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    Novel derivatives of 2-hydroxytetrahydrofuran and their use as medicaments
    53.
    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。

    Dermopharmaceutically and cosmetically active oligopeptides
    54.
    发明申请
    Dermopharmaceutically and cosmetically active oligopeptides 有权
    药物和化妆品活性寡肽

    公开(公告)号：US20050065090A1

    公开(公告)日：2005-03-24

    申请号：US10493856

    申请日：2002-10-30

    申请人： Christian Ludin ,  Marc Heidl ,  Hugo Ziegler

    发明人： Christian Ludin ,  Marc Heidl ,  Hugo Ziegler

    IPC分类号： A61K38/00 ,  A61P17/00 ,  C07K5/068 ,  C07K14/78 ,  A61K38/08 ,  C07K7/06

    CPC分类号： C07K14/78 ,  A61K38/00 ,  C07K5/06086

    摘要： Oligopeptides and derivatives thereof, peptide analogs and derivatives thereof as well as pharmaceutically acceptable salts of these compounds, which correspond to general formula (I) wherein R1 represents H, —C(O)—R7, —SO2—R7, —C(O)—OR7 or —C(O)—N(R7)2 R2 represents, independent of one another, H or —(C1-C4)-alkyl, R3 and R6 represent, independent of one another, —(CH2)q—N(R1)R8 R4 and R5 represent, independent of one another, —CH2—OR2, —CH(CH3)OR8 or —CH2—CH2—OR8 R7 represents hydrogen, optionally substituted (C1-C19)-alkyl; optionally substituted (C1-C19)-alkenyl; phenyl-(C1-C4)-alkyl whose phenyl radical is optionally substituted with amino in the para position R8 represents H, —(C1-C4)-alkyl, —C(O)—R7, —C(O)—OR7, —C(O)—N(R7)2 or —SO2—R7 X represents oxygen (—O—) or —NH—; or XR7, with X=O, also represents the esters of α-tocopherol, tocotrienol or retinol or the carboxylic acid (with R7=H) m, n, p represent, independent of one another, zero or 1 and q in R3 and R6 represent, independent of one another, an integer from 1 to 4, with the provision that the following conditions do not simultaneously occur: R4=—CH(CH3)—OH and R5=—CH(CH3)—OH and R6=—(CH2)4—NH2; dermopharmaceutically and/or cosmetically active compositions containing at least one compound of formula (I).

    摘要翻译： 对应于通式（I）的寡肽及其衍生物，肽类似物及其衍生物以及这些化合物的药学上可接受的盐，其中R 1表示H，-C（O）-R 7，-SO 2 - R 7，-C（O）-OR 7或-C（O）-N（R 7）2 R 2彼此独立地表示H或 - （C 1 -C 4） - 烷基，R 3和R 6彼此独立地表示 - （CH 2）q N（R 1）R 8 R 4和R 5彼此独立地表示 - CH2-OR2，-CH（CH3）OR8或-CH2-CH2-OR8表示氢，任选取代的（C 1 -C 19） - 烷基; 任选取代的（C 1 -C 19） - 烯基; 苯基 - （C 1 -C 4） - 烷基，其苯基任选被对位R 8中的氨基取代，代表H， - （C 1 -C 4） - 烷基，-C（O）-R 7，-C （O）-OR 7，-C（O）-N（R 7）2或-SO 2 -R 7表示氧（-O-）或-NH-; 或XR 7，X = O也表示α-生育酚，生育三烯酚或视黄醇或羧酸（R 7 = H）m，n，p彼此独立地为0或 1和q在R 3和R 6中彼此独立地表示1至4的整数，条件是不同时发生以下条件：R 4 = -CH（CH 3） - OH和R 5 = -CH（CH 3）-OH，R 6 = - （CH 2）4 -NH 2; 含有至少一种药物的药物和/或化妆品活性组合物