N-环丙基氧杂-3-胺 | 1340518-89-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 氧杂环丁烷
• 中文名称: N-环丙基氧杂-3-胺
• 英文名称: N-cyclopropyloxetan-3-amine
• CAS: 1340518-89-9
• 化学式: C₆H₁₁NO
• 分子量: 113.159
• InChiKey: WRHIQBUDVKMWPJ-UHFFFAOYSA-N

物化性质

• 沸点：
  174.6±33.0 °C(Predicted)
• 密度：
  1.07±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0
• 重原子数：
  8
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  21.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  3-氧杂环丁酮 、 环丙胺 在 溶剂黄146 、 三乙酰氧基硼氢化钠 作用下， 以 1,2-二氯乙烷 为溶剂， 反应 0.03h， 生成 N-环丙基氧杂-3-胺
  参考文献：
  名称：

  [EN] BICYCLIC HETEROARYL AMINE COMPOUNDS AS PI3K INHIBITORS
  [FR] COMPOSÉS AMINE HÉTÉROARYLES BICYCLIQUES UTILISÉS COMME INHIBITEURS DE LA PI3K

  摘要：

  公开了Formula (I)或其盐的化合物；其中：X为N或CH；Q1为：(i) C1、Br、I、-CN、-CH3或-CF3；(ii)从吡咯基、吡唑基、咪唑基、噁唑基、噻唑基、三唑基、噁二唑基和噻二唑基中选择的5-成员杂芳基；(iii)从吡啶基、吡啶嗪基和嘧啶基中选择的6-成员杂芳基；或(iv)从吲哚基、吡咯吡啶基、吡唑吡啶基和苯并[d]噁唑基中选择的双环杂芳基；其中所述的5-成员、6-成员和双环杂芳基中的每一个都被零至1个Ra和零至1个Rb取代；R1、R2、R3、R4、R5、R6、Ra和Rb在此处被定义。还公开了使用这些化合物作为PI3K调节剂的方法，以及包含这些化合物的药物组合物。这些化合物在治疗、预防或减缓炎症性和自身免疫性疾病方面是有用的。

  公开号：

  WO2016064957A1

文献信息

• MELT-EXTRUDED SOLID DISPERSIONS CONTAINING AN APOPTOSIS-INDUCING AGENT
  申请人：Birtalan Esther

  公开号：US20120108590A1

  公开（公告）日：2012-05-03

  A pro-apoptotic solid dispersion comprises, in essentially non-crystalline form, a Bcl-2 family protein inhibitory compound of Formula I as defined herein, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises subjecting to elevated temperature the compound of Formula I, the water-soluble polymeric carrier and the surfactant, to provide an extrudable semi-solid mixture; extruding the semi-solid mixture; and cooling the resulting extrudate to to provide a solid matrix comprising the polymeric carrier and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer or an immune or autoimmune disease.

  一种促凋亡的固态分散物包括本文所定义的化合物I公式的Bcl-2家族蛋白抑制剂，以基本非结晶形式分散在固态基质中，该基质包括（a）药学上可接受的水溶性聚合物载体和（b）药学上可接受的表面活性剂。制备这种固态分散物的过程包括将公式I的化合物、水溶性聚合物载体和表面活性剂暴露于高温下，以提供可挤出的半固体混合物；挤出半固体混合物；并冷却所得到的挤出物，以提供包含聚合物载体和表面活性剂的固态基质，并在其中分散化合物的基本非结晶形式。这种固态分散物适用于口服给予需要治疗由一个或多个抗凋亡Bcl-2家族蛋白过度表达所特征的疾病的患者，例如癌症或免疫或自身免疫性疾病。
• [EN] SOLID DISPERSIONS CONTAINING AN APOPTOSIS-INDUCING AGENT<br/>[FR] DISPERSIONS SOLIDES CONTENANT UN AGENT INDUISANT L'APOPTOSE
  申请人：ABBOTT LAB

  公开号：WO2012058392A1

  公开（公告）日：2012-05-03

  A pro-apoptotic solid dispersion comprises, in essentially non-crystalline form, a Bcl-2 family protein inhibitory compound of Formula I as defined herein, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises dissolving the compound, the polymeric carrier and the surfactant in a suitable solvent, and removing the solvent to provide a solid matrix comprising the polymeric carrier and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.

