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发明公开
CN102947265A 赖氨酸特异性脱甲基酶-1抑制剂及其应用 有权

赖氨酸特异性脱甲基酶-1抑制剂及其应用
摘要：
本发明涉及式1的化合物，其中：(A)是杂芳基或芳基；每个(A’)，如果存在的话，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、卤代烷氧基和氰基，其中每个(A’)利用0、1、2或3个独立地选自下述的取代基取代：卤素、卤代烷基、卤代烷氧基、芳基、芳基烷氧基、烷基、烷氧基、酰氨基、-CH2C(=O)NH2、杂芳基、氰基、磺酰基和亚磺酰基；X是0、1、2或3；(B)是环丙基环，其中(A)和(Z)与(B)的不同碳原子共价结合；(Z)是-NH-；(L)选自单键、-CH2-、-CH2CH2-、-CH2CH2CH2-和-CH2CH2CH2CH2-；并且(D)是脂族碳环基团或者苯并环烷基，其中所述脂族碳环基团或者所述苯并环烷基具有0、1、2或3个独立地选自下述的取代基：-NH2、-NH(C1-C6烷基)、-N(C1-C6烷基)(C1-C6烷基)、烷基、卤素、酰氨基、氰基、烷氧基、卤代烷基和卤代烷氧基。(A’)X-(A)-(B)-(Z)-(L)-(D)式1。本发明的化合物对于抑制LSD1显示活性，这使得可以将它们用于疾病如癌症的治疗或预防。
摘要（英）：

The present invention relates to a compound of Formula 1, wherein: (A) is heteroaryl or aryl; each (?'), if present, is independently chosen from aryl, arylalkoxy, arylalkyl, heterocyclyl, aryloxy, halo, alkoxy, haloalkyl, cycloalkyl, haloalkoxy, and cyano, wherein each (?') 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.

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