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1. 发明申请

WO2004097026B1 THE ENZYMATIC METHOD OF MAKING 1,2-DIOL DERIVATIVES AND THEIR ESTERS 审中-公开
标题翻译：制备1,2-二醇衍生物及其酯的方法
公开(公告)号：WO2004097026B1
公开(公告)日：2005-01-27
申请号：PCT/KR2004001005
申请日：2004-04-30
申请人： ENZYTECH LTD , HWANG SOON OOK , KIM DO HOON , RYU HYE YOUN
发明人： HWANG SOON OOK , KIM DO HOON , RYU HYE YOUN
IPC分类号： C12P7/02 , C12P7/62 , C12P41/00
CPC分类号： C12P7/02 , C12P7/62 , C12P41/004
摘要： The present invention relates to a new process for the preparation of optically active alcohols represented by the general formula 2 and their esters represented by the general formula 3 by enzymatic method from racemic alcohols represented by the general formula 1 in scheme 1. In more details, this invention relates to a process for producing optically active alcohols and their esters which are used as pharmaceutical intermediates from alcohols represented by the general formula 1 by stereospecific transesterification of secondary hydroxyl group using lipases as catalyst with acyl donors in organic solvent or with acyl donors only without using organic solvent. According to this invention, optically active alcohols and esters of high optical purity in high yield can be produced by transforming the primary hydroxyl group of 1,2-diols by tosyl group and transesterifying the secondary hydroxyl group stereospecifically by lipase.
摘要翻译：本发明涉及由方案1中由通式1表示的外消旋醇通过酶法由制备由通式2表示的光学活性醇及其由通式3表示的酯的新方法。更具体地，本发明涉及一种用于制备光学活性醇及其酯的方法，其通过使用脂肪酶作为催化剂的有机溶剂中的酰基供体的催化剂或仅与酰基供体的立体特异性酯交换作为由通式1表示的醇用作药物中间体不使用有机溶剂。根据本发明，可以通过将1,2-二醇的伯羟基转化为甲苯磺酰基并通过脂肪酶立体特异性酯交换酯酸化，可以制备高产率的高光学纯度的光学活性醇和酯。

2. 发明申请

WO2004106534B1 THE ENZYMATIC METHOD OF MAKING 1,2-DIOL DERIVATIVES AND THEIR ESTERS WITH SUCCINE ANHYDRIDE 审中-公开
标题翻译：制备1,2-二醇衍生物的方法及其与无水异氰酸酯的酯化
公开(公告)号：WO2004106534B1
公开(公告)日：2005-06-16
申请号：PCT/KR2004001313
申请日：2004-06-02
申请人： ENZYTECH LTD , HWANG SOON OOK , KIM DO HOON , RYU HYE YOUN , LEE TAE IM , CHUNG SUN HO
发明人： HWANG SOON OOK , KIM DO HOON , RYU HYE YOUN , LEE TAE IM , CHUNG SUN HO
IPC分类号： C12P7/04 , C12P7/62 , C12P41/00
CPC分类号： C12P7/62 , C12P7/04 , C12P41/004
摘要： The present invention relates to a new process for the preparation of optically active alcohols represented by the general formula 2 and their esters represented by the general formula 3 in scheme 1. In more detail, this invention relates to the process for the preparation of optically active alcohols and their esters which are used as pharmaceutical intermediates by reacting the hydroxyl group stereospecifically by lipase after adding racemic alcohols represented by the general formula 1 and succinic anhydride as an acylating agent to the organic solvent. According to this invention, the primary hydroxyl group of 1,2-diols is transformed by other functional group and the secondary hydroxyl group is esterified stereospecifically with succinic anhydride as an acylating agent. Optically active alcohols and their esters of high optical purity in high yield can be produced by using succinic anhydride as an acylating agent because alcohols can be separated from their esters more easily than those of other conventional methods.
摘要翻译：本发明涉及制备由通式2表示的光学活性醇的新方法及其在方案1中由通式3表示的酯。更详细地说，本发明涉及制备光学活性的方法醇和它们的酯，其通过在将通式1表示的外消旋醇和琥珀酸酐作为酰化剂加入到有机溶剂中之后通过脂肪酶立体特异性地使羟基反应而用作药物中间体。根据本发明，1,2-二醇的伯羟基被其它官能团转变，仲羟基与琥珀酸酐作为酰化剂立体特异性酯化。通过使用琥珀酸酐作为酰化剂可以生产高产率的高光学纯度的光学活性醇及其酯，因为与其它常规方法相比，可以更容易地将醇与其酯分离。

