4-(吗啉-4-基)哌啶二盐酸盐 | 334942-10-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 中文名称: 4-(吗啉-4-基)哌啶二盐酸盐
• 中文别名: 4-(哌啶-4-基)吗啉盐酸盐；4-(4-哌啶基)吗啉盐酸盐
• 英文名称: 4-(Morpholin-4-yl)-piperidine dihydrochloride
• 英文别名: 4-piperidin-4-ylmorpholine;dihydrochloride
• CAS: 334942-10-8
• 化学式: C9H20Cl2N2O
• 分子量: 243.17
• InChiKey: YMFXRJRQDSSRQP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.91
• 重原子数：
  14
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  24.5
• 氢给体数：
  3
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  盐酸 、 水 、 氢气 、 N-苄基-4-(4-吗啉基)哌啶 、 在 氢氧化钯 氢气 、 水合茚三酮 作用下， 以 甲醇 为溶剂， 反应 10.84h， 以to yield the 4-(morpholin-4-yl)piperidine dihydrochloride as an off-white solid的产率得到4-(吗啉-4-基)哌啶二盐酸盐
  参考文献：
  名称：

  3-[4-Substituted heterocyclyl)-pyrrol-2-ylmethylidene]-2- indolinone derivatives as kinase inhibitors

  摘要：

  本发明涉及某些3-[4-(取代杂环基)-吡咯-2-基甲基]-2-吲哚酮衍生物，其抑制激酶，尤其是VEGFR和/或PDGFR激酶。还公开了包含这些化合物的药物组合物、利用包含这些化合物的药物组合物治疗通过激酶介导的疾病的方法以及制备它们的方法。

  公开号：

  US20030130235A1

文献信息

• [EN] SUBSTITUTED PYRIDINES AS INHIBITORS OF DNMT1<br/>[FR] PYRIDINES SUBSTITUÉES EN TANT QU'INHIBITEURS DE DNMT1
  申请人：GLAXOSMITHKLINE IP DEV LTD

  公开号：WO2017216726A1

  公开（公告）日：2017-12-21

  The invention is directed to substituted pyridine derivatives. Specifically, the invention is directed to compounds according to Formula (Iar): (Iar) wherein Yar, X1ar, X2ar, R1ar, R2ar, R3ar, R4ar and R5ar are as defined herein; or a pharmaceutically acceptable salt or prodrug thereof. The compounds of the invention are selective inhibitors of DNMT1 and can be useful in the treatment of cancer, pre-cancerous syndromes, beta hemoglobinopathy disorders, sickle cell disease, sickle cell anemia, and beta thalassemia, and diseases associated with DNMT1 inhibition. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting DNMT1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

  该发明涉及取代吡啶衍生物。具体而言，该发明涉及符合以下式（Iar）的化合物：（Iar）其中Yar、X1ar、X2ar、R1ar、R2ar、R3ar、R4ar和R5ar如本文所定义；或其药学上可接受的盐或前药。该发明的化合物是DNMT1的选择性抑制剂，可用于治疗癌症、癌前综合征、β血红蛋白病、镰状细胞病、镰状细胞贫血、β地中海贫血以及与DNMT1抑制相关的疾病。因此，该发明进一步涉及包含该发明化合物的药物组合物。该发明还进一步涉及使用该发明化合物或包含该发明化合物的药物组合物抑制DNMT1活性和治疗相关疾病的方法。
• Treatment of acute myeloid leukemia with indolinone compounds
  申请人：SUGEN, Inc.

  公开号：US20030130280A1

  公开（公告）日：2003-07-10

  A method of treating acute myeloid leukemia in patient positive for FLT-3-ITD is described. The treatment is accomplished by administration of a compound of Formula I or II as defined herein.

  描述了一种治疗FLT-3-ITD阳性患者急性髓系白血病的方法。该治疗通过给予本文中定义的I或II式化合物来实现。
• Treatment of excessive osteolysis with indolinone compounds
  申请人：SUGEN, INC.

  公开号：US20040209937A1

  公开（公告）日：2004-10-21

  Compounds of Formula I and Formula II, as described herein, are useful for treating excessive osteolysis, by inhibiting M-CSF mediated osteoclast development. The compounds also are useful for inhibiting phosphorylation of CSF1R, and for treating cancers that express CSF1R.

  本文描述的式I和式II的化合物可用于治疗过度骨溶解，通过抑制M-CSF介导的破骨细胞发育。这些化合物还可用于抑制CSF1R的磷酸化，并用于治疗表达CSF1R的癌症。
• [EN] INDOLE DERIVATIVE AND USE FOR TREATMENT OF CANCER<br/>[FR] DÉRIVÉ D'INDOLE ET USAGE POUR LE TRAITEMENT DU CANCER
  申请人：TAKEDA PHARMACEUTICAL

  公开号：WO2005118587A1

  公开（公告）日：2005-12-15

  The present invention relates to a compound represented by the formula (I’) wherein A is a benzene ring optionally having substituents, R1, R2a and R3 are each a hydrogen atom, a hydrocarbon group optionally having substituents or a heterocyclic group optionally having substituents, R1 and R2a may form a ring via X, when R1 and R2a form a ring via X, R1 and R2a are each a bond or a divalent C1-5 acyclic hydrocarbon group optionally having substituents, and X is a bond, an oxygen atom, an optionally oxidized sulfur atom or an imino group optionally having a substituent, provided that R1, R2a and X are not bonds at the same time, or a salt thereof, and an agent for inhibiting kinase (phosphorylation enzyme), which contains this compound or a prodrug thereof. The compound of the present invention has an inhibitory activity against kinase such as a vascular endothelial growth factor receptor (VEGFR) and the like, and is useful as an agent for the prophylaxis or threatment of cancer and the like.

  本发明涉及一种由式(I')表示的化合物，其中A是一个苯环，可选地具有取代基，R1、R2a和R3分别是氢原子，可选地具有取代基的碳氢基团或可选地具有取代基的杂环基团，R1和R2a可以通过X形成环，当R1和R2a通过X形成环时，R1和R2a分别是键或可选地具有取代基的二价C1-5非环烃基团，X是键，氧原子，可选地氧化的硫原子或可选地具有取代基的亚胺基团，前提是R1、R2a和X不同时为键，或其盐，以及含有该化合物或其前药的抑制激酶（磷酸化酶）的药剂。本发明的化合物对激酶如血管内皮生长因子受体（VEGFR）等具有抑制活性，并可用作预防或治疗癌症等疾病的药剂。
• NOVEL PREPARATION PROCESS
  申请人：Schnaubelt Juergen

  公开号：US20110087021A1

  公开（公告）日：2011-04-14

  A process for preparing compounds of the formula (I) in which R 1 and R 2 are as defined in the description.

  一种制备化合物（I）的方法，其中R1和R2如描述中所定义。