4-[4-(3-Oxo-3,5-dihydro-pyrazolo[4,3-c]quinolin-2-yl)-phenylcarbamoyl]-2-phenyl-butyric acid | 486449-42-7

• 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: 4-[4-(3-Oxo-3,5-dihydro-pyrazolo[4,3-c]quinolin-2-yl)-phenylcarbamoyl]-2-phenyl-butyric acid
• CAS: 486449-42-7
• 化学式: C₂₇H₂₂N₄O₄
• 分子量: 466.496
• InChiKey: MPFRAXWBRTUADJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.41
• 重原子数：
  35.0
• 可旋转键数：
  7.0
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.11
• 拓扑面积：
  117.08
• 氢给体数：
  3.0
• 氢受体数：
  5.0

文献信息

• Novel immunomodulating compounds
  申请人：——

  公开号：US20030022913A1

  公开（公告）日：2003-01-30

  The present invention relates to a novel heterocyclic compound, a pharmaceutical composition comprisining said compound, a method and use of said compound for clinical treatment of medical conditions which may benefit from immunomodulation, e.g. rheumatoid arthritis, multiple sclerosis, diabetes, asthma, transplantation, systemic lupus erythematosis and psoriasis. More particularly the present invention relates to novel heterocyclic compounds, which are CD80 antagonists capable of inhibiting the interactions between CD80 and CD28. A method of screening compounds for their ability of inhibiting ligand-induced co-stimulatory receptor internalisation pathways in immune competent human cells is described. Said immune competent human cells are incubated at conditions capable of inducing co-stimulatory receptor internalisation in the presence of at least one test compound and the suppression of the ligand-induced co-stimulatory receptor internalisation determined. There is also described a kit for use in such a method, as well as an immunoregulatory drug capable of blocking down-modulation of a ligand-induced receptor.

  本发明涉及一种新颖的杂环化合物，一种包含该化合物的药物组合物，以及该化合物在临床治疗可能受益于免疫调节的医疗状况的方法和用途，例如类风湿关节炎、多发性硬化症、糖尿病、哮喘、移植、系统性红斑狼疮和牛皮癣。更具体地，本发明涉及一种新颖的杂环化合物，这些化合物是CD80拮抗剂，能够抑制CD80和CD28之间的相互作用。描述了一种筛选化合物的方法，用于评估它们抑制免疫能力的能力，即抑制免疫能力的人类细胞内的配体诱导的共刺激受体内化途径。在至少一种试验化合物存在的条件下，孵育这些免疫能力的人类细胞，能够诱导共刺激受体内化，并确定抑制配体诱导的共刺激受体内化。还描述了一种用于此类方法的试剂盒，以及一种能够阻断配体诱导受体下调的免疫调节药物。
• Therapeutic targets and agents useful in treating ischemia reperfusion injury
  申请人：Cardio3 Biosciences S.A.

  公开号：EP2883883A1

  公开（公告）日：2015-06-17

  The application teaches a therapeutic agent for use in the treatment of cardiac warm ischemia reperfusion injury, wherein said therapeutic agent is capable of interacting with at least one of the CD80 or CD86 polypeptides, and wherein said interaction interferes with the binding of the at least one of the CD80 or CD86 polypeptides to the CD28 polypeptide. The application also teaches a therapeutic agent for use in the treatment of cardiac warm ischemia reperfusion injury, wherein said therapeutic agent is capable of preventing or inhibiting the expression of at least one of the CD80 or CD86 polypeptides by a cell or on the surface of a cell.

  本申请教导了一种用于治疗心脏温缺血再灌注损伤的治疗剂，其中所述治疗剂能够与CD80或CD86多肽中的至少一种相互作用，并且所述相互作用干扰CD80或CD86多肽中的至少一种与CD28多肽的结合。本申请还教导了一种用于治疗心脏温缺血再灌注损伤的治疗剂，其中所述治疗剂能够阻止或抑制细胞或细胞表面至少一种 CD80 或 CD86 多肽的表达。
• NOVEL IMMUNOMODULATING COMPOUNDS
  申请人：Active Biotech AB

  公开号：EP1409485A1

  公开（公告）日：2004-04-21
• IMMUNOMODULATING COMPOUNDS
  申请人：Active Biotech AB

  公开号：EP1409485B1

  公开（公告）日：2006-04-26
• US6642249B2
  申请人：——

  公开号：US6642249B2

  公开（公告）日：2003-11-04