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公开(公告)号：US20210284694A1
公开(公告)日：2021-09-16
申请号：US17253864
申请日：2019-06-20
发明人： Alonso Ricardo , Thomas Joseph Tucker , Nicolas Cedric Boyer , Joseph R. Stringer , Derek M. LaPlaca , Angela Dawn Kerekes , Chengwei Wu , Sookhee Nicole Ha , Hyewon Youm , Mark W. Embrey , Elisabetta Bianchi , Danila Branca , Raffaele Ingenito , Willy Costantini , Alessia Santoprete , Roberto Costante , Immacolata Conte , Stefania Colarusso , Eric J. Gilbert , Aurash Shahripour , Yusheng Xiong
IPC分类号： C07K7/64
摘要： Provided herein are cyclic polypeptide compounds that can, e.g., bind specifically to human proprotein convertase subtilisin/kexin type 9 (PCSK9) and optionally also inhibit interaction between human PCSK9 and human low density lipoprotein receptor (LDLR), and pharmaceutical compositions comprising one or more of these compounds. Also provided are methods of reducing LDL cholesterol level in a subject in need thereof that include administering to the subject one or more of the cyclic polypeptide compounds or a pharmaceutical composition provided herein.
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公开(公告)号：US11306125B2
公开(公告)日：2022-04-19
申请号：US17253815
申请日：2019-06-20
发明人： Yusheng Xiong , Thomas Joseph Tucker , Chengwei Wu , Elisabetta Bianchi , Danila Branca , Angela Dawn Kerekes , Abbas M. Walji , Hubert B. Josien , Fa-Xiang Ding , Hyewon Youm , Alessia Santoprete , Raffaele Ingenito
摘要： Disclosed are compounds of Formula I, or a salt thereof cyclic polypeptide of Formula I: Formula I where A, B, E, R4, and R8 are as defined herein, which compounds have properties for antagonizing PCSK9. Also described are pharmaceutical formulations comprising the compounds of Formula I or their salts, and methods of treating cardiovascular disease and conditions related to PCSK9 activity, e.g. atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, acute coronary syndrome, or related cardiovascular disease and cardiometabolic conditions
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公开(公告)号：US09593155B2
公开(公告)日：2017-03-14
申请号：US14686760
申请日：2015-04-14
申请人： MERCK SHARP & DOHME CORP. , ISTITUTO DI RICERCHE DI BIOLOGIA P. ANGELETTI S.R.L. , INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION
发明人： Paul E. Carrington , George J. Eiermann , Donald J. Marsh , Joseph M. Metzger , Alessandro Pocai , Ranabir Sinha Roy , Elisabetta Bianchi , Paolo Ingallinella , Antonello Pessi , Alessia Santoprete , Elena Capito , Richard Dimarchi , Brian Ward
IPC分类号： C07K14/605 , A61K38/00 , C07K14/575
CPC分类号： C07K14/605 , A61K38/00 , C07K14/575
摘要： Peptide analogs of oxyntomodulin (OXM, glucagon-37), which have been modified to be resistant to cleavage and inactivation by dipeptidyl peptidase IV (DPP-IV) and to increase in vivo half-life of the peptide analog while enabling the peptide analog to act as a dual GLP-1/glucagon receptor (GCGR) agonist are described. The peptide analogs are useful for treatment of metabolic disorders such as diabetes and obesity.
摘要翻译： 已经修饰为对二肽基肽酶IV（DPP-IV）的切割和失活具有抗性并且增加肽类似物的体内半衰期的胃泌酸调节蛋白（OXM，胰高血糖素-37）的肽类似物， 作为双重GLP-1 /胰高血糖素受体（GCGR）激动剂。 肽类似物可用于治疗代谢性疾病如糖尿病和肥胖症。
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公开(公告)号：US20210214395A1
公开(公告)日：2021-07-15
申请号：US17253815
申请日：2019-06-20
发明人： Yusheng Xiong , Thomas Joseph Tucker , Chengwei Wu , Elisabetta Bianchi , Danila Branca , Angela Dawn Kerekes , Abbas M. Walji , Hubert B. Josien , Fa-Xiang Ding , Hyewon Youm , Alessia Santoprete , Raffaele Ingenito
IPC分类号： C07K7/56
摘要： Disclosed are compounds of Formula I, or a salt thereof cyclic polypeptide of Formula I: Formula I where A, B, E, R4, and R8 are as defined herein, which compounds have properties for antagonizing PCSK9. Also described are pharmaceutical formulations comprising the compounds of Formula I or their salts, and methods of treating cardiovascular disease and conditions related to PCSK9 activity, e.g. atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, acute coronary syndrome, or related cardiovascular disease and cardiometabolic conditions
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