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    Heterocyclic compounds and their use as medicines
    11.
    发明授权
    Heterocyclic compounds and their use as medicines 失效
    杂环化合物及其作为药物的用途

    公开(公告)号：US06747024B1

    公开(公告)日：2004-06-08

    申请号：US10111994

    申请日：2002-04-30

    申请人： Serge Auvin ,  Pierre-Etienne Chabrier de Lassauniere

    发明人： Serge Auvin ,  Pierre-Etienne Chabrier de Lassauniere

    IPC分类号： C07D40712

    CPC分类号： C07D407/12 ,  C07D263/24 ,  C07D307/24 ,  C07D405/12 ,  C07D413/12

    摘要： The present invention relates to new heterocyclic derivatives having an inhibitory activity on calpains and/or a trapping activity on reactive oxygen species, of formula in which A, X, Y, R1, R2 and Het represent variable groups. The invention also relates to their preparation methods, the pharmaceutical preparations containing them and their use for therapeutic purposes, in particular as inhibitors of calpains and/or traps of reactive oxygen species, selectively or non-selectively.

    摘要翻译： 本发明涉及对A，X，Y，R 1，R 2和Het表示可变基团的甲醛的具有抑制活性氧的抑制活性和/或活性氧捕获活性的新型杂环衍生物。本发明还涉及 其制备方法，含有它们的药物制剂及其用于治疗目的，特别是作为活性氧的钙蛋白酶抑制剂和/或捕获物的选择性或非选择性的抑制剂。

    Novel derivatives of 2-hydroxytetrahydrofuran and their use as medicaments
    13.
    发明申请
    Novel derivatives of 2-hydroxytetrahydrofuran and their use as medicaments 失效
    2-羟基四氢呋喃的新型衍生物及其作为药物的用途

    公开(公告)号：US20050222045A1

    公开(公告)日：2005-10-06

    申请号：US11115480

    申请日：2005-04-27

    申请人： Serge Auvin ,  Pierre-Etienne Chabrier De Lassauniere

    发明人： Serge Auvin ,  Pierre-Etienne Chabrier De Lassauniere

    IPC分类号： A61K38/00 ,  C07K5/06 ,  C07K5/065 ,  C07K5/068 ,  C07K5/078 ,  C07K5/097 ,  C07K5/117 ,  A61K38/05 ,  A61K31/538 ,  A61K31/5415 ,  A61K31/55 ,  A61K38/04

    CPC分类号： C07K5/1024 ,  A61K38/00 ,  C07K5/06026 ,  C07K5/06043 ,  C07K5/06052 ,  C07K5/0606 ,  C07K5/06078 ,  C07K5/06086 ,  C07K5/06139 ,  C07K5/06165 ,  C07K5/0821

    摘要： The invention relates to derivatives of 2-hydroxytetrahydrofuran corresponding to general formula (I) in which A represents the radical, in which R1, R2, R4, R5 and R6 represent (in particular), independently, H, a halogen atom, OH, alkyl or alkoxy, R3 represents H, alkyl or —COR10, R10 representing H, alkyl or alkoxy, and W represents a bond, —CH2—CH2—, —CH═CH—, —O—, —S— or —NR11— in which R11 represents H or alkyl; X represents —CO—, —Y—CO—, —O—Y—CO— or —NR12—Y—CO—, Y represents an alkylene or haloalkylene alkyl, R12 represents H, alkyl or —COR13, R13 represents H, alkyl, haloalkyl or alkoxy, AA represents, each time that it occurs, a natural or non-natural amino acid; n represents 2 or 3; and finally R represents H, alkyl or —CO—R19, R19 representing alkyl. These compounds have a calpain inhibiting activity and/or an activity which traps the reactive oxygen species and can be used for preparing a medicament intended to treat the inflammatory and immunological diseases, cardio-vascular and cerebro-vascular diseases, disorders of the central or peripheral nervous system, cachexia, osteoporosis, muscular dystrophy, proliferative diseases, cataract, rejection reactions following organ transplants and autoimmune and viral diseases.

    摘要翻译： 本发明涉及对应于通式（I）的2-羟基四氢呋喃的衍生物，其中A表示基团，其中R 1，R 2，R 4， R 5和R 6独立地表示H，卤素原子，OH，烷基或烷氧基，R 3， 代表H，烷基或-COR 10，R 10表示H，烷基或烷氧基，W表示键，-CH 2 -CH 2 - ， - CH-，-O-，-S-或-NR 11 - ，其中R 11表示 H或烷基; X表示-CO-，-Y-CO-，-OY-CO-或-NR 12 -Y-CO-，Y表示亚烷基或卤代亚烷基烷基，R 12 >表示H，烷基或-COR 13，R 13表示H，烷基，卤代烷基或烷氧基，AA表示每次发生时，天然或非天然 氨基酸; n表示2或3; 最后R代表烷基，烷基或-CO-R 19，R 19代表烷基。 这些化合物具有钙蛋白酶抑制活性和/或捕获活性氧的活性，并且可用于制备旨在治疗炎症和免疫疾病，心血管和脑血管疾病，中枢或外周疾病的药物 神经系统，恶病质，骨质疏松症，肌营养不良，增殖性疾病，白内障，器官移植后的排斥反应以及自身免疫性和病毒性疾病。