SyK inhibitor | 1956296-96-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: SyK inhibitor
• 英文别名: (3Z)-3-[(1-methylindol-3-yl)methylidene]-2-oxo-1H-indole-5-sulfonamide
• CAS: 1956296-96-0
• 化学式: C₁₈H₁₅N₃O₃S
• 分子量: 353.401
• InChiKey: MLKHXLFEYOOYEY-NVNXTCNLSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  25
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.06
• 拓扑面积：
  103
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  2-氧代吲哚啉-5-磺酰氯 在 哌啶 、 ammonium hydroxide 作用下， 以 乙醇 为溶剂， 反应 20.0h， 生成 SyK inhibitor
  参考文献：
  名称：

  Potent small molecule inhibitors of spleen tyrosine kinase (Syk)

  摘要：

  A series of oxindoles demonstrating inhibition of the pbosphorylation of biotinylated substrates of Syk and IgE/FcepsilonRI triggered basophil cell degranulation has been identified. A study of the SAR around sulfonamide 31 (IC50=5 nM, EC50= 1400 nM) is discussed. The modest cellular activity representative of the sulfonamide series was overcome when the Polar surface Area was lowered to < 110 Angstrom(2), leading to the identification of amide 32 (IC50= 145 nM, EC50= 100 nM). (C) 2003 Published by Elsevier Ltd.

  DOI：

  10.1016/s0960-894x(03)00658-9

文献信息

• TREATMENT OF CANCERS HAVING RESISTANCE TO CHEMOTHERAPEUTIC AGENTS
  申请人：Wilhelm Scott

  公开号：US20100173954A1

  公开（公告）日：2010-07-08

  The present invention provides compositions and methods for treating cancer with DAST, 44-[3-(4-chloro-3-trifluoromethylphenyl)-ureido]-3-fluorophenoxy}-pyridine-2-carboxylic acid methylamide of the formula I, including all polymorphs, hydrates, pharmaceutically acceptable salts, metabolites, prodrugs, solvates or combinations thereof. Any cancer can be treated, including cancers that have acquired resistance to another therapeutic agent, such as kinase inhibitors. DAST can also be used to treat cancers which have become refractory to other chemotherapeutic agents

  本发明提供了使用DAST（44-[3-(4-氯-3-三氟甲基苯基)-尿素]-3-氟苯氧基}-吡啶-2-羧酸甲酰胺，I式），包括所有多晶形态、水合物、药学上可接受的盐、代谢物、前药、溶剂化合物或其组合物，治疗癌症的组合物和方法。可以治疗任何癌症，包括已经对其他治疗药物（如激酶抑制剂）产生耐药性的癌症。DAST还可用于治疗已经对其他化疗药物产生耐药性的癌症。
• SCREENING METHODS USING SYK IN COMBINATION WITH TAU PROTEIN
  申请人：PROTEOME SCIENCES PLC

  公开号：EP2441847A2

  公开（公告）日：2012-04-18

  The present invention provides materials and methods relating to screening for compounds useful in the treatment of Alzheimer's disease and related conditions. In particular, screening methods using tyrosine kinases are provided, as are methods relating to the role of tyrosine kinases as therapeutic targets.

  本发明提供了与筛选用于治疗阿尔茨海默病及相关疾病的化合物有关的材料和方法。特别是提供了使用酪氨酸激酶的筛选方法，以及与酪氨酸激酶作为治疗靶点的作用有关的方法。
• IgG stimulated remyelination of peripheral nerves
  申请人：Baxalta Incorporated

  公开号：US10494418B2

  公开（公告）日：2019-12-03

  The present invention is based on the discovery of polyclonal IgG's ability to promote Schwann cell maturation, differentiation, and myelin production. Methods for treating non-idiopathic, demyelinating peripheral neuropathies in mammals, where the neuropathy is not immune-mediated or infection-mediated, through the administration of polyclonal IgG are provided. Types of demyelinating peripheral neuropathies treatable with the present invention include peripheral nerve trauma and toxin-induced peripheral neuropathies. Alternatively, a composition of polyclonal IgGs can be applied directly to a peripheral nerve cell to induce maturation, differentiation into a myelinating state, and myelin expression or promote cell survival.

  本发明基于多克隆 IgG 能够促进许旺细胞成熟、分化和髓鞘生成的发现。本发明提供了通过施用多克隆 IgG 治疗哺乳动物非特发性脱髓鞘周围神经病的方法，其中神经病不是免疫介导或感染介导的。本发明可治疗的脱髓鞘性周围神经病包括周围神经创伤和毒素引起的周围神经病。另外，多克隆 IgG 组合物可直接应用于周围神经细胞，以诱导成熟、分化为髓鞘化状态、髓鞘表达或促进细胞存活。
• SCREENING METHODS USING C-ABL, FYN AND SYK IN COMBINATION WITH TAU PROTEIN
  申请人：PROTEOME SCIENCES PLC

  公开号：EP1794313A2

  公开（公告）日：2007-06-13
• IGG STIMULATED REMYELINATION OF PERIPHERAL NERVES
  申请人：Baxter International Inc

  公开号：EP2820042A2

  公开（公告）日：2015-01-07