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1. 发明申请

US20050043237A1 Pituitary adenylate cyclase activating peptide (PACAP) receptor 3 (R3) agonists and their pharmacological methods of use 有权
标题翻译：垂体腺苷酸环化酶活化肽（PACAP）受体3（R3）激动剂及其药理学用途
公开(公告)号：US20050043237A1
公开(公告)日：2005-02-24
申请号：US10892981
申请日：2004-07-15
申请人： Clark Pan , Manami Tsutsumi , Armen Shanafelt
发明人： Clark Pan , Manami Tsutsumi , Armen Shanafelt
IPC分类号： A61K38/00 , A61K48/00 , C07K14/575 , C07K14/705 , A61K38/17 , C07H21/04
CPC分类号： C07K14/575 , A61K38/00 , A61K48/00
摘要： This invention provides novel peptides that function in vivo to stimulate insulin release from pancreatic beta cells in a glucose-dependent fashion. These insulin secretagogue peptides are shown to stimulate insulin release in rat islet cells in vitro, and in vivo. The peptides of the present invention provide a new therapy for patients with decreased endogenous insulin secretion, in particular type 2 diabetics. In particular, the invention is a polypeptide selected from a specific group of VIP/PACAP-related polypeptides, or functional equivalents thereof. The invention is also directed to a method of treating a metabolic disease in a mammal comprising administering a therapeutically effective amount of the insulin secretagogue peptides to said mammal. Also disclosed are methods of making the peptides, both recombinant and synthetic.
摘要翻译：本发明提供了新的肽，其在体内起作用以以葡萄糖依赖的方式刺激胰腺β细胞的胰岛素释放。这些胰岛素促分泌肽显示能够在体外和体内刺激大鼠胰岛细胞中的胰岛素释放。本发明的肽为具有降低的内源性胰岛素分泌的患者特别是2型糖尿病患者提供了新的疗法。特别地，本发明是选自VIP / PACAP相关多肽的特定组的多肽或其功能等同物。本发明还涉及一种治疗哺乳动物代谢疾病的方法，包括向所述哺乳动物施用治疗有效量的胰岛素促分泌肽。还公开了制备重组体和合成肽的方法。

2. 发明授权

US06972319B1 Pituitary adenylate cyclase activating peptide (PACAP)receptor 3 (R3) agonists and their pharmacological methods of use 失效
标题翻译：垂体腺苷酸环化酶活化肽（PACAP）受体3（R3）激动剂及其药理学用途
公开(公告)号：US06972319B1
公开(公告)日：2005-12-06
申请号：US09671773
申请日：2000-09-27
申请人： Clark Pan , Manami Tsutsumi , Armen B. Shanafelt
发明人： Clark Pan , Manami Tsutsumi , Armen B. Shanafelt
IPC分类号： A61K38/00 , A61K38/16 , C07K14/00 , C07K14/47 , C07K14/72
CPC分类号： C07K14/72 , A61K38/00 , C07K14/4705
摘要： This invention provides novel peptides that function in vivo to stimulate insulin release from pancreatic beta cells in a glucose-dependent fashion. These insulin secretagogue peptides are shown to stimulate insulin release in rat islet cells in vitro, and in vivo. The peptides of the present invention provide a new therapy for patients with decreased endogenous insulin secretion, in particular type 2 diabetics. In particular, the invention is a polypeptide selected from a specific group of VIP/PACAP-related polypeptides, or functional equivalents thereof. The invention is also directed to a method of treating a metabolic disease in a mammal comprising administering a therapeutically effective amount of the insulin secretagogue peptides to said mammal. Also disclosed are methods of making the peptides, both recombinant and synthetic.
摘要翻译：本发明提供了新的肽，其在体内起作用以以葡萄糖依赖的方式刺激胰腺β细胞的胰岛素释放。这些胰岛素促分泌肽显示能够在体外和体内刺激大鼠胰岛细胞中的胰岛素释放。本发明的肽为具有降低的内源性胰岛素分泌的患者特别是2型糖尿病患者提供了新的疗法。特别地，本发明是选自VIP / PACAP相关多肽的特定组的多肽或其功能等同物。本发明还涉及一种治疗哺乳动物代谢疾病的方法，包括向所述哺乳动物施用治疗有效量的胰岛素促分泌肽。还公开了制备重组体和合成肽的方法。

