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28 条记录 (耗时 0.039 秒)

    Spirocyclic derivatives as histone deacetylase inhibitors
    14.
    发明授权
    Spirocyclic derivatives as histone deacetylase inhibitors 有权
    螺环衍生物作为组蛋白脱乙酰酶抑制剂

    公开(公告)号：US08592444B2

    公开(公告)日：2013-11-26

    申请号：US12988197

    申请日：2009-04-14

    申请人： Mario Varasi ,  Florian Thaler ,  Agnese Abate ,  Giacomo Carenzi ,  Ciro Mercurio ,  Saverio Minucci

    发明人： Mario Varasi ,  Florian Thaler ,  Agnese Abate ,  Giacomo Carenzi ,  Ciro Mercurio ,  Saverio Minucci

    IPC分类号： C07D401/04 ,  A61K31/438

    CPC分类号： C07D498/10 ,  A61K31/438 ,  C07D471/10 ,  C07D491/107 ,  Y02A50/409 ,  Y02A50/411

    摘要： This invention is related to new histone deacetylase inhibitors according to the general formula (I) wherein: the dotted line is an optional additional bond; n is zero or an integer from 1 to 4; R1 is hydrogen; C1-C6 alkyl, optionally substituted by cycloalkyl, aryl or by heteroaryl; (CO)R3; (SO2)R4; cycloalkyl; aryl; or heteroaryl; R2 is C1-C6 alkyl, optionally substituted by aryl or by heteroaryl; aryl; heteroaryl; or (CO)R5; X is CH2, oxygen or NR6; Y is a bond, CHR7 or NR8; Z is oxygen, CR9R10 or C═R11; and R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as further defined in the specification; and pharmaceutical acceptable salts thereof.

    摘要翻译： 本发明涉及根据通式（I）的新的组蛋白脱乙酰酶抑制剂，其中：虚线是任选的附加键; n为0或1至4的整数; R1是氢; 任选被环烷基，芳基或杂芳基取代的C 1 -C 6烷基; （CO）R3; （SO2）R4; 环烷基 芳基; 或杂芳基; R2是任选被芳基或杂芳基取代的C 1 -C 6烷基; 芳基; 杂芳基; 或（CO）R5; X是CH 2，氧或NR 6; Y是一个键，CHR7或NR8; Z是氧，CR9R10或C = R11; R3，R4，R5，R6，R7，R8，R9，R10和R11在说明书中进一步定义; 及其药学上可接受的盐。

    Phenyl substituted maleimides as medicaments for blocking degenerative tissue damages by inhibiting MPT
    15.
    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。