂肽和胰高血糖素拮抗肽的肽组合。在一些实施方案中，肽组合作为组合物例如药物组合物提供，而在其它实施方案中，肽组合作为试剂盒提供。在其它实施方案中，肽组合作为缀合物提供，例如融合肽，异二聚体。在具体方面，GIP激动剂肽是天然人胰高血糖素的类似物。在具体方面，胰高血糖素拮抗剂肽是天然人胰高血糖素的类似物。在一些实施方案中，GIP激动剂肽通过接头共价连接到胰高血糖素拮抗剂肽。进一步提供治疗疾病例如代谢紊乱（例如糖尿病和肥胖症）的方法，其包括施用本文所述的肽组合物。

3. 发明授权

US08551946B2 Glucagon antagonist-GIP agonist conjugates and compositions for the treatment of metabolic disorders and obesity 有权
标题翻译：胰岛素拮抗剂-GIP激动剂缀合物和用于治疗代谢紊乱和肥胖症的组合物
公开(公告)号：US08551946B2
公开(公告)日：2013-10-08
申请号：US13575363
申请日：2011-01-26
申请人： Richard D. Dimarchi , Tao Ma
发明人： Richard D. Dimarchi , Tao Ma
IPC分类号： A61K38/26 , A61K38/00 , A61K38/16
CPC分类号： C07K14/605 , A61K38/26 , A61K2300/00
摘要： Provided herein are peptide combinations comprising a GIP agonist peptide and a glucagon antagonist peptide. In some embodiments, the peptide combination is provided as a composition, e.g., a pharmaceutical composition, while in other embodiments, the peptide combination is provided as a kit. In yet other embodiments, the peptide combination is provided as a conjugate, e.g., a fusion peptide, a heterodimer. In specific aspects, the GIP agonist peptide is an analog of native human glucagon. In specific aspects, the glucagon antagonist peptide is an analog of native human glucagon. In some embodiments, the GIP agonist peptide is covalently attached to the glucagon antagonist peptide via a linker. Methods of treating a disease, e.g., a metabolic disorder, such as diabetes and obesity, comprising administering the peptide compositions described herein are further provided.
摘要翻译：本文提供了包含GIP激动剂肽和胰高血糖素拮抗肽的肽组合。在一些实施方案中，肽组合作为组合物例如药物组合物提供，而在其它实施方案中，肽组合作为试剂盒提供。在其它实施方案中，肽组合作为缀合物提供，例如融合肽，异二聚体。在具体方面，GIP激动剂肽是天然人胰高血糖素的类似物。在具体方面，胰高血糖素拮抗剂肽是天然人胰高血糖素的类似物。在一些实施方案中，GIP激动剂肽通过接头共价连接到胰高血糖素拮抗剂肽。进一步提供治疗疾病例如代谢紊乱（例如糖尿病和肥胖症）的方法，包括施用本文所述的肽组合物。

4. 发明授权

US09150632B2 GIP receptor-active glucagon compounds 有权
标题翻译： GIP受体活性胰高血糖素化合物
公开(公告)号：US09150632B2
公开(公告)日：2015-10-06
申请号：US13378001
申请日：2010-06-16
申请人： Richard D. Dimarchi , Tao Ma
发明人： Richard D. Dimarchi , Tao Ma
IPC分类号： C07K14/605 , A61K38/26 , A61P3/04 , A61P3/10 , A61K38/00
CPC分类号： C07K14/605 , A61K38/00 , A61K38/26
摘要： Glucagon peptides with increased GIP activity are provided, optionally with GLP-I and/or glucagon activity. In some embodiments, C-terminally extended glucagon peptides comprising an amino acid sequence substantially similar to native glucagon are provided herein.
摘要翻译：提供具有增加的GIP活性的胰高血糖素肽，任选地具有GLP-1和/或胰高血糖素活性。在一些实施方案中，本文提供了包含与天然胰高血糖素基本相似的氨基酸序列的C末端扩增的胰高血糖素肽。