3. 发明授权

US07507714B2 Pituitary adenylate cyclase activating peptide (PACAP) receptor 3 (R3) agonists and their pharmacological methods of use 有权
标题翻译：垂体腺苷酸环化酶活化肽（PACAP）受体3（R3）激动剂及其药理学用途
公开(公告)号：US07507714B2
公开(公告)日：2009-03-24
申请号：US10892981
申请日：2004-07-15
申请人： Clark Pan , Manami Tsutsumi , Armen B. Shanafelt
发明人： Clark Pan , Manami Tsutsumi , Armen B. Shanafelt
IPC分类号： A61K38/16 , C07K14/00
CPC分类号： C07K14/575 , A61K38/00 , A61K48/00
摘要： This invention provides novel peptides that function in vivo to stimulate insulin release from pancreatic beta cells in a glucose-dependent fashion. These insulin secretagogue peptides are shown to stimulate insulin release in rat islet cells in vitro, and in vivo. The peptides of the present invention provide a new therapy for patients with decreased endogenous insulin secretion, in particular type 2 diabetics. In particular, the invention is a polypeptide selected from a specific group of VIP/PACAP-related polypeptides, or functional equivalents thereof. The invention is also directed to a method of treating a metabolic disease in a mammal comprising administering a therapeutically effective amount of the insulin secretagogue peptides to said mammal. Also disclosed are methods of making the peptides, both recombinant and synthetic.
摘要翻译：本发明提供了新的肽，其在体内起作用以以葡萄糖依赖的方式刺激胰腺β细胞的胰岛素释放。这些胰岛素促分泌肽显示能够在体外和体内刺激大鼠胰岛细胞中的胰岛素释放。本发明的肽为具有降低的内源性胰岛素分泌的患者特别是2型糖尿病患者提供了新的疗法。特别地，本发明是选自VIP / PACAP相关多肽的特定组的多肽或其功能等同物。本发明还涉及一种治疗哺乳动物代谢疾病的方法，包括向所述哺乳动物施用治疗有效量的胰岛素促分泌肽。还公开了制备重组体和合成肽的方法。

4. 发明申请

US20110183920A1 MODIFIED IL-4 MUTEIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：修饰的IL-4 MUTEIN受体拮抗剂
公开(公告)号：US20110183920A1
公开(公告)日：2011-07-28
申请号：US12868621
申请日：2010-08-25
申请人： Clark Pan , Steve Roczniak , Jeffrey Michael Greve , Stephanie L. Yung , Malinda Longphre , Teresa Mo-Fun Wong , Adrian Tomkinson , David Boisvert , Elise Burmeister-Getz , Kathy Delaria
发明人： Clark Pan , Steve Roczniak , Jeffrey Michael Greve , Stephanie L. Yung , Malinda Longphre , Teresa Mo-Fun Wong , Adrian Tomkinson , David Boisvert , Elise Burmeister-Getz , Kathy Delaria
IPC分类号： A61K38/16 , C07K14/00 , C07H21/00 , A61P11/06
CPC分类号： C07K14/5406 , A61K38/00 , C07K14/7155
摘要： This invention relates to modified IL-4 mutein receptor antagonists comprising an IL-4 mutein receptor antagonist coupled to polyethylene glycol. Related formulations and dosages and methods of administration thereof for therapeutic purposes are also provided. These modified IL-4 mutein receptor antagonists, compositions and methods provide a treatment option for those individuals afflicted with a respiratory disorder such as asthma by inhibiting IL-4 and IL-13-mediated airway hyperresponsiveness and eosinophilia. More particularly, these antagonists have an increased duration of effect versus unmodified IL-4RA by virtue of a greater plasma half-life.
摘要翻译：本发明涉及包含与聚乙二醇偶联的IL-4突变蛋白受体拮抗剂的经修饰的IL-4突变蛋白受体拮抗剂。还提供了用于治疗目的的相关制剂和剂量及其施用方法。这些修饰的IL-4突变蛋白受体拮抗剂，组合物和方法通过抑制IL-4和IL-13介导的气道高反应性和嗜酸性粒细胞增多为患有呼吸系统疾病如哮喘的个体提供治疗选择。更具体地，这些拮抗剂由于更大的血浆半衰期而对未改性的IL-4RA具有增加的作用持续时间。

