扎那米韦(抗流感药) | 171094-50-1

• 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
• 中文名称: 扎那米韦(抗流感药)
• 英文名称: Zanamivir hydrate
• 英文别名: (2R,3R,4S)-3-acetamido-4-(diaminomethylideneamino)-2-[(1R,2R)-1,2,3-trihydroxypropyl]-3,4-dihydro-2H-pyran-6-carboxylic acid;hydrate
• CAS: 171094-50-1
• 化学式: C12H22N4O8
• 分子量: 350.33
• InChiKey: OELRRAURPSTFEX-VCFRRRQNSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -4.61
• 重原子数：
  24
• 可旋转键数：
  6
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.58
• 拓扑面积：
  202
• 氢给体数：
  8
• 氢受体数：
  9

文献信息

• A MEDICAMENT FOR TREATING INFLUENZA CHARACTERIZED BY COMBINING A CAP-DEPENDENT ENDONUCLEASE INHIBITOR AND AN ANTI-INFLUENZA DRUG
  申请人：Shionogi & Co., Ltd.

  公开号：US20200261481A1

  公开（公告）日：2020-08-20

  A medicament characterized in that (A) a compound represented by the formula (I): its pharmaceutically acceptable salt, or a solvate thereof, wherein P is hydrogen or a group to form a prodrug; A 1 is CR 1A R 1B , S or O; A 2 is CR 2A R 2B , S or O; A 3 is CR 3A R 3B , S or O; A 4 is each independently CR 4A R 4B , S or O; the number of hetero atoms among atoms constituting the ring which consists of A 1 , A 2 , A 3 , A 4 , nitrogen atom adjacent to A 1 and carbon atom adjacent to A 4 is 1 or 2; R 1A and R 1B are each independently hydrogen, halogen, alkyl or the like; R 2A and R 2B are each independently hydrogen, halogen, alkyl, or the like; R 3A and R 3B are each independently hydrogen, halogen, alkyl, or the like; R 4A are each independently hydrogen, halogen, alkyl, or the like; R 4B are each independently hydrogen, halogen, alkyl, or the like; R 3A and R 3B may be taken together with an adjacent carbon atom to form non-aromatic carbocycle or non-aromatic heterocycle; n is any integer of 1 to 2; and R 1 is or the like, is combined with (B) compound(s) having an anti-influenza activity, its pharmaceutically acceptable salt or a solvate thereof and/or an antibody having anti-influenza activity, is useful for treating or preventing influenza.

  一种药物，其特征在于（A）由以下式（I）表示的化合物： 其药学上可接受的盐，或其溶剂合物， 其中 P为氢或形成前药的基团; A 1 为CR 1A R 1B 、S或O; A 2 为CR 2A R 2B 、S或O; A 3 为CR 3A R 3B 、S或O; A 4 分别为独立的CR 4A R 4B 、S或O; 构成由A 1 、A 2 、A 3 、A 4 、邻接到A 1 的氮原子和邻接到A 4 的碳原子的环的原子中的杂原子数为1或2; R 1A 和R 1B 分别为独立的氢、卤素、烷基或类似物; R 2A 和R 2B 分别为独立的氢、卤素、烷基或类似物; R 3A 和R 3B 分别为独立的氢、卤素、烷基或类似物; R 4A 分别为独立的氢、卤素、烷基或类似物; R 4B 分别为独立的氢、卤素、烷基或类似物; R 3A 和R 3B 可以与相邻的碳原子结合形成非芳香碳环或非芳香杂环; n为1到2的任意整数; 和 R 1 为 或类似物， 与具有抗流感活性的（B）化合物，其药学上可接受的盐或其溶剂合物和/或具有抗流感活性的抗体结合，用于治疗或预防流感。
• TEST AGENTS FOR EVALUATING PHARMACOLOGICAL EFFECT OF DRUG, AND METHOD AND REAGENTS FOR SCREENING DRUG HAVING EXCELLENT ADMINISTRATION EFFECT AND/OR LITTLE SIDE EFFECT FROM AMONG DRUGS COMPRISING ENZYMES, ENZYME INHIBITORS OR RECEPTOR LIGANDS AND/OR PRODURGS THEREOF
  申请人：Tokyo Gas Company Limited

  公开号：EP1486785A1

  公开（公告）日：2004-12-15

  A diagnostic reagent for use in the evaluation of a pharmacological effect of a medicine containing a pharmaceutical agent including an enzyme, an enzyme inhibitor or a receptor ligand or a prodrug of the pharmaceutical agent; and a method of screening pharmaceutical agents each comprising an enzyme, an enzyme inhibitor or a receptor ligand and/or prodrugs of the pharmaceutical agents for one or ones having high medicative efficacy and/or a small side effect are provided. The diagnostic reagent and the reagent used in the method comprise: (a) a compound which serves as a substrate for the enzyme contained in the medicine or the pharmaceutical agent to be evaluated or for an enzyme generated from the prodrug contained in the medicine or the pharmaceutical agent to be evaluated, or a pharmaceutically acceptable salt thereof; (b) a compound which serves as a substrate for a different enzyme capable of exhibiting an alteration in activity by coupling to the effect of the enzyme in (a), or a pharmaceutically acceptable salt thereof; (c) a compound which serves as a substrate for an enzyme which is directly inhibited by the enzyme inhibitor contained in the medicine or the pharmaceutical agent to be evaluated or by an enzyme inhibitor generated from the prodrug contained in the medicine or the pharmaceutical agent to be evaluated, or a pharmaceutically acceptable salt thereof; (d) a compound which serves as a substrate for an enzyme capable of exhibiting an alteration in activity by coupling to the effect of the enzyme inhibitor in (c), or a pharmaceutically acceptable salt thereof; (e) a compound which serves as a substrate for an enzyme capable of exhibiting an alteration in activity by the binding between a receptor and the receptor ligand contained in the medicine or the pharmaceutical agent to be evaluated or a receptor ligand generated from the prodrug contained in the medicine or the pharmaceutical agent to be evaluated, or a pharmaceutically acceptable salt thereof; or (f) a labeled form of any one of the substances (a) to (e).

