디아민 유도체의 산부가염 및 이의 제조 방법
    2.
    发明申请
    디아민 유도체의 산부가염 및 이의 제조 방법 审中-公开
    二胺衍生物的酸加成盐及其制备方法

    公开(公告)号:WO2018038426A1

    公开(公告)日:2018-03-01

    申请号:PCT/KR2017/008576

    申请日:2017-08-08

    CPC classification number: C07C269/06 C07C269/08 C07C271/24

    Abstract: 본 발명은 광학 활성 디아민 유도체의 신규한 산부가염 및 이의 제조 방법에 관한 것이다. 본 발명의 디아민 유도체의 산부가염은 에독사반을 고순도 및 고수율로 제조할 수 있고, 독성 문제가 없으며, 비교적 간단한 공정 및 저렴한 비용으로 제조할 수 있는 제조 방법을 제공하여, 비용 및/또는 시간 면에서 경제적으로, 대량 생산에 유리하여 산업화에 사용될 수 있다.

    Abstract translation: 本发明涉及光学活性二胺衍生物的新型酸加成盐及其制备方法。 本发明的二胺衍生物的酸加成盐可以提供一种制备方法,该方法能够以高纯度和高收率生产环氧化剂,无毒性问题,并且可以以相对简单的工艺和低成本制造, 它可用于工业化,因为它在批量生产方面具有经济优势。

    개선된 자보플록사신의 제조방법
    4.
    发明公开
    개선된 자보플록사신의 제조방법 审中-实审
    ZABOFLOXACIN的改进制造方法

    公开(公告)号:KR1020150133433A

    公开(公告)日:2015-11-30

    申请号:KR1020140060112

    申请日:2014-05-20

    CPC classification number: C07D471/04 C07D487/10

    Abstract: 본발명은자보플록사신 D-아스파르트산염의개선된제조방법에관한것이다. 본발명은자보플록사신 D-아스파르트산염을제조하기위하여사용하는출발물질인 8-메톡시이미노-2,6-디아자-스피로[3,4]옥탄-2-카르복실산 t-부틸에스테르숙신산염(TBDCS) 또는 2-(2,2,2-트리플루오로-아세틸)-2,6-디아자-스피로[3.4]옥탄-8-온-메틸옥심메탄설폰산염(TDMOS)의신규한제조방법을제공한다. 본발명에따른제조방법은상기출발물질을높은수율과높은품질(HPLC 순도; 99.5% 이상)로제조할수 있어, 대량생산에적합하며, 치환반응시 TBDCS나 TDMOS를 1.0~1.1 당량을사용하여획기적으로생산단가를절감할수 방법을제공하기때문에자보플록사신 D-아스파르트산염의대량생산에유용하게이용될수 있다.

    Abstract translation: 本发明涉及一种制造扎布沙星D-天冬氨酸盐的改进方法。 本发明提供了制备用于制备扎布沙星D-天冬氨酸盐,8-甲氧基亚氨基-2,6-二氮杂 - 螺[3,4]辛烷-2-甲酸叔丁酯琥珀酸酯的引发剂的新方法 酸性盐(TBDCS)或2-(2,2,2-三氟 - 乙酰基)-2,6-二氮杂 - 螺[3,4]辛烷-8-对O-甲基肟甲磺酸盐(TDMOS)。 根据本发明的制造方法可以以高产率和质量(HPLC纯度;高于99.5%)制造引发剂,从而适合批量生产。 另外,该方法提供了在取代反应的情况下使用1.0〜1.1当量的TBDCS或者TDMOS来显着降低生产成本的方法,从而有效地用于批量生产扎布沙星D-天冬氨酸盐。

    도네페질 중간체의 제조방법
    5.
    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

    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
    6.
    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

    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
    8.
    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

    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。

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