LH-846抑制剂 | 639052-78-1

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: LH-846抑制剂
• 中文别名: N-(5-氯-6-甲基苯并[D]噻唑-2-基)-2-苯乙酰胺；N-(5-氯-6-甲基-2-苯并噻唑基)苯乙酰胺；CK1Δ抑制剂(LH846)
• 英文名称: N-(5-chloro-6-methyl-1,3-benzothiazol-2-yl)-2-phenylacetamide
• CAS: 639052-78-1
• 化学式: C₁₆H₁₃ClN₂OS
• 分子量: 316.8
• InChiKey: DYHAMRNAHTWYKY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.5
• 重原子数：
  21
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  70.2
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• Compounds for reducing c-Myc in c-Myc overexpressing cancers background
  申请人：The Trustees of Columbia University in the City of New York

  公开号：US10882863B2

  公开（公告）日：2021-01-05

  The invention relates to new compounds that reduce c-Myc expression and useful for cancer treatment, particularly hematological cancers such as aggressive B- and T-cell lymphomas. The new compounds may be combined with adjunct c-Myc inhibor agents such as a PI3K inhibitor, CK-1 inhibitor, Akt-inhibitor, proteasome inhibitor and/or mTor inhibitor. The c-Myc reducing agent may be provided as a lead-in treatment to reduce or initiate reduction of c-Myc prior to administration of the adjunct cancer therapeutic agent. Treatment with a c-Myc reducing agent modulates the disease state of the c-Myc overexpressing cancer making it less malignant and more susceptible to adjunctive cancer therapies.

  本发明涉及可降低 c-Myc 表达并可用于癌症治疗的新化合物，特别是血液肿瘤，如侵袭性 B 细胞和 T 细胞淋巴瘤。新化合物可与辅助性 c-Myc 抑制剂如 PI3K 抑制剂、CK-1 抑制剂、Akt-抑制剂、蛋白酶体抑制剂和/或 mTor 抑制剂结合使用。c-Myc还原剂可作为先导疗法，在使用辅助癌症治疗剂之前减少或开始减少c-Myc。使用c-Myc还原剂治疗可调节c-Myc过表达癌症的疾病状态，使其恶性程度降低，更容易接受辅助癌症疗法。
• Treatment of hearing loss by inhibition of casein kinase 1
  申请人：Massachusetts Eye & Ear Infirmary

  公开号：US11185536B2

  公开（公告）日：2021-11-30

  Methods for treating hearing loss that include administering an inhibitor, e.g., a small molecule inhibitor, of casein kinase 1, preferably in combination with a treatment that stimulates Atoh1 gene expression, e.g., a gamma-secretase inhibitor, an Atoh1 stimulatory compound, or a GSK-3-beta inhibitor.

  治疗听力损失的方法，包括施用酪蛋白激酶1的抑制剂，如小分子抑制剂，最好与刺激Atoh1基因表达的治疗剂，如γ-分泌酶抑制剂、Atoh1刺激化合物或GSK-3-beta抑制剂联合使用。
• Targeting Casein Kinase-1 and PI3K/AKT/mTOR Pathways for Treatment of c-Myc-Overexpressing Cancers, Organ Transplant Associated Complications and Autoimmune Diseases
  申请人：The Trustees of Columbia University in the City of New York

  公开号：US20190070183A1

  公开（公告）日：2019-03-07

  The invention relates to the co-administration of select proteasome and PI3K inhibitors is useful for treating c-Myc-overexpressing cancers, particularly hematological cancers such as aggressive B- and T-cell lymphomas. In exemplified embodiments, coadministration of a dual PI3K/CK-1 inhibitor with a proteasome inhibitor synergistically increases cell death of aggressive B- and T-cell lymphomas as well as multiple myeloma over the individual or additive effect of either or both agents. This synergistic effect is associated with the previously unknown inhibition of the kinase casein kinase 1 epsilon (CK-1ε) by a PI3K inhibitor, such as TGR-1202. Accordingly, use of PI3K inhibitors that possess CK-1ε inhibition in combination with proteasome inhibitors provides a new therapy regime for treating c-Myc-overexpressing cancers, and particularly hematological cancers.
• Compounds For Reducing c-Myc In c-Myc Overexpressing Cancers Background
  申请人：The Trustees of Columbia University in the City of New York

  公开号：US20190194212A1

  公开（公告）日：2019-06-27

  The invention relates to new compounds that reduce c-Myc expression and useful for cancer treatment, particularly hematological cancers such as aggressive B- and T-cell lymphomas. The new compounds may be combined with adjunct c-Myc inhibor agents such as a PI3K inhibitor, CK-1 inhibitor, Akt-inhibitor, proteasome inhibitor and/or mTor inhibitor. The c-Myc reducing agent may be provided as a lead-in treatment to reduce or initiate reduction of c-Myc prior to adminstration of the adjunct cancer therapeutic agent. Treatment with a c-Myc reducing agent modulates the disease state of the c-Myc overexpressing cancer making it less malignant and more susceptible to adjunctive cancer therapies.
• Treatment of Hearing Loss by Inhibition of Casein Kinase 1
  申请人：Massachusetts Eye & Ear Infirmary

  公开号：US20190247381A1

  公开（公告）日：2019-08-15

  Methods for treating hearing loss that include administering an inhibitor, e.g., a small molecule inhibitor, of casein kinase 1, preferably in combination with a treatment that stimulates Atoh1 gene expression, e.g., a gamma-secretase inhibitor, an Atoh1 stimulatory compound, or a GSK-3-beta inhibitor.