Monocyclic L-nucleosides, analogs and uses thereof
    2.
    发明授权
    Monocyclic L-nucleosides, analogs and uses thereof 有权
    单环L-核苷类似物及其用途

    公开(公告)号:US06573248B2

    公开(公告)日:2003-06-03

    申请号:US09969355

    申请日:2001-12-31

    IPC分类号: A61K3170

    CPC分类号: C07H19/04

    摘要: Novel monocyclic L-Nucleoside compounds have the general formula Embodiments of these compounds are contemplated to be useful in treating a wide variety of diseases including infections, infestations, neoplasms, and autoimmune diseases. Viewed in terms of mechanism, embodiments of the novel compounds show immunomodulatory activity, and are expected to be useful in modulating the cytokine pattern, including modulation of Th1 and Th2 response.

    摘要翻译: 新型单环L-核苷化合物具有通式。这些化合物的实施方案被认为可用于治疗各种疾病,包括感染,感染,肿瘤和自身免疫性疾病。 从机理来看,新化合物的实施方案显示免疫调节活性,并且预期可用于调节细胞因子模式,包括Th1和Th2应答的调节。

    Cytokine related treatments of disease

    公开(公告)号:US06423695B1

    公开(公告)日:2002-07-23

    申请号:US09467443

    申请日:1999-12-20

    IPC分类号: A61K31675

    CPC分类号: A61K31/675

    摘要: Nucleosides and other compounds to selectively modulate Th1 and Th2 responses relative to each other in the treatment of disease. In one aspect of the invention, administration of a nucleoside or other compound reduces the dosage at which a primary drug is administered. In another aspect of the invention, an abnormality reflected in increased response in one group of cytokines is treated by administering a nucleoside or other compound that increases response in another group of cytokines. In yet another aspect of the invention, a patient is prophylactically treated by administering a nucleoside or other compound that selectively reduces Th1 activity without significantly reducing Th2 activity. In yet another aspect of the invention, a nucleoside or other compound is administered to a patient at a dose that reduces the patient's GTP pool to a degree that selectively reduces one of the Th1 or Th2 responses without significantly reducing the other response. Controlled release dosage forms are particularly contemplated to achieve that result.

    Moncyclic L-nucleosides analogs
    4.
    发明授权
    Moncyclic L-nucleosides analogs 有权
    单环L-核苷类似物

    公开(公告)号:US06552183B1

    公开(公告)日:2003-04-22

    申请号:US09633493

    申请日:2000-08-07

    IPC分类号: C07H19044

    CPC分类号: C07H19/04

    摘要: Novel monocyclic L-Nucleoside compounds have the general formula Embodiments of these compounds are contemplated to be useful in treating a wide variety of diseases including infections, infestations, neoplasms, and autoimmune diseases. Viewed in terms of mechanism, embodiments of the novel compounds show immunomodulatory activity, and are expected to be useful in modulating the cytokine pattern, including modulation of Th1 and Th2 response.

    摘要翻译: 新型单环L-核苷化合物具有通式。这些化合物的实施方案被认为可用于治疗各种疾病,包括感染,感染,肿瘤和自身免疫性疾病。 从机理来看,新化合物的实施方案显示免疫调节活性,并且预期可用于调节细胞因子模式,包括Th1和Th2应答的调节。

    Method of producing tiazofurin and other C-nucleosides
    5.
    发明授权
    Method of producing tiazofurin and other C-nucleosides 失效
    制备噻唑呋喃和其他C-核苷的方法

    公开(公告)号:US06613896B1

    公开(公告)日:2003-09-02

    申请号:US09445713

    申请日:2000-06-06

    IPC分类号: C07H706

    CPC分类号: C07D417/04 C07H9/02 C07H19/04

    摘要: C-nucleosides are synthesized by a method in which a sugar is derivatized in a single step to provide a heterocycle at the C1 position, and then the heterocycle is aromatized in another single step. In one class of preferred embodiments a cyano sugar is converted into thiocarboxamide, and subsequently condensed to form an azole ring. In a second class of preferred embodiments a cyano sugar is condensed with an amino acid to provide the azole ring. In a third class of preferred embodiments a halo sugar is condensed with a preformed heterocycle to provide the azole ring.

