N-hydroxyphthalamide | 32015-80-8

• 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: N-hydroxyphthalamide
• 英文别名: n-Hydroxy phthalamide；2-N-hydroxybenzene-1,2-dicarboxamide
• CAS: 32015-80-8
• 化学式: C₈H₈N₂O₃
• 分子量: 180.163
• InChiKey: QQKAZZAULUMMKR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.8
• 重原子数：
  13
• 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：
  92.4
• 氢给体数：
  3
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  N-hydroxyphthalamide 、 (1-溴乙基)苯 在 potassium carbonate 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 生成 2-(1-phenylethoxy)isoindoline-1,3-dione
  参考文献：
  名称：

  Hydrazide and alkoxyamide angiogenesis inhibitors

  摘要：

  具有以下化学式的化合物是蛋氨酸氨肽酶2型（MetAP2）抑制剂，对抑制血管生成有用。还公开了抑制MetAP2的组合物和在哺乳动物中抑制血管生成的方法。

  公开号：

  US20020002152A1
• 作为试剂：
  描述：

  胆固醇 在 N-hydroxyphthalamide 、 氧气 、 过氧化苯甲酰 作用下， 以 乙酸乙酯 、 丙酮 为溶剂， 反应 72.0h， 以62%的产率得到5-胆甾烯-3β-醇-7-酮
  参考文献：
  名称：

  Synthesis and antifungal activity of oxygenated cholesterol derivatives

  摘要：

  A series of oxygenated cholesterol derivatives were prepared from new synthetic methods and evaluated for their in vitro antimicrobial properties against human pathogens. The activity was highly dependent on the structure of the different compounds involved. The best results were obtained with hydroxy ketones 2, 4 and 5 and diketone 7 exhibiting activities against S. cerevisiae (ATCC 28383) and Candida albicans (CIP 1663-86). For example, compound 2 exhibited high activities against C. albicans (CIP 1663-86) and Amphotericine B and miconazole resistant strain C. albicans (CIP 1180-79) at a concentration of 1.5 mu g/mL. (c) 2005 Elsevier Inc. All rights reserved.

  DOI：

  10.1016/j.steroids.2005.06.007

文献信息

• [EN] AMINO PYRAZINE DERIVATIVES AS PHOSPHATIDYLINOSITOL 3-KINASE INHIBITORS<br/>[FR] DÉRIVÉS AMINÉS DE PYRAZINE UTILISABLES EN TANT QU'INHIBITEURS DE LA PHOSPHATIDYLINOSITOL 3-KINASE
  申请人：NOVARTIS AG

  公开号：WO2015162459A1

  公开（公告）日：2015-10-29

  The present invention provides compounds of formula (I) which inhibit the activity of PI 3-kinase gamma isoform, which are useful for the treatment of diseases mediated by the activation of PI 3-kinase gamma isoform.

  本发明提供了一种公式（I）的化合物，该化合物抑制PI 3-激酶γ同工酶的活性，对于治疗由PI 3-激酶γ同工酶激活介导的疾病是有用的。
• HETEROAROMATIC COMPOUNDS FOR USE AS HIF INHIBITORS
  申请人：Härter Michael

  公开号：US20110301122A1

  公开（公告）日：2011-12-08

  The present application relates to novel substituted aryl compounds, processes for their preparation, their use for treatment and/or prevention of diseases and their use for the preparation of medicaments for treatment and/or prevention of diseases, in particular for treatment and/or prevention of hyperproliferative and angiogenic diseases and those diseases which arise from metabolic adaptation to hypoxic states. Such treatments can be carried out as monotherapy or also in combination with other medicaments or further therapeutic measures.

