1-(2-methoxyethyl)-1H-indol-4-amine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: 1-(2-methoxyethyl)-1H-indol-4-amine
• 英文别名: 1-(2-methoxyethyl)indol-4-amine
• 化学式: C₁₁H₁₄N₂O
• mdl: MFCD19691789
• 分子量: 190.245
• InChiKey: QTWCDCABFPLRHP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  14
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.27
• 拓扑面积：
  40.2
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  1-(2-methoxyethyl)-1H-indol-4-amine 在 sodium cyanoborohydride 、 溶剂黄146 作用下， 反应 3.0h， 以61%的产率得到1-(2-methoxyethyl)indolin-4-amine
  参考文献：
  名称：

  [EN] PYRIMIDINE DERIVATIVES AS KINASE INHIBITORS
  [FR] COMPOSÉS HÉTÉROCYCLIQUES ET LEURS UTILISATIONS

  摘要：

  公开号：

  WO2015006754A3
• 作为产物：
  描述：

  4-硝基吲哚 在 palladium on activated charcoal 、 氢气 、 caesium carbonate 作用下， 以 甲醇 、 N,N-二甲基甲酰胺 为溶剂， 反应 32.0h， 生成 1-(2-methoxyethyl)-1H-indol-4-amine
  参考文献：
  名称：

  [EN] 2,4-DIOXOTETRAHYDROPYRIMIDINYL DERIVATIVES AS DEGRONS IN PROTACS
  [FR] DÉRIVÉS DE 2,4-DIOXOTÉTRAHYDROPYRIMIDINYLE UTILISÉS COMME DÉGRONS DANS DES PROTACS

  摘要：

  The present invention provides a series of 2,4- dioxotetrahydropyrimidinyl derivatives that bind cereblon, and their application as degrons in PROTACs. Androgen receptor PROTACs containing the 2,4-dioxotetrahydropyrimidinyl containing degrons and medical uses of these PROTACS are also disclosed.

  公开号：

  WO2023180388A1

文献信息

• HETEROCYCLIC COMPOUNDS AND USES THEREOF
  申请人：ACEA BIOSCIENCES INC.

  公开号：US20150133457A1

  公开（公告）日：2015-05-14

  The present invention relates to pharmaceutical compounds, compositions and methods, especially as they are related to compositions and methods for the treatment and/or prevention of a proliferation disorder, a cancer, a tumor, an inflammatory disease, an autoimmune disease, psoriasis, dry eye or an immunologically related disease, and in some embodiments diseases or disorders related to the dysregulation of kinase such as, but not limited to, EGFR (including HER), Alk, PDGFR, BLK, BMX/ETK, FLT3(D835Y), ITK, TEC, TXK, BTK, or JAK, and the respective pathways.

  本发明涉及制药化合物、组合物和方法，特别是涉及用于治疗和/或预防增殖障碍、癌症、肿瘤、炎症性疾病、自身免疫疾病、银屑病、干眼症或免疫相关疾病的组合物和方法，以及在某些实施方式中与激酶失调相关的疾病或疾病，例如但不限于EGFR（包括HER）、Alk、PDGFR、BLK、BMX/ETK、FLT3（D835Y）、ITK、TEC、TXK、BTK或JAK及其相应的通路。
• NOVEL NICOTINAMIDE DERIVATIVE OR SALT THEREOF
  申请人：FUJIWARA Hideyasu

  公开号：US20130116430A1

  公开（公告）日：2013-05-09

  An object of the present invention is to provide to a compound and a pharmaceutical composition, which have excellent Syk-inhibitory activity. The present invention provides a nicotinamide derivative represented by the following formula (I) (wherein R 1 represents a halogen atom; R 2 represents a C 1-12 alkyl group, a C 2-12 alkenyl group, a C 2-12 alkynyl group, a C 3-8 cycloalkyl group, an aryl group, an ar-C 1-6 alkyl group or a heterocyclic group, each optionally having at least one substituent; R 3 represents an aryl group or a heterocyclic group each optionally having at least one substituent; and R 4 and R 5 each independently represent a hydrogen atom; and R 2 and R 4 may form a cyclic amino group optionally having at least one substituent together with the nitrogen atom to which they bind) or a salt thereof, and a pharmaceutical composition for use in the treatment of a Syk-related disease which comprises the nicotinamide derivative or a salt thereof.

