1-d-Ribofuranosyl-1,2,4-triazole-3-carboxamide

• 分子结构分类: 有机化合物 - 核苷、核苷酸和类似物 - 三唑核糖核苷和核糖核苷酸
• 英文名称: 1-d-Ribofuranosyl-1,2,4-triazole-3-carboxamide
• 英文别名: 1-[(3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-1,2,4-triazole-3-carboxamide
• 化学式: C₈H₁₂N₄O₅
• 分子量: 244.2
• InChiKey: IWUCXVSUMQZMFG-SHXFMUIJSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.8
• 重原子数：
  17
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.62
• 拓扑面积：
  144
• 氢给体数：
  4
• 氢受体数：
  7

文献信息

• Cationic Steroid Antimicrobial Compositions and Methods of Use
  申请人：Savage B. Paul

  公开号：US20070190067A1

  公开（公告）日：2007-08-16

  The invention provides methods for decreasing or inhibiting human immunodeficiency virus (HIV) infection or pathogenesis (e.g., illness) of a cell in vitro, ex vivo or in vivo, a symptom or pathology associated with human immunodeficiency virus (HIV) infection or pathogenesis (e.g., illness) in vitro, ex vivo or in vivo, or an adverse side effect of human immunodeficiency virus (HIV) infection or pathogenesis (e.g., illness) in vitro, ex vivo or in vivo. In one embodiment, a method of the invention includes treating a subject with an invention compound (e.g., cationic steroid antimicrobial or CSA).

  这项发明提供了用于在体外、体外或体内减少或抑制人类免疫缺陷病毒（HIV）感染或病理发生（例如，疾病）、在体外、体外或体内与人类免疫缺陷病毒（HIV）感染或病理发生（例如，疾病）相关的症状或病理、或在体外、体外或体内人类免疫缺陷病毒（HIV）感染或病理发生（例如，疾病）的不良副作用的方法。在一种实施方式中，该发明的方法包括使用一种发明化合物（例如，阳离子类固体抗菌剂或CSA）治疗受试者。
• Cationic Steroid Microbial Compositions and Methods of Use
  申请人：Savage B. Paul

  公开号：US20070191322A1

  公开（公告）日：2007-08-16

  The invention relates to methods for decreasing or inhibiting influenza virus infection or pathogenesis of a cell in vitro, ex vivo or in vivo, a symptom or pathology associated with influenza infection or pathogenesis in vitro, ex vivo or in vivo, or an adverse side effect of influenza infection or pathogenesis in vitro, ex vivo or in vivo. In one embodiment, a method of the invention includes treating a subject with an invention compound (e.g., cationic steroid antimicrobial or CSA).

  该发明涉及减少或抑制体外、体内或体外细胞的流感病毒感染或发病机制，体外、体内或体外与流感感染或发病机制相关的症状或病理学，或体外、体内或体外流感感染或发病机制的不良副作用的方法。在一种实施方式中，该发明的方法包括使用一种发明化合物（例如，阳离子类固醇抗微生物药物或CSA）治疗受试者。
• CELL DELIVERY COMPOSITIONS
  申请人：——

  公开号：US20010006817A1

  公开（公告）日：2001-07-05

  The present invention provides improved cell delivery compositions. In particular, the invention provides biocompatible endosomolytic agents. In a preferred embodiment, the endosomolytic agents are also biodegradable and can be broken down within cells into components that the cells can either reuse or dispose of. Preferred endosomolytic agents include cationic polymers, particularly those comprised of biomolecules, such as histidine, polyhistidine, polylysine or any combination thereof. Other exemplary endosomolytic agents include, but are not limited to, other imidazole containing compounds such as vinylimidazole and histamine. More particularly preferred are those agents having multiple proton acceptor sites and acting as a “proton sponge”, disrupting the endosome by osmolytic action. In preferred embodiments, the endosomolytic agent comprises a plurality of proton acceptor sites having pKas within the range of 4 to 7, which endosomal lysing component is polycationic at pH 4. The present invention also contemplates the use of these endosomolytic agents as delivery agents by complexation with the desired compound to be delivered. Thus, the present invention also acts as a cell delivery system comprising an endosomolytic agent, a delivery agent, and a compound to be delivered.

  本发明提供了改进的细胞递送组合物。具体而言，本发明提供了生物相容的内体溶解剂。在一个优选实施例中，内体溶解剂也是可生物降解的，可以在细胞内分解为细胞可以重新利用或处置的组分。优选的内体溶解剂包括阳离子聚合物，特别是由生物分子组成的聚组氨酸，如组氨酸、多组氨酸、多赖氨酸或二者的任意组合。其他示例性的内体溶解剂包括但不限于其他含咪唑醇基的化合物，如乙烯咪唑和组胺。更具体优选的是那些具有多个质子受体位点并作为“质子海绵”起作用的剂，通过渗透调节作用破坏内体。在优选实施例中，内体溶解剂包括具有pKa在4到7范围内的多个质子受体位点的内体溶解组分，在pH 4时为多阳离子性的。本发明还考虑了将这些内体溶解剂作为递送剂通过与要递送的化合物结合的复合物的使用。因此，本发明还作为一个细胞递送系统，包括一个内体溶解剂、一个递送剂和一个要递送的化合物。
• [EN] SUBSTITUTED PROLINE INHIBITORS OF HEPATITIS C VIRUS REPLICATION<br/>[FR] INHIBITEURS PROLINE SUBSTITUÉE DE RÉPLICATION DU VIRUS DE L'HÉPATITE C
  申请人：INTERMUNE INC

  公开号：WO2012040242A1

  公开（公告）日：2012-03-29

  The embodiments provide compounds of the general Formulae I, la, II,IIa,III, IIIa, Illb, IV, IVa, IVb, V, Va, Vb, VI, VIa, VIb, and VIc, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition. The embodiments also provide methods for the synthesis of subject compounds and intermediates in the synthetic methods.

  该实施例提供了一般式I、Ia、II、IIa、III、IIIa、IIIb、IV、IVa、IVb、V、Va、Vb、VI、VIa、VIb和VIc的化合物，以及包括药物化合物的组合物，包括制药组合物。该实施例还提供了治疗方法，包括治疗丙型肝炎病毒感染和治疗肝纤维化的方法，这些方法通常涉及向需要的个体施用所述化合物或组合物的有效量。该实施例还提供了用于合成所述化合物和合成方法中间体的方法。
• Use of MDL-100,907 for treatment of allergic and eosinophil mediated diseases
  申请人：Rao Srirama P.

  公开号：US20060069124A1

  公开（公告）日：2006-03-30

  Methods of modulating eosinophil migration, chemotaxis or generation, in vitro, ex vivo, and in vivo are provided. Methods include contacting eosinophils with an amount of 5-HT2A receptor agonist or antagonist sufficient to modulate eosinophil migration, chemotaxis or generation.

  提供了调节嗜酸性粒细胞在体外、体内和体内迁移、趋化或生成的方法。方法包括将嗜酸性粒细胞与足以调节嗜酸性粒细胞迁移、趋化或生成的5-HT2A受体激动剂或拮抗剂进行接触。