3-[2-(methanesulphinyl)thieno[2,3-b]pyridine-3-carbonyl]azetidine-1-carboxylic acid tert-butyl ester | 1105070-83-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 噻吩并吡啶类
• 英文名称: 3-[2-(methanesulphinyl)thieno[2,3-b]pyridine-3-carbonyl]azetidine-1-carboxylic acid tert-butyl ester
• 英文别名: Tert-butyl 3-(2-methylsulfinylthieno[2,3-b]pyridine-3-carbonyl)azetidine-1-carboxylate
• CAS: 1105070-83-4
• 化学式: C₁₇H₂₀N₂O₄S₂
• 分子量: 380.489
• InChiKey: SUQWBDXWFRZDHZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  25
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.47
• 拓扑面积：
  124
• 氢给体数：
  0
• 氢受体数：
  7

反应信息

• 作为反应物：
  描述：

  3-[2-(methanesulphinyl)thieno[2,3-b]pyridine-3-carbonyl]azetidine-1-carboxylic acid tert-butyl ester 、 2-氟-4-碘苯胺 在 lithium hexamethyldisilazane 、 水 作用下， 以 四氢呋喃 为溶剂， 反应 0.67h， 生成 3-[2-((2-fluoro-4-iodophenyl)amino)thieno[2,3-b]pyridine-3-carbonyl]azetidine-1-carboxylic acid tert-butyl ester
  参考文献：
  名称：

  [EN] THIENO-PYRIDINE DERIVATIVES AS MEK INHIBITORS
  [FR] DÉRIVÉS DE THIÉNO-PYRIDINE COMME INHIBITEURS DE MEC

  摘要：

  一系列在2-位置被取代苯胺基团取代的噻吩[2,3-b]吡啶衍生物，作为选择性抑制人类MEK（MAPKK）酶的药物，在医学上具有益处，例如在治疗炎症、自身免疫、心血管、增殖（包括肿瘤学）和疼痛条件方面。

  公开号：

  WO2009013462A1
• 作为产物：
  描述：

  3-[2-(methylsulphanyl)thieno[2,3-b]pyridine-3-carbonyl]azetidine-1-carboxylic acid tert-butyl ester 在 Oxone 作用下， 以 甲醇 、 水 为溶剂， 反应 2.0h， 生成 3-[2-(methanesulphinyl)thieno[2,3-b]pyridine-3-carbonyl]azetidine-1-carboxylic acid tert-butyl ester
  参考文献：
  名称：

  [EN] THIENO-PYRIDINE DERIVATIVES AS MEK INHIBITORS
  [FR] DÉRIVÉS DE THIÉNO-PYRIDINE COMME INHIBITEURS DE MEC

  摘要：

  一系列在2-位置被取代苯胺基团取代的噻吩[2,3-b]吡啶衍生物，作为选择性抑制人类MEK（MAPKK）酶的药物，在医学上具有益处，例如在治疗炎症、自身免疫、心血管、增殖（包括肿瘤学）和疼痛条件方面。

  公开号：

  WO2009013462A1

文献信息

• THIENO-PYRIDINE DERIVATIVES AS MEK INHIBITORS
  申请人：Johnson James Andrew

  公开号：US20100179124A1

  公开（公告）日：2010-07-15

  A series of thieno[2,3-b]pyridine derivatives which are substituted in the 2-position by a substituted anilino moiety, being selective inhibitors of human MEK (MAPKK) enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, proliferative (including oncological) and nociceptive conditions.

  一系列在2位被取代的苯胺基团取代的噻吩[2,3-b]吡啶衍生物，是人类MEK (MAPKK)酶的选择性抑制剂，在医学上具有益处，例如在治疗炎症、自身免疫、心血管、增殖性（包括肿瘤）和疼痛性疾病方面。
• BIOMAKER COMPOSITION FOR DETECTING DIABETIC RETINOPATHY AND DIAGNOSTIC KIT THEREFOR
  申请人：Kim Young-Soo

  公开号：US20100179307A1

  公开（公告）日：2010-07-15

  The present invention provides a biomarker composition for detecting diabetic retinopathy comprising at least one protein selected from the group consisting of proteins as set forth in SEQ ID NOS: 1 to 169. And also, the present invention provides a kit for diagnosing diabetic retinopathy, comprising a molecule specifically binding to at least one protein selected from the group consisting of proteins as set forth in SEQ ID NOS: 1 to 169. It has been newly found that 105 proteins as set forth in SEQ ID NOS: 1 to 105 are significantly over-expressed in the vitreous humors obtained from PDR patients, while 64 proteins as set forth in SEQ ID NOS: 106 to 169 are significantly over-expressed in those obtained from normal people. Therefore, the proteins can be used for biomarker capable of detecting diabetic retinopathy. The biomarker can provide fundamental information in researching vitreoretinal disorders, such as diabetic retinopathy. Especially, the newly found proteins may be applied to a kit for diagnosing diabetic retinopathy with a molecule specifically binding thereto, e.g., a monoclonal antibody. And also, it has been newly found that the levels of thyroxine-binding globulin precursor (TBG) in both vitreous and plasma of PDR and NPDR states and in plasma of diabetes mellitus state, are outstandingly higher than in non-diabetic control (MH or normal control). Therefore, TBG may be applied to a diabetes mellitus biomarker, and a kit for diagnosing diabetes mellitus with a molecule specifically binding thereto.
• US8350037B2
  申请人：——

  公开号：US8350037B2

  公开（公告）日：2013-01-08