2-[(2Z)-2-hydroxyiminoethyl]isoindole-1,3-dione

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 异吲哚及其衍生物
• 英文名称: 2-[(2Z)-2-hydroxyiminoethyl]isoindole-1,3-dione
• 化学式: C₁₀H₈N₂O₃
• 分子量: 204.18
• InChiKey: SKNUUPDUURWSIK-WZUFQYTHSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  70
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• AZOLE HETEROCYCLIC COMPOUND, PREPARATION METHOD, PHARMACEUTICAL COMPOSITION AND USE
  申请人：Shen Jianhua

  公开号：US20140171431A1

  公开（公告）日：2014-06-19

  The present invention relates to the field of pharmaceutical chemistry, and in particular, to a novel class of azole compounds represented by general formula (I), (II) or (III) and a preparation method thereof, a pharmaceutical composition with the compounds as active components, and a use of the azole compounds and the pharmaceutical composition in the preparation of a medicament for treatment of diseases associated with Lp-PLA 2 enzyme activities, wherein each substituent is as defined in the specification.

  本发明涉及制药化学领域，特别是一种由通式（I）、（II）或（III）表示的新型类唑化合物，以及其制备方法，以这些化合物为活性成分的药物组合物，以及在制备用于治疗与Lp-PLA2酶活性相关疾病的药物中使用这些唑化合物和药物组合物的用途，其中每个取代基如规范中定义。
• [EN] 4,5-DIHYDROISOXAZOLE DERIVATIVES AS NAMPT INHIBITORS<br/>[FR] DÉRIVÉS DE 4,5-DIHYDROISOXAZOLE UTILISÉS COMME INHIBITEURS DE NAMPT
  申请人：AURIGENE DISCOVERY TECH LTD

  公开号：WO2014111871A1

  公开（公告）日：2014-07-24

  The present invention provides substituted 4,5-dihydroisoxazole derivatives of formula (I), which may be therapeutically useful, more particularly NAMPT inhibitors and in which R1 R2, Y, X, "Het" and "p" have the meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention of diseases or disorder caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPT) in a mammal. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted 4,5-dihydroisoxazole derivatives of formula (I) or a pharmaceutically acceptable salts or stereoisomers or N-oxide thereof.

  本发明提供了式(I)的取代4,5-二氢异噁唑衍生物，可能在治疗上有用，更具体地是NAMPT抑制剂，其中R1、R2、Y、X、“Het”和“p”的含义如规范中所述，并且它们的药学上可接受的盐，在哺乳动物中治疗和预防由尼古酰胺磷酸核糖转移酶(NAMPT)水平升高引起的疾病或紊乱。本发明还提供了化合物的制备以及包含式(I)的取代4,5-二氢异噁唑衍生物中至少一个或其药学上可接受的盐或立体异构体或N-氧化物的制药配方。
• [EN] 4,5-DIHYDROISOXAZOLE DERIVATIVES AS NAMPT INHIBITORS<br/>[FR] DÉRIVÉS DE 4,5-DIHYDROISOXAZOLE COMME INHIBITEURS DE NAMPT
  申请人：AURIGENE DISCOVERY TECH LTD

  公开号：WO2016012958A1

  公开（公告）日：2016-01-28

  The present invention provides 4,5-dihydroisoxazole derivatives of formula (I), which may be therapeutically useful, more particularly as NAMPT inhibitors. wherein, ring A, L1, L2, X1, X2, X3, Z, R1, R2, R3, R4, R5, m, n, p and q have the meanings given in the specification and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention of diseases or disorder, caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPT) in a mammal. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted 4,5-dihydroisoxazole derivatives of formula (I) or a pharmaceutically acceptable salt thereof or a stereoisomer thereof.

  本发明提供了式(I)的4,5-二氢异噁唑衍生物，可能在治疗上有用，更具体地作为NAMPT抑制剂。其中，环A、L1、L2、X1、X2、X3、Z、R1、R2、R3、R4、R5、m、n、p和q在说明书中给出了它们的含义，以及它们的药用盐，在哺乳动物体内由于烟碱酸磷酸核糖转移酶(NAMPT)水平升高而引起的疾病或紊乱的治疗和预防中有用。本发明还提供了所述化合物的制备以及包含至少一种取代的式(I)的4,5-二氢异噁唑衍生物或其药用盐或立体异构体的制药配方。
• 4,5-DIHYDROISOXAZOLE DERIVATIVES AS NAMPT INHIBITORS
  申请人：AURIGENE DISCOVERY TECHNOLOGIES LIMITED

  公开号：US20170204092A1

  公开（公告）日：2017-07-20

  The present invention provides 4,5-dihydroisoxazole derivatives of formula (I), which may be therapeutically useful, more particularly as NAMPT inhibitors. wherein, ring A, L 1 , L 2 , X 1 , X 2 , X 3 , Z, R 1 , R 2 , R 3 , R 4 , R 5 , m, n, p and q have the meanings given in the specification and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention of diseases or disorder, caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPT) in a mammal. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted 4,5-di hydroisoxazole derivatives of formula (I) or a pharmaceutically acceptable salt thereof or a stereoisomer thereof.