6-(2-{[3-(1-Piperazinyl)-2-pyrazinyl]oxy}ethoxy)-1H-indole | 313656-46-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: 6-(2-{[3-(1-Piperazinyl)-2-pyrazinyl]oxy}ethoxy)-1H-indole
• 英文别名: 6-[2-(3-piperazin-1-ylpyrazin-2-yl)oxyethoxy]-1H-indole
• CAS: 313656-46-1
• 化学式: C₁₈H₂₁N₅O₂
• 分子量: 339.397
• InChiKey: GDWJIQSVXAJGCA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  25
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  75.3
• 氢给体数：
  2
• 氢受体数：
  6

文献信息

• CERTAIN ARYLALIPHATIC AND HETEROARYL-ALIPHATIC PIPERAZINYL PYRAZINES AND THEIR USE IN THE TREATMENT OF SEROTONIN-RELATED DISEASES
  申请人：Biovitrum, AB, a Stockholm, Sweden corporation

  公开号：US20040242554A1

  公开（公告）日：2004-12-02

  The invention relates to compounds of the general formula (I): 1 wherein Ar is optionally substituted aryl or heteroaryl; A is (i) —O—, —S—, —SO 2 —, —NH—, (ii) a C 1-4 -alkyl- or C 1-6 -acyl-substituted nitrogen atom or (iii) a C 1-8 -alkylene chain or a heteroalkylene chain having 2 to 8 chain atoms, which optionally contains at least one unsaturation, and which may be substituted and/or contain a bridge to form a saturated or partially or fully unsaturated ring having 3-8 ring members; B is —C(R 4 )(R 5 )—, —OC(R 4 )(R 5 )—, —N(R 6 )C(R 4 )(R 5 )—, —N(R 6 )—, —O—, —S— or —SO 2 —; R is optionally substituted C 3-8 -cycloalkyl, aryl or heteroaryl; R 1 is (i) a saturated or unsaturated azacyclic or aminoazacyclic ring, or a saturated diazacyclic or aminodiazacyclic ring, which has 4 to 7 ring members, or a saturated aminoazabicyclic, azabicyclic or diazabicyclic ring which has 7 to 10 ring members, which rings optionally are substituted in one or more positions, or a group —[C(R 4 )(R 5 )] x N(R 2a )(R 3a )]; R 2a , R 3a , R 4 , R 5 , R 6 and x are as defined in the claims, and n is 0 or 1; and pharmaceutically acceptable salts, hydrates and prodrug forms thereof. The compounds may be prepared by per se conventional methods and can be used for treating a human or animal subject suffering from a serotonin-related disorder, such as eating disorders, especially obesity, memory, disorders, schizophrenia, mood disorders, anxiety disorders, pain, sexual dysfunctions, and urinary disorders. The invention also relates to such use as well as to pharmaceutical compositions comprising a compound of formula (I).

  本发明涉及通式（I）的化合物：其中Ar是可选取代的芳基或杂芳基；A是（i）—O—，—S—，—SO2—，—NH—，（ii）C1-4烷基或C1-6酰基取代的氮原子，或（iii）C1-8烷基链或具有2-8链原子的杂烷基链，其可选包含至少一个不饱和度，并且可以取代和/或含有桥接以形成具有3-8环成员的饱和或部分或完全不饱和环；B是—C（R4）（R5）—，—OC（R4）（R5）—，—N（R6）C（R4）（R5）—，—N（R6）—，—O—，—S—或—SO2—；R是可选取代的C3-8环烷基，芳基或杂芳基；R1是（i）饱和或不饱和的氮杂环或氨基氮杂环，或饱和的二氮杂环或氨基二氮杂环，其具有4-7环成员，或饱和的氨基氮杂双环、氮杂双环或二氮杂双环，其具有7-10环成员，这些环在一个或多个位置上可选取代，或者是一个组—[C（R4）（R5）]xN（R2a）（R3a）；R2a，R3a，R4，R5，R6和x如权利要求中所定义，n为0或1；以及其药学上可接受的盐、水合物和前药形式。这些化合物可以通过常规方法制备，并可用于治疗患有血清素相关疾病的人或动物，例如进食障碍，尤其是肥胖症，记忆障碍，精神分裂症，情绪障碍，焦虑障碍，疼痛，性功能障碍和泌尿系统疾病。本发明还涉及这种用途以及包含通式（I）化合物的制药组合物。
• Certain arylaliphatic and heteroaryl-aliphatic piperazinyl pyrazines and their use in the treatment of serotonin-related diseases
  申请人：Biovitrum, AB, a Stockholm, Sweden corporation

