tert-butyl 3-(2-amino-2-oxoethyl)azetidine-1-carboxylate | 898271-19-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 氮杂环丁烷
• 英文名称: tert-butyl 3-(2-amino-2-oxoethyl)azetidine-1-carboxylate
• CAS: 898271-19-7
• 化学式: C₁₀H₁₈N₂O₃
• 分子量: 214.265
• InChiKey: SFRFJBXTSQLWBB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0
• 重原子数：
  15
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.8
• 拓扑面积：
  72.6
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  tert-butyl 3-(2-amino-2-oxoethyl)azetidine-1-carboxylate 在 dimethyl sulfide borane 、 碘 、 N,N-二异丙基乙胺 作用下， 以 四氢呋喃 、 甲醇 为溶剂， 反应 6.0h， 以53.5%的产率得到1-叔丁氧羰基-3-氨基乙基氮杂
  参考文献：
  名称：

  WO2006/73366

  摘要：

  公开号：
• 作为产物：
  描述：

  N-Boc-3-氮杂环丁烷乙酸 在 benzotriazol-1-yloxyl-tris-(pyrrolidino)-phosphonium hexafluorophosphate 、 氨 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 以57.5%的产率得到tert-butyl 3-(2-amino-2-oxoethyl)azetidine-1-carboxylate
  参考文献：
  名称：

  WO2006/73366

  摘要：

  公开号：

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。
• Non-Anilinic Derivatives of Isothiazol-3(2H)-one 1,1-Dioxides as Liver X Receptor Modulators
  申请人：Broo Anders

  公开号：US20090005353A1

  公开（公告）日：2009-01-01

  The present invention relates to certain novel compounds of the formula (I) to processes for preparing such compounds, to their the utility in modulation of nuclear hormone receptors Liver X Receptor (LXR) α (NR1H3) and/or β (NR1H2) and in treating and/or preventing clinical conditions including cardiovascular diseases such as atherosclerosis; inflammatory diseases, Alzheimer's disease, lipid disorders (dyslipidemias) whether or not associated with insulin resistance, type 2 diabetes and other manifestations of the metabolic syndrome, to methods for their therapeutic use and to pharmaceutical compositions containing them.

  本发明涉及公式（I）的某些新化合物，以及制备这些化合物的方法，它们在调节核激素受体肝X受体（LXR）α（NR1H3）和/或β（NR1H2）以及治疗和/或预防包括心血管疾病如动脉粥样硬化，炎症性疾病，阿尔茨海默病，脂质紊乱（无论是否伴随胰岛素抵抗），2型糖尿病和代谢综合征的其他表现在内的临床疾病中的用途，以及它们的治疗使用方法和含有它们的制药组合物。
• Non-anilinic derivatives of isothiazol-3(2H)-one 1,1-dioxides as liver X receptor modulators
  申请人：AstraZeneca AB

  公开号：US07960380B2

  公开（公告）日：2011-06-14

  The present invention relates to certain novel compounds of the formula (I) to processes for preparing such compounds, to their the utility in modulation of nuclear hormone receptors Liver X Receptor (LXR) α (NR1H3) and/or β (NR1H2) and in treating and/or preventing clinical conditions including cardiovascular diseases such as atherosclerosis; inflammatory diseases, Alzheimer's disease, lipid disorders (dyslipidemias) whether or not associated with insulin resistance, type 2 diabetes and other manifestations of the metabolic syndrome, to methods for their therapeutic use and to pharmaceutical compositions containing them.

  本发明涉及某些新型化合物(I)的公式，以制备这些化合物的过程，以及它们在调节核激素受体肝X受体(LXR)α (NR1H3)和/或β (NR1H2)以及治疗和/或预防包括心血管疾病（如动脉粥样硬化）、炎症性疾病、阿尔茨海默病、脂质紊乱（无论是否与胰岛素抵抗有关）、2型糖尿病和代谢综合征的其他表现在内的临床病症方面的用途，以及它们的治疗用途的方法和含有它们的制药组合物。
• Non-Anilinic Derivatives Of Isothiazol-3(2H)-one 1,1-Dioxides As Liver X Receptor Modulators
  申请人：Broo Anders

  公开号：US20100227847A1

  公开（公告）日：2010-09-09

  The present invention relates to certain novel compounds of the formula (I) to processes for preparing such compounds, to their the utility in modulation of nuclear hormone receptors Liver X Receptor (LXR) α (NR1H3) and/or β (NR1H2) and in treating and/or preventing clinical conditions including cardiovascular diseases such as atherosclerosis; inflammatory diseases, Alzheimer's disease, lipid disorders (dyslipidemias) whether or not associated with insulin resistance, type 2 diabetes and other manifestations of the metabolic syndrome, to methods for their therapeutic use and to pharmaceutical compositions containing them.

  本发明涉及公式（I）的某些新化合物，以及制备这些化合物的方法，它们在调节核激素受体肝X受体（LXR）α（NR1H3）和/或β（NR1H2）以及治疗和/或预防临床疾病方面具有用途，包括心血管疾病（如动脉粥样硬化），炎症性疾病，阿尔茨海默病，脂质代谢紊乱（无论是否与胰岛素抵抗有关），2型糖尿病和代谢综合征的其他表现，以及它们的治疗用途的方法和包含它们的制药组合物。
• Substituted pyridines as inhibitors of DNMT1
  申请人：GlaxoSmithKline Intellectual Property Development Limited

  公开号：US10975056B2

  公开（公告）日：2021-04-13

  The invention is directed to substituted pyridine derivatives. Specifically, the invention is directed to compounds according to Formula (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.

  本发明涉及取代的吡啶衍生物。具体地说，本发明是针对符合式（Iar）的化合物： 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原药。 本发明的化合物是 DNMT1 的选择性抑制剂，可用于治疗癌症、癌前综合征、β 血红蛋白病疾病、镰状细胞病、镰状细胞性贫血和β 地中海贫血以及与 DNMT1 抑制相关的疾病。因此，本发明进一步涉及包含本发明化合物的药物组合物。本发明还进一步涉及使用本发明化合物或包含本发明化合物的药物组合物抑制 DNMT1 活性和治疗与之相关疾病的方法。