2-(1,4-dioxa-8-azaspiro[4,5]decan-8-yl)ethan-1-amine | 259180-76-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 氮杂螺癸烷衍生物
• 英文名称: 2-(1,4-dioxa-8-azaspiro[4,5]decan-8-yl)ethan-1-amine
• 英文别名: 1-(2-Aminoethyl)-4,4-ethylenedioxypiperidine；1,4-dioxa-8-azaspiro[4.5]decane-8-ethanamine；2-(1,4-Dioxa-8-azaspiro[4.5]decan-8-yl)ethanamine
• CAS: 259180-76-2
• 化学式: C₉H₁₈N₂O₂
• 分子量: 186.254
• InChiKey: AJMIEHWSRRZZFV-UHFFFAOYSA-N

物化性质

• 沸点：
  292.0±40.0 °C(Predicted)
• 密度：
  1.13±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -0.7
• 重原子数：
  13
• 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：
  47.7
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2-(1,4-dioxa-8-azaspiro[4,5]decan-8-yl)ethan-1-amine 、 2,6-二氯苯甲酰氯 在 N,N-二异丙基乙胺 作用下， 以 二氯甲烷 为溶剂， 生成 2,6-dichloro-N-[2-(1,4-dioxa-8-azaspiro[4.5]decan-8-yl)ethyl]benzamide
  参考文献：
  名称：

  [EN] EQUILIBRATIVE NUCLEOSIDE TRANSPORTER ENT1 INHIBITORS
  [FR] INHIBITEURS DU TRANSPORTEUR ÉQUILIBRANT DES NUCLÉOSIDES ENT1

  摘要：

  公开号：

  WO2009062990A3
• 作为产物：
  描述：

  benzyl (2-(1,4-dioxa-8-azaspiro[4.5]decan-8-yl)ethyl)carbamate 在 palladium on activated charcoal 、 氢气 作用下， 以 甲醇 为溶剂， 反应 2.0h， 以67.9%的产率得到2-(1,4-dioxa-8-azaspiro[4,5]decan-8-yl)ethan-1-amine
  参考文献：
  名称：

  [EN] COMPOUNDS USEFUL FOR INHIBITING RAF DIMERS
  [FR] COMPOSÉS UTILES POUR L'INHIBITION DE DIMÈRES DE RAF

  摘要：

  该披露提供了Formula I（公式I）（c）的化合物及其药学上可接受的盐。在此定义了A、B、C和D环以及变量RA、RB、RC、RD、L0、L1、L2和L2。Formula I的化合物和盐可用作RAF激酶二聚体的抑制剂，包括野生型和突变型BRAF激酶的二聚化。该披露包括包含Formula I的化合物或盐的药物组合物。该披露还包括治疗对BRAF二聚体或BRAF二聚化抑制剂敏感的癌症的方法，包括向需要此类治疗的患者投予Formula I的化合物或盐的治疗有效量。这些对BRAF二聚体或BRAF二聚化抑制剂敏感的癌症包括黑色素瘤、甲状腺癌、毛细胞白血病、卵巢癌、肺癌和结肠癌。

  公开号：

  WO2020176501A1

文献信息

• 1H-imidazopyridine derivatives
  申请人：Hokuriku Seiyaku Co., Ltd.

  公开号：US06518265B1

  公开（公告）日：2003-02-11

  1H-Imidazopyridine derivatives represented by the following general formula or salts thereof: wherein R1 represents hydrogen atom, hydroxyl group, an alkyl group, a cycloalkyl group, styryl group, or an aryl group; R2 represents hydrogen atom, an alkyl group, a halogen atom, hydroxyl group, amino group, a cyclic amino group, or phenoxy group; ring A represents a homocyclic or heterocyclic ring which may be substituted; R3 represents a saturated nitrogen-containing heterocyclic group; and m represents an integer of from 0 to 3. The derivatives have excellent inhibitory actions against production of TNF or IL-1 and are extremely useful as preventive or therapeutic agents for diseases in which a cytokine is mediated.

  以下是1H-咪唑吡啶衍生物的一般式或其盐：其中R1代表氢原子，羟基，烷基，环烷基，苯乙烯基或芳基；R2代表氢原子，烷基，卤原子，羟基，氨基，环氨基或苯氧基；环A代表可以被取代的同环或异环；R3代表饱和含氮杂环基团；m表示从0到3的整数。这些衍生物具有出色的抑制TNF或IL-1生成的作用，并且非常有用作为细胞因子介导的疾病的预防或治疗剂。
• 1H-IMIDAZOPYRIDINE DERIVATIVES
  申请人：HOKURIKU SEIYAKU CO., LTD.

  公开号：EP1104764A1

  公开（公告）日：2001-06-06

  1H-Imidazopyridine derivatives represented by the following general formula or salts thereof: wherein R1 represents hydrogen atom, hydroxyl group, an alkyl group, a cycloalkyl group, styryl group, or an aryl group; R2 represents hydrogen atom, an alkyl group, a halogen atom, hydroxyl group, amino group, a cyclic amino group, or phenoxy group; ring A represents a homocyclic or heterocyclic ring which may be substituted; R3 represents a saturated nitrogen-containing heterocyclic group; and m represents an integer of from 0 to 3. The derivatives have excellent inhibitory actions against production of TNF or IL-1 and are extremely useful as preventive or therapeutic agents for diseases in which a cytokine is mediated.

  由以下通式代表的 1H-咪唑吡啶衍生物或其盐： 其中 R1 代表氢原子、羟基、烷基、环烷基、苯乙烯基或芳基；R2 代表氢原子、烷基、卤素原子、羟基、氨基、环氨基或苯氧基；环 A 代表可被取代的同环或杂环；R3 代表饱和含氮杂环基；m 代表 0 至 3 的整数。这些衍生物对 TNF 或 IL-1 的产生具有极佳的抑制作用，可作为细胞因子介导的疾病的预防或治疗药物。
• EQUILIBRATIVE NUCLEOSIDE TRANSPORTER ENT1 INHIBITORS
  申请人：Janssen Pharmaceutica, N.V.

  公开号：EP2209790B1

  公开（公告）日：2016-02-17
• COMPOUNDS USEFUL FOR INHIBITING RAF DIMERS
  申请人：ALBERT EINSTEIN COLLEGE OF MEDICINE

  公开号：US20220265669A1

  公开（公告）日：2022-08-25

  The disclosure provides compounds of Formula I (Formula I) (c) And the pharmaceutically acceptable salts thereof. The A, B, C, and D rings and the variables R A , R B , R C , R D , L 0 , L 1 , L 2 , and L 2 , are defined herein. Compounds and salts of Formula I are useful as inhibitors of RAF kinase dimerization, including dimerization of wild type and mutant BRAF kinases. The disclosure includes pharmaceutical compositions comprising a compound or salt of Formula I. The disclosure also includes methods of treating a cancer susceptible to treatment with an inhibitor of BRAF dimers or BRAF dimerization, comprising administering a therapeutically effective amount of a compound or salt of Formula I to a patient in need of such treatment. These cancers susceptible to treatment with an inhibitor of BRAF dimers or BRAF dimerization include melanoma, thyroid cancer, hairy cell leukemia, ovarian cancer, lung cancer, and colorectal cancer.
• US6518265B1
  申请人：——

  公开号：US6518265B1

  公开（公告）日：2003-02-11