阿芬达占 | 37669-57-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯二氮卓类
• 中文名称: 阿芬达占
• 英文名称: Arfendazam
• 英文别名: ethyl 7-chloro-4-oxo-5-phenyl-2,3-dihydro-1,5-benzodiazepine-1-carboxylate
• CAS: 37669-57-1
• 化学式: C₁₈H₁₇ClN₂O₃
• 分子量: 344.8
• InChiKey: NXJWVCHVPUCWJS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.3
• 重原子数：
  24
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  49.8
• 氢给体数：
  0
• 氢受体数：
  3

文献信息

• [EN] AN IMPROVED PROCESS FOR THE PREPARATION OF CLOBAZAM AND ITS INTERMEDIATE<br/>[FR] PROCÉDÉ AMÉLIORÉ DE PRÉPARATION DE CLOBAZAM ET SON INTERMÉDIAIRE
  申请人：PIRAMAL ENTPR LTD

  公开号：WO2016151464A1

  公开（公告）日：2016-09-29

  The present invention provides an improved process for the preparation of 8-chloro-1-phenyl- 1H-benzo[b][1,4]diazepine-2,4(3H,5H)-dione (hereafter referred to as the compound (IV)), which is useful as a key intermediate for the synthesis of Clobazam (referred to as the compound (I)) 7-chloro-1-methyl-5-phenyl-1H-benzo[b][1,4]diazepine-2,4(3H,5H)-dione. The process of the present invention further involves transformation of the compound (IV) into Clobazam (I), comprising (a) reacting the compound (II) (as described herein) with monoalkyl malonate in the presence of a coupling agent to obtain the compound (III) (as described herein); followed by the cyclization using a base; (b) reacting the compound-IV (as described herein) obtained from step (a) with methylating agent. The process of the present invention involves formation of novel intermediates methyl 3-((4- chloro-2-(phenylamino)phenyl)amino)-3-oxopropanoate (IlIa) and 3-((4-chloro-2- (phenylamino)phenyl)amino)-3-oxopropanoic acid (V).

  本发明提供了一种改进的制备8-氯-1-苯基-1H-苯并[b][1,4]二氮杂环-2,4(3H,5H)-二酮（以下简称为化合物（IV））的过程，该过程用作合成氯硝安（简称为化合物（I））7-氯-1-甲基-5-苯基-1H-苯并[b][1,4]二氮杂环-2,4(3H,5H)-二酮的关键中间体。本发明的过程还涉及将化合物（IV）转化为氯硝安（I），包括(a)在偶联剂存在下将化合物（II）（如本文所述）与单烷基马隆酸酯反应，以获得化合物（III）（如本文所述）；随后使用碱进行环化；(b)将从步骤(a)中获得的化合物-IV（如本文所述）与甲基化试剂反应。本发明的过程涉及新型中间体甲基3-((4-氯-2-(苯胺基)苯基)氨基)-3-氧代丙酸酯（IlIa）和3-((4-氯-2-(苯胺基)苯基)氨基)-3-氧代丙酸（V）的形成。
• Diagnostic/therapeutic agents
  申请人：Klaveness Jo

  公开号：US20050002865A1

  公开（公告）日：2005-01-06

  Targetable diagnostic and/or therapeutically active agents, e.g. ultrasound contrast agents, comprising a suspension in an aqueous carrier liquid of a reporter comprising gas-containing or gas-generating material, said agent being capable of forming at least two types of binding pairs with a target.

  可定位的诊断和/或治疗活性剂，例如超声对比剂，包括悬浮在水载体液中的报告物，该报告物包含含气体或生成气体的材料，该剂能够与目标形成至少两种结合对。
• CD38-BINDING CD31 PEPTIDES AND USES THEREOF
  申请人：ENCEFA

  公开号：EP3943505A1

  公开（公告）日：2022-01-26

  The present invention relates to peptides derived from CD31, specifically binding to CD38; and their use in the prevention and/or treatment of diseases.

