噻吩并[2,3-b]吡啶-4-酮(7H) | 65075-96-9

• 物质功能分类: 有机原料 - 杂环化合物
• 分子结构分类: 有机化合物 - 有机杂环化合物 - 噻吩并吡啶类
• 中文名称: 噻吩并[2,3-b]吡啶-4-酮(7H)
• 中文别名: 噻吩并[2,3-B]吡啶-4-醇
• 英文名称: 4-hydroxythieno<2,3-b>pyridine
• 英文别名: thieno[2,3-b]pyridin-4-ol；7H-thieno[2,3-b]pyridin-4-one；7H-thieno[2,3-b]pyridin-4-one
• CAS: 65075-96-9
• 化学式: C₇H₅NOS
• mdl: MFCD18802558
• 分子量: 151.189
• InChiKey: OGLNUUIOLDYMHM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  10
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  57.3
• 氢给体数：
  1
• 氢受体数：
  3

安全信息

• 海关编码：
  2934999090

反应信息

• 作为反应物：
  描述：

  噻吩并[2,3-b]吡啶-4-酮(7H) 在 双氧水 、 三氯氧磷 作用下， 以 溶剂黄146 为溶剂， 反应 28.0h， 生成 4-chlorothieno[2,3-b]pyridine 7-oxide
  参考文献：
  名称：

  Klemm,L.H.; Hartling,R., Journal of Heterocyclic Chemistry, 1976, vol. 13, p. 1197 - 1200

  摘要：

  DOI：
• 作为产物：
  描述：

  4-羟基噻吩并[3,2-B]吡啶-5-甲酸乙酯 在 sodium hydroxide 作用下， 反应 1.5h， 生成 噻吩并[2,3-b]吡啶-4-酮(7H)
  参考文献：
  名称：

  Khan,M.A.; Guarconi,A.E., Journal of Heterocyclic Chemistry, 1977, vol. 14, p. 807 - 812

  摘要：

  DOI：

文献信息

• Novel tetrahydrocarbazole derivatives having improved biological action and improved solubility as ligands of G-protein coupled receptors (GPCRs)
  申请人：Paulini Klaus

  公开号：US20060014818A1

  公开（公告）日：2006-01-19

  The present invention provides novel tetrahydrocarbazole derivatives which have improved properties and which can be employed as inhibitors of GPCRs. This results in the possibility of using the novel compounds to treat pathological conditions whose severity depends on the pathobiochemical effect of GPCRs. The compounds of the invention act in particular via an antagonistic inhibition of the LHRH receptor. The invention further provides medicaments which comprise one or more of the novel compounds as active ingredient. The medicaments are suitable in particular to be employed in an oral dosage form for a mammal, in particular a human.

  本发明提供了新颖的四氢咔唑衍生物，具有改进的性能，并可用作GPCR的抑制剂。这导致可以利用这些新型化合物来治疗病理条件，其严重程度取决于GPCR的病理生物化学效应。本发明的化合物特别通过对LHRH受体的拮抗性抑制发挥作用。本发明还提供了包含一种或多种新型化合物作为活性成分的药物。这些药物特别适合用于口服剂型，用于哺乳动物，特别是人类。
• [EN] URACIL-TYPE GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS AND METHODS RELATED THERETO<br/>[FR] ANTAGONISTES DE TYPE URACIL GONADOLIBÉRINE ET LES MÉTHODES AFFÉRENTES
  申请人：NEUROCRINE BIOSCIENCES INC

  公开号：WO2005113516A1

  公开（公告）日：2005-12-01

  Compounds having utility as GnRH receptor antagonists and for treatment of a variety of sex-hormone related conditions in both men and women. Such compounds have the following structure (I): (I) wherein R1a, R1b, R1c, R2a, R2b, R3, R4, R5, R6, R7, n and X are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of structure (I) in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

  具有作为GnRH受体拮抗剂的效用，并用于治疗男性和女性的各种与性激素相关疾病的化合物。这些化合物具有以下结构（I）：（I）其中R1a、R1b、R1c、R2a、R2b、R3、R4、R5、R6、R7、n和X如本文所定义，包括立体异构体、前药和其药用可接受盐。还公开了含有结构（I）化合物的组合物，与药用可接受载体结合，以及与使用该组合物拮抗需要该物质的受试者中的促性腺激素释放激素相关的方法。
• THIAZOLECARBOXAMIDES AND PYRIDINECARBOXAMIDE COMPOUNDS USEFUL AS PIM KINASE INHIBITORS
  申请人：Incyte Corporation

  公开号：US20140200227A1

  公开（公告）日：2014-07-17

  The present disclosure describes thiazole and pyridine carboxamide derivatives, their compositions and methods of use. The compounds inhibit the activity of the Pim kinases and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.

  本公开描述了噻唑和吡啶羧酰胺衍生物，它们的组成以及使用方法。这些化合物抑制Pim激酶的活性，并且在治疗与Pim激酶活性相关的疾病方面具有用途，例如癌症和其他疾病。
• [EN] PYRIMIDINE-2, 4-DIONE DERIVATIVES AS GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS<br/>[FR] DERIVES DE PYRIMIDINE-2, 4-DIONE UTILISES COMME ANTAGONISTES DU RECEPTEUR D'HORMONE LIBERANT DE LA GONADOTROPHINE
  申请人：NEUROCRINE BIOSCIENCES INC

  公开号：WO2005007165A1

  公开（公告）日：2005-01-27

  GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R2a, R2b, R3, R4, R5, R6 and X are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

  GnRH受体拮抗剂被披露，对男性和女性的各种与性激素相关的疾病具有治疗作用。本发明的化合物具有以下结构：其中R1a、R1b、R1c、R2a、R2b、R3、R4、R5、R6和X的定义如本文所述，包括立体异构体、前药和其药用可接受盐。还披露了含有本发明化合物的组合物与药用可接受载体的组合物，以及与在需要时对抗性腺激素释放激素的使用方法。
• Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
  申请人：Neurocrine Biosciences, Inc.

  公开号：US20030109535A1

  公开（公告）日：2003-06-12

  GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: 1 wherein A, R 1 , R 2 , R 3a , R 3b , R 4 , R 5 , R 6 , and n are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

  GnRH受体拮抗剂已被披露，对男性和女性的各种与性激素有关的疾病具有治疗作用。本发明的化合物具有以下结构：其中A、R1、R2、R3a、R3b、R4、R5、R6和n的定义如本文所述，包括立体异构体、前药和其药用可接受的盐。还披露了含有本发明化合物的组合物与药用可接受载体，以及与使用该化合物在需要的受试者中拮抗促性腺激素释放激素相关的方法。