1,2,3,4-tetrahydro-benzo[4,5]thieno[3,2-c]pyridine | 260273-74-3

• 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: 1,2,3,4-tetrahydro-benzo[4,5]thieno[3,2-c]pyridine
• 英文别名: 1,2,3,4-Tetrahydro-benzo[4,5]thieno[3,2-c]pyridin；1,2,3,4-tetrahydro-benzothieno[3,2-c]pyridine；1,2,3,4-Tetrahydro-benzo[4,5]thieno[3,2-c]pyridine；1,2,3,4-tetrahydro-[1]benzothiolo[3,2-c]pyridine
• CAS: 260273-74-3
• 化学式: C₁₁H₁₁NS
• 分子量: 189.281
• InChiKey: STIFURPZTKYNJV-UHFFFAOYSA-N

物化性质

• 沸点：
  165-167 °C(Press: 4-5 Torr)
• 密度：
  1.214±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  13
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.27
• 拓扑面积：
  40.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  1,2,3,4-tetrahydro-benzo[4,5]thieno[3,2-c]pyridine 在 palladium on activated charcoal 作用下， 生成 benzo[4,5]thieno[3,2-c]pyridine
  参考文献：
  名称：

  Thianaphtheno [3,2-c]pyridine and Certain Derivatives

  摘要：

  DOI：

  10.1021/ja01099a054
• 作为产物：
  描述：

  苯并噻吩-2-羧酸 在 喹啉 、 盐酸 、 正丁基锂 、 铜 、 三乙胺 、 sodium iodide 作用下， 以 乙醚 、 乙醇 、 氯仿 、 丙酮 为溶剂， 生成 1,2,3,4-tetrahydro-benzo[4,5]thieno[3,2-c]pyridine
  参考文献：
  名称：

  New 2-substituted 1,2,3,4-tetrahydrobenzofuro[3,2- c ]pyridine having highly active and potent central α 2 -antagonistic activity as potential antidepressants

  摘要：

  The synthesis and biological activity of a series of benzofuro[3,2-c]pyridines and a benzothieno[3,2-c]pyridine are described. These compounds exhibit high affinity for the alpha(2)-adrenoceptor, with high selectivity versus the alpha(1)-receptor. Compound 1 also shows potent in vivo central activity and has been selected for further biological and clinical evaluation. (C) 1999 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(99)00591-0

文献信息

• Tricylic delta 3-piperidines as pharmaceuticals
  申请人：Janssen Pharmaceutica N.V.

  公开号：US06352999B1

  公开（公告）日：2002-03-05

  The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Alk is C1-6alkanediyl; n is 1 or 2; X is —O—, —S—, —S(═O)— or —S(═O)2—; each R1 is independently hydrogen, halogen, C1-6alkyl, nitro, hydroxy or C1-4alkyloxy; D is an indole, a benzisoxazole, a benzisothiazole, a 2H-benzopyranone, a phenoxyphenyl, a benzamide, a benzophenone or a benzopyrimidinone having central &agr;2-adrenoceptor antagonist activity. It further relates to their preparation, pharmaceutical use and compositions.

  本发明涉及公式N-氧化物形式的化合物，其药学上可接受的加盐物和立体化学异构形式，其中Alk为C1-6烷二基；n为1或2；X为—O—、—S—、—S(═O)—或—S(═O)2—；每个R1独立地为氢、卤素、C1-6烷基、硝基、羟基或C1-4烷氧基；D为吲哚、苯并异噁唑、苯并噻唑、2H-苯并吡喃酮、苯氧苯基、苯甲酰胺、苯甲酮或具有中枢α2-肾上腺素受体拮抗活性的苯基吡啶酮。它还涉及它们的制备、药用和组合物。
• INHIBITORS OF NUCLEOPHOSMIN (NPM) AND METHODS FOR INDUCING APOPTOSIS
  申请人：Mahadevan Daruka