5. 发明申请

US20120172295A1 GIP RECEPTOR-ACTIVE GLUCAGON COMPOUNDS 有权
标题翻译： GIP受体活性GLUCAGON化合物
公开(公告)号：US20120172295A1
公开(公告)日：2012-07-05
申请号：US13378001
申请日：2010-06-16
申请人： Richard D. Dimarchi , David L. Smiley , Maria Dimarchi , Joseph Chabenne , Jonathan Day , James Patterson , Brian P. Ward , Tao Ma
发明人： Richard D. Dimarchi , David L. Smiley , Maria Dimarchi , Joseph Chabenne , Jonathan Day , James Patterson , Brian P. Ward , Tao Ma
IPC分类号： A61K38/26 , A61P3/10 , C07K14/605 , A61P3/04
CPC分类号： C07K14/605 , A61K38/00 , A61K38/26
摘要： Glucagon peptides with increased GIP activity are provided, optionally with GLP-I and/or glucagon activity. In some embodiments, C-terminally extended glucagon peptides comprising an amino acid sequence substantially similar to native glucagon are provided herein.
摘要翻译：提供具有增加的GIP活性的胰高血糖素肽，任选地具有GLP-1和/或胰高血糖素活性。在一些实施方案中，本文提供了包含与天然胰高血糖素基本相似的氨基酸序列的C-末端扩增的胰高血糖素肽。

6. 发明授权

US08981047B2 Glucagon antagonists 有权
标题翻译：胰高血糖素拮抗剂
公开(公告)号：US08981047B2
公开(公告)日：2015-03-17
申请号：US12739342
申请日：2008-10-23
申请人： Richard D. Dimarchi , Bin Yang
发明人： Richard D. Dimarchi , Bin Yang
IPC分类号： A61K38/26 , C07K14/605 , C07K14/00 , A61K38/00
CPC分类号： C07K14/605 , A61K38/00
摘要： Glucagon antagonists are provided which comprise amino acid substitutions and/or chemical modifications to glucagon sequence. In one embodiment, the glucagon antagonists comprise a native glucagon peptide that has been modified by the deletion of the first two to five amino acid residues from the N-terminus and (i) an amino acid substitution at position 9 (according to the numbering of native glucagon) or (ii) substitution of the Phe at position 6 (according to the numbering of native glucagon) with phenyl lactic acid (PLA). In another embodiment, the glucagon antagonists comprise the structure A-B-C as described herein, wherein A is PLA, an oxy derivative thereof, or a peptide of 2-6 amino acids in which two consecutive amino acids of the peptide are linked via an ester or ether bond.
摘要翻译：提供了包含对胰高血糖素序列的氨基酸取代和/或化学修饰的胰高血糖素拮抗剂。在一个实施方案中，胰高血糖素拮抗剂包含通过从N-末端缺失前两个至五个氨基酸残基而修饰的天然胰高血糖素肽，以及（i）在第9位的氨基酸取代（根据天然胰高血糖素）或（ii）用苯基乳酸（PLA）取代第6位的Phe（根据天然胰高血糖素的编号）。在另一个实施方案中，胰高血糖素拮抗剂包含如本文所述的结构ABC，其中A是PLA，其氧衍生物或2-6个氨基酸的肽，其中肽的两个连续氨基酸经由酯或醚连接键。

7. 发明授权

US08697838B2 Ester-based insulin prodrugs 有权
标题翻译：基于酯的胰岛素前药
公开(公告)号：US08697838B2
公开(公告)日：2014-04-15
申请号：US12845455
申请日：2010-07-28
申请人： Richard D. Dimarchi , Arnab De
发明人： Richard D. Dimarchi , Arnab De
IPC分类号： C07K14/62
CPC分类号： A61K38/28 , A61K9/0019 , A61K38/26 , A61K39/395 , A61K47/48215 , A61K47/48246 , A61K47/60 , A61K47/64
摘要： Prodrug formulations of bioactive polypeptides are provided wherein the bioactive polypeptide has been modified by the linkage of a dipeptide to the bioactive polypeptide through an ester linkage. The prodrugs disclosed herein in some embodiments have extended half lives of at least 1.5 hours (e.g., at least 10 hours), and more typically greater than 20 hours and less than 70 hours, and are converted to the active form at physiological conditions through a non-enzymatic reaction driven by chemical instability.
摘要翻译：提供生物活性多肽的前药制剂，其中生物活性多肽已经通过二酯与生物活性多肽的连接通过酯键进行了修饰。在一些实施方案中本文公开的前体药物具有至少1.5小时（例如，至少10小时），更通常大于20小时和小于70小时的半衰期延长，并且在生理条件下通过由化学不稳定驱动的非酶反应。

