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    Water-soluble ursodeoxycholic acid prodrugs
    1.
    发明授权
    Water-soluble ursodeoxycholic acid prodrugs 有权
    水溶性熊去氧胆酸前药

    公开(公告)号：US09580459B2

    公开(公告)日：2017-02-28

    申请号：US14261963

    申请日：2014-04-25

    申请人： Metselex, Inc.

    发明人： Peter Ian Dosa ,  Clifford John Steer ,  Ingrid Gunda Georg

    IPC分类号： C07J51/00

    CPC分类号： C07J51/00

    摘要： Ursodeoxycholic acid (UDCA) is a bile acid with demonstrated anti-apoptotic activity in both in vitro and in vivo models. Water-soluble prodrugs of UDCA for use in indications where intravenous administration of UDCA may be preferable, such as reducing damage from stroke or acute kidney injury, are disclosed. The disclosed prodrugs showed significant anti-apoptotic activity in a series of in vitro assays.

    摘要翻译： 熊去氧胆酸（UDCA）是一种在体外和体内模型中都具有抗凋亡活性的胆汁酸。 公开了用于UDCA的静脉内给药可能是优选的适应症的UDCA的水溶性前药，例如减轻中风或急性肾损伤的损伤。 所公开的前药在一系列体外测定中显示出显着的抗细胞凋亡活性。

    PREVENTION AND TREATMENT OF KIDNEY DAMAGE
    8.
    发明申请
    PREVENTION AND TREATMENT OF KIDNEY DAMAGE 审中-公开
    防治和治疗KIDNEY损害

    公开(公告)号：US20160051567A1

    公开(公告)日：2016-02-25

    申请号：US14780288

    申请日：2014-03-27

    申请人： METSELEX, INC.

    发明人： Clifford STEER ,  Sandeep GUPTA

    IPC分类号： A61K31/575 ,  A61K9/00

    CPC分类号： A61K31/575 ,  A61K9/0019

    摘要： A method of treating or preventing kidney injury includes administering to a patient an effective amount of bile acid, a salt thereof, an analog thereof, or a combination thereof. Methods of preventing or retarding, reversing or abolishing the onset of kidney injuries are discussed. This is achieved through the administration of a bile acid, a salt of the bile acid, an analog of the bile acid or any combinations of these compounds. The bile acid abolishes or interferes or down-regulates metabolic pathways leading to the onset of kidney injury. The bile acid also activates metabolic pathways leading to the slowing or reversing or complete abolishment of the progression of acute kidney injury.

    摘要翻译： 治疗或预防肾损伤的方法包括向患者施用有效量的胆汁酸，其盐，其类似物或其组合。 讨论了预防或阻滞，逆转或消除肾损伤发作的方法。 这通过施用胆汁酸，胆汁酸的盐，胆汁酸的类似物或这些化合物的任何组合来实现。 胆汁酸消除或干扰或下调导致肾损伤发作的代谢途径。 胆汁酸还能激活代谢途径，导致急性肾损伤进展的减缓或逆转或完全消退。

    PREVENTION OR ATTENUATION OF NEUROPATHIC PAIN AND KIDNEY INJURY BY TAUROURSODEOXYCHOLIC ACID
    9.
    发明申请
    PREVENTION OR ATTENUATION OF NEUROPATHIC PAIN AND KIDNEY INJURY BY TAUROURSODEOXYCHOLIC ACID 有权
    神经病性疼痛预防或衰竭及龋齿损伤

    公开(公告)号：US20140296194A1

    公开(公告)日：2014-10-02

    申请号：US14355759

    申请日：2012-11-01

    申请人： Metselex, Inc.

    发明人： Mai Lan Leong ,  Clifford Steer ,  Martin Wessendorf

    IPC分类号： A61K31/575 ,  G01N33/50 ,  A61B5/00 ,  A61K31/573

    CPC分类号： G01N33/5058 ,  A61B5/4827 ,  A61K31/573 ,  A61K31/575 ,  A61K2300/00

    摘要： Methods of reducing or abolishing neuropathic pain in humans and animals are discussed. In some examples administration of the apoptosis inhibitor taurours-odeoxycholic acid (TUDCA), greatly reduced both neuronal loss and the increase in glia, and partially reversed spinal nerve ligation (SNL)-induced mechanical hypersensitivity. Among RVM neurons, serotonergic (5-HT) neurons decreased by 35% ipsilateral to SNL. In some examples, the density of 5-HT immunoreactive varicosities in the superficial dorsal horn of the spinal cord was lower ipsilateral to SNL. The RVM 5-HT neurons that remained after SNL appeared to facilitate nociception. When rats that had undergone SNL were treated with the 5-HT neurotoxin, 5,7-dihydroxytryptamine (5,7-DHT), mechanical withdrawal thresholds increased significantly. In some examples nerve injury induces death of antinociceptive RVM neurons which can be reduced or abolished by TUDCA. In some examples, that the loss of RVM neurons shifts the balance of descending control from pain inhibition to pain facilitation.

    摘要翻译： 讨论减少或消除人类和动物神经性疼痛的方法。 在一些实施例中，细胞凋亡抑制剂牛磺酸脱氧胆酸（TUDCA）的给药大大降低了神经元损失和神经胶质增加，部分逆转脊髓神经结扎（SNL）诱导机械超敏反应。 在RVM神经元中，血清素能（5-HT）神经元与SNL同侧减少35％。 在一些实例中，脊髓浅表背角中5-HT免疫反应性静脉曲张的密度与SNL同侧较低。 在SNL后保留的RVM 5-HT神经元似乎促进伤害感受。 用5-HT神经毒素5,7-二羟基色胺（5,7-DHT）处理经历SNL的大鼠，机械戒断阈值显着增加。 在一些例子中，神经损伤引起可由TUDCA减少或消除的抗伤害感受性RVM神经元的死亡。 在一些例子中，RVM神经元的损失将降低控制的平衡从疼痛抑制转移到疼痛促进。