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    도네페질 중간체의 제조방법
    11.
    发明公开
    도네페질 중간체의 제조방법 无效
    一种制备多奈哌齐中间体的方法

    公开(公告)号：KR1020080092515A

    公开(公告)日：2008-10-16

    申请号：KR1020070035881

    申请日：2007-04-12

    Applicant: 동화약품주식회사

    Inventor： 오윤석 ,  임재경 ,  권오진 ,  최정욱 ,  신동혁 ,  정진용 ,  유제만

    IPC: C07D211/22 ,  C07D295/02

    CPC classification number: C07D211/32

    Abstract: A process for preparing an intermediate of donepezil having dementia-treating effects is provided to improve preparation yield and convenience of mass production of the intermediate by replacing the base which is difficult to be used industrially. An intermediate of donepezil, 2-[(E)-1-(1-benzyl-4-piperidyl)methylidene]-5,6-dimethoxy-1-indanone represented by the formula(1) is prepared by reacting 1-indanone compound represented by the formula(2) with aldehyde compound represented by the formula(3) by using a base selected from sodium methoxide(MeONa), sodium ethoxide(EtONa), potassium t-butoxide, sodium hydride, sodium hydroxide, potassium hydroxide and sodium amide in a reaction solvent selected from methanol, ethanol, isopropanol, t-butanol, tetrahydrofuran, 1,4-dioxane, diisopropyl ether, dimethylform amide, dimethylsulfoxide and nitromethane.

    Abstract translation: 提供一种制备具有痴呆症治疗效果的多奈哌齐中间体的方法，以通过更换难以在工业上使用的碱来改善中间体的制备产率和方便大量生产。 由式（1）表示的多奈哌齐2 - [（E）-1-（1-苄基-4-哌啶基）亚甲基] -5,6-二甲氧基-1-二氢茚酮的中间体是通过1- 由式（2）表示的醛与式（3）表示的醛化合物通过使用选自甲醇钠（MeONa），乙醇钠（EtONa），叔丁醇钾，氢化钠，氢氧化钠，氢氧化钾和钠 酰胺在选自甲醇，乙醇，异丙醇，叔丁醇，四氢呋喃，1,4-二恶烷，二异丙基醚，二甲基甲酰胺，二甲基亚砜和硝基甲烷的反应溶剂中。

    신규한 이마티닙 캠실레이트 및 그의 제조방법
    12.
    发明授权
    신규한 이마티닙 캠실레이트 및 그의 제조방법 失效
    新型樟脑磺酸钠及其制备方法

    公开(公告)号：KR100799821B1

    公开(公告)日：2008-01-31

    申请号：KR1020070011556

    申请日：2007-02-05

    Applicant: 동화약품주식회사

    Inventor： 오윤석 ,  임재경 ,  신동혁 ,  성승규 ,  이상호 ,  이학수 ,  조은희 ,  유제만

    IPC: C07D401/14

    CPC classification number: C07D401/04

    Abstract: An imatinib camsylate is provided to be more rapidly absorbed and show higher absorption concentration and excellent solubility in water than those of a commercially available imatinib mesylate in the pharmacokinetic aspect. An imatinib camsylate is represented by the formula(1), wherein HX is D-(+)-camphorsulfonic acid, L-(-)-camphorsulfonic acid or D,L-(±)-camphorsulfonic acid. A method for preparing the imatinib camsylate comprises the steps of: (a) dissolving an imatinib represented by the formula(2) in an organic solvent; (b) dissolving one acid represented by the formula(3) or (4), or an acid which is a mixture of the formula(3) and the formula(4) in a ratio of 1:1 in an organic solvent or adding the acid as it is to the reaction solution obtained from the step(a) to prepare a mixture; (c) filtering a solid extracted by agitating the mixture to form an acid addition salt; and (d) after dissolving the acid addition salt in an organic solvent and re-filtering it to extract crystal, purifying the crystal.

