4-乙酰基-1-哌嗪羧酸 | 148490-38-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 中文名称: 4-乙酰基-1-哌嗪羧酸
• 英文名称: 4-acetyl-1-piperazinecarboxylic acid
• 英文别名: 1-Piperazinecarboxylic acid, 4-acetyl-；4-Acetylpiperazine-1-carboxylic acid
• CAS: 148490-38-4
• 化学式: C₇H₁₂N₂O₃
• 分子量: 172.184
• InChiKey: DDOWCQQXWQWZQD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.9
• 重原子数：
  12
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.71
• 拓扑面积：
  60.8
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• Novel pyridine derivative and pyrimidine derivative
  申请人：Matsushima Tomohiro

  公开号：US20050277652A1

  公开（公告）日：2005-12-15

  A compound represented by the following formula, a salt thereof or a hydrate of the foregoing has an excellent hepatocyte growth factor receptor (HGFR) inhibitory activity, and exhibits anti-tumor activity, angiogenesis inhibitory activity and cancer metastasis inhibitory activity. [R 1 represents C 1-6 alkyl or the like; R 2 and R 3 represent hydrogen; R 4 , R 5 , R 6 , and R 7 may be the same or different and each represents hydrogen, halogen, C 1-6 alkyl or the like; R 8 represents hydrogen or the like; R 9 represents C 1-6 alkyl or the like; V 1 represents oxygen or the like; V 2 represents oxygen or sulfur; W represents —NH— or the like; X represents —CH═, nitrogen or the like; and Y represents oxygen or the like.]

  以下化合物的分子式，其盐或前述水合物具有出色的肝细胞生长因子受体（HGFR）抑制活性，并表现出抗肿瘤活性、抑制血管生成活性和抑制癌转移活性。 [R 1 代表C 1-6 烷基或类似物；R 2 和R 3 代表氢；R 4 ，R 5 ，R 6 和R 7 可以相同也可以不同，每个代表氢、卤素、C 1-6 烷基或类似物；R 8 代表氢或类似物；R 9 代表C 1-6 烷基或类似物；V 1 代表氧或类似物；V 2 代表氧或硫；W代表—NH—或类似物；X代表—CH═、氮或类似物；Y代表氧或类似物。]
• [EN] THIENOPYRANONES AND FURANOPYRANONES AS KINASE, BROMODOMAIN, AND CHECKPOINT INHIBITORS<br/>[FR] THIÉNOPYRANONES ET FURANOPYRANONES EN TANT QU'INHIBITEURS DE KINASE, DE BROMODOMAINE ET DE POINTS DE CONTRÔLE
  申请人：SIGNALRX PHARMACEUTICALS INC

  公开号：WO2018140730A1

  公开（公告）日：2018-08-02

  The invention relates to compounds and methods of treating diseases including but not limited to, cancer, non-cancer proliferative disease, sepsis, autoimmune disease, viral infaction, atheroscleosis. Type 1 or 2 diabetes, obesity, inflammatory disease, or Myc-depenent disorder including by modulating biological processes by the inhibition of cell cycle checkpoint targets CDKs, and/or PI3 kinase, and/or bromodomain protein binding to substrates, comprising the administration of a compound(s) of Formula 1 -Vl (or pharmaceutically acceptable salts thereof) as defined herein.

  这项发明涉及化合物和治疗疾病的方法，包括但不限于癌症、非癌性增生性疾病、败血症、自身免疫疾病、病毒感染、动脉粥样硬化、1型或2型糖尿病、肥胖症、炎症性疾病或通过通过抑制细胞周期检查点靶点CDKs、和/或PI3激酶、和/或溴结构域蛋白结合到底物来调节生物过程，包括根据本文所定义的将化合物的给药作为公式1-Vl（或其药学上可接受的盐）的组成部分。
• [EN] HSP70 MODULATORS AND METHODS FOR MAKING AND USING THE SAME<br/>[FR] MODULATEURS DE HSP70 ET LEUR PROCÉDÉS DE FABRICATION ET LEUR UTILISATION
  申请人：SLOAN KETTERING INST CANCER

  公开号：WO2015175707A1

  公开（公告）日：2015-11-19

  The present invention provides compounds I and II and compositions thereof for use in the modulation of Hsp70. In some embodiments, the present invention provides a method for inhibiting Hsp70 activity. In some embodiments, the present invention provides a method of treating a subject suffering from or susceptible to a disease, disorder, or condition responsive to Hsp70 inhibition comprising administering to the subject a therapeutically effective amount of a provided compound. In some embodiments, the present invention provides a method for treating or preventing cancer in a subject suffering therefrom, comprising administering to a patient in need thereof a therapeutically effective amount of a provided compound.

  本发明提供化合物I和II及其组合物，用于调节Hsp70。在某些实施例中，本发明提供一种抑制Hsp70活性的方法。在某些实施例中，本发明提供一种治疗患有或易受Hsp70抑制性疾病、紊乱或病况的受试者的方法，包括向受试者施用所提供化合物的治疗有效量。在某些实施例中，本发明提供一种治疗或预防患有癌症的受试者的方法，包括向需要的患者施用所提供化合物的治疗有效量。
• OXINDOLE DERIVATIVES
  申请人：Chen Li

  公开号：US20080081810A1

  公开（公告）日：2008-04-03

  There is provided compounds of the formula wherein R 6 , V, W, X, Y, Q and n are as described. The compounds exhibit activity as anticancer agents.

  提供的化合物具有以下结构式，其中R6、V、W、X、Y、Q和n如所述。这些化合物表现出抗癌药物的活性。
• [EN] HETEROCYCLIC SPIRO-COMPOUNDS AS AM2 RECEPTOR INHIBITORS<br/>[FR] COMPOSÉS SPIRO HÉTÉROCYCLIQUES CONSTITUANT DES INHIBITEURS DU RÉCEPTEUR DE L'AM2
  申请人：UNIV SHEFFIELD

  公开号：WO2020099882A1

  公开（公告）日：2020-05-22

  Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof: wherein HET, R1, R2, R3, R4, R5, L, L1, X1, X2, X3 and q are as defined herein. The compounds are inhibitors of adrenomedullin receptor subtype 2 (AM2). Also disclosed are the compounds for use in the treatment of diseases modulated AM2, including proliferative diseases such as cancer; pharmaceutical compositions comprising the compounds; methods for preparing the compounds; and intermediates useful in the preparation of the compounds.

  揭示了式(I)的化合物及其药学上可接受的盐：其中HET、R1、R2、R3、R4、R5、L、L1、X1、X2、X3和q如本文所定义。这些化合物是肾上腺髓质素受体亚型2（AM2）的抑制剂。还揭示了这些化合物用于治疗调节AM2的疾病，包括增殖性疾病如癌症；包含这些化合物的药物组合物；制备这些化合物的方法；以及制备这些化合物的有用中间体。