5. 发明授权

US07378494B2 Pituitary adenylate cyclase activating peptide (PACAP) receptor (VPAC2) agonist peptide 失效
标题翻译：垂体腺苷酸环化酶激活肽（PACAP）受体（VPAC2）激动剂肽
公开(公告)号：US07378494B2
公开(公告)日：2008-05-27
申请号：US10618126
申请日：2003-07-11
申请人： Wayne A. Froland , Drew N. Kelner , Michael L. Dumas , Clark Pan , James Whelan , Yu-chang John Wang , Wei Wang
发明人： Wayne A. Froland , Drew N. Kelner , Michael L. Dumas , Clark Pan , James Whelan , Yu-chang John Wang , Wei Wang
IPC分类号： C07K14/705
CPC分类号： C07K14/70503 , A61K38/00 , C07K14/57563
摘要： This invention provides novel peptides that function in vivo as agonists of the VPAC2 receptor. These insulin secretagogue polypeptides are shown to lower blood glucose in vivo more than controls upon glucose challenge. The polypeptides of this invention are also stable in formulation and have long half-lives. The peptides of the present invention provide a new therapy for patients with decreased endogenous insulin secretion, in particular type 2 diabetics. In particular, the invention is a polypeptide selected from a specific group of VPAC2-related polypeptides, or functional equivalents thereof. The invention is also directed to a method of treating a metabolic disease in a mammal comprising administering a therapeutically effective amount of the insulin secretagogue peptides to said mammal. Also disclosed are methods of making the peptides, both recombinant and synthetic.
摘要翻译：本发明提供了在体内作为VPAC2受体的激动剂起作用的新型肽。显示这些胰岛素促分泌素多肽比葡萄糖攻击时的对照降低体内血糖。本发明的多肽在制剂中也是稳定的并且具有长的半衰期。本发明的肽为具有降低的内源性胰岛素分泌的患者特别是2型糖尿病患者提供了新的疗法。特别地，本发明是选自VPAC2相关多肽的特定组的多肽或其功能等同物。本发明还涉及一种治疗哺乳动物代谢疾病的方法，包括向所述哺乳动物施用治疗有效量的胰岛素促分泌肽。还公开了制备重组体和合成肽的方法。

6. 发明申请

US20050288248A1 Peptides acting as both GLP-1 receptor agonists and glucagon receptor antagonists and their pharmacological methods of use 失效
公开(公告)号：US20050288248A1
公开(公告)日：2005-12-29
申请号：US11212439
申请日：2005-08-26
申请人： Clark Pan , James Whelan , Kevin Clairmont
发明人： Clark Pan , James Whelan , Kevin Clairmont
IPC分类号： C12N15/09 , A61K31/7088 , A61K38/00 , A61K38/22 , A61K48/00 , A61P3/00 , A61P3/04 , A61P3/08 , A61P3/10 , A61P43/00 , C07K14/47 , C07K14/575 , C07K14/605 , C07K14/745 , C07K16/00 , C07K16/18 , C12N1/15 , C12N1/19 , C12N1/21 , C12N5/10 , C12N15/00 , C12P21/02 , C07H21/04 , C07K14/705 , C12Q1/68
CPC分类号： C07K14/605 , A61K38/00
摘要： The invention provides polypeptides that act both as an agonist of the GLP-1 receptor and an antagonist of the glucagon receptor. Such polypeptides are useful for treating individuals with type 2 diabetes or other metabolic disorders.

7. 发明申请

US20050203009A1 VPAC1 selective antagonists and their pharmacological methods of use 审中-公开
标题翻译： VPAC1选择性拮抗剂及其药理学用途
公开(公告)号：US20050203009A1
公开(公告)日：2005-09-15
申请号：US10799897
申请日：2004-03-12
申请人： Clark Pan , Steve Roczniak
发明人： Clark Pan , Steve Roczniak
IPC分类号： A61K38/17 , C07H21/04 , C07K14/71 , C12N15/09
CPC分类号： C07K14/57563 , A61K38/00 , C07K14/70571 , C07K2319/00
摘要： The disclosed invention relates to selective VPAC1 antagonists, related formulations, dosages and methods of use. The selective VPAC1 antagonists of the invention comprise a vasoactive intestinal peptide component and a growth hormone releasing hormone component capable of selectively binding to and antagonizing the VPAC1 receptor at significantly lower concentrations than those concentrations at which it binds to and antagonizes the VPAC2 receptor.
摘要翻译：所公开的发明涉及选择性VPAC1拮抗剂，相关制剂，剂量和使用方法。本发明的选择性VPAC1拮抗剂包含血管活性肠肽组分和生长激素释放激素组分，其能够以比其结合并拮抗VPAC2受体的浓度低得多的浓度选择性地结合并拮抗VPAC1受体。

