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61. 发明申请

WO1997034864A1 STEREOSELECTIVE PROCESS FOR PREPARATION OF (2R,3S)-'beta'-PHENYLISOSERINE DERIVATIVE 审中-公开
标题翻译：制备（2R，3S） - β-苯并二氢吡喃衍生物的立体选择性方法
公开(公告)号：WO1997034864A1
公开(公告)日：1997-09-25
申请号：PCT/KR1997000041
申请日：1997-03-19
申请人： HANMI PHARMACEUTICAL CO., LTD. , KIM, Wan, Joo , LEE, Gwan, Sun , CHAI, Ki, Byung , KIM, Kyoung, Soo , MOON, Young, Ho , KIM, Nam, Du , LEE, Kwang, Ok , HA, Tae, Hee
发明人： HANMI PHARMACEUTICAL CO., LTD.
IPC分类号： C07C229/34
CPC分类号： C07C227/32
摘要： The present invention relates to a novel stereoselective process for preparing the (2R,3S)- beta -phenylisoserine derivative represented by formula (1), which can be used as an intermediate for synthesizing the terpene taxan derivatives paclitaxel and taxotere. In said formula, R1 represents hydrogen, benzoyl or t-butoxycarbonyl, and R2 represents hydrogen, C1-C4 alkyl, C1-C4 alkenyl, C1-C4 alkynyl or benzyl.
摘要翻译：本发明涉及一种制备式（1）所示的（2R，3S）-β-苯基异丝氨酸衍生物的新型立体选择性方法，其可用作合成萜烯紫杉醇衍生物紫杉醇和泰索帝的中间体。在所述式中，R 1表示氢，苯甲酰基或叔丁氧基羰基，R 2表示氢，C 1 -C 4烷基，C 1 -C 4烯基，C 1 -C 4炔基或苄基。

62. 发明申请

WO1992012155A1 NOVEL QUINOLONE COMPOUNDS AND PROCESSES FOR PREPARATION THEREOF 审中-公开
标题翻译：新型喹啉酮化合物及其制备方法
公开(公告)号：WO1992012155A1
公开(公告)日：1992-07-23
申请号：PCT/KR1992000003
申请日：1992-01-14
申请人： HANMI PHARMACEUTICAL CO., LTD. , MOON, Soon, Ku , LEE, Gwan, Sun , RYOO, Eui, Sang , CHANG, Young, Kil , MOON, Young, Ho , KIM, Sang, Tae , CHUN, Jong, Pil , KOH, Joon, Hyung , GIL, Young, Hwan
发明人： HANMI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D487/08
CPC分类号： C07D487/04 , Y02P20/55
摘要： This invention relates to the novel quinolone compound of formula (I) having excellent antimicrobial activity both against gram positive and negative bacteria, its pharmaceutically acceptable salt, and the process for preparation thereof; wherein R is hydrogen or protective group, R is hydrogen, amino, alkylamino from one to four carbon atoms, hydroxy, alkoxy from one to four carbon atoms, mercapto, alkylthio from one to four carbon atoms, or halogen, R is alkyl from one to four carbon atoms, alkenyl from two to four carbon atoms, cycloalkyl from three to six carbon atoms, haloalkyl, hydroxyalkyl from two to four carbon atoms, methoxy, amino, alkylamino from one to two carbon atoms, dimethylamino, or optionally substituted phenyl with more than one of halogen atoms or alkyl from one to three carbon atoms, Z is an amine of formula (II), (wherein R is hydrogen or alkyl from one to four carbon atoms, R and R are, same or different, hydrogen or alkyl from one to two carbon atoms), X is N or C-R (wherein R is hydrogen, hydroxy, methyl, cyano, nitro, methoxy, halogen, or can form a bridge of formula (a), (b), (c) or (d) with R .
摘要翻译：本发明涉及对革兰氏阳性细菌和阴性细菌具有优异的抗微生物活性及其药学上可接受的盐的式（I）的新型喹诺酮化合物及其制备方法; 其中R 1为氢或保护基，R 2为氢，氨基，1至4个碳原子的烷基氨基，羟基，1至4个碳原子的烷氧基，1至4个碳原子的巯基，烷硫基，或卤素 R 3为1至4个碳原子的烷基，2至4个碳原子的烯基，3至6个碳原子的环烷基，2至4个碳原子的卤代烷基，羟基烷基，甲氧基，氨基，1至2个碳原子的烷基氨基原子，二甲基氨基或具有多于一个卤素原子或1-3个碳原子的任选取代的苯基，Z是式（II）的胺，其中R 4是氢或1-4个碳原子的烷基 R 5和R 7相同或不同，氢或一至两个碳原子的烷基），X是N或CR 6（其中R 6是氢，羟基，甲基，氰基，硝基，甲氧基，卤素，或可以与R 3形成式（a），（b），（c）或（d）的桥。

