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1. 发明申请

US20190338008A1 LONG-ACTING CO-AGONISTS OF THE GLUCAGON AND GLP-1 RECEPTORS 审中-公开
公开(公告)号：US20190338008A1
公开(公告)日：2019-11-07
申请号：US15759911
申请日：2016-10-21
申请人： Anandan PALANI , Ravi NARGUND , Paul E. CARRINGTON , Tomi SAWYER , Qiaolin DENG , Antonello PESSI , Elisabetta BIANCHI , Fe-derica ORYIETO , Merck Sharp & Dohme Corp.
发明人： Anandan Palani , Ravi Nargund , Paul E. Carrington , Tomi Sawyer , Qiaolin Deng , Antonello Pessi , Elisabetta Bianchi , Federica Orvieto
IPC分类号： C07K14/605 , A61P3/04 , A61K38/28
摘要： Long-acting co-agonists of the glucagon and GLP-1 receptors are described.

2. 发明申请

US20100075907A1 NEUROMEDIN U RECEPTOR AGONISTS AND USES THEREOF 审中-公开
标题翻译： NEUROMEDIN U受体激素及其用途
公开(公告)号：US20100075907A1
公开(公告)日：2010-03-25
申请号：US12623085
申请日：2009-11-20
申请人： Donald J. Marsh , Antonello Pessi , Maria A. Bednarek , Elisabetta Bianchi , Paolo Ingallinella , Andrea M. Peier
发明人： Donald J. Marsh , Antonello Pessi , Maria A. Bednarek , Elisabetta Bianchi , Paolo Ingallinella , Andrea M. Peier
IPC分类号： A61K38/16 , C07K14/00 , C07K7/06 , C07K7/08 , A61P9/00 , A61K38/08 , A61K38/10 , A61P3/00 , A61P35/00
CPC分类号： C07K14/575 , A61K38/00 , A61K47/543 , A61K47/554 , A61K47/60
摘要： Neuromedin U receptor agonists for use in the treatment of metabolic disorders such as obesity and diabetes are disclosed.
摘要翻译：公开了用于治疗代谢性疾病如肥胖症和糖尿病的神经介肽U受体激动剂。

3. 发明申请

US20070224212A1 Stable Peptide Mimetic of Hiv Gp41 Fusion Intermediate 有权
标题翻译：稳定肽模拟的HIF Gp41融合中间体
公开(公告)号：US20070224212A1
公开(公告)日：2007-09-27
申请号：US11628483
申请日：2005-05-27
申请人： Elisabetta Bianchi , Antonello Pessi , Romas Geleziunas , David Bramhill
发明人： Elisabetta Bianchi , Antonello Pessi , Romas Geleziunas , David Bramhill
IPC分类号： C12Q1/70
CPC分类号： C07K14/005 , A61K38/00 , A61K39/00 , A61K39/12 , C12N2740/15022 , C12N2740/16122 , C12N2740/16134 , G01N2333/16 , G01N2500/02
摘要： Methods of covalently-stabilizing alpha-helical, chimeric peptides constrained within a homotrimeric or heterotrimeric coiled-coil structure are disclosed. The coiled-coil structures made by the methods disclosed within this specification mimic all or a portion of the internal, trimeric coiled-coil motif contained within the fusogenic conformation of an enveloped virus membrane-fusion protein, particularly the internal coiled-coil domain of the HIV gp41 ectodomain. The HIV-derived, chimeric peptides disclosed comprise a non-HIV, soluble, trimeric form of a coiled-coil fused in helical phase to all or a portion of the N-helix of HIV gp41 and are covalently-stabilized in a homotrimeric or heterotrimeric coiled-coil structure through the formation of disulfide or chemoselective bonds between said peptides. The covalently-stabilized, HIV-derived, homotrimeric or heterotrimeric coiled-coil structures made by the methods disclosed herein represent a close mimetic of a HIV gp41 fusion intermediate and are potent inhibitors of HIV infectivity. These HIV-derived chimeric peptides may provide for therapeutic treatment against HIV infection by inhibiting the virus-host cell membrane fusion process.
摘要翻译：公开了限制在同三聚体或异三聚体卷曲螺旋结构内的共价稳定的α-螺旋嵌合肽的方法。通过本说明书中公开的方法制备的盘绕线圈结构模拟包含在包膜病毒膜 - 融合蛋白的融合构象内的内部三聚体卷曲螺旋基序的全部或一部分，特别是内部卷曲螺旋结构域 HIV gp41胞外域。所公开的HIV衍生的嵌合肽包含螺旋状螺旋状的非HIV，可溶性三聚体形式，其与HIV gp41的全部或部分N-螺旋融合，并且以同三聚或异三聚体共价稳定通过在所述肽之间形成二硫键或化学选择性键来进行卷曲螺旋结构。由本文公开的方法制备的共价稳定的HIV衍生的同源三聚体或异三聚体卷曲螺旋结构代表HIV gp41融合中间体的密切模拟物，并且是HIV感染性的有效抑制剂。这些HIV衍生的嵌合肽可以通过抑制病毒宿主细胞膜融合过程来提供针对HIV感染的治疗性治疗。

