신규한 이마티닙 캠실레이트 및 그의 제조방법
    5.
    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
    7.
    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。

    신규한 2-이미다졸론유도체 및 그의 제조방법
    8.
    发明公开
    신규한 2-이미다졸론유도체 및 그의 제조방법 失效
    新颖的2-咪唑啉酮衍生物及其制备方法

    公开(公告)号:KR1019970015588A

    公开(公告)日:1997-04-28

    申请号:KR1019950029425

    申请日:1995-09-07

    Abstract: 본 발명은 항암작용을 갖는 신규한 이미다졸론 유도체, 즉 다음 일반식(Ⅰ)의 4-페닐-1-아릴설포닐-4,5-디하이드로-2-이미다졸론 유도체와 다음 일반식(Ⅱ)으로 표시되는 그의 위치이성체 및 그의 제조방법과 항암제로서 그의 용도에 관한 것이다.


    상기 식에서, Y는 1-나프틸, 2-나프틸, 1,2,3,4-테트라하이드로나프탈렌-6-일, 2,3-디하이드로벤조푸란-5-일 또는 다음 일반식(A)의 인돌린-5-일을 나타내며,

    여기에서 R은 수소, C
    1 ~C
    4 의 알킬, 트리플루오로메틸, C
    1 ~C
    4 의 아실, 클로로아세틸, 트리플루오로아세틸, 브로모아세틸, 하이드록시아세틸, 메르캅토아세틸, C
    1 ~C
    4 의 알콕시카보닐, 치환되거나 비치환된 페닐옥시카보닐, 하이드록시카보닐메틸 또는 그의 에스테르를 나타낸다.

    정향 에탄올 추출물의 용매 분획물을 유효성분으로 함유하는 고지혈증 예방 및 치료용 지질개선제
    9.
    发明公开
    정향 에탄올 추출물의 용매 분획물을 유효성분으로 함유하는 고지혈증 예방 및 치료용 지질개선제 无效
    预防高脂血症和固化脂质体改良剂含有溶血性脂肪分解物的提取物

    公开(公告)号:KR1020120114790A

    公开(公告)日:2012-10-17

    申请号:KR1020110032546

    申请日:2011-04-08

    CPC classification number: A61K36/61 A23V2200/326 A23V2200/3262 A61K2236/33

    Abstract: PURPOSE: A lipid improving agent for prevention and treating hyperlipidemia which contains solvent fraction of caryophylli flos ethanol extracts is provided to enhance ACAT enzyme inhibition effects. CONSTITUTION: A lipid improving agent for prevention and treating hyperlipidemia contains Caryophylli Flos ethylacetate fraction as an active ingredient. The Caryophylli Flos ethylacetate fraction is obtained by the following steps: extracting the Caryophylli Flos as ethanol at the room temperature and concentrating at 60 deg. Or less and suspends in water; solvent extracting the suspended solution using hexane and removing the separated hexane layer; solvent extracting the remaining water layer by using the methylene chloride solvent and isolating and removing the methylenechloride layer; isolation extracting the remaining water layer by using ethylacetate solvent and separating the ethylacetate layer and compressing and concentrating thereof at 60 deg. Celsius or less. [Reference numerals] (AA) Caryophylli flos; (BB) 95% ethanol; (CC) Caryophylli flos 95% ethanol extract(comparative example 1); (DD) Water; (EE) Suspended solution; (FF) Hexane; (GG) Hexane layer(comparative example 2); (HH, KK, NN) Water layer; (II) Methylenechloride; (JJ) Methylenechloride layer(comparative example 3); (LL) Ethyl acetate; (MM) Ethyl acetate layer(practical example 1); (OO) Butanol; (PP) Butanol layer(comparative example 4); (QQ) Water layer(comparative example 5)

    Abstract translation: 目的:提供一种用于预防和治疗含有caryophylli flos乙醇提取物的溶剂级分的高脂血症的脂质改善剂,以增强ACAT酶的抑制作用。 构成:用于预防和治疗高脂血症的脂质改善剂含有Caryophylli Flos乙酸乙酯部分作为活性成分。 通过以下步骤获得Caryophylli Flos乙酸乙酯级分:在室温下将Caryophylli Flos作为乙醇提取,并在60℃浓缩。 或更少,并在水中暂停; 溶剂用己烷萃取悬浮溶液,除去分离的己烷层; 溶剂通过使用二氯甲烷溶剂萃取剩余的水层并分离和除去二氯甲烷层; 通过使用乙酸乙酯溶剂分离萃取剩余的水层并分离乙酸乙酯层并在60℃压缩并浓缩。 摄氏度以下。 (附图标记)(AA)Caryophylli flos; (BB)95%乙醇; (CC)Caryophylli flos 95%乙醇提取物(比较例1); (DD)水; (EE)悬浮溶液; (FF)己烷; (GG)己烷层(比较例2)。 (HH,KK,NN)水层; (二)亚甲基氯; (JJ)亚甲基氯化物层(比较例3); (LL)乙酸乙酯; (MM)乙酸乙酯层(实施例1); (OO)丁醇; (PP)丁醇层(比较例4); (QQ)水层(比较例5)

    고지혈증 치료시 유발되는 간 손상 예방 및 간 기능 개선을위한 정향 추출물 함유 기능성식품
    10.
    发明授权
    고지혈증 치료시 유발되는 간 손상 예방 및 간 기능 개선을위한 정향 추출물 함유 기능성식품 有权
    包括来自Eugenia caryophyllata的提取物的功能食品用于改善和预防由高脂血症治疗引起的肝损伤症状

    公开(公告)号:KR101134176B1

    公开(公告)日:2012-04-24

    申请号:KR1020080123424

    申请日:2008-12-05

    Abstract: PURPOSE: Functional food containing eugenia caryophyllata extract is provided to protect tissue of liver while restricting enzyme activity of alanine aminotransferase and aspartate aminotransferase in blood, and to restrict accumulation of fat in liver. CONSTITUTION: Functional food preventing liver damage caused by high fat and improving liver function contains eugenia caryophyllata extract. The functional food further contains mixed herbal mixtures of cinnamomi Cortex, myristicae Semen, gambir, aurantii nobilis Pericarpium, atractylodis Rhizoma, magnoliae Cortex, corydalis Tuber and Capsicum annuum. The function food further contains a mixed herb extract mixture.

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