1-[(3-溴-1-苯并呋喃-2-基)磺酰基]咪唑烷-2,4-二酮 | 128851-36-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑烷类
• 中文名称: 1-[(3-溴-1-苯并呋喃-2-基)磺酰基]咪唑烷-2,4-二酮
• 英文名称: 1-(3-bromobenzofuran-2-yl-sulfonyl)hydantoin
• 英文别名: 1-(3-bromobenzo[b]furan-2-ylsulfonyl)hydantoin；1-(3-bromobenzofuran-2-ylsulfonyl)hydantoin；M16209；1-[(3-bromo-2-benzofuranyl)sulfonyl]-2,4-imidazolidinedione；M-16209；1-[(3-bromo-1-benzofuran-2-yl)sulfonyl]imidazolidine-2,4-dione
• CAS: 128851-36-5
• 化学式: C₁₁H₇BrN₂O₅S
• 分子量: 359.157
• InChiKey: ZJSUDHQFSBHLDV-UHFFFAOYSA-N

物化性质

• 密度：
  1.898±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  20
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.09
• 拓扑面积：
  105
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  1-[(3-Bromo-1-benzofuran-2-yl)sulfonyl]-2-sulfanylideneimidazolidin-4-one 生成 1-[(3-溴-1-苯并呋喃-2-基)磺酰基]咪唑烷-2,4-二酮
  参考文献：
  名称：

  Hydantoin derivatives

  摘要：

  本发明涉及新型咪唑烷酮衍生物，生产所述咪唑烷酮衍生物的方法，含有至少一种所述咪唑烷酮衍生物作为醛糖还原酶抑制剂的药物组合物，以及在合成所述咪唑烷酮衍生物中的新型中间化合物。本发明基于选择一种咪唑烷酮，该咪唑烷酮通过磺酰基与咪唑烷酮骨架的1位上的各种取代基结合。本发明的化合物对醛糖还原酶具有强烈的抑制活性。这些化合物对于治疗和/或预防基于多元醇代谢产物积累的各种糖尿病并发症非常有用。

  公开号：

  US05004751A1

文献信息

• [EN] ARYL DICARBOXAMIDES<br/>[FR] ARYL-DICARBOXAMIDES
  申请人：APPLIED RESEARCH SYSTEMS

  公开号：WO2005011685A1

  公开（公告）日：2005-02-10

  The present invention is related to aryl dicarboxamides of formula (I) and use thereof for the treatment and/or prevention of obesity and/or metabolic disorders mediated by insulin resistance or hyperglycernia, comprising diabetes type I and/or II, inadequate glucose tolerance, insulin resistance, hyperlipidemia, hypertriglyceridemia, hypercholes-terolemia, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of aryl dicarboxamides of formula (I) to modulate, notably to inhibit the activity of PTPs. A is an airninocarbonyl moiety; Cy is an aryl, heteroaryl, aryl-heteroaryl, heteroaryl-aryl, aryl-aryl, cycloalkyl or heterocycle group; n is either 0 or 1; R1 and R2 are independently from each other is selected from the group consisting of hydrogen or C1-C6-alkyl; R4 and R5 are each independently from each other selected from the group consisting of H, hydroxy, C1-C6 alkyl, carboxy, C1-C6 alkoxy, C1-C3 alkyl carboxy, C2-C3 alkenyl carboxy, C2-C3 alkynyl carboxy, amino or R4 and R5 may form an unsaturated or saturated heterocyclic ring, whereby at least one of R4 or R5 is not a hydrogen or C1-C6 alkyl.

  本发明涉及式(I)的芳基二羧酰胺及其用于治疗和/或预防肥胖和/或由胰岛素抵抗或高血糖介导的代谢紊乱的使用，包括I型和/或II型糖尿病、葡萄糖耐量不足、胰岛素抵抗、高脂血症、高甘油三酯血症、高胆固醇血症、多囊卵巢综合征(PCOS)。特别是，本发明涉及使用式(I)的芳基二羧酰胺调节，尤其是抑制PTPs的活性。A是氨基甲酰基团；Cy是芳基、杂芳基、芳基-杂芳基、杂芳基-芳基、芳基-芳基、环烷基或杂环组；n为0或1；R1和R2独立地选自由氢或C1-C6-烷基组成的组；R4和R5各自独立地选自由H、羟基、C1-C6烷基、羧基、C1-C6烷氧基、C1-C3烷基羧基、C2-C3烯基羧基、C2-C3炔基羧基、氨基组成的组，或者R4和R5可以形成一个不饱和或饱和的杂环，其中至少R4或R5不是氢或C1-C6烷基。
• Drug comprising combination
  申请人：——

  公开号：US20030060488A1

  公开（公告）日：2003-03-27

  A TNF-&agr; inhibitor comprising an insulin sensitizer in combination with an HMG-CoA reductase inhibitor is useful as an agent for the prophylaxis or treatment of an inflammatory disease and the like.

