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    LYSINE DEMETHYLASE INHIBITORS FOR DISEASES AND DISORDERS ASSOCIATED WITH HEPADNAVIRIDAE
    41.
    发明申请
    LYSINE DEMETHYLASE INHIBITORS FOR DISEASES AND DISORDERS ASSOCIATED WITH HEPADNAVIRIDAE 有权
    与HEPADNAVIRIDAE相关的疾病和疾病的LYSINE DEMETHYLASE抑制剂

    公开(公告)号：US20130095067A1

    公开(公告)日：2013-04-18

    申请号：US13580710

    申请日：2011-02-24

    Applicant: Jonathan Alleman Baker ,  Matthew Colin Thor Fyfe

    Inventor： Jonathan Alleman Baker ,  Matthew Colin Thor Fyfe

    IPC: A61K31/135 ,  A61K38/21 ,  A61K31/137 ,  A61K31/131 ,  A61K31/165 ,  A61K45/06

    CPC classification number: A61K31/135 ,  A61K31/131 ,  A61K31/137 ,  A61K31/15 ,  A61K31/165 ,  A61K38/21 ,  A61K45/06 ,  A61K2300/00

    Abstract: The present invention provides for the treatment or prevention of Hepadnaviridae infection and disease caused by Hepadnaviridae infection. In particular, the invention provides compositions and methods that affect the ability of Hepadnaviridae to utilize the host's cellular machinery as part of the virus' lifecycle. The invention relates to the discovery that interfering with the normal ability of viruses to utilize the host cell machinery with LSD1 inhibitors reduces HBV replication. Thus, the treatment and prevention of Hepadnaviridae infection and disease caused by Hepadnaviridae according to the invention comprises administering to an individual in need of treatment, a therapeutically effective amount of a LSD1 inhibitor. The individual in need of treatment can be a human or, e.g., another mammal.

    Abstract translation: 本发明提供治疗或预防肝炎病毒科感染和由肝炎病毒科感染引起的疾病。 特别地，本发明提供影响Hepadnaviridae利用宿主细胞机制作为病毒生命周期的一部分的能力的组合物和方法。 本发明涉及干扰病毒利用宿主细胞机制与LSD1抑制剂的正常能力的发现降低HBV复制。 因此，根据本发明的肝炎病毒科感染和肝炎病毒科引起的疾病的治疗和预防包括向需要治疗的个体施用治疗有效量的LSD1抑制剂。 需要治疗的个体可以是人或例如另一种哺乳动物。

    Substituted heteroaryl- and aryl-cyclopropylamine acetamides and their use
    50.
    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。

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