N-(2-Chloro-1H-pyrrol-1-yl)-N-(4-pyridinyl)-3,4-dimethoxyphenylacetamide hydrochloride

• 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-Chloro-1H-pyrrol-1-yl)-N-(4-pyridinyl)-3,4-dimethoxyphenylacetamide hydrochloride
• 英文别名: N-(2-chloropyrrol-1-yl)-2-(3,4-dimethoxyphenyl)-N-pyridin-4-ylacetamide;hydrochloride
• 化学式: C₁₉H₁₈ClN₃O₃*ClH
• 分子量: 408.284
• InChiKey: ODOBSGGRRXSWPP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.01
• 重原子数：
  27
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.16
• 拓扑面积：
  56.6
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  N-(2-Chloro-1H-pyrrol-1-yl)-N-(4-pyridinyl)-3,4-dimethoxyphenylacetamide 生成 N-(2-Chloro-1H-pyrrol-1-yl)-N-(4-pyridinyl)-3,4-dimethoxyphenylacetamide hydrochloride
  参考文献：
  名称：

  EFFLAND, RICHARD C.;KLEIN, JOSEPH T.;KAPPLES, KEVIN J.

  摘要：

  DOI：

文献信息

• N-(pyrrol-1-yl)pyridinamines having memory enhancing activity
  申请人：Hoechst-Roussel Pharmaceuticals, Inc.

  公开号：US04792562A1

  公开（公告）日：1988-12-20

  There are disclosed novel compounds of the formula ##STR1## where n is 0 or 1; R is hydrogen or loweralkyl; R.sub.1 is hydrogen, loweralkyl, halogen, cyano, loweralkanoyl, arylloweralkanoyl, aroyl, --CH(OH)R.sub.4, --C(OH)R.sub.4 R.sub.5 or --CH.sub.2 OR.sub.5, --CH.dbd.CR.sub.6 R.sub.7, --CH.dbd.CHCN, --CH.dbd.CHOCH.sub.3, --CH.dbd.CHCO.sub.2 C.sub.2 H.sub.5, ##STR2## --CH.sub.2 CHR.sub.6 R.sub.7, --CH.sub.2 CH.sub.2 CN, --CH.sub.2 CH.sub.2 OCH.sub.3, --CH.sub.2 CH.sub.2 CO.sub.2 C.sub.2 H.sub.5, ##STR3## R.sub.4 being hydrogen, loweralkyl, arylloweralkyl or aryl, R.sub.5 being loweralkyl, aryl or arylloweralkyl, R.sub.6 being hydrogen or loweralkyl and R.sub.7 being hydrogen, loweralkyl or aryl; R.sub.2 is hydrogen, loweralkyl, loweralkenyl, loweralkynyl, --CH.sub.2 CO.sub.2 C.sub.2 H.sub.5, arylloweralkyl, phenyl, nitrophenyl, cyanophenyl, trifluoromethylphenyl, aminophenyl, loweralkanoylaminophenyl, loweralkoxycarbonyl, arylloweralkoxycarbonyl, aryloxycarbonyl, loweralkylaminocarbonyl, arylloweralkylaminocarbonyl, arylaminocarbonyl, alkanoyl, arylloweralkanoyl, aroyl, alkenoyl, alkynoyl, --CH.sub.2 C.tbd.CCH.sub.2 --NR'R", --CH.sub.2 CH.dbd.CHCH.sub.2 --NR'R" or --CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 --NR'R", R' and R" being independently loweralkyl or --NR'R" taken as a whole being ##STR4## and R.sub.3 is hydrogen, NO.sub.2, NH.sub.2, halogen, loweralkanoylamino, arylloweralkanoylamino, aroylamino or loweralkyl; with the proviso that when n is 0, R.sub.2 is phenyl, R.sub.3 is hydrogen and the pyridine moiety is 2-pyridinyl, R and R.sub.1 may not be 2-methyl and 5-methyl; or pharmaceutically acceptable acid addition salts thereof, which are useful for enhancing memory, methods for synthesizing them, pharmaceutical compositions comprising an effective memory enhancing amount of such a compound and a method of treating a patient in need of memory enhancement which comprises administering such a compound to the patient.

  揭示了一种新颖的化合物，其化学式为##STR1##其中n为0或1；R为氢或低碳烷基；R.sub.1为氢、低碳烷基、卤素、氰基、低碳酰基、芳基低碳酰基、芳酰基、--CH(OH)R.sub.4、--C(OH)R.sub.4 R.sub.5或--CH.sub.2 OR.sub.5、--CH.dbd.CR.sub.6 R.sub.7、--CH.dbd.CHCN、--CH.dbd.CHOCH.sub.3、--CH.dbd.CHCO.sub.2 C.sub.2 H.sub.5、##STR2##--CH.sub.2 CHR.sub.6 R.sub.7、--CH.sub.2 CH.sub.2 CN、--CH.sub.2 CH.sub.2 OCH.sub.3、--CH.sub.2 CH.sub.2 CO.sub.2 C.sub.2 H.sub.5、##STR3##其中R.sub.4为氢、低碳烷基、芳基低碳烷基或芳基，R.sub.5为低碳烷基、芳基或芳基低碳烷基，R.sub.6为氢或低碳烷基，R.sub.7为氢、低碳烷基或芳基；R.sub.2为氢、低碳烷基、低碳烯基、低碳炔基、--CH.sub.2 CO.sub.2 C.sub.2 H.sub.5、芳基低碳烷基、苯基、硝基苯基、氰基苯基、三氟甲基苯基、氨基苯基、低碳酰胺基苯基、低碳氧羰基、芳基低碳氧羰基、芳氧羰基、低碳烷基氨基羰基、芳基低碳烷基氨基羰基、芳基氨基羰基、烷酰基、芳基低碳酰基、芳酰基、烯酰基、炔酰基、--CH.sub.2 C.tbd.CCH.sub.2 --NR'R"、--CH.sub.2 CH.dbd.CHCH.sub.2 --NR'R"或--CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 --NR'R"，其中R'和R"独立地为低碳烷基或--NR'R"作为一个整体为##STR4##，R.sub.3为氢、NO.sub.2、NH.sub.2、卤素、低碳酰胺基、芳基低碳酰胺基、芳酰胺基或低碳烷基；但当n为0时，R.sub.2为苯基，R.sub.3为氢，吡啶基为2-吡啶基时，R和R.sub.1可能不是2-甲基和5-甲基；或其药学上可接受的酸盐，用于增强记忆，合成它们的方法，包含有效增强记忆量的这种化合物的药物组合物以及治疗需要记忆增强的患者的方法，包括将这种化合物给患者服用。
• N-(pyrrol-1-yl)pyridinamines, a process for their preparation and their use as medicaments
  申请人：HOECHST-ROUSSEL PHARMACEUTICALS INCORPORATED