  公开号：US20080221146A1

  公开（公告）日：2008-09-11

  Nucleophosmin inhibitors are disclosed which inhibit the multimerization of nucleophosmin and the biological activity of nucleophosmin, such as the ability of nucleophosmin to inhibit apoptosis and inhibit cellular differentiation. These small molecule inhibitors are useful for treating diseases and disorders, such as cancer associated with dysregulated nucleophosmin expression. Methods for identifying small molecule inhibitors of nucleophosmin involving multimerization sites for nucleophosmin are also disclosed. An exemplary small molecule inhibitor of nucleophosmin is NSC348884 which has the following chemical structure:

  揭示了抑制核磷蛋白多聚化和核磷蛋白生物活性的核磷蛋白抑制剂，例如核磷蛋白抑制凋亡和抑制细胞分化的能力。这些小分子抑制剂可用于治疗与核磷蛋白表达失调相关的癌症等疾病和疾病。还披露了识别核磷蛋白小分子抑制剂的方法，涉及核磷蛋白的多聚化位点。核磷蛋白的一个示例小分子抑制剂是NSC348884，其化学结构如下：
• Benzothieno[3,2-c]pyridines as &agr;2 antagonists
  申请人：Janssen Pharmaceutica N.V.

  公开号：US06426350B1

  公开（公告）日：2002-07-30

  The present invention concerns the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein each R1 is independently hydrogen, halogen, C1-6alkyl, nitro, hydroxy or C1-4alkyloxy; Alk is C1-6alkanediyl; n is 1 or 2; p is 0, 1 or 2; D is an optionally substituted mono-, bi- or tricyclic nitrogen containing heterocycle having central &agr;2-adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and their use as a medicine.

  本发明涉及具有公式N-氧化物、药学上可接受的加合盐和其立体化学同分异构体的化合物，其中每个R1独立地表示氢、卤素、C1-6烷基、硝基、羟基或C1-4烷氧基；Alk表示C1-6烷二基；n为1或2；p为0、1或2；D为一个具有中央α2-肾上腺素能受体拮抗剂活性的可选取代的单、双或三环氮杂环。它进一步涉及它们的制备、包含它们的组合物以及它们作为药物的用途。
• Benzothieno[3,2-c]pyridines as alpha2 antagonists
  申请人：——

  公开号：US20020169178A1

  公开（公告）日：2002-11-14

  The present invention concerns the compounds of formula 1 the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein each R 1 is independently hydrogen, halogen, C 1-6 alkyl, nitro, hydroxy or C 1-4 alkyloxy; Alk is C 1-6 alkanediyl; n is 1 or 2; p is 0, 1 or 2; D is an optionally substituted mono-, bi- or tricyclic nitrogen containing heterocycle having central &agr; 2 -adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and their use as a medicine.

  本发明涉及式1化合物，其N-氧化物，药学上可接受的加合盐和其立体化学异构体，其中每个R1独立地为氢，卤素，C1-6烷基，硝基，羟基或C1-4烷氧基; Alk为C1-6烷二基; n为1或2; p为0，1或2; D为中心α2-肾上腺素受体拮抗剂具有选择性的可选取代的单、双或三环氮杂环。本发明还涉及它们的制备，包含它们的组合物以及它们作为药物的用途。
• Compounds with two fused bicyclic heteroaryl moieties as modulators of leukotriene A4 hydrolase
  申请人：Bacani Genesis

  公开号：US08399465B2

  公开（公告）日：2013-03-19

  Compounds with two fused bicyclic heteroaryl moieties and their pharmaceutical compositions, and methods of using them as leukotriene A4 hydrolase (LTA4H) modulators and for the treatment of diseases, disorders and conditions mediated by LTA4H.

  具有两个融合的双环杂环芳基基团的化合物及其制药组合物，以及将其用作白三烯A4水解酶（LTA4H）调节剂的方法，以及用于治疗由LTA4H介导的疾病，疾病和状况的方法。