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公开(公告)号：EP3156424A4
公开(公告)日：2018-01-24
申请号：EP15799360
申请日：2015-05-27
发明人： KIM YONG ZU , PARK TAE KYO , WOO SUNG HO , KIM SUN YOUNG , CHO JONG UN , JUNG DOO HWAN , YANG JEON , MIN JI YOUNG , LEE HYANG SOOK , PARK YUN HEE , RYU JEONG HEE , OH KYU MAN , OH YEONG SOO , CHAE JEIWOOK , SONG HO YOUNG , CHUNG CHUL-WOONG
CPC分类号： A61K47/48715 , A61K47/48 , A61K47/48092 , A61K47/48338 , A61K47/48384 , A61K47/48415 , A61K47/48584 , A61K47/48646 , A61K47/549 , A61K47/6803 , A61K47/6855 , A61K47/6889 , 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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2.发明公开NOVEL CRYSTALLINE FORM OF 5-CHLORO-N-({(5S)-2-OXO-3-[4-(5,6-DIHYDRO-4H-[1,2,4]TRIAZIN-1-YL)PHENYL]-1,3-OXAZOLIDIN-5-YL}METHYL)THIOPHENE-2-CARBOXAMIDE METHANESULFONATE AND PHARMACEUTICAL COMPOSITION CONTAINING SAME 审中-公开5-氯基-N-新结晶形式 - （{（5S）-2-氧代-3- [4-（5,6-二氢-4H- [1,2,4]三嗪-1-基）苯基] - 1,3-恶唑烷-5-基}甲基）噻吩-2-甲酰胺甲磺酸盐和SO的药物组合物
公开(公告)号：EP3170819A1
公开(公告)日：2017-05-24
申请号：EP14897871.1
申请日：2014-07-18
发明人： CHOI, Soongyu , CHOI, Jungsub , YOON, So-Hyun , KIM, Yoo Hoon , KIM, Jae Yeon , LEE, Suk Ho , CHO, Young Lag , SONG, Ho Young , LEE, Dae Yon , BAEK, Sung Yoon , CHAE, Sang Eun , PARK, Tae Kyo , WOO, Sung Ho , KIM, Yong Zu
IPC分类号： C07D413/14 , C07D413/10 , A61K31/53 , A61P9/10 , A61P29/00
CPC分类号： C07D413/14 , A61K31/53 , A61P7/02 , A61P9/00 , A61P29/00 , C07B2200/13 , C07D253/065 , C07D409/10
摘要： The present invention relates to a novel crystalline form of 5-chloro-N-({(5S)-2-oxo-3-[4-(5,6-dihydro-4H-[1,2,4]triazin-1-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene-2-carboxamide methanesulfonate and a pharmaceutical composition containing the same. The novel crystalline form of a compound according to the present invention exhibits excellent stability even in high-temperature and humidity environments, and thus can be favorably used to prevent or treat diseases, such as thrombosis, myocardial infarction, atherosclerosis, inflammation, stroke, angina pectoris, restenosis after angioplasty, and thromboembolism. (FR)La présente invention concerne une nouvelle forme cristalline de methanesulfonate de 5-chloro-N-({(5S)-2-oxo-3-[4-(5,6-dihydro-4H-[1,2,4]triazin-1-yl)phenyl]-1,3-oxazolidin-5-yl}méthyl)thiophène-2-carboxamide et une composition pharmaceutique le contenant. La nouvelle forme cristalline d'un compose selon la présente invention présente une excellente stabilité, même dans des environnements à haute temperature et haute humidité et peut donc etre utilisée favorablement pour prévenir ou traiter des maladies, telles qu'une thrombose, un infarctus du myocarde, l'athérosclérose, une inflammation, un AVC, une angine de poitrine, une resténose après angioplastie et la thromboembolie.
