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    Compounds
    82.
    发明申请
    Compounds 审中-公开
    化合物

    公开(公告)号：US20080103110A1

    公开(公告)日：2008-05-01

    申请号：US11662896

    申请日：2005-09-15

    申请人： Jo Klaveness ,  Bjarne Brudeli

    发明人： Jo Klaveness ,  Bjarne Brudeli

    IPC分类号： A61K31/7068 ,  A61P25/00 ,  A61P29/00 ,  A61P31/00 ,  A61P35/00 ,  C07H19/067

    CPC分类号： A61K47/555 ,  A61K47/542

    摘要： The invention provides a water-soluble prodrug compound comprising a therapeutically effective moiety coupled via a metabolically cleavable bond to a protein binding moiety, wherein said therapeutically effective moiety has an anticancer, antiinflammatory, antiinfective or antipain effect, said protein binding moiety binds non-covalently to blood proteins, and the protein binding of said compound is at least 100% higher than that of the therapeutically effective moiety itself, with the exclusion of (i) the monoester of gemcitabine with azelaic acid, (ii) the monoester of dideoxycytidine with 1,12-dodecanedicarboxylic acid, (iii) 2-amino-1,9-dihydro-9(2′-(1-(10-acetyl-decanoyloxy)ethoxymethyl))-guanine, (iv) 5′-cytarabine monoester with 1,4-phenylene diacetic acid, (v) the monoester of metronidazole with 1,4-butanedicarboxylic acid, and (vi) the monoester of metronidazole with 1,6-phenylene diacetic acid; and pre-prodrugs metabolizable thereto.

    摘要翻译： 本发明提供了一种水溶性前药化合物，其包含通过可代谢切割键与蛋白质结合部分相连的治疗有效部分，其中所述治疗有效部分具有抗癌，抗炎，抗感染或抗胰蛋白酶作用，所述蛋白质结合部分非共价结合 并且所述化合物的蛋白质结合比治疗有效部分本身的蛋白质结合至少高100％，排除（i）吉西他滨与壬二酸的单酯，（ii）双脱氧胞苷的单酯与1 ，12-十二烷二羧酸，（iii）2-氨基-1,9-二氢-9（2' - （1-（10-乙酰基 - 癸酰氧基）乙氧基甲基）） - 鸟嘌呤，（iv）5'-阿糖胞苷单酯与1 ，4-亚苯基二乙酸，（v）甲硝唑与1,4-丁烷二羧酸的单酯，和（vi）甲硝唑与1,6-亚苯基二乙酸的单酯; 和其可代谢的前药前药。

    COMPOUNDS AND METHODS FOR LOWERING THE ABUSE POTENTIAL AND EXTENDING THE DURATION OF ACTION OF A DRUG
    83.
    发明申请
    COMPOUNDS AND METHODS FOR LOWERING THE ABUSE POTENTIAL AND EXTENDING THE DURATION OF ACTION OF A DRUG 审中-公开
    降低滥用潜力并延长药物持续时间的化合物和方法

    公开(公告)号：US20070203165A1

    公开(公告)日：2007-08-30

    申请号：US11742566

    申请日：2007-04-30

    申请人： Jules Shafer ,  Vladislav Telyatnikov ,  Zhiwei Guo

    发明人： Jules Shafer ,  Vladislav Telyatnikov ,  Zhiwei Guo

    IPC分类号： A61K31/485 ,  C07D489/02

    CPC分类号： C07D489/08 ,  A61K47/555 ,  A61K47/60

    摘要： The abuse potential of a bioavailable drug such as an opiate analgesic agent is reduced and its duration of action is extended by converting it to a poorly absorbed ester prodrug or other prodrug derivative prior to formulation. Unlike many existing sustained release formulations of active pharmaceutical agents wherein an active pharmaceutical agent can be released by chewing, crushing, or otherwise breaking tablets or capsule beads containing the active pharmaceutical agent, such mechanical processing of tablets or capsule beads containing a prodrug of this invention neither releases the active drug nor compromises the controlled conversion of prodrug to drug. Moreover, tablets and capsule beads containing prodrugs of this invention or other drugs can be formulated with a sufficient amount of a thickening agent such as hydroxypropylmethylcellulose or carboxymethylcellulose to impede inappropriate intravenous and nasal administration of formulations that are not indicated for these modes of administration.