    Abstract translation: 提供了一种伊马替尼樟脑磺酸盐以在药代动力学方面比在商业上可获得的甲磺酸伊马替尼的那些更快速地吸收并显示更高的吸收浓度和在水中的优异的溶解性。 伊马替尼樟脑磺酸盐由式（1）表示，其中HX是D - （+） - 樟脑磺酸，L - （ - ） - 樟脑磺酸或D，L-（±） - 樟脑磺酸。 制备伊马替尼樟脑磺酸盐的方法包括以下步骤：（a）将由式（2）表示的伊马替尼溶解在有机溶剂中; （b）在有机溶剂中溶解由式（3）或（4）表示的一种酸或以式（3）和式（4）的混合物形式的酸的比例为1:1，或者将 将酸从原来的步骤（a）获得的反应溶液制备成混合物; （c）过滤通过搅拌混合物提取的固体形成酸加成盐; 和（d）将酸加成盐溶解在有机溶剂中并对其进行再过滤以萃取晶体，纯化晶体。

    방사성물질-키토산 복합체를 함유하는 전립선암 치료용조성물 및 조성물 제조용 키트
    14.
    发明公开
    방사성물질-키토산 복합체를 함유하는 전립선암 치료용조성물 및 조성물 제조용 키트 失效
    用于治疗前列腺癌的组合物和包含放射性自由基 - 替康复合物

    公开(公告)号：KR1020050025933A

    公开(公告)日：2005-03-14

    申请号：KR1020040071693

    申请日：2004-09-08

    Applicant: 한국원자력연구원 ,  동화약품주식회사

    Inventor： 유제만 ,  신동혁 ,  성승규 ,  양희복 ,  배은정 ,  송영준 ,  박경배 ,  신병철

    IPC: A61K51/00 ,  A61K31/722

    CPC classification number: A61K51/06 ,  A61K51/1282

    Abstract: A composition and kit for treatment of prostate cancer comprising the radioisotope-chitosan complex are provided, which radioisotope-chitosan complex is concentrated to a local region administered so as to prevent leakage of radiation, inhibits growth of prostate cancer cells, and minimizes side effects including urinary incontinence, stricture urethra and rectal hematochezia. The composition for treatment of prostate cancer comprises the radioisotope-chitosan complex, wherein the radioisotope emits high energy beta-ray and low energy gamma-ray simulteneously; the radioisotope is selected from 153Sm, 165Dy, 166Ho and 169 Er; and the molecular weight of chitosan is 100,000 to 1,500, 000 dalton. A kit for treatment of prostate cancer comprises a kit A containing 0.5 to 150 mCi of radioisotope and a kit B containing chitosan with molecular weight of 400,000 to 1,300,00 dalton, wherein the chitosan is weak acid chitosan solution; the chitosan solution comprises one or more selected from pH regulating agent, tonicity adjustment agent, preservative and stabilizing agent.

    Abstract translation: 提供了一种用于治疗包括放射性同位素 - 壳聚糖复合物的前列腺癌的组合物和试剂盒，其将放射性同位素 - 壳聚糖复合物浓缩至施用的局部区域，以防止辐射泄漏，抑制前列腺癌细胞的生长，并且最小化副作用，包括 尿失禁，尿道狭窄和直肠血尿。 用于治疗前列腺癌的组合物包括放射性同位素 - 壳聚糖复合物，其中放射性同位素同时发射高能β射线和低能γ射线; 放射性同位素选自153Sm，165Dy，166Ho和169Er; 壳聚糖的分子量为100,000〜1,500,000道尔顿。 用于治疗前列腺癌的试剂盒包含含有0.5至150mCi的放射性同位素的试剂盒A和含有分子量为400,000至1,300,00道尔顿的壳聚糖的试剂盒B，其中壳聚糖是弱酸性壳聚糖溶液; 壳聚糖溶液包含选自pH调节剂，张力调节剂，防腐剂和稳定剂中的一种或多种。

    방사성물질-키토산 복합체를 함유하는 전립선암 치료용조성물 및 조성물 제조용 키트
    18.
    发明授权
    방사성물질-키토산 복합체를 함유하는 전립선암 치료용조성물 및 조성물 제조용 키트 失效
    含有用于治疗前列腺癌的放射性同位素 - 壳聚糖复合物的组合物和试剂盒