摘要翻译： 本发明涉及5-氯-N新结晶形式 - （{（5S）-2-氧代-3- [4-（5,6-二氢-4H- [1,2,4]三嗪-1 基）苯基] -1,3-恶唑烷-5-基}甲基）噻吩-2-甲酰胺甲磺酸盐和含有其的药物组合物。 雅鼎的化合物在本发明的新的结晶形式，表现出优异的稳定性，即使在高温和高湿度的环境中，并因此可以有利地用于预防或治疗疾病，：如血栓形成，心肌梗死，动脉粥样硬化，炎症，中风，心绞痛 心绞痛，血管成形术，和血栓栓塞后的再狭窄。 （FR）的LaprésenteUNE努韦勒发明concerne印版晶质DE DE甲磺酸盐5-氯-N - （{（5S）-2-氧代-3- [4-（5,6-二氢-4H- [1,2,4 ]三嗪-1-基）苯基] -1,3-恶唑烷-5-基}甲基）噻吩-2-甲酰胺等UNE组合物pharmaceutique勒contenant。 香格里拉中篇小说印版晶质科特迪瓦联合国组成，聚赛龙拉présente发明présenteUNE excellentestabilité，即使得到丹斯DES Environnementsà高级温度等高级humidité等peut donc理由utiliséefavorablement倒鸥prévenirtraiter DES疾病，特列斯qu'une血栓形成，取消你myocarde梗死 ，动脉粥样硬化L'，炎症UNE，未AVC，UNE angine德poitrine，UNE再狭窄滑雪后angioplastie等LA血栓栓塞。
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公开(公告)号：EP2706062A2
公开(公告)日：2014-03-12
申请号：EP12765589.2
申请日：2012-03-29
发明人： CHO, Young Lag , YUN, Joung Yul , PARK, Chul Soon , CHAE, Sang Eun , LEE, Hyang Sook , OH, Kyuman , HEO, Hye Jin , KANG, Dae Hyuck , YANG, Young Jae , KWON, Hyun Jin , PARK, Tae Kyo , WOO, Sung Ho , KIM, Yong Zu
IPC分类号： C07D501/34 , A61K31/546 , A61P31/00
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, R 1 , and R 2 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与本发明的说明书中所定义相同。 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，其溶剂化物，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，其溶剂合物，其异构体或其药学上可接受的盐作为广谱抗生素抗性，低毒性，特别是革兰氏阳性的有效成分 - 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：EP2692727A2
公开(公告)日：2014-02-05
申请号：EP12764499.5
申请日：2012-03-29
发明人： CHO, Young Lag , BAEK, Sung Yoon , CHAE, Sang Eun , KIM, Sun Young , LEE, Hong Bum , LEE, Hyang Sook , OH, Kyuman , HEO, Hye Jin , PARK, Tae Kyo , WOO, Sung Ho , KIM, Yong Zu
IPC分类号： C07D413/14 , A61K31/53 , A61P31/04
CPC分类号： C07D413/14
摘要： Disclosed is a novel oxazolidinone derivative represented by Formula 1 above, in particular, a novel oxazolidinone compound having a cyclic amidoxime or cyclic amidrazone group.
In Formula 1, R and Q are the same as defined in the detailed description.
In addition, disclosed is a pharmaceutical composition for an antibiotic which includes the novel oxazolidinone derivative of Formula 1, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof as an active ingredient.
