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    카바페넴 항생물질의 중간체 및 그의 제조방법
    61.
    发明公开
    카바페넴 항생물질의 중간체 및 그의 제조방법 失效
    卡巴因抗生素的中间体及其制备方法

    公开(公告)号：KR1020020013988A

    公开(公告)日：2002-02-25

    申请号：KR1020000046447

    申请日：2000-08-10

    Applicant: 동화약품주식회사 ,  한국화학연구원

    Inventor： 이철해 ,  김봉진 ,  정원장 ,  김재학 ,  정희정 ,  김은정 ,  송신섭 ,  정용호 ,  곽현정 ,  이진수 ,  편도규

    IPC: C07D413/14

    CPC classification number: C07D413/06 ,  C07D205/08 ,  C07D265/06 ,  C07D265/14 ,  C07D487/04 ,  C07F9/65611 ,  Y02P20/55

    Abstract: PURPOSE: Provided is an intermediate, azetidinone compound which is useful in manufacturing beta-methylcarbapenem antibiotics. And its manufacturing method is provided. CONSTITUTION: The intermediate of carbapenem, azetidinone compound, is represented by the formula(1), wherein R is hydrogen or hydroxy protective group, R1 and R2 are individually C1-C15 alkyl, benzyl, represent 5-6 membered cyclic compound to which R1 and R2 are linked, or hetero cyclic group including at least one oxygen or sulfur atom; R3 is lower alkyl group or lower alkylester group; and R4 is benzene, halogen, lower alkyloxy group, or nitro group substituted benzene ring.

    Abstract translation: 目的：提供可用于制备β-甲基碳青霉烯类抗生素的中间体氮杂环丁酮化合物。 并提供其制造方法。 构成：碳青霉烯类氮杂环丁酮化合物的中间体由式（1）表示，其中R是氢或羟基保护基，R1和R2分别是C1-C15烷基，苄基，代表5-6元环状化合物，其中R1 或R 2连接，或包含至少一个氧原子或硫原子的杂环基; R3是低级烷基或低级烷基酯基; R4为苯，卤素，低级烷氧基或硝基取代苯环。

    광학활성을 유발하는 7-피롤리딘 치환체를 갖는광학활성의 퀴놀린 카르복실산 유도체 및 그의 제조방법
    62.
    发明公开
    광학활성을 유발하는 7-피롤리딘 치환체를 갖는광학활성의 퀴놀린 카르복실산 유도체 및 그의 제조방법 无效
    具有诱导光学活性的7-吡咯烷酮取代基的光学活性喹啉羧酸衍生物及其制备方法

    公开(公告)号：KR1020010029698A

    公开(公告)日：2001-04-06

    申请号：KR1020000024657

    申请日：2000-05-09

    Applicant: 동화약품주식회사

    Inventor： 윤성준 ,  정용호 ,  이치우 ,  이진수 ,  김남두 ,  진윤호 ,  송완진 ,  김익회 ,  양왕용 ,  최동락 ,  신정한

    IPC: C07D403/04

    Abstract: PURPOSE: Provided is a method for manufacturing 4-aminomethyl-4-methyl-3-(Z)-alkoxyamino derivative which has antibacterial effects on both gram positive and negative bacteria so that the derivative is useful for medical purposes. And Its pharmaceutically acceptable salt and its solvate are also provided. CONSTITUTION: A method for producing 4-aminomethyl-4-methyl-3-(Z)-alkoxyamino derivative comprises the following steps of: i) reacting the compound of the formula (3) with ketal compound of the formula (2a) in the presence of acid receptor, for 1-24 hours at 0-150 deg.C, preferably from room temperature to 90 deg.C, to manufacture optically active quinoline carboxylic acid derivative of the formula (4); ii) deketalizing the quinoline carboxylic acid derivative to manufacture pyrrolidinone of the formula (5) at from room temperature to 100 deg.C; and iii) reacting the pyrrolidinone with alkoxylamine in the presence of base at 0-90 deg.C. In the formula (1), Q is C-H, C-F, C-CL, or N. Y is H or NH2. R is a C1-C4 linear or branched alkyl, aryl, or benzyl group. * is an optically pure asymmetric carbon.

    Abstract translation: 目的：提供对革兰氏阳性细菌和阴性细菌都具有抗菌作用的4-氨基甲基-4-甲基-3-（Z） - 烷氧基氨基衍生物的制备方法，因此该衍生物可用于医疗目的。 还提供其药学上可接受的盐及其溶剂合物。 构成：4-氨基甲基-4-甲基-3-（Z） - 烷氧基氨基衍生物的制备方法包括以下步骤：i）使式（3）的化合物与式（2a）的缩酮化合物反应于 存在酸受体，在0-150℃，优选室温至90℃下进行1-24小时，以制备式（4）的光学活性喹啉羧酸衍生物; ii）将喹啉羧酸衍生物缩酮化，制备式（5）的吡咯烷酮，室温至100℃; 和iii）在0-90℃下，在碱的存在下使吡咯烷酮与烷氧基胺反应。 在式（1）中，Q是C-H，C-F，C-CL或N.Y是H或NH 2。 R是C1-C4直链或支链烷基，芳基或苄基。 *是光学纯的不对称碳。

    골 대사 이상에서 기인하는 질환의 예방제 또는 치료제
    68.
    发明公开
    골 대사 이상에서 기인하는 질환의 예방제 또는 치료제 无效
    与异常骨代谢有关的疾病预防或治疗药物

    公开(公告)号：KR1020110120277A

    公开(公告)日：2011-11-03

    申请号：KR1020117017757

    申请日：2010-01-29

    Applicant: 데이진 화-마 가부시키가이샤 ,  동화약품주식회사

    Inventor： 오치아이에이지 ,  나카야마야스노리 ,  이진수 ,  황윤하 ,  정덕균

    IPC: A61K31/593 ,  A61K31/426 ,  A61P1/02 ,  A61P3/14

    CPC classification number: A61K31/426 ,  A61K31/593

    Abstract: PURPOSE: An agent for preventing or treating diseases caused by bone metabolic abnormality using N-hydroxybenzamidine derivatives or salt thereof is provided. CONSTITUTION: An agent for preventing or treating diseases caused by bone metabolic abnormality contains N-hydroxybenzamidine derivatives of formula I or salt thereof; and active vitamin D or prodrug thereof as an active ingredient. The N-hydroxybenzamidine derivative of formula I is N-hydroxy-4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazole-4-yl)phenoxy]pentoxy}benzamidine.

    Abstract translation: 目的：提供使用N-羟基苄脒衍生物或其盐预防或治疗由骨代谢异常引起的疾病的药剂。 构成：用于预防或治疗由骨代谢异常引起的疾病的药剂含有式I的N-羟基苄脒衍生物或其盐; 和活性维生素D或其前药作为活性成分。 式I的N-羟基苄脒衍生物是N-羟基-4- {5- [4-（5-异丙基-2-甲基-1,3-噻唑-4-基）苯氧基]戊氧基}苄脒。

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