4-[4-(1-Methoxy-naphtalen-2-yl)-piperidin-1-yl]-butylamine | 443130-98-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: 4-[4-(1-Methoxy-naphtalen-2-yl)-piperidin-1-yl]-butylamine
• 英文别名: 4-[4-(1-Methoxynaphthalen-2-yl)piperidin-1-yl]butan-1-amine
• CAS: 443130-98-1
• 化学式: C₂₀H₂₈N₂O
• 分子量: 312.455
• InChiKey: GLYLWTGLAYVGAD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  23
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  38.5
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  2-{4-[4-(1-methoxy-naphtalen-2-yl)-piperidin-1-yl]-butyl}-isoindole-1,3-dione 在 肼 作用下， 以 甲醇 为溶剂， 反应 16.0h， 以97%的产率得到4-[4-(1-Methoxy-naphtalen-2-yl)-piperidin-1-yl]-butylamine
  参考文献：
  名称：

  Pharmaceutical compositions

  摘要：

  该发明涉及一种筛选治疗剂的方法，该治疗剂被定义为SCAP拮抗剂，用于对抗与升高脂质水平相关的疾病，所述方法包括检测或测定在存在和不存在所述剂的情况下，控制SCAP拮抗剂与SCAP之间的转录活性或结合程度或结果。还声明了这种方法鉴定的SCAP拮抗剂治疗剂以及它们在对抗与升高脂质水平相关的疾病中的使用。

  公开号：

  US20030224347A1

文献信息

• Methods of screening for SCAP antagonists
  申请人：——

  公开号：US20030224348A1

  公开（公告）日：2003-12-04

  The invention relates to a method for screening therapeutic agents, defined as SCAP antagonists, for use in combating diseases associated with elevated lipid levels, said method comprising detecting or assaying the extent or result of transcriptional activity or binding between a control SCAP antagonist and SCAP, in the presence of and absence of said agent. Also claimed are therapeuic agents which are antagonists of SCAP, identified by such a method and their use in combating diseases associated with elevated lipid levels.

  本发明涉及一种筛选治疗剂的方法，定义为SCAP拮抗剂，用于对抗与升高脂质水平相关的疾病，该方法包括在存在和不存在该剂的情况下检测或测定控制SCAP拮抗剂和SCAP之间的转录活性或结合程度或结果。还声明了通过这种方法鉴定的SCAP拮抗剂治疗剂，并用于对抗与升高脂质水平相关的疾病。
• Aryl piperidine derivatives as inducers of ldl-receptor expression
  申请人：——

  公开号：US20040147557A1

  公开（公告）日：2004-07-29

  The invention relates to a compound of formula (I), wherein Ar 1 represents phenyl, naphthyl or phenyl fused by a C 3-8 cycloalkyl, where each group is optionally substituted by methylenedioxy or one or two groups independently represented by R 1 ; Ar 2 represents phenyl or a 5-6 membered heteroaromatic group, where each group is optionally substituted by one to four groups independently selected from halogen, C 1-4 alkyl and C 1-4 alkoxy; Ar 3 represents a phenyl or a 5-6 membered heteroaromatic group, where each group is optionally substituted by one to four groups independently selected from hydroxy, alkyl, C 1-4 alkoxy, C 2-4 alkenyl, C 2-4 alkenyloxy, C 1-4 perfluoroalkoxy, C 1-4 acylamino or an electron withdrawing group; A represents —C(H)—; E represents —C 1-6 alkylene-; X represents —CON(H or C 1-4 alkyl)- or —N(H or C 1-4 alkyl)CO—; Y represents a direct link; R 1 represents halogen, —S(C 1-4 alkyl)-, —O—(C 0-4 alkylene)-R 2 or —(C 0-4 alkylene)-R 2 , where each alkylene group may additionally incorporate an oxygen in the chain, with the proviso that there are at least two carbon atoms between any chain heteroatoms; R 2 represents: i) hydrogen, C 1-4 perfluoroalkyl, C 2-3 alkenyl, ii) phenyl, naphthyl, a 5- or 6-membered heteroaromatic group or 1,2,3,4-tetrahydronaphthyl, optionally substituted by one or two halogen, hydroxy, C 1-4 alkyl, C 1-4 alkoxy groups, iii) C 3-8 cycloalkyl, a 3-7 membered heterocycloalkyl, iv) amino, C 1-4 alkylamino or di-C 1-4 alkylamino, with the proviso that there are at least two carbon atoms between any chain heteroatoms; to salts, solvates and compositions thereof and their use in treating disorders associated with elevated levels of circulating LDL-cholesterol. 1

