公开(公告)号：US20080124347A1

公开(公告)日：2008-05-29

申请号：US11747153

申请日：2007-05-10

Applicant: Young Min Kim ,  Dae Jin Kim ,  Sung Min Bae ,  Chang Ki Lim ,  Se Chang Kwon ,  Gwan Sun Lee ,  Dae Hae Song ,  Young Hoon Kim

Inventor： Young Min Kim ,  Dae Jin Kim ,  Sung Min Bae ,  Chang Ki Lim ,  Se Chang Kwon ,  Gwan Sun Lee ,  Dae Hae Song ,  Young Hoon Kim

IPC: A61K39/395 ,  C07K14/62 ,  A61P3/10 ,  A61P3/04 ,  A61P15/00 ,  A61P9/00

CPC classification number: A61K47/68 ,  A61K47/6811 ,  A61K47/6813 ,  A61K47/6835 ,  C07K14/505 ,  C07K14/535 ,  C07K14/56 ,  C07K14/61 ,  C07K16/46 ,  C07K19/00 ,  C07K2317/52 ,  C07K2317/732 ,  C07K2317/734 ,  C07K2319/30

Abstract: The present invention relates to an insulinotropic peptide conjugate having improved in-vivo duration of efficacy and stability, comprising an insulinotropic peptide, a non-peptide polymer and a carrier substance, which are covalently linked to each other, and a use of the same. The insulinotropic peptide conjugate of the present invention has the in-vivo activity which is maintained relatively high, and has remarkably increased blood half-life, and thus it can be desirably employed in the development of long acting formulations of various peptide drugs.

Abstract translation: 本发明涉及具有改善的功效和稳定性的体内持续时间的促胰岛素肽缀合物，其包含彼此共价连接的促胰岛素肽，非肽聚合物和载体物质及其用途。 本发明的促胰岛素肽缀合物具有保持较高的体内活性，并且血液半衰期显着增加，因此可以理想地用于开发各种肽药物的长效制剂。

公开(公告)号：US20080009509A1

公开(公告)日：2008-01-10

申请号：US11722096

申请日：2005-12-20

Applicant: Young Jin Ham ,  Ji Hyeon Gong ,  Mi Yong Cha ,  Jong Woo Kim ,  Maeng Sup Kim ,  Eun Young Kim ,  Ji Yeon Song ,  Chang In Kim ,  Se Young Kim ,  Gwan Sun Lee

Inventor： Young Jin Ham ,  Ji Hyeon Gong ,  Mi Yong Cha ,  Jong Woo Kim ,  Maeng Sup Kim ,  Eun Young Kim ,  Ji Yeon Song ,  Chang In Kim ,  Se Young Kim ,  Gwan Sun Lee

IPC: C07D239/94 ,  A61K31/517 ,  A61P35/00

CPC classification number: C07D403/12 ,  C07D239/94 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12

Abstract: The present invention relates to a novel quinazoline derivative and a pharmaceutically acceptable salt thereof for inhibiting the growth of cancer cells, a method for the preparation thereof and a pharmaceutical composition comprising same as an active ingredient.

Abstract translation: 本发明涉及用于抑制癌细胞生长的新型喹唑啉衍生物及其药学上可接受的盐，其制备方法和包含该活性成分的药物组合物。

公开(公告)号：US07084274B2

公开(公告)日：2006-08-01

申请号：US10524922

申请日：2003-08-13

Applicant: Young-Ho Moon ,  Kyung-Ik Lee ,  Gha-Seung Park ,  Chul-Hyun Park ,  Jae-Cheol Lee ,  Gwan-Sun Lee ,  Young-Kil Chang

Inventor： Young-Ho Moon ,  Kyung-Ik Lee ,  Gha-Seung Park ,  Chul-Hyun Park ,  Jae-Cheol Lee ,  Gwan-Sun Lee ,  Young-Kil Chang

IPC: C07D221/18 ,  C07D221/02

CPC classification number: C07J73/005 ,  C07D221/18

Abstract: This invention relates to a method for selectively preparing the 3-oxo-4-aza-5¥á-androstane compound which is used as an intermediate of finasteride by heating 3-oxo-4-aza-5-androstene in a mixture of formic acid and an alkanediol in the presence of zinc.