  本发明的目的是提供一种具有优异的Syk抑制活性的化合物和制药组合物。本发明提供了一种由以下式(I)表示的烟酰胺衍生物（其中R1表示卤素原子；R2表示C1-12烷基、C2-12烯基、C2-12炔基、C3-8环烷基、芳基、芳基-C1-6烷基或杂环基，每种均可选地具有至少一个取代基；R3表示芳基或杂环基，每种均可选地具有至少一个取代基；R4和R5各自独立地表示氢原子；且R2和R4可以与它们结合的氮原子一起形成具有至少一个取代基的环状氨基团）或其盐，并且用于治疗Syk相关疾病的制药组合物包括该烟酰胺衍生物或其盐。
• 1,2,4-TRIAZINE-6-CARBOXAMIDE DERIVATIVE
  申请人：Taiho Pharmaceutical Co., Ltd.

  公开号：EP2762476A1

  公开（公告）日：2014-08-06

  The present invention provides a compound represented by the following general formula (I) or a salt thereof which has a Syk inhibitory effect (in the formula R1 represents a hydrogen atom or an optionally Ra-substituted C1-C6 alkyl group; A represents a hydrogen atom, an optionally Ra-substituted C1-C8 alkyl group, an optionally Ra-substituted C2-C6 alkenyl group, an optionally Ra-substituted C2-C6 alkynyl group, an optionally Rb-substituted C3-C10 cycloalkyl group, an optionally Rb-substituted C6-C14 aromatic hydrocarbon group, an optionally Rb-substituted 4- to 10-membered unsaturated heterocyclic group, or an optionally Rb-substituted 4-to 10-membered saturated heterocyclic group, or optionally forms a 4- to 10-membered unsaturated heterocyclic ring or a 4- to 10-membered saturated heterocyclic ring together with R1 and the nitrogen atom bonded thereto; R2 represents a hydrogen atom or an optionally Ra-substituted C1-C6 alkyl group; and B represents an optionally Rc-substituted unsaturated heterocyclic group).

  本发明提供了由下通式（I）代表的化合物或其盐，该化合物具有抑制 Syk 的作用（式中 R1 代表氢原子或任选 Ra 取代的 C1-C6 烷基；A代表氢原子、任选Ra取代的C1-C8烷基、任选Ra取代的C2-C6烯基、任选Ra取代的C2-C6炔基、任选Rb取代的C3-C10环烷基、任选Rb取代的C6-C14芳烃基、任选 Rb 取代的 4 至 10 元不饱和杂环基团，或任选 Rb 取代的 4 至 10 元饱和杂环基团，或任选与 R1 及其键合的氮原子一起形成 4 至 10 元不饱和杂环或 4 至 10 元饱和杂环；R2 代表氢原子或任选 Ra 取代的 C1-C6 烷基；以及 B 代表任选 Rc 取代的不饱和杂环基团）。
• Heterocyclic compounds and uses thereof
  申请人：ACEA BIOSCIENCES INC.

  公开号：US10562918B2

  公开（公告）日：2020-02-18

  The present invention relates to pharmaceutical compounds, compositions and methods, especially as they are related to compositions and methods for the treatment and/or prevention of a proliferation disorder, a cancer, a tumor, an inflammatory disease, an autoimmune disease, psoriasis, dry eye or an immunologically related disease, and in some embodiments diseases or disorders related to the dysregulation of kinase such as, but not limited to, EGFR (including HER), Alk, PDGFR, BLK, BMX/ETK, FLT3(D835Y), ITK, TEC, TXK, BTK, or JAK, and the respective pathways.

  本发明涉及药物化合物、组合物和方法，特别是涉及用于治疗和/或预防增殖障碍、癌症、肿瘤、炎症性疾病、自身免疫性疾病、银屑病、干眼症或免疫相关疾病的组合物和方法、干眼症或免疫相关疾病，以及在某些实施方案中与激酶失调相关的疾病或紊乱，例如但不限于表皮生长因子受体（包括 HER）、Alk、表皮生长因子受体、BLK、BMX/ETK、FLT3(D835Y)、ITK、TEC、TXK、BTK 或 JAK 以及各自的通路。
• NOVEL NICOTINAMIDE DERIVATIVES OR SALTS THEREOF
  申请人：FUJIFILM Corporation

  公开号：EP2589592B1

  公开（公告）日：2018-08-22