(2Z)-N-(3,4-dimethylphenyl)-2-hydroxyiminoacetamide

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: (2Z)-N-(3,4-dimethylphenyl)-2-hydroxyiminoacetamide
• 化学式: C₁₀H₁₂N₂O₂
• 分子量: 192.21
• InChiKey: WDWMUOGEOATZNF-WDZFZDKYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  14
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  61.7
• 氢给体数：
  2
• 氢受体数：
  3

文献信息

• Piperidine derivatives having ccr3 antagonism
  申请人：Matsumoto Yoshiyuki

  公开号：US20070032525A1

  公开（公告）日：2007-02-08

  The invention provides low molecular compounds having activity which inhibits binding of CCR3 ligands to CCR3 on target cells, i.e. CCR3 antagonists. The invention also provides compounds represented by formula (I) below, pharmaceutically acceptable acid adducts thereof, or pharmaceutically acceptable C 1 -C 6 alkyl adducts thereof, as well as pharmaceutical compositions comprising them as effective ingredients, which are useful for treatment or prevention of diseases associated with CCR3, such as asthma and allergic rhinitis.

  本发明提供了具有抑制CCR3配体结合到靶细胞CCR3的活性的低分子化合物，即CCR3拮抗剂。本发明还提供了由下式（I）表示的化合物，其药学上可接受的酸加合物或药学上可接受的C1-C6烷基加合物，以及包含它们作为有效成分的制药组合物，用于治疗或预防与CCR3相关的疾病，例如哮喘和过敏性鼻炎。
• 4,4-Disubstituted) piperidine derivatives having ccr3 antagonism
  申请人：Matsumoto Yoshiyuki

  公开号：US20070037851A1

  公开（公告）日：2007-02-15

  The invention provides low molecular compounds having activity which inhibits binding of CCR3 ligands to CCR3 on target cells, i.e. CCR3 antagonists. The invention also provides 4,4-(disubstituted)piperidine derivatives represented by formula (I) below, pharmaceutically acceptable acid adducts thereof, or pharmaceutically acceptable C 1 -C 6 alkyl adducts thereof, as well as pharmaceutical compositions comprising them as effective ingredients, which are useful for treatment or prevention of diseases associated with CCR3, such as asthma and allergic rhinitis.

  本发明提供了具有抑制CCR3配体与靶细胞上CCR3结合活性的低分子化合物，即CCR3拮抗剂。本发明还提供了由下式（I）所表示的4,4-(二取代)哌啶衍生物，其药学上可接受的酸加合物或药学上可接受的C1-C6烷基加合物，以及包含它们作为有效成分的药物组合物，用于治疗或预防与CCR3相关的疾病，如哮喘和过敏性鼻炎。
• 3-Substituted 2-oxindole-1-carboxamides as analgesic and anti-inflammatory agents
  申请人：PFIZER INC.

  公开号：EP0156603A2

  公开（公告）日：1985-10-02

  2-Oxindole-1-carboxamides of the formula: and their pharmaceutically acceptable base-salts, where X and Y are certain optional substituents or can be taken together to form certain ring structures; and R1 is alkyl, cycloalkyl, cycloalkenyl, optionally substituted phenyl, optionally substituted phenylalkyl, optionally substituted phenoxyalkyl, (thiophenoxy) alkyl, naphthyl, bicyclo [2.2.1]heptan-2-yl, bicyclo [2.2.1]hept-5-en-2-yl or a group of the formula -(CH2)n-O-R° where n is 0, 1 or 2, Q is a divalent radical which is a specified heterocycle, and R° is H or alkyl. The compounds are useful as analgesic and anti-inflammatory agents. Also covered are certain intermediates useful in the preparation of the compounds (I), these intermediates having H in place of -CORI.

