1-(2,6-dichlorobenzoyl)-3-(1,2,3,5,8,8a-hexahydro-7-indolizinyl)-5-azaindole

• 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: 1-(2,6-dichlorobenzoyl)-3-(1,2,3,5,8,8a-hexahydro-7-indolizinyl)-5-azaindole
• 英文别名: [3-(1,2,3,5,8,8a-Hexahydroindolizin-7-yl)pyrrolo[3,2-c]pyridin-1-yl]-(2,6-dichlorophenyl)methanone
• 化学式: C₂₂H₁₉Cl₂N₃O
• 分子量: 412.318
• InChiKey: NJGJYYJRKPMKJU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.5
• 重原子数：
  28
• 可旋转键数：
  2
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.27
• 拓扑面积：
  38.1
• 氢给体数：
  0
• 氢受体数：
  3

文献信息

• [EN] PYRROLIDINE-2-ONES AS FACTOR XA INHIBITORS<br/>[FR] PYRROLIDINE-2-ONES UTILISEES COMME INHIBITEURS DU FACTEUR XA
  申请人：GLAXO GROUP LTD

  公开号：WO2003053925A1

  公开（公告）日：2003-07-03

  The invention relates to compounds of formula (I): , and pharmaceutically acceptable derivatives thereof. The invention also relates to processes for the preparation of compounds of formula (I), pharmaceutical compositions containing compounds of formula (I) and to the use of compounds of formula (I) in medicine, particularly in the amelioration of a clinical condition for which a Factor Xa inhibitor is indicated.

  该发明涉及式（I）的化合物，以及其药学上可接受的衍生物。该发明还涉及制备式（I）化合物的方法，含有式（I）化合物的药物组合物以及在医学上使用式（I）化合物，特别是在改善需要使用FXa抑制剂的临床病情方面的用途。
• Azaindoles having serotonin receptor affinity
  申请人：Edwards Louise

  公开号：US20050239788A1

  公开（公告）日：2005-10-27

  Described herein are compounds with affinity for the 5-HT 6 receptor, which have the general formula I: wherein: R represents a group of Formula II or Formula III; one of A, B D or E is a N atom, the remainder being CH groups; R 1 is selected from the group consisting of SO 2 Ar, C(O)Ar, CH 2 Ar and Ar; R 2 , R 3 and R 4 are independently selected from the group consisting of H and alkyl; represents a single or double bond, with the proviso that there is only one double bond in the ring at a time; n is an integer of from 1-3; Z is selected from the group consisting of C, CH and N, provided that when is a double bond, Z is C and when is a single bond, Z is selected from CH and N; Ar is an optionally substituted aryl group; with the proviso that when R is a group of Formula II, R 1 is SO 2 Ar. Also described is the use of these compounds as pharmaceuticals to treat indications where inhibition of the 5-HT 6 receptor is implicated, such as schizophrenia.

  本文描述了具有亲和力的化合物5-HT6受体，其具有一般式I：其中：R代表式II或式III的一个基团；A、B、D或E中的一个是N原子，其余为CH基团；R1从SO2Ar、C（O）Ar、CH2Ar和Ar的组中选择；R2、R3和R4独立地从H和烷基的组中选择；表示单键或双键，但环中只有一个双键；n为1-3的整数；Z从C、CH和N的组中选择，但当为双键时，Z为C，当为单键时，Z从CH和N中选择；Ar是可选取代的芳基基团；条件是当R为式II的基团时，R1为SO2Ar。还描述了这些化合物作为药物的使用，用于治疗5-HT6受体抑制所涉及的症状，如精神分裂症。
• Azaindoles having serotonin receptor affnity
  申请人：Allelix Biopharmaceuticals, Inc.

  公开号：US20010049441A1

  公开（公告）日：2001-12-06

  Described herein are compounds with affinity for the 5-HT 6 receptor, which have the general formula I: 1 wherein: R represents a group of Formula II or Formula III; one of A, B D or E is a N atom, the remainder being CH groups; R 1 is selected from the group consisting of SO 2 Ar, C(O)Ar, CH 2 Ar and Ar; R 2 , R 3 and R 4 are independently selected from the group consisting of H and alkyl; ----- represents a single or double bond, with the proviso that there is only one double bond in the ring at a time; n is an integer of from 1-3; Z is selected from the group consisting of C, CH and N, provided that when ----- is a double bond, Z is C and when ----- is a single bond, Z is selected from CH and N; Ar is an optionally substituted aryl group; with the proviso that when R is a group of Formula II, R 1 is SO 2 Ar. Also described is the use of these compounds as pharmaceuticals to treat indications where inhibition of the 5-HT 6 receptor is implicated, such as schizophrenia.

  本文描述了具有对5-HT6受体亲和力的化合物，其具有通式I：其中：R表示式II或式III的基团；A、B、D或E中的一个是N原子，其余为CH基团；R1选自SO2Ar、C（O）Ar、CH2Ar和Ar组成的群；R2、R3和R4独立地选自H和烷基组成的群；-----表示单键或双键，但环中只有一个双键；n为1-3的整数；Z选自C、CH和N组成的群，但当-----为双键时，Z为C，当-----为单键时，Z选自CH和N；Ar是可选取代的芳基基团；但当R是式II的基团时，R1为SO2Ar。还描述了将这些化合物用作药物治疗5-HT6受体抑制相关的疾病，例如精神分裂症。
• Azaindoles Having Serotonin Receptor Affinity
  申请人：Edwards Louise

  公开号：US20080004307A1

  公开（公告）日：2008-01-03

  Described herein are compounds with affinity for the 5-HT 6 receptor, which have the general formula I: wherein A, B, D, E, R 1 to R 3 and n are described herein. Also described is the use of these compounds as pharmaceuticals to treat indications where inhibition of the 5-HT 6 receptor is implicated, such as schizophrenia.

  本文描述了具有亲和力的化合物5-HT6受体，其通式为I:其中A、B、D、E、R1至R3和n如本文所述。还描述了这些化合物作为药物治疗5-HT6受体抑制涉及的症状（如精神分裂症）的用途。
• AZAINDOLES HAVING SEROTONIN RECEPTOR AFFINITY
  申请人：Edwards Louise

  公开号：US20120302596A1

  公开（公告）日：2012-11-29

  Described herein are compounds with affinity for the 5-HT 6 receptor, which have the general formula I: wherein A, B, D, E, R 1 to R 3 and n are described herein. Also described is the use of these compounds as pharmaceuticals to treat indications where inhibition of the 5-HT 6 receptor is implicated, such as schizophrenia.

  本文介绍了具有亲和力的化合物，其与5-HT6受体具有亲和力，其通式为I：其中A、B、D、E、R1至R3和n的描述如本文所述。还描述了这些化合物作为药物用于治疗抑制5-HT6受体有所涉及的适应症，例如精神分裂症。