发明名称 LYSINE SPECIFIC DEMETHYLASE-1 INHIBITORS AND THEIR USE
摘要 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.
申请公布号 EP2560947(A1) 申请公布日期 2013.02.27
申请号 EP20110723284 申请日期 2011.04.19
申请人 ORYZON GENOMICS, S.A. 发明人 ORTEGA MUNOZ, ALBERTO;CASTRO-PALOMINO LARIA, JULIO;FYFE, MATTHEW COLIN THOR
分类号 C07C211/35;A61K31/135;A61K31/16;A61P31/12;A61P35/04;C07C211/42;C07C217/52;C07C237/24 主分类号 C07C211/35
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