  公开号：US20030092694A1

  公开（公告）日：2003-05-15

  The invention relates to compounds of the general formula (I): 1 wherein Ar is optionally substituted aryl or heteroaryl; A is (i) —O—, —S—, —SO 2 —, —NH—, (ii) a C 1-4 -alkyl- or C 1-6 -acyl-substituted nitrogen atom or (iii) a C 1-8 -alkylene chain or a heteroalkylene chain having 2 to 8 chain atoms, which optionally contains at least one unsaturation, and which may be substituted and/or contain a bridge to form a saturated or partially or fully unsaturated ring having 3-8 ring members; B is —C(R 4 )(R 5 )—, —OC(R 4 )(R 5 )—, —N(R 6 )C(R 4 )(R 5 )—, —N(R 6 )—, —O—, —S— or —SO 2 —; R is optionally substituted C 3-8 -cycloalkyl, aryl or heteroaryl; R 1 is (i) a saturated or unsaturated azacyclic or aminoazacyclic ring, or a saturated diazacyclic or aminodiazacyclic ring, which has 4 to 7 ring members, or a saturated aminoazabicyclic, azabicyclic or diazabicyclic ring which has 7 to 10 ring members, which rings optionally are substituted in one or more positions, or a group —[C(R 4 )(R 5 )] x N(R 2a )(R 3a )]; R 2a , R 3a , R 4 , R 5 , R 6 and x are as defined in the claims, and n is 0 or 1; and pharmaceutically acceptable salts, hydrates and prodrug forms thereof The compounds may be prepared by per se conventional methods and can be used for treating a human or animal subject suffering from a serotonin-related disorder, such as eating disorders, especially obesity, memory disorders, schizophrenia, mood disorders, anxiety disorders, pain, sexual dysfunctions, and urinary disorders The invention also relates to such use as well as to pharmaceutical compositions comprising a compound of formula (I)

  本发明涉及一般式（I）的化合物：其中Ar是可选取代的芳基或杂环芳基；A是（i）-O-，-S-，-SO2-，-NH-，（ii）C1-4-烷基或C1-6-酰基取代的氮原子或（iii）C1-8-烷基链或具有2至8个链原子的杂烷基链，可选地含有至少一个不饱和度，并且可以取代和/或包含桥以形成具有3-8个环成员的饱和或部分或完全不饱和的环；B是-C（R4）（R5）-，-OC（R4）（R5）-，-N（R6）C（R4）（R5）-，-N（R6）-，-O-，-S-或-SO2-；R是可选取代的C3-8-环烷基，芳基或杂环芳基；R1是（i）饱和或不饱和的氮杂环或氨基氮杂环环，或具有4至7个环成员的饱和二氮杂环或氨基二氮杂环环，或具有7至10个环成员的饱和氨基氮杂双环、氮杂双环或二氮杂双环环，这些环可选地在一个或多个位置上取代，或一个组-［C（R4）（R5）］xN（R2a）（R3a）；其中R2a，R3a，R4，R5，R6和x如所述，n为0或1；以及其药学上可接受的盐、水合物和前药形式。这些化合物可以通过常规方法制备，并可用于治疗患有血清素相关疾病的人类或动物受试者，例如进食障碍，特别是肥胖，记忆障碍，精神分裂症，情绪障碍，焦虑症，疼痛，性功能障碍和泌尿系统疾病。本发明还涉及这种用途以及包含式（I）化合物的药物组合物。
• NOVEL COMPOUNDS, THEIR USE AND PREPARATION
  申请人：Pharmacia AB

  公开号：EP1178973A2

  公开（公告）日：2002-02-13
• US6465467B1
  申请人：——

  公开号：US6465467B1

  公开（公告）日：2002-10-15
• US7071180B2
  申请人：——

  公开号：US7071180B2

  公开（公告）日：2006-07-04