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    LYSINE SPECIFIC DEMETHYLASE-1 INHIBITORS AND THEIR USE
    31.
    发明申请
    LYSINE SPECIFIC DEMETHYLASE-1 INHIBITORS AND THEIR USE 有权

    公开(公告)号：US20120283266A1

    公开(公告)日：2012-11-08

    申请号：US13497994

    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: A61K31/135 ,  A61K31/495 ,  C07C211/36 ,  A61P35/00 ,  A61K31/40 ,  C07D211/26 ,  A61K31/445 ,  C07C323/29 ,  C07D241/04 ,  C07D207/14

    CPC classification number: C07D241/04 ,  A61K31/075 ,  A61K31/095 ,  A61K31/40 ,  A61K31/495 ,  A61K45/06 ,  C07C211/40 ,  C07C217/08 ,  C07C217/74 ,  C07C323/25 ,  C07C2601/02 ,  C07D207/14 ,  C07D211/14 ,  A61K2300/00

    Abstract: The invention relates to a compound of Formula (I): (A′)x-(A)-(B)-(Z)-(L)-(D), 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, aryl, arylalkoxy, alkyl, alkoxy, cyano, sulfonyl, amido, 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 —CH2CH2—, —CH2CH2CH2—, and —CH2CH2CH2CH2—; and (D) is chosen from —N(—R1)—R2, —O—R3, and —S—R3, wherein: R1 and R2 are mutually linked to form a heterocyclic ring together with the nitrogen atom that R1 and R2 are attached to, wherein said heterocyclic ring has 0, 1, 2, or 3 substituents independently chosen from —NH2, —NH(C1-C6 alkyl), —N(C1-C6 alkyl)(C1-C6 alkyl), alkyl, halo, cyano, alkoxy, haloalkyl, and haloalkoxy, or R1 and R2 are independently chosen from —H, alkyl, cycloalkyl, haloalkyl, and heterocyclyl, wherein the sum of substituents on R1 and R2 together is 0, 1, 2, or 3, and the substituents are independently chosen from —NH2, —NH(C1-C6 alkyl), —N(C1-C6 alkyl)(C1-C6 alkyl), and fluoro; and R3 is chosen from —H, alkyl, cycloalkyl, haloalkyl, and heterocyclyl, wherein R3 has 0, 1, 2, or 3 substituents independently chosen from —NH2, —NH(C1-C6 alkyl), —N(C1-C6 alkyl)(C1-C6 alkyl), and fluoro; or an enantiomer, diastereomer, or mixture thereof, or a pharmaceutically acceptable salt or solvate thereof. The compounds of the invention show inhibitory LSD1 activity, which makes them useful in the treatment or prevention of diseases such as cancer.

    Lysine specific demethylase-1 inhibitors and their use
    39.
    发明授权
    Lysine specific demethylase-1 inhibitors and their use 有权
    赖氨酸特异性脱甲基酶-1抑制剂及其用途

    公开(公告)号：US08722743B2

    公开(公告)日：2014-05-13

    申请号：US13641916

    申请日：2011-04-19

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

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

    IPC: A61K31/165 ,  C07C211/00

    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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