p-Aminoethyl-sulfonanilid | 337912-53-5

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: p-Aminoethyl-sulfonanilid
• 英文别名: N-(4-aminophenyl)ethane-1-sulfonamide；N-(4-aminophenyl)ethanesulfonamide
• CAS: 337912-53-5
• 化学式: C₈H₁₂N₂O₂S
• mdl: MFCD09048564
• 分子量: 200.261
• InChiKey: CPPJVBODPOBMCV-UHFFFAOYSA-N

物化性质

• 沸点：
  370.6±44.0 °C(Predicted)
• 密度：
  1.346±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  13
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  80.6
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  5-硝基-2-糠酸 、 p-Aminoethyl-sulfonanilid 在 吡啶 、 三乙胺 、 Methanaminium,N-[(dimethylamino)(3H-1,2,3-triazolo[4,5-b]pyridin-3-yloxy)methylene]-N-methyl-, hexafluorophosphate(1-) 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 0.25h， 以85.3%的产率得到N-(4-(ethylsulfonamido)phenyl)-5-nitrofuran-2-carboxamide
  参考文献：
  名称：

  N-(4-acetamidophenyl)-5-acetylfuran-2-carboxamide as a novel orally available diuretic that targets urea transporters with improved PD and PK properties

  摘要：

  DOI：

  10.1016/j.ejmech.2021.113859
• 作为产物：
  描述：

  N-(4-nitrophenyl)ethanesulfonamide 在 铁粉 、 氯化铵 作用下， 以 乙醇 、 水 为溶剂， 生成 p-Aminoethyl-sulfonanilid
  参考文献：
  名称：

  N-(4-acetamidophenyl)-5-acetylfuran-2-carboxamide as a novel orally available diuretic that targets urea transporters with improved PD and PK properties

  摘要：

  DOI：

  10.1016/j.ejmech.2021.113859

文献信息

• [EN] TRIAZINE DERIVATIVES AND THEIR THERAPEUTICAL APPLICATIONS<br/>[FR] DÉRIVÉS DE LA TRIAZINE ET LEURS APPLICATIONS THÉRAPEUTIQUES
  申请人：ABRAXIS BIOSCIENCE LLC

  公开号：WO2010144359A1

  公开（公告）日：2010-12-16

  Compounds of the formula (I) and formula (II) and pharmaceutically acceptable salts thereof.

  式(I)和式(II)的化合物及其药用盐。
• Synthesis and use of retinoid compounds having negative hormone and/or antagonist activities
  申请人：——

  公开号：US20020156054A1

  公开（公告）日：2002-10-24

  Aryl-substituted and aryl and (3-oxo-1-propenly)-substituted benzopyran, benzothiopyran, 1,2-dihydroquinoline, and 5,6-dihydronaphthalene derivatives have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists. For example, the retinoid negative hormone called AGN 193109 effectively increased the effectiveness of other retinoids and steroid hormones in in vitro transactivation assays. Additionally, transactivation assays can be used to identify compounds having negative hormone activity. These assays are based on the ability of negative hormones to down-regulate the activity of chimeric retinoid receptors engineered to possess a constitutive transcription activator domain.

  芳基取代和芳基和(3-氧代-1-丙烯基)-取代的苯并吡喃、苯并硫吡喃、1,2-二氢喹啉和5,6-二氢萘衍生物具有视黄醇负性激素和/或拮抗剂样生物活性。发明的RAR拮抗剂可用于哺乳动物，包括人类，以预防或减轻RAR激动剂对受体位点的作用。具体而言，可以与视黄醇药物共同使用RAR激动剂，以预防或改善视黄醇或维生素A或维生素A前体引起的毒性或副作用。视黄醇负性激素可用于增强其他视黄醇和核受体激动剂的活性。例如，名为AGN 193109的视黄醇负性激素在体外转录激活实验中有效增强了其他视黄醇和类固醇激素的效果。此外，可以使用转录激活实验来鉴定具有负性激素活性的化合物。这些实验基于负性激素下调工程化嵌合视黄醇受体的构成转录激活子域的能力。
• Substituted oxindole derivatives as tyrosine kinase inhibitors
  申请人：Dickerson Howard Scott

  公开号：US20050228025A1

  公开（公告）日：2005-10-13

  The present invention is related to oxindole derivatives of structure (I), compositions containing the same, and methods of use and manufacture of the same. Such compounds generally are useful pharmacologically as agents in those disease states alleviated by the alteration of mitogen activated signaling pathways in general, and in particular in the inhibition or antagonism of protein kinases, which pathologically involve aberrant cellular proliferation. Such disease states include tumor growth, restenosis, atherosclerosis, pain and thrombosis. In particular, the present invention relates to a series of substituted oxindole compounds, which exhibit Trk family protein tyrosine kinase inhibition, and which are useful in cancer therapy and chronic pain indications.