Abstract translation: 本发明涉及选择性制备3-氧代-4-氮杂-5α-雄甾烷化合物的方法，该化合物通过将3-氧代-4-氮杂-5-雄甾烯在甲酸的混合物中加热而用作非那雄胺的中间体 酸和链烷二醇在锌的存在下。

公开(公告)号：US20060019979A1

公开(公告)日：2006-01-26

申请号：US10524922

申请日：2003-08-13

Applicant: Young-Ho Moon ,  Kyung-Ik Lee ,  Gha-Seung Park ,  Chul-Hyun Park ,  Jae-Cheol Lee ,  Gwan-Sun Lee ,  Young-kil Chang

Inventor： Young-Ho Moon ,  Kyung-Ik Lee ,  Gha-Seung Park ,  Chul-Hyun Park ,  Jae-Cheol Lee ,  Gwan-Sun Lee ,  Young-kil Chang

IPC: C07D221/18 ,  A61K31/473

CPC classification number: C07J73/005 ,  C07D221/18

Abstract: This invention relates to a method for selectively preparing the 3-oxo-4-aza-5¥á-androstane compound which is used as an intermediate of finasteride by heating 3-oxo-4-aza-5-androstene in a mixture of formic acid and an alkanediol in the presence of zinc.

Abstract translation: 本发明涉及选择性制备3-氧代-4-氮杂-5α-雄甾烷化合物的方法，该化合物通过将3-氧代-4-氮杂-5-雄甾烯在甲酸的混合物中加热而用作非那雄胺的中间体 酸和链烷二醇在锌的存在下。

公开(公告)号：US20060004024A1

公开(公告)日：2006-01-05

申请号：US10531299

申请日：2003-10-17

Applicant: Nam-Du Kim ,  Jae-Heon Lee ,  Moon-Sub Lee ,  Young-Kil Chang ,  Gwan-Sun Lee

Inventor： Nam-Du Kim ,  Jae-Heon Lee ,  Moon-Sub Lee ,  Young-Kil Chang ,  Gwan-Sun Lee

IPC: A61K31/519 ,  C07D487/04

CPC classification number: C07D471/04

Abstract: Risperidone is prepared in a high yield by reacting 2,4-difluorophenyl(4-piperidinyl)methanone oxime hydrochloride and 3-(2-chloroethyl)-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one in an aqueous alkali hydroxide solution having an alkali hydroxide concentration in the range of 20 to 40%.

Abstract translation: 通过使2,4-二氟苯基（4-哌啶基）甲酮肟盐酸盐和3-（2-氯乙基）-6,7,8,9-四氢-2-甲基-4H-吡啶并[1 ，2-a]嘧啶-4-酮在碱金属氢氧化物浓度为20〜40％范围内的碱金属氢氧化物水溶液中。

公开(公告)号：US06900245B2

公开(公告)日：2005-05-31

申请号：US10678325

申请日：2003-10-03

Applicant: Jae-Heon Lee ,  Gha-Seung Park ,  Jae-Cheol Lee ,  Han-Kyong Kim ,  Young-Kil Chang ,  Gwan-Sun Lee

Inventor： Jae-Heon Lee ,  Gha-Seung Park ,  Jae-Cheol Lee ,  Han-Kyong Kim ,  Young-Kil Chang ,  Gwan-Sun Lee

IPC: A61K31/13 ,  A61K31/205

CPC classification number: A61K31/205 ,  C30B7/00

Abstract: The present invention relates to a pharmaceutical composition for treating or preventing obesity, comprising novel crystalline sibutramine methanesulfonate hemihydrate of formula (I). The crystalline sibutramine methanesulfonate hemihydrate according to the present invention has a much higher solubility in water, and enhanced stability under a high humidity/temperature condition, as compared with sibutramine hydrochloride monohydrate

Abstract translation: 本发明涉及用于治疗或预防肥胖症的药物组合物，其包含式（I）的新型结晶西布曲明甲磺酸盐半水合物。 与西布曲明盐酸盐一水合物相比，本发明的结晶西布曲明甲磺酸盐半水合物在水中的溶解度高，并且在高湿度/温度条件下提高了稳定性

