5-chloro-1-[[4-[2-(2,5-dioxopyrrolidin-1-yl)ethoxy]-3-methylphenyl]methyl-(2-methylpropyl)amino]-2,3-dihydro-1H-indene-2-carboxylic acid

• 分子结构分类: 有机化合物 - 苯类化合物 - 茚满类
• 英文名称: 5-chloro-1-[[4-[2-(2,5-dioxopyrrolidin-1-yl)ethoxy]-3-methylphenyl]methyl-(2-methylpropyl)amino]-2,3-dihydro-1H-indene-2-carboxylic acid
• 化学式: C₂₈H₃₃ClN₂O₅
• 分子量: 513.0
• InChiKey: BTOHTQCFIPQOFQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  36
• 可旋转键数：
  10
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.46
• 拓扑面积：
  87.2
• 氢给体数：
  1
• 氢受体数：
  6

文献信息

• [EN] SUBSTITUTED ß-AMINO ACID DERIVATIVES AS CXCR3 RECEPTOR ANTAGONISTS<br/>[FR] DÉRIVÉS D'ACIDES AMINÉS SS SUBSTITUÉS COMME ANTAGONISTES DU RÉCEPTEUR CXCR3
  申请人：SANOFI SA

  公开号：WO2013174485A1

  公开（公告）日：2013-11-28

  The present invention relates to compounds of formula 1 that are useful as an active ingredient of a medicament for preventive and/or therapeutic treatment of diseases caused by abnormal activation of CXCR3 chemokines. The invention relates furthermore to a process for the preparation of said compounds, to pharmaceutical compositions containing said compounds and to the novel intermediates used in the preparation of said compounds.

  本发明涉及公式1的化合物，该化合物作为药物活性成分用于预防性和/或治疗由CXCR3趋化因子异常激活引起的疾病。此外，发明还涉及制备所述化合物的方法、包含所述化合物的药物组合物以及用于制备所述化合物的新中间体。
• SUBSTITUTED B-AMINO ACID DERIVATIVES AS CXCR3 RECEPTOR ANTAGONISTS
  申请人：SANOFI

  公开号：US20150073004A1

  公开（公告）日：2015-03-12

  The present invention relates to compounds of formula 1 that are useful for the preventive and/or therapeutic treatment of diseases caused by abnormal activation of CXCR3 chemokines. The invention relates furthermore to a process for the preparation of said compounds, to pharmaceutical compositions containing said compounds and to novel intermediates used in the preparation of said compounds.

  本发明涉及公式1的化合物，其对由CXCR3趋化因子异常激活引起的疾病的预防和/或治疗具有用处。本发明还涉及制备该化合物的方法，含有该化合物的制药组合物以及用于制备该化合物的新型中间体。
• SUBSTITUTED ß-AMINO ACID DERIVATIVES AS CXCR3 RECEPTOR ANTAGONISTS
  申请人：SANOFI

  公开号：EP2852578A1

  公开（公告）日：2015-04-01
• US9447038B2
  申请人：——

  公开号：US9447038B2

  公开（公告）日：2016-09-20
• [EN] USE OF SUBSTITUTED 2-PHENYL-3H-QUINAZOLIN-4-ONES AND ANALOGS FOR INHIBITING BROMODOMAIN AND EXTRA TERMINAL DOMAIN (BET) PROTEINS<br/>[FR] TRAITEMENT DE MALADIES PAR LA RÉGULATION ÉPIGÉNÉTIQUE
  申请人：RVX THERAPEUTICS INC

  公开号：WO2013175281A1

  公开（公告）日：2013-11-28

  The present application is directed to the use of substituted 2-phenyl-3H-quinazolin-4-ones and analogs for inhibiting bromodomain and extra terminal domain (BET) proteins. The disclosed compounds can be used for the treatment of cancers that exhibit c-myc overexpression, cancers that overexpress n-myc, and cancers that rely on the recruitment of p-TEFb to regulate activated oncogenes, such as Burkitt's lymphoma, acute myelogenous leukemia, multiple myeloma, aggressive human medulloblastoma, hematological, epithelial cancers, lung cancers, breast cancers, colon carcinomas, midline carcinomas, mesenchymal tumors, hepatic tumors, renal tumors and neurological tumors.