3-iodo-4-methyl-N-(2-methyl-3-(2-morpholinoacetamido)phenyl)benzamide | 882678-75-3

• 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: 3-iodo-4-methyl-N-(2-methyl-3-(2-morpholinoacetamido)phenyl)benzamide
• 英文别名: 3-iodo-4-methyl-N-[2-methyl-3-[(2-morpholin-4-ylacetyl)amino]phenyl]benzamide
• CAS: 882678-75-3
• 化学式: C₂₁H₂₄IN₃O₃
• 分子量: 493.344
• InChiKey: HLFLZLTZLWJNMY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  28
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  70.7
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2-氨基喹唑啉-6-硼酸频哪醇酯 、 3-iodo-4-methyl-N-(2-methyl-3-(2-morpholinoacetamido)phenyl)benzamide 在 dichloro[1,1'-bis(diphenylphosphino)ferrocene]palladium(II) chloride potassium carbonate 作用下， 以 水 、 乙腈 为溶剂， 反应 18.0h， 生成 3-(2-amino-6-quinazolinyl)-4-methyl-N-(2-methyl-3-((4-morpholinylacetyl)amino)phenyl)benzamide
  参考文献：
  名称：

  Aryl nitrogen-containing bicyclic compounds and methods of use

  摘要：

  这项发明涉及一类新的化合物，用于预防和治疗蛋白激酶介导的疾病，包括炎症、癌症和相关疾病。这些化合物具有一般的化学式I，其中A1、A2、A3、B、R1、R2、R3和R4在此有定义。因此，该发明还涉及包括该发明的化合物的药物组合物，使用该发明的化合物和组合物预防和治疗激酶介导的疾病的方法，以及用于制备该发明的化合物的中间体和方法。

  公开号：

  US20070054916A1
• 作为产物：
  描述：

  N-(3-amino-2-methylphenyl)-2-morpholinoacetamide 、 3-碘-4-甲基苯甲酰氯 在 三乙胺 作用下， 以 二氯甲烷 为溶剂， 反应 16.0h， 生成 3-iodo-4-methyl-N-(2-methyl-3-(2-morpholinoacetamido)phenyl)benzamide
  参考文献：
  名称：

  Aryl nitrogen-containing bicyclic compounds and methods of use

  摘要：

  这项发明涉及一类新的化合物，用于预防和治疗蛋白激酶介导的疾病，包括炎症、癌症和相关疾病。这些化合物具有一般的化学式I，其中A1、A2、A3、B、R1、R2、R3和R4在此有定义。因此，该发明还涉及包括该发明的化合物的药物组合物，使用该发明的化合物和组合物预防和治疗激酶介导的疾病的方法，以及用于制备该发明的化合物的中间体和方法。

  公开号：

  US20070054916A1

文献信息

• HETEROARYL-SUBSTITUTED ALKYNE COMPOUNDS AND METHOD OF USE
  申请人：Chaffee Stuart C.

  公开号：US20100160283A1

  公开（公告）日：2010-06-24

  The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation, cancer and related conditions. The compounds have a general Formula I wherein A 1 , A 2 , A 3 , A 4 , R 1 and R 2 are defined herein. Accordingly, the invention also comprises pharmaceutical compositions comprising the compounds of the invention, methods for the prophylaxis and treatment of kinase mediated diseases using the compounds and compositions of the invention, and intermediates and processes useful for the preparation of compounds of the invention.

  本发明涉及一类新的化合物，用于预防和治疗蛋白激酶介导的疾病，包括炎症、癌症和相关疾病。该化合物具有一般式I，其中A1、A2、A3、A4、R1和R2的定义如本文所述。因此，本发明还涉及包括本发明化合物的制药组合物，使用本发明化合物和组合物预防和治疗激酶介导的疾病的方法，以及用于制备本发明化合物的中间体和过程。
• Anti-smudge and anti-graffiti compositions
  申请人：Queen's University at Kingston

  公开号：US10023751B2

  公开（公告）日：2018-07-17

  Polyurethane-based and epoxy-based coating compositions are described that provide coatings and adhesives that are clear, amphiphobic and durable. Both water and hexadecane readily slide off these surfaces without leaving a residue. Coatings with thicknesses ranging from about 10 nm to about 10 μm exhibited excellent transmittance properties. Such films exhibited durability against abrasion, ink-resistance, anti-graffiti, anti-fingerprint, and strong adhesion to glass surfaces. The coatings are applicable to electronic devices, fabrics, glass, etc. to prepare optically clear, stain-resistant, and smudge-resistant surfaces.

  聚氨酯基和环氧基涂料组合物具有透明、疏油和耐久性等特点。水和十六烷都很容易从这些表面滑落，不会留下残留物。厚度在 10 纳米到 10 微米之间的涂层具有出色的透光性能。这些薄膜具有耐磨性、耐墨性、防涂鸦性、防指纹性以及与玻璃表面很强的附着力。这种涂层适用于电子设备、织物、玻璃等，可制备出光学清晰、防污、防污的表面。
• Iron garnet nanoparticles for cancer radiotherapy and chemotherapy
  申请人：UNIVERSITY OF NORTH TEXAS HEALTH SCIENCE CENTER AT FORT WORTH

  公开号：US10195297B2

  公开（公告）日：2019-02-05

  Iron garnet nanoparticles and or iron garnet particles containing various activatable nuclides, such as holmium-165 (165Ho) and dysprosium-164 (164Dy), are disclosed in this application. The iron garnet (e.g., HoIG and DyIG) nanoparticles and iron garnet particles can prepared using hydroxide co-precipitation methods. In some embodiments, radiosensitizers can be loaded on radioactive magnetic nanoparticles or radioactive iron garnet particles and, optionally, coated with suitable lipid bilayers. Methods of using the disclosed nanoparticles and particles for mediating therapeutic benefit in diseases responsive to radiation therapy are also provided. Another aspect of the invention provides films, electrospun fabrics or bandage coverings for the delivery of radiation to the site of a skin lesion amenable to treatment with radiation (e.g., skin cancers or psoriasis).

