trans-1-Cyclohexylamino-2-phenylcyclopropan | 32751-99-8

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: trans-1-Cyclohexylamino-2-phenylcyclopropan
• 英文别名: N-[(1R,2S)-2-phenylcyclopropyl]cyclohexanamine
• CAS: 32751-99-8
• 化学式: C₁₅H₂₁N
• 分子量: 215.338
• InChiKey: YPEIHBUSSOFCJK-LSDHHAIUSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  16
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.6
• 拓扑面积：
  12
• 氢给体数：
  1
• 氢受体数：
  1

文献信息

• [EN] LYSINE SPECIFIC DEMETHYLASE-1 INHIBITORS AND THEIR USE<br/>[FR] INHIBITEURS DE LA DÉMÉTHYLASE-1 SPÉCIFIQUES DE LA LYSINE, ET LEUR UTILISATION
  申请人：ORYZON GENOMICS SA

  公开号：WO2011131697A1

  公开（公告）日：2011-10-27

  The present invention relates to a compound of Formula 1, wherein: (A) is heteroaryl or aryl; each (Α'), if present, is independently chosen from aryl, arylalkoxy, arylalkyl, heterocyclyl, aryloxy, halo, alkoxy, haloalkyl, cycloalkyl, haloalkoxy, and cyano, wherein each (Α') is substituted with 0, 1, 2, or 3 substituents independently chosen from halo, haloalkyl, haloalkoxy, aryl, arylalkoxy, alkyl, alkoxy, amido, -CH2C(=0)NH2, heteroaryl, cyano, sulfonyl, and sulfinyl; X is 0, 1, 2, or 3; (B) is a cyclopropyl ring, wherein (A) and (Z) are covalently bonded to different carbon atoms of (B); (Z) is -NH-; (L) is chosen from a single bond, -CH2-, -CH2CH2-, -CH2CH2CH2-, and -CH2CH2CH2CH2-; and (D) is an aliphatic carbocyclic group or benzocycloalkyl, wherein said aliphatic carbocyclic group or said benzocycloalkyl has 0, 1, 2, or 3 substituents independently chosen from - NH2, -NH(C1-C6 alkyl), -N(C1-C6 alkyl)(C1-C6 alkyl), alkyl, halo, amido, cyano, alkoxy, haloalkyl, and haloalkoxy. (A')X-(A)-(B)-(Z)-(L)-(D) formula (I) The compounds of the invention show activity for inhibiting LSD1, which makes them useful in the treatment or prevention of diseases such as cancer.

  本发明涉及式I化合物，其中：(A)是杂芳基或芳基；每个(Α')，如果有，独立地选自芳基、芳基烷氧基、芳基烷基、杂环基、芳氧基、卤素、烷氧基、卤代烷基、环烷基、卤代烷氧基和腈，其中每个(Α')被0、1、2或3个独立选自卤素、卤代烷基、卤代烷氧基、芳基、芳基烷氧基、烷基、烷氧基、酰胺、- C(=0)NH2、杂芳基、腈、磺酰基和亚磺酰基的取代基取代；X是0、1、2或3；(B)是环丙基环，其中(A)和(Z)与(B)的不同碳原子以共价键连接；(Z)是-NH-；(L)选自单一键、-CH2-、- -、- -和- -；以及(D)是脂肪族碳环组或苯并环烷基，其中所述脂肪族碳环组或所述苯并环烷基具有0、1、2或3个独立选自-NH2、-NH(C1-C6烷基)、-N(C1-C6烷基)(C1-C6烷基)、烷基、卤素、酰胺、腈、烷氧基、卤代烷基和卤代烷氧基的取代基。式(I) (A')X-(A)-(B)-(Z)-(L)-(D)本发明的化合物对于抑制LSD1具有活性，这使得它们在治疗或预防诸如癌症等疾病方面有用。
• LYSINE SPECIFIC DEMETHYLASE-1 INHIBITORS AND THEIR USE
  申请人：Ortega Munoz Alberto

  公开号：US20130090386A1

  公开（公告）日：2013-04-11

  The present invention relates to a compound of Formula 1, wherein: (A) is heteroaryl or aryl; each (A′), if present, is independently chosen from aryl, arylalkoxy, arylalkyl, heterocyclyl, aryloxy, halo, alkoxy, haloalkyl, cycloalkyl, haloalkoxy, and cyano, wherein each (A′) is substituted with 0, 1, 2, or 3 substituents independently chosen from halo, haloalkyl, haloalkoxy, aryl, arylalkoxy, alkyl, alkoxy, amido, —CH 2 C(=0)NH 2 , heteroaryl, cyano, sulfonyl, and sulfinyl; X is 0, 1, 2, or 3; (B) is a cyclopropyl ring, wherein (A) and (Z) are covalently bonded to different carbon atoms of (B); (Z) is —NH—; (L) is chosen from a single bond, —CH 2 —, —CH 2 CH 2 —, —CH 2 CH 2 CH 2 —, and —CH 2 CH 2 CH 2 CH 2 —; and (D) is an aliphatic carbocyclic group or benzocycloalkyl, wherein said aliphatic carbocyclic group or said benzocycloalkyl has 0, 1, 2, or 3 substituents independently chosen from —NH 2 , —NH(C 1 -C 6 alkyl), —N(C 1 -C 6 alkyl)(C 1 -C 6 alkyl), alkyl, halo, amido, cyano, alkoxy, haloalkyl, and haloalkoxy. (A′)X-(A)-(B)—(Z)-(L)-(D) formula (I) The compounds of the invention show activity for inhibiting LSD1, which makes them useful in the treatment or prevention of diseases such as cancer.

