US9670136, 56 N1-((trans)-2-(4-(pyridin-3-ylmethoxy)phenyl)cyclopropyl)cyclohexane-1,4-diamine

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 英文名称: US9670136, 56 N1-((trans)-2-(4-(pyridin-3-ylmethoxy)phenyl)cyclopropyl)cyclohexane-1,4-diamine
• 英文别名: 4-N-[(1S,2R)-2-[4-(pyridin-3-ylmethoxy)phenyl]cyclopropyl]cyclohexane-1,4-diamine
• 化学式: C₂₁H₂₇N₃O
• 分子量: 337.5
• InChiKey: FUXLXWZVYUFWPI-FMFRFZGHSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  25
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.48
• 拓扑面积：
  60.2
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• (HETERO)ARYL CYCLOPROPYLAMINE COMPOUNDS AS LSD1 INHIBITORS
  申请人：ORYZON GENOMICS, S.A.

  公开号：US20150119396A9

  公开（公告）日：2015-04-30

  The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and theft use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.

  本发明涉及（杂）芳基环丙胺化合物，特别是公式（I）所描述和定义的化合物，以及它们在治疗中的应用，包括但不限于治疗或预防癌症、神经系统疾病或病情，或病毒感染。
• Combinations of LSD1 inhibitors for use in the treatment of solid tumors
  申请人：ORYZON GENOMICS, S.A.

  公开号：US10265279B2

  公开（公告）日：2019-04-23

  The instant invention relates to therapeutic combinations of LSD1 inhibitors and one or more other active pharmaceutical ingredient(s) or pharmaceutically acceptable salts thereof. The combinations are particularly useful for treating neoplastic diseases, such as cancer, particularly small cell lung cancer (SCLC).

  本发明涉及 LSD1 抑制剂和一种或多种其他活性药物成分或其药学上可接受的盐的治疗组合。这些组合物特别适用于治疗肿瘤性疾病，如癌症，尤其是小细胞肺癌（SCLC）。
• US20140256729A1
  申请人：——

  公开号：US20140256729A1

  公开（公告）日：2014-09-11
• COMBINATIONS OF LSD1 INHIBITORS FOR USE IN THE TREATMENT OF SOLID TUMORS
  申请人：HOFFMANN-LA ROCHE INC.

  公开号：US20170281567A1

  公开（公告）日：2017-10-05

  The instant invention relates to therapeutic combinations of LSD1 inhibitors and one or more other active pharmaceutical ingredient(s) or pharmaceutically acceptable salts thereof. The combinations are particularly useful for treating neoplastic diseases, such as cancer, particularly small cell lung cancer (SCLC).
• GENE EXPRESSION BIOMARKERS FOR PERSONALIZED CANCER CARE TO EPIGENETIC MODIFYING AGENTS
  申请人：Oryzon Genomics, S.A.

  公开号：US20190153538A1

  公开（公告）日：2019-05-23

  The present application discloses a method to predict responsiveness of a patient, with cancer, to treatment with LSD1 inhibitors, said method comprising measuring mRNA expression levels of one or more genes selected from the list of ASCL1, DDC, CEACAM6, LRRIQ4, NR0B2, GRP, CEACAM5, SOX21, OR51E2, SEC11C, BAALC, CCDC40, RAB3B, RGS17, ABCE1, ETS2, CCDC154, SPAG6, PON1, TMEM176A, C1orf127, IGF2BP2, IGFBP5, FAM84A, FOXA2, HOXA10, NCAM1, NCAM2, NEUROD1, KRT8, ENO2, AVP, OXT, SYP, CHGA, CHGB, BCL2 and MYC.