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公开(公告)号：US20220339291A1
公开(公告)日：2022-10-27
申请号：US16964965
申请日：2020-03-05
发明人： Chang Sik Park , Min Ji Choi , Tae Ik Jang , Yun-Hee Park , Ho Young Song , Ju Yuel Baek , Sung Min Kim , Hyeun Joung Lee , Ju Young Lee , Hyoung Rae Kim , Kun Jung Lee , Yong Zu Kim , Chang Sun Lee , Jeiwook Chae , Sang Pil Lee , Ji-Young Shin , Sunha Yoon , Yunseon Choi , Jae Eun Park , Jisu Lee , Bum-Chan Park , Young Woo Park
摘要： The present invention relates to new antibody-drug conjugates (ADCs) targeting DLK1, active metabolites of such ADCs, methods for preparation of such ADCs, uses for such ADCs in treatment and/or prevention of illnesses, and uses for such ADCs in production of drugs for treatment and/or prevention of diseases, more specifically, uses for such ADCs in producing drugs for treatment and/or prevention of proliferative and/or angiogenetic diseases, for example, cancer. More particularly, the present invention relates to an antibody-drug conjugate comprising an antibody binding with DLK1 or an antigen-binding fragment thereof, and a pharmaceutical composition comprising the same.
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公开(公告)号：US09919057B2
公开(公告)日：2018-03-20
申请号：US14865778
申请日：2015-09-25
发明人： Yong Zu Kim , Tae Kyo Park , Sung Ho Woo , Sun Young Kim , Jong Un Cho , Doo Hwan Jung , Jeon Yang , Ji Young Min , Hyang Sook Lee , Yun Hee Park , Jeong Hee Ryu , Kyu Man Oh , Yeong Soo Oh , Jeiwook Chae , Ho Young Song , Chul-Woong Chung
IPC分类号： C07D309/10 , A61K47/48 , C07D249/04 , C07K19/00
CPC分类号： A61K47/6871 , A61K47/549 , A61K47/6801 , A61K47/6803 , A61K47/6811 , A61K47/6813 , A61K47/6855 , A61K47/6889 , A61K47/69 , A61K2039/505 , C07D249/04 , C07D487/04 , C07D519/00 , C07K16/32 , C07K19/00 , C07K2317/24
摘要： Provided are compounds comprising a self-immolative group, and the compounds comprising a self-immolative group according to the present invention may include a protein (for example, an oligopeptide, a polypeptide, an antibody, or the like) having substrate-specificity for a target and an active agent (for example, a drug, a toxin, a ligand, a detection probe, or the like) having a specific function or activity.
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3.发明申请METHOD FOR PREPARING (R)-3-(3-FLUORO-4-(1-METHYL-5,6-DIHYDRO-1,2,4-TRIAZIN-4(1H)-YL)PHENYL)-5-(SUBSTITUTED METHYL)OXAZOLIDIN-2-ONE DERIVATIVES 有权制备（R）-3-（3-氟-4-（1-甲基-5,6-二氢-1,2,4-三氮杂-4（1H） - 基）苯基）-5-（取代的甲基） ）OXAZOLIDIN-2-ONE衍生物公开(公告)号：US20130005967A1
公开(公告)日：2013-01-03
申请号：US13583492
申请日：2011-03-08
申请人： Young Lag Cho , Sung Yoon Baek , Sang Eun Chae , Hong Bum Lee , Tae Kyo Park , Sung Ho Woo , Yong Zu Kim
发明人： Young Lag Cho , Sung Yoon Baek , Sang Eun Chae , Hong Bum Lee , Tae Kyo Park , Sung Ho Woo , Yong Zu Kim
IPC分类号： C07D413/10 , C07D253/06
CPC分类号： C07D255/02 , C07D253/06 , C07D413/10
摘要： Provided are a method for preparing (R)-3-(3-fluoro-4-(1-methyl-5,6-dihydro-1,2,4-triazin-4(1H)-yl)phenyl)-5-(substituted methyl)oxazolidin-2-one derivatives, which are oxazolidinone antibiotic compounds having a cyclic amidrazone group, represented by Chemical Formula 1, and intermediates thereof, and uses 3,4-difluoro-4-nitrobenzen as a starting material. According to the preparation method of the present invention, (R)-3-(3-fluoro-4-(1-methyl-5,6-dihydro-1,2,4-triazin-4(1H)-yl)phenyl)-5-(substituted methyl)oxazolidin-2-one derivatives, which are useful as oxazolidinone antibiotics, can be prepared in high purity and high yield in a simpler manner than conventional methods.