    摘要翻译： 降低生物可利用药物如鸦片止痛剂的滥用潜力，并且通过在制剂前将其转化为不良吸收的酯前药或其它前药衍生物来延长其作用时间。 与活性药物的许多现有持续释放制剂不同，其中通过咀嚼，破碎或以其它方式破坏含有活性药剂的片剂或胶囊珠可以释放活性药剂，这种包含本发明前药的片剂或胶囊珠粒的机械加工 既不释放活性药物也不妥协药物对药物的受控转化。 此外，含有本发明前药或其他药物的片剂和胶囊珠可以用足量的增稠剂如羟丙基甲基纤维素或羧甲基纤维素配制，以阻止对这些给药模式未注明的制剂的不适当的静脉内和鼻内施用。

    Amino acid and peptide conjugates of amiloride and methods of use thereof
    84.
    发明申请
    Amino acid and peptide conjugates of amiloride and methods of use thereof 有权
    阿米洛利的氨基酸和肽缀合物及其使用方法

    公开(公告)号：US20060160746A1

    公开(公告)日：2006-07-20

    申请号：US11040831

    申请日：2005-01-21

    申请人： Fredric Gorin ,  Michael Nantz

    发明人： Fredric Gorin ,  Michael Nantz

    IPC分类号： A61K38/06 ,  A61K38/05 ,  A61K38/04 ,  A61K31/497

    CPC分类号： C07K7/06 ,  A61K38/00 ,  A61K47/542 ,  A61K47/555 ,  A61K47/64

    摘要： The present invention provides compositions comprising amiloride amino acid and peptide conjugates. Efficient methods are also provided for administering the amiloride conjugates of the present invention for treating cancer or a central nervous system disease or disorder or for preventing or reducing ischemia-reperfusion injury. Further, kits are provided for the treatment of a central nervous system disease or disorder or for the prevention or reduction of ischemia-reperfusion injury using the amiloride conjugates of the present invention.

    摘要翻译： 本发明提供了包含阿米洛利氨基酸和肽缀合物的组合物。 还提供了有效的方法用于施用本发明的用于治疗癌症或中枢神经系统疾病或病症或用于预防或减少缺血再灌注损伤的阿米洛利共轭物。 此外，提供了用于治疗中枢神经系统疾病或病症或使用本发明的阿米洛利共轭物预防或减少缺血再灌注损伤的试剂盒。

    Beta-tubulin inhibitors
    86.
    发明申请
    Beta-tubulin inhibitors 审中-公开
    β-微管蛋白抑制剂

    公开(公告)号：US20050250853A1

    公开(公告)日：2005-11-10

    申请号：US11072334

    申请日：2005-03-07

    申请人： Rene Gaudreault ,  Jean Legault

    发明人： Rene Gaudreault ,  Jean Legault

    IPC分类号： A61K31/17 ,  G01N33/566

    CPC分类号： G01N33/566 ,  A61K31/17 ,  A61K47/542 ,  A61K47/555

    摘要： Disclosed herein are β-tubulin inhibitors of formula I, prodrugs thereof and therapeutically acceptable salts thereof, wherein R is selected from the group consisting of: t-butyl, i-propyl and sec-butyl and their use as anti-cancer cell proliferation agents.

    摘要翻译： 本文公开了式I的β-微管蛋白抑制剂，其前药和其治疗上可接受的盐，其中R选自：叔丁基，异丙基和仲丁基，以及它们作为抗癌细胞增殖剂的用途 。

    Mutant purine nucleoside phosphorylase proteins and cellular delivery thereof
    88.
    发明申请
    Mutant purine nucleoside phosphorylase proteins and cellular delivery thereof 有权
    突变型嘌呤核苷磷酸化酶蛋白及其细胞递送

    公开(公告)号：US20050214901A1

    公开(公告)日：2005-09-29

    申请号：US10493729

    申请日：2002-10-28

    申请人： Steven Ealick ,  William Parker ,  John Secrist III ,  Eric Sorscher

    发明人： Steven Ealick ,  William Parker ,  John Secrist III ,  Eric Sorscher

    IPC分类号： A61K47/48 ,  C07H19/16 ,  C07H19/20 ,  C07H21/04 ,  C12N1/21 ,  C12N9/10 ,  C12N9/22 ,  C12N15/74

    CPC分类号： C12N9/1077 ,  A61K47/555 ,  A61K47/67 ,  B82Y5/00 ,  C07H19/16 ,  C07H19/20 ,  C12Y204/02001

    摘要： A host cell stably transformed or transfected by a vector including a DNA sequence encoding for mutant purine nucleoside cleavage enzymes is provided. The transformed or transfected host cell can be used in combination with a purine substrate to treat tumour cells and/or virally infected cells. A nucleotide sequence encoding mutant E. coli derived purine nucleoside phosphorylase proteins which can be used in conjunction with an appropriate substrate to produce toxins which impair abnormal cell growth is also provided. A method is detailed for the delivery of toxin by generation withing target cells or by administration and delivery to the cells from without. Novel purine nucleosides are detailed that yield a cytotoxic purine upn enzymatic cleavage. A synthetic process for nucleosides is also detailed.

