α-Phthalimidooxy-γ-butyrolactone | 78931-05-2

• 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: α-Phthalimidooxy-γ-butyrolactone
• 英文别名: N-(2-oxo-3-tetrahydrofuryloxy)phthalimide；2-[(2-Oxooxolan-3-yl)oxy]-1H-isoindole-1,3(2H)-dione；2-(2-oxooxolan-3-yl)oxyisoindole-1,3-dione
• CAS: 78931-05-2
• 化学式: C₁₂H₉NO₅
• 分子量: 247.207
• InChiKey: AYTOSMACNLSHJY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  18
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  72.9
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  α-Phthalimidooxy-γ-butyrolactone 、 盐酸 在 ice 、 甲苯 、 水 作用下， 反应 0.17h， 以0.75 g of the desired material was obtained的产率得到α-Aminooxy-γ-butyrolactone hydrochloride
  参考文献：
  名称：

  Indole-2,3-dione-3-oxime derivatives

  摘要：

  Indole-2,3-二酮-3-肟衍生物，例如由以下公式表示的化合物，能够拮抗兴奋性氨基酸（如谷氨酸）的作用。还公开了制备这些化合物的方法、包含它们的制药组合物以及治疗对兴奋性氨基酸受体拮抗剂有反应的疾病或疾病的方法。

  公开号：

  US06693111B1

文献信息

• [EN] ISATINE DERIVATIVES WITH NEUROTROPHIC ACTIVITY<br/>[FR] DERIVES DE L'ISATINE A ACTIVITE NEUROTROPHIQUE
  申请人：NEUROSEARCH AS

  公开号：WO2001055110A1

  公开（公告）日：2001-08-02

  The present invention relates to novel isatin derivatives, pharmaceutical compositions comprising the isatin derivatives of the invention, methods of preparing the isatin derivatives of the invention, their use in the treatment of neurodegenerative diseases and for the regeneration or prevention of degeneration of lesioned and damaged neurons, and methods of treatment of neurodegenerative diseases and for the regeneration or prevention of degeneration of lesioned and damaged neurons.

  本发明涉及新型异喹啉衍生物，包括本发明的异喹啉衍生物的制药组合物，制备本发明的异喹啉衍生物的方法，它们在治疗神经退行性疾病和再生或预防损伤和受损神经元的退化中的使用，以及神经退行性疾病的治疗和再生或预防受损神经元的退化的方法。
• Indole-2,3-dione-3-oxime derivatives for therapeutic use
  申请人：Neurosearch A/S

  公开号：US06239128B1

  公开（公告）日：2001-05-29

  The present invention relates to the use of indole-2,3-dione-3-oxime derivatives in a method of combating diseases and disorders associated with or mediated by the release of excitatory amino acids.

  本发明涉及使用吲哚-2,3-二酮-3-肟衍生物来对抗与兴奋性氨基酸释放相关或介导的疾病和障碍的方法。
• Indole-2,3-dione-3-oxime derivatives
  申请人：Neurosearch A/S

  公开号：US06124285A1

  公开（公告）日：2000-09-26

  The present invention relates to novel indole-2,3-dione-3-oxime derivatives capable of antagonising the effect of excitatory amino acids, such as glutamate. More specifically the novel indole-2,3-dione-3-oxime derivatives of the invention may be described by general formula (I), wherein R.sup.3 represents "Het", or a group of formula (II), wherein "Het" represents a saturated or unsaturated, 4 to 7 membered, monocyclic, heterocyclic ring, at least one of R.sup.31, R.sup.32, and R.sup.33 independendy represents hydrogen, alkyl, or hydroxyalkyl, and at least one of R.sup.31, R.sup.32, and R.sup.33 independently represents (CH.sub.2).sub.n R.sup.34 ; wherein R.sup.34 represents hydroxy, carboxy, alkoxycarbonyl, alkenyloxycarbonyl, alkynyloxycarbonyl, cycloalkoxycarbonyl, cycloalkyl-alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, CONR.sup.35 R.sup.36, or "Het"; wherein n is 0, 1, 2, or 3; and R.sup.5 represents phenyl, naphthyl, thienyl, or pyridyl, all of which may be substituted. "A" represents a ring of five to seven atoms fused with the benzo ring at the positions marked "a" and "b", and formed by the following bivalent radicals: a-NR.sup.6 --CH.sub.2 --CH.sub.2 -b; a-CH.sub.2 --NR.sup.6 --CH.sub.2 -b; a-CH.sub.2 --CH.sub.2 --NR.sup.6 -b; a-NR.sup.6 --CH.sub.2 --CH.sub.2 --H.sub.2 -b; a-CH.sub.2 --NR.sup.6 --CH.sub.2 --CH.sub.2 -b; a--CH.sub.2 --CH.sub.2 --NR.sup.6 --CH.sub.2 -b; a-CH.sub.2 --CH.sub.2 --CH.sub.2 --NR.sup.6 -b; a-NR.sup.6 --CH.sub.2 --CH.sub.2 --CH.sub.2 --CH.sub.2 -b; a-CH.sub.2 --NR.sup.6 --CH.sub.2 --CH.sub.2 --CH.sub.2 -b; a-CH.sub.2 --CH.sub.2 --NR.sup.6 --CH.sub.2 --CH.sub.2 -b; a-CH.sub.2 --CH.sub.2 --CH.sub.2 --NR.sup.6 --CH.sub.2 -b; or a-CH.sub.2 --CH.sub.2 --CH.sub.2 --CH.sub.2 --NR.sup.6 -b; wherein R.sup.6 represents hydrogen, alkyl or CH.sub.2 CH.sub.2 OH; or a pharmaceutically acceptable salt thereof.

