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41 条记录 (耗时 0.044 秒)

    Reversible pegylated drugs
    21.
    发明授权
    Reversible pegylated drugs 有权
    可逆的聚乙二醇化药物

    公开(公告)号：US07585837B2

    公开(公告)日：2009-09-08

    申请号：US11244402

    申请日：2005-10-06

    申请人： Yoram Shechter ,  Matityahu Fridkin ,  Haim Tsubery

    发明人： Yoram Shechter ,  Matityahu Fridkin ,  Haim Tsubery

    IPC分类号： A61K38/00 ,  A61K47/48 ,  C07K2/00

    CPC分类号： A61K47/60 ,  A61K31/7036 ,  A61K38/1709 ,  A61K38/212 ,  A61K38/22 ,  A61K38/2242 ,  A61K38/2278 ,  A61K38/26 ,  A61K38/27 ,  A61K38/28 ,  A61K47/54 ,  A61K47/545 ,  C07D207/404 ,  C07D207/416 ,  C07D207/452 ,  C07D403/12

    摘要： Reversible pegylated drugs are provided by derivatization of free functional groups of the drug selected from amino, hydroxyl, mercapto, phosphate and/or carboxyl with groups sensitive to mild basic conditions such as 9-fluorenylmethoxycarbonyl (Fmoc) or 2-sulfo-9-fluorenylmethoxycarbonyl (FMS), to which group a PEG moiety is attached. In these pegylated drugs, the PEG moiety and the drug residue are not linked directly to each other, but rather both residues are linked to different positions of the scaffold Fmoc or FMS structure that is highly sensitive to bases and is removable under physiological conditions. The drugs are preferably drugs containing an amino group, most preferably peptides and proteins of low or medium molecular weight. Similar molecules are provided wherein a protein carrier or another polymer carrier replaces the PEG moiety.

    摘要翻译： 可逆的聚乙二醇化药物通过衍生自选自氨基，羟基，巯基，磷酸酯和/或羧基的药物的游离官能团与对温和碱性条件敏感的基团如9-芴基甲氧基羰基（Fmoc）或2-磺基-9-芴基甲氧基羰基 （FMS），连接有PEG部分的基团。 在这些聚乙二醇化药物中，PEG部分和药物残留物不直接相互连接，而是两个残基都连接到对碱基高度敏感并在生理条件下可去除的支架Fmoc或FMS结构的不同位置。 药物优选是含有氨基的药物，最优选低分子量或中等分子量的肽和蛋白质。 提供了类似的分子，其中蛋白质载体或另一种聚合物载体取代了PEG部分。

    Long-acting derivatives of pyy agonists
    22.
    发明申请
    Long-acting derivatives of pyy agonists 审中-公开
    长效衍生物的pyy激动剂

    公开(公告)号：US20070027073A1

    公开(公告)日：2007-02-01

    申请号：US10552591

    申请日：2004-04-08

    申请人： Menachem Rubinstein ,  Yoram Shechter ,  Matityahu Fridkin

    发明人： Menachem Rubinstein ,  Yoram Shechter ,  Matityahu Fridkin

    IPC分类号： A61K38/22 ,  C07K14/575

    CPC分类号： C07K14/575 ,  A61K38/00

    摘要： The invention provides a PYY agonist derivative of the formula: (X)n-Z, wherein X is a radical 9-fluorenylmethoxy-carbonyl (Fmoc) or 2-sulfo-9-fluorenyl-methoxycarbonyl (FMS), Z is the residue of a PYY agonist linked to the radical X through an amino or hydroxyl group, and n is 1 to 3, or a pharmaceutically acceptable salt thereof, for reducing food intake and treatment of a disease, condition or disorder that can be alleviated by reduction of food intake such as obesity, hypertension, dyslipidemia, cardiovascular risk, eating disorder, insulin-resistance, or diabetes mellitus.

    摘要翻译： 本发明提供下式的PYY激动剂衍生物：其中X是9-芴基甲氧基羰基（Fmoc）或2-磺基-9-芴基 - 甲氧羰基（FMS） ），Z是通过氨基或羟基与X基团连接的PYY激动剂的残基，n为1至3，或其药学上可接受的盐，用于减少食物摄取和治疗疾病，病症或病症，其中 可通过减少食物摄取如肥胖，高血压，血脂异常，心血管风险，进食障碍，胰岛素抵抗或糖尿病来缓解。

    Neuroprotective iron chelators and pharmaceutical compositions comprising them
    23.
    发明申请
    Neuroprotective iron chelators and pharmaceutical compositions comprising them 有权
    神经保护性铁螯合剂和包含它们的药物组合物

    公开(公告)号：US20060234927A1

    公开(公告)日：2006-10-19

    申请号：US10534357

    申请日：2006-02-21

    申请人： Moussa Youdim ,  Matityahu Fridkin ,  Hailin Zheng ,  Abraham Warshawsky ,  Rivka Warshawsky

    发明人： Moussa Youdim ,  Matityahu Fridkin ,  Hailin Zheng ,  Abraham Warshawsky ,  Rivka Warshawsky

    IPC分类号： A61K38/22 ,  C07K14/575 ,  A61K31/496 ,  A61K31/4709 ,  C07D403/14

    CPC分类号： C07D295/15 ,  A61K38/00 ,  A61K45/06 ,  A61K47/547 ,  C07D213/69 ,  C07D215/26 ,  C07D295/205 ,  C07K7/06 ,  C07K7/22 ,  C07K7/23 ,  C07K14/57563 ,  C07K14/70 ,  Y02A50/411