    摘要翻译： 提供了通过包含编码突变型嘌呤核苷切割酶的DNA序列的载体稳定转化或转染的宿主细胞。 转化或转染的宿主细胞可以与嘌呤底物组合使用以治疗肿瘤细胞和/或病毒感染的细胞。 还提供了编码突变大肠杆菌衍生的嘌呤核苷磷酸化酶蛋白的核苷酸序列，其可以与适当的底物结合使用以产生损害异常细胞生长的毒素。 详细说明了通过用靶细胞一代递送毒素或通过从没有给予和递送至细胞的方法。 详细介绍了新的嘌呤核苷，其产生细胞毒性嘌呤以进行酶裂解。 还详细介绍了核苷的合成过程。

    Melphalan prodrugs
    89.
    发明申请
    Melphalan prodrugs 审中-公开
    美法仑前药

    公开(公告)号：US20050214310A1

    公开(公告)日：2005-09-29

    申请号：US11043428

    申请日：2005-01-24

    申请人： Brian Toki ,  Peter Senter

    发明人： Brian Toki ,  Peter Senter

    IPC分类号： A61K39/395 ,  A61K39/40 ,  A61K39/42 ,  A61K39/44 ,  A61K47/48 ,  C12N9/00

    CPC分类号： B82Y5/00 ,  A61K47/555 ,  A61K47/60 ,  A61K47/6815 ,  A61K47/6899

    摘要： Shown and described are the synthesis of more potent forms of C-Mel, a prodrug used in Antibody-Directed Enzyme Prodrug Therapy, that releases the clinically used anticancer alkylating agent melphalan extracellularly. Shown and described are the synthesis of a variety of melphalan analogues with the intention to promote facile intracellular drug access. Esters, amides, and peptides of melphalan are shown. Cephalosporin prodrugs of the most interesting melphalan derivatives were synthesized and evaluated for potency, toxicity, therapeutic window, plasma stability, and solubility.

    摘要翻译： 显示和描述的是更有效形式的C-Mel的合成，C-Mel是用于抗体定向酶前药治疗的前药，其在细胞外释放临床使用的抗癌烷化剂美法仑。 显示和描述的是各种美法仑类似物的合成，其目的是促进细胞内药物进入。 显示了美法仑的酯，酰胺和肽。 合成了最令人感兴趣的美法仑衍生物的头孢菌素前药，并评价其效力，毒性，治疗窗口，血浆稳定性和溶解度。

    Method of modulating release of saccharides and uses thereof
    90.
    发明申请
    Method of modulating release of saccharides and uses thereof 审中-公开
    调节糖类释放的方法及其用途

    公开(公告)号：US20050070500A1

    公开(公告)日：2005-03-31

    申请号：US10498002

    申请日：2002-12-12

    申请人： Isabelle Boucher l ,  Serge Brunet

    发明人： Isabelle Boucher l ,  Serge Brunet

    IPC分类号： A61K31/702 ,  A61K31/726 ,  A61K31/728 ,  A61K31/737 ,  A61K47/48 ,  A61P19/00

    CPC分类号： A61K31/737 ,  A61K31/702 ,  A61K31/726 ,  A61K31/728 ,  A61K47/54 ,  A61K47/555 ,  A61K47/61

    摘要： The present invention relates to a method of controlled release of saccharides and oligosaccharides in human and animal. Polysaccharides are digested in a manner to provide oligomers having desired numbers of units of saccharides or monosaccharides, most particularly glucosamine and N-acetyl-glucosamine and derivatives thereof. The rate of release of monosaccharides is proportional to the length of the oligomers administered to an organism, and has targeted physiological effects depending on the length of the oligomers used.

    摘要翻译： 本发明涉及一种在人和动物中控制糖和寡糖的释放方法。 多糖以提供具有所需数量的糖或单糖单元的寡聚物的方式被消化，最特别是葡糖胺和N-乙酰基 - 葡糖胺及其衍生物。 单糖的释放速率与施用于生物体的寡聚体的长度成比例，并且具有取决于所用寡聚体的长度的生理效应。