3-thienylboric acid

• 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: 3-thienylboric acid
• 英文别名: 3-Thiopheneboric acid；thiophene-3-boric acid；thiophen-3-yloxyboronic acid
• 化学式: C₄H₅BO₃S
• 分子量: 143.959
• InChiKey: IDSWJMDPKPOHRX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.1
• 重原子数：
  9
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  77.9
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  3-thienylboric acid 、 4-溴-3-硝基苯甲酸甲酯 在 四(三苯基膦)钯 、 sodium carbonate 作用下， 以 1,4-二氧六环 、 水 为溶剂， 反应 8.0h， 以85.1%的产率得到methyl 3-nitro-4-(thiophen-3-yl)benzoate
  参考文献：
  名称：

  PHENYLUREA DERIVATIVES AS ISOCITRATE DEHYDROGENASE 2 INHIBITORS FOR TREATING CANCER

  摘要：

  公开号：

  EP3330263B1
• 作为产物：
  描述：

  3-溴噻吩 、 正丁基锂 、 硼酸三异丙酯 在 盐酸 作用下， 以 四氢呋喃 、 正己烷 为溶剂， 以80%的产率得到3-thienylboric acid
  参考文献：
  名称：

  Thienyl-, furyl- and pyrrolyl sulfonamides and derivatives thereof that

  摘要：

  提供了噻吩基、呋喃基和吡咯基磺酰胺以及调节或改变内皮素家族肽活性的方法。具体来说，提供了N-(异噁唑基)噻吩磺酰胺、N-(异噁唑基)呋喃磺酰胺和N-(异噁唑基)吡咯磺酰胺，以及使用这些磺酰胺通过将其与受体接触来抑制内皮素肽与内皮素受体结合的方法。还提供了通过给予这些磺酰胺或其前药的有效量来治疗内皮素介导的疾病的方法，这些磺酰胺或其前药可以抑制或增加内皮素的活性。

  公开号：

  US05594021A1

文献信息

• THERAPEUTIC AGENT FOR DIABETES
  申请人：Japan Tobacco Inc.

  公开号：EP0885869A1

  公开（公告）日：1998-12-23

  A therapeutic agent for diabetes, which comprises a compound of the formula [I] wherein Xis a group of the formula wherein R4 and R5 are the same or different and each is a hydrogen atom, an optionally substituted alkyl having 1 to 5 carbon atoms and the like, and R6 is a hydrogen atom or an amino-protecting group; R1 is an optionally substituted alkyl having 1 to 5 carbon atoms, an optionally substituted alkenyl having 2 to 6 carbon atoms and the like, R2 is a hydrogen atom, an optionally substituted alkyl having 1 to 5 carbon atoms and the like, R2' is a hydrogen atom, and R3 is an optionally substituted alkyl having 1 to 5 carbon atoms and the like, a prodrug thereof, a pharmaceutically acceptable salt thereof, a hydrate thereof and a solvate thereof. The compound of the present invention shows superior blood sugar decreasing action on the state of hyperglycemia, but does not affect the blood sugar when it is in the normal range or in the hypoglycemic state, which means that it is free of serious side effects such as hypoglycemia. Therefore, the compound of the present invention is useful as a therapeutic drug for diabetes and also useful as a preventive of the chronic complications of diabetes.

  用于治疗糖尿病的疗法剂，包括公式[I]的化合物 其中 X是公式的组 其中R4和R5相同或不同，每个都是氢原子，可选地取代的具有1至5个碳原子的烷基等等，R6是氢原子或氨基保护基团；R1是具有1至5个碳原子的可选取代烷基，具有2至6个碳原子的可选取代烯基等等，R2是氢原子，具有1至5个碳原子的可选取代烷基等等，R2'是氢原子，R3是具有1至5个碳原子的可选取代烷基等等，其前药，药用可接受盐，水合物和溶剂化物。 本发明的化合物在血糖升高状态下表现出优越的降血糖作用，但在正常范围或低血糖状态下不影响血糖，这意味着它没有低血糖等严重副作用。因此，本发明的化合物作为治疗糖尿病的药物很有用，也用作预防糖尿病慢性并发症。
• Thienyl-, furyl- and pyrrolyl-sulfonamides and derivatives thereof that
  申请人：Texas Biotechnology Corporation

  公开号：US05962490A1

  公开（公告）日：1999-10-05

  Thienyl-, furyl- and pyrrolyl-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)-furylsulfonamides and N-(isoxazolyl)pyrrolylsulfonamides and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided.

