N-{4-[4-(2,3-Dichlorophenyl)-1-piperazinyl]butyl}-2-anthracenecarboxamide | 197242-80-1

• 分子结构分类: 有机化合物 - 苯类化合物 - 蒽
• 英文名称: N-{4-[4-(2,3-Dichlorophenyl)-1-piperazinyl]butyl}-2-anthracenecarboxamide
• 英文别名: N-(4-(4-(2,3-Dichlorophenyl)-1-piperazinyl)butyl)-2-anthracenecarboxamide；N-[4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl]anthracene-2-carboxamide
• CAS: 197242-80-1
• 化学式: C₂₉H₂₉Cl₂N₃O
• 分子量: 506.475
• InChiKey: ZITQUAHPZJHCJH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  7
• 重原子数：
  35
• 可旋转键数：
  7
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.28
• 拓扑面积：
  35.6
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  2-蒽甲酸 、 N,N'-羰基二咪唑 、 4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butylamine 在 乙酸乙酯 、 水 、 disodium;carbonate 、 Sodium sulfate-III 作用下， 以 四氢呋喃 为溶剂， 反应 8.5h， 以to give the title compound (183 mg, 80%)的产率得到N-{4-[4-(2,3-Dichlorophenyl)-1-piperazinyl]butyl}-2-anthracenecarboxamide
  参考文献：
  名称：

  N-piperidinyl- and N-tetrahydropyridinyl-2-anthracenecarboxamides:

  摘要：

  本发明涉及以下公式的化合物：##STR1##或其药学上可接受的酸加合物盐，其中：R1、R2、R3、R4、R5、R6、R7、R8和R9相同或不同，代表氢、C1-C6烷基、卤素、羟基、氨基、氰基、硝基、三氟甲基、三氟甲氧基、C1-C6烷氧基、-O2CR'、-NHCOR'、-COR'、-SOmR'，其中R'为C1-C6烷基，m为0、1或2；或R1、R2、R3、R4、R5、R6、R7、R8和R9分别独立地代表--CONR'R"或--NR'R"，其中R'和R"独立地代表氢或C1-C6烷基；R10为氢或C1-C6烷基；R代表氨基烷基；这些化合物在治疗情感障碍，如精神分裂症、抑郁症、阿尔茨海默病、运动障碍，如帕金森病和肌张力障碍，以及其他对多巴胺能阻滞有反应的疾病，如物质滥用和强迫症方面有用。此外，本发明的化合物可能在治疗与传统神经类药物使用相关的锥体外副作用方面有用。

  公开号：

  US05883257A1

文献信息

• N-Aminoalkyl-2-anthracenecarboxamides; new dopamine receptor subtype
  申请人：Neurogen Corporation

  公开号：US05703235A1

  公开（公告）日：1997-12-30

  Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof, wherein: R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 are the same or different and represent hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, hydroxy, amino, cyano, nitro, trifluoromethyl, trifluoromethoxy, C.sub.1 -C.sub.6 alkoxy, --O.sub.2 CR', --NHCOR', --COR', --SO.sub.m R', where R' is C.sub.1 -C.sub.6 alkyl and wherein m is 0, 1 or 2; or R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 independently represent --CONR'R", or --NR'R" where R' and R" independently represent hydrogen or C.sub.1 -C.sub.6 alkyl; R.sub.10 is hydrogen or C.sub.1 -C.sub.6 alkyl; and R represents an aminoalkyl group; which compounds are useful in the treatment of affective disorders such as schizophrenia, depression, Alzheimer's disease, movement disorders such as Parkinsonism and dystonia, and other disorders which respond to dopaminergic blockade such as substance abuse and obsessive compulsive disorders. Further, compounds of this invention may be useful in treating the extrapyramidal side effects associated with the use of conventional neuroleptic agents.

  本发明涉及以下公式的化合物：##STR1##或其药学上可接受的酸加成盐，其中：R.sub.1，R.sub.2，R.sub.3，R.sub.4，R.sub.5，R.sub.6，R.sub.7，R.sub.8和R.sub.9相同或不同，分别代表氢，C.sub.1-C.sub.6烷基，卤素，羟基，氨基，氰基，硝基，三氟甲基，三氟甲氧基，C.sub.1-C.sub.6烷氧基，--O.sub.2CR'，--NHCOR'，--COR'，--SO.sub.mR'，其中R'为C.sub.1-C.sub.6烷基，而m为0、1或2；或R.sub.1，R.sub.2，R.sub.3，R.sub.4，R.sub.5，R.sub.6，R.sub.7，R.sub.8和R.sub.9分别独立地代表--CONR'R"或--NR'R"，其中R'和R"独立地代表氢或C.sub.1-C.sub.6烷基；R.sub.10代表氢或C.sub.1-C.sub.6烷基；而R代表氨基烷基。这些化合物在治疗情感障碍，如精神分裂症、抑郁症、阿尔茨海默病、运动障碍，如帕金森综合症和肌张力障碍，以及其他对多巴胺能阻断有反应的疾病，如物质滥用和强迫症方面有用。此外，本发明的化合物可能有助于治疗与传统神经类药物使用有关的锥体外系副作用。
• N-piperidinyl- and N-tetrahydropyridinyl-2-anthracenecarboxamides:
  申请人：Neurogen Corporation

