2,3-dihydropyrrolo[1,2,3-de]-1,4-benzoxazine-5,6-dione | 99435-07-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并恶嗪类
• 英文名称: 2,3-dihydropyrrolo[1,2,3-de]-1,4-benzoxazine-5,6-dione
• 英文别名: 9-oxa-1-azatricyclo[6.3.1.04,12]dodeca-4(12),5,7-triene-2,3-dione
• CAS: 99435-07-1
• 化学式: C₁₀H₇NO₃
• 分子量: 189.17
• InChiKey: ZLOJHYZGNQHKPP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  14
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  46.6
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2,3-dihydropyrrolo[1,2,3-de]-1,4-benzoxazine-5,6-dione 生成 ethyl (2Z)-2-cyano-2-(2-oxo-9-oxa-1-azatricyclo[6.3.1.04,12]dodeca-4(12),5,7-trien-3-ylidene)acetate
  参考文献：
  名称：

  IRIKURA, TSUTOMU;TAKANI, XIROKADZU;FUDZIMORI, KIEESI;XIRATA, JOSIXIRO;XIR+

  摘要：

  DOI：
• 作为产物：
  描述：

  4-(氯乙酰基)-3,4-二氢-2H-1,4-苯并噁嗪 在 盐酸 、 sodium hydroxide 、 N,N-二甲基-4-亚硝基苯胺 作用下， 生成 2,3-dihydropyrrolo[1,2,3-de]-1,4-benzoxazine-5,6-dione
  参考文献：
  名称：

  Synthesis and antirheumatic activity of novel tetrahydroquinoline-8-carboxylic acid derivatives

  摘要：

  A study of the modification of N-alkylanthranilic acids to develop novel DMARDs is detailed. 1,2,3,4-Tetrahydroquinoline-8-carboxylic acid derivatives were found to exhibit a therapeutic effect on adjuvant arthritis and a suppressive effect on bone destruction. (C) 1997 Elsevier Science Ltd.

  DOI：

  10.1016/s0960-894x(97)00261-8

文献信息

• Cyclic anthranilic acid derivatives and process for their preparation
  申请人：Kyorin Pharmaceutical Co., Ltd.

  公开号：US04956372A1

  公开（公告）日：1990-09-11

  An antirheumatoid pharmaceutical composition containing a cyclic anthranilic acid derivative of the following formula, ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 each independently indicate a hydrogen atom, lower alkyl group having 1 to 3 carbon atoms, lower alkoxy group having 1 to 3 carbon atoms, amino group, nitro group, hydroxy group, sulfonamide group, trifluoromethyl group, cyano group, carboxyl group, carbamoyl group, acetyl group, benzoylmethyl group which may be substituted, methylthio group, phenylethynyl group which may be substituted, ethynyl group which may be substituted, alkanoylamino group having 1 to 3 carbon atoms, benzoylamino group which may be substituted, alkylsulfonylamino group having 1 to 3 carbon atoms or phenylsulfonylamino group which may be substituted; R.sup.4 and R.sup.5 each independently indicate a hydrogen atom, lower alkyl group having 1 to 3 carbon atoms, cyano group, carboxyl group, hydroxymethyl group, phenyl group which may be substituted or benzyl group; R.sup.6 indicates a hydrogen atom, lower alkyl group having 1 to 3 carbon atoms or benzyl group; X indicates a methylene group; their acid or alkali salts and an inert, pharmaceutically acceptable carrier.

  一种抗风湿药物组合物，包含下列公式的环状蒽醌酸衍生物：##STR1## 其中R.sup.1，R.sup.2和R.sup.3各自独立表示氢原子，具有1至3个碳原子的低级烷基，具有1至3个碳原子的低级烷氧基，氨基，硝基，羟基，磺酰胺基，三氟甲基基团，氰基，羧基，氨基甲酰基，乙酰基，苯甲酰甲基基团，可以被取代的甲硫基基团，可以被取代的苯乙炔基团，可以被取代的乙炔基团，具有1至3个碳原子的脂肪酰胺基，可以被取代的苯甲酰胺基，具有1至3个碳原子的烷基磺酰胺基或可以被取代的苯基磺酰胺基；R.sup.4和R.sup.5各自独立表示氢原子，具有1至3个碳原子的低级烷基，氰基，羧基，羟甲基基团，可以被取代的苯基或苄基；R.sup.6表示氢原子，具有1至3个碳原子的低级烷基或苄基；X表示亚甲基基团；它们的酸或碱盐以及惰性的、药学上可接受的载体。
• Cyclic anthranilic acid derivatives
  申请人：Kyorin Pharmaceutical Co., Ltd.

  公开号：US05281600A1

  公开（公告）日：1994-01-25

  An antirheumatoid pharmaceutical composition containing a cyclic anthranilic acid derivative of the following formula, ##STR1## wherein R.sup.1, and R.sup.2 and R.sup.3 each independently indicate a hydrogen atom, halogen atom, lower alkyl group having 1 to 3 carbon atoms, lower alkoxy group having 1 to 3 carbon atoms, amino group, nitro group, hydroxy group, sulfonamide group, trifluoromethyl group, cyano group, carboxyl group, carbamoyl group, acetyl group, benzoylmethyl group which may be substituted, methylthio group, phenylethynyl group which may be substituted, ethynyl group which may be substituted, alkanoylamino group having 1 to 3 carbon atoms, benzoylamino group which may be substituted, alkylsulfonylamino group having 1 to 3 carbon atoms or phenylsulfonylamino group which may be substituted; R.sup.4 and R.sup.5 each independently indicate a hydrogen atom, lower alkyl group having 1 to 3 carbon atoms, cyano group, carboxyl group, hydroxymethyl group, phenyl group which may be substituted or benzyl group; R.sup.6 indicates a hydrogen atom, lower alkyl group having 1 to 3 carbon atoms or benzyl group; X is a methylene; the acid or alkali salts thereof and an insert, pharamaceutically acceptable carrier.

