(1R,2R)-2-(5-bromothiophen-2-yl)cyclopropan-1-amine

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: (1R,2R)-2-(5-bromothiophen-2-yl)cyclopropan-1-amine
• 化学式: C₇H₈BrNS
• 分子量: 218.12
• InChiKey: YOZWARUYCJJUCK-RFZPGFLSSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  10
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.428
• 拓扑面积：
  54.3
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• [EN] CYCLOPROPANAMINE COMPOUND AND USE THEREOF<br/>[FR] COMPOSÉ DE CYCLOPROPANAMINE ET SON UTILISATION
  申请人：TAKEDA PHARMACEUTICAL

  公开号：WO2015156417A1

  公开（公告）日：2015-10-15

  The present invention provides a compound having a lysine-specific demethylase-1 inhibitory action, and useful as a medicament such as a prophylactic or therapeutic agent for schizophrenia, developmental disorders, particularly diseases having intellectual disability (e.g., autistic spectrum disorders, Rett syndrome, Down's syndrome, Kabuki syndrome, fragile X syndrome, Kleefstra syndrome, neurofibromatosis type 1, Noonan syndrome, tuberous sclerosis), neurodegenerative diseases (e.g., Alzheimer's disease, Parkinson's disease, spinocerebellar degeneration (e.g., dentatorubural pallidoluysian atrophy) and Huntington's disease), epilepsy (e.g., Dravet syndrome) or drug dependence, and the like. A compound represented by the formula wherein each symbol is as defined in the present specification, or a salt thereof.

  本发明提供了一种具有赖氨酸特异性去甲基化酶-1抑制作用的化合物，可用作药物，例如作为精神分裂症、发育障碍，特别是智力障碍性疾病（例如自闭症谱系障碍、雷特综合征、唐氏综合征、歌舞综合征、脆性X综合征、克里夫斯特拉综合征、神经纤维瘤病1型、努南综合征、结节性硬化症等）神经退行性疾病（例如阿尔茨海默病、帕金森病、脊髓小脑变性疾病（例如小脑纹状体苍白松解性萎缩）和亨廷顿病）、癫痫（例如德拉综合征）或药物依赖等的预防或治疗剂。化合物如下式所示，其中每个符号如本说明书中定义，或其盐。
• FLUORINATED CYCLOPROPYLAMINE COMPOUND, PREPARATION METHOD THEREFOR, PHARMACEUTICAL COMPOSITION THEREOF, AND USERS THEREOF
  申请人：Shanghai Institute of Materia Medica, Chinese Academy of Sciences

  公开号：EP3431471A1

  公开（公告）日：2019-01-23

  Provided are a compound represented by formula I, a raceme thereof, an R-isomer thereof, an S-isomer thereof, a pharmaceutical salt thereof, and a mixture thereof, a preparation method therefor, a pharmaceutical composition comprising the compound, and uses thereof serving as an lysine specific demethylase 1 (LSD1) inhibitor. Provided are uses of the fluorinated cyclopropylamine compound represented by formula I in the treatment of cancers.

  提供一种由式 I 代表的化合物、其外消旋体、其 R-异构体、其 S-异构体、其药用盐和其混合物、其制备方法、包含该化合物的药物组合物以及其作为赖氨酸特异性去甲基化酶 1（LSD1）抑制剂的用途。提供了式 I 所代表的氟化环丙胺化合物在治疗癌症中的用途。
• Fluorinated cyclopropylamine compound, preparation method therefor, pharmaceutical composition thereof, and uses thereof
  申请人：SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

  公开号：US10836743B2

  公开（公告）日：2020-11-17

  Provided is a fluorinated cyclopropylamine compound represented by formula I, a racemate thereof, an R-isomer thereof, an S-isomer thereof, a pharmaceutical salt thereof, and a mixture thereof. Also provided are pharmaceutical compositions containing the compound, a preparation method for the compound, and uses thereof as a lysine specific demethylase 1 (LSD1) inhibitor, and in the treatment of cancers.

  本发明提供了一种由式 I 代表的氟化环丙胺化合物、其外消旋体、其 R-异构体、其 S-异构体、其药用盐以及其混合物。还提供了含有该化合物的药物组合物、该化合物的制备方法，以及其作为赖氨酸特异性去甲基化酶 1（LSD1）抑制剂和治疗癌症的用途。
• (HETERO)ARYL CYCLOPROPYLAMINE COMPOUNDS AS LSD1 INHIBITORS
  申请人：Oryzon Genomics, S.A.

  公开号：EP2776394B1

  公开（公告）日：2018-12-26
• CYCLOPROPANAMINE COMPOUND AND USE THEREOF
  申请人：Takeda Pharmaceutical Company Limited

  公开号：EP3129369A1

  公开（公告）日：2017-02-15