thieno[3,2-b]pyridine-2-sulfonamide

• 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: thieno[3,2-b]pyridine-2-sulfonamide
• 英文别名: 2-sulfamoylthieno[3,2-b]pyridine
• 化学式: C₇H₆N₂O₂S₂
• 分子量: 214.269
• InChiKey: RVOIHSVYASOEAL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  110
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  氨 在 叔丁基锂 作用下， 以 四氢呋喃 、 正己烷 、 水 、 丙酮 为溶剂， 反应 3.17h， 以24%的产率得到thieno[3,2-b]pyridine-2-sulfonamide
  参考文献：
  名称：

  [EN] ANTITUMOR BENZOYLSULFONAMIDES
  [FR] BENZOYLSULFONAMIDES ANTITUMORAUX

  摘要：

  本发明提供了化合物(I)的抗肿瘤化合物；以及抗肿瘤方法。

  公开号：

  WO2004048329A1

文献信息

• COMPOUNDS
  申请人：Nogradi Katalin

  公开号：US20100022521A1

  公开（公告）日：2010-01-28

  The present invention relates to new mGluR1 and mGluR5 receptor subtype preferring ligands of formula (I) wherein X represents a group selected from SO, SO2; Y represents a group selected from (CH 2 ) n , NH, NHCH 2 ; n is an integer of 0 to 1; Z is H or monosubstituted by alkyl, nitro, halogen, alkoxy, trifluoromethyl, cyano, amino, alkylamino, dialkylamino, aminomethyl, e alkylaminomethyl, dialkylaminomethyl, hydroxyl, alkylsulfonylamino; R 1 is an optionally substituted alkyl, cycloalkyl, phenyl, biphenyl, heterocyclyl; R 2 is an optionally substituted phenyl, heterocyclyl, or NR 3 R 4 group wherein R 3 and R 4 are independently selected from the group of hydrogen and an optionally substituted alkyl, or R 3 and R 4 together with the N atom to which they are attached form an optionally substituted C 5-7 heterocyclyl group, containing one or more heteroatom(s), or NH—CO—NR 5 R 6 group, wherein R 5 and R 6 are independently selected from the group of hydrogen and an optionally substituted alkyl, or R 5 and R 6 together with the N atom to which they are attached form an optionally substituted C 5-7 heterocyclyl group, containing one or more heteroatom(s); and/or hydrates and/or solvates and/or pharmaceutically acceptable salts thereof formed with acids or bases, to the processes for producing the same, to pharmaceutical compositions containing the same and to their use in therapy and/or prevention of pathological conditions which require the modulation of mGluR1 and mGluR5 receptors such as neurological disorders, psychiatric disorders, acute and chronic pain, neuromuscular dysfunctions of the lower urinary tract and gastrointestinal disorders.

  本发明涉及一种新的mGluR1和mGluR5受体亚型偏好配体，其化学式为(I)，其中X代表从SO、SO2中选择的一个基团；Y代表从(CH2)n、NH、NHCH2中选择的一个基团；n为0到1的整数；Z为H或者被烷基、硝基、卤素、烷氧基、三氟甲基、氰基、氨基、烷基氨基、二烷基氨基、氨甲基、烷基氨甲基、二烷基氨甲基、羟基、烷基磺酰氨基单取代；R1为可选择取代的烷基、环烷基、苯基、联苯基、杂环基；R2为可选择取代的苯基、杂环基，或者NR3R4基团，其中R3和R4分别从氢和可选择取代的烷基中选择，或者R3和R4与它们连接的N原子一起形成一个可选择取代的含有一个或多个杂原子的C5-7杂环基，或者NH—CO—NR5R6基团，其中R5和R6分别从氢和可选择取代的烷基中选择，或者R5和R6与它们连接的N原子一起形成一个可选择取代的含有一个或多个杂原子的C5-7杂环基；以及与酸或碱形成的水合物和/或溶剂合物和/或药学上可接受的盐，以及制备这些化合物的方法，包括含有这些化合物的药物组合物，以及在治疗和/或预防需要调节mGluR1和mGluR5受体的病理条件的疗法中的使用，如神经系统疾病、精神疾病、急性和慢性疼痛、下尿路神经肌肉功能障碍和胃肠道疾病。
• THIENO-PYRIDINE SULFONAMIDES DERIVATIVES THEREOF AND RELATED COMPOUNDS THAT MODULATE THE ACTIVITY OF ENDOTHELIN
  申请人：——

