1-(1H-benzimidazol-5-yl)-5-(1,1'-biphenyl-4-yl)imidazolidine-2,4-dione | 1215088-78-0

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 1-(1H-benzimidazol-5-yl)-5-(1,1'-biphenyl-4-yl)imidazolidine-2,4-dione
• 英文别名: 1-(3H-benzimidazol-5-yl)-5-(4-phenylphenyl)imidazolidine-2,4-dione
• CAS: 1215088-78-0
• 化学式: C₂₂H₁₆N₄O₂
• 分子量: 368.395
• InChiKey: HEXVNBQITIFOKU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  28
• 可旋转键数：
  3
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.05
• 拓扑面积：
  78.1
• 氢给体数：
  2
• 氢受体数：
  3

文献信息

• NOVEL INHIBITORS OF GLUTAMINYL CYCLASE
  申请人：Heiser Ulrich

  公开号：US20100119475A1

  公开（公告）日：2010-05-13

  Compounds of general formula (I): wherein R 1 , R 2 , R 3 , R 4 , X and Y are as defined herein are inhibitors of glutaminyl cyclase and are therefore useful in treating conditions that can be treated by modulation of glutaminyl cyclase activity.

  通式(I)的化合物：其中R1、R2、R3、R4、X和Y的定义如本文所述，是谷氨酰环化酶的抑制剂，因此可用于治疗可通过调节谷氨酰环化酶活性来治疗的疾病。
• USE OF ISOQC INHIBITORS
  申请人：Demuth Hans-Ulrich

  公开号：US20100125086A1

  公开（公告）日：2010-05-20

  The present invention relates in general to an inhibitor of a glutaminyl peptide cyclotransferase-like protein (QPCTL), and the use thereof for the treatment and/or prevention of an inflammatory disease or disorder selected from the group consisting of (a) chronic and acute inflammations, e.g. rheumatoid arthritis, atherosclerosis, restenosis, pancreatitis; (b) other inflammatory diseases, e.g. neuropathic pain, graft rejection/graft failure/graft vasculopathy, HIV infections/AIDS, gestosis, tuberous sclerosis, Guillain-Barré syndrome, chronic inflammatory demyelinising polyradiculoneuropathy and multiple sclerosis; (c) neuroinflammation; and (d) neurodegenerative diseases, e.g. mild cognitive impairment (MCI), Alzheimer's disease, neurodegeneration in Down Syndrome, Familial British Dementia, and Familial Danish Dementia, which may result from neuroinflammation.

  本发明涉及一种谷氨酰肽环转移酶类似蛋白（QPCTL）的抑制剂及其用于治疗和/或预防从以下疾病或障碍中选择的炎症性疾病或障碍的使用：（a）慢性和急性炎症，例如类风湿性关节炎，动脉硬化，再狭窄，胰腺炎；（b）其他炎症性疾病，例如神经病性疼痛，移植排斥/移植失败/移植血管病，HIV感染/艾滋病，妊娠高血压综合症，结节性硬化，格林-巴利综合症，慢性炎性脱髓鞘性多发性神经根神经病和多发性硬化症；（c）神经炎症；以及（d）神经退行性疾病，例如轻度认知障碍（MCI），阿尔茨海默病，唐氏综合症中的神经退行性变，英国家族痴呆症和丹麦家族痴呆症，这些疾病可能是由神经炎症引起的。
• TREATING PATHOLOGICAL CONDITIONS BY DIRECT AND INDIRECT TARGETING OF SIRPA - CD47 INTERACTION
  申请人：Stichting Het Nederlands Kanker Instituut- Antoni van Leeuwenhoek Ziekenhuis

  公开号：EP3747438A1

  公开（公告）日：2020-12-09

  The present invention relates to active agents or compounds as well as pharmaceutical compositions comprising said compounds, which are capable of reducing or inhibiting or blocking the enzymatic activity of the glutaminyl-peptide cyclotransferase (QPCT) protein, the glutaminyl-peptide cyclotransferase-like protein (QPCTL) protein, or combinations thereof or are capable of reducing or inhibiting the expression of QPCT gene, the QPCTL gene, or combinations thereof. Also provided are methods for screening or selecting for said compounds. The present invention further relates to a pharmaceutical composition comprising a first active agent for use in a method of treating a condition in a subject that would benefit from reducing the signaling or the binding between SIRPa and CD47 in the subject (e.g. cancer), wherein the method of treating comprises reducing expression or enzymatic activity of QPCTL, QPCT, or combinations thereof in the cell with CD47 on the surface. The compounds and pharmaceutical compositions of the invention may be particularly useful for treating a subject suffering from a disease or condition involving the CD47-SIRPa signaling axis such including e.g., various cancer types, atherosclerosis, fibrotic diseases, and infectious diseases.

  本发明涉及活性剂或化合物以及包含所述化合物的药物组合物，它们能够降低或抑制或阻断谷氨酰胺酰肽环转酶（QPCT）蛋白、谷氨酰胺酰肽环转酶样蛋白（QPCTL）蛋白或其组合的酶活性，或者能够降低或抑制QPCT基因、QPCTL基因或其组合的表达。还提供了筛选或选择所述化合物的方法。本发明进一步涉及一种药物组合物，该药物组合物包含第一活性剂，用于治疗受试者（如癌症）中可从减少SIRPa和CD47之间的信号转导或结合中获益的病症的方法，其中治疗方法包括减少表面有CD47的细胞中QPCTL、QPCT或其组合的表达或酶活性。本发明的化合物和药物组合物可能特别适用于治疗患有涉及 CD47-SIRPa 信号轴的疾病或病症的受试者，例如包括各种癌症类型、动脉粥样硬化、纤维化疾病和传染性疾病。
• NOVEL INHIBITORS
  申请人：Probiodrug AG

  公开号：EP2344157B1

  公开（公告）日：2016-05-25
• Use of isoQC inhibitors
  申请人：Probiodrug AG

  公开号：EP2344158A1

  公开（公告）日：2011-07-20