  公开号：US05883257A1

  公开（公告）日：1999-03-16

  Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof, wherein: R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 are the same or different and represent hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, hydroxy, amino, cyano, nitro, trifluoromethyl, trifluoromethoxy, C.sub.1 -C.sub.6 alkoxy, --O.sub.2 CR', --NHCOR', --COR', --SO.sub.m R', where R' is C.sub.1 -C.sub.6 alkyl and wherein m is 0, 1 or 2; or R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 independently represent --CONR'R", or --NR'R" where R' and R" independently represent hydrogen or C.sub.1 -C.sub.6 alkyl; R.sub.10 is hydrogen or C.sub.1 -C.sub.6 alkyl; and R represents an aminoalkyl group; which compounds are useful in the treatment of affective disorders such as schizophrenia, depression, Alzheimer's disease, movement disorders such as Parkinsonism and dystonia, and other disorders which respond to dopaminergic blockade such as substance abuse and obsessive compulsive disorders. Further, compounds of this invention may be useful in treating the extrapyramidal side effects associated with the use of conventional neuroleptic agents.

  本发明涉及以下公式的化合物：##STR1##或其药学上可接受的酸加合物盐，其中：R1、R2、R3、R4、R5、R6、R7、R8和R9相同或不同，代表氢、C1-C6烷基、卤素、羟基、氨基、氰基、硝基、三氟甲基、三氟甲氧基、C1-C6烷氧基、-O2CR'、-NHCOR'、-COR'、-SOmR'，其中R'为C1-C6烷基，m为0、1或2；或R1、R2、R3、R4、R5、R6、R7、R8和R9分别独立地代表--CONR'R"或--NR'R"，其中R'和R"独立地代表氢或C1-C6烷基；R10为氢或C1-C6烷基；R代表氨基烷基；这些化合物在治疗情感障碍，如精神分裂症、抑郁症、阿尔茨海默病、运动障碍，如帕金森病和肌张力障碍，以及其他对多巴胺能阻滞有反应的疾病，如物质滥用和强迫症方面有用。此外，本发明的化合物可能在治疗与传统神经类药物使用相关的锥体外副作用方面有用。
• US6025493A
  申请人：——

  公开号：US6025493A

  公开（公告）日：2000-02-15
• N-piperazinylalkyl-2-anthracenecarboxamides
  申请人：Neurogen Corporation

  公开号：US06025493A1

  公开（公告）日：2000-02-15

  Disclosed arm compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof, wherein: R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 are the same or different and represent hydrogen, C.sub.1 -C.sub.6 allyl, halogen, hydroxy, amino, cyano, nitro, trifluoromethyl, trifluoromethoxy, C.sub.1 -C.sub.6 alkoxy, --O.sub.2 CR', --NHCOR', --COR', --SO.sub.m R', where R' is C.sub.1 -C.sub.6 alkyl and wherein m is 0, 1 or 2; or R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 independently represent --CONR'R", or --NR'R" where R' and R" independently represent hydrogen or C.sub.1 -C.sub.6 alkyl; R.sub.10 is hydrogen or C.sub.1 -C.sub.6 alkyl; and R represents an aminoalkyl group; which compounds are useful in the treatment of affective disorders such as schizophrenia, depression, Alzheimer's disease, movement disorders such as Parkinsonism and dystonia, and other disorders which respond to dopaminergic blockade such as substance abuse and obsessive compulsive disorders. Further, compounds of this invention may be useful in treating the extrapyramidal side effects associated with the use of conventional neuroleptic agents.

  公开了以下化合物的结构式：##STR1##或其药学上可接受的酸加盐，其中：R.sub.1、R.sub.2、R.sub.3、R.sub.4、R.sub.5、R.sub.6、R.sub.7、R.sub.8和R.sub.9相同或不同，分别代表氢、C.sub.1-C.sub.6烯丙基、卤素、羟基、氨基、氰基、硝基、三氟甲基、三氟甲氧基、C.sub.1-C.sub.6烷氧基、--O.sub.2CR'、--NHCOR'、--COR'、--SO.sub.mR'，其中R'为C.sub.1-C.sub.6烷基，m为0、1或2；或R.sub.1、R.sub.2、R.sub.3、R.sub.4、R.sub.5、R.sub.6、R.sub.7、R.sub.8和R.sub.9分别独立地表示--CONR'R"或--NR'R"，其中R'和R"独立地表示氢或C.sub.1-C.sub.6烷基；R.sub.10表示氢或C.sub.1-C.sub.6烷基；R代表一种氨基烷基，这些化合物在治疗情感障碍（如精神分裂症、抑郁症、阿尔茨海默病）、运动障碍（如帕金森病和肌张力障碍）以及对多巴胺能阻滞有反应的其他障碍（如物质滥用和强迫性障碍）方面有用。此外，本发明的化合物可用于治疗与传统神经类药物使用相关的锥体外副作用。