63. 发明申请

WO2011040717A3 METHOD FOR PREPARING INTERMEDIATE OF SITAGLIPTIN USING CHIRAL OXIRANE 审中-公开
标题翻译：使用CHIRAL OXIRANE制备SITAGLIPTIN中间体的方法
公开(公告)号：WO2011040717A3
公开(公告)日：2011-10-13
申请号：PCT/KR2010006346
申请日：2010-09-16
申请人： HANMI HOLDINGS CO LTD , KIM NAM DU , CHANG JI YEON , JUNG JAE HYUK , LEE HYUN SEUNG , KIM DONG JUN , CHANG YOUNG KIL , LEE GWAN SUN
发明人： KIM NAM DU , CHANG JI YEON , JUNG JAE HYUK , LEE HYUN SEUNG , KIM DONG JUN , CHANG YOUNG KIL , LEE GWAN SUN
IPC分类号： C07C51/08 , C07C59/56 , C07C255/36 , C07D303/08
CPC分类号： C07C255/36 , C07C51/08 , C07D303/08 , C07C59/56
摘要： Disclosed is: a novel, simple and low-cost method for preparing 3-hydroxy-4-(2,4,5-trifluorophenyl)-butyric acid, particularly (3S)-3-hydroxy-4-(2,4,5-trifluorophenyl)-butyric acid, which is used as a key intermediate in the preparation of sitagliptin.
摘要翻译：公开了一种用于制备3-羟基-4-（2,4,5-三氟苯基） - 丁酸，特别是（3S）-3-羟基-4-（2,4,5,5-三氟苯基）丁酸的新型简单且低成本的方法。 - 三氟苯基） - 丁酸，其用作西格列汀的制备中的关键中间体。

64. 发明申请

WO2011002184A2 PHOSPHORIC ACID ESTER OF BICALUTAMIDE FOR TREATING PROSTATE CANCER 审中-公开
标题翻译：用于治疗前列腺癌的贝伐菌胺的磷酸酯
公开(公告)号：WO2011002184A2
公开(公告)日：2011-01-06
申请号：PCT/KR2010004153
申请日：2010-06-25
申请人： HANMI PHARM IND CO LTD , JANG SUN YOUNG , KIM SUNG BUM , KIM BYUNG KU , HEO MIN HOE , KIM EUN YOUNG , SONG TAE HUN , KIM YOUNG HOON , SUH KWEE HYUN , LEE GWAN SUN
发明人： JANG SUN YOUNG , KIM SUNG BUM , KIM BYUNG KU , HEO MIN HOE , KIM EUN YOUNG , SONG TAE HUN , KIM YOUNG HOON , SUH KWEE HYUN , LEE GWAN SUN
IPC分类号： C07F9/09 , A61K31/661 , A61P13/08 , A61P35/00
CPC分类号： C07F9/091
摘要： Provided is a phosphoric acid ester of bicalutamide and a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same as an active ingredient for treating prostate cancer, with which a linear correlation between the systemic exposure to bicalutamide and the dosage level can be achievable, making it possible to increase the bioavailability of bicalutamide upon oral administration at a high dosage level.
摘要翻译：提供了比卡鲁胺及其药学上可接受的盐的磷酸酯以及含有该磷酸酯作为治疗前列腺癌的活性成分的药物组合物，可以实现全身暴露于比卡鲁胺与剂量水平之间的线性相关性，使得可以在高剂量水平下口服给药时提高比卡鲁胺的生物利用度。

65. 发明申请

WO2010120074A2 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：WO2010120074A2
公开(公告)日：2010-10-21
申请号：PCT/KR2010/002233
申请日：2010-04-12
申请人： HANMI PHARM. 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。