  提供了噻吩基、呋喃基和吡咯基磺酰胺以及用于调节或改变内皮素肽家族活性的方法。特别是，提供了N-(异恶唑基)噻吩磺酰胺、N-(异恶唑基)呋喃磺酰胺和N-(异恶唑基)吡咯磺酰胺以及使用这些磺酰胺通过将受体与磺酰胺接触来抑制内皮素肽与内皮素受体结合的方法。还提供了通过给予有效量的一个或多个这些磺酰胺或其前药来治疗内皮素介导的疾病的方法，这些磺酰胺或其前药抑制或增加内皮素的活性。
• Thienyl-, furyl- and pyrrolyl sulfonamides and derivatives thereof that
  申请人：Texas Biotechnology Corporation

  公开号：US05594021A1

  公开（公告）日：1997-01-14

  Thienyl-, furyl- and pyrrolyl-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)furylsulfonamides and N-(isoxazolyl)pyrrolylsulfonamides and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided.

  提供了噻吩基、呋喃基和吡咯基磺酰胺以及调节或改变内皮素家族肽活性的方法。具体来说，提供了N-(异噁唑基)噻吩磺酰胺、N-(异噁唑基)呋喃磺酰胺和N-(异噁唑基)吡咯磺酰胺，以及使用这些磺酰胺通过将其与受体接触来抑制内皮素肽与内皮素受体结合的方法。还提供了通过给予这些磺酰胺或其前药的有效量来治疗内皮素介导的疾病的方法，这些磺酰胺或其前药可以抑制或增加内皮素的活性。
• Sulfonamides and derivatives thereof that modulate the activity of
  申请人：Texas Biotechnology Corporation

  公开号：US05571821A1

  公开（公告）日：1996-11-05

  Sulfonamides and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided. The sulfonamides have formula I: ##STR1## in which Ar.sup.1 is a 3- or 5-isoxazolyl and Ar.sup.2 is selected from among alkyl, including straight and branched chains, aromatic rings, fused aromatic rings and heterocyclic rings, including 5-membered heterocycles with one, two or more heteroatoms and fused ring analogs thereof and 6-membered rings with one, two or more heteroatoms and fused ring analogs thereof. Ar.sup.2 is preferably thiophenyl, furyl, pyrrolyl, naphthyl, and phenyl. Compounds in which Ar.sup.1 is a 4-halo-substituted isoxazole are more active than the corresponding alkyl-substituted compound and compounds in which Ar.sup.1 is substituted at this position with a higher alkyl tend to exhibit greater affinity for ET.sub.B receptors than the corresponding lower alkyl-substituted compound.

  提供了一种使用磺胺类化合物抑制内皮素肽与内皮素受体结合的方法，该方法是通过将磺胺类化合物与受体接触实现的。还提供了一种治疗内皮素介导疾病的方法，该方法是通过给予一种或多种有效量的磺胺类化合物或其前药，该化合物或前药能够抑制或增加内皮素的活性。磺胺类化合物的化学式为I：##STR1## 其中Ar.sup.1是3-或5-异恶唑基，Ar.sup.2选自烷基，包括直链和支链，芳香环，融合的芳香环和杂环，包括带有一个、两个或多个杂原子的5-成员杂环和其融合环的类似物以及带有一个、两个或多个杂原子的6-成员环和其融合环的类似物。Ar.sup.2优选为噻吩基，呋喃基，吡咯基，萘基和苯基。其中，Ar.sup.1为4-卤代异恶唑基的化合物比相应的烷基取代化合物更活性，而Ar.sup.1在该位置上取代较高烷基的化合物往往表现出比相应的较低烷基取代化合物更大的亲和力ET.sub.B受体。
• N,N-SUBSTITUTED CYCLIC AMINE DERIVATIVES
  申请人：Eisai Co., Ltd.

  公开号：EP1099692B1

  公开（公告）日：2006-05-03