1-[(2R,3R,4S,5R)-3,4-二羟基-5-(羟基甲基)四氢呋喃-2-基]吡唑-3,4-二甲酰胺 | 123027-69-0

• 分子结构分类: 有机化合物 - 核苷、核苷酸和类似物 - 吡唑核糖核苷和核糖核苷酸
• 中文名称: 1-[(2R,3R,4S,5R)-3,4-二羟基-5-(羟基甲基)四氢呋喃-2-基]吡唑-3,4-二甲酰胺
• 英文名称: 1-β-D-ribofuranosylpyrazole-3,4-dicarboxamide
• 英文别名: 1-beta-D-ribofuranosylpyrazole-3,4-dicarboxamide；1-Ribofuranosylpyrazole-3,4-dicarboxamide；1-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrazole-3,4-dicarboxamide
• CAS: 123027-69-0
• 化学式: C₁₀H₁₄N₄O₆
• 分子量: 286.244
• InChiKey: AJZDKCDLDNDFBE-KQYNXXCUSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -2.7
• 重原子数：
  20
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  174
• 氢给体数：
  5
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  1-乙酰基-三-苄氧基-罗伯糖 在 三氟甲磺酸三甲基硅酯 、 氨 作用下， 以 甲醇 、 乙腈 为溶剂， 反应 28.0h， 生成 1-[(2R,3R,4S,5R)-3,4-二羟基-5-(羟基甲基)四氢呋喃-2-基]吡唑-3,4-二甲酰胺
  参考文献：
  名称：

  利巴韦林的氨基甲酰基同源物抑制培养物中人骨髓白血病细胞的生长并诱导其细胞分化。

  摘要：

  合成了一系列具有两个相邻氨基甲酰基的1,2,3-三唑（2），吡唑（3和5）和吡咯（4）核糖核苷，并评估了它们对HL-60的细胞生长抑制和诱导细胞分化的作用培养中的细胞。1,2,3-三唑-4,5-二羧酸二甲酯（6）和吡唑-3,4-二羧酸二乙酯（7）的TMS衍生物与1-O-乙酰基2,3,5-三-甘油的糖基化在TMS三氟甲磺酸酯存在下，O-苯甲酰基-D-呋喃核糖（8）分别主要产生β-核苷9和14。9和14的氨解分别提供了2-β-D-呋喃核糖基-1,2,3-三唑-4,5-二甲酰胺（2）和1-β-D-呋喃核糖基吡唑-3,4-二甲酰胺（3）。1-脱氧-1-肼基-2,3-O-异亚丙基-D-核糖（16）与四氰基乙烯（15）的立体选择环环化得到5-氨基-1-（2，3-O-异亚丙基-β-D-呋喃呋喃糖基）吡唑-3,4-二腈（17）。17的脱异丙基亚基化，然后反应产物（18）的氧化水解，得到3（5）的5-氨基衍生物。预先形成的3

  DOI：

  10.1021/jm00163a054

文献信息

• Modulation of Th1/Th2 Cytokine expression by Ribavirin and Ribavirin analogs in actived T-Lymphocytes for treating HCV infections
  申请人：ICN Pharmaceuticals, Inc.

  公开号：EP1240899A2

  公开（公告）日：2002-09-18

  Ribavirin® is administered to a patient in a dosage range which is effective to modulate lymphokine expression in activated T cells. In particular, Ribavirin® is used to suppress Th2-mediated T cell responses and promote Th1-mediated T cell response. In other apsects of the invention, one or more Ribavirin® analogs are administered to a patient in a dosage range which is effective to modulate lymphokine expression in activated T cells. The Ribavirin® analog(s) may be used to suppress or enhance Th1 or Th2-mediated T cell responses.

  利巴韦林®给患者的剂量范围可有效调节活化 T 细胞中淋巴因子的表达。特别是，利巴韦林®可用于抑制Th2介导的T细胞反应，促进Th1介导的T细胞反应。在本发明的其他部分中，向患者施用一种或多种利巴韦林® 类似物，其剂量范围可有效调节活化 T 细胞中淋巴因子的表达。利巴韦林® 类似物可用于抑制或增强 Th1 或 Th2 介导的 T 细胞反应。
• IMPLANT SYSTEM FOR TREATING SINUSITIS OR ALLERGIC RHINITIS
  申请人：Puyi (Shanghai) Biotechnology Co., Ltd

  公开号：EP2921138A1

  公开（公告）日：2015-09-23

  An implanted system for treating sinusitis or allergic rhinitis is provided, wherein the implanted system has a circumferentially extending wall formed of a biodegradable polymer, and the wall includes a plurality of interspaces, with biodegradable fiber bundles containing drugs interspersed in the interspaces. The implanted system formed of the biodegradable polymer can provide a sufficient normal force perpendicular to the external surface during a compression, and prevent the supported channel from being closed after the release in a location for the implantation (a location of pathological changes or ostium of the sinus). The implanted system formed of the biodegradable polymer has an axial internal bore to guarantee the aeration for the nasal cavity after the implantation. The implanted system formed of the biodegradable polymer can be naturally degraded in the nasal cavity. Compared with prior stents which cannot directly contact with certain locations of pathological changes, the biodegradable fiber bundles containing drugs carried on the implanted system can reach those locations of pathological changes to optimize the therapeutic effect.

