阿美帕利 | 1227156-72-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 中文名称: 阿美帕利
• 英文名称: 10-etoxy-8-(morpholinomethyl)-1,2,3,4-tetrahydrobenzo[h][1,6]naphthyridine-5(6H)-one
• 英文别名: 10-ethoxy-8-(morpholinomethyl)-1,2,3,4-tetrahydrobenzo[h][1,6]naphthyridine-5(6H)-one；Amelparib；10-ethoxy-8-(morpholin-4-ylmethyl)-2,3,4,6-tetrahydro-1H-benzo[h][1,6]naphthyridin-5-one
• CAS: 1227156-72-0
• 化学式: C₁₉H₂₅N₃O₃
• 分子量: 343.426
• InChiKey: WBBZUHMHBSXBDT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  25
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.53
• 拓扑面积：
  62.8
• 氢给体数：
  2
• 氢受体数：
  5

文献信息

• NOVEL TRICYCLIC DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME
  申请人：Kim Myung-Hwa

  公开号：US20110218193A1

  公开（公告）日：2011-09-08

  The present invention relates to a novel tricyclic derivative with efficient inhibitory activity against poly(ADP-ribose)polymerases (PARP) or pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition containing the same. The tricyclic derivative of the invention is useful for the prevention or treatment of diseases caused by excess PARP activity, especially neuropathic pain, neurodegenerative diseases, cardiovascular diseases, diabetic nephropathy, inflammatory diseases, osteoporosis, and cancer, by inhibiting the activity of poly(ADP-ribose)polymerases.

  本发明涉及一种新型三环衍生物，具有高效的抑制聚(ADP-核糖)聚合酶（PARP）或其药用可接受盐的活性，以及其制备方法和含有该衍生物的药物组合物。本发明的三环衍生物通过抑制聚(ADP-核糖)聚合酶的活性，对于预防或治疗由过度PARP活性引起的疾病特别有效，包括神经病痛、神经退行性疾病、心血管疾病、糖尿病肾病、炎症性疾病、骨质疏松症和癌症。
• CRYSTALLINE FORMS OF TRICYCLIC COMPOUND ACID SALT OR HYDRATE THEREOF, AND METHOD FOR MAKING THEREOF
  申请人：Jeil Pharmaceutical Co., Ltd.

  公开号：US20140350007A1

  公开（公告）日：2014-11-27

  The present invention relates to a novel crystalline acid salt of a tricyclic derivative or a hydrate thereof and a production method thereof. The crystalline acid salt or the hydrate thereof according to the present invention is stable with respect to humidity and stable with respect to hygroscopicity, and the quality control during manufacturing drugs is favorable. In addition, the crystalline acid salt or the hydrate thereof may be used in a pharmaceutical composition for preventing or treating neuropathic pain, epilepsy, stroke, Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis (ALS), Huntington's disease, schizophrenia, chronic and acute pain, ischemic brain injury, neuronal loss after hypoxia, trauma and nerve damage, which are medical conditions induced by PARP overactivity.

  本发明涉及一种新型三环衍生物的结晶酸盐或其水合物及其生产方法。根据本发明的结晶酸盐或其水合物对湿度稳定且对吸湿性稳定，制药过程中的质量控制良好。此外，根据本发明的结晶酸盐或其水合物可用于预防或治疗由PARP过度活化引起的神经病症状，如神经痛、癫痫、中风、阿尔茨海默病、帕金森病、肌萎缩侧索硬化症（ALS）、亨廷顿病、精神分裂症、慢性和急性疼痛、缺血性脑损伤、缺氧后神经元丧失、创伤和神经损伤等医疗状况中的药物组合物。
• Histone methyltransferase inhibitors
  申请人：GLOBAL BLOOD THERAPEUTICS, INC.

  公开号：US10829452B2

  公开（公告）日：2020-11-10

  The present disclosure provides compounds of Formula (I) that are histone methyltransferases G9a and/or GLP inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of G9a and/or GLP such as cancers and hemoglobinpathies (e.g., beta thalassemia and sickle cell disease). Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds. where R1, alk, R2, Z1, Z2, X, R3, R4, B, a, and b are as described herein.

  本公开提供的式(I)化合物是组蛋白甲基转移酶G9a和/或GLP抑制剂，因此可用于治疗可通过抑制G9a和/或GLP治疗的疾病，如癌症和血红蛋白病（如β地中海贫血和镰状细胞病）。此外，还提供了含有此类化合物的药物组合物和制备此类化合物的工艺。 其中 R1、alk、R2、Z1、Z2、X、R3、R4、B、a 和 b 如本文所述。
• Methods of treating acute kidney injury
  申请人：Mitobridge, Inc.

  公开号：US10874641B2

  公开（公告）日：2020-12-29

  The present invention also contemplates a method of treating a human patient with acute kidney injury or reducing the likelihood of developing acute kidney injury in a human patient at risk of developing acute kidney injury comprising administering to the patient a poly-ADP ribose polymerase (PARP) inhibitor in a therapeutically effective dose so as to thereby treat the patient.

  本发明还考虑了一种治疗急性肾损伤患者或降低有患急性肾损伤风险的患者患急性肾损伤可能性的方法，该方法包括向患者施用治疗有效剂量的多-ADP核糖聚合酶（PARP）抑制剂，从而治疗患者。
• [EN] PHOSPHAMIDE DERIVATIVE, METHOD FOR MANUFACTURING THE SAME, AND USES THEREOF<br/>[FR] DÉRIVÉ DE PHOSPHAMIDE, SON PROCÉDÉ DE FABRICATION ET SES UTILISATIONS<br/>[ZH] 一种磷酰胺衍生物及制备方法和用途
  申请人：SICHUAN HAISCO PHARMACEUTICAL CO LTD

  公开号：WO2017133517A1

  公开（公告）日：2017-08-10

  公开了一种磷酰胺衍生物及制备方法和用途。特别公开了一种通式(I)所示化合物及其药学上可接受的盐或立体异构体 (I)，其中，G、L、Q、s如说明书中所定义。