  本发明涉及一种式子1的化合物，其中：(A)是杂环芳基或芳基；每个(A')，如果存在，则独立选择自芳基、芳基烷氧基、芳基烷基、杂环烷基、芳氧基、卤素、烷氧基、卤代烷基、环烷基、卤代烷氧基和氰基，其中每个(A')被取代为0、1、2或3个取代基，独立选择自卤素、卤代烷基、卤代烷氧基、芳基、芳基烷氧基、烷基、烷氧基、酰胺基、— C（=0）NH2、杂环芳基、氰基、磺酰基和亚磺酰基；X为0、1、2或3；(B)为环丙基环，其中(A)和(Z)与(B)的不同碳原子共价键结合；(Z)为—NH—；(L)选择自单键、—CH2—、— —、— —和— —；(D)为脂肪环烷基或苯环烷基，其中所述脂肪环烷基或所述苯环烷基具有0、1、2或3个取代基，独立选择自—NH2、—NH（C1-C6烷基）、—N（C1-C6烷基）（C1-C6烷基）、烷基、卤素、酰胺基、氰基、烷氧基、卤代烷基和卤代烷氧基。(A')X-(A)-(B)-(Z)-(L)-(D)式（I）本发明的化合物表现出抑制LSD1的活性，使它们在治疗或预防癌症等疾病方面有用。
• Lysine specific demethylase-1 inhibitors and their use
  申请人：ORYZON GENOMICS S.A.

  公开号：US10202330B2

  公开（公告）日：2019-02-12

  The present invention relates to a compound of Formula 1, wherein: (A) is heteroaryl or aryl; each (A′), if present, is independently chosen from aryl, arylalkoxy, arylalkyl, heterocyclyl, aryloxy, halo, alkoxy, haloalkyl, cycloalkyl, haloalkoxy, and cyano, wherein each (A′) is substituted with 0, 1, 2, or 3 substituents independently chosen from halo, haloalkyl, haloalkoxy, aryl, arylalkoxy, alkyl, alkoxy, amido, —CH2C(=0)NH2, heteroaryl, cyano, sulfonyl, and sulfinyl; X is 0, 1, 2, or 3; (B) is a cyclopropyl ring, wherein (A) and (Z) are covalently bonded to different carbon atoms of (B); (Z) is —NH—; (L) is chosen from a single bond, —CH2—, —CH2CH2—, —CH2CH2CH2—, and —CH2CH2CH2CH2—; and (D) is an aliphatic carbocyclic group or benzocycloalkyl, wherein said aliphatic carbocyclic group or said benzocycloalkyl has 0, 1, 2, or 3 substituents independently chosen from —NH2, —NH(C1-C6 alkyl), —N(C1-C6 alkyl)(C1-C6 alkyl), alkyl, halo, amido, cyano, alkoxy, haloalkyl, and haloalkoxy. (A′)X-(A)-(B)—(Z)-(L)-(D) formula (I) The compounds of the invention show activity for inhibiting LSD1, which makes them useful in the treatment or prevention of diseases such as cancer.

  本发明涉及式 1 的化合物，其中：(A)是杂芳基或芳基；每个(A′)（如果存在）独立地选自芳基、芳烷氧基、芳烷基、杂环基、芳氧基、卤代、烷氧基、卤代烷基、环烷基、卤代烷氧基和氰基，其中每个(A′)被 0、1、2 或 3 个取代基，这些取代基独立选自卤代、卤代烷基、卤代烷氧基、芳基、芳基烷氧基、烷基、烷氧基、氨基、- C(=0)NH2、杂芳基、氰基、磺酰基和亚砜基；X 是 0、1、2 或 3；(B) 是环丙基环，其中(A)和(Z)与(B)的不同碳原子共价键合；(Z)是-NH-；(L)选自单键、-CH2-、- -、- -和- -；和 (D) 是脂肪族碳环基团或苯并环烷基，其中所述脂肪族碳环基团或所述苯并环烷基具有 0、1、2 或 3 个取代基，这些取代基独立选自-NH2、-NH(C1-C6 烷基)、-N(C1-C6 烷基)(C1-C6 烷基)、烷基、卤代、氨基、氰基、烷氧基、卤代烷基和卤代烷氧基。(A′)X-(A)-(B)-(Z)-(L)-(D) 式(I) 本发明的化合物显示出抑制 LSD1 的活性，这使它们在治疗或预防癌症等疾病中有用。
• LYSINE DEMETHYLASE INHIBITORS FOR INFLAMMATORY DISEASES OR CONDITIONS
  申请人：Oryzon Genomics, S.A.

  公开号：EP2741741A2

  公开（公告）日：2014-06-18
• LYSINE DEMETHYLASE INHIBITORS FOR THROMBOSIS AND CARDIOVASCULAR DISEASES
  申请人：Oryzon Genomics, S.A.

  公开号：EP2750671A2

  公开（公告）日：2014-07-09