  一种抗风湿药物组合物，包含下列公式的环状蒽醌酸衍生物：##STR1##其中，R.sup.1、R.sup.2和R.sup.3各自独立表示氢原子、卤素原子、具有1至3个碳原子的低级烷基基团、具有1至3个碳原子的低级烷氧基基团、氨基基团、硝基基团、羟基基团、磺酰胺基团、三氟甲基基团、氰基、羧基、氨基甲酰基、乙酰基基团、苯甲酰甲基基团，其可以被取代、甲硫基基团、苯乙炔基团，其可以被取代、乙炔基团，其可以被取代、具有1至3个碳原子的烷酰胺基团、可以被取代的苯甲酰胺基团、具有1至3个碳原子的烷基磺酰胺基团或可以被取代的苯基磺酰胺基团；R.sup.4和R.sup.5各自独立表示氢原子、具有1至3个碳原子的低级烷基基团、氰基、羧基、羟甲基基团、可以被取代的苯基或苯甲基基团；R.sup.6表示氢原子、具有1至3个碳原子的低级烷基基团或苯甲基基团；X为亚甲基；其酸或碱盐以及插入物、药学上可接受的载体。
• Spiro-linked pyrrolidine-2,5-diones and process for their preparation
  申请人：KYORIN PHARMACEUTICAL CO., LTD.

  公开号：EP0147805A2

  公开（公告）日：1985-07-10

  The invention provides a novel spiro-linked pyrrolidine-2,5-dione of the formula;- wherein X1 and X2 each independently represent a hydrogen, a halogen atom, a lower alkyl or lower alkoxy group; Y is a methylene group, oxygen or sulfur atom; R1, R2, R3 and R4 each independently represent a hydrogen atom, a lower alkyl group or forming a benzene ring together with their adjacent carbon atoms; the base salts thereof with pharmaceutically acceptable cations, and processes for their manufactures. The compounds of formula [I] useful as aldose reductase inhibitors and as therapeutic agents for treatment of chronic diabetic complications are also disclosed.

  本发明提供了一种新颖的螺联吡咯烷-2,5-二酮，其式如下 其中X1和X2各自独立地代表氢、卤素原子、低级烷基或低级烷氧基；Y是亚甲基、氧原子或硫原子；R1、R2、R3和R4各自独立地代表氢原子、低级烷基或与其相邻碳原子一起形成苯环；其与药学上可接受的阳离子的基盐及其制造工艺。 还公开了作为醛糖还原酶抑制剂和治疗慢性糖尿病并发症的治疗剂的式[I]化合物。
• Novel cyclic anthranilic acid derivatives and process for their preparation
  申请人：KYORIN PHARMACEUTICAL CO., LTD.

  公开号：EP0310096A2

  公开（公告）日：1989-04-05

  Cyclic anthranilic acid derivatives of the following formula, wherein R¹, R² and R³ each independently indicate a hydrogen atom, lower alkyl group having 1 to 3 carbon atoms, lower alkoxy group having 1 to 3 carbon atoms, amino group, nitro group, hydroxy group, sulfonamide group, trifluoromethyl group, cyano group, carboxyl group, carbamoyl group, acetyl group, benzoyl­methyl group which may be substituted, methylthio group, phenyl­ethynyl group which may be substituted, ethynyl group which may be substituted, alkanoylamino group having 1 to 3 carbon atoms, benzoylamino group which may be substituted, alkylsulfonylamino group having 1 to 3 carbon atoms or phenylsulfonylamino group which may be substituted; R⁴ and R⁵ each independently indicate a hydrogen atom, lower alkyl group having 1 to 3 carbon atoms, cyano group, carboxyl group, hydroxymethyl group, phenyl group which may be substituted or benzyl group; R⁶ indicates a hydrogen atom, lower alkyl group having 1 to 3 carbon atoms or benzyl group; X indicates a methylene group, oxygen atom, sulfur atom, sulfinyl group or sulfonyl group; their acid or alkali salts thereof are useful as antirheumatoid agents.

  下式的环状蒽酸衍生物、 其中 R¹、R² 和 R³ 各自独立地表示氢原子、具有 1 至 3 个碳原子的低级烷基、具有 1 至 3 个碳原子的低级烷氧基、氨基、硝基、羟基、磺酰胺基、三氟甲基、氰基、羧基、氨基甲酰基、乙酰基、可被取代的苯甲酰甲基、甲硫基、可被取代的苯乙炔基、可被取代的乙炔基、具有 1 至 3 个碳原子的烷酰氨基、可被取代的苯甲酰氨基、具有 1 至 3 个碳原子的烷磺酰氨基或可被取代的苯磺酰氨基；R⁴ 和 R⁵ 各自独立地表示氢原子、具有 1 至 3 个碳原子的低级烷基、氰基、羧基、羟甲基、可被取代的苯基或苄基；R⁶ 表示氢原子、具有 1 至 3 个碳原子的低级烷基或苄基；X 表示亚甲基、氧原子、硫原子、亚磺酰基或磺酰基；它们的酸盐或碱盐可用作抗类风湿剂。
• IRIKURA, TSUTOMU;TAKANI, XIROKADZU;FUDZIMORI, KIEESI;XIRATA, JOSIXIRO;XIR+
  作者：IRIKURA, TSUTOMU、TAKANI, XIROKADZU、FUDZIMORI, KIEESI、XIRATA, JOSIXIRO、XIR+

  DOI：——

  日期：——