  式中的 2-吲哚-1-甲酰胺： 及其药学上可接受的碱基盐，其中 X 和 Y 是某些任选取代基，或可共同形成某些环结构；R1 是烷基、环烷基、环烯基、任选取代的苯基、任选取代的苯基烷基、任选取代的苯氧基烷基、（噻吩氧基）烷基、萘基、双环 [2.2.2.1]庚-2-基、双环[2.2.1]庚-5-烯-2-基或式-(CH2)n-O-R°的基团，其中 n 为 0、1 或 2，Q 为指定杂环的二价基，R° 为 H 或烷基。 这些化合物可用作镇痛剂和消炎剂。 此外，还包括某些用于制备化合物（I）的中间体，这些中间体中的 H 取代了-CORI。
• N,3-disubstituted 2-oxindole-1-carboxamides as analgesic and antiinflammatory agents
  申请人：PFIZER INC.

  公开号：EP0164860A1

  公开（公告）日：1985-12-18

  Certain 2-oxindole-lcarboxamide compounds having an acyl substituent at the 3-position, and also further substituted on the carboxamide nitrogen by an alkyl, cycloalkyl, phenyl or substituted phenyl group, are inhibitors of the cyclooxygenase (CO) and lipoxygenase (LO) enzymes, and are useful as analgesic and antiinflammatory agents in mammalian subjects. These 2-oxindole-lcarboxamide compounds are of particular value for ameliorating pain in human patients recovering from surgery or trauma, and alleviating the symptoms of chronic diseases, such as rheumatoid arthritis and ostoarthritis, in human subjects. Certain 2-oxind ole-1-carboxamide compounds unsubstituted at C-3, but having a substituent on the carboxamide nitrogen, are useful as intermediates to the analgesic and antiinflammatory agents of the invention.

  某些 2-氧吲哚-甲酰胺化合物在 3 位上具有酰基取代基，在羧酰胺氮上还进一步被烷基、环烷基、苯基或取代苯基取代，是环氧化酶（CO）和脂氧合酶（LO）的抑制剂，可用作哺乳动物的镇痛剂和抗炎剂。这些 2-氧化吲哚-甲酰胺化合物对于改善手术或创伤后恢复期人类患者的疼痛，以及减轻人类慢性疾病（如类风湿性关节炎和骨关节炎）的症状具有特殊价值。 某些在 C-3 处未被取代但在羧酰胺氮上具有取代基的 2-氧代吲哚-1-甲酰胺化合物可作为本发明镇痛剂和抗炎剂的中间体。
• Process for making 2-oxindole-1-carboxamides and intermediates therefor
  申请人：PFIZER INC.

  公开号：EP0155828A2

  公开（公告）日：1985-09-25

  Covers oxindole intermediates, and their preparation, of the formula: wherein X and Y are certain stated substituents or may when taken together form certain ring structures, and R is H or -COR1 where R1 is alkyl, cycloalkyl, cycloalkenyl, optionally substituted phenyl, optionally substituted phenylalkyl, optionally substituted phenoxyalkyl, (thiophenoxy)alkyl, naphthyl, bicyclo[2.2.1]heptan-2-yl, bicyclo[2.2.1]hept-5-en-2-yl or -(CH2)n-Q-R' where n is 0, 1 or 2, Q is a divalent radical which is a specified heterocycle, and R° is H or alkyl; and also covers the hydrolysis of the compounds (II) to end products of the formula:

  包括式中的吲哚中间体及其制备方法： 其中 X 和 Y 是某些指定的取代基，或共同形成某些环结构，R 是 H 或 -COR1 其中 R1 是烷基、环烷基、环烯基、任选取代的苯基、任选取代的苯基烷基、任选取代的苯氧基烷基、（噻吩氧基）烷基、萘基、双环[2.2.2.1]庚-2-基、双环[2.2.1]庚-5-烯-2-基或-(CH2)n-Q-R'，其中 n 是 0、1 或 2，Q 是二价基，它是特定的杂环，R° 是 H 或烷基；还包括将化合物 (II) 水解成式中的最终产物：