8. 发明申请

US20050170365A1 Human DNase I hyperactive variants 有权
标题翻译：人类DNase I活性变异
公开(公告)号：US20050170365A1
公开(公告)日：2005-08-04
申请号：US10838691
申请日：2004-05-03
申请人： Robert Lazarus , Clark Pan
发明人： Robert Lazarus , Clark Pan
IPC分类号： C12N15/09 , A61K9/08 , A61K38/00 , A61K38/46 , A61P11/12 , C12N9/16 , C12N9/22 , C12N15/55 , C12R1/91 , C12Q1/68 , C07H21/04 , C12P19/34
CPC分类号： C12N9/22 , A61K38/00
摘要： The present invention relates to amino acid sequence variants of human DNase I that have increased DNA-hydrolytic activity. The invention provides nucleic acid sequences encoding such hyperactive variants, thereby enabling the production of these variants in quantities sufficient for clinical use. The invention also relates to pharmaceutical compositions and therapeutic uses of hyperactive-variants of human DNase I.
摘要翻译：本发明涉及具有增加的DNA-水解活性的人类DNA酶I的氨基酸序列变体。本发明提供了编码这种多活性变体的核酸序列，从而使得能够以足以临床使用的量生产这些变体。本发明还涉及人DNase I的活性变异体的药物组合物和治疗用途。

9. 发明申请

US20050153890A1 Peptides acting as both GLP-1 receptor agonists and glucagon receptor antagonists and their pharmacological methods of use 失效
公开(公告)号：US20050153890A1
公开(公告)日：2005-07-14
申请号：US10999622
申请日：2004-11-29
申请人： Clark Pan , James Whelan , Kevin Clairmont
发明人： Clark Pan , James Whelan , Kevin Clairmont
IPC分类号： C12N15/09 , A61K31/7088 , A61K38/00 , A61K38/22 , A61K48/00 , A61P3/00 , A61P3/04 , A61P3/08 , A61P3/10 , A61P43/00 , C07K14/47 , C07K14/575 , C07K14/605 , C07K14/745 , C07K16/00 , C07K16/18 , C12N1/15 , C12N1/19 , C12N1/21 , C12N5/10 , C12N15/00 , C12P21/02 , A61K38/17 , C07H21/04 , C07K14/72 , C07K16/28
CPC分类号： C07K14/605 , A61K38/00
摘要： The invention provides polypeptides that act both as an agonist of the GLP-1 receptor and an antagonist of the glucagon receptor. Such polypeptides are useful for treating individuals with type 2 diabetes or other metabolic disorders.

10. 发明授权

US06864069B2 Peptides acting as both GLP-1 receptor agonists and glucagon receptor antagonists and their pharmacological methods of use 失效
标题翻译：作为GLP-1受体激动剂和胰高血糖素受体拮抗剂的肽及其药理学用途
公开(公告)号：US06864069B2
公开(公告)日：2005-03-08
申请号：US10265345
申请日：2002-10-03
申请人： Clark Pan , James Whelan , Kevin B. Clairmont
发明人： Clark Pan , James Whelan , Kevin B. Clairmont
IPC分类号： A61K38/00 , C07K14/605 , C12P21/06 , C07H21/02 , C07K14/00 , C12N5/00 , C12N15/63
CPC分类号： C07K14/605 , A61K38/00
摘要： The invention provides polypeptides that act both as an agonist of the GLP-1 receptor and an antagonist of the glucagon receptor. Such polypeptides are useful for treating individuals with type 2 diabetes or other metabolic disorders.
摘要翻译：本发明提供了作为GLP-1受体的激动剂和胰高血糖素受体拮抗剂的作用的多肽。这样的多肽可用于治疗2型糖尿病或其他代谢紊乱的个体。

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