摘要翻译： 提供制备（R）-3-（3-氟-4-（1-甲基-5,6-二氢-1,2,4-三嗪-4（1H） - 基）苯基）-5- （取代甲基）恶唑烷-2-酮衍生物，它们是由化学式1表示的具有环状氨基腙基的恶唑烷酮类抗生素化合物及其中间体，并以3,4-二氟-4-硝基苯为起始原料。 根据本发明的制备方法，将（R）-3-（3-氟-4-（1-甲基-5,6-二氢-1,2,4-三嗪-4（1H） - 基）苯基 ）-5-（取代的甲基）恶唑烷-2-酮衍生物可以以比常规方法更简单的方式以高纯度和高产率制备，其可用作恶唑烷酮抗生素。
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公开(公告)号：US20120264727A1
公开(公告)日：2012-10-18
申请号：US13467019
申请日：2012-05-08
申请人： Young Lag CHO , Hye Jin HEO , Kyu Man OH , Hyang Sook LEE , Chul Soon PARK , Sang Eun CHAE , Joung Yul YUN , Hyun Jin KWON , Young Jae YANG , Dae Hyuck KANG , Yong Zu KIM , Sung Ho WOO , Tae Kyo PARK
发明人： Young Lag CHO , Hye Jin HEO , Kyu Man OH , Hyang Sook LEE , Chul Soon PARK , Sang Eun CHAE , Joung Yul YUN , Hyun Jin KWON , Young Jae YANG , Dae Hyuck KANG , Yong Zu KIM , Sung Ho WOO , Tae Kyo PARK
IPC分类号： A61K31/546 , A61P31/04 , C07D501/60
CPC分类号： C07D501/60 , C07D501/24 , C07D501/46
摘要： The present invention relates to novel cephalosporin derivatives represented by Chemical Formula 1. Wherein, X, Y, L, R1, and R2 are as same as defined in the description of the invention.The present invention also relates to pharmaceutical antibiotic compositions comprising a novel celphalosporin derivative represented by Chemical Formula 1, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof as an effective ingredient.According to the present invention, novel cephalosporin derivatives, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof as an effective ingredient for the broad spectrum of antibiotic resistant, low toxicity, particularly in Gram-negative bacteria, which can be useful with strong antimicrobial activity.
摘要翻译： 本发明涉及由化学式1表示的新型头孢菌素衍生物。其中，X，Y，L，R 1和R 2与本发明的描述中所定义相同。 本发明还涉及药物抗生素组合物，其包含由化学式1表示的新型胞孢素衍生物，其前药，其水合物，其溶剂合物，其异构体或其药学上可接受的盐作为有效成分。 根据本发明，新型头孢菌素衍生物，其前体药物，其水合物，其溶剂化物，其异构体或其药学上可接受的盐作为有效成分，用于广谱抗生素抗性，低毒性，特别是革兰氏阴性 - 阴性细菌，其可用于具有强的抗微生物活性。
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公开(公告)号：US20230123569A1
公开(公告)日：2023-04-20
申请号：US18073120
申请日：2022-12-01
发明人： Dae Yon Lee , Sang Eun Chae , Eun Mi Jung , Eun Hye Yang , Yoon Jeong Choi , Chul-Woong Chung , Ju Hyun Shin , Yun Ki Kim , Hyun Jin Kwon , Jeong Hee Ryu , Eun Hye Ban , Yong Zu Kim , Yeong Soo Oh , Jeiwook Chae
IPC分类号： C07D413/14 , C07D239/42 , C07D401/14 , C07D413/12 , C07D471/04 , C07D471/10 , C07D498/10 , C07D519/00
摘要： The present invention relates to novel compounds as autotoxin inhibitors for treatment and prophylaxis of conditions or a disorder caused by autotaxin activation or increased concentration of lysophosphatidic acid, and also a pharmaceutical composition containing the same.
The novel compounds of the present invention are autotoxin inhibitors, and by inhibiting the production of lysophosphatidic acid, they are useful for treatment or prophylaxis of cardiovascular disorder, cancer, metabolic disorder, kidney disorder, liver disorder, inflammatory disorder, nervous system disorder, respiratory system disorder, fibrotic disease, ocular disorder, cholestatic and other forms of chronic pruritus, or acute or chronic organ transplant rejection.-
公开(公告)号：US11548883B2
公开(公告)日：2023-01-10
申请号：US16098748
申请日：2018-05-15
发明人： Dae Yon Lee , Sang Eun Chae , Eun Mi Jung , Eun Hye Yang , Yoon Jeong Choi , Chul-Woong Chung , Ju Hyun Shin , Yun Ki Kim , Hyun Jin Kwon , Jeong Hee Ryu , Eun Hye Ban , Yong Zu Kim , Yeong Soo Oh , Jeiwook Chae
IPC分类号： C07D413/14 , C07D239/42 , C07D401/14 , C07D413/12 , C07D471/04 , C07D471/10 , C07D498/10 , C07D519/00
摘要： The present invention relates to novel compounds as autotoxin inhibitors for treatment and prophylaxis of conditions or a disorder caused by autotaxin activation or increased concentration of lysophosphatidic acid, and also a pharmaceutical composition containing the same.