  本申请公开了含有各种可活化核素（如钬-165（165Ho）和镝-164（164Dy））的纳米铁榴石颗粒和或铁榴石颗粒。铁榴石（如 HoIG 和 DyIG）纳米颗粒和铁榴石颗粒可采用氢氧化物共沉淀法制备。在某些实施方案中，可将放射增敏剂装载在放射性磁性纳米颗粒或放射性铁榴石颗粒上，还可选择涂上合适的脂质双层膜。本发明还提供了使用所公开的纳米粒子和颗粒对放射治疗反应性疾病进行治疗的方法。本发明的另一个方面提供了薄膜、电纺织物或绷带覆盖物，用于向可接受放射治疗的皮肤病变部位（如皮肤癌或牛皮癣）输送放射线。
• Oral transmucosal compositions including aromatase inhibitors for low testosterone levels in men
  申请人：Professional Compounding Centers of America

  公开号：US10792247B2

  公开（公告）日：2020-10-06

  Formulations for oral transmucosal compositions that include aromatase inhibitors (AIs) in combination with transmucosal absorption enhancers are disclosed. Disclosed oral transmucosal compositions may be for immediate release or slow release, and may be administered to increase bloodstream testosterone levels and thereby reduce symptoms of testosterone deficiency. Disclosed oral transmucosal compositions may include liquid dosage forms, solid dosage forms, and chewing gums. Further dosage forms may include mucoadhesive thin strips, thin films, tablets, patches, and tapes, among others. Other dosage forms may be: mucoadhesive liquids such as gel-forming liquid; gel-forming; semisolids; and gel-forming powders, among other dosage forms that exhibit mucoadhesive properties, and provide oral transmucosal delivery of AIs. Disclosed oral transmucosal compositions may allow the delivery of AIs directly into the patient's bloodstream, thus providing high bioavailability of AIs; therefore, required dose may be lower. Additionally, adjustments of AIs dosages may be achieved when using disclosed oral transmucosal compositions.

  本研究公开了包括芳香化酶抑制剂（AIs）与透粘膜吸收促进剂的口服透粘膜组合物配方。所公开的口服经黏膜组合物可以是速释或缓释的，可以用于提高血液中的睾酮水平，从而减轻睾酮缺乏的症状。公开的口服经黏膜组合物可包括液体剂型、固体剂型和口香糖。其他剂型可包括粘液黏附薄条、薄膜、片剂、贴片和胶带等。其他剂型可包括：粘液粘附性液体，如凝胶剂型液体；凝胶剂型；半固体；凝胶剂型粉末，以及其他表现出粘液粘附特性的剂型，可提供口腔黏膜给药的人工合成药物。所公开的口腔黏膜给药组合物可以将人工合成药物直接输送到患者的血液中，从而提供较高的人工合成药物生物利用度；因此，所需剂量可能较低。此外，使用所公开的口腔黏膜组合物时，还可以调整人工合成药物的剂量。
• Silicone copolymers, methods of making, and articles
  申请人：3M INNOVATIVE PROPERTIES COMPANY

  公开号：US10941252B2

  公开（公告）日：2021-03-09

  A copolymer composition that includes a silicone copolymer, methods of making the composition, and articles that include the composition, wherein the copolymer composition includes a silicone copolymer having a backbone composition that includes: silicone segments in an amount of 5 wt-% to 40 wt-%, based on the total weight of the silicone copolymer; hydrophilic segments in an amount of 40 wt-% to 75 wt-%, based on the total weight of the silicone copolymer; and reinforcing segments in an amount of 5 wt-% to 30 wt-%, based on the total weight of the silicone copolymer, wherein the reinforcing segments are derived from the reaction of one or more chain extenders with one or more multi-functional isocyanates, multi-functional carboxylic acids, multi-functional anhydrides, multi-functional esters, and/or multi-functional acid halides; wherein the silicone segments, hydrophilic segments, and reinforcing segments are connected through urea, urethane, amide, and/or oxamide linkages; wherein the hydrophilic segments and the reinforcing segments are present in a weight ratio of 1.8:1 to 8:1; and the hydrophilic segments and the silicone segments are present in a weight ratio of 1.3:1 to 4.5:1.

  一种包括有机硅共聚物的共聚物组合物、制造该组合物的方法以及包括该组合物的物品，其中该共聚物组合物包括有机硅共聚物，该有机硅共聚物具有骨架组合物，该骨架组合物包括：基于有机硅共聚物总重量，含量为 5 wt-% 至 40 wt-%的有机硅段； 基于有机硅共聚物总重量，含量为 40 wt-% 至 75 wt-%的亲水段；和增强段，其用量为有机硅共聚物总重量的 5 wt-% 至 30 wt-%，其中增强段由一种或多种扩链剂与一种或多种多功能异氰酸酯、多功能羧酸、多功能酸酐、多功能酯和/或多功能酸卤化物反应而得；其中硅酮段、亲水段和增强段通过脲、聚氨酯、酰胺和/或草酰胺连接；其中亲水段和增强段的重量比为 1.8:1至8:1；亲水段和硅酮段的重量比为1.3:1至4.5:1。