4. 发明授权

US10793615B2 Long-acting co-agonists of the glucagon and GLP-1 receptors 有权
公开(公告)号：US10793615B2
公开(公告)日：2020-10-06
申请号：US15759911
申请日：2016-10-21
申请人： Merck Sharp & Dohme Corp. , Anandan Palani , Ravi Nargund , Paul E. Carrington , Tomi Sawyer , Qiaolin Deng , Antonello Pessi , Elisabetta Bianchi , Federica Orvieto
发明人： Anandan Palani , Ravi Nargund , Paul E. Carrington , Tomi Sawyer , Qiaolin Deng , Antonello Pessi , Elisabetta Bianchi , Federica Orvieto
IPC分类号： A61K38/00 , A61K38/28 , A61P3/04 , A61P7/12 , A61P3/10 , C07K14/435 , C07K14/605
摘要： Long-acting co-agonists of the glucagon and GLP-1 receptors are described.

5. 发明申请

US20110046056A1 APOA-1 PEPTIDE MIMETICS 审中-公开
标题翻译： APOA-1肽类物质
公开(公告)号：US20110046056A1
公开(公告)日：2011-02-24
申请号：US12664510
申请日：2008-06-18
申请人： Elisabetta Bianchi , Antonello Pessi , Raffaele Ingenito , Jun Wang , Ester Carballo-Jane , Ching H. Chang
发明人： Elisabetta Bianchi , Antonello Pessi , Raffaele Ingenito , Jun Wang , Ester Carballo-Jane , Ching H. Chang
IPC分类号： A61K38/16 , C07K14/00 , A61P9/10
CPC分类号： C07K14/775 , A61K38/00
摘要： The invention relates to peptide mimetics for treating disorders associated with hypercholesterolemia and cardio-vascular disease. In particular, the invention relates to peptides that mimic the activity of apolipoprotein A-I (Apo AI).
摘要翻译：本发明涉及用于治疗与高胆固醇血症和心血管疾病相关的疾病的肽模拟物。特别地，本发明涉及模拟载脂蛋白A-1（Apo AI）的活性的肽。

6. 发明申请

US20100305028A1 CHOLESTEROL DERIVATIVES OF INHIBITORS OF VIRAL FUSION 有权
标题翻译：维生素D抑制剂的胆固醇衍生物
公开(公告)号：US20100305028A1
公开(公告)日：2010-12-02
申请号：US12738998
申请日：2008-10-20
申请人： Antonello Pessi , Elisabetta Bianchi , Paolo Ingallinella
发明人： Antonello Pessi , Elisabetta Bianchi , Paolo Ingallinella
IPC分类号： A61K38/16 , C07K7/06 , C07K7/08 , C07K14/00 , A61K38/10 , A61K38/08 , A61P31/18
CPC分类号： C07K14/005 , A61K47/554
摘要： The present invention relates to compounds comprising at least ten contigous amino acids of the HR2 domain of a Type 1 viral fusogenic protein of an enveloped virus, or a derivative thereof, attached at the C-terminal to cholesterol or a derivative thereof; or a pharmaceutically acceptable salt thereof which inhibit viral fusion. Thus compounds of the invention are useful to prevent or treat diseases caused by an enveloped virus.
摘要翻译：本发明涉及包含病毒包膜病毒的1型病毒融合蛋白或其衍生物的HR2结构域至少10个连接氨基酸的化合物，其在C-末端连接至胆固醇或其衍生物; 或其药学上可接受的盐，其抑制病毒融合。因此，本发明的化合物可用于预防或治疗由包膜病毒引起的疾病。

