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598 条记录 (耗时 0.029 秒)

    Compounds and methods for treatment of solid tumors
    22.
    发明授权
    Compounds and methods for treatment of solid tumors 失效
    用于治疗实体瘤的化合物和方法

    公开(公告)号：US08778892B2

    公开(公告)日：2014-07-15

    申请号：US12381914

    申请日：2009-03-18

    申请人： Donald L. Barbeau

    发明人： Donald L. Barbeau

    IPC分类号： A01N43/04 ,  A61K31/70 ,  C07H1/00 ,  C08B37/00 ,  A61K31/715 ,  A61K31/7042 ,  C07H5/04 ,  C08B37/08

    CPC分类号： A61K31/715 ,  A61K31/7042 ,  C07H5/04 ,  C08B37/0063 ,  C08B37/0072

    摘要： The present invention relates to pharmaceutical compositions containing targetable bioconjugates of hydralazine, a direct vasodilating agent previously shown to decrease tumor blood flow, oxygenation and interstitial fluid pressure in solid tumors. These bioconjugates are hydralazine prodrugs that contain hydralazine conjugated to biocompatible carrier molecules which specifically bind to sites that are expressed on a diverse variety of tumor cell types. These hydralazine prodrugs are preferably conjugated through an acid-labile hydrazone link that is designed to be stable in plasma and release hydralazine through acid-catalyzed hydrolysis in the acidic environment of the target tumor. Because these prodrugs are stable at physiological pH and in plasma, they are devoid of systemic vasoactive activity; however, they are acid-labile conjugates that can be hydrolyzed upon reaching the more acid environment of the tumor where the vasoactive activity of hydralazine is restored. These prodrugs selectively bind to tumor-specific receptors on tumor cells, and are degraded in the acidic tumor cell environment or the acidic lysosomal compartments after being internalized into the cell.

    摘要翻译： 本发明涉及包含可屈曲的肼屈嗪生物缀合物的药物组合物，其是先前显示的减少肿瘤血流量的直接血管舒张剂，实体瘤中的氧合和间质液压。 这些生物缀合物是含有与生物相容性载体分子结合的肼屈嗪的肼苯拉嗪前药，其特异性结合于在多种肿瘤细胞类型上表达的位点。 这些肼屈嗪前药优选通过设计为在血浆中稳定并且在靶肿瘤的酸性环境中通过酸催化水解释放肼屈嗪的酸不稳定的腙连接物缀合。 因为这些前药在生理pH和血浆中是稳定的，所以它们没有全身血管活性; 然而，它们是酸不稳定的缀合物，其可以在到达愈合肼屈嗪的血管活性恢复的肿瘤的更酸性环境时被水解。 这些前药选择性地结合肿瘤细胞上的肿瘤特异性受体，并且在被内化到细胞中之后在酸性肿瘤细胞环境或酸性溶酶体隔室中降解。

    Glycosylated chlorambucil analogs and uses thereof
    26.
    发明授权
    Glycosylated chlorambucil analogs and uses thereof 有权
    糖基化的苯丁酸氮芥类似物及其用途

    公开(公告)号：US08552176B2

    公开(公告)日：2013-10-08

    申请号：US13274814

    申请日：2011-10-17

    申请人： Jon S. Thorson ,  Randal D. Goff

    发明人： Jon S. Thorson ,  Randal D. Goff

    IPC分类号： C07H5/04 ,  C40B40/12

    CPC分类号： C07H15/18 ,  C40B40/12

    摘要： A library of glycosylated chlorambucil analogs which are useful as anti-tumor and/or anti-metastatic agents is disclosed. The glycosylated chlorambucil analogs have the general formula wherein represents a reducing sugar moiety.

    摘要翻译： 公开了可用作抗肿瘤和/或抗转移剂的糖基化的苯丁酸氮芥类似物文库。 糖基化的苯丁酸氮芥类似物具有通式，其中代表还原糖部分。

    Therapeutic agent for pain disease
    29.
    发明授权
    Therapeutic agent for pain disease 有权
    疼痛病治疗剂

    公开(公告)号：US08492350B2

    公开(公告)日：2013-07-23

    申请号：US12449152

    申请日：2008-02-06

    申请人： Yoshitaka Nakazawa

    发明人： Yoshitaka Nakazawa

    IPC分类号： A61K31/70 ,  C07H5/04 ,  C07H5/06 ,  C08B37/00 ,  A01N43/04

    CPC分类号： A61K31/7012 ,  C07H7/027

    摘要： A method for treating neuropathic pain by administering a pharmaceutical preparation containing N-acetylneuraminic acid or a pharmaceutically acceptable salt thereof to a person in need of treatment of neuropathic pain. Examples of neuropathic pain include trigeminal neuralgia, postherpetic neuralgia, strangulated neuropathy, complex regional pain syndrome (CRPS), diabetic neuropathy, neuropathy caused by trauma, phantom limb pain, central pain, and neuropathic pain caused by drug therapy or radiation therapy.