  本发明提供了一种诊断试剂，用于评估含有药剂（包括酶、酶抑制剂或受体配体或药剂的原药）的药物的药理作用；以及一种筛选药剂的方法，筛选出一种或多种药效高和/或副作用小的药剂，每种药剂都包括酶、酶抑制剂或受体配体和/或药剂的原药。诊断试剂和方法中使用的试剂包括(a) 作为待评价的药物或药剂中所含酶或由待评价的药物或药剂中所含原药生成的酶的底物的化合物，或其药学上可接受的盐； (b) 作为能通过与(a)中酶的作用偶联而显示活性改变的不同酶的底物的化合物，或其药学上可接受的盐；(c) 作为一种酶的底物的化合物，该酶被待评价的药物或药剂中所含的酶抑制剂或 由待评价的药物或药剂中所含的原药生成的酶抑制剂直接抑制，或其药学上可接 受的盐；(d) 作为酶底物的化合物，该酶能通过与(c)中酶抑制剂的作用偶联而显示活性的改变，或其药学上可接受的盐；(e) 可作为酶底物的化合物，通过受体与待评价药物或药剂中所含受体配体或由待 评价药物或药剂中所含原药生成的受体配体之间的结合而显示出活性的改变， 或其药学上可接受的盐；或 (f) (a)至(e)中任何一种物质的标记形式。
• USE OF IMMUNESUPPRESSANT RECEPTOR
  申请人：ONO PHARMACEUTICAL CO., LTD.

  公开号：EP1806147A1

  公开（公告）日：2007-07-11

  The present invention relates to use of an antagonist of BIR1 (B cell immunoglobulin receptor 1) related to the present invention, a method for screening the antagonist, in addition to subtype polypeptides of BIR1, the polynucleotide encoding them and antibodies for the polypeptides. BIR1 functions as an immunosuppressive receptor, and the antagonist of BIRI has immunopotentive activity, which is able to use for preventing and/or treating a cancer, an immunodeficiency disease or an infectious disease.

  本发明涉及与本发明相关的BIR1（B细胞免疫球蛋白受体1）拮抗剂的用途、筛选拮抗剂的方法，此外还涉及BIR1的亚型多肽、编码它们的多核苷酸和多肽抗体。 BIR1 具有免疫抑制受体的功能，BIRI 的拮抗剂具有免疫刺激活性，可用于预防和/或治疗癌症、免疫缺陷病或传染病。
• MULTIMER OF EXTRACELLULAR DOMAIN OF CELL SURFACE FUNCTIONAL MOLECULE
  申请人：Kyoto University

  公开号：EP1997887A1

  公开（公告）日：2008-12-03

  As a substance which pharmacologically regulates the function of a cell surface functional molecule, a substance which has specificity and an activity or efficacy equal or superior to an antibody and does not require an advanced production technique and facility for application thereof to a pharmaceutical product has been demanded. The invention relates to a multimer of an extracellular domain of a cell surface functional molecule, particularly a tetramer of an extracellular domain of PD-1 or PD-L1. Further, the invention relates to an application of such a tetramer as a preventive and/or therapeutic agent for cancer, cancer metastasis, immunodeficiency, an infectious disease or the like and an application of PD-1 or PD-L1 as a testing or diagnostic agent or a research agent for such a disease.

  作为一种对细胞表面功能分子的功能进行药理调节的物质，人们需要一种特异性强、活性或疗效等同或优于抗体，并且不需要先进的生产技术和设备就能将其应用于医药产品的物质。本发明涉及一种细胞表面功能分子胞外结构域的多聚体，特别是 PD-1 或 PD-L1 胞外结构域的四聚体。此外，本发明还涉及这种四聚体作为癌症、癌症转移、免疫缺陷、传染性疾病或类似疾病的预防和/或治疗剂的应用，以及PD-1或PD-L1作为此类疾病的检测剂、诊断剂或研究剂的应用。
• SPRAYABLE GEL-TYPE SKIN/MUCOSA-ADHESIVE PREPARATION AND ADMINISTRATION SYSTEM USING THE PREPARATION
  申请人：Toko Yakuhin Kogyo Kabushiki Kaisha

  公开号：EP2014305A1

  公开（公告）日：2009-01-14

  The present invention provides a sprayable gel-type skin/mucosa-adhesive preparation comprising a gel formulation which contains an active pharmaceutical ingredient in a gel base material comprising a skin/mucosa-adhesive agent and an administration system comprising the preparation.

  本发明提供了一种可喷雾凝胶型皮肤/粘膜粘合剂制剂，它包括一种凝胶制剂（在包含皮肤/粘膜粘合剂的凝胶基质材料中含有活性药物成分）和一种包含该制剂的给药系统。