公开(公告)号：US09422349B2

公开(公告)日：2016-08-23

申请号：US12669372

申请日：2008-07-16

Applicant: Sung Youb Jung ,  Chang Ki Lim ,  Dae Hae Song ,  Sung Min Bae ,  Young Hoon Kim ,  Se Chang Kwon ,  Gwan Sun Lee

Inventor： Sung Youb Jung ,  Chang Ki Lim ,  Dae Hae Song ,  Sung Min Bae ,  Young Hoon Kim ,  Se Chang Kwon ,  Gwan Sun Lee

IPC: C07K14/605 ,  A61K38/26 ,  C07K14/46 ,  C07K14/575

CPC classification number: C07K14/46 ,  A61K38/26 ,  C07K14/57563 ,  C07K14/605

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US08957196B2

公开(公告)日：2015-02-17

申请号：US12444567

申请日：2007-10-16

Applicant: In Young Choi ,  Chang Hwan Kim ,  Hyun Ji Lee ,  Seong Hee Park ,  Se Chang Kwon ,  Gwan Sun Lee

Inventor： In Young Choi ,  Chang Hwan Kim ,  Hyun Ji Lee ,  Seong Hee Park ,  Se Chang Kwon ,  Gwan Sun Lee

IPC: C07H21/04 ,  C12N15/63 ,  C12N9/06 ,  C12N15/85

CPC classification number: C12N9/003 ,  C12N15/85 ,  C12N2510/00

Abstract: 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.

Abstract translation: 本文公开了一种可诱导的高表达盒，其包含二氢叶酸还原酶（DHFR）启动子，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。

公开(公告)号：US08846699B2

公开(公告)日：2014-09-30

申请号：US12093108

申请日：2006-11-08

Applicant: Young-Gil Ahn ,  Jong Woo Kim ,  Keuk Chan Bang ,  Bum Woo Park ,  Se Young Kim ,  Kyungik Lee ,  Kyuhang Lee ,  Myoung-Sil Ko ,  Han Kyong Kim ,  Young Hoon Kim ,  Maeng Sup Kim ,  Gwan Sun Lee

Inventor： Young-Gil Ahn ,  Jong Woo Kim ,  Keuk Chan Bang ,  Bum Woo Park ,  Se Young Kim ,  Kyungik Lee ,  Kyuhang Lee ,  Myoung-Sil Ko ,  Han Kyong Kim ,  Young Hoon Kim ,  Maeng Sup Kim ,  Gwan Sun Lee

IPC: A61K31/517 ,  C07D239/94

CPC classification number: C07D239/94

Abstract: The present invention relates to a novel quinazoline derivative compound having the formula (1) as follows: with the constituents defined in claim 1, and a pharmaceutically acceptable salt thereof as a multiplex inhibitor, a method for the preparation thereof, and a pharmaceutical composition and a therapeutic composition comprising same as an active ingredient. The inventive quinazoline derivative as a multiplex inhibitor can selectively and effectively inhibit diseases caused by the overactivity of a tyrosine kinase.

Abstract translation: 本发明涉及一种具有式（1）的新型喹唑啉衍生物化合物，其具有如权利要求1所定义的组分及其药学上可接受的盐作为多重抑制剂，其制备方法和药物组合物， 包含其作为活性成分的治疗组合物。 作为多重抑制剂的本发明喹唑啉衍生物可以选择性和有效地抑制由酪氨酸激酶的过度活性引起的疾病。

公开(公告)号：US08263769B2

公开(公告)日：2012-09-11

申请号：US12669002

申请日：2008-08-04

Applicant: Young Ho Moon ,  Moon Sub Lee ,  Jae Ho Yoo ,  Ji Sook Kim ,  Han Kyong Kim ,  Chang Ju Choi ,  Young Kil Chang ,  Gwan Sun Lee

Inventor： Young Ho Moon ,  Moon Sub Lee ,  Jae Ho Yoo ,  Ji Sook Kim ,  Han Kyong Kim ,  Chang Ju Choi ,  Young Kil Chang ,  Gwan Sun Lee

IPC: C07D403/06 ,  C07D239/38

CPC classification number: C07D403/06

Abstract: 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.

Abstract translation: 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加成型偶联反应 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。