3. 发明申请

WO2011122840A3 INHIBITOR FOR MELANIN, AND COSMETIC COMPOSITION CONTAINING SAME 审中-公开
标题翻译：用于梅毒素的抑制剂和含有它们的化妆品组合物
公开(公告)号：WO2011122840A3
公开(公告)日：2012-03-01
申请号：PCT/KR2011002170
申请日：2011-03-30
申请人： AMOREPACIFIC CORP , SHIN HONG JU , KIM DO HOON , KIM JEONG HWAN , KOH HYUN JU , PARK WON SEOK
发明人： SHIN HONG JU , KIM DO HOON , KIM JEONG HWAN , KOH HYUN JU , PARK WON SEOK
IPC分类号： A61K8/34 , A61K8/30 , A61K8/42 , A61Q19/00
CPC分类号： A61K8/44 , A61K8/675 , A61Q19/00 , A61Q19/02
摘要： The present invention relates to an inhibitor for melanin which contains tranexamic acid and niacinamide as active ingredients for inhibiting the formation of melanin cells in the skin, and a cosmetic composition containing the inhibitor for melanin as an active ingredient for relieving liver spots, blemishes, freckles and inflammatory hyperpigmentation, improving skin tone and texture, and skin whitening.
摘要翻译：本发明涉及含有氨甲环酸和烟酰胺作为抑制皮肤黑色素细胞形成的活性成分的黑色素抑制剂，含有黑色素抑制剂作为缓解肝斑，瑕疵，雀斑的活性成分的化妆品组合物和炎性色素沉着过敏，改善肤色和质地，以及皮肤美白。

4. 发明申请

WO2010110545A3 NOVEL HYDROXAMATE DERIVATIVE, A PRODUCTION METHOD FOR THE SAME, AND A PHARMACEUTICAL COMPOSITION COMPRISING THE SAME 审中-公开
标题翻译：新型羟肟酸衍生物，其生产方法和包含其的药物组合物
公开(公告)号：WO2010110545A3
公开(公告)日：2011-03-24
申请号：PCT/KR2010001656
申请日：2010-03-18
申请人： CHONG KUN DANG PHARM CORP , LEE SUNG SOOK , LEE KYUNG JOO , LEE CHANG SIK , YANG HYUN MO , KIM DO HOON , CHOI DAE KYU , CHOI HO JIN , KIM DAL HYUN , HWANG IN CHANG , KIM MI JEONG , HAN BYEONG HOON
发明人： LEE SUNG SOOK , LEE KYUNG JOO , LEE CHANG SIK , YANG HYUN MO , KIM DO HOON , CHOI DAE KYU , CHOI HO JIN , KIM DAL HYUN , HWANG IN CHANG , KIM MI JEONG , HAN BYEONG HOON
IPC分类号： C07D209/04 , C07D209/08 , C07D209/44
CPC分类号： C07D401/04 , C07D209/08 , C07D209/14 , C07D209/44 , C07D231/56 , C07D235/14 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/12
摘要： The present invention relates to a hydroxamate derivative, to an isomer of the hydroxamate derivative and to pharmaceutically acceptable salts, hydrates or solvates of the hydroxamate derivative or the isomer of the hydroxamate derivative, as well as to an application for the same in the production of a pharmaceutical composition, to a pharmaceutical composition containing the same and to a method for the prophylaxis and treatment of medical conditions in which the pharmaceutical composition is employed, and also to a production method for the hydroxamate derivative.
摘要翻译：本发明涉及异羟肟酸酯衍生物，异羟肟酸衍生物的异构体以及异羟肟酸酯衍生物的药学上可接受的盐，水合物或溶剂合物或异羟肟酸衍生物的异构体，以及其用于生产药物组合物，含有该药物组合物的药物组合物，以及预防和治疗其中使用药物组合物的医疗条件的方法，以及用于异羟肟酸衍生物的制备方法。

