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    Substituted heteroaryl- and aryl-cyclopropylamine acetamides and their use
    28.
    发明授权
    Substituted heteroaryl- and aryl-cyclopropylamine acetamides and their use 有权
    取代的杂芳基 - 和芳基 - 环丙胺乙酰胺及其用途

    公开(公告)号：US08946296B2

    公开(公告)日：2015-02-03

    申请号：US13500687

    申请日：2010-04-19

    Applicant: Alberto Ortega Muñoz ,  Julio Castro-Palomino Laria ,  Matthew Colin Thor Fyfe

    Inventor： Alberto Ortega Muñoz ,  Julio Castro-Palomino Laria ,  Matthew Colin Thor Fyfe

    IPC: A61K31/165 ,  C07C237/20 ,  C07C237/06 ,  C07C255/54 ,  C07D213/36

    CPC classification number: C07C237/06 ,  C07C255/54 ,  C07C2601/02 ,  C07D213/36

    Abstract: The invention relates to compounds of Formula (I): (A′)x-(A)-(B)—(Z)-(L)-C(═O)NH2 or pharmaceutically acceptable salts or solvates thereof, wherein: (A) is heteroaryl or aryl; each (A′), if present, is indepedently 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, aryl, arylalkoxy, alkyl, alkoxy, cyano, sulfonyl, sulfinyl, and carboxamide; 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—; and (L) is —(CH2)mCR1,R2—, wherein m is 0, 1, 2, 3, 4, 5, or 6, and wherein R1 and R2 are each independently hydrogen or C1-C6 alkyl; provided that, if (L) is —CH2— or —CH(CH3)—, then X is not 0. The compounds of the invention are useful in the treatment of diseases such as cancer and neurodegenerative diseases.

    Abstract translation: 本发明涉及式（I）化合物：（A'）x-（A） - （B） - （Z） - （L）-C（= O）NH 2或其药学上可接受的盐或溶剂合物，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'）被0,1,2 或3个独立地选自卤素，卤代烷基，芳基，芳基烷氧基，烷基，烷氧基，氰基，磺酰基，亚磺酰基和羧酰胺的取代基; X为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）为-NH-; 和（L）是 - （CH 2）m CR 1，R 2 - ，其中m是0,1,2,3,4,5或6，并且其中R 1和R 2各自独立地是氢或C 1 -C 6烷基; 条件是，如果（L）是-CH 2 - 或-CH（CH 3） - ，则X不为0.本发明的化合物可用于治疗疾病如癌症和神经变性疾病。

    LYSINE SPECIFIC DEMETHYLASE-1 INHIBITORS AND THEIR USE
    30.
    发明申请
    LYSINE SPECIFIC DEMETHYLASE-1 INHIBITORS AND THEIR USE 有权
    LYSINE SPECIFIC DEMETHYLASE-1 INHIBITORS及其使用

    公开(公告)号：US20130090386A1

    公开(公告)日：2013-04-11

    申请号：US13641916

    申请日：2011-04-19

    Applicant: Alberto Ortega Munoz ,  Juio Castro-Palomino Laria ,  Matthew Colin Thor Fyfe

    Inventor： Alberto Ortega Munoz ,  Juio Castro-Palomino Laria ,  Matthew Colin Thor Fyfe

    IPC: A61K31/135 ,  C07C211/42 ,  A61K45/06 ,  C07C237/24 ,  A61K31/165 ,  C07C217/74 ,  C07C211/40

    CPC classification number: C07C217/74 ,  A61K31/135 ,  A61K31/165 ,  A61K45/06 ,  A61N5/10 ,  C07C211/35 ,  C07C211/40 ,  C07C211/42 ,  C07C217/52 ,  C07C237/24 ,  C07C2101/02 ,  C07C2101/14 ,  C07C2101/18 ,  C07C2102/08 ,  C07C2102/10 ,  C07C2601/02 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2602/08 ,  C07C2602/10

    Abstract: 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.

    Abstract translation: 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'）被0,1,2 ，或3个独立地选自卤素，卤代烷基，卤代烷氧基，芳基，芳基烷氧基，烷基，烷氧基，酰氨基，-CH 2 C（= O）NH 2，杂芳基，氰基，磺酰基和亚磺酰基的取代基。 X为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）为-NH-; （L）选自单键-CH 2 - ， - CH 2 CH 2 - ， - CH 2 CH 2 CH 2 - 和-CH 2 CH 2 CH 2 CH 2 - ; - 和（D）是脂族碳环基或苯并环烷基，其中所述脂族碳环基或所述苯并环烷基具有0,1,2或3个独立地选自-NH 2，-NH（C 1 -C 6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）本发明化合物显示出抑制LSD1的活性，使其可用于治疗或预防 疾病如癌症。

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