(4-aminoadamantan-1-yl)methanol | 865980-55-8

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: (4-aminoadamantan-1-yl)methanol
• 英文别名: Z-(4-amino-adamantan-1-yl)-methanol；4-amino-1-hydroxymethyladamantane；(4-amino-1-adamantyl)methanol
• CAS: 865980-55-8
• 化学式: C₁₁H₁₉NO
• mdl: MFCD18800649
• 分子量: 181.278
• InChiKey: QFKQPWVSSXAIRC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  46.2
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  3-(2-pyridin-2-ylethoxy)benzoic acid 、 (4-aminoadamantan-1-yl)methanol 生成 N-(5-Hydroxymethyl-adamantan-2-yl)-3-(2-pyridin-2-yl-ethoxy)-benzamide
  参考文献：
  名称：

  N-adamantyl benzamides as inhibitors of 11-β-hydroxysteroid dehydrogenase

  摘要：

  本发明涉及一种新型的取代酰胺抑制剂，其在治疗中的使用、包含该化合物的制药组合物、利用该化合物制备药物以及包括该化合物的治疗方法。本发明中的化合物调节11β-羟基类固醇脱氢酶1型（11βHSD1）的活性，因此在调节有益的情况下，如代谢综合征等疾病的治疗中具有应用价值。

  公开号：

  US08334305B2
• 作为产物：
  描述：

  4-氨基金刚烷-1-羧酸甲酯 在 lithium aluminium tetrahydride 作用下， 以 四氢呋喃 为溶剂， 反应 3.0h， 以90%的产率得到(4-aminoadamantan-1-yl)methanol
  参考文献：
  名称：

  WO2008/101907

  摘要：

  公开号：

文献信息

• Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV)
  申请人：Madar J. David

  公开号：US20050215784A1

  公开（公告）日：2005-09-29

  The present invention relates to compounds that inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, Syndrome X, hyperinsulinemia, obesity, atherosclerosis, and various immunomodulatory diseases.

  本发明涉及抑制二肽基肽酶IV（DPP-IV）的化合物，用于预防或治疗糖尿病，特别是II型糖尿病，以及高血糖、X综合征、高胰岛素血症、肥胖、动脉粥样硬化和各种免疫调节性疾病。
• [EN] 2, 4 -DIAMINOPYRIMIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS<br/>[FR] DÉRIVÉS DE 2,4-DIAMINOPYRIMIDINE EN TANT QU'INHIBITEURS DE PROTÉINE KINASES
  申请人：AURIGENE DISCOVERY TECH LTD

  公开号：WO2012059932A1

  公开（公告）日：2012-05-10

  The present invention relates to novel pyrimide derivatives of formula (I): that are useful as kinase inhibitors. More particularly, the present invention relates to novel pyrimidine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders.

  本发明涉及一种新型的式（I）的嘧啶衍生物，其作为激酶抑制剂具有用途。更具体地，本发明涉及新型嘧啶化合物、其制备方法、含有这些化合物的药物组合物以及这些化合物在治疗增殖性疾病中的用途。
• [EN] MULTICYCLIC COMPOUNDS AND USE OF SAME FOR TREATING TUBERCULOSIS<br/>[FR] COMPOSÉS MULTICYCLIQUES ET LEUR UTILISATION POUR LE TRAITEMENT DE LA TUBERCULOSE
  申请人：HARVARD COLLEGE

  公开号：WO2019140254A1

  公开（公告）日：2019-07-18

  Provided herein are multicyclic compounds useful for treating tuberculosis. Also provided are methods of treating tuberculosis using the compounds of the invention.

  本文提供了用于治疗结核病的多环化合物。还提供了使用本发明化合物治疗结核病的方法。
• TETRAHYDROQUINOXALINE UREA DERIVATIVES, PREPARATION THEREOF, AND THERAPEUTIC USE THEREOF
  申请人：Crespin Olivier