5. 发明申请

WO2012050359A3 HYDROGEL PARTICLE COATED WITH LIPID AND METHOD FOR MANUFACTURING SAME 审中-公开
标题翻译：涂有脂质的水凝胶颗粒及其制造方法
公开(公告)号：WO2012050359A3
公开(公告)日：2012-07-05
申请号：PCT/KR2011007578
申请日：2011-10-12
申请人： AMOREPACIFIC CORP , AN EUN JUNG , KIM DO HOON , LIM HYUNG JUN , SHIM JONG WON , KIM JIN WOONG , KIM HAN KON , JEONG CHOON BOK , KWON LEE KYOUNG , KIM JUN OH
发明人： AN EUN JUNG , KIM DO HOON , LIM HYUNG JUN , SHIM JONG WON , KIM JIN WOONG , KIM HAN KON , JEONG CHOON BOK , KWON LEE KYOUNG , KIM JUN OH
IPC分类号： A61K9/16 , A61K8/02 , A61K8/97 , A61K9/28 , A61K47/30 , A61K47/36 , A61K47/38
CPC分类号： A61K9/14 , A61K8/0241 , A61K8/042 , A61K8/14 , A61K8/553 , A61K8/735 , A61K2800/10 , A61K2800/622 , A61K2800/654 , A61Q19/00
摘要： The present invention relates to hydrogel particles coated with lipid, which are made from dispersing hydrogel particles in an organic solvent in which lipids are dissolved, and to a method for manufacturing same. Unlike the existing method for manufacturing hydrogel core vesicles, the present invention can effectively manufacture same by using an emulsification method, without involving the steps of chemical treatment of the surface of hydrogels or dilution, thereby facilitating mass production and preventing the decrease of drug encapsulation efficiency. The present method could be widely used for research on delivery carriers of oil/water-soluble active material or cell structure reproduction, and more particularly, a karatinocyte mimetic of the present invention containing natural moisturizing factors can contain a large quantity of bound water for a long time, thereby exhibiting superior capability to retain moisture and moisturize, and providing a composition for an ingredient in cosmetics for moisturizing.
摘要翻译：本发明涉及由脂质包覆的水凝胶粒子及其制造方法，该水凝胶粒子是将水凝胶粒子分散于溶解有脂质的有机溶剂中而成的。与现有的水凝胶核心泡囊的制造方法不同，本发明可以通过使用乳化方法有效地制造它，而不涉及化学处理水凝胶表面或稀释的步骤，从而有助于大规模生产并且防止药物包封效率的降低。本发明方法可广泛应用于油水溶性活性物质递送载体或细胞结构复制的研究，特别是含有天然保湿因子的本发明的角质形成细胞模拟物可含有大量的结合水从而表现出优异的保湿和保湿能力，并提供用于保湿化妆品中成分的组合物。

6. 发明申请

WO2009041789A3 NOVEL 3-CHLORO-5-SUBSTITUTED-QUINOXALINE-2-AMINE DERIVATIVES AND PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, METHOD FOR PREPARATION, THERAPEUTIC AGENT FOR INFLAMMATORY DISEASE INDUCED BY SPC ACTIVITY CONTAINING 3-CHLORO-5-SUBSTITUTED-QUINOXALINE-2-AMIN 审中-公开
标题翻译：新的3-氯-5-取代的喹喔啉-2-胺衍生物及其药学上可接受的盐，制备治疗由SPC活性引起的炎性疾病包含3-氯-5-取代的喹喔啉-2-胺的方法
公开(公告)号：WO2009041789A3
公开(公告)日：2009-05-14
申请号：PCT/KR2008005725
申请日：2008-09-26
申请人： KOREA RES INST CHEM TECH , AMOREPACIFIC CORP , GONG YOUNG-DAE , CHO HEEYEONG , JEON MOON-KOOK , LEE TAEHO , CHOI GILDON , KONG JAE-YANG , PARK WOO-KYU , HWANG SOON-HEE , KIM JUNG JU , LEE CHANG-HOON , KO JAEYOUNG , NOH MINSOO , HAN EUN SIL , KIM HYUK , YUN JUN-WON , MOH JOO HYUN , KIM DO HOON
发明人： GONG YOUNG-DAE , CHO HEEYEONG , JEON MOON-KOOK , LEE TAEHO , CHOI GILDON , KONG JAE-YANG , PARK WOO-KYU , HWANG SOON-HEE , KIM JUNG JU , LEE CHANG-HOON , KO JAEYOUNG , NOH MINSOO , HAN EUN SIL , KIM HYUK , YUN JUN-WON , MOH JOO HYUN , KIM DO HOON
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： Provided are a 3-chloro-5-substiuted-quinoxalin-2-amine derivative represented by the following Chemical Formula 1, a pharmaceutically acceptable salt thereof, a method for preparation thereof, and a use thereof as an effective ingredient in a therapeutic agent for inflammatory disease induced by activity of sphingosyl phosphorylcholine (SPC) receptor. The 3-chloro-5-substiuted-quinoxalin-2-amine derivative of the present invention has been confirmed to have superior inhibition activity against SPC receptor in an animal experiment using human-derived endothelial cells and mice. Thus, a therapeutic agent for inflammatory disease containing the 3- chloro-5-substiuted-quinoxalin-2-amine derivative or a pharmaceutically acceptable salt thereof as an effective ingredient may be useful for treating inflammation, itching or skin infection associated with atopic dermatitis or other disease induced by activity of SPC receptor.
摘要翻译：本发明提供由以下化学式1表示的3-氯-5-取代的喹喔啉-2-胺衍生物，其药学上可接受的盐，其制备方法及其作为有效成分在治疗剂中的用途由鞘氨醇磷酸胆碱（SPC）受体活性诱导的炎性疾病。已证实本发明的3-氯-5-取代的喹喔啉-2-胺衍生物在使用源于人的内皮细胞和小鼠的动物实验中对SPC受体具有优异的抑制活性。因此，含有3-氯-5-取代的喹喔啉-2-胺衍生物或其药学上可接受的盐作为有效成分的炎症性疾病治疗剂可用于治疗与特应性皮炎相关的炎症，发痒或皮肤感染或其他由SPC受体活性诱导的疾病。