  一种促凋亡的固体分散体包括本文所定义的化合物I的Bcl-2家族蛋白抑制剂，在基本非晶态形式下分散在固体基质中，该固体基质包括（a）一种药用可接受的水溶性聚合物载体和（b）一种药用可接受的表面活性剂。制备这种固体分散体的过程包括在适当的溶剂中溶解化合物、聚合物载体和表面活性剂，并去除溶剂，以提供包含聚合物载体和表面活性剂的固体基质，并在其中分散化合物的基本非晶态形式。该固体分散体适用于口服给予需要治疗一种或多种抗凋亡Bcl-2家族蛋白过度表达的疾病的受试者，例如癌症。
• SOLID DISPERSIONS CONTAINING AN APOPTOSIS-INDUCING AGENT
  申请人：Catron Nathaniel

  公开号：US20120277210A1

  公开（公告）日：2012-11-01

  A pro-apoptotic solid dispersion comprises, in essentially non-crystalline form, a Bcl-2 family protein inhibitory compound of Formula I as defined herein, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises dissolving the compound, the polymeric carrier and the surfactant in a suitable solvent, and removing the solvent to provide a solid matrix comprising the polymeric carrier and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.

  一种促凋亡的固体分散物，其主要以非晶态形式分散在固体基质中，该基质包括以下成分：(a)一种药用可接受的水溶性聚合物载体和(b)一种药用可接受的表面活性剂，其中所述化合物为以下公式I所定义的Bcl-2家族蛋白抑制剂。制备这种固体分散物的方法包括将化合物、聚合物载体和表面活性剂溶解在适宜的溶剂中，并去除溶剂以提供包含聚合物载体和表面活性剂并在其中以基本非晶态形式分散有化合物的固体基质。该固体分散物适用于口服给予需要治疗由一个或多个抗凋亡Bcl-2家族蛋白过度表达引起的疾病，例如癌症的患者。
• [EN] MELT-EXTRUDED SOLID DISPERSIONS CONTAINING AN APOPTOSIS-INDUCING AGENT<br/>[FR] DISPERSIONS SOLIDES EXTRUDÉES EN FUSION CONTENANT UN AGENT INDUISANT L'APOPTOSE
  申请人：ABBVIE INC

  公开号：WO2012121758A1

  公开（公告）日：2012-09-13

  A pro-apoptotic solid dispersion comprises, in essentially non-crystalline form, a Bcl-2 family protein inhibitory compound of Formula I as defined herein, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises subjecting to elevated temperature the compound of Formula I, the water-soluble polymeric carrier and the surfactant, to provide an extrudable semi-solid mixture; extruding the semi-solid mixture; and cooling the resulting extrudate to to provide a solid matrix comprising the polymeric carrier and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer or an immune or autoimmune disease.

  一种促凋亡的固体分散体，其在基本非晶态形式下包含一种由以下公式定义的Bcl-2家族蛋白质抑制剂化合物，分散在包括（a）药用可接受的水溶性聚合物载体和（b）药用可接受的表面活性剂的固体基质中。制备这种固体分散体的过程包括将公式I的化合物、水溶性聚合物载体和表面活性剂置于高温下，以提供可挤出的半固体混合物；挤出半固体混合物；并冷却所得的挤出物，以提供包含聚合物载体和表面活性剂的固体基质，并在其中分散化合物的基本非晶态形式。这种固体分散体适用于口服给予需要治疗由一个或多个抗凋亡Bcl-2家族蛋白质过度表达所表征的疾病的患者，例如癌症或免疫或自身免疫性疾病。
• PYRAZOLOPYRIMIDINE COMPOUNDS AS KINASE INHIBITORS
  申请人：PRINCIPIA BIOPHARMA INC.

  公开号：US20140364410A1

  公开（公告）日：2014-12-11

  The present disclosure provides compounds of Formula (IA) and/or pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BTK, and are potentially useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer, inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and/or pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof.

  本公开提供公式（IA）的化合物和/或其药学上可接受的盐，它们是酪氨酸激酶抑制剂，特别是BTK，并且可能用于治疗通过抑制酪氨酸激酶治疗的疾病，如癌症，炎症性疾病（如关节炎）等。还提供包含这些化合物和/或药学上可接受的盐的制药组合物以及制备这些化合物和药学上可接受的盐的过程。