Sphingosine-1-phosphate essentially free of L-threo isomer
    1.
    发明授权
    Sphingosine-1-phosphate essentially free of L-threo isomer 失效
    基本上不含L-苏式异构体的鞘氨醇-1-磷酸

    公开(公告)号:US5663404A

    公开(公告)日:1997-09-02

    申请号:US371866

    申请日:1995-01-12

    摘要: A method of inhibiting tumor cell chemotactic and/or chemoinvasion motility comprising contacting the tumor cell with an inhibitory amount of an agent selected from the group consisting of sphingosine-1-phosphate, derivatives of sphingosine-1-phosphate and mimetics of the sphingosine-1-phosphate or of the derivatives. A method of inhibiting phagokinetic activity of tumor cells and neutrophils comprising contacting the cells with a phagokinetic inhibitory amount of an agent selected from the group consisting of sphingosine-1-phosphate, derivatives of sphingosine-1-phosphate, and mimetics of the sphingosine-1-phosphate or of the derivatives. A method of inhibiting tumor cell metastasis comprising administering to a host in need of treatment a metastasis inhibitory amount of an agent selected from the group consisting of sphingosine-1-phosphate, derivatives of sphingosine-1-phosphate, and mimetics of the sphingosine-1-phosphate or of the derivatives, and pharmaceutically acceptable salts of the agent. A method of inhibiting inflammation due to motility and invasion into blood vessel walls of neutrophils comprising administering to a host in need of treatment an inflammation inhibitory amount of an agent selected from the group consisting of sphingosine-1-phosphate, derivatives of sphingosine-1-phosphate, and mimetics of the sphingosine-1-phosphate or of the derivatives, and pharmaceutically acceptable salts of the agent. A method of preparing sphingosine-1-phosphate and its derivatives.

    摘要翻译: 一种抑制肿瘤细胞趋化性和/或化学侵袭运动性的方法,包括使肿瘤细胞与抑制量的选自鞘氨醇-1-磷酸的鞘氨醇-1-磷酸,鞘氨醇-1-磷酸的衍生物和鞘氨醇-1的模拟物 磷酸盐或衍生物。 一种抑制肿瘤细胞和嗜中性粒细胞的吞噬作用的方法包括使细胞与吞噬动力学抑制量的选自鞘氨醇-1-磷酸的鞘氨醇-1-磷酸,鞘氨醇-1-磷酸的衍生物和鞘氨醇-1的模拟物 磷酸盐或衍生物。 一种抑制肿瘤细胞转移的方法,包括向需要治疗的宿主施用转移抑制量的选自鞘氨醇-1-磷酸的鞘氨醇-1-磷酸,鞘氨醇-1-磷酸的衍生物和鞘氨醇-1的模拟物 磷酸盐或其衍生物,以及药学上可接受的盐。 抑制由于运动性而侵入嗜中性粒细胞的血管壁的炎症的方法,包括对需要治疗的宿主施用炎症抑制量的选自鞘氨醇-1-磷酸的鞘氨醇-1-磷酸,鞘氨醇-1-磷酸的衍生物, 磷酸盐,以及鞘氨醇-1-磷酸酯或衍生物的模拟物,以及药物的药学上可接受的盐。 鞘氨醇-1-磷酸及其衍生物的制备方法。

    Method for inhibition of cell motility by sphingosine-1-phosphate, its
derivatives and mimetics and method of synthesizing
sphingosine-1-phosphate and its derivatives
    2.
    发明授权
    Method for inhibition of cell motility by sphingosine-1-phosphate, its derivatives and mimetics and method of synthesizing sphingosine-1-phosphate and its derivatives 失效
    鞘氨醇-1-磷酸及其衍生物和模拟物抑制细胞运动性的方法及合成鞘氨醇-1-磷酸酯及其衍生物的方法

