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11. 发明申请

WO2008123751A1 STABLE ANHYDROUS CRYSTALLINE DOCETAXEL AND METHOD FOR THE PREPARATION THEREOF 审中-公开
标题翻译：稳定的无水结晶白蛋白及其制备方法
公开(公告)号：WO2008123751A1
公开(公告)日：2008-10-16
申请号：PCT/KR2008/002014
申请日：2008-04-10
申请人： HANMI PHARM. CO., LTD. , KIM, Namdu , SHIN, Woo Seob , JUNG, Jaehyuk , KIM, Gi Jeong , CHO, Seung Hwan , LIM, Eun Jung , MOON, Youngho , CHANG, Young-Kil , LEE, Gwan Sun
发明人： KIM, Namdu , SHIN, Woo Seob , JUNG, Jaehyuk , KIM, Gi Jeong , CHO, Seung Hwan , LIM, Eun Jung , MOON, Youngho , CHANG, Young-Kil , LEE, Gwan Sun
IPC分类号： C07D305/14
CPC分类号： C07D305/14
摘要： The present invention provides a stable anhydrous crystalline docetaxel which has anti-tumor and anti-leukemia activity, and method for the preparation thereof.
摘要翻译：本发明提供了具有抗肿瘤和抗白血病活性的稳定的无水结晶多西紫杉醇及其制备方法。

12. 发明申请

WO2008048037A1 A NOVEL VECTOR AND EXPRESSION CELL LINE FOR MASS PRODUCTION OF RECOMBINANT PROTEIN AND A PROCESS OF PRODUCING RECOMBINANT PROTEIN USING SAME 审中-公开
标题翻译：用于生产重组蛋白质的新型载体和表达细胞系以及使用其生产重组蛋白的方法
公开(公告)号：WO2008048037A1
公开(公告)日：2008-04-24
申请号：PCT/KR2007/005064
申请日：2007-10-16
申请人： HANMI PHARMACEUTICAL CO., LTD. , CHOI, In Young , KIM, Chang Hwan , LEE, Hyun Ji , PARK, Seong Hee , KWON, Se Chang , LEE, Gwan Sun
发明人： CHOI, In Young , KIM, Chang Hwan , LEE, Hyun Ji , PARK, Seong Hee , KWON, Se Chang , LEE, Gwan Sun
IPC分类号： C12N15/63 , C12N15/79 , C12N15/09
CPC分类号： C12N9/003 , C12N15/85 , C12N2510/00
摘要： Disclosed herein is an inducible high-expression cassette comprising a dihydrofolate reductase (DHFR) promoter from which GC-rich repeat sequences are partially or entirely removed, the cassette capable of more effectively improving a gene amplification system. Also disclosed are an expression vector comprising the inducible expression cassette and optionally a gene encoding a recombinant protein of interest, an animal cell line transformed with the expression vector, and a method of mass producing and purifying a recombinant protein by culturing the transformant. The present invention enables the shortening of the time required to establish a cell line producing a recombinant protein of interest at high levels using a low concentration of a DHFR inhibitor, thereby allowing more effective production of the recombinant protein.
摘要翻译：本文公开了包含二氢叶酸还原酶（DHFR）启动子的诱导型高表达盒，从其中部分或全部除去富含GC的重复序列，所述盒能够更有效地改善基因扩增系统。还公开了包含可诱导表达盒和任选的编码目标重组蛋白的基因，用表达载体转化的动物细胞系的表达载体，以及通过培养转化体大量生产和纯化重组蛋白的方法。本发明能够缩短使用低浓度的DHFR抑制剂以高水平建立产生重组蛋白质的细胞系所需的时间，从而允许更有效地产生重组蛋白质。

