SNX9-1 | 2447-23-6

• 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: SNX9-1
• 英文别名: 2-(5,7-dichloro-1H-indol-3-yl)ethanamine
• CAS: 2447-23-6
• 化学式: C₁₀H₁₀Cl₂N₂
• 分子量: 229.109
• InChiKey: MOPMGVMKLSZZPB-UHFFFAOYSA-N

物化性质

• 熔点：
  150 °C
• 沸点：
  406.2±40.0 °C(Predicted)
• 密度：
  1.411±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  14
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  41.8
• 氢给体数：
  2
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  二硫化碳 、 SNX9-1 、 碘甲烷 在 吡啶 、 三乙胺 作用下， 以68%的产率得到methyl 2-(5,7-dichloro-1H-indol-3-yl)ethylcarbamodithioate
  参考文献：
  名称：

  IDO inhibitors

  摘要：

  目前提供的方法包括：(a) 调节吲哚胺2,3-二氧化酶的活性，包括将吲哚胺2,3-二氧化酶与本文描述的某一方面中描述的化合物的调节有效量接触；(b) 治疗需要吲哚胺2,3-二氧化酶（IDO）介导的免疫抑制的受试者，包括给予本文描述的某一方面中描述的化合物的有效吲哚胺2,3-二氧化酶抑制量；(c) 治疗受益于吲哚胺-2,3-二氧化酶酶活性抑制的医疗状况，包括给予本文描述的某一方面中描述的化合物的有效吲哚胺2,3-二氧化酶抑制量；(d) 增强抗癌治疗的有效性，包括给予抗癌药物和本文描述的某一方面中描述的化合物；(e) 治疗与癌症相关的肿瘤特异性免疫抑制，包括给予本文描述的某一方面中描述的化合物的有效吲哚胺2,3-二氧化酶抑制量；以及(f) 治疗与传染病相关的免疫抑制，例如HIV-I感染，包括给予本文描述的某一方面中描述的化合物的有效吲哚胺2,3-二氧化酶抑制量。

  公开号：

  US10047066B2
• 作为产物：
  描述：

  3-(2-Amino-ethyl)-5,7-dichloro-1H-indole-2-carboxylic acid 以42%的产率得到
  参考文献：
  名称：

  CYBOPOB, N. N.;VINOGRAD, L. X.;TURCHIN, K. F.;ILINA, G. N.;VIGDORCHIK, M.+, XIMIYA GETEROTSIKL. SOEDIN., 1984, N 8, 1093-1100

  摘要：

  DOI：

文献信息

• IDO Inhibitors
  申请人：NewLink Genetics Corporation

  公开号：US20130289083A1

  公开（公告）日：2013-10-31

  Presently provided are methods for (a) modulating an activity of indoleamine 2,3-dioxygenase comprising contacting an indoleamine 2,3-dioxygenase with a modulation effective amount of a compound as described in one of the aspects described herein; (b) treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression in a subject in need thereof, comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; (c) treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; (d) enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent and a compound as described in one of the aspects described herein; (e) treating tumor-specific immunosuppression associated with cancer comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; and (f) treating immunsupression associated with an infectious disease, e.g., HIV-1 infection, comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount a compound as described in one of the aspects described herein.

  目前提供的方法包括：(a) 通过将一种如本文所述的化合物的调节有效量与吲哚胺2,3-双加氧酶接触来调节其活性；(b) 治疗需要抑制吲哚胺2,3-双加氧酶(IDO)介导的免疫抑制的患者，包括给予如本文所述的化合物的有效抑制吲哚胺2,3-双加氧酶的量；(c) 治疗需要抑制吲哚胺2,3-双加氧酶酶活性的医疗状况，包括给予如本文所述的化合物的有效抑制吲哚胺2,3-双加氧酶的量；(d) 增强抗癌治疗的有效性，包括给予抗癌药物和如本文所述的化合物；(e) 治疗与癌症相关的肿瘤特异性免疫抑制，包括给予如本文所述的化合物的有效抑制吲哚胺2,3-双加氧酶的量；(f) 治疗与传染病相关的免疫抑制，例如HIV-1感染，包括给予如本文所述的化合物的有效抑制吲哚胺2,3-双加氧酶的量。
• IDO INHIBITORS
  申请人：Newlink Genetics

  公开号：EP2227233B1

  公开（公告）日：2013-02-13
• CDKI pathway inhibitors as inhibitors of tumor cell growth
  申请人：Chang Bey-Dih

  公开号：US20080200531A1

  公开（公告）日：2008-08-21

  The invention provides new methods for inhibiting the CDKI pathway and specifically inhibiting tumor cell growth. The invention further provides new and specific inhibitors of tumor cell growth, as well as means for discovery of additional such inhibitors. The present inventors have surprisingly discovered that Cyclin-Dependent Kinase 3 (CDK3) is specifically required for tumor cell growth, in contrast to other members of the CDK family.
• Non-Peptidic Inhibitors of AKAP/PKA Interaction
  申请人：Klussmann Enno

  公开号：US20090176773A1

  公开（公告）日：2009-07-09

  The invention relates to non-peptidic molecules which modulate, especially inhibit, the interaction of protein kinase A (PKA) and A kinase anchor proteins (AKAP) and to a host or target organism that comprises said non-peptidic compounds or recognition molecules directed to said compounds, such as e.g. antibodies or chelating agents. The invention also relates to a pharmaceutical agent, especially for use in the treatment of diseases that are associated with a disturbance of the cAMP signal path, especially insipid diabetes, hypertonia, pancreatic diabetes, duodenal ulcer, asthma, heart failure, obesity, AIDS, edema, hepatic cirrhosis, schizophrenia and others. The invention also relates to the use of the inventive molecules.
• METHODS AND COMPOUNDS FOR THE TREATMENT OF GENETIC DISEASE
  申请人：Design Therapeutics, Inc.

  公开号：US20210238226A1

  公开（公告）日：2021-08-05

  The present disclosure relates to compounds and methods for modulating the expression of dmpk, atxn1, atxn2, atxn3, cacna1a, atxn7, ppp2r2br tbp, htt, jph3r ar, or atn1 and treating diseases and conditions in which dmpk, atxn1, atxn2, atxn3, cacna1a, atxn1, ppp2r2b, tbp, htt, jph3, ar, or atn1 plays an active role. The compound can be a transcription modulator molecule having a first terminus, a second terminus, and oligomeric backbone, wherein: a) the first terminus comprises a DNA-binding moiety capable of noncovalently binding to a nucleotide repeat sequence CAG or CTG; b) the second terminus comprises a protein-binding moiety binding to a regulatory molecule that modulates an expression of a gene comprising the nucleotide repeat sequence CAG or CTG; and c) the oligomeric backbone comprising a linker between the first terminus and the second terminus.