acetyl-dimethyl-(6-oxo-5H-phenanthridin-2-yl)azanium

• 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
• 英文名称: acetyl-dimethyl-(6-oxo-5H-phenanthridin-2-yl)azanium
• 化学式: C17H17N2O2+
• 分子量: 281.33
• InChiKey: JUBATZWOOUQYHU-UHFFFAOYSA-O

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  21
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.18
• 拓扑面积：
  46.2
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• 3-OXO-2,3-DIHYDRO-1H-ISOINDOLE-4-CARBOXAMIDES AS PARP INHIBITORS
  申请人：Papeo Gianluca Mariano Enrico

  公开号：US20120245142A1

  公开（公告）日：2012-09-27

  There are provided substituted 3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide derivatives (I) which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of this invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating, diseases utilizing pharmaceutical compositions comprising these compounds.

  本发明提供了替代的3-氧代-2,3-二氢-1H-异吲哚-4-羧酰胺衍生物（I），其能够选择性地抑制PARP-1相对于PARP-2的活性。因此，本发明的化合物可用于治疗癌症、心血管疾病、中枢神经系统损伤和不同形式的炎症等疾病。本发明还提供了制备这些化合物的方法、包含这些化合物的制药组合物以及利用包含这些化合物的制药组合物治疗疾病的方法。
• 3-0X0-2,3-DIHYDRO-1H-ISOINDOLE-4-CARBOXAMIDES WITH SELECTIVE PARP-1 INHIBITION
  申请人：Papeo Gianluca Mariano Enrico

  公开号：US20120245143A1

  公开（公告）日：2012-09-27

  There are provided substituted 3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide derivatives (I) which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of this invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.

  提供了替代3-氧代-2,3-二氢-1H-异吲哚-4-羧酰胺衍生物(I)，其对聚(ADP-核糖)聚合酶PARP-1的活性具有选择性抑制作用，相对于聚(ADP-核糖)聚合酶PARP-2。因此，本发明的化合物可用于治疗癌症、心血管疾病、中枢神经系统损伤和不同形式的炎症等疾病。本发明还提供了制备这些化合物的方法，包括这些化合物的制药组合物，以及利用这些化合物的制药组合物治疗疾病的方法。
• Induced extended pluripotent stem cells, method of making and using
  申请人：Beihao Stem Cell and Regenerative Medicine Research Institute Co., Ltd.

  公开号：US11028369B2

  公开（公告）日：2021-06-08

  Factors for extending the ability of isolated pluripotent stem cells to generate extraembryonic lineages in vivo, following in vitro culture, herein, chemical extenders of pluripotency (CEP). Methods of extending the ability of a pluripotent cell to generate embryonic and extraembryonic lineages. The cell to be reprogrammed is contacted with effective amounts of the CEPs for a sufficient period of time to reprogram the cell into a chemically induced extended pluripotent cell (ciEPSC). ciEPSC are identified as an extended pluripotent cell based on properties including: (i) morphologically and (ii) functionally for example, based on their ability contribute to both TE and ICM, in vivo. The ciEPSCs can be cultured or induced to differentiate into cells of a desired type, and used in a number of applications, including but not limited to cell therapy and tissue engineering.

  在体外培养后，延长分离的多能干细胞在体内产生胚外系的能力的因素，这里称为多能性化学延长剂（CEP）。延长多能细胞生成胚胎和胚外系能力的方法。将待重编程的细胞与有效量的 CEPs 接触足够长的时间，以将细胞重编程为化学诱导的扩展多能性细胞（ciEPSC）。ciEPSC 可根据以下特性确定为扩展多能性细胞：(i) 形态学上；(ii) 功能上，例如，根据它们在体内对 TE 和 ICM 的贡献能力。ciEPSCs 可培养或诱导分化为所需类型的细胞，并可用于多种应用，包括但不限于细胞疗法和组织工程。
• Poly-(ADP) ribose polymerase enzyme and uses thereof
  申请人：——

  公开号：US20040127444A1

  公开（公告）日：2004-07-01

  Poly(ADP)-ribose polymerase (PARP) becomes activated at sites of DNA damage and is thought to promote repair by modifying local chromatin proteins and transcription factors. Disclosed is an isoform of PARP, PARP-e, which lacks enzymatic function and which is encoded by a gene having a novel structure. Also disclosed are methods of modulating chromatin structure resulting in modulation of gene activation, gene repression and chromatin condensation and decondensation.

  聚（ADP）-核糖聚合酶（PARP）在 DNA 损伤部位被激活，被认为能通过改变局部染色质蛋白和转录因子促进修复。本研究公开了一种 PARP 的异构体--PARP-e，它缺乏酶的功能，由具有新结构的基因编码。还公开了调节染色质结构的方法，从而调节基因活化、基因抑制以及染色质的凝集和解凝。
• Method of treating or preventing pathologic effects of acute increases in hyperglycemia and/or acute increases of free fatty acid flux
  申请人：Gurtner C. Geoffrey

  公开号：US20060100189A1

  公开（公告）日：2006-05-11

  One aspect of the present invention relates to a method of treating or preventing pathologic sequelae of acute hyperglycemia and/or increased fatty acid flux in a subject. This method involves administering an ROS inhibitor to the subject. In addition, methods of promoting neovascularization, inhibiting oxidation or excessive release of free fatty acids, and identifying compounds suitable for treatment or prevention of ROS-mediated injury are also disclosed.

  本发明的一个方面涉及一种治疗或预防受试者急性高血糖和/或脂肪酸通量增加的病理后遗症的方法。该方法包括向受试者施用 ROS 抑制剂。此外，还公开了促进新生血管生成、抑制氧化或游离脂肪酸过度释放的方法，以及鉴定适合治疗或预防 ROS 介导的损伤的化合物的方法。