  提供了一种用于治疗鼻窦炎或过敏性鼻炎的植入系统，其中该植入系统具有由可生物降解聚合物形成的周向延伸壁，该壁包括多个间隙，间隙中穿插有含有药物的可生物降解纤维束。由生物可降解聚合物形成的植入系统可在压缩过程中提供垂直于外表面的足够法向力，并防止植入位置（病理变化位置或窦腔）的支撑通道在释放后关闭。由生物可降解聚合物形成的植入系统具有轴向内孔，以保证植入后鼻腔的通气性。由生物可降解聚合物形成的植入系统可在鼻腔内自然降解。与以往不能直接接触某些病变部位的支架相比，植入系统所携带的含有药物的可降解纤维束可以到达病变部位，从而达到最佳治疗效果。
• Expandable devices and methods for treating a nasal or sinus condition
  申请人：Abbate Anthony J.

  公开号：US10357640B2

  公开（公告）日：2019-07-23

  Described here are expandable devices and methods for using them. The devices generally comprise a hub and a plurality of legs extending therefrom. In some variations, the hub may comprise one or more domed portions, tapered portions, or the like. The legs may comprise one or more straight segments, one or more curved segments, or a combination thereof. The devices may comprise one or more polymers, and/or one or more portions of the device may be configured to biodegrade. In other variations, the device may be configured to release one or more drugs therefrom. Additionally, in some variations the devices may be configured to be self-expandable from a low-profile configuration to an expanded configuration.

  这里描述的是可扩展装置及其使用方法。这些装置一般包括一个轮毂和从轮毂延伸出来的多个支脚。在某些变化中，轮毂可包括一个或多个圆顶部分、锥形部分或类似部分。支腿可包括一个或多个直段、一个或多个弯段或其组合。装置可包括一个或多个聚合物，和/或装置的一个或多个部分可配置为生物降解。在其他变体中，装置可配置为从中释放一种或多种药物。此外，在某些变体中，装置可配置为可从低调配置自行扩展到扩展配置。
• Drug-coated balloon
  申请人：Intersect ENT, Inc.

  公开号：US10603473B2

  公开（公告）日：2020-03-31

  Described here are devices, systems, and methods for treating conditions or diseases of the nose, ear, or throat with an expandable device having a drug coating. The expandable devices may be delivered to a body cavity in a low-profile configuration and expanded to contact surrounding tissue. The expandable devices may deliver or release the drug coating to the tissue. Multiple expansions of a single device may be employed during treatment. Various coating excipients and manufacturing parameters for the expandable devices may also be adjusted to enhance or slow transfer of the drug coating and/or release of the drug to the target tissue site. The drug transferred to the tissue may act as an in situ depot that enables maintenance of a therapeutic level of locally delivered drug for a desired time period after removal of the expandable devices.

  这里描述的是使用具有药物涂层的可膨胀装置治疗鼻、耳或喉部病症或疾病的装置、系统和方法。可膨胀装置可以低调配置的方式输送到体腔，并膨胀以接触周围组织。可膨胀装置可向组织输送或释放药物涂层。在治疗过程中，可对单个装置进行多次扩张。还可以调整可膨胀装置的各种包衣辅料和制造参数，以增强或减缓药物包衣向目标组织部位的转移和/或药物释放。转移到组织中的药物可作为原位药库，在移除可膨胀装置后的一段所需时间内维持局部给药的治疗水平。
• Formulations and methods for treating rhinosinusitis
  申请人：——

  公开号：US20040209852A1

  公开（公告）日：2004-10-21

  The invention involves methods and formulations for treating or preventing rhinosinusitis, including fungus-induced rhinosinusitis in mammals. In one embodiment, the formulation of the present invention comprises a steroidal anti-inflammatory agent having a specific particle size distribution profile. The formulation may also comprise an antifungal agent, antibiotic or antiviral agent.

  本发明涉及治疗或预防哺乳动物鼻炎（包括真菌引起的鼻炎）的方法和制剂。在一个实施方案中，本发明的制剂包括具有特定粒径分布特征的类固醇抗炎剂。制剂还可包括抗真菌剂、抗生素或抗病毒剂。