5-Hydroxy-1-methylpiperidin-2-one | 33342-01-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: 5-Hydroxy-1-methylpiperidin-2-one
• CAS: 33342-01-7
• 化学式: C₆H₁₁NO₂
• mdl: MFCD22399025
• 分子量: 129.16
• InChiKey: UCSPSEUVPQTOQD-UHFFFAOYSA-N

物化性质

• 沸点：
  193-195 °C(Press: 13 Torr)
• 密度：
  1.163±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -0.8
• 重原子数：
  9
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.833
• 拓扑面积：
  40.5
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  2-fluoro-5-(4-((4-(4-(oxetan-3-yl)piperazin-1-yl)phenyl)amino)-1,3,5-triazin-2-yl)benzonitrile 、 5-Hydroxy-1-methylpiperidin-2-one 生成 2-((1-methyl-6-oxopiperidin-3-yl)oxy)-5-(4-((4-(4-(oxetan-3-yl)piperazin-1-yl)phenyl)amino)-1,3,5-triazin-2-yl)benzonitrile
  参考文献：
  名称：

  TANK-BINDING KINASE INHIBITOR COMPOUNDS

  摘要：

  本发明公开了具有以下式(I)的化合物及其使用和制备方法：

  公开号：

  US20160096827A1

文献信息

• 8-AMINOISOQUINOLINE COMPOUNDS AND USES THEREOF
  申请人：Genentech, Inc.

  公开号：US20200108075A1

  公开（公告）日：2020-04-09

  3-Carbonylamino-8-aminoisoquinoline compounds of formula (I): variations thereof, and their use as inhibitors of HPK1 (hematopoietic kinase 1) are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods of inhibiting HPK1, methods of treating HPK1-dependent disorders, methods for enhancing an immune response, and methods for preparing the 3-carbonylamino-8-aminoisoquinoline compounds.

  公式（I）的3-羰基氨基异喹啉化合物及其变体，以及它们作为HPK1（造血激酶1）抑制剂的用途被描述。这些化合物在治疗HPK1依赖性疾病和增强免疫应答方面是有用的。还描述了抑制HPK1的方法，治疗HPK1依赖性疾病的方法，增强免疫应答的方法，以及制备3-羰基氨基异喹啉化合物的方法。
• [EN] HYDROXAMATE COMPOUNDS AS ANTAGONISTS OF THE ADENOSINE A2A RECEPTOR<br/>[FR] COMPOSÉS HYDROXAMATE EN TANT QU'ANTAGONISTES DU RÉCEPTEUR A2A DE L'ADÉNOSINE
  申请人：ADORX THERAPEUTICS LTD

  公开号：WO2020260857A1

  公开（公告）日：2020-12-30

  The present invention relates to compounds of formula I shown below: (I) wherein R1, R2 and R3 are each as defined in the application. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of diseases or conditions in which adenosine A2a receptor activity is implicated, such as, for example, cancer.

  本发明涉及下面所示的式I的化合物：(I)，其中R1、R2和R3在申请中各自定义。本发明还涉及制备这些化合物的方法，包括含有它们的药物组合物，以及它们在治疗腺苷A2a受体活性参与的疾病或症状中的用途，例如癌症。
• [EN] 1,3-THIAZOL-2-YL SUBSTITUTED BENZAMIDES<br/>[FR] BENZAMIDES À SUBSTITUTION 1,3-THIAZOL-2-YL
  申请人：EVOTEC AG

  公开号：WO2016091776A1

  公开（公告）日：2016-06-16

  The present invention relates to 1,3-thiazol-2-yl substituted benzamide compounds of general formula (I) as described and defined herein, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neurogenic disorder, as a sole agent or in combination with other active ingredients.

  本发明涉及一般式（I）所述和定义的1,3-噻唑-2-基取代苯甲酰胺化合物，以及包含所述化合物的药物组合物和药物组合物的用途，用于制造用于治疗或预防疾病的药物组合物，特别是神经源性疾病，作为唯一药剂或与其他活性成分组合使用。
• VEGFR-2 and VEGFR-3 inhibitory anthranilamide pyridines
  申请人：Huth Andreas

  公开号：US20070015794A1

  公开（公告）日：2007-01-18

  VEGFR-2 and VEGFR-3 inhibitory anthranilamide pyridinamides, their production and use as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis, as well as intermediate products for the production of the compounds are described. The compounds according to the invention can be used as or in the case of tumor or metastasis growth, psoriasis, Kaposi's sarcoma, restenosis, such as, e.g., stent-induced restenosis, endometriosis, Crohn's disease, Hodgkin's disease, leukemia; arthritis, such as rheumatoid arthritis, hemangioma, angiofibroma; eye diseases, such as diabetic retinopathy, neovascular glaucoma; renal diseases, such as glomerulonephritis, diabetic nephropathy, malignant nephrosclerosis, thrombic microangiopathic syndrome, transplant rejections and glomerulopathy; fibrotic diseases, such as cirrhosis of the liver, mesangial cell proliferative diseases, arteriosclerosis, injuries to nerve tissue, and inhibition of the reocclusion of vessels after balloon catheter treatment, in vascular prosthetics or after mechanical devices are used to keep vessels open, such as, e.g., stents, as immunosuppressive agents, as a support in scar-free healing, senile keratosis and contact dermatitis. The compounds according to the invention can also be used as VEGFR-3 inhibitors in the case of lymphangiogenesis.

  本发明涉及VEGFR-2和VEGFR-3抑制剂类蒽酰胺吡啶酰胺，以及它们的制备和用途作为治疗由持续血管生成引起的疾病的药物，还包括制备该化合物的中间体。根据本发明的化合物可用于肿瘤或转移性生长、银屑病、卡波西肉瘤、再狭窄（例如支架导致的再狭窄）、子宫内膜异位症、克罗恩病、霍奇金病、白血病、关节炎（例如类风湿性关节炎）、血管瘤、血管纤维瘤、眼部疾病（例如糖尿病性视网膜病变、新生血管性青光眼）、肾脏疾病（例如肾小球肾炎、糖尿病性肾病、恶性肾硬化、血栓性微血管病综合征、移植排斥和肾小球病）、纤维化疾病（例如肝硬化、系膜细胞增生性疾病、动脉硬化、神经组织损伤以及在血管假体、机械设备（例如支架）用于保持血管开放之后抑制再闭塞的药物，作为免疫抑制剂、支持无疤痕愈合、老年角化病和接触性皮炎。根据本发明的化合物还可以用作淋巴生成抑制剂VEGFR-3。
• Tank-binding kinase inhibitor compounds
  申请人：Gilead Sciences, Inc.

  公开号：US10040781B2

  公开（公告）日：2018-08-07

  Compounds having the following formula (I) and methods of their use and preparation are disclosed:

  公开了具有下式（I）的化合物及其使用和制备方法：