  本发明涉及新颖的吲哚-2,3-二酮-3-羟肟衍生物，能够拮抗兴奋性氨基酸（如谷氨酸）的作用。更具体地，本发明的新颖吲哚-2,3-二酮-3-羟肟衍生物可以由通式（I）表示，其中R.sup.3表示“Het”，或式（II）的基团，其中“Het”表示饱和或不饱和，4至7个成员的单环杂环，R.sup.31、R.sup.32和R.sup.33中的至少一个独立地表示氢、烷基或羟基烷基，R.sup.31、R.sup.32和R.sup.33中的至少一个独立地表示（CH.sub.2）.sub.nR.sup.34；其中R.sup.34表示羟基、羧基、烷氧基羰基、烯基氧基羰基、炔基氧基羰基、环烷氧基羰基、环烷基-烷氧基羰基、芳基氧基羰基、芳基烷氧基羰基、CONR.sup.35R.sup.36或“Het”；其中n为0、1、2或3；R.sup.5表示苯基、萘基、噻吩基或吡啶基，均可被取代。“A”表示在标记为“a”和“b”的位置与苯环融合的五至七原子环，由以下双价基团形成：a-NR.sup.6--CH.sub.2--CH.sub.2-b；a-CH.sub.2--NR.sup.6--CH.sub.2-b；a-CH.sub.2--CH.sub.2--NR.sup.6-b；a-NR.sup.6--CH.sub.2--CH.sub.2--H.sub.2-b；a-CH.sub.2--NR.sup.6--CH.sub.2--CH.sub.2-b；a--CH.sub.2--CH.sub.2--NR.sup.6--CH.sub.2-b；a-CH.sub.2--CH.sub.2--CH.sub.2--NR.sup.6-b；a-NR.sup.6--CH.sub.2--CH.sub.2--CH.sub.2--CH.sub.2-b；a-CH.sub.2--NR.sup.6--CH.sub.2--CH.sub.2--CH.sub.2-b；a-CH.sub.2--CH.sub.2--NR.sup.6--CH.sub.2--CH.sub.2-b；a-CH.sub.2--CH.sub.2--CH.sub.2--NR.sup.6--CH.sub.2-b；或a-CH.sub.2--CH.sub.2--CH.sub.2--CH.sub.2--NR.sup.6-b；其中R.sup.6表示氢、烷基或CH.sub.2CH.sub.2OH；或其药学上可接受的盐。
• Cephem and cepham compounds, processes for their preparation, pharmaceutical compositions containing them
  申请人：FUJISAWA PHARMACEUTICAL CO., LTD.

  公开号：EP0013762A2

  公开（公告）日：1980-08-06

  Cephem and Cepham compounds of the formula: wherein R1 is amino or a protected amino, R2 is hydrogen or certain substituent. R3 is hydrogen or lower alkyl, R4 is hydrogen or certain substituent, Rs is carboxy or a protected carboxy and the heavy solid line means single or double-bond and pharmaceutically acceptable salt thereof and processes for their preparation, and also an antibacterial composition comprising, as an effective ingredient, the above compound in association with a pharmaceutically acceptable, substantially nontoxic carrier or excipient. The invention also relates to the starting compounds and their preparation.

  式中的 Cephem 和 Cepham 化合物： 式中 R1 是氨基或受保护的氨基、 R2 是氢或某些取代基 R3 是氢或低级烷基、 R4 是氢或某些取代基、 Rs 是羧基或受保护的羧基 重实线表示单键或双键及其药学上可接受的盐和它们的制备工艺，以及一种抗菌组合物，其有效成分包括上述化合物与药学上可接受的、基本上无毒的载体或赋形剂。本发明还涉及起始化合物 及其制备。
• Cephem compounds, processes for their preparation and pharmaceutical compositions containing them
  申请人：FUJISAWA PHARMACEUTICAL CO., LTD.

  公开号：EP0027599A2

  公开（公告）日：1981-04-29

  New cephem compounds of the formula: wherein R1 is amino or a protected amino group; R2 is hydrogen, lower alkyl which may be substituted with suitable substituent(s), lower alkenyl, lower alkynyl, cyclo(lower)-alkyl, cyclo(lower)alkenyl, or O containing 5-membered heterocyclic group substituted with oxo group(s); R3 is a group of the formula: wherein X is hydrogen or carbamoyl; and R' is -COO-; or R3 is 2-lower alkyl-5-oxo-6-hydroxy-2,5-dihydro-1, 2,4-triazinylthio; and R4 is carboxy or protected carboxy, and pharmaceutically acceptable salts thereof, and process for their preparation, and also a pharmaceutical composition comprising, as an effective ingredient, the above compound in association with a pharmaceutically acceptable, substantially nontoxic carrier or excipient. The invention also relates to the inter. mediate compounds and and their preparation,

  新的 cephem 化合物式： 其中 R1 是氨基或受保护的氨基； R2 是氢、可被适当取代基取代的低级烷基、低级烯基、低级炔基、环（低）烷基、环（低）烯基或被氧代基取代的含 O 的 5 元杂环基团； R3 是式中的基团： 其中 X 是氢或氨基甲酰基；以及 R' 是 -COO-；或 R3 是 2-低级烷基-5-氧代-6-羟基-2,5-二氢-1、 2，4-三嗪硫基；以及 R4是羧基或受保护的羧基，及其药学上可接受的盐和制备方法，以及一种药物组合物，其有效成分包括上述化合物与药学上可接受的、基本上无毒的载体或赋形剂。本发明还涉及中间体化合物 和 及其制备、