13. 发明申请

WO2006071090A1 METHOD FOR THE PREPARATION OF 2'-DEOXY-2',2'-DIFLUOROCYTIDINE 审中-公开
标题翻译：制备2'-脱氧-2'，2'-二氟尿嘧啶的方法
公开(公告)号：WO2006071090A1
公开(公告)日：2006-07-06
申请号：PCT/KR2005/004633
申请日：2005-12-29
申请人： HANMI PHARM. CO., LTD. , LEE, Jaeheon , PARK, Gha Seung , LEE, Moonsub , BANG, Hyo-Jeong , LEE, Jae Chul , KIM, Cheol Kyong , CHOI, Chang-Ju , KIM, Han Kyong , LEE, Hoe Chul , CHANG, Young-Kil , LEE, Gwan Sun
发明人： LEE, Jaeheon , PARK, Gha Seung , LEE, Moonsub , BANG, Hyo-Jeong , LEE, Jae Chul , KIM, Cheol Kyong , CHOI, Chang-Ju , KIM, Han Kyong , LEE, Hoe Chul , CHANG, Young-Kil , LEE, Gwan Sun
IPC分类号： C07H19/04
CPC分类号： C07H19/04
摘要： This invention relates to an improved method for stereoselectively preparing 2¢¥-deoxy-2¢¥,2¢¥-difluorocytidine of formula (I), which comprises the steps of reacting a 1-halo ribofuranose compound of formula (III) with a nucleobase of formula (IV) in a solvent to obtain a nucleoside of formula (II) with removing the silyl halide of formula (V) produced during the reaction; and deprotecting the nucleoside of formula (II) to obtain 2¢¥-deoxy-2¢¥,2¢¥-difluorocytidine of formula (I).
摘要翻译：本发明涉及一种用于立体选择性制备式（I）的2'-二脱氧-2¢¥，2¢-二氟胞苷的改进方法，其包括以下步骤：使式（III）的1-卤代呋喃核糖化合物与（IV）的核碱基在溶剂中得到式（II）的核苷，同时除去在反应过程中产生的式（Ⅴ）的甲硅烷基卤化物; 并使式（II）的核苷脱保护，得到式（I）的2¢¥脱氧-2¢¥，2¢¥ - 二氟胞苷。

14. 发明申请

WO2005038031A1 EXPRESSION VECTOR FOR SECRETING ANTIBODY FRAGMENT USING E. COLI SIGNAL SEQUENCE AND METHOD FOR MASS-PRODUCING ANTIBODY FRAGMENT 审中-公开
标题翻译：使用大肠杆菌信号序列分析抗体片段的表达载体和产生抗体片段的方法
公开(公告)号：WO2005038031A1
公开(公告)日：2005-04-28
申请号：PCT/KR2004/002625
申请日：2004-10-14
申请人： HANMI PHARM. CO., LTD. , JUNG, Sung Youb , KIM, Jin Sun , KWON, Se Chang , LEE, Gwan Sun
发明人： JUNG, Sung Youb , KIM, Jin Sun , KWON, Se Chang , LEE, Gwan Sun
IPC分类号： C12N15/70
CPC分类号： C12P21/02 , C07K16/00 , C07K16/241 , C07K2317/55 , C07K2319/00 , C07K2319/02 , C12N15/70
摘要： A recombinant expression vector capable of expressing and secreting an antibody fragment fused with E. coli thermostable enterotoxin signal sequence derivative or E. coli outer membrane protein A (Omp A) signal sequence in the form of a soluble heterozygote protein is used to mass-produce the antibody fragment by culturing a microorganism transformed with the expression vector in a medium and collecting the antibody fragment secreted from the transformed microorganism into the medium.
摘要翻译：能够表达和分泌与大肠杆菌热稳定性肠毒素信号序列衍生物或可溶性杂合子蛋白质形式的大肠杆菌外膜蛋白A（Omp A）信号序列融合的抗体片段的重组表达载体用于大规模生产通过在培养基中培养用表达载体转化的微生物并将从转化的微生物分泌的抗体片段收集到培养基中的抗体片段。

15. 发明申请

WO2002083692A1 PROCESS FOR THE SELECTIVE PREPARATION OF 3-(Z) PROPENYL-CEPHEM COMPOUND 审中-公开
标题翻译：选择性制备3-（Z）丙烯酰化合物的方法
公开(公告)号：WO2002083692A1
公开(公告)日：2002-10-24
申请号：PCT/KR2002/000700
申请日：2002-04-17
申请人： HANMI PHARM. CO., LTD. , LEE, Gwan Sun , CHANG, Young Kil , KIM, Hong Sun , LEE, Jae Heon , PARK, Chul Hyun , PARK, Gha Seung , KIM, Cheol Kyung
发明人： LEE, Gwan Sun , CHANG, Young Kil , KIM, Hong Sun , LEE, Jae Heon , PARK, Chul Hyun , PARK, Gha Seung , KIM, Cheol Kyung
IPC分类号： C07D501/04
CPC分类号： C07D501/00 , Y02P20/55
摘要： A 3-(Z)-propenyl cephem compound is selectively prepared by reacting a phosphoranylidene cephemcompound with acetaldehyde in the presence of a base in a solvent mixture comprising diethyl ether, formula (I), wherein R is a carboxyl protecting group; R 1 is hydrogen or R 2 CH 2 CO-; and R 2 is ethyl, 2-thiophenyl, phenyl, p-hydroxyphenyl or phenoxy.
摘要翻译：通过在碱存在下，将亚正膦基头孢烯化合物与乙醛反应在包含二乙醚，式（I）的溶剂混合物中，其中R是羧基保护基，选择性地制备3-（Z） - 丙烯基头孢烯化合物。 R 1是氢或R 2 CH 2 CO-; R 2是乙基，2-噻吩基，苯基，对羟基苯基或苯氧基。