    摘要翻译： 一种通过向需要治疗神经性疼痛的人施用含有N-乙酰神经氨酸或其药学上可接受的盐的药物制剂来治疗神经性疼痛的方法。 神经性疼痛的例子包括三叉神经痛，带状疱疹后神经痛，窒息性神经病变，复杂区域性疼痛综合征（CRPS），糖尿病性神经病变，由创伤引起的神经病变，幻肢疼痛，中枢性疼痛和药物治疗或放射治疗引起的神经性疼痛。

    Carbohydrate conjugates as delivery agents for oligonucleotides
    30.
    发明授权
    Carbohydrate conjugates as delivery agents for oligonucleotides 有权
    碳水化合物缀合物作为寡核苷酸的递送剂

    公开(公告)号：US08450467B2

    公开(公告)日：2013-05-28

    申请号：US13326203

    申请日：2011-12-14

    申请人： Muthiah Manoharan ,  Kallanthottathil G. Rajeev ,  Narayanannair K. Jayaprakash ,  Martin Maier

    发明人： Muthiah Manoharan ,  Kallanthottathil G. Rajeev ,  Narayanannair K. Jayaprakash ,  Martin Maier

    IPC分类号： C07H5/04 ,  C07H5/06 ,  C08B37/00

    CPC分类号： A61K47/28 ,  A61K31/70 ,  A61K31/7004 ,  A61K31/7052 ,  A61K31/7088 ,  A61K31/713 ,  A61K47/16 ,  A61K47/22 ,  A61K47/543 ,  A61K47/549 ,  A61K47/60 ,  A61K48/00 ,  C07H21/02 ,  Y02A50/385 ,  Y02A50/411 ,  Y02A50/467 ,  Y02P20/55

    摘要： The present invention provides iRNA agents comprising at least one subunit of the formula (I): wherein: A and B are each independently for each occurrence O, N(RN) or S; X and Y are each independently for each occurrence H, OH, a hydroxyl protecting group, a phosphate group, a phosphodiester group, an activated phosphate group, an activated phosphite group, a phosphoramidite, a solid support, —P(Z′)(Z″)O-nucleoside, —P(Z′)(Z″)O-oligonucleotide, a lipid, a PEG, a steroid, a lipophile, a polymer, —P(Z′)(Z″)O-Linker-OP(Z′″)(Z″″)O-oligonucleotide, a nucleotide, an oligonucleotide, —P(Z′)(Z″)-formula (I), —P(Z′)(Z″)— or -Linker-R; R is LG, -Linker-LG, or has the structure shown below: LG is independently for each occurrence a carbohydrate, e.g., monosaccharide, disaccharide, trisaccharide, tetrasaccharide, oligosaccharide, polysaccharide; RN is independently for each occurrence H, methyl, ethyl, propyl, isopropyl, butyl, or benzyl; and Z′, Z″, Z′″ and Z″″ are each independently for each occurrence O or S.

    摘要翻译： 本发明提供包含至少一个式（I）亚基的iRNA试剂：其中：A和B各自独立地为O，N（RN）或S; X和Y各自独立地为H，OH，羟基保护基，磷酸基，磷酸二酯基，活化磷酸酯基，活化亚磷酸酯基，亚磷酰胺，固体载体，-P（Z'）（ Z'）（Z“）O - 寡核苷酸，脂质，PEG，类固醇，亲脂体，聚合物，-P（Z'）（Z”）O （Z'）（Z“） - （Z”）（Z“）（Z”）（Z“）（Z”） （Z“） - 或-Linker-R; R是LG，-Linker-LG，或具有如下结构：每次出现LG独立为碳水化合物，例如单糖，二糖，三糖，四糖，寡糖，多糖; 乙烯基，丙基，异丙基，丁基或苄基各自独立地为N， Z'，Z“，Z”“和Z”“各自独立地为O或S.