发明名称 CYCLOPROPYLAMINE DERIVATIVES USEFUL AS LSD1 INHIBITORS
摘要 The invention relates to cyclopropylamine compounds, in particular the compounds of Formula (I), and their use in therapy, including e.g. in the treatment or prevention of cancer, a neurological disease or condition, or viral infection.;
申请公布号 US2016052865(A1) 申请公布日期 2016.02.25
申请号 US201514640395 申请日期 2015.03.06
申请人 Oryzon Genomics, S.A. 发明人 FYFE Matthew Colin Thor;ORTEGA MUÑOZ Alberto;CASTRO-PALOMINO LARIA Julio;MARTINELL PEDEMONTE Marc;ESTIARTE-MARTINEZ Maria de los Angeles;VALLS VIDAL Nuria
分类号 C07C211/40;C07C311/09;C07C311/08;C07C255/59;C07C215/64;C07C311/21 主分类号 C07C211/40
代理机构 代理人
主权项 1. A compound of Formula (I) or an enantiomer, a diastereomer, or a mixture thereof, or a pharmaceutically acceptable salt or solvate thereof: wherein: E is —X3═X4—, and X1, X2, X3 and X4 are independently C(R2); (G) is an aryl or heterocyclyl group; each (R1) is independently chosen from alkyl, alkenyl, alkynyl, cyclyl, -L1-cyclyl, -L1-amino, -L1-hydroxyl, amino, amido, nitro, halo, haloalkyl, haloalkoxy, cyano, sulfinyl, sulfonyl, sulfonamide, hydroxyl, alkoxy, urea, carbamate, acyl, and carboxyl; each (R2) is independently chosen from —H, alkyl, alkenyl, alkynyl, cyclyl, -L1-cyclyl, -L1-amino, -L1-hydroxyl, amino, amido, nitro, halo, haloalkyl, haloalkoxy, cyano, sulfinyl, sulfonyl, sulfonamide, hydroxyl, alkoxy, urea, carbamate, acyl, and carboxyl, wherein each (R2) group has 1, 2, or 3 independently chosen optional substituents or two (R2) groups can be taken together to form a heterocyclyl or aryl group having 1, 2, or 3 independently chosen optional substituents, wherein said optional substituents are independently chosen from alkyl, alkanoyl, heteroalkyl, heterocyclyl, haloalkyl, cycloalkyl, carbocyclyl, arylalkoxy, heterocyclylalkoxy, aryl, aryloxy, heterocyclyloxy, alkoxy, haloalkoxy, oxo, acyloxy, carbonyl, carboxyl, carboxamido, cyano, halogen, hydroxyl, amino, aminoalkyl, amidoalkyl, amido, nitro, thiol, alkylthio, arylthio, sulfonamide, sulfinyl, sulfonyl, urea, and carbamate; R3 is —H or a (C1-C6)alkyl group; each L1 is independently alkylene or heteroalkylene; and n is 0, 1, 2, 3, 4 or 5;with the proviso that the compound of Formula (I) is not: (1S,2R)-2-([1,1′-biphenyl]-4-yl)cyclopropanamine, (1S,2R)-2-(4′-chloro-[1,1′-biphenyl]-4-yl)cyclopropanamine, (1S,2R)-2-(3-chloro-4′-(trifluoromethyl)-[1,1′-biphenyl]-4-yl)cyclopropanamine, 2-(3,4′,5-trichloro-[1,1′-biphenyl]-4-yl)cyclopropanamine, 2-(3,3′,4′,5-tetrachloro-[1,1′-biphenyl]-4-yl)cyclopropanamine, 2-(3,3′,4′-trichloro-[1,1′-biphenyl]-4-yl)cyclopropanamine, or 2-(3,5-dichloro-4′-methyl-[1,1′-biphenyl]-4-yl)cyclopropanamine.
地址 Barcelona ES