    公开(公告)号:US5391800A

    公开(公告)日:1995-02-21

    申请号:US104504

    申请日:1993-08-09

    摘要: A method of inhibiting tumor cell chemotactic and/or chemoinvasion motility comprising contacting the tumor cell with an inhibitory amount of an agent selected from the group consisting of sphingosine-1-phosphate, derivatives of sphingosine-1-phosphate and mimetics of the sphingosine-1-phosphate or of the derivatives. A method of inhibiting phagokinetic activity of tumor cells and neutrophils comprising contacting the cells with a phagokinetic inhibitory amount of an agent selected from the group consisting of sphingosine-1-phosphate, derivatives of sphingosine-1-phosphate, and mimetics of the sphingosine-1-phosphate or of the derivatives. A method of inhibiting tumor cell metastasis comprising administering to a host in need of treatment a metastasis inhibitory amount of an agent selected from the group consisting of sphingosine-1-phosphate, derivatives of sphingosine-1-phosphate, and mimetics of the sphingosine-1-phosphate or of the derivatives, and pharmaceutically acceptable salts of the agent. A method of inhibiting inflammation due to motility and invasion into blood vessel walls of neutrophils comprising administering to a host in need of treatment an inflammation inhibitory amount of an agent selected from the group consisting of sphingosine-1-phosphate, derivatives of sphingosine-1-phosphate, and mimetics of the sphingosine-1-phosphate or of the derivatives, and pharmaceutically acceptable salts of the agent. A method of preparing sphingosine-1-phosphate and its derivatives.

    摘要翻译: 一种抑制肿瘤细胞趋化性和/或化学侵袭运动性的方法,包括使肿瘤细胞与抑制量的选自鞘氨醇-1-磷酸的鞘氨醇-1-磷酸,鞘氨醇-1-磷酸的衍生物和鞘氨醇-1的模拟物 磷酸盐或衍生物。 一种抑制肿瘤细胞和嗜中性粒细胞的吞噬作用的方法包括使细胞与吞噬动力学抑制量的选自鞘氨醇-1-磷酸的鞘氨醇-1-磷酸,鞘氨醇-1-磷酸的衍生物和鞘氨醇-1的模拟物 磷酸盐或衍生物。 一种抑制肿瘤细胞转移的方法,包括向需要治疗的宿主施用转移抑制量的选自鞘氨醇-1-磷酸的鞘氨醇-1-磷酸,鞘氨醇-1-磷酸的衍生物和鞘氨醇-1的模拟物 磷酸盐或其衍生物,以及药学上可接受的盐。 抑制由于运动性而侵入嗜中性粒细胞的血管壁的炎症的方法,包括对需要治疗的宿主施用炎症抑制量的选自鞘氨醇-1-磷酸的鞘氨醇-1-磷酸,鞘氨醇-1-磷酸的衍生物, 磷酸盐,以及鞘氨醇-1-磷酸酯或衍生物的模拟物,以及药剂的药学上可接受的盐。 鞘氨醇-1-磷酸及其衍生物的制备方法。

    HETEROCYCLIC COMPOUNDS AND USES THEREOF
    4.
    发明申请

    公开(公告)号:US20190308963A1

    公开(公告)日:2019-10-10

    申请号:US16375828

    申请日:2019-04-04

    申请人: Fuqiang Ruan

    发明人: Fuqiang Ruan

    摘要: In recognition of the unmet need to develop novel therapeutic agents, the present invention discloses a novel class of heterocycles as dual inhibitors of BRD4 and class I PI3Ks. The compounds claimed herein could be used alone or in combination therapies for the effective treatment of a wide range of age-related diseases, including cancer. The present invention also provides methods for preparing compounds of the invention thereto.

    Compositions and methods for treating or preventing hypoxic or ischemic injury
    8.
    发明授权
    Compositions and methods for treating or preventing hypoxic or ischemic injury 失效
    用于治疗或预防缺氧或缺血性损伤的组合物和方法

    公开(公告)号:US08202997B2

    公开(公告)日:2012-06-19

    申请号:US12580458

    申请日:2009-10-16

    摘要: A method for treating or preventing injury of a biological material exposed to hypoxic or ischemic conditions comprising contacting the biological material with an effective amount of a compound is disclosed. The compound has the following structure (I): R1—(S)n—R2   (I) or a stereoisomer, pharmaceutically acceptable salt or prodrug thereof, wherein R1, R2, and n are as defined herein. Compounds, methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

    摘要翻译: 公开了一种治疗或预​​防暴露于缺氧或缺血状况的生物材料损伤的方法,包括使生物材料与有效量的化合物接触。 化合物具有以下结构(I):R1-(S)n-R2(I)或其立体异构体,药学上可接受的盐或前药,其中R 1,R 2和n如本文所定义。 还公开了与制备和使用这些化合物有关的化合物,与包含这些化合物的药物组合物相关的方法。