5H-dibenzo[b,e][1,4]diazepine | 256-98-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯二氮卓类
• 英文名称: 5H-dibenzo[b,e][1,4]diazepine
• 英文别名: 5H-dibenzo[b,e][1,4]diazepine；5H-Dibenzo<1,4>diazepin；Dibenzo[b,e][1,4]diazepine；11H-benzo[b][1,4]benzodiazepine
• CAS: 256-98-4
• 化学式: C₁₃H₁₀N₂
• 分子量: 194.236
• InChiKey: BLOPFAKSIQBSIG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  15
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  24.4
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  2-(2'-aminophenylamino)benzyl alcohol 在 manganese(IV) oxide 作用下， 以 乙醚 为溶剂， 反应 5.0h， 生成 5H-dibenzo[b,e][1,4]diazepine
  参考文献：
  名称：

  Black, David St. C.; Rothnie, Neil E., Australian Journal of Chemistry, 1983, vol. 36, # 6, p. 1149 - 1157

  摘要：

  DOI：

文献信息

• [EN] HDAC INHIBITORS AND USES THEREOF<br/>[FR] INHIBITEURS DE LA HDAC ET SES UTILISATIONS
  申请人：ENVIVO PHARMACEUTICALS INC

  公开号：WO2009137503A1

  公开（公告）日：2009-11-12

  Inhibitors of histone deacetylase, including compounds having a diazabicyclo[2.2.1]heptan-2-yl moiety are described together with methods for treating various disorders with such compounds.

  抑制组蛋白去乙酰化酶的抑制剂，包括具有二氮杂双环[2.2.1]庚烷-2-基基团的化合物，以及使用这些化合物治疗各种疾病的方法被描述。
• [EN] PIPERAZINE SUBSTITUTED ARYL BENZODIAZEPINES<br/>[FR] ARYL BENZODIAZEPINES SUBSTITUEES PAR DE LA PIPERAZINE
  申请人：LILLY CO ELI

  公开号：WO2004014895A1

  公开（公告）日：2004-02-19

  Described herein are compounds of formula (I) wherein: is an optionally benzo-fused five or six member aromatic ring having zero to three hetero atoms independently selected from N, S, and O; Alk is (C1-4) alkylene or hydroxy substituted (C1-4) alkylene; X is oxygen or sulfur; R1 is hydrogen, (C1-6) fluoroalkyl, (C3-6) cycloalkyl, or (C1-4) alkyl, wherein the (C1-4) alkyl is unsubstituted or substituted with hydroxy, methoxy, ethoxy, OCH2CH2OH, or -CN; R2 is H, halogen, (C1-6) fluoroalkyl, (C1-6) cycloalkyl, OR4, SR4, N02, CN, COR4, C(O)OR4, CONR5R6 , NR5R6, S02NR5R6, NR5COR4, NR5SO2R4, optionally substituted aromatic, or (C1-6) alkyl, wherein (C1-6) alkyl is unsubstituted or substituted with a hydroxy group; R3 is hydrogen, (C1-6) fluoroalkyl, (C2-6) alkenyl, Ar, (C1-4)alkyl-Ar, or (C1-4) alkyl wherein (C1-4) alkyl is unsubsituted or substituted with a phenyl; R4 is hydrogen, (C1-6 alkyl, (C1-6) fluoroalkyl, or optionally substituted aromatic; R5 and R6 are independently hydrogen, (C1-6) alkyl, or optionally substituted aromatic, R7 is hydrogen, (C1-6) alkyl, (C1-6) fluoroalkyl, or optionally substituted aromatic; R8 and R9 are independently hydrogen, (C1-6) alkyl, or optionally substituted aromatic; Ar is optionally substituted phenyl, napthyl, monocyclic heteroaromatic or bicyclic heteroaromatic; Z1 and Z2 are independently selected from hydrogen, halogen, (C1-6) alkyl, (C1-6) fluoroalkyl, OR7, SR7, NO2, CN, COR7, CONR8R9, NR8R9, and optionally substituted aromatic; and all salts, solvates, optical and geometric isomers, and crystalline forms thereof. Also, described are the use of the compounds of formula (I) as antagonists of the dopamine D2 receptor and as agents for the treament of psychosis and bipolar disorders, and pharmaceutical formulations of the compounds of formula (I).