    公开(公告)号：KR100700418B1

    公开(公告)日：2007-03-29

    申请号：KR1020040071693

    申请日：2004-09-08

    Applicant: 한국원자력연구원 ,  동화약품주식회사

    Inventor： 유제만 ,  신동혁 ,  성승규 ,  양희복 ,  배은정 ,  송영준 ,  박경배 ,  신병철

    IPC: A61K51/00 ,  A61K31/722

    CPC classification number: A61K51/06 ,  A61K51/1282

    Abstract: 본 발명은 방사성물질-키토산 복합체를 유효성분으로 포함하는 전립선암 치료용 조성물 및 그 조성물 제조용 키트에 관한 것으로서, 보다 상세하게는 베타선을 방출하는 치료용 방사성 물질과 키토산을 포함하는 방사성물질-키토산 복합체를 유효성분으로 포함하는 전립선암 치료용 조성물 및 그 조성물 제조용 키트에 관한 것이다. 전립선 암조직에 직접 투여된 방사성물질-키토산 복합체는 투여 부위내에 집적되어 표적부위 이외로는 방사능이 누출되지 않고, 전립선 암세포의 성장을 탁월하게 억제하며, 기존의 치료법이 갖는 부작용인 요실금, 요도협착, 직장출혈 등을 최소화하고 또한 호르몬요법을 시행할 수 없는 호르몬 비의존성 전립선암에 대해서도 효과적인 치료제로 사용될 수 있다.

    플라보노이드 계열 화합물 또는 이를 포함하는 강진향추출물을 함유한 매트릭스 메탈로프로테이나제 활성저해제 및 기능성 식품
    20.
    发明公开
    플라보노이드 계열 화합물 또는 이를 포함하는 강진향추출물을 함유한 매트릭스 메탈로프로테이나제 활성저해제 및 기능성 식품 失效
    基质金属蛋白酶抑制剂和含有FLAVONOID衍生物的功能性食品或含有黄酮衍生物的DALBERGIA ODORIFERA的提取物

    公开(公告)号：KR1020030075396A

    公开(公告)日：2003-09-26

    申请号：KR1020020014588

    申请日：2002-03-18

    Applicant: 동화약품주식회사 ,  이승택

    Inventor： 이승택 ,  장진욱 ,  김주현 ,  장윤정 ,  정용호 ,  임문정 ,  성희진 ,  노양국 ,  신동혁 ,  장환봉

    IPC: C07D311/40

    Abstract: PURPOSE: A matrix metalloproteinase inhibitor and functional food containing flavonoid derivatives or extracts of Dalbergia odorifera containing the flavonoid derivatives are provided, thereby effectively treating diseases associated with matrix metalloproteinase. CONSTITUTION: Extracts of Dalbergia odorifera containing fisetin of formula 1 and 3'-hydroxydidzein of formula 2 are prepared by dissolving pulverized Dalbergia odorifera in a solvent selected from methanol, a mixed solvent of methanol and water and ethylacetate, filtering the solution, and concentrating the filtered solution under reduced pressure. A fraction of Dalbergia odorifera containing fisetin and 3'-hydroxydidzein is prepared by dissolving Dalbergia odorifera in methanol or a mixed solvent of water and methanol, filtering the solution, adding ethylacetate or butanol into the filtered solution, filtering the solution, and concentrating the filtered solution under reduced pressure.

    Abstract translation: 目的：提供一种基质金属蛋白酶抑制剂和含有黄酮类衍生物的黄酮类衍生物或含有黄酮衍生物的提取物的功能性食品，从而有效治疗与基质金属蛋白酶相关的疾病。 构成：通过将粉碎的Dalbergia odorifera溶解在选自甲醇，甲醇和水与乙酸乙酯的混合溶剂的溶剂中，过滤该溶液并浓缩，得到含有式1的非瑟酮和式2的3'-氢氧根霉素的Dalbergia odorifera的提取物 在减压下过滤溶液。 通过将Dalbergia odorifera在甲醇或水和甲醇的混合溶剂中溶解，过滤该溶液，向过滤的溶液中加入乙酸乙酯或丁醇，过滤溶液，浓缩过滤的溶液，制备含有非丝氨酸和3'-羟基溶解素的Dalbergia odorifera的一小部分 溶液在减压下。

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