16. 发明申请

WO2002079158A1 NOVEL AMLODIPINE CAMSYLATE AND METHOD FOR PREPARING THEREOF 审中-公开
标题翻译：新型茉莉酸甲酯及其制备方法
公开(公告)号：WO2002079158A1
公开(公告)日：2002-10-10
申请号：PCT/KR2002/000543
申请日：2002-03-28
申请人： HANMI PHARM. CO., LTD. , MOON, Young Ho , KIM, Nam Du , LEE, Kyung Ik , LEE, Gwan Sun , WOO, Jong Soo
发明人： MOON, Young Ho , KIM, Nam Du , LEE, Kyung Ik , LEE, Gwan Sun , WOO, Jong Soo
IPC分类号： C07D211/84
CPC分类号： C07D211/90
摘要： Amlodipine camsylate of the present invention is a crystalline salt of amlodipine suitable for pharmaceutical formulation, which is prepared by using low toxic camphor sulfonic acid to meet required pharmaceutical properties for treating cadiovacular diseases.
摘要翻译：本发明的氨氯地平樟脑磺酸盐是适用于药物制剂的氨氯地平的结晶盐，其通过使用低毒樟脑磺酸来满足治疗癌症性疾病所需的药物性质来制备。

17. 发明申请

WO1998008832A1 PROCESS FOR PREPARING PACLITAXEL 审中-公开
标题翻译：制备PACLITAXEL的方法
公开(公告)号：WO1998008832A1
公开(公告)日：1998-03-05
申请号：PCT/KR1997000157
申请日：1997-08-25
申请人： HANMI PHARM. CO., LTD. , KIM, Kyoung, Soo , CHAI, Ki, Byung , MOON, Young, Ho , LEE, Kwang, Ok , KIM, Nam, Du , HA, Tae, Hee , SHIN, Jung, Ae , LEE, Gwan, Sun , KIM, Wan, Joo
发明人： HANMI PHARM. CO., LTD.
IPC分类号： C07D305/14
CPC分类号： C07D263/04 , C07D305/14 , C07D413/12 , Y02P20/55
摘要： The present invention relates to a process for preparing paclitaxel represented by formula (1) characterized in that: (a) an oxazolidine derivative represented by formula (2) or its salt in which X represents halogen, is coupled with a 7-trihaloacetyl-baccatin III represented by formula (3) in which R1 represents trihaloacetyl, in a solvent in the presence of a condensing agent to produce an oxazolidine substituent-containing taxane represented by formula (4) in which X and R1 are each as previously defined; (b) the oxazolidine ring is opened in a solvent in the presence of an acid, and the product thus obtained is reacted with benzoyl chloride in the presence of a base to produce a protected paclitaxel wherein the hydroxy group at 7-position is protected with trihaloacetyl group represented by formula (5) in which R1 is as previously defined; (c) then the protecting group at 7-position is removed by ammonia or a salt of ammonia with a weak acid in a solvent.
摘要翻译：本发明涉及一种制备由式（1）表示的紫杉醇的方法，其特征在于：（a）由式（2）表示的恶唑烷衍生物或其中X表示卤素的盐与7-三卤代乙酰基浆果赤霉素（3）表示的化合物，其中R 1表示三卤代乙酰基，在溶剂中，在缩合剂存在下制备由式（4）表示的含恶唑烷取代基的紫杉烷，其中X和R 1各自如上所定义; （b）在酸存在下，在溶剂中打开恶唑烷环，将得到的产物与苯甲酰氯在碱的存在下反应，得到保护的紫杉醇，其中7位的羟基被由式（5）表示的三卤代乙酰基，其中R 1如前所定义; （c）然后在溶剂中用氨或氨与弱酸将7位保护基除去。