  本文描述了以下式(I)的化合物：其中：是一个可选的苯并嵌合的五元或六元芳香环，其中含有从N、S和O中独立选择的零至三个杂原子；Alk是(C1-4)烷基或羟基取代的(C1-4)烷基；X是氧或硫；R1是氢、(C1-6)氟烷基、(C3-6)环烷基或(C1-4)烷基，其中(C1-4)烷基未取代或取代为羟基、甲氧基、乙氧基、OCH2CH2OH或-CN；R2是H、卤素、(C1-6)氟烷基、(C1-6)环烷基、OR4、SR4、N02、CN、COR4、C(O)OR4、CONR5R6、NR5R6、S02NR5R6、NR5COR4、NR5SO2R4、可选取代的芳香基或(C1-6)烷基，其中(C1-6)烷基未取代或取代为羟基；R3是氢、(C1-6)氟烷基、(C2-6)烯基、Ar、(C1-4)烷基-Ar或(C1-4)烷基，其中(C1-4)烷基未取代或取代为苯基；R4是氢、(C1-6)烷基、(C1-6)氟烷基或可选取代的芳香基；R5和R6独立地是氢、(C1-6)烷基或可选取代的芳香基，R7是氢、(C1-6)烷基、(C1-6)氟烷基或可选取代的芳香基；R8和R9独立地是氢、(C1-6)烷基或可选取代的芳香基；Ar是可选取代的苯基、萘基、单环杂芳基或双环杂芳基；Z1和Z2独立地选自氢、卤素、(C1-6)烷基、(C1-6)氟烷基、OR7、SR7、NO2、CN、COR7、CONR8R9、NR8R9和可选取代的芳香基；以及其所有盐、溶剂化合物、光学和几何异构体以及结晶形式。此外，还描述了将上述式(I)的化合物用作多巴胺D2受体拮抗剂以及用于治疗精神病和双相情感障碍的药剂，以及上述式(I)的药物配方。
• Methods for Treating Cognitive Disorders Using Inhibitors of Histone Deacetylase
  申请人：Forum Pharmaceuticals, Inc.

  公开号：US20170000749A1

  公开（公告）日：2017-01-05

  This disclosure relates to compounds for the inhibition of histone deacetylase and treatment of a cognitive disorder or deficit. More particularly, the disclosure provides for compounds of formula (I) wherein Q, J, L and Z are as defined in the specification.

  这份披露涉及用于抑制组蛋白去乙酰化酶和治疗认知障碍或缺陷的化合物。更具体地，该披露提供了公式（I）的化合物 其中 Q、J、L和Z如规范中所定义。
• [EN] INHIBITORS OF HISTONE DEACETYLASE<br/>[FR] INHIBITEURS DE L'HISTONE DÉSACÉTYLASE
  申请人：ENVIVO PHARMACEUTICALS INC

  公开号：WO2009137499A1

  公开（公告）日：2009-11-12

  Compounds which are histone deacetylase inhibitors and their use in treating various disorders, including Alzheimer's Disease.

  组合物是组蛋白去乙酰化酶抑制剂，用于治疗各种疾病，包括阿尔茨海默病。
• [EN] INHIBITORS OF HISTONE DEACETYLASE<br/>[FR] INHIBITEURS DE L'HISTONE DÉACÉTYLASE
  申请人：METHYLGENE INC

  公开号：WO2009055917A1

  公开（公告）日：2009-05-07

  This invention relates to compounds and methods for the inhibition of HDAC enzymatic activity. More particularly, the invention provides for compounds of formula (I), (I) and N-oxides, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, and racemic and scalemic mixtures, diastereomers and enantiomers thereof, wherein L, M, n, R, W, X and Y are as defined in the specification.

  这项发明涉及化合物和用于抑制HDAC酶活性的方法。更具体地，该发明提供了符合式(I)、(I)和N-氧化物、水合物、溶剂合物、药用可接受盐、前药和其复合物、外消旋和手性混合物、非对映异构体和对映体的化合物，其中L、M、n、R、W、X和Y如规范中定义的。