2-Isopropyl-tetrahydro-1,2-oxazin | 22524-91-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 恶嗪烷类
• 英文名称: 2-Isopropyl-tetrahydro-1,2-oxazin
• 英文别名: N-Isopropyltetrahydro-1,2-oxazin；2-isopropyl-[1,2]oxazinane；2-Propan-2-yloxazinane
• CAS: 22524-91-0
• 化学式: C₇H₁₅NO
• 分子量: 129.202
• InChiKey: XTRCSOBLUQUDPM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  9
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  12.5
• 氢给体数：
  0
• 氢受体数：
  2

文献信息

• Substituted Tetracycline Compounds
  申请人：Kim Oak K.

  公开号：US20100305072A1

  公开（公告）日：2010-12-02

  The present invention pertains, at least in part, to novel substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms.

  本发明至少部分涉及新型替代四环素化合物。这些四环素化合物可用于治疗许多对四环素化合物敏感的疾病状态，如细菌感染和肿瘤。
• [EN] HEPATITIS C INHIBITOR PEPTIDE ANALOGS<br/>[FR] ANALOGUES PEPTIDIQUES D'INHIBITEURS DE L'HEPATITE C
  申请人：BOEHRINGER INGELHEIM INT

  公开号：WO2006000085A1

  公开（公告）日：2006-01-05

  The invention relates to compounds of formula (I) wherein R', R2, R3, R4, R5, R6, Y, n and m are as defined herein. The compounds are useful for the treatment and prevention of hepatitis C viral infections in mammals by inhibiting HCV NS3 protease. The invention further relates to azalactone compounds of the formula (III) which can be reacted with an amide anion to produce the compounds of formula (I).

  本发明涉及式(I)的化合物，其中R'，R2，R3，R4，R5，R6，Y，n和m如本文所述定义。这些化合物通过抑制HCV NS3蛋白酶，用于治疗和预防哺乳动物中的丙型肝炎病毒感染。本发明进一步涉及可以与酰胺阴离子反应以产生式(I)化合物的azalactone化合物（III）。
• SUBSTITUTED TETRACYCLINE COMPOUNDS
  申请人：PARATEK PHARMACEUTICALS, INC.

  公开号：US20160046561A1

  公开（公告）日：2016-02-18

  The present invention pertains, at least in part, to novel substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms.

  本发明至少部分涉及新型取代四环素化合物。这些四环素化合物可用于治疗许多对四环素化合物敏感的疾病状态，如细菌感染和肿瘤。
• Auristatin compounds and conjugates thereof
  申请人：Mersana Therapeutics, Inc.

  公开号：US10226535B2

  公开（公告）日：2019-03-12

  An auristatin compound conjugate is provided herein. The conjugate comprises a protein based recognition-molecule (PBRM) and a polymeric carrier substituted with one or more -LD-D, the protein based recognition-molecule being connected to the polymeric carrier by LP. Each occurrence of D is independently an auristatin compound having a molecular weight ≤5 kDa. LD and LP are distinct linkers connecting the auristatin compound and PBRM to the polymeric carrier respectively. Also disclosed are polymeric scaffolds useful for conjugating with a PBRM to form a polymer-auristatin compound-PBRM conjugate described herein, compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions.

  本文提供了一种阿司他丁化合物共轭物。该共轭物包括一个基于蛋白质的识别分子（PBRM）和一个或多个-LD-D取代的聚合物载体，基于蛋白质的识别分子通过 LP 连接到聚合物载体上。每一个 D 都是分子量≤5 kDa 的独立的 Auristatin 化合物。LD 和 LP 分别是连接 Auristatin 化合物和 PBRM 与聚合物载体的不同连接体。还公开了用于与PBRM共轭以形成本文所述聚合物-阿瑞司他汀化合物-PBRM共轭物的聚合物支架、包含该共轭物的组合物、其制备方法以及用该共轭物或其组合物治疗各种疾病的方法。
• Derivatives of amphotericin B
  申请人：Sfunga Therapeutics, Inc.

  公开号：US10882883B2

  公开（公告）日：2021-01-05

  Disclosed are derivatives of amphotericin B (AmB) characterized by improved therapeutic index compared to AmB. The AmB derivatives include C16 ureas, carbamates, and amides according to Formula (I); C3′-substituted C16 ureas, carbamates, and amides according to Formula (II); C16 acyls according to Formula (III); C2′epi-C16 ureas, carbamates, and amides according to Formula (IV); and C16 oxazolidinone derivatives according to Formula (V). Also disclosed are pharmaceutical compositions comprising the AmB derivatives, and therapeutic methods of using the AmB derivatives.

  本发明公开了两性霉素B（AmB）的衍生物，其特点是与AmB相比，治疗指数有所提高。AmB衍生物包括根据式（I）的C16脲、氨基甲酸酯和酰胺；根据式（II）的C3′-取代的C16脲、氨基甲酸酯和酰胺；根据式（III）的C16酰基；根据式（IV）的C2′-环-C16脲、氨基甲酸酯和酰胺；以及根据式（V）的C16噁唑烷酮衍生物。还公开了包含AmB衍生物的药物组合物，以及使用AmB衍生物的治疗方法。