7. 发明申请

US20100092505A1 Method for Shielding Functional Sites or Epitopes on Proteins 审中-公开
标题翻译：屏蔽蛋白质功能位点或表位的方法
公开(公告)号：US20100092505A1
公开(公告)日：2010-04-15
申请号：US11887604
申请日：2006-03-31
申请人： Elisabetta Bianchi , Antonello Pessi
发明人： Elisabetta Bianchi , Antonello Pessi
IPC分类号： A61K39/385 , C07K17/00 , A61P37/04
CPC分类号： C07K14/005 , A61K39/00 , A61K47/60 , C12N2740/16122
摘要： Methods of site-specifically shielding one or more binding sites within a polypeptide are disclosed, comprising attaching at least one small molecular weight, water-soluble polymer to said polypeptide such that the binding site is masked by said polymer. The shielding of a binding site (e.g., epitope) as per the disclosed methods acts to either eliminate or substantially reduce the biological response induced by the interaction between said binding site and its cognate receptor, helping to refocus the biological response toward unmasked portions of the polypeptide. Pharmaceutical products generated as per the methods described herein (e.g., polymer-modified antigens and vaccine compositions comprising them), as well as the use thereof, induce a specific immune response against unmasked portions of the polypeptides when directly introduced into living vertebrate tissue, preferably a mammalian host such as a human or a non-human mammal of commercial or domestic veterinary importance, generating selective immunoprotection in said mammal.
摘要翻译：公开了特异性屏蔽多肽内的一个或多个结合位点的方法，包括将至少一种小分子量的水溶性聚合物连接到所述多肽上，使得结合位点被所述聚合物掩蔽。根据所公开的方法，结合位点（例如，表位）的屏蔽用于消除或显着降低由所述结合位点与其同源受体之间的相互作用诱导的生物反应，有助于将生物反应重新聚焦到未被掩蔽的部分多肽。根据本文所述的方法（例如，聚合物修饰的抗原和包含它们的疫苗组合物）产生的药物产品及其用途当直接引入活的脊椎动物组织时诱导针对多肽的未掩蔽部分的特异性免疫应答哺乳动物宿主，例如商业或家庭兽医重要的人或非人哺乳动物，在所述哺乳动物中产生选择性免疫保护。

8. 发明授权

US08629101B2 Cholesterol derivatives of inhibitors of viral fusion 有权
标题翻译：病毒融合抑制剂的胆固醇衍生物
公开(公告)号：US08629101B2
公开(公告)日：2014-01-14
申请号：US12738998
申请日：2008-10-20
申请人： Antonello Pessi , Elisabetta Bianchi , Paolo Ingallinella
发明人： Antonello Pessi , Elisabetta Bianchi , Paolo Ingallinella
IPC分类号： A61K38/16 , C07K14/00
CPC分类号： C07K14/005 , A61K47/554
摘要： The present invention relates to compounds comprising at least ten contigous amino acids of the HR2 domain of a Type 1 viral fusogenic protein of an enveloped virus, or a derivative thereof, attached at the C-terminal to cholesterol or a derivative thereof; or a pharmaceutically acceptable salt thereof which inhibit viral fusion. Thus compounds of the invention are useful to prevent or treat diseases caused by an enveloped virus.
摘要翻译：本发明涉及包含病毒包膜病毒的1型病毒融合蛋白或其衍生物的HR2结构域至少10个连接氨基酸的化合物，其在C-末端连接至胆固醇或其衍生物; 或其药学上可接受的盐，其抑制病毒融合。因此，本发明的化合物可用于预防或治疗由包膜病毒引起的疾病。

