2'-Hydroxy-2,5-dimethyl-6,7-benzomorphan | 20649-16-5

• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 6,7-苯并吗啡烷
• 英文名称: 2'-Hydroxy-2,5-dimethyl-6,7-benzomorphan
• 英文别名: 3,6-Dimethyl-1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocin-8-ol；1,10-dimethyl-10-azatricyclo[7.3.1.02,7]trideca-2(7),3,5-trien-4-ol
• CAS: 20649-16-5
• 化学式: C₁₄H₁₉NO
• 分子量: 217.311
• InChiKey: SGPDQCOZBVOUMT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  16
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.57
• 拓扑面积：
  23.5
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  alkaline earth salt of/the/ methylsulfuric acid 在 甲醇 、 Pd-BaSO₄ 作用下， 生成 2'-Hydroxy-2,5-dimethyl-6,7-benzomorphan
  参考文献：
  名称：

  Structures Related to Morphine. IX.^*1 Extension of the Grewe Morphinan Synthesis in the Benzomorphan Series and Pharmacology of Some Benzomorphans

  摘要：

  DOI：

  10.1021/jo01362a018

文献信息

• Aryl-and Heteroarylcarbonyl derivatives of benzomorphanes and related scaffolds, medicaments containing such compounds and their use
  申请人：Himmelsbach Frank

  公开号：US20110190262A1

  公开（公告）日：2011-08-04

  The present invention relates to compounds defined by formula I wherein the groups R 1 to R 3 , X, m, n and o are defined as in claim 1 , possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11β-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity and dyslipidemia.

  本发明涉及公式I所定义的化合物，其中R1至R3、X、m、n和o的定义如权利要求书中所述，具有有价值的药理活性。特别地，这些化合物是11β-羟基类固醇脱氢酶（HSD）1的抑制剂，因此适用于治疗和预防可以通过抑制该酶而受影响的疾病，如代谢性疾病，特别是2型糖尿病、肥胖症和血脂异常。
• Urea derivatives of benzomorphanes and related scaffolds, medicaments containing such compounds and their use
  申请人：Eckhardt Matthias

  公开号：US20110028445A1

  公开（公告）日：2011-02-03

  The present invention relates to compounds defined by formula (I) wherein the groups A, B, X, m, n and o are defined as in claim 1 , possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11 β-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity and dyslipidemia.

  本发明涉及由式(I)定义的化合物，其中A，B，X，m，n和o的基团如权利要求1中所定义，具有有价值的药理活性。特别地，这些化合物是11β-羟基类固醇脱氢酶（HSD）1的抑制剂，因此适用于治疗和预防可以通过抑制该酶而受到影响的疾病，如代谢性疾病，特别是2型糖尿病，肥胖症和血脂异常。
• BENZOMORPHAN ANALOGS AND THE USE THEREOF
  申请人：Purdue Pharma L.P.

  公开号：EP3333156A2

  公开（公告）日：2018-06-13

  The present invention is directed to Benzomorphan Analog compounds of the Formula I", Formula IA", Formula IB", Formula IC", or Formula ID" as shown below; and related Formula I', Formula IA', Formula IB', Formula IC', or Formula ID'; Formula I, Formula IA, Formula IB, Formula IC, or Formula ID;wherein R1, R2a, R2b, R3 and R4 are as defined herein Compounds of the Invention are useful for treating pain, constipation, and other conditions modulated by activity of opioid and ORL-1 receptors.

  本发明涉及如下所示的式I"、式IA"、式IB"、式IC "或式ID "的苯并吗啡类似物化合物；以及相关的式I'、式IA'、式IB'、式IC'或式ID'；式I、式IA、式IB、式IC或式ID；其中R1、R2a、R2b、R3和R4如本文所定义。 本发明的化合物可用于治疗疼痛、便秘和其他受阿片和 ORL-1 受体活性调节的疾病。
• TUBERY, FRANCOISE;GRIERSON, DAVID S.;HUSSON, HENRI-PHILIPPE, TETRAHEDRON LETT., 28,(1987) N 51, 6457-6460
  作者：TUBERY, FRANCOISE、GRIERSON, DAVID S.、HUSSON, HENRI-PHILIPPE

  DOI：——

  日期：——
• ARYL- AND HETEROARYLCARBONYL DERIVATIVES OF BENZOMORPHANES AND RELATED SCAFFOLDS, MEDICAMENTS CONTAINING SUCH COMPOUNDS AND THEIR USE
  申请人：Boehringer Ingelheim International GmbH

  公开号：EP2220048A2

  公开（公告）日：2010-08-25