    摘要： Novel iron chelators exhibiting neuroprotective and good transport properties are useful in iron chelation therapy for treatment of a disease, disorder or condition associated with iron overload and oxidative stress, eg. a neurodegenerative or cerebrovascular disease or disorder, a neoplastic disease, hemochromatosis, thalassemia, a cardiovascular disease, diabetes, a inflammatory disorder, anthracycline cardiotoxicity, a viral infection, a protozoal infection, a yeast infection, retarding ageing, and prevention and/or treatment of skin ageing and skin protection against sunlight and/or UV light. The iron chelator function is provided by a 8-hydroxyquinoline, a hydroxypyridinone or a hydroxamate moiety, the neuroprotective function is imparted to the compound e.g. by a neuroprotective peptide, and a combined antiapoptotic and neuroprotective function by a propargyl group.

    摘要翻译： 显示出神经保护和良好转运性质的新型铁螯合剂可用于铁螯合治疗用于治疗与铁过载和氧化应激相关的疾病，病症或病症，例如， 神经变性或脑血管疾病或病症，肿瘤性疾病，血色素沉着病，地中海贫血，心血管疾病，糖尿病，炎性病症，蒽环类心脏毒性，病毒感染，原生动物感染，酵母感染，延迟衰老以及预防和/或治疗 的皮肤老化和皮肤防晒防晒和/或紫外线。 铁螯合剂功能由8-羟基喹啉，羟基吡啶酮或异羟肟酸盐部分提供，神经保护功能被赋予化合物例如 通过神经保护肽，以及由炔丙基组合的抗细胞凋亡和神经保护功能。

    Derivatives of structurally modified VIP and pharmaceutical compositions containing them
    26.
    发明授权
    Derivatives of structurally modified VIP and pharmaceutical compositions containing them 失效
    结构改性的VIP衍生物和含有它们的药物组合物

    公开(公告)号：US05998368A

    公开(公告)日：1999-12-07

    申请号：US897624

    申请日：1997-07-21

    申请人： Illana Gozes ,  Matityahu Fridkin

    发明人： Illana Gozes ,  Matityahu Fridkin

    IPC分类号： A61K38/00 ,  A61P15/10 ,  C07K14/575 ,  C07K5/00 ,  C07K7/00

    CPC分类号： C07K14/57563 ,  A61K38/00

    摘要： There are provided novel compounds for the treatment of male impotence. The compounds are derived from vasoactive intestinal peptide (VIP) in which the natural amino acid sequence is modified by replacement of any of the 5, 17 and 19 amino acid residues by other natural or non-natural amino acids, and they bear at least one terminal lipophilic group.The modified VIP sequences are prepared by conventional peptide chain assembling methods.The novel compounds and compositions containing them are suitable for transdermal application for treating male impotence.

    摘要翻译： 提供了用于治疗男性阳provided的新型化合物。 该化合物衍生自血管活性肠肽（VIP），其中天然氨基酸序列被其他天然或非天然氨基酸替代5,17和19个氨基酸残基中的任何一个被修饰，并且它们至少具有一个 末端亲脂基团。 经修饰的VIP序列通过常规肽链组装方法制备。 含有它们的新化合物和组合物适用于经皮施用以治疗男性阳。。

    Anti-inflammatory peptides derived from C-reactive protein
    29.
    发明授权
    Anti-inflammatory peptides derived from C-reactive protein 失效
    衍生自C反应蛋白的抗炎肽

    公开(公告)号：US07182945B2

    公开(公告)日：2007-02-27

    申请号：US10373794

    申请日：2003-02-27

    申请人： Matityahu Fridkin ,  Eran Yavin

    发明人： Matityahu Fridkin ,  Eran Yavin

    IPC分类号： A61K38/43 ,  A61K38/00 ,  C12N9/50 ,  A01N37/18 ,  C07K1/00

    CPC分类号： C07K14/4737 ,  A61K38/00

    摘要： A peptide corresponding to positions 62–71 of the sequence of human C-reactive protein (CRP) of the formula: Glu62-Ile-Leu-Ile-Phe-Trp-Ser-Lys-Asp-Ile71 and modifications thereof obtained by substitution, deletion, or addition of amino acids, amidation of the C-terminal or acylation of the N-terminal, are capable of inhibiting in vitro the enzymatic activity of human Leukocyte Elastase (hLE) and/or of human Cathepsin G (hCG) and can be used for the treatment of chronic inflammation conditions such as rheumatoid arthritis, pulmonary emphysema, cystic fibrosis, bronchitis, asthma and some acute respiratory distress syndrome.

    摘要翻译： 对应于下式的人C反应蛋白（CRP）序列的第62-71位的肽：Glu 62 -Ile-Leu-Ile-Phe-Trp-Ser-Lys-Asp- Ile 71及其通过氨基酸的取代，缺失或添加获得的修饰，N-末端的C末端酰胺化或N-末端的酰化能够在体外抑制人白细胞的酶活性 弹性蛋白酶（hLE）和/或人类组织蛋白酶G（hCG），可用于治疗慢性炎症病症如类风湿性关节炎，肺气肿，囊性纤维化，支气管炎，哮喘和一些急性呼吸窘迫综合征。