[1,4a(2)-Bipiperidin]-1a(2)-amine | 173903-92-9

• 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: [1,4a(2)-Bipiperidin]-1a(2)-amine
• 英文别名: 4-piperidin-1-ylpiperidin-1-amine
• CAS: 173903-92-9
• 化学式: C₁₀H₂₁N₃
• 分子量: 183.297
• InChiKey: MLODPYDTHHAICY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  32.5
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  二苯基乙酰氯 、 [1,4a(2)-Bipiperidin]-1a(2)-amine 以 乙腈 为溶剂， 反应 6.0h， 以70%的产率得到
  参考文献：
  名称：

  Amide derivatives with H1-antihistaminic effect

  摘要：

  The synthesis and the structure-activity correlation of a series of N-aminoalkylacetamides as H1-antihistaminic agents have been carried out. The compounds were tested in vitro by measurement of the inhibition of histamine-induced contractions on isolated guinea pig ileum; the results are expressed as pA2.

  DOI：

  10.1016/s0031-6865(97)00025-3

文献信息

• [EN] NEW 6-AMINO-QUINOLINONE COMPOUNDS AND DERIVATIVES AS BCL6 INHIBITORS<br/>[FR] NOUVEAUX COMPOSÉS 6-AMINO-QUINOLINONE ET DÉRIVÉS EN TANT QU'INHIBITEURS DE BCL6
  申请人：BOEHRINGER INGELHEIM INT

  公开号：WO2018108704A1

  公开（公告）日：2018-06-21

  The present invention encompasses compounds of formula (I), wherein the groups R1 to R5, X, Y and W have the meanings given in the claims and specification, their use as inhibitors of BCL6, pharmaceutical compositions which contain compounds of this kind and their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases.

  本发明涵盖了式(I)的化合物，其中基团R1至R5、X、Y和W具有权利要求和说明中给定的含义，它们作为BCL6的抑制剂的用途，含有这种化合物的药物组合物以及它们作为药物的用途，特别是作为治疗和/或预防肿瘤疾病的药剂。
• Synthesis and antitumor activity of duocarmycin derivatives: modification at C-8 position of A-ring pyrrole compounds bearing the simplified DNA-binding groups
  作者：Nobuyoshi Amishiro、Satoru Nagamura、Chikara Murakata、Akihiko Okamoto、Eiji Kobayashi、Masao Asada、Katsushige Gomi、Tatsuya Tamaoki、Masami Okabe、Naoko Yamaguchi、Kazuo Yamaguchi、Hiromitsu Saito

  DOI：10.1016/s0968-0896(99)00293-x

  日期：2000.2

  A series of the 8-O-substituted A-ring pyrrole derivatives of duocarmycin bearing the simplified DNA-binding moieties such as cinnamoyl or heteroarylacryloyl groups were synthesized, and evaluated for in vitro anticellular activity against HeLa S-3 cells and in vivo antitumor activity against murine sarcoma 180 in mice. In addition, the stability of the 8-O-substituted analogues in aqueous solution and the conversion to their active form (cyclopropane compound) from the 8-O-substituted analogues in mice or human serum were examined. The 8-O-substituted A-ring pyrrole derivatives bearing the simplified DNA-binding moieties showed remarkably potent in vivo antitumor activity and low peripheral blood toxicity compared with the 8-O-substituted A-ring pyrrole derivatives having the trimethoxyindole skeleton in segment-B (Seg-B), which were equal to 8-O-[(N-methylpiperazinyl)carbonyl] derivatives of 4'-methoxycinnamates and 4'-methoxy-beta-heteroarylacrylates. Moreover, among 8-O-substituted analogues, several compounds can be chemically or enzymatically converted to their active form in human serum. This result indicated that new 8-O-substituted derivatives were different prodrugs from KW-2189 and 8-O-substituted analogues being the same type of prodrug as KW-21S9. (C) 2000 Elsevier Science Ltd. All rights reserved.
• DC-89 DERIVATIVE
  申请人：KYOWA HAKKO KOGYO CO., LTD.

  公开号：EP0705833B1

  公开（公告）日：2004-07-21
• 2-METHYLMORPHOLINE PYRIDO-,PYRAZO- AND PYRIMIDO-PYRIMIDINE DERIVATIVES AS MTOR INHIBITORS
  申请人：KuDOS Pharmaceuticals Limited

  公开号：EP2057156B1

  公开（公告）日：2017-02-01
• 6-AMINO-QUINOLINONE COMPOUNDS AND DERIVATIVES AS BCL6 INHIBITORS
  申请人：Boehringer Ingelheim International GmbH

  公开号：EP3555063B1

  公开（公告）日：2020-09-16