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    Compositions and methods for the treatment of metabolic disorders
    4.
    发明授权
    Compositions and methods for the treatment of metabolic disorders 有权
    用于治疗代谢紊乱的组合物和方法

    公开(公告)号：US09522884B2

    公开(公告)日：2016-12-20

    申请号：US14399195

    申请日：2013-02-01

    申请人： CELLIXBIO PRIVATE LIMITED

    发明人： Mahesh Kandula

    IPC分类号： C07D213/66 ,  C07D409/12 ,  A61K31/44 ,  A61K47/48

    CPC分类号： C07D213/66 ,  A61K31/44 ,  A61K47/48038 ,  A61K47/48061 ,  A61K47/542 ,  A61K47/545 ,  C07D409/12

    摘要： The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for treating or preventing metabolic disorders may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be also used to the treatment of diabetes, lipid peroxidation, hypertriglyceridemia, metabolic disorders, free radical generated due to reactive oxygen and carbonyl groups, ionizing radiation, advanced glycation end products, kidney disease, renal complications and kidney stone disease.

    摘要翻译： 本发明涉及式I化合物或其药学上可接受的盐，以及其多晶型物，溶剂合物，对映体，立体异构体和水合物。 包含有效量的式I化合物的药物组合物，以及用于治疗或预防代谢紊乱的方法可以配制用于口服，口腔，直肠，局部，透皮，经粘膜，静脉内，肠胃外给药，糖浆或注射。 此类组合物也可用于治疗糖尿病，脂质过氧化，高甘油三酯血症，代谢紊乱，由于活性氧和羰基产生的自由基，电离辐射，晚期糖基化终产物，肾脏疾病，肾并发症和肾结石疾病。

    Means and methods of enhancing delivery to biological systems
    8.
    发明授权
    Means and methods of enhancing delivery to biological systems 有权
    增强对生物系统传播的手段和方法

    公开(公告)号：US09211340B2

    公开(公告)日：2015-12-15

    申请号：US12443236

    申请日：2007-09-26

    申请人： Paolo Botti

    发明人： Paolo Botti

    IPC分类号： A61K47/48

    CPC分类号： A61K47/48038 ,  A61K47/542 ,  A61K47/543 ,  A61K47/60 ,  C07K7/08

    摘要： This invention relates to a peptide or polypeptide (a) which is esterified or thio-esterified (i) at the carboxylate of the C-terminus with a guanidinium alkanol, a guanidinium alkanethiol, a PEG substituted with a guanidinium group and having a free hydroxyl group, or a PEG substituted with a guanidinium group and a sulfhydryl group; (ii) at a side-chain carboxylate of one or more Asp or GIu residues, if present, with a guanidinium alkanol, a guanidinium alkanethiol, a PEG substituted with a guanidinium group and having a free hydroxyl group, or a PEG substituted with a guanidinium group and a sulfhydryl group; (iii) at a hydroxyl group of one or more Ser, Thr or Tyr residues, if present, with a guanidinium alkanoic acid or a PEG substituted with a guanidinium group and a carboxyl group; (iv) at a sulfhydryl group of one or more Cys residues, if present, with a guanidinium alkanoic acid or a PEG substituted with a guanidinium group and a carboxyl group; and/or (v) at the N-terminus with a guanidinium alkanoic acid or a PEG substituted with a guanidinium group and a carboxyl group, wherein said N-terminus is previously amidated with an alpha- or beta-hydroxy acid, and wherein the ester is formed between the hydroxy group of said alpha- or beta-hydroxy acid and the carboxylic group of said guanidinium alkanoic acid or said PEG substituted with a guanidinium group and a carboxyl group; and/or (b) which contains one or more disulfides, the disulfide being formed between the sulfhydryl group of a Cys reside, if present, and a guanidinium alkanethiol or a PEG substituted with a guanidinium group and a sulfhydryl group.

    摘要翻译： 本发明涉及一种肽或多肽（a），其在C末端的羧酸酯上被酯化或硫酯化（i）与胍烷醇，胍链烷硫醇，被胍基取代并具有游离羟基的PEG 或被胍基和巯基取代的PEG; （ii）在一个或多个Asp或Glu残基的侧链羧酸酯上，如果存在的话，可以使用胍烷醇，胍烷硫醇，被胍基取代并具有游离羟基的PEG，或被 胍基和巯基; （iii）在一个或多个Ser，Thr或Tyr残基的羟基（如果存在）与链烷酸胍或被胍基和羧基取代的PEG的羟基; （iv）在一个或多个Cys残基的巯基（如果存在）与链烷酸胍或被胍基和羧基取代的PEG的巯基; 和/或（v）在N末端具有胍基链烷酸或被胍基和羧基取代的PEG，其中所述N-末端预先用α-或β-羟基酸酰胺化，并且其中 所述α-羟基酸或β-羟基酸的羟基与所述胍链烷酸的羧基或所述被胍基和羧基取代的PEG之间形成酯; 和/或（b）其中含有一个或多个二硫化物，在Cys的巯基之间形成的二硫键存在于烷基硫醇胍或被胍基和巯基取代的PEG之间。

    Fatty acid-salicylate conjugates with enhanced therapeutic properties
    9.
    发明授权
    Fatty acid-salicylate conjugates with enhanced therapeutic properties 有权
    具有增强治疗性能的脂肪酸 - 水杨酸酯缀合物

    公开(公告)号：US09056139B2

    公开(公告)日：2015-06-16

    申请号：US13929921

    申请日：2013-06-28

    申请人： KEAN UNIVERSITY

    发明人： Evros Vassiliou

    IPC分类号： A61K47/48

    CPC分类号： A61K47/48038 ,  A61K31/616 ,  A61K47/542

    摘要： The invention provides compositions and methods for treating or preventing cancer with an inventive composition. The invention relates to the fields of biomedicine, pharmacology, and molecular biology.

    摘要翻译： 本发明提供用本发明组合物治疗或预防癌症的组合物和方法。 本发明涉及生物医学，药理学和分子生物学领域。

    Conjugates for cancer therapy and diagnosis
    10.
    发明授权
    Conjugates for cancer therapy and diagnosis 有权
    用于癌症治疗和诊断的共轭物

    公开(公告)号：US08993278B2

    公开(公告)日：2015-03-31

    申请号：US13164204

    申请日：2011-06-20

    申请人： Stela Gengrinovitch ,  Esther Izakovich

    发明人： Stela Gengrinovitch ,  Esther Izakovich

    IPC分类号： C12P13/20 ,  C12P13/04 ,  C12P13/14 ,  G01N33/574 ,  A61P35/00 ,  A61K47/48

    CPC分类号： A61K47/48038 ,  A61K47/481 ,  A61K47/542 ,  A61K47/55

    摘要： The present invention relates to conjugates of a drug and an amino acid or an amino acid derivative or analog, pharmaceutical compositions that include the conjugates and methods of use thereof. In particular, the present invention relates to conjugates of anti-proliferative drugs and asparagine and glutamine and analogs thereof as compositions for treatment of cancer, and conjugates of imaging agent carriers and amino acids for the diagnosis of tumors and metastases.

    摘要翻译： 本发明涉及药物和氨基酸或氨基酸衍生物或类似物的缀合物，包括缀合物的药物组合物及其使用方法。 特别地，本发明涉及抗增殖药物和天冬酰胺和谷氨酰胺及其类似物作为治疗癌症的组合物的缀合物，以及用于诊断肿瘤和转移瘤的成像剂载体和氨基酸的缀合物。