2-(1-Thiophen-2-ylethylideneamino)oxyacetic acid | 30005-32-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 杂芳族化合物
• 英文名称: 2-(1-Thiophen-2-ylethylideneamino)oxyacetic acid
• CAS: 30005-32-4
• 化学式: C₈H₉NO₃S
• mdl: MFCD02600678
• 分子量: 199.23
• InChiKey: OMCSQJVGJMCOKB-UHFFFAOYSA-N

物化性质

• 沸点：
  347.7±48.0 °C(Predicted)
• 密度：
  1.30±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  13
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  87.1
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• IDO Inhibitors
  申请人：Mautino Mario

  公开号：US20110053941A1

  公开（公告）日：2011-03-03

  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 immunosuppression associated with an infectious disease, e.g., HIV-I infection, comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount a compound as described in one of the aspects described herein.

  目前提供以下方法：(a) 通过接触本文中描述的化合物的调节有效量与吲哚胺2,3-二氧化酶相互作用，从而调节吲哚胺2,3-二氧化酶的活性；(b) 治疗需要吲哚胺2,3-二氧化酶(IDO)介导的免疫抑制的患者，包括给予本文中描述的化合物的有效吲哚胺2,3-二氧化酶抑制剂量；(c) 治疗需要抑制吲哚胺-2,3-二氧化酶酶活性的医疗状况，包括给予本文中描述的化合物的有效吲哚胺2,3-二氧化酶抑制剂量；(d) 增强抗癌治疗的有效性，包括给予抗癌剂和本文中描述的化合物；(e) 治疗与癌症相关的肿瘤特异性免疫抑制，包括给予本文中描述的化合物的有效吲哚胺2,3-二氧化酶抑制剂量；(f) 治疗与传染病相关的免疫抑制，例如HIV-1感染，包括给予本文中描述的化合物的有效吲哚胺2,3-二氧化酶抑制剂量。
• NOVEL AMINOOXYAMIDE TRICYCLIC INHIBITORS OF FARNESYLPROTEIN TRANSFERASE
  申请人：SCHERING CORPORATION

  公开号：EP0991643A1

  公开（公告）日：2000-04-12
• US5945430A
  申请人：——

  公开号：US5945430A

  公开（公告）日：1999-08-31
• [EN] NOVEL AMINOOXYAMIDE TRICYCLIC INHIBITORS OF FARNESYLPROTEIN TRANSFERASE<br/>[FR] NOUVEAUX COMPOSES TRICYCLIQUES AMINOOXYAMIDE INHIBITEURS DE FARNESYL-PROTEINE TRANSFERASE
  申请人：SCHERING CORPORATION

  公开号：WO1998057965A1

  公开（公告）日：1998-12-23

  (EN) Novel aminooxyamide tricyclic compounds and pharmaceutical compositions are disclosed which are inhibitors of the enzyme, farnesyl protein transferase. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering the novel aminooxyamide tricyclic compound to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human.(FR) La présente invention concerne de nouveaux composés tricycliques aminooxyamide et des compositions pharmaceutiques acceptables qui sont des inhibiteurs de l'enzyme farsényl protéine transférase. La présente invention concerne également un procédé d'inhibition de la fonction Ras et donc d'inhibition de la croissance anormale des cellules. Le procédé consiste à administrer le nouveau composé tricyclique aminooxyamide à un système biologique. Ce procédé permet d'inhiber, en particulier, la croissance anormale des cellules chez des mammifères tels que l'homme.