  本发明涉及一种式（I）的化合物，其中Ar1代表苯基，萘基或由C3-8环烷基融合的苯基，其中每个基团可以被甲亚氧基或由R1独立表示的一或两个基团取代；Ar2代表苯基或5-6成员杂芳基，其中每个基团可以被从卤素、C1-4烷基和C1-4烷氧基中独立选择的1到4个基团取代；Ar3代表苯基或5-6成员杂芳基，其中每个基团可以被从羟基、烷基、C1-4烷氧基、C2-4烯基、C2-4烯氧基、C1-4全氟烷氧基、C1-4酰胺基或电子吸引基中独立选择的1到4个基团取代；A代表-C（H）-；E代表-C1-6烷基-；X代表—CON（H或C1-4烷基）-或—N（H或C1-4烷基）CO-；Y代表直接连接；R1代表卤素、—S（C1-4烷基）-、—O—（C0-4烷基）-R2或—（C0-4烷基）-R2，其中每个烷基组可能在链中还包含一个氧原子，但必须保证链中任何异原子之间至少有两个碳原子；R2代表：i）氢、C1-4全氟烷基、C2-3烯基，ii）苯基、萘基、5-或6-成员杂芳基或1,2,3,4-四氢萘基，可以选择地被1或2个卤素、羟基、C1-4烷基、C1-4烷氧基取代，iii）C3-8环烷基、3-7成员杂环烷基，iv）氨基、C1-4烷基氨基或二-C1-4烷基氨基，但必须保证链中任何异原子之间至少有两个碳原子；以及其盐、溶剂化合物和组合物及其用于治疗与循环低密度脂蛋白胆固醇水平升高相关的疾病的用途。
• ARYL PIPERIDINE DERIVATIVES AS INDUCERS OF LDL-RECEPTOR EXPRESSION
  申请人：GLAXO GROUP LIMITED

  公开号：EP1351937A1

  公开（公告）日：2003-10-15
• US6673555B1
  申请人：——

  公开号：US6673555B1

  公开（公告）日：2004-01-06
• [EN] ARYL PIPERIDINE DERIVATIVES AS INDUCERS OF LDL-RECEPTOR EXPRESSION<br/>[FR] DERIVES D'ARYLEPIPERIDINE UTILISES COMME INDUCTEURS D'EXPRESSION DE LDL
  申请人：GLAXO GROUP LTD

  公开号：WO2002055497A1

  公开（公告）日：2002-07-18

  The invention relates to a compound of formula (I), wherein Ar1 represents phenyl, naphthyl or phenyl fused by a C3-8cycloalkyl, where each group is optionally substituted by methylenedioxy or one or two groups independently represented by R1; Ar2 represents phenyl or a 5-6 membered heteroaromatic group, where each group is optionally substituted by one to four groups independently selected from halogen, C1-4 alkyl and C1-4 alkoxy; Ar3 represents a phenyl or a 5-6 membered heteroaromatic group, where each group is optionally substituted by one to four groups independently selected from hydroxy, alkyl, C1-4 alkoxy, C2-4 alkenyl, C2-4 alkenyloxy, C1-4 perfluoroalkoxy, C1-4 acylamino or an electron withdrawing group; A represents -C(H)-; E represents -C1-6 alkylene-; X represents -CON(H or C1-4alkyl)- or -N(H or C1-4alkyl)CO-; Y represents a direct link; R1 represents halogen, -S(C¿1-4? alkyl)-, -O-(C0-4 alkylene)-R?2¿ or -(C¿0-4?alkylene)-R?2¿, where each alkylene group may additionally incorporate an oxygen in the chain, with the proviso that there are at least two carbon atoms between any chain heteroatoms; R2 represents: i) hydrogen, C¿1-4? perfluoroalkyl, C2-3 alkenyl, ii) phenyl, naphthyl, a 5- or 6-membered heteroaromatic group or 1,2,3,4-tetrahydronaphthyl, optionally substituted by one or two halogen, hydroxy, C1-4 alkyl, C1-4 alkoxy groups, iii) C3-8cycloalkyl, a 3-7 membered heterocycloalkyl, iv) amino, C1-4 alkylamino or di-C1-4alkylamino, with the proviso that there are at least two carbon atoms between any chain heteroatoms; to salts, solvates and compositions thereof and their use in treating disorders associated with elevated levels of circulating LDL-cholesterol.