  公开号：EP0226099A2

  公开（公告）日：1987-06-24

  There are disclosed novel compounds of the formula where n is 0 or 1; R is hydrogen or loweralkyl; R, is hydrogen, loweralkyl, halogen, cyano, loweralkanoyl, arylloweralkanoyl, aroyl, -CH(OH)R4, -C(OH)R4R5 or -CH2OR5, or , R, being hydrogen, loweralkyl, arylloweralkyl or aryl, Rs being loweralkyl, aryl or arylloweralkyl, R6 being hydrogen or loweralkyl and R7 being hydrogen, loweralkyl or aryl; R2 is hydrogen, loweralkyl, loweralkenyl, loweralkynyl, -CH2CO2C2H5, arylloweralkyl, phenyl, nitrophenyl, cyanophenyl, trifluoromethylphenyl, aminophenyl, loweralkanoylaminophenyl, loweralkoxycarbonyl, arylloweralkoxycarbonyl, aryloxycarbonyl, loweralkylaminocarbonyl, arylloweralkylaminocarbonyl, arylaminocarbonyl, alkanoyl, arylloweralkanoyl, aroyl, alkenoyl, alkynoyl, -CH2C≡CCH2-NR'R", -CH2CH=CHCH2-NR'R", or -CH2CH2CH2CH2-NR'R", R' and R" being independently loweralkyl or NR'R" taken as a whole being or ; and R3 is hydrogen, NO2, NH2, halogen, loweralkanoylamino, arylloweralkanoylamino, aroylamino or loweralkyl; with the proviso that when n is 0, R2 is phenyl, R3 is hydrogen and the pyridine moiety is 2-pyridinyl, R and R, may not be 2-methyl and 5-methyl; or pharmaceutically acceptable acid addition salts thereof, which are useful for enhancing memory, methods for synthesizing them, pharmaceutical compositions comprising an effective memory enhancing amount of such a compound and a method of treating a patient in need of memory enhancement which comprises administering such a compound to the patient.

  公开了式中的新型化合物 其中 n 是 0 或 1；R 是氢或低级烷基；R，是氢、低级烷基、卤素、氰基、低级烷酰基、芳基低级烷酰基、芳基、-CH(OH)R4、-C(OH)R4R5 或 -CH2OR5、 或 R2 为氢、低级烷基、芳低级烷基或芳基，Rs 为低级烷基、芳基或芳低级烷基，R6 为氢或低级烷基，R7 为氢、低级烷基或芳基；R2 是氢、低级烷基、低级烯基、低级炔基、-CH2CO2C2H5、芳低级烷基、苯基、硝基苯基、氰苯基、三氟甲基苯基、氨基苯基、低级烷酰氨基苯基、低级烷氧基羰基、芳低级烷氧基羰基、芳氧基羰基、低级烷基氨基羰基、芳基低级烷基氨基羰基、芳基氨基羰基、烷酰基、芳基低级烷酰基、芳基、烯酰基、炔酰基、-CH2C≡CCH2-NR'R"、-CH2CH=CHCH2-NR'R "或-CH2CH2CH2-NR'R"，R'和 R "独立为低级烷基或 NR'R "作为一个整体是 或 和 R3 为氢、NO2、NH2、卤素、低级烷酰基氨基、芳基低级烷酰基氨基、芳基氨基或低级烷基；但当 n 为 0、R2 为苯基、R3 为氢且吡啶基为 2-吡啶基时，R 和 R 不得为 2-甲基和 5-甲基；或其药学上可接受的酸加成盐，它们对增强记忆有用；合成它们的方法；包含有效记忆增强量的这种化合物的药物组合物；以及治疗需要增强记忆的病人的方法，这种方法包括给病人施用这种化合物。
• EFFLAND, RICHARD C.;KLEIN, JOSEPH T.;KAPPLES, KEVIN J.
  作者：EFFLAND, RICHARD C.、KLEIN, JOSEPH T.、KAPPLES, KEVIN J.

  DOI：——

  日期：——
• US4752610A
  申请人：——

  公开号：US4752610A

  公开（公告）日：1988-06-21
• US4792562A
  申请人：——

  公开号：US4792562A

  公开（公告）日：1988-12-20