Deuterated Atazanivir-D3-3

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: Deuterated Atazanivir-D3-3
• 英文别名: methyl N-[1-[2-[2-hydroxy-3-[[2-(methoxycarbonylamino)-3,3-dimethylbutanoyl]amino]-4-phenylbutyl]-2-[(4-pyridin-2-ylphenyl)methyl]hydrazinyl]-3,3-dimethyl-1-oxobutan-2-yl]carbamate
• 化学式: C₃₈H₅₂N₆O₇
• 分子量: 704.9
• InChiKey: AXRYRYVKAWYZBR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.6
• 重原子数：
  51
• 可旋转键数：
  18
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  171
• 氢给体数：
  5
• 氢受体数：
  9

文献信息

• ANTI-HIV COMPOUNDS
  申请人：Gilead Sciences, Inc.

  公开号：US20200030327A1

  公开（公告）日：2020-01-30

  The invention provides compounds having Formula (I): or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions comprising the same, processes for their preparation, and methods of treating and preventing HIV infection by their administration.

  这项发明提供了具有化学式（I）的化合物： 或其药用可接受盐，以及包含这些化合物的药物组合物，其制备方法，以及通过其给药治疗和预防HIV感染的方法。
• PROTEASE INHIBITORS HAVING ENHANCED FEATURES
  申请人：Nektar Therapeutics

  公开号：US20170028077A1

  公开（公告）日：2017-02-02

  Provided herein (among other things) are protease inhibitor compounds having enhanced features, along with methods for administering such compounds. For example, the subject compounds can be administered without concomitant administration of a CYP3A4 inhibitor, have increased therapeutic index and/or increased potency, and are low-resistance inducing in nature.

  本文提供了具有增强特性的蛋白酶抑制剂化合物，以及用于给药此类化合物的方法。例如，这些化合物可以在不伴随CYP3A4抑制剂的情况下给药，具有增加的治疗指数和/或增加的效力，并且在性质上不易产生抗药性。
• Protease Inhibitors
  申请人：Riggs-Sauthier Jennifer

  公开号：US20120108501A1

  公开（公告）日：2012-05-03

  The invention relates to (among other things) protease inhibitors containing both a water-soluble, non-peptidic oligomer and a lipophilic moiety-containing residue. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over protease inhibitor compounds lacking the water-soluble, non-peptidic oligomer and a lipophilic moiety-containing residue.

  本发明涉及含有水溶性非肽寡聚体和含有亲脂性基团残基的蛋白酶抑制剂（除其他外）。本发明的化合物在通过多种给药途径任何一种给予时，比缺乏水溶性非肽寡聚体和含有亲脂性基团残基的蛋白酶抑制剂化合物具有优点。
• OLIGOMER-PROTEASE INHIBITOR CONJUGATES
  申请人：NEKTAR THERAPEUTICS

  公开号：US20140045770A1

  公开（公告）日：2014-02-13

  The invention provides small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the small molecule drug not attached to the water-soluble oligomer.

  本发明提供了通过共价结合水溶性寡聚物进行化学修饰的小分子药物。本发明的结合物在通过任何一种给药途径给予时，表现出与未连接水溶性寡聚物的小分子药物不同的特性。
• [EN] PROCESS FOR THE PREPARATION OF 3,4-EPOXY-2-AMINO-1-SUBSTITUTED BUTANE DERIVATIVES AND INTERMEDIATE COMPOUNDS THEREOF<br/>[FR] PROCÉDÉ DE PRÉPARATION DE DÉRIVÉS DE BUTANE 3,4-ÉPOXY-2-AMINO-1-SUBSTITUÉS ET LEURS COMPOSÉS INTERMÉDIAIRES
  申请人：RANBAXY LAB LTD

  公开号：WO2009136365A1

  公开（公告）日：2009-11-12

  The present invention relates to a process for the preparation of threo-3,4-epoxy-2- amino-1-substituted butane derivatives represented by general Formula I which comprises reacting compound of Formula III or salt thereof with an active ester of acid of Formula IV and treating the product thereof with base. The carbon atom bonded to the radical R3 in Formula I and IV is in the (R)-, (S)- or (R,S)-configuration. The compounds of Formula I and III, particularly in their (2S,3R) configuration are useful intermediates for the preparation of atazanavir bisulfate.

  本发明涉及一种制备一般式I所代表的threo-3,4-环氧-2-氨基-1-取代丁烷衍生物的方法，包括将一般式III化合物或其盐与一般式IV酸的活性酯反应，并用碱处理其产物。在公式I和IV中与基团R3键合的碳原子处于(R)-、(S)-或(R,S)-构型。公式I和III的化合物，特别是它们的(2S,3R)构型，可用作atazanavir硫酸盐的中间体。