N-2-adamantyl-1-phenylcyclopropanecarboxamide

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: N-2-adamantyl-1-phenylcyclopropanecarboxamide
• 英文别名: N-(2-adamantyl)-1-phenylcyclopropane-1-carboxamide
• 化学式: C₂₀H₂₅NO
• 分子量: 295.425
• InChiKey: UOAATJFGYDPHIK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.9
• 重原子数：
  22
• 可旋转键数：
  3
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.65
• 拓扑面积：
  29.1
• 氢给体数：
  1
• 氢受体数：
  1

文献信息

• Inhibitors of the 11-beta-hydroxysteroid dehydrogenase type 1 enzyme
  申请人：Rohde J. Jeffrey

  公开号：US20060149070A1

  公开（公告）日：2006-07-06

  The present invention relates to compounds that are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.

  本发明涉及抑制11-β-羟基类固醇脱氢酶1型酶的化合物。本发明进一步涉及利用11-β-羟基类固醇脱氢酶1型酶的抑制剂治疗非胰岛素依赖型2型糖尿病、胰岛素抵抗、肥胖、脂质紊乱、代谢综合征以及其他由过度糖皮质激素作用介导的疾病和症状。
• Metabolic stabilization of substituted adamantane
  申请人：Rohde J. Jeffrey

  公开号：US20060148871A1

  公开（公告）日：2006-07-06

  The present invention is directed to the method of increasing the metabolic stability of adamantane containing compounds that are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 (11-beta-HSD-1) enzyme. The stability is achieved by substitutions of the adamantane ring.

  本发明涉及一种增加含有金刚烷基化合物代谢稳定性的方法，这些化合物是11-β-羟基类固醇脱氢酶1（11-β-HSD-1）酶的抑制剂。通过对金刚烷环进行取代实现稳定性。
• Adamantyl acetamides as 11-beta hydroxysteroid dehydrogenase inhibitors
  申请人：Linders Theodorus Maria Joannes

  公开号：US20060079506A1

  公开（公告）日：2006-04-13

  the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n represents an integer being 1 or 2; R 1 and R 2 each independently represents hydrogen C 1-4 alkyl, NR 9 R 10 , C 1-4 alkyloxy; or R 1 and R 2 taken together with the carbon atom with which they are attached form a C 3-6 cycloalkyl; and where n is 2, either R 1 or R 2 may be absent to form an unsaturated bond; R 3 represents a C 6-12 cycloalkyl, preferably selected from cylo-octanyl and cyclohexyl or R 3 represents a monovalent radical having one of the following formulae wherein said C 6-12 cycloalkyl or monovalent radical may optionally be substituted with one, or where possible two, three or more substituents selected from the group consisting of C 1-4 alkyl, C 1-4 alkyloxy, halo or hydroxy; Q represents Het 1 or Ar 2 wherein said C 3-8 cycloalkyl, Het 1 or Ar 2 are optionally substituted with one or where possible two or more substituents selected from halo, C 1-4 alkyl, C 1-4 alkyloxy, hydroxy, nitro, NR 5 R 6 , C 1-4 alkyloxy substituted with one or where possible two, three or more substituents each independently selected from hydroxycarbonyl, Het 2 and NR 7 R 8 , and C 1-4 alkyl substituted with one or where possible two or three halo substituents, preferably trifluoromethyl; R 5 and R 6 each independently represent hydrogen, C 1-4 alkyl, or C 1-4 alkyl substituted with phenyl; R 7 and R 8 each independently represent hydrogen or C 1-4 alkyl; R 9 and R 10 each independently represent hydrogen, C 1-4 alkyl or C 1-4 alkyloxycarbonyl; L represents C 1-4 alkyl; Het 1 represents a heterocycle selected from pyridinyl, thiophenyl, or 1,3-benzodioxolyl; Het 2 represents piperidinyl, pyrrolidinyl or morpholinyl; Ar 2 represents phenyl, naphtyl or indenyl.

  N-氧化物形式，其药学上可接受的加合盐以及立体化学异构体形式，其中n表示1或2的整数；R1和R2各自独立地表示氢C1-4烷基，NR9R10，C1-4烷氧基; 或者R1和R2与它们附着的碳原子一起形成C3-6环烷基; 当n为2时，R1或R2中的任一可以不存在以形成不饱和键; R3表示C6-12环烷基，优选从环辛基和环己基中选择，或者R3表示具有以下式子之一的单价基团，其中所述的C6-12环烷基或单价基团可以选择地被一个、或可能两个、三个或更多来自C1-4烷基，C1-4烷氧基，卤素或羟基的取代基所取代; Q表示Het1或Ar2，其中所述的C3-8环烷基，Het1或Ar2可以选择地被一个或可能两个或更多来自卤素，C1-4烷基，C1-4烷氧基，羟基，硝基，NR5R6，C1-4烷氧基取代，其中每个独立地选择自羟基羰基，Het2和NR7R8，以及C1-4烷基取代，其中每个独立地选择自三氟甲基等卤素取代基; R5和R6各自独立地表示氢，C1-4烷基，或C1-4烷基取代苯基; R7和R8各自独立地表示氢或C1-4烷基; R9和R10各自独立地表示氢，C1-4烷基或C1-4烷氧羰基; L表示C1-4烷基; Het1表示从吡啶基，噻吩基或1,3-苯并二氧杂环中选择的杂环; Het2表示哌啶基，吡咯烷基或吗啉基; Ar2表示苯基，萘基或茚基。
• INHIBITORS OF THE 11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 ENZYME
  申请人：Rohde J. Jeffrey

  公开号：US20070179186A1

  公开（公告）日：2007-08-02

  The present invention relates to compounds that are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme, The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.

  本发明涉及抑制11-β-羟基类固醇脱氢酶1型酶的化合物。本发明还涉及使用11-β-羟基类固醇脱氢酶1型酶抑制剂治疗非胰岛素依赖性2型糖尿病、胰岛素抵抗、肥胖症、脂质代谢紊乱、代谢综合症和其他由过度糖皮质激素作用介导的疾病和病症。
• Inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme
  申请人：Bitner R. Scott

  公开号：US20120289512A1

  公开（公告）日：2012-11-15

  The present invention relates to inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme and their use in treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, central nervous system disorders, and diseases and conditions that are related to excessive glucocorticoids.

  本发明涉及11-β-羟基类固醇脱氢酶1型酶的抑制剂及其在治疗非胰岛素依赖性2型糖尿病、胰岛素抵抗、肥胖症、脂质代谢紊乱、代谢综合征、中枢神经系统疾病以及与过度糖皮质激素相关的疾病和病症中的应用。