7. 发明申请

WO2012087062A3 SUSTAINED-RELEASE POLYMERIC MICROPARTICLES CONTAINING POORLY WATER-SOLUBLE DRUG AND METHOD FOR PREPARING THE SAME 审中-公开
标题翻译：含有水难溶性药物的持续释放型聚合物微粒及其制备方法
公开(公告)号：WO2012087062A3
公开(公告)日：2012-08-23
申请号：PCT/KR2011010030
申请日：2011-12-23
申请人： SAMYANG BIOPHARMACEUTICALS , LEE SA WON , KIM DO HOON , KIM BONG OH , SEO MIN HYO
发明人： LEE SA WON , KIM DO HOON , KIM BONG OH , SEO MIN HYO
IPC分类号： A61K9/16 , A61K9/22 , A61K47/14 , A61K47/36
CPC分类号： A61K47/34 , A01N25/28 , A61K9/1635 , A61K9/1647 , A61K9/1694 , A61K31/175 , A61K31/27 , A61K31/436 , A61K31/485 , A61K31/519 , A61K31/554 , A61K31/565 , A61K31/57
摘要： Disclosed are sustained-release polymeric microparticles containing a poorly water-soluble drug and a method for preparing the same.
摘要翻译：公开了含有难溶于水的药物的持续释放聚合物微粒及其制备方法。

8. 发明申请

WO2012091357A3 COMPOSITION FOR PREVENTION OF NAUSEA OR VOMITING 审中-公开
标题翻译：防止鼻孔或呕吐的组合物
公开(公告)号：WO2012091357A3
公开(公告)日：2012-08-16
申请号：PCT/KR2011009908
申请日：2011-12-21
申请人： SAMYANG BIOPHARMACEUTICALS , SEO MIN HYO , LEE SA WON , KIM DO HOON
发明人： SEO MIN HYO , LEE SA WON , KIM DO HOON
IPC分类号： A61K31/4178 , A61K31/4184 , A61K31/573 , A61P1/08
CPC分类号： A61K31/573 , A61K9/0019 , A61K31/4178 , A61K31/4184 , A61K45/06 , A61K47/12 , A61K2300/00
摘要： Provided is a composition for preventing nausea or vomiting, including a 5-HT3 receptor antagonist and a corticosteroid, and having a pH adjusted to 3.0-6.0. Provided also is a method for preparing a composition for preventing nausea or vomiting, including: mixing a 5-HT3 receptor antagonist with a corticosteroid; and adjusting pH of the mixture obtained from the preceding operation to 3.0-6.0.
摘要翻译：本发明提供一种用于预防恶心或呕吐的组合物，包括5-HT 3受体拮抗剂和皮质类固醇，pH调节至3.0-6.0。还提供了一种制备用于预防恶心或呕吐的组合物的方法，包括：将5-HT 3受体拮抗剂与皮质类固醇混合; 并将从前述操作获得的混合物的pH调节至3.0-6.0。

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