  公开号：US20010014684A1

  公开（公告）日：2001-08-16

  Methods, compositions, and compounds for modulating the activity of an endothelin peptide are provided. The methods use compositions that contain compounds that include those of the formula: 1 where X is selected from groups that include O, S, and NH; Y is selected from O + and N, and R 1 and R 2 are each selected independently from among alkyl, lower alkenyl, lower alkynyl, lower haloalkyl, halide, pseudohalide or H, except that R 2 is not halide. R 3 , R 4 and R 5 are selected from among groups that include hydrogen, halide, alkoxy, alkyl, haloalkyl; and R 7 is selected from groups that include (CH 2 ) r R 18 , in which r is 0 to 6 and R 18 is selected from groups that include aryl, particularly pyrimidinyl and phenyl. The methods are effected by contacting endothelin receptors with one or more of the compounds or with compositions containing one or more of the compounds prior to, simultaneously with, or subsequent to contacting the receptors with an endothelin peptide.

  本发明提供了用于调节内皮素肽活性的方法、组合物和化合物。该方法使用包含下列公式1中化合物的组合物：其中X选自包括O、S和NH的基团；Y选自O+和N，R1和R2各自独立地选自烷基、较低烯基、较低炔基、较低卤代烷基、卤素、伪卤素或H，但R2不是卤素。R3、R4和R5选自包括氢、卤素、烷氧基、烷基、卤代烷基的基团；R7选自包括(CH2)rR18的基团，其中r为0到6，R18选自包括芳基，特别是嘧啶基和苯基的基团。该方法通过在与内皮素肽接触之前、同时或之后将内皮素受体与一个或多个化合物或包含一个或多个化合物的组合物接触来实现。
• Antitumor benzoylsulfonamides
  申请人：Mader Margaret Mary

  公开号：US20060106053A1

  公开（公告）日：2006-05-18

  The present invention provides antitumor compounds of the formula (I); and antitumor methods.

  本发明提供了式(I)的抗肿瘤化合物；以及抗肿瘤方法。
• Thieno-pyridine sulfonamides derivatives thereof and related compounds that modulate the activity of endothelin
  申请人：——

  公开号：US20020028829A1

  公开（公告）日：2002-03-07

  Methods, compositions, and compounds for modulating the activity of an endothelin peptide are provided. The methods use compositions that contain compounds that include those of the formula: 1 where X is selected from groups that include O, S, and NH; Y is selected from O + and N, and R 1 and R 2 are each selected independently from among alkyl, lower alkenyl, lower alkynyl, lower haloalkyl, halide, pseudohalide or H, except that R 2 is not halide. R 3 , R 4 and R 5 are selected from among groups that include hydrogen, halide, alkoxy, alkyl, haloalkyl; and R 7 is selected from groups that include (CH 2 ),R 18 , in which r is 0 to 6 and R 18 is selected from groups that include aryl, particularly pyrmidinyl and phenyl. The methods are effected by contacting endothelin receptors with one or more of the compounds or with compositions containing one or more of the compounds prior to, simultaneously with, or subsequent to contacting the receptors with an endothelin peptide.

  提供用于调节内皮素肽活性的方法、组合物和化合物。这些方法使用含有化合物的组合物，所述化合物包括下式中的化合物：1，其中X从包括O、S和NH的基团中选择；Y从O+和N中选择，R1和R2各自独立地从烷基、较低的烯基、较低的炔基、较低的卤代烷基、卤素、伪卤素或H中选择，但R2不是卤素。R3、R4和R5从包括氢、卤素、烷氧基、烷基、卤代烷基的基团中选择；R7从包括(CH2)、R18的基团中选择，其中r为0到6，R18从包括芳基，特别是吡啶基和苯基的基团中选择。这些方法通过在接触内皮素受体之前、同时或之后使用含有一种或多种化合物的组合物与内皮素肽受体接触来实现。
• ANTITUMOR BENZOYLSULFONAMIDES
  申请人：Mader Mary Margaret

  公开号：US20090118323A1

  公开（公告）日：2009-05-07

  The present invention provides antitumor compounds of the formula (I); and antitumor methods.

  本发明提供了公式(I)的抗肿瘤化合物和抗肿瘤方法。