9. 发明申请

US20110183902A1 PHARMACEUTICAL COMPOSITION COMPRISING OXYNTOMODULIN DERIVATIVES AND A METHOD FOR REDUCING BODY WEIGHT USING THE COMPOSITION 有权
标题翻译：包含氧亚氨基青霉素衍生物的药物组合物和使用组合物降低身体重量的方法
公开(公告)号：US20110183902A1
公开(公告)日：2011-07-28
申请号：US13052270
申请日：2011-03-21
申请人： Ranabir Sinha Roy , Elisabetta Bianchi , Antonello Pessi , Paolo Ingallinella , Donald J. Marsh , George J. Eiermann , Yingjun Mu , Yun-Ping Zhou
发明人： Ranabir Sinha Roy , Elisabetta Bianchi , Antonello Pessi , Paolo Ingallinella , Donald J. Marsh , George J. Eiermann , Yingjun Mu , Yun-Ping Zhou
IPC分类号： A61K38/22 , C07K14/575 , A61P3/08
CPC分类号： C07K14/575 , A61K38/00
摘要： Modified oxyntomodulin derivatives. Such derivatives can be used for the treatment of metabolic diseases such as diabetes and obesity.
摘要翻译：改良的胃泌酸调节蛋白衍生物。这样的衍生物可用于治疗代谢性疾病如糖尿病和肥胖症。

10. 发明授权

US07811577B2 Covalently stabilized chimeric coiled-coil HIV gp41 N-peptides with improved antiviral activity 有权
标题翻译：具有改善的抗病毒活性的共价稳定的嵌合卷曲螺旋HIV gp41 N-肽
公开(公告)号：US07811577B2
公开(公告)日：2010-10-12
申请号：US11628483
申请日：2005-05-27
申请人： Elisabetta Bianchi , Antonello Pessi , Romas Geleziunas , David Bramhill
发明人： Elisabetta Bianchi , Antonello Pessi , Romas Geleziunas , David Bramhill
IPC分类号： A61K39/00 , A61K39/21
CPC分类号： C07K14/005 , A61K38/00 , A61K39/00 , A61K39/12 , C12N2740/15022 , C12N2740/16122 , C12N2740/16134 , G01N2333/16 , G01N2500/02
摘要： Methods of covalently-stabilizing alpha-helical, chimeric peptides constrained within a homotrimeric or heterotrimeric coiled-coil structure are disclosed. The coiled-coil structures made by the methods disclosed within this specification mimic all or a portion of the internal, trimeric coiled-coil motif contained within the fusogenic conformation of an enveloped virus membrane-fusion protein, particularly the internal coiled-coil domain of the HIV gp41 ectodomain. The HIV-derived, chimeric peptides disclosed comprise a non-HIV, soluble, trimeric form of a coiled-coil fused in helical phase to all or a portion of the N-helix of HIV gp41 and are covalently-stabilized in a homotrimeric or heterotrimeric coiled-coil structure through the formation of disulfide or chemoselective bonds between said peptides. The covalently-stabilized, HIV-derived, homotrimeric or heterotrimeric coiled-coil structures made by the methods disclosed herein represent a close mimetic of a HIV gp41 fusion intermediate and are potent inhibitors of HIV infectivity. These HIV-derived chimeric peptides may provide for therapeutic treatment against HIV infection by inhibiting the virus-host cell membrane fusion process.
摘要翻译：公开了限制在同三聚体或异三聚体卷曲螺旋结构内的共价稳定的α-螺旋嵌合肽的方法。通过本说明书中公开的方法制备的盘绕线圈结构模拟包含在包膜病毒膜 - 融合蛋白的融合构象内的内部三聚体卷曲螺旋基序的全部或一部分，特别是内部卷曲螺旋结构域 HIV gp41胞外域。所公开的HIV衍生的嵌合肽包含螺旋状螺旋状的非HIV，可溶性三聚体形式，其与HIV gp41的全部或部分N-螺旋融合，并以共三聚体或异三聚体共价稳定通过在所述肽之间形成二硫键或化学选择性键来进行卷曲螺旋结构。由本文公开的方法制备的共价稳定的HIV衍生的同源三聚体或异三聚体卷曲螺旋结构代表HIV gp41融合中间体的密切模拟物，并且是HIV感染性的有效抑制剂。这些HIV衍生的嵌合肽可以通过抑制病毒宿主细胞膜融合过程来提供针对HIV感染的治疗性治疗。

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