The novel compounds of the present invention are autotoxin inhibitors, and by inhibiting the production of lysophosphatidic acid, they are useful for treatment or prophylaxis of cardiovascular disorder, cancer, metabolic disorder, kidney disorder, liver disorder, inflammatory disorder, nervous system disorder, respiratory system disorder, fibrotic disease, ocular disorder, cholestatic and other forms of chronic pruritus, or acute or chronic organ transplant rejection.-
公开(公告)号：US11413353B2
公开(公告)日：2022-08-16
申请号：US15779446
申请日：2016-11-23
发明人： Yong Zu Kim , Yeong Soo Oh , Jeiwook Chae , Ho Young Song , Chul-Woong Chung , Yun Hee Park , Hyo Jung Choi , Kyung Eun Park , Hyoungrae Kim , Jinyeong Kim , Ji Young Min , Sung Min Kim , Byung Soo Lee , Dong Hyun Woo , Ji Eun Jung , Su In Lee
摘要： In some aspects, the invention relates to an antibody-drug conjugate, comprising an antibody; a linker; and an active agent. The antibody-drug conjugate may comprise a self-immolative group. The linker may comprise an O-substituted oxime, e.g., wherein the oxygen atom of the oxime is substituted with a group that covalently links the oxime to the active agent; and the carbon atom of the oxime is substituted with a group that covalently links the oxime to the antibody.
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公开(公告)号：US20220226496A1
公开(公告)日：2022-07-21
申请号：US17607678
申请日：2020-04-29
发明人： Ho Young SONG , Yun-Hee PARK , Sang Eun CHAE , Ju Yuel BAEK , Kyung Eun PARK , Ju Young LEE , Su In LEE , Jeiwook CHAE , Chang Sun LEE , Yong Zu KIM
摘要： The present invention relates to a ligand-drug conjugate including a ligand; a linker that is connected to the ligand by a covalent bond and has a tris structure represented by a specific structural formula; and an active agent connected to the linker by a covalent bond. In the ligand-drug conjugate, the active agent is bound by the tris structure of the linker, and thus a greater number of active agents can be connected through one linker. Accordingly, a greater number of active agents per antibody binding can be delivered to the target cell, and the drug and/or toxin can stably reach the target cell and effectively exert the drug efficacy.
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公开(公告)号：US20170088614A1
公开(公告)日：2017-03-30
申请号：US15276209
申请日：2016-09-26
发明人： Yong Zu Kim , Yun Hee Park , Jeong Hee Ryu , Ho Young Song , Jeiwook Chae , Chul-Woong Chung , Ji Eun Jung , Hyo Jung Choi
CPC分类号： C07K16/2803 , A61K31/351 , A61K47/6803 , A61K47/6831 , A61K47/6849 , A61K47/6889 , A61K2039/505 , C07D301/10 , C07K2317/24 , C07K2317/73 , C07K2317/92 , C07K2317/94 , Y02A50/475
摘要： In some aspects, the invention relates to an antibody-drug conjugate, comprising an anti-CD19 antibody; a linker; and an active agent. The antibody-drug conjugate may comprise a self-immolative group. The linker may comprise an O-substituted oxime, e.g., wherein the oxygen atom of the oxime is substituted with a group that covalently links the oxime to the active agent; and the carbon atom of the oxime is substituted with a group that covalently links the oxime to the antibody.
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公开(公告)号：US20140161829A1
公开(公告)日：2014-06-12
申请号：US14181648
申请日：2014-02-15
发明人： Yongzu Kim , Taekyo Park , Sungho Woo , Hyangsook Lee , Sunyoung Kim , Jongun Cho , Doohwan Jung , Youngun Kim , Hyunjin Kwon , Kyuman Oh , Yunseo Chung , Yun-Hee Park
IPC分类号： A61K47/48
CPC分类号： A61K47/6811 , A61K47/549 , A61K47/55 , A61K47/65 , A61K47/6803 , A61K47/6817 , A61K47/6849 , A61K47/6851 , A61K47/6855 , A61K47/6859 , A61K47/6889 , C07K16/2863 , C07K16/32 , C12Q1/48
摘要： The invention provides protein-active agent conjugates having an amino acid motif that can be recognized by an isoprenoid transferase. The invention also provides compositions containing the conjugates. The invention further provides methods for using the conjugates to deliver the active agent to a target cell, as well as methods for using the conjugates to treat a subject in need thereof (e.g., a subject in need of the active agent).
摘要翻译： 本发明提供了具有可被类异戊二烯转移酶识别的氨基酸基序的蛋白质 - 活性剂缀合物。 本发明还提供含有缀合物的组合物。 本发明还提供了使用结合物将活性剂递送至靶细胞的方法，以及使用缀合物治疗有此需要的受试者（例如需要活性剂的受试者）的方法。
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