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    Ｎ-아실-Ｎ'-벤질-알킬렌디아미노 유도체
    6.
    发明公开
    Ｎ-아실-Ｎ'-벤질-알킬렌디아미노 유도체 无效
    N-乙酰基-N'-苄基-L-鸟氨酸衍生物

    公开(公告)号：KR1020060111523A

    公开(公告)日：2006-10-27

    申请号：KR1020067010037

    申请日：2004-11-12

    申请人： 뉴론 파마슈티칼즈 에스. 피. 에이.

    发明人： 탈레르플로리안 ,  사비도다비드시벨레마리아 ,  파라벨리라우라 ,  가글리아르디스테파니아 ,  콜롬보엘레나 ,  살바티파트리시아

    IPC分类号： C07C233/36 ,  C07D207/27 ,  C07D207/267

    CPC分类号： C07D207/27 ,  C07C233/36

    摘要： This invention is related to compounds and use of N-Acyl-N'-benzyl-alkylendiamino derivatives of the following general formula (I), wherein A is a straight or branched C 2-C8 alkyl chain; X is a methylene, oxygen, sulphur or a NR7 group; R1is a straight or branched C1-C8 alkyl or C3-C8 alkenylene or C3-C8alkynylene chain, optionally substituted with CF3, phenyl, phenoxy or naphthyl, the aromatic rings optionally substituted by one or more C1-C4 alkyl, halogens, trifluoromethyl, hydroxy or C1-C4 alkoxy groups; R2, R3 are independently hydrogen, a C1 -C3 alkyl chain, halogen, trifluoromethyl, hydroxy or C1 -C4 alkoxy groups; R4, R5 are independently hydrogen or C1-C6alkyl; R6 is a hydrogen or a straight or branched C1-C8 alkyl or linked to R 5 can form a five to seven membered lactam; R7is hydrogen or C1-C6 alkyl; and the pharmaceutically acceptable salts thereof that are active as sodium and/or calcium channel modulators and therefore useful in preventing, alleviating and curing a wide range of pathologies, including, but not limited to, neurological, psychiatric, cardiovascular, inflammatory, ophthalmic, urologic, metabolic and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role.

    摘要翻译： 本发明涉及以下通式（I）的N-酰基-N'-苄基 - 烷基二氨基衍生物的化合物和用途，其中A是直链或支链C 2 -C 8烷基链; X是亚甲基，氧，硫或NR 7基团; R1是任选被CF 3，苯基，苯氧基或萘基取代的直链或支链C 1 -C 8烷基或C 3 -C 8亚链烯基或C 3 -C 8亚炔基链，芳环任选被一个或多个C 1 -C 4烷基，卤素，三氟甲基，羟基 或C 1 -C 4烷氧基; R2，R3独立地是氢，C1-C3烷基链，卤素，三氟甲基，羟基或C1-C4烷氧基; R4，R5独立地是氢或C1-C6烷基; R 6是氢或直链或支链C 1 -C 8烷基或与R 5连接可以形成5至7元的内酰胺; R7是氢或C1-C6烷基; 其作为钠和/或钙通道调节剂具有活性的药学上可接受的盐，因此可用于预防，减轻和治愈广泛范围的病症，包括但不限于神经，精神，心血管，炎症，眼科，泌尿系统 ，代谢和胃肠道疾病，其中上述机制被描述为发挥病理作用。

    옥시라세탐의 제조방법
    9.
    发明公开
    옥시라세탐의 제조방법 失效
    OXIRACETAM的制备方法

    公开(公告)号：KR1020030083466A

    公开(公告)日：2003-10-30

    申请号：KR1020020022150

    申请日：2002-04-23

    申请人： 주식회사 바이넥스 ,  이백천

    发明人： 박민수 ,  강재선 ,  안병근 ,  김원석 ,  박유수 ,  손철훈

    IPC分类号： C07D207/27

    摘要： PURPOSE: A manufacturing method of oxiracetam is provided, thereby manufacturing oxiracetam at room temperature under mild condition in higher yield. CONSTITUTION: A manufacturing method of oxiracetam comprises the steps of: condensation of vinyl acetyl chloride of the formula 1 with glycine ethyl ester to prepare 3-butenoylamino-acetic ethyl ester of the formula 2: epoxylation of 3-butenoylamino-acetic ethyl ester of the formula 2 using HO-X in which X is halogen or CH2Cl2 to prepare an epoxy compound of the formula 3 as an intermediate; adding a base to the epoxy compound of the formula 3 for cyclization of the epoxy compound to form 5-membered ring of the formula 4; and dissolving the 5-membered ring of the formula 4 in ammonia water to prepare oxiracetam of the formula 5.

    摘要翻译： 目的：提供奥拉西坦的制造方法，由此在温和条件下以较高的产率在室温下制造奥拉西坦。 构成：奥拉西坦的制备方法包括以下步骤：将式1的乙烯基乙酰氯与甘氨酸乙酯的缩合制备式2的3-丁烯酰氨基 - 乙酸乙酯：3-丁烯酰氨基 - 乙酸乙酯的环氧化 式2使用其中X为卤素或CH 2 Cl 2的HO-X，以制备作为中间体的式3的环氧化合物; 向式3的环氧化合物加入碱，使环氧化合物环化形成式4的5元环; 并将式4的5元环溶解在氨水中以制备式5的奥拉西坦。