66. 发明申请

WO2010071358A2 METHOD OF PREPARING EZETIMIBE AND INTERMEDIATES USED THEREIN 审中-公开
标题翻译：制备EZETIMIBE和其中使用的中间体的方法
公开(公告)号：WO2010071358A2
公开(公告)日：2010-06-24
申请号：PCT/KR2009/007535
申请日：2009-12-16
申请人： HANMI PHARM. CO., LTD. , KIM, Gi Jeong , KIM, Choong Hahn , CHANG, Ji Yeon , KIM, Nam Du , CHANG, Young Kil , LEE, Gwan Sun
发明人： KIM, Gi Jeong , KIM, Choong Hahn , CHANG, Ji Yeon , KIM, Nam Du , CHANG, Young Kil , LEE, Gwan Sun
IPC分类号： C07D205/08
CPC分类号： C07D205/08
摘要： Disclosed is a method for preparing ezetimibe which is effective for preventing or treating arteriosclerosis, and novel intermediates used therein. In accordance with the method which does not use expensive reagents, unwanted diastereoisomers can be easily removed by a step-by-step crystallization procedure, and the ezetimibe of formula 1 can be prepared in a high yield without the use of a hydrogenation procedure under a high pressure.
摘要翻译：公开了一种用于预防或治疗动脉硬化有效的依泽替米贝的制备方法，以及其中使用的新型中间体。根据不使用昂贵试剂的方法，不需要的非对映异构体可以通过逐步结晶步骤容易地除去，并且可以高收率地制备式1的依泽替米贝而不使用氢化程序在高压。

67. 发明申请

WO2009151299A2 STYRYLBENZOFURAN DERIVATIVES AS INHIBITORS FOR BETA-AMYLOID FIBRIL FORMATION AND PREPARATION METHOD THEREOF 审中-公开
标题翻译：作为抗坏血酸纤维素形成的抑制剂的苯乙烯苯并呋喃衍生物及其制备方法
公开(公告)号：WO2009151299A2
公开(公告)日：2009-12-17
申请号：PCT/KR2009/003165
申请日：2009-06-12
申请人： KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY , HANMI PHARM. CO., LTD. , KIM, Dong Jin , YOO, Kyung Ho , BYUN, Ji Hun , KIM, YoungSoo , KIM, Hye Yun , LEE, Gwan Sun , KIM, Maeng Sup , AHN, Young Gil , LEE, Ji Hoon , LEE, Myoung-Hwan , HWANG, Hana , RYU, Jiyeon
发明人： KIM, Dong Jin , YOO, Kyung Ho , BYUN, Ji Hun , KIM, YoungSoo , KIM, Hye Yun , LEE, Gwan Sun , KIM, Maeng Sup , AHN, Young Gil , LEE, Ji Hoon , LEE, Myoung-Hwan , HWANG, Hana , RYU, Jiyeon
IPC分类号： C07D307/78
CPC分类号： C07D307/81 , C07D307/80
摘要： The present invention relates to a novel compound which efficiently inhibits the formation of beta-amyloid fibrils in the brain to be useful for preventing or treating a degenerative brain disease, a method for preparing same, and a pharmaceutical composition comprising same as an active ingredient.
摘要翻译：本发明涉及有效抑制脑中β-淀粉样蛋白原纤维形成以用于预防或治疗退行性脑病的新型化合物，其制备方法和含有该衍生物作为活性成分的药物组合物。

