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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：US20210163538A1
公开(公告)日：2021-06-03
申请号：US17253783
申请日：2019-06-20
发明人： Alonso Ricardo , Thomas Joseph Tucker , Nicolas Cedric Boyer , Ketki Ashok Dhamnaskar , Zhong Ma , Angela Dawn Kerekes , Chengwei Wu , Sookhee Nicole Ha , Hyewon Youm , Elisabetta Bianchi , Danila Branca , Raffaele Ingenito , Willy Costantini , 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：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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公开(公告)号：US11932705B2
公开(公告)日：2024-03-19
申请号：US17898220
申请日：2022-08-29
发明人： Alonso Ricardo , Thomas Joseph Tucker , Nicolas Cedric Boyer , Ketki Ashok Dhamnaskar , Zhong Ma , Angela Dawn Kerekes , Chengwei Wu , Sookhee Nicole Ha , Hyewon Youm , Elisabetta Bianchi , Danila Branca , Raffaele Ingenito , Willy Costantini , Aurash Shahripour , Yusheng Xiong
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：US11530244B2
公开(公告)日：2022-12-20
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
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：US20230122330A1
公开(公告)日：2023-04-20
申请号：US17898220
申请日：2022-08-29
发明人： Alonso Ricardo , Thomas Joseph Tucker , Nicolas Cedric Boyer , Ketki Ashok Dhamnaskar , Zhong Ma , Angela Dawn Kerekes , Chengwei Wu , Sookhee Nicole Ha , Hyewon Youm , Elisabetta Bianchi , Danila Branca , Raffaele Ingenito , Willy Costantini , 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：US11505575B2
公开(公告)日：2022-11-22
申请号：US17253783
申请日：2019-06-20
发明人： Alonso Ricardo , Thomas Joseph Tucker , Nicolas Cedric Boyer , Ketki Ashok Dhamnaskar , Zhong Ma , Angela Dawn Kerekes , Chengwei Wu , Sookhee Nicole Ha , Hyewon Youm , Elisabetta Bianchi , Danila Branca , Raffaele Ingenito , Willy Costantini , Aurash Shahripour , Yusheng Xiong
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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