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28 条记录 (耗时 0.034 秒)

    Tranylcypromine derivatives as inhibitors of histone demethylases LSD1 and/or LSD2
    16.
    发明授权
    Tranylcypromine derivatives as inhibitors of histone demethylases LSD1 and/or LSD2 有权
    作为组蛋白脱甲基酶LSD1和/或LSD2的抑制剂的苯丙氨酸衍生物

    公开(公告)号：US08765820B2

    公开(公告)日：2014-07-01

    申请号：US13641715

    申请日：2011-04-15

    申请人： Saverio Minucci ,  Antonello Mai ,  Andrea Mattevi

    发明人： Saverio Minucci ,  Antonello Mai ,  Andrea Mattevi

    IPC分类号： A61K31/015 ,  C07C329/00

    CPC分类号： C07C271/26 ,  C07C233/44 ,  C07C233/80 ,  C07C259/06 ,  C07C271/22 ,  C07C271/28 ,  C07C275/24 ,  C07C2601/02 ,  C07C2601/14 ,  C07D333/60

    摘要： Tranylcypromine derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of histone demethylases LSD1 and LSD2, such as the diseases characterized by deregulation of gene transcription, cell differentiation and proliferation, e.g. tumors, viral infections, are herein described. These compounds belong to the structural formula (I) wherein A and R3 are as defined in the specification. The invention also relates to the preparation of these compounds, as well as to compositions containing them and to therapeutic use thereof.

    摘要翻译： 可用作治疗剂的特兰基嘧啶衍生物，特别是用于预防和/或治疗与组蛋白脱甲基酶LSD1和LSD2的活性相关的疾病和病症，例如以基因转录，细胞分化和增殖为特征的疾病，例如， 肿瘤，病毒感染。 这些化合物属于结构式（I），其中A和R3如说明书中所定义。 本发明还涉及这些化合物的制备，以及含有它们的组合物及其治疗用途。

    Phenyl substituted maleimides as medicaments for blocking degenerative tissue damages by inhibiting MPT
    18.
    发明授权
    Phenyl substituted maleimides as medicaments for blocking degenerative tissue damages by inhibiting MPT 有权
    苯基取代的马来酰亚胺作为通过抑制MPT阻断退行性组织损伤的药物

    公开(公告)号：US07915304B2

    公开(公告)日：2011-03-29

    申请号：US12444407

    申请日：2007-09-21

    申请人： PierGiuseppe Pellicci ,  Marco Giorgio ,  Saverio Minucci ,  Paolo Bernardi ,  Gilles Pain ,  Stephen Martin Courtney ,  Christopher John Yarnold ,  Joachim Kraemer

    发明人： PierGiuseppe Pellicci ,  Marco Giorgio ,  Saverio Minucci ,  Paolo Bernardi ,  Gilles Pain ,  Stephen Martin Courtney ,  Christopher John Yarnold ,  Joachim Kraemer

    IPC分类号： A01N43/36 ,  A61K31/40

    CPC分类号： A61K31/4025 ,  C07D207/444 ,  C07D207/448 ,  C07D207/452 ,  Y10S514/866

    摘要： The invention discloses the use of a compound of formula (I), wherein R1, R2, R3, and R4 each independently represents: hydrogen; halo; hydroxy; (C1-C6) alkyl optionally substituted by hydroxy or (C1-C4) alkoxy; (C1-C6) haloalkyl; (C1-C6) alkoxy; and (C1-C6) haloalkoxy; for the preparation of a medicament for the prevention and/or treatment of diseases resulting from opening of the MPTP which are characterized by degenerative tissue damages, in particular, diabetes and diabetic complications, neurological diseases and stroke, heart infarction, inherited dystrophies and hepatitis, more particularly, diabetic vascular diseases, such as diabetic retinopathy, and neurodegenerative disorders, such as multiple sclerosis. Further objects are a group of selected individual compounds of formula (I) for use as medicaments and a further group of selected individual compounds of formula (I) as novel compounds.

    摘要翻译： 本发明公开了式（I）化合物的用途，其中R 1，R 2，R 3和R 4各自独立地表示：氢; 光环; 羟基; 任选被羟基或（C 1 -C 4）烷氧基取代的（C 1 -C 6）烷基; （C 1 -C 6）卤代烷基; （C 1 -C 6）烷氧基; 和（C 1 -C 6）卤代烷氧基; 用于制备用于预防和/或治疗MPTP开放引起的疾病的药物，其特征在于退行性组织损伤，特别是糖尿病和糖尿病并发症，神经系统疾病和中风，心脏梗死，遗传性营养不良和肝炎， 更具体地，糖尿病性血管疾病，例如糖尿病性视网膜病变，和神经变性疾病如多发性硬化。 另外的目的是用作药物的一组选定的式（I）化合物和另一组选择的式（I）化合物作为新化合物。