  本申请涉及新型取代芳基化合物，其制备方法，它们用于治疗和/或预防疾病以及用于制备治疗和/或预防疾病的药物，特别是用于治疗和/或预防过度增殖和血管生成性疾病以及那些由于代谢适应缺氧状态而引起的疾病。这种治疗可以作为单独治疗进行，也可以与其他药物或进一步的治疗措施结合使用。
• HETEROCYCLICALLY SUBSTITUTED ARYL COMPOUNDS AS HIF INHIBITORS
  申请人：Härter Michael

  公开号：US20130196964A1

  公开（公告）日：2013-08-01

  The present application relates to novel aryl compounds with heterocyclic substituents, processes for their preparation, their use for treatment and/or prevention of diseases and their use for the preparation of medicaments for treatment and/or prevention of diseases, in particular for treatment and/or prevention of hyperproliferative and angiogenic diseases and those diseases which arise from metabolic adaptation to hypoxic states. Such treatments can be carried out as monotherapy or also in combination with other medicaments or further therapeutic measures.

  本申请涉及具有杂环取代基的新型芳基化合物，其制备方法，它们用于治疗和/或预防疾病以及用于制备治疗和/或预防疾病的药物，特别是用于治疗和/或预防过度增殖和血管生成性疾病以及那些由于代谢适应缺氧状态而引起的疾病。这种治疗可以作为单独治疗进行，也可以与其他药物或进一步治疗措施结合使用。
• QUINAZOLIN-OXIME DERIVATIVES AS HSP90 INHIBITORS
  申请人：Courtney Stephen Martin

  公开号：US20110118258A1

  公开（公告）日：2011-05-19

  Compounds of general formula (I); or a stereoisomers, tautomers, pharmaceutically acceptable salts, or prodrugs thereof, wherein R1, R2, R3, R4, R5, R6, R8 and R9 are as defined herein, are useful for the treatment of diseases and conditions which are mediated by excessive or inappropriate Hsp90 activity such as cancers, viral infection and inflammatory diseases or conditions.

  通式（I）的化合物；或其立体异构体、互变异构体、药学上可接受的盐或前药，其中R1、R2、R3、R4、R5、R6、R8和R9如本文所定义，对于治疗由过度或不恰当的Hsp90活性介导的疾病和病况，如癌症、病毒感染和炎症性疾病或病况，是有用的。
• [EN] METHODS FOR POST-FABRICATION FUNCTIONALIZATION OF POLY(ESTER UREAS)<br/>[FR] PROCÉDÉS POUR LA FONCTIONNALISATION DE POLY(ESTER-URÉES) APRÈS FABRICATION
  申请人：BECKER MATTHEW

  公开号：WO2015048728A1

  公开（公告）日：2015-04-02

  Amino acid-based poly(ester urea)s (PEU) are emerging as a class of polymers that have shown promise in regenerative medicine applications. Embodiments of the invention relate to the synthesis of PEUs carrying pendent "clickable" groups on modified tyrosine amino acids. The pendent species include alkyne, azide, alkene, tyrosine-phenol, and ketone groups. PEUs with Mw exceeding 100k Da were obtained via interfacial polycondensation methods and the concentration of pendent groups was varied by copolymerization. The incorporation of derivatizable functionalities is demonstrated using 1H NMR and UV-Vis spectroscopy methods. Electrospinning was used to fabricate PEU nanofibers with a diameters ranging from 350 nm to 500 nm. The nanofiber matricies possess mechanical strengths suitable for tissue engineering (Young's modulus: 30045 MPa; tensile stress: 8.51.2 MPa). A series of bioactive peptides and fluorescent molecules were conjugated to the surface of the nanofibers following electrospinning using bio-orthogonal reactions in aqueous media.

  基于氨基酸的聚（酯脲）（PEU）作为一类聚合物正在成为再生医学应用中显示出潜力的材料。发明的实施例涉及合成携带修饰酪氨酸氨基酸上“可点击”基团的PEU。这些基团包括炔基、叠氮基、烯烃、酪氨酸酚和酮基团。通过界面缩聚方法获得了分子量超过100k Da的PEU，并通过共聚合改变基团的浓度。使用1H核磁共振和紫外-可见光谱方法证明了可衍生功能的结合。电纺技术用于制备直径在350纳米至500纳米范围内的PEU纳米纤维。这些纳米纤维基质具有适用于组织工程的机械强度（杨氏模量：30045 MPa；拉伸应力：8.51.2 MPa）。在电纺后，一系列生物活性肽和荧光分子通过生物正交反应结合到纳米纤维表面。