  公开号：US20120165337A1

  公开（公告）日：2012-06-28

  The invention relates to compounds of formula (I), where: A is a bond, an oxygen atom, or an -CH 2 — group; Ar 1 is a phenyl or heteroaryl group; Ar 2 is a phenyl, heteroaryl, or heterocycloalkyl group; R 1a,b,c and R2a,b,c are a hydrogen or halogen atom, or an alkyl, cycloalkyl, or lkyl-cycloalkyl group optionally substituted by one or more halogen atoms, or an —OR 5 (hydroxy or alkoxy), hydroxy-alkyl, alkoxy-alkyl, alkoxy-alkoxy, halogenoalkyl, —O-halogenoalkyl, oxo, —CO-alkyl, —CO-alkyl-NR 6 R 7 , —CO-halogenoalkyl, —COOR 5 , alkyl-COOR 5 , —O-alkyl-COOR 5 , —SO 2 -alkyl, —SO 2 -cycloalkyl, —SO 2 -alkyl-cycloalkyl, —SO 2 -alkyl-OR 5 , —SO 2 -alkyl-COOR 5 , —SO 2 -alkyl-NR 6 R 7 , —SO 2 -halogenoalkyl, alkyl-SO 2 -alkyl, —SO 2 —NR 6 R 7 , —SO 2 -alkyl-O-alkyl-OR 5 , —CONR 6 R 7 , -alkyl-CONR 6 R 7 , or -alkyl-NR 6 R 7 group, or further R 1a , R 1b , and R 1c are bonded to R 2a , R 2b , R 2c , respectively, as well as to the carbon atom having same, and are -alkyl-O—; R 3 is a hydrogen atom or an alkyl group; R 4 is a ONR 6 R 7 group, a hydroxyalkyl group substituted by a halogenoalkyl group, or an lkyl-NH—SO 2 -alkyl, NH—SO 2 -alkyl, —O—SO 2 —NR 6 R 7 , -alkyl-CO—NR 6 R 7 , —O-alkyl-CO—NR 6 R 7 , -alkyl-NR 6 R 7 , —O—CO—NR 6 R 7 , -alkyl-heteroaryl, a heteroaryl group optionally substituted by an alkyl, alkoxy-imino, or —NH—NH—CO-alkyl group, with the proviso that R 4 is in the cis position when it is the ONR 6 R 7 group and that R 6 and R 7 are each hydrogen, or an lkyl or lkyl-phenyl group; R 5 is hydrogen, an lkyl group, or lkyl-phenyl; R 6 and R 7 , identical or different, are each a hydrogen atom, an alkyl group, alkoxy, or an alkyl-phenyl group; and R 8 is a hydrogen atom or an O 2 -alkyl group, or a group of formula -Het, where B can be absent or be a bond, an oxygen atom, or a O— or O 2 —(CH 2 ) n group, with n being equal to 0, 1, or 2, and where Het is a heteroaryl or heterocycloaryl optionally substituted by the alkyl, —SO 2 -alkyl, and —COOR 5 groups. The invention also relates to a method for preparing same to the therapeutic use thereof.

  该发明涉及式(I)的化合物，其中：A是键合，氧原子，或-CH2-基团；Ar1是苯基或杂环芳基；Ar2是苯基，杂环芳基，或杂环烷基基团；R1a，b，c和R2a，b，c是氢原子或卤素原子，或烷基，环烷基，或烷基-环烷基基团，可选择地被一个或多个卤素原子取代，或-OR5（羟基或烷氧基），羟基-烷基，烷氧基-烷基，烷氧基-烷氧基，卤代烷基，-O-卤代烷基，酮基，-CO-烷基，-CO-烷基-NR6R7，-CO-卤代烷基，-COOR5，烷基-COOR5，-O-烷基-COOR5，-SO2-烷基，-SO2-环烷基，-SO2-烷基-环烷基，-SO2-烷基-OR5，-SO2-烷基-COOR5，-SO2-烷基-NR6R7，-SO2-卤代烷基，烷基-SO2-烷基，-SO2-NR6R7，-SO2-烷基-O-烷基-OR5，-CONR6R7，-烷基-CONR6R7，或-烷基-NR6R7基团，或进一步R1a，R1b和R1c与R2a，R2b，R2c分别键合到相同的碳原子，并且是-烷基-O-；R3是氢原子或烷基基团；R4是ONR6R7基团，一个被卤代烷基取代的羟基烷基基团，或烷基-NH-SO2-烷基，NH-SO2-烷基，-O-SO2-NR6R7，-烷基-CO-NR6R7，-O-烷基-CO-NR6R7，-烷基-NR6R7，-O-CO-NR6R7，-烷基-杂环芳基，一个可选择地被烷基，烷氧基亚胺，或-NH-NH-CO-烷基基团取代的杂环芳基，但R4在ONR6R7基团时处于顺式位置，并且R6和R7各自是氢，或烷基或烷基-苯基；R5是氢，烷基基团，或烷基-苯基；R6和R7，相同或不同，各自是氢原子，烷基基团，烷氧基，或烷基-苯基；R8是氢原子或O2-烷基基团，或式-Het的基团，其中B可以不存在或是键合，氧原子，或O-或O2-(CH2)n基团，其中n等于0，1或2，而Het是一个可选择地被烷基，-SO2-烷基，和-COOR5基团取代的杂环芳基或杂环烷基。该发明还涉及制备这些化合物的方法以及它们的治疗用途。
• Pharmaceutical Compositions as Inhibitors of Dipeptidyl Peptidase-IV (DPP-IV)
  申请人：Madar J. David

  公开号：US20070238753A1

  公开（公告）日：2007-10-11

  The present invention relates to compounds that inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, Syndrome X, hyperinsulinemia, obesity, atherosclerosis, and various immunomodulatory diseases.

  本发明涉及抑制二肽基肽酶IV（DPP-IV）的化合物，适用于预防或治疗糖尿病，特别是2型糖尿病，以及高血糖、X综合症、高胰岛素血症、肥胖症、动脉硬化和各种免疫调节性疾病。