2-噻吩磺酰氯，5-[（1,3-二氢-1,3-二氧代-2H-异吲哚-2-基）甲基]- | 332361-07-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 异吲哚及其衍生物
• 中文名称: 2-噻吩磺酰氯，5-[（1,3-二氢-1,3-二氧代-2H-异吲哚-2-基）甲基]-
• 英文名称: 5-phthalimidomethyl-thiophene-2-sulfonyl chloride
• 英文别名: 5-Phthalimidomethyl-thiophen-2-sulfonylchlorid；5-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl]thiophene-2-sulfonyl chloride；5-(1,3-Dioxo-1,3-dihydro-isoindol-2-ylmethyl)-thiophene-2-sulfonyl chloride；5-[(1,3-Dioxoisoindol-2-yl)methyl]thiophene-2-sulfonyl chloride
• CAS: 332361-07-6
• 化学式: C₁₃H₈ClNO₄S₂
• 分子量: 341.796
• InChiKey: KZRZSNJPWGKGQU-UHFFFAOYSA-N

物化性质

• 熔点：
  147-147.5 °C
• 沸点：
  516.8±45.0 °C(Predicted)
• 密度：
  1.651±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  21
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.08
• 拓扑面积：
  108
• 氢给体数：
  0
• 氢受体数：
  5

安全信息

• 海关编码：
  2934999090

SDS

MSDS英文版

反应信息

• 作为反应物：
  描述：

  2-噻吩磺酰氯，5-[（1,3-二氢-1,3-二氧代-2H-异吲哚-2-基）甲基]- 在 碳酸氢钠 、 sodium sulfite 作用下， 生成 5-phthalimidomethyl-thiophene-2-sulfinic acid
  参考文献：
  名称：

  潜在的噻吩化学疗法。第三部分 一些5-取代的2-噻吩基硫醚和砜

  摘要：

  DOI：

  10.1039/jr9540000237
• 作为产物：
  描述：

  2-(thiophen-2-ylmethyl)isoindoline-1,3-dione 在 氯磺酸 作用下， 以 二氯甲烷 为溶剂， 以67%的产率得到2-噻吩磺酰氯，5-[（1,3-二氢-1,3-二氧代-2H-异吲哚-2-基）甲基]-
  参考文献：
  名称：

  WO2007/93557

  摘要：

  公开号：

文献信息

• Pharmaceutically active sulfonyl hydrazide derivatives
  申请人：Applied Research Systems ARS Holding N.V.

  公开号：EP1088822A1

  公开（公告）日：2001-04-04

  The present invention is related to sulfonyl hydrazide derivatives according to formula I with its geometrical isomers, in an optically active form as enantiomers, diastereomers, as well as in the form of racemates, as well as pharmaceutically acceptable salts thereof, wherein Ar1 and Ar2 are independently from each other an unsubstituted or substituted aryl or heteroaryl group, X1 and X2 are independently from each other O or S; R1, R2, R3 are independently from each other hydrogen or a C1-C6-alkyl substituent or R1 forms a substituted or unsubstituted 5-6-membered saturated or unsaturated ring with Ar1; or R2 and R3 form a substituted or unsubstituted 5-6-membered saturated or unsaturated ring; n is an integer from 0 to 5; G is selected from a group comprising or consisting of an unsubstituted or substituted 4-8-membered heterocycle containing at least one heteroatom, or G is a substituted or unsubstituted C1-C6-alkyl group; for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such sulfonyl hydrazide derivatives. Said sulfonyl hydrazide derivatives are efficient modulators of the JNK pathway, they are in particular efficient inhibitors of JNK 2 and 3. The present invention is furthermore related to novel sulfonyl hydrazide derivatives as well as to methods of their preparation.