The novel oxazolidinone derivative, the prodrug thereof, the hydrate thereof, the solvate thereof, the isomer thereof, and the pharmaceutically acceptable salt thereof have broad antibacterial spectrum against resistant bacteria, low toxicity and strong antibacterial effects against Gram-positive and Gram-negative bacteria and thus may be effectively used as antibiotics.-
公开(公告)号：EP2707031B1
公开(公告)日：2019-06-26
申请号：EP12782658.4
申请日：2012-05-08
发明人： KIM, Yongzu , PARK, Taekyo , WOO, Sungho , LEE, Hyangsook , KIM, Youngun , CHO, Jongun , JUNG, Doohwan , KIM, Sunyoung , KWON, Hyunjin , OH, Kyuman , CHUNG, Yunseo , PARK, Yun-hee
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公开(公告)号：EP3380125A1
公开(公告)日：2018-10-03
申请号：EP16868095.7
申请日：2016-11-23
发明人： KIM, Yong Zu , OH, Yeong Soo , CHAE, Jeiwook , SONG, Ho Young , CHUNG, Chul-Woong , PARK, Yun Hee , CHOI, Hyo Jung , PARK, Kyung Eun , KIM, Hyoungrae , KIM, Jinyeong , MIN, Ji Young , KIM, Sung Min , LEE, Byung Soo , WOO, Dong Hyun , JUNG, Ji Eun , LEE, Su In
CPC分类号： A61K47/6863 , A61K47/6803 , A61K47/6855 , A61K47/6857 , A61K47/6889
摘要： In some aspects, the invention relates to an antibody-drug conjugate, comprising an antibody; a linker; and at least two active agents. In preferred embodiments, the linker comprises a peptide sequence of a plurality of amino acids, and at least two of the active agents are covalently coupled to side chains of the amino acids. The antibody-drug conjugate may comprise a self-immolative group, preferably two-self-immolative groups. 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：EP3356357A1
公开(公告)日：2018-08-08
申请号：EP16850453.8
申请日：2016-09-30
发明人： CHANG, Hye, Kyung , BAEK, Sung, Yoon , KIM, Min, Jung , OH, Kyu, Man , CHOI, Jeung, Soon , HA, Soo, Bong , KIM, Sung, Min , CHUNG, Chul-Woong , KANG, Dae, Hyuck , KWON, Hyun, Jin , CHO, Young, Lag , KIM, Yong, Zu
IPC分类号： C07D413/04 , C07D471/08 , C07D487/08 , A61K31/437 , A61K31/42
CPC分类号： C07D471/08 , A61K31/46 , C07D519/00
摘要： Substituted dihydroisoxazole derivatives useful as inhibitors of β-lactamases are provided. The invention further provides medical uses of substituted dihydroisoxazole derivatives, for example, as antibacterial agents.
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公开(公告)号：EP2706062B1
公开(公告)日：2018-05-09
申请号：EP12765589.2
申请日：2012-03-29
发明人： CHO, Young Lag , YUN, Joung Yul , PARK, Chul Soon , CHAE, Sang Eun , LEE, Hyang Sook , OH, Kyuman , HEO, Hye Jin , KANG, Dae Hyuck , YANG, Young Jae , KWON, Hyun Jin , PARK, Tae Kyo , WOO, Sung Ho , KIM, Yong Zu
IPC分类号： C07D501/34 , A61K31/546 , A61P31/00 , C07D501/24 , C07D501/46
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, R 1 , and R 2 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.
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9.发明授权NOVEL OXAZOLIDINONE DERIVATIVES WITH CYCLIC AMIDOXIME OR CYCLIC AMIDRAZONE AND PHARMACEUTICAL COMPOSITIONS THEREOF 有权与环偕胺肟或环状脒腙和药物组合物的新型恶唑烷酮衍生物
公开(公告)号：EP2331529B1
公开(公告)日：2014-11-05
申请号：EP09816393.4
申请日：2009-09-22
发明人： CHO, Young Lag , CHAE, Sang Eun , BAEK, Sung Yoon , KIM, Yeon Ok , KIM, Seong Jin , LEE, Hyang Sook , PARK, Ju Hyun , PARK, Tae Kyo , WOO, Sung Ho , KIM,Yong Zu
IPC分类号： C07D403/08 , A61K31/497 , A61K31/53 , A61P31/04
CPC分类号： C07D403/08
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公开(公告)号：EP4321180A1
公开(公告)日：2024-02-14
申请号：EP22781627.9
申请日：2022-03-30
摘要： The present disclosure relates to a novel antibody-drug conjugate (ADC) targeting claudin 18 isoform 2 (CLDN18.2), an active metabolite of the ADC, a method of producing the ADC, use of the ADC for the treatment and/or prevention of diseases, and use of the ADC for producing a drug for the treatment and/or prevention of diseases, more specifically hyperproliferative and/or angiogenic diseases, for example, cancer, and more particularly, to an antibody-drug conjugate including a novel antibody or antigen-binding fragment thereof that binds to CLDN18.2, and a pharmaceutical composition including the same.
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