  本发明涉及结构式（I）的氧吲哚衍生物、含有它们的组合物以及它们的使用和制造方法。这些化合物通常在改变通常的有丝分裂原活化信号通路并在特别地抑制或拮抗蛋白激酶的病理性细胞增殖所缓解的疾病状态中，具有药理学上的作用。这些疾病状态包括肿瘤生长、再狭窄、动脉硬化、疼痛和血栓形成。特别地，本发明涉及一系列取代氧吲哚化合物，它们表现出Trk家族蛋白酪氨酸激酶抑制作用，并且在癌症治疗和慢性疼痛指示中有用。
• Pyrimidine derivatives, processes for preparation thereof and use thereof
  申请人：FUJISAWA PHARMACEUTICAL CO., LTD.

  公开号：EP0168262A2

  公开（公告）日：1986-01-15

  A pyrimidine derivative of the formula : wherein R' is hydrogen, aryl optionally having substituent(s) selected from lower alkoxy, lower alkyl, halogen and lower +alkylthio or , in which N D is a N-containing heterocyclic group; R2 is a) =N-R2 or in which R2 is aryl optionally substituted with lower alkyl, lower alkoxy, amino and/or acylamino and is hydrogen or lower alkyl, -N B is a N-containing heterocyclic group optionally substituted with acyl and/or ar(lower) alkyl; R3 is hydrogen or lower alkyl; R4 is a) imino optionally substituted with lower alkyl, aryl or ar(lower)alkyl, or b) lower alkyl, hydrogen, halogen, lower alkylthio, amino optionally substituted with lower alkyl, aryl, ar(lower)alkyl and/or acyl, or hydrazino optionally substituted with acyl, in which is a N-containing heterocyclic goup optionally substituted with acyl, and/or ar(lower)alkyl; R5 is hydrogen, lower alkyl, lower alkanoyl optionally substituted with lower alkylamino or no significance; or R3 and R4 or R4 and R5 are taken together with the adjacent nitrogen atom and carbon atom to form a N-containing heterocyclic ring; R6 is hydrogen, lower alkyl, halogen or aryl optionally having substituent(s) selected from lower alkoxy, lower alkyl, halogen and lower alkylthio substituents; the bond represents single bond or double bond; and the dotted line in the ring A represents one, two or three additional C-C and/or C-N bond(s) in the ring system, provided that R' and R6 are not both hydrogen; and pharmaceutically acceptable salt thereof. These compounds are useful in the treatment of heart disease, hypertension, cerebrovascular disease and thrombosis. Processes for the preparation of these compounds are also described, together with novel starting compounds for use in such processes and pharmaceutical compositions comprising pyrimidine derivatives of the above formula.

  式中的嘧啶衍生物 其中 R'是氢、可任选具有选自低级烷氧基、低级烷基、卤素和低级 +其中 N D 是含 N 的杂环基团； R2 是 a) =N-R2 或 其中 R2 是可选被低级烷基、低级烷氧基、氨基和/或酰氨基取代的芳基，并且是氢或低级烷基，-N B 是可选被酰基和/或芳基（低级）取代的含 N 杂环基团； R3 是氢或低级烷基； R4 是 a) 可选择被低级烷基、芳基或芳基取代的亚氨基，或 b) 低级烷基、氢、卤素、低级烷硫基、可选择被低级烷基、芳基、芳基和/或酰基取代的氨基、 或可选被酰基取代的肼，其中 是任选被酰基和/或芳基（低级）烷基取代的含 N 杂环基团； R5 是氢、低级烷基、任选被低级烷基氨基取代的低级烷酰基或无意义；或 R3 和 R4 或 R4 和 R5 与相邻的氮原子和碳原子一起形成含 N 的杂环； R6 是氢、低级烷基、卤素或芳基，可选择具有选自低级烷氧基、低级烷基、卤素和低级烷硫基的取代基； 键代表单键或双键；以及 环 A 中的虚线代表环系中一个、两个或三个额外的 C-C 和/或 C-N 键，条件是 R' 和 R6 不同时为氢；及其药学上可接受的盐。 这些化合物可用于治疗心脏病、高血压、脑血管疾病和血栓形成。 本文还描述了制备这些化合物的工艺，以及用于此类工艺的新型起始化合物和包含上式嘧啶衍生物的药物组合物。
• N-substituted p-aminoethylsulphon anilides as antiarrhythmic agents, and intermediates therefor
  申请人：Pfizer Limited

  公开号：EP0245997B1

  公开（公告）日：1992-04-15