I-Cbp112

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并恶嗪类
• 英文名称: I-Cbp112
• 英文别名: 1-[7-(3,4-dimethoxyphenyl)-9-[[(3S)-1-methylpiperidin-3-yl]methoxy]-3,5-dihydro-2H-1,4-benzoxazepin-4-yl]propan-1-one
• 化学式: C₂₇H₃₆N₂O₅
• 分子量: 468.6
• InChiKey: YKNAKDFZAWQEEO-IBGZPJMESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  34
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.52
• 拓扑面积：
  60.5
• 氢给体数：
  0
• 氢受体数：
  6

文献信息

• [EN] P53 MODULATORS AND USES THEREOF<br/>[FR] MODULATEURS DE p53 ET UTILISATIONS DE CEUX-CI
  申请人：UNIV CALIFORNIA

  公开号：WO2021087096A1

  公开（公告）日：2021-05-06

  Described herein, inter alia, are p53 modulator compounds and methods of using the same. In an aspect is provided a p53 protein covalently bonded to a compound described herein. In an aspect is provided a pharmaceutical composition including a compound described herein and a pharmaceutically acceptable excipient. In an aspect is provided a method of treating cancer in a subject in need of such treatment, including administering to the subject an effective amount of a compound described herein.

  本文描述了p53调节剂化合物及其使用方法等内容。在一个方面，提供了一种p53蛋白与本文描述的化合物共价结合的方法。在一个方面，提供了一种包含本文描述的化合物和药用辅料的药物组合物。在一个方面，提供了一种治疗需要此类治疗的受试者的癌症的方法，包括向受试者施用本文描述的化合物的有效量。
• THERAPEUTIC COMPOUNDS AND USES THEREOF
  申请人：Constellation Pharmaceuticals, Inc.

  公开号：US20160158207A1

  公开（公告）日：2016-06-09

  The present invention relates to compounds of formula (I) or formula (II): and to salts thereof, wherein R 1 -R 4 of formula (I) and R 1 -R 3 of formula (II) have any of the values defined herein, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) of formula (II) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders.

  本发明涉及公式（I）或公式（II）的化合物及其盐，其中公式（I）的R1-R4和公式（II）的R1-R3具有以下定义的任何值，以及其组合物和用途。这些化合物可用作CBP和/或EP300的抑制剂。还包括含有公式（I）或公式（II）的化合物或其药学上可接受的盐的制药组合物，以及使用这些化合物和盐治疗各种CBP和/或EP300介导的疾病的方法。
• Methods for production of functional beta cells
  申请人：Janssen Biotech, Inc.

  公开号：US10633635B2

  公开（公告）日：2020-04-28

  The invention provides for methods of differentiating pancreatic endocrine cells into pancreatic beta cells expressing PDX1, NKX6.1, MAFA, UCN3 and SLC2A. These pancreatic beta cells may be obtained by step-wise differentiation of pluripotent stem cells. The pancreatic beta cells exhibit glucose-dependent mitochondrial respiration and glucose-stimulated insulin secretion similar to islet cells.

  本发明提供了将胰腺内分泌细胞分化成表达PDX1、NKX6.1、MAFA、UCN3和SLC2A的胰腺β细胞的方法。这些胰腺β细胞可通过多能干细胞的逐步分化获得。胰岛β细胞表现出与胰岛细胞相似的葡萄糖依赖性线粒体呼吸和葡萄糖刺激的胰岛素分泌。
• Compositions and methods for reprogramming non-neuronal cells into neuron-like cells
  申请人：Beihao Stem Cell and Regenerative Medicine Research Institutes Co., Ltd.

  公开号：US10857185B2

  公开（公告）日：2020-12-08

  Cocktails of chemical inducers of neuron-like properties (CINP) is provided, which includes cAMP agonists, neurogenic small molecules, glycogen synthase kinase inhibitors, TGFβ receptor inhibitors, and BET family bromodomain inhibitors and optionally, a selective inhibitor of ROCK or p38 MAPK. These cocktails are used in a method of inducing neuron-like properties in partially or completely differentiated non-neuronal cells. The method includes contacting cells of a first type (non-neuronal) with the CINPs for a sufficient period of time to result in reprogramming the cell into cells of a second type having neuron-like characteristics (CiNs). Isolated chemically induced neurons (CiNs) can be used in a number of applications, including but not limited to cell therapy.

  本研究提供了神经元样特性化学诱导剂（CINP）鸡尾酒，其中包括 cAMP 激动剂、神经原小分子、糖原合酶激酶抑制剂、TGFβ 受体抑制剂、BET 家族溴域抑制剂以及 ROCK 或 p38 MAPK 的选择性抑制剂。这些鸡尾酒可用于在部分或完全分化的非神经元细胞中诱导神经元样特性的方法。该方法包括将第一种类型（非神经元）的细胞与 CINPs 接触足够长的时间，使细胞重编程为具有神经元样特性（CiNs）的第二种类型的细胞。分离的化学诱导神经元（CiNs）可用于多种应用，包括但不限于细胞疗法。
• [EN] 4,5,6,7-TETRAHYDRO-1 H-PYRAZOLO[4,3-C]PYRIDIN-3-AMINE COMPOUNDS AS CBP AND/OR EP300 INHIBITORS<br/>[FR] COMPOSÉS 4,5,6,7-TETRAHYDRO-1 H-PYRAZOLO[4,3-C]PYRIDIN-3-AMINE UTILISÉS COMME INHIBITEURS DE CBP ET/OU DE EP300
  申请人：GENENTECH INC

  公开号：WO2016086200A9

  公开（公告）日：2016-06-23