    摘要翻译: C-核苷通过其中糖在单一步骤中衍生化以在C1位置提供杂环的方法合成,然后在另一个单一步骤中使杂环芳构化。 在一类优选实施方案中,将氰基糖转化为硫代羧酰胺,随后冷凝以形成唑环。 在第二类优选实施方案中,将氰基糖与氨基酸缩合以提供唑环。 在第三类优选实施方案中,将卤糖与预先形成的杂环缩合以提供唑环。

    Nucleoside analogs with carboxamidine modified monocyclic base
    7.
    发明授权
    Nucleoside analogs with carboxamidine modified monocyclic base 有权
    具有甲脒改性单环碱的核苷类似物

    公开(公告)号:US07638496B2

    公开(公告)日:2009-12-29

    申请号:US10227235

    申请日:2002-08-22

    IPC分类号: A01N43/04 A61K31/70

    摘要: Novel nucleoside analog compounds are disclosed. The novel compounds or pharmaceutically acceptable esters or salts thereof may be used in pharmaceutical compositions, and such compositions may be used to treat an infection, an infestation, a neoplasm, or an autoimmune disease. The novel compounds may also be used to modulate aspects of the immune system, including modulation of Type 1 and Type 2 activity.

    摘要翻译: 公开了新的核苷类似物化合物。 新化合物或其药学上可接受的酯或其盐可以用于药物组合物中,并且这些组合物可用于治疗感染,感染,肿瘤或自身免疫性疾病。 新化合物也可用于调节免疫系统的方面,包括调节1型和2型活性。

    Multivalent salts of pyridostigmine and related compounds
    8.
    发明授权
    Multivalent salts of pyridostigmine and related compounds 有权
    吡斯的明和相关化合物的多价盐

    公开(公告)号:US06211201B1

    公开(公告)日:2001-04-03

    申请号:US09308723

    申请日:1999-06-29

    IPC分类号: A61K31444

    摘要: A quaternary ammonium cholinergic agent is complexed with a multivalent anion, or with multiple monovalent anions. The complex may be administered orally to a patient to treat pain, or for some other purpose. Numerous modifications are contemplated, including modifications to the ring structure of the compound, substitution and functionalization of the ring. Other contemplated modifications include the use of different anions, including various monovalent and polyvalent anions, and both organic and inorganic anions. The compounds have utility as cholinergic agents, and especially in the treatment of mysasthenia gravis, chest pain, and carpal tunnel syndrome.

    摘要翻译: 季铵胆碱能药剂与多价阴离子或多价单价阴离子络合。 复合物可以口服给予患者以治疗疼痛或用于其它目的。 考虑到许多修饰,包括化合物的环结构的修饰,环的取代和官能化。 其他预期的修改包括使用不同的阴离子,包括各种单价和多价阴离子,以及有机和无机阴离子。 该化合物具有胆碱能药物的功效,特别是治疗重症肌无力,胸痛和腕管综合症。

    Oligonucleotide analogs with an amino acid or a modified amino alcohol
residue
    10.
    发明授权
    Oligonucleotide analogs with an amino acid or a modified amino alcohol residue 失效
    具有氨基酸或修饰的氨基醇残基的寡核苷酸类似物

    公开(公告)号:US5969135A

    公开(公告)日:1999-10-19

    申请号:US551947

    申请日:1995-11-02

    摘要: The present invention provides various novel oligonucleotide analogs having one or more properties that make the subject compounds superior to conventional oligonucleotides for use in procedures employing oligonucleotides. The compounds of the invention are oligonucleotide analogs in which the furanose ring of a naturally occurring nucleic acid is replaced with an amino acid or a modified amino alcohol residue. Some embodiments of the novel compounds of the invention are particularly useful for the antisense control of gene expression. The compounds of the invention may also be used as nucleic acid hybridization probes or as primers. Another aspect of the invention is to provide monomeric precursors of the oligonucleotide analogs of the invention. These monomeric precursors may be used to synthesize the subject polynucleotide analogs. Another aspect of the invention is to provide formulations of the subject polynucleotide analogs that are designed for the treatment or prevention of disease conditions. Yet another aspect of the invention is to provide methods for treating or preventing diseases, particularly viral infections and cell growth disorders. The subject disease treatment methods comprise the step of administering an effective amount of the subject polynucleotide analogs for use as antisense inhibitors.

    摘要翻译: 本发明提供了具有使得本发明化合物优于常规寡核苷酸的一种或多种性质的各种新型寡核苷酸类似物,用于使用寡核苷酸的方法中。 本发明的化合物是其中天然存在的核酸的呋喃糖环被氨基酸或修饰的氨基醇残基替代的寡核苷酸类似物。 本发明的新化合物的一些实施方案对于基因表达的反义控制特别有用。 本发明的化合物也可以用作核酸杂交探针或引物。 本发明的另一方面是提供本发明的寡核苷酸类似物的单体前体。 这些单体前体可用于合成受试多核苷酸类似物。 本发明的另一方面是提供被设计用于治疗或预防疾病状况的受试多核苷酸类似物的制剂。 本发明的另一方面是提供用于治疗或预防疾病,特别是病毒感染和细胞生长障碍的方法。 受试者疾病治疗方法包括施用有效量的用作反义抑制剂的受试多核苷酸类似物的步骤。