5-morpholin-2-ylmethyl-10,11-dihydro-5H-dibenzo[b,f]azepine | 61282-26-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯氮卓类
• 英文名称: 5-morpholin-2-ylmethyl-10,11-dihydro-5H-dibenzo[b,f]azepine
• 英文别名: 5-(2-morpholinylmethyl)-10,11-dihydro-5H-dibenzo[b,f]azepine；5-(2-morpholinylmethyl)-10,11-dihydro-5H-dibenz[b,f]azepine；2-(5,6-dihydrobenzo[b][1]benzazepin-11-ylmethyl)morpholine
• CAS: 61282-26-6
• 化学式: C₁₉H₂₂N₂O
• 分子量: 294.396
• InChiKey: WKULXSQWEYBIOG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.2
• 重原子数：
  22
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.37
• 拓扑面积：
  24.5
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  5-morpholin-2-ylmethyl-10,11-dihydro-5H-dibenzo[b,f]azepine 生成 2-(5,6-dihydrobenzo[b][1]benzazepin-11-ylmethyl)morpholine;oxalic acid
  参考文献：
  名称：

  TAKASIMA, JOSINORI;MARUYAMA, ISAMU;KATSUBEH, SUMIMOTO

  摘要：

  DOI：

文献信息

• Heterocyclic compounds
  申请人：Novo Nordisk A/S

  公开号：US06214816B1

  公开（公告）日：2001-04-10

  The compounds are N-substituted azaheterocyclic compounds of formula I wherein R1 and R2 independently are hydrogen, halogen, trifluoromethyl, hydroxy, C1-6-alkyl or C1-6-alkoxy; and Y is >N—CH2— wherein only the underscored atom participates in the ring system; and X is —C(R6R7)—, —CH2CH2—, —CH═CH—CH2—, —CH2—CH═CH—, —CH2—(C═O)—, —(C═O)—CH2—, —CH2CH2CH2—, —CH═CH—, CH(R10)CH2—, —CH2CH(R10) or —(C═O)— wherein R6 and R7 independently are hydrogen or C1-6-alkyl and wherein R10 is C1-6-alkyl or phenyl; and r is 0, 1 or 2; and Z is selected from wherein A is —CH2—, —O—, —S— or —N(R5)— wherein R5 is H or C1-6-alkyl; and R3 is —(CH2)pCOR4 wherein p is 1, 2, 3 or 4 and R4 is OH, NH2, NHOH or C1-6-alkoxy; or a pharmaceutically acceptable salt thereof. These compounds are useful for treating painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation. They are also useful for treating indications caused by or related to the secretion and circulation of insulin antagonizing peptides, e.g., non-insulin-dependent diabetes mellitus (NIDDM) and ageing-associated obesity.

  这些化合物是公式I的N-取代氮杂环化合物，其中R1和R2独立地是氢、卤素、三氟甲基、羟基、C1-6烷基或C1-6烷氧基；Y是>N—CH2—，其中只有下划线的原子参与环系统；而X是—C(R6R7)—、—CH2CH2—、—CH═CH—CH2—、—CH2—CH═CH—、—CH2—(C═O)—、—(C═O)—CH2—、—CH2CH2CH2—、—CH═CH—、CH(R10)CH2—、—CH2CH(R10)或—(C═O)—，其中R6和R7独立地是氢或C1-6烷基，而R10是C1-6烷基或苯基；r是0、1或2；而Z是选择自其中A是—CH2—、—O—、—S—或—N(R5)—，其中R5是H或C1-6烷基；而R3是—(CH2)pCOR4，其中p是1、2、3或4，而R4是OH、NH2、NHOH或C1-6烷氧基；或其药学上可接受的盐。这些化合物可用于治疗C纤维通过引发神经源性疼痛或炎症在其中发挥病理生理作用的疼痛、过敏和/或炎症疾病。它们还可用于治疗由胰岛素拮抗肽的分泌和循环引起或相关的症状，例如非胰岛素依赖性糖尿病（NIDDM）和与衰老相关的肥胖症。
• 2-Morpholinyl tricyclic dibenzazepine compounds
  申请人：Sumitomo Chemical Company, Limited

  公开号：US04017621A1

  公开（公告）日：1977-04-12

  Novel tricyclic compounds of the formula: ##STR1## wherein A is --CH.sub.2 --CH.sub.2 --, --CH=CH-- or ##STR2## X is hydrogen, halogen, nitro, trifluoromethyl, C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy, R.sub.1 and R.sub.2 are each hydrogen or C.sub.1 -C.sub.4 alkyl and R.sub.3 is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.5 alkenyl, C.sub.3 -C.sub.5 alkynyl, C.sub.3 -C.sub.6 cycloalkyl (C.sub.1 -C.sub.3)alkyl, ar(C.sub.1 -C.sub.3)alkyl, polyhalo(C.sub.1 -C.sub.2)alkyl, C.sub.1 -C.sub.4 alkoxy(C.sub.1 -C.sub.3)alkyl or hydroxy(C.sub.1 -C.sub.3)alkyl, and non-toxic salts thereof which are useful as antidepressants and can be prepared by reduction of a compound of the formula: ##STR3## wherein A, X, R.sub.1, R.sub.2 and R.sub.3 are each as defined above.

  式子如下：##STR1##其中，A为--CH.sub.2 --CH.sub.2 --，--CH=CH--或##STR2## X为氢、卤素、硝基、三氟甲基、C.sub.1-C.sub.3烷基或C.sub.1-C.sub.3烷氧基，R.sub.1和R.sub.2分别为氢或C.sub.1-C.sub.4烷基，R.sub.3为氢、C.sub.1-C.sub.4烷基、C.sub.3-C.sub.5烯基、C.sub.3-C.sub.5炔基、C.sub.3-C.sub.6环烷基（C.sub.1-C.sub.3）烷基、ar(C.sub.1-C.sub.3)烷基、多卤（C.sub.1-C.sub.2）烷基、C.sub.1-C.sub.4烷氧基（C.sub.1-C.sub.3）烷基或羟基（C.sub.1-C.sub.3）烷基。这些化合物的非毒性盐可作为抗抑郁剂，可通过还原式子：##STR3##其中A、X、R.sub.1、R.sub.2和R.sub.3均如上所述。
• TAKASIMA, JOSINORI;MARUYAMA, ISAMU;KATSUBEH, SUMIMOTO
  作者：TAKASIMA, JOSINORI、MARUYAMA, ISAMU、KATSUBEH, SUMIMOTO

  DOI：——

  日期：——
• NOVEL HETEROCYCLIC COMPOUNDS
  申请人：NOVO NORDISK A/S

  公开号：EP1071679A1

  公开（公告）日：2001-01-31
• US4017621A
  申请人：——

  公开号：US4017621A

  公开（公告）日：1977-04-12