  本发明涉及按照式I的磺酰基腙衍生物及其几何异构体，以对映体、二对映体的光学活性形式，以及它们的盐的药学上可接受的形式，其中Ar1和Ar2分别独立地是未取代或取代的芳基或杂环芳基，X1和X2分别独立地是O或S；R1、R2、R3分别独立地是氢或C1-C6-烷基取代基，或R1与Ar1形成取代或未取代的5-6元饱和或不饱和环；或R2和R3形成取代或未取代的5-6元饱和或不饱和环；n是0到5的整数；G选自包含或仅包含至少一个杂原子的未取代或取代的4-8元杂环的群，或G是取代或未取代的C1-C6烷基基团；用作药学活性化合物，以及含有这种磺酰基腙衍生物的制药配方。所述磺酰基腙衍生物是JNK途径的高效调节剂，特别是JNK 2和3的高效抑制剂。本发明还涉及新型磺酰基腙衍生物以及其制备方法。
• Substituted methylene amide derivatives as modulators of protein tyrosine phosphatases(ptps)
  申请人：Swinnen Dominique

  公开号：US20050124656A1

  公开（公告）日：2005-06-09

  The present invention is related to substituted methylene amide derivatives of formula (I) and use thereof for the treatment and/or prevention of metabolic disorders mediated by insulin resistance or pyperglycemia, comprising diabetes type I and/or II, inadequate glucose tolerance, insulin resistance, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, obesity, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of substituted methylene amide derivatives of formula (I) to modulate, notably to inhibit the activity of PTPs. Also the present invention relates to a method of treating diabetes type II, obesity and to regulate the appetite of mammals. The present invention is furthermore related to novel substituted methylene amide derivatives and method of preparation thereof. Formula (I).

  本发明涉及公式（I）的取代亚甲基酰胺衍生物及其用于治疗和/或预防由胰岛素抵抗或高血糖引起的代谢障碍，包括1型和/或2型糖尿病、不足的葡萄糖耐受性、胰岛素抵抗、高脂血症、高三酰甘油血症、高胆固醇血症、肥胖症、多囊卵巢综合症（PCOS）。特别是，本发明涉及使用公式（I）的取代亚甲基酰胺衍生物来调节，尤其是抑制PTP的活性。本发明还涉及一种治疗2型糖尿病、肥胖症和调节哺乳动物食欲的方法。此外，本发明还涉及新的取代亚甲基酰胺衍生物及其制备方法。公式（I）。
• PHARMACEUTICALLY ACTIVE SULFONYL HYDRAZIDE DERIVATIVES
  申请人：ARKINSTALL Stephen

  公开号：US20090005426A1

  公开（公告）日：2009-01-01

  Sulfonyl hydrazide compounds according to formula I geometrical isomers thereof, optically active enantiomers thereof, diastereomers thereof, racemates thereof, and/or pharmaceutically acceptable salts thereof are useful in method for treating a neuronal disorder, an autoimmune disease, a cardiovascular disease, or cancer in a patient in need of such treatment.

  根据I式的磺酰肼化合物及其几何异构体、光学活性对映体、差向异构体、外消旋体和/或药学上可接受的盐，在治疗神经性疾病、自身免疫性疾病、心血管疾病或癌症的方法中，对于需要此类治疗的患者是有用的。
• Sulfonamide Derivatives for the Treatment of Bacterial Infections
  申请人：Gonzalez Jerome

  公开号：US20090018169A1

  公开（公告）日：2009-01-15

  This present invention is related to sulfonamide derivatives of Formula (I), pharmaceutical composition thereof, methods of preparation thereof and to their use for the treatment and/or prophylaxis of bacterial infections such as tuberculosis.

  本发明涉及公式（I）的磺酰胺衍生物，其制药组合物，制备方法以及用于治疗和/或预防细菌感染，如结核病的用途。
• Pyrazine Derivatives and Use as P13k Inhibitors
  申请人：Gaillard Pascale

  公开号：US20090082356A1

  公开（公告）日：2009-03-26

  The present invention is related to pyrazine derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.

  本发明涉及式（I）的吡嗪衍生物，特别用于治疗和/或预防自身免疫性疾病和/或炎症性疾病、心血管疾病、神经退行性疾病、细菌或病毒感染、肾脏疾病、血小板聚集、癌症、移植、移植排斥或肺部损伤。