  一种包含胰岛素增敏剂和HMG-CoA还原酶抑制剂的TNF-α抑制剂，可用作预防或治疗炎症性疾病等的药剂。
• Neovascularization inhibitors
  申请人：——

  公开号：US20030134884A1

  公开（公告）日：2003-07-17

  An angiogenesis inhibitor containing a compound represented by the formula 1 wherein R 4 is an optionally substituted hydrocarbon group and the like; Xa is a bond and the like; k is an integer of 1 to 3; Ya is an oxygen atom and the like; ring Ea is a benzene ring optionally having additional substituent(s); p is an integer of 1 to 8; R 5 is a hydrogen atom and the like; q is an integer of 0 to 6; r is 0 or 1; R 8 is a hydroxy group and the like; and R 6 and R 7 are hydrogen atoms and the like, or a salt thereof is useful as an agent for the prophylaxis or treatment of tumor and the like.

  一种含有由下式表示的化合物的血管生成抑制剂 其中R4是可选择地取代的碳氢基团等；Xa是键等；k是1到3的整数；Ya是氧原子等；环Ea是苯环，可选择地具有额外的取代基；p是1到8的整数；R5是氢原子等；q是0到6的整数；r为0或1；R8是羟基等；R6和R7是氢原子等，或其盐，可用作预防或治疗肿瘤等的药剂。
• [EN] 1,2,3-TRISUBSTITUTED ARYL AND HETEROARYL DERIVATIVES AS MODULATORS OF METABOLISM AND THE PRPPHYLAXIS AND TREATMENT OF DISORDERS RELATED THERETO SUCH AS DIABETES AND HYPERGLYCEMIA<br/>[FR] DERIVES ARYLES ET HETEROARYLES TRI-SUBSTITUES EN POSITION 1,2,3 EN TANT QUE MODULATEURS DE METABOLISME ET PROPHYLAXIE ET TRAITEMENT DE TROUBLES LIES AU METABOLISME
  申请人：ARENA PHARM INC

  公开号：WO2004065380A1

  公开（公告）日：2004-08-05

  The present invention relates to certain 1,2,3-trisubstituted aryl and heteroaryl derivatives of Fomula (Ia) that are modulators of metabolism. Accordingly, compounds of the present invention are useful in the prophylaxis or treatment of metabolic disorders and complications thereof, such as, diabetes and obesity.

  本发明涉及某些Fomula（Ia）的1,2,3-三取代芳基和杂芳基衍生物，它们是代谢调节剂。因此，本发明的化合物在预防或治疗代谢紊乱及其并发症，如糖尿病和肥胖方面是有用的。
• Alpha substituted carboxylic acids
  申请人：Su Guo Wei

  公开号：US20050187266A1

  公开（公告）日：2005-08-25

  Alpha substituted carboxylic acids of formula (I): wherein R 1 and R 2 are as defined in the specification and R 3 is wherein Y, Ar 1 , Ar 2 , Ar 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 9a , R 10 , R 11 , R 12 , R 17 , ring A, and p are as defined in the specification; pharmaceutical compositions containing effective amounts of said compounds or their salts are useful for treating PPAR, specifically PPAR α/γ related disorders, such as diabetes, dyslipidemia, obesity and inflammatory disorders.

  式(I)的α取代羧酸，其中R1和R2如规范中定义，R3为，其中Y、Ar1、Ar2、Ar3、R4、R5、R6、R7、R8、R9、R9a、R10、R11、R12、R17、环A和p如规范中定义；含有所述化合物或其盐的有效量的药物组合物对于治疗PPAR，特别是PPAR α/γ相关疾病，如糖尿病、血脂异常、肥胖和炎症性疾病是有用的。