68. 发明申请

WO2009011544A3 INSULINOTROPIC PEPTIDE DERIVATIVE WHEREIN ITS N-TERMINAL AMINO ACID IS MODIFIED 审中-公开
标题翻译：胰岛素衍生物其N-末端氨基酸被修饰
公开(公告)号：WO2009011544A3
公开(公告)日：2009-03-19
申请号：PCT/KR2008004170
申请日：2008-07-16
申请人： HANMI PHARMACEUTICAL CO LTD , SONG DAE HAE , LIM CHANG KI , KIM YOUNG HOON , KWON SE CHANG , LEE GWAN SUN , BAE SUNG MIN , JUNG SUNG YOUB
发明人： SONG DAE HAE , LIM CHANG KI , KIM YOUNG HOON , KWON SE CHANG , LEE GWAN SUN , BAE SUNG MIN , JUNG SUNG YOUB
IPC分类号： C07K14/65
CPC分类号： C07K14/46 , A61K38/26 , C07K14/57563 , C07K14/605
摘要： The present invention relates to an N-terminal amino acid-modified insulinotropic peptide having a high activity, and to a pharmaceutical composition comprising the same. The insulinotropic peptide derivatives according to the present invention exhibit therapeutic effects, which are not observed in native and other insulinotropic peptide analogs. Therefore, the insulinotropic peptide derivatives and the pharmaceutical composition comprising the same according to the present invention can be effectively provided for the treatment of the diseases.
摘要翻译：本发明涉及具有高活性的N-末端氨基酸修饰的促胰岛素肽以及包含其的药物组合物。根据本发明的促胰岛素肽衍生物显示出在天然和其他促胰岛素肽类似物中未观察到的治疗效果。因此，可以有效地提供促胰岛素肽衍生物和包含其的本发明的药物组合物用于治疗疾病。

69. 发明申请

WO2009020323A3 PROCESS FOR PREPARING VORICONAZOLE 审中-公开
公开(公告)号：WO2009020323A3
公开(公告)日：2009-02-12
申请号：PCT/KR2008/004516
申请日：2008-08-04
申请人： HANMI PHARM. CO., LTD. , MOON, Young Ho , LEE, Moon Sub , YOO, Jae Ho , KIM, Ji Sook , KIM, Han Kyong , CHOI, Chang Ju , CHANG, Young Kil , LEE, Gwan Sun
发明人： MOON, Young Ho , LEE, Moon Sub , YOO, Jae Ho , KIM, Ji Sook , KIM, Han Kyong , CHOI, Chang Ju , CHANG, Young Kil , LEE, Gwan Sun
IPC分类号： C07D401/06
摘要： Optically pure voriconazole can be prepared in a high yield by a) subjecting 1-(2,4-difluorophenyl)-2(1H-1,2,4-triazol-1-yl)ethanone to Reformatsky-type coupling reaction with a substituted thiopyrimidine derivative to obtain a desired (2R,3S)/(2S,3R)-enantiomeric pair; b) removing the thiol derivative from the enantiomer to obtain racemic voriconazole; and c) isolating the racemic voriconazole by way of optical resolution using an optically active acid.

70. 发明申请

WO2009020323A2 PROCESS FOR PREPARING VORICONAZOLE 审中-公开
标题翻译：制备VORICONAZOLE的方法
公开(公告)号：WO2009020323A2
公开(公告)日：2009-02-12
申请号：PCT/KR2008004516
申请日：2008-08-04
申请人： HANMI PHARM IND CO LTD , MOON YOUNG HO , LEE MOON SUB , YOO JAE HO , KIM JI SOOK , KIM HAN KYONG , CHOI CHANG JU , CHANG YOUNG KIL , LEE GWAN SUN
发明人： MOON YOUNG HO , LEE MOON SUB , YOO JAE HO , KIM JI SOOK , KIM HAN KYONG , CHOI CHANG JU , CHANG YOUNG KIL , LEE GWAN SUN
IPC分类号： C07D401/06
CPC分类号： C07D403/06
摘要： Optically pure voriconazole can be prepared in a high yield by a) subjecting 1-(2,4-difluorophenyl)-2(1H-1,2,4-triazol-1-yl)ethanone to Reformatsky-type coupling reaction with a substituted thiopyrimidine derivative to obtain a desired (2R,3S)/(2S,3R)-enantiomeric pair; b) removing the thiol derivative from the enantiomer to obtain racemic voriconazole; and c) isolating the racemic voriconazole by way of optical resolution using an optically active acid.
摘要翻译：可以通过以下方法制备光学纯的伏立康唑：a）使1-（2,4-二氟苯基）-2（1H-1,2,4-三唑-1-基）乙酮与取代基进行重新形成偶联反应硫代嘧啶衍生物，得到所需的（2R，3S）/（2S，3R） - 对映异构体对; b）从对映异构体中除去硫醇衍生物，得到外消旋的伏立康唑; 和c）使用光学活性酸通过光学拆分分离外消旋的伏立康唑。

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