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37 条记录 (耗时 0.035 秒)

    GLUCAGON/GLP-1 RECEPTOR CO-AGONISTS
    1.
    发明申请
    GLUCAGON/GLP-1 RECEPTOR CO-AGONISTS 有权
    GLUCAGON / GLP-1受体协同作用

    公开(公告)号：US20130090286A1

    公开(公告)日：2013-04-11

    申请号：US13567858

    申请日：2012-08-06

    申请人： Elisabetta Bianchi ,  Antonello Pessi ,  Jonathan Day ,  Richard Dimarchi ,  David Smiley

    发明人： Elisabetta Bianchi ,  Antonello Pessi ,  Jonathan Day ,  Richard Dimarchi ,  David Smiley

    IPC分类号： C07K14/605

    CPC分类号： C07K14/605

    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 intramolecular 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, acylation, alkylation, substitution of carboxy terminal amino acids, C-terminal truncation, or the addition of a carboxy terminal peptide selected from the group consisting of SEQ ID NO: 26 (GPSSGAPPPS), SEQ ID NO: 27 (KRNRNNIA) 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。 通过形成分子内桥或通过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。 通过聚乙二醇化，酰化，烷基化，羧基末端氨基酸的取代，C-末端截短或加入选自下组的羧基末端肽，可以进一步改善这些高效胰高血糖素类似物的溶解度和稳定性 由SEQ ID NO：26（GPSSGAPPPS），SEQ ID NO：27（KRNRNNIA）和SEQ ID NO：28（KRNR）组成。

    Glucagon/GLP-1 receptor co-agonists
    2.
    发明授权
    Glucagon/GLP-1 receptor co-agonists 有权
    胰高血糖素/ GLP-1受体共激动剂

    公开(公告)号：US08969294B2

    公开(公告)日：2015-03-03

    申请号：US13567858

    申请日：2012-08-06

    申请人： Elisabetta Bianchi ,  Antonello Pessi ,  Jonathan Day ,  Richard Dimarchi ,  David Smiley

    发明人： Elisabetta Bianchi ,  Antonello Pessi ,  Jonathan Day ,  Richard Dimarchi ,  David Smiley

    IPC分类号： A61K38/26 ,  A61K38/12 ,  A61K38/00 ,  C07K14/605

    CPC分类号： C07K14/605

    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 intramolecular 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, acylation, alkylation, substitution of carboxy terminal amino acids, C-terminal truncation, or the addition of a carboxy terminal peptide selected from the group consisting of SEQ ID NO: 26 (GPSSGAPPPS), SEQ ID NO: 27 (KRNRNNIA) 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。 通过形成分子内桥或通过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。 通过聚乙二醇化，酰化，烷基化，羧基末端氨基酸的取代，C-末端截短或加入选自下组的羧基末端肽，可以进一步改善这些高效胰高血糖素类似物的溶解度和稳定性 由SEQ ID NO：26（GPSSGAPPPS），SEQ ID NO：27（KRNRNNIA）和SEQ ID NO：28（KRNR）组成。

    Stable Peptide Mimetic of Hiv Gp41 Fusion Intermediate
    5.
    发明申请
    Stable Peptide Mimetic of Hiv Gp41 Fusion Intermediate 有权
    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。

    HCV NS3 protease inhibitors
    8.
    发明授权
    HCV NS3 protease inhibitors 失效
    HCV NS3蛋白酶抑制剂

    公开(公告)号：US06995177B1

    公开(公告)日：2006-02-07

    申请号：US10129421

    申请日：2000-11-02

    申请人： Elisabetta Bianchi ,  Daniela Fattori ,  Paolo Ingallinella ,  Antonello Pessi

    发明人： Elisabetta Bianchi ,  Daniela Fattori ,  Paolo Ingallinella ,  Antonello Pessi

    IPC分类号： A61K38/06

    CPC分类号： C07K5/0202 ,  A61K38/00 ,  C07C237/22 ,  C07C2601/14 ,  C07K5/0812

    摘要： Compounds of formula (I) and pharmaceutically acceptable salts and esters thereof are active as inhibitors of hepatitis C virus NS3 protease. Consequently they are potentially useful in the treatment and prevention of hepatitis C virus infection and related conditions. In formula: (I) represents an aromatic or aliphatic carbocyclic ring and (n) is the total number of carbon atoms in the ring and is form 4 to 8.

    摘要翻译： 式（I）化合物及其药学上可接受的盐和酯作为丙型肝炎病毒NS3蛋白酶的抑制剂是有活性的。 因此，它们可用于治疗和预防丙型肝炎病毒感染和相关病症。 式中：（I）表示芳族或脂族碳环，（n）是环中碳原子的总数，为4-8。