  本发明涉及从 CD31 衍生的肽，特别是与 CD38 结合的肽；以及它们在预防和/或治疗疾病中的用途。
• Process for the preparation of clobazam and its intermediate
  申请人：PIRAMAL ENTERPRISES LIMITED

  公开号：US10150745B2

  公开（公告）日：2018-12-11

  The present invention provides an improved process for the preparation of 8-chloro-1-phenyl-1H-benzo[b][1,4]diazepine-2,4(3H,5H)-dione (hereafter referred to as the compound (IV)), which is useful as a key intermediate for the synthesis of Clobazam (referred to as the compound (I)) 7-chloro-1-methyl-5-phenyl-1H-benzo[b][1,4]diazepine-2,4(3H,5H)-dione. The process of the present invention further involves transformation of the compound (IV) into Clobazam (I), comprising (a) reacting the compound (II) (as described herein) with monoalkyl malonate in the presence of a coupling agent to obtain the compound (III) (as described herein); followed by the cyclization using a base; (b) reacting the compound-IV (as described herein) obtained from step (a) with methylating agent. The process of the present invention involves formation of novel intermediates methyl 3-((4-chloro-2-(phenylamino)phenyl)amino)-3-oxopropanoate (IIIa) and 3-((4-chloro-2-(phenylamino)phenyl)amino)-3-oxopropanoic acid (V).

  本发明提供了一种制备 8-氯-1-苯基-1H-苯并[b][1,4]二氮杂卓-2,4(3H,5H)-二酮（以下简称化合物(IV)）的改进工艺，该化合物可作为合成氯巴扎姆（简称化合物(I)）的关键中间体。7-chloro-1-methyl-5-phenyl-1H-benzo[b][1,4]diazepine-2,4(3H,5H)-dione.本发明的工艺还包括将化合物(IV)转化为氯巴扎姆(I)，包括(a)在偶联剂存在下，将化合物(II)（如本文所述）与丙二酸单烷基酯反应，得到化合物(III)（如本文所述）；然后使用碱进行环化；(b)将步骤(a)得到的化合物-IV（如本文所述）与甲基化剂反应。本发明的工艺包括形成新型中间体 3-((4-氯-2-(苯基氨基)苯基)氨基)-3-氧代丙酸甲酯(IIIa)和 3-((4-氯-2-(苯基氨基)苯基)氨基)-3-氧代丙酸(V)。
• Controlled absorption water-soluble pharmaceutically active organic compound formulation for once-daily administration
  申请人：Counts David F.

  公开号：US10463611B2

  公开（公告）日：2019-11-05

  The present disclosure provides a once-daily water-soluble pharmaceutically active formulation for oral administration. In certain embodiments, the composition comprises a water-soluble pharmaceutically active organic compound incorporated into a small particulate, each particulate having a core of the water-soluble pharmaceutically active organic compound or an acceptable salt thereof in reversible association with a pharmaceutically acceptable drug-binding polymer. The core of the composition being surrounded by an insoluble water permeable membrane that is capable of delaying the dissolution of the pharmaceutically active compound therewithin and providing for extended release of the pharmaceutically active compound. In some embodiments, the formulation of the invention are designed to extend release of the pharmaceutically active organic compound for about 3 hours to about 8 hours, thereby enabling preparation of an extended release formulation for any pharmaceutically active compound with a half-life of from about 16 hours to about 21 hours.

  本公开提供了一种用于口服的每日一次水溶性药用活性制剂。在某些实施方案中，该组合物包括掺入小颗粒中的水溶性药用活性有机化合物，每个颗粒都有一个水溶性药用活性有机化合物或其可接受盐的核心，该核心与药学上可接受的药物结合聚合物可逆结合。组合物的核心由不溶性透水膜包围，该膜能够延迟其中的药用活性化合物的溶解，并延长药用活性化合物的释放时间。在某些实施方案中，本发明的制剂可将药用活性有机化合物的释放时间延长约 3 小时至约 8 小时，从而能够制备半衰期为约 16 小时至约 21 小时的任何药用活性化合物的缓释制剂。