8. 发明申请

US20130116172A1 GLUCAGON SUPERFAMILY PEPTIDES EXHBITING G PROTEIN COUPLED RECEPTOR ACTIVITY 有权
标题翻译： 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
申请人： Richard D. Dimarchi , Lianshan Zhang
发明人： Richard D. Dimarchi , Lianshan Zhang
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。

9. 发明授权

US08022186B2 Modified human plasma polypeptide or Fc scaffolds and their uses 有权
公开(公告)号：US08022186B2
公开(公告)日：2011-09-20
申请号：US11927139
申请日：2007-10-29
申请人： Joseph Sheffer , Thea Norman , Richard D. Dimarchi , Anna-Maria A. Hays Putnam , Feng Tian , Stephanie Chu , Denise Krawitz , Ho Sung Cho
发明人： Joseph Sheffer , Thea Norman , Richard D. Dimarchi , Anna-Maria A. Hays Putnam , Feng Tian , Stephanie Chu , Denise Krawitz , Ho Sung Cho
IPC分类号： A61K38/38 , C07K14/765 , C12N15/14
CPC分类号： C07K14/47 , A61K38/00 , C07K14/765 , C07K19/00 , C07K2319/00
摘要： Modified human plasma polypeptides or Fc and uses thereof are provided.

10. 发明申请

US20100190701A1 GLUCAGON/GLP-1 RECEPTOR CO-AGONISTS 有权
标题翻译： GLUCAGON / GLP-1受体协同作用
公开(公告)号：US20100190701A1
公开(公告)日：2010-07-29
申请号：US12527140
申请日：2008-02-13
申请人： Jonathan Day , James Patterson , Joseph Chabenne , Maria Dimarchi , David Smiely , Richard D. Dimarchi
发明人： Jonathan Day , James Patterson , Joseph Chabenne , Maria Dimarchi , David Smiely , Richard D. Dimarchi
IPC分类号： A61K38/26 , C07K14/605 , A61P3/10 , A61P3/04
CPC分类号： C07K14/605 , A61K38/00 , A61K38/26 , A61K47/60 , C07K16/00 , C07K2317/52 , C07K2319/30
摘要： Modified glucagon peptides are disclosed having enhanced potency at the glucagon receptor relative to native glucagon. Further modification of the glucagon peptides by forming lactam bridges or the substitution of the terminal carboxylic acid with an amide group produces peptides exhibiting glucagon/GLP-1 receptor co-agonist activity. The solubility and stability of these high potency glucagon analogs can be further improved by modification of the polypeptides by pegylation, substitution of carboxy terminal amino acids, or the addition of a carboxy terminal peptide selected from the group consisting of SEQ ID NO: 26 (GPSSGAPPPS), SEQ ID NO: 27 (K-RNRNNIA) and SEQ ID NO: 28 (KRNR).
摘要翻译：公开了相对于天然胰高血糖素在胰高血糖素受体上具有增强的效力的改良的胰高血糖素肽。通过形成内酰胺桥或用酰胺基取代末端羧酸对胰高血糖素肽进一步修饰产生显示胰高血糖素/ GLP-1受体共激动剂活性的肽。这些高效胰高血糖素类似物的溶解度和稳定性可以通过聚乙二醇化，多肽羧基末端氨基酸的取代或加入选自SEQ ID NO：26（GPSSGAPPPS ），SEQ ID NO：27（K-RNRNNIA）和SEQ ID NO：28（KRNR）。

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