18. 发明申请

WO1996001262A1 NOVEL QUINOLINE COMPOUND AND PROCESS FOR PREPARATION THEREOF 审中-公开
标题翻译：新型喹啉化合物及其制备方法
公开(公告)号：WO1996001262A1
公开(公告)日：1996-01-18
申请号：PCT/KR1995000084
申请日：1995-06-30
申请人： HANMI PHARMACEUTICAL CO., LTD. , MOON, Soon, Ku , LEE, Gwan, Sun , RYOO, Eui, Sang , MOON, Yound, Ho , KIM, Nam, Du
发明人： HANMI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D487/08
CPC分类号： C07D487/04
摘要： The present invention relates to a novel quinoline compound represented by general formula (I) and its pharmaceutically acceptable salt, which shows a superior antibacterial activity in contrast to the known quinoline based antibacterial agents, wherein R represents hydrogen or ester forming group; R represents hydrogen, amino, lower alkylamino, hydroxy, lower alkoxy, mercapto, lower alkylthio or halogen; Z represents an amine compound having general formula alpha , (wherein, R represents hydrogen or lower alkyl; R and R are identical to or different from each other, and independently represent hydrogen or C1-C2 alkyl); and X represents N or C-R (wherein R represents hydrogen, halogen, hydroxy, methyl, cyano, nitro or methoxy).
摘要翻译：本发明涉及通式（I）表示的新颖喹啉化合物及其药学上可接受的盐，其与已知的喹啉类抗菌剂相比显示出优异的抗菌活性，其中R 1表示氢或酯形成基团; R 2表示氢，氨基，低级烷基氨基，羟基，低级烷氧基，巯基，低级烷硫基或卤素; Z表示具有通式α的胺化合物（其中，R 3表示氢或低级烷基; R 4和R 5彼此相同或不同，并且独立地表示氢或C 1 -C 2烷基）; X表示N或C-R 6（其中R 6表示氢，卤素，羟基，甲基，氰基，硝基或甲氧基）。

19. 发明申请

WO2011046303A2 NOVEL METHOD FOR PREPARING ENTECAVIR AND INTERMEDIATE USED THEREIN 审中-公开
标题翻译：用于制备ENTECAVIR和中间体的新方法
公开(公告)号：WO2011046303A2
公开(公告)日：2011-04-21
申请号：PCT/KR2010/006306
申请日：2010-09-15
申请人： HANMI HOLDINGS CO., LTD. , LEE, Jae Heon , PARK, Gha Seung , KIM, Jin Hee , CHOI, Tae Jin , LEE, Ji Eun , HAN, Jung Hee , BANG, Hyo Jeong , JUNG, Sun Young , CHANG, Young KiI , LEE, Gwan Sun , KIM, Maeng Sup
发明人： LEE, Jae Heon , PARK, Gha Seung , KIM, Jin Hee , CHOI, Tae Jin , LEE, Ji Eun , HAN, Jung Hee , BANG, Hyo Jeong , JUNG, Sun Young , CHANG, Young KiI , LEE, Gwan Sun
IPC分类号： C07D473/18 , A61K31/522 , A61P31/14
CPC分类号： C07D473/04
摘要： Disclosed are: a novel, high-yield method for preparing entecavir and intermediates used therein.
摘要翻译：公开了一种用于制备恩替卡韦和其中使用的中间体的新颖的高产率方法。

20. 发明申请

WO2010120074A3 METHOD FOR PREPARING CRYSTALLINE ADEFOVIR DIPIVOXIL AND ADEFOVIR DIPIVOXIL BUTANOLATE USED THEREIN 审中-公开
标题翻译：用于制备水杨酸二氯吡啶的方法及其使用的对羟基苯甲酸丁酯
公开(公告)号：WO2010120074A3
公开(公告)日：2011-03-17
申请号：PCT/KR2010002233
申请日：2010-04-12
申请人： HANMI HOLDINGS CO LTD , OH HEE SOOK , BYUN EUN YOUNG , JANG SUK MAN , HA TAE HEE , KIM HAN KYONG , SUH KWEE HYUN , LEE GWAN SUN
发明人： OH HEE SOOK , BYUN EUN YOUNG , JANG SUK MAN , HA TAE HEE , KIM HAN KYONG , SUH KWEE HYUN , LEE GWAN SUN
IPC分类号： C07D473/34 , C07D473/16
CPC分类号： C07D473/16 , C07D473/34
摘要： Pure Form V crystals of adefovir dipivoxil can be prepared by a high-yield process comprising the steps of dissolving adefovir dipivoxil in butanol, cooling the resulting solution to give crystalline adefovir dipivoxil butanolate, dissolving the adefovir dipivoxil butanolate in ethyl acetate, and adding the resulting solution to diethyl ether.
摘要翻译：阿德福韦酯的纯V型晶体可以通过高产率方法制备，其包括将阿德福韦酯溶解在丁醇中的步骤，冷却所得溶液，得到结晶的阿德福韦酯丁醇酯，将阿德福韦酯的丁酸酯溶于乙酸乙酯中，溶于乙醚。

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