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公开(公告)号：US12209144B2
公开(公告)日：2025-01-28
申请号：US17296679
申请日：2019-11-26
Applicant: Novartis AG
Inventor： Alec Nathanson Flyer , Andrei Alexandrovich Golosov , Philipp Grosche , Ian Lewis , Eugene Yuejin Liu , Andreas Marzinzik , Lauren Gilchrist Monovich , Johannes Ottl , Tajesh Jayprakash Patel , Patrick Crawford Reid , Mohindra Seepersaud
Abstract: The disclosure relates to inhibitors of PCSK9 useful in the treatment of lipid metabolism, and other diseases in which PCSK9 plays a role, having the Formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, stereoisomer, or tautomer thereof, wherein R1, X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, X11, X12, and X13 are described herein.
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Patent Agency Ranking
公开(公告)号：US10005829B2
公开(公告)日：2018-06-26
申请号：US14440198
申请日：2013-11-19
Applicant: Novartis AG
Inventor： Frederic Zecri , Kayo Yasoshima , Philipp Grosche , Jun Yuan , Hongjuan Zhao
IPC: A61K38/10 , C07K14/765 , C07K14/47 , A61K45/06 , A61K38/38
CPC classification number: C07K14/765 , A61K38/385 , A61K45/06 , C07K14/47 , A61K38/1709 , A61K2300/00
Abstract: The invention relates to novel compositions comprising modified apelin-13 peptide sequences designed to treat cardiovascular disease in subjects to whom they are administered, and which exhibit greater resistance to degradation, and equivalent or greater bioactivity than their wild type counterparts. The invention also relates to methods of making said compositions and using said compositions as pharmaceutically active agents to treat cardiovascular disease.
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公开(公告)号：US09982017B2
公开(公告)日：2018-05-29
申请号：US14714914
申请日：2015-05-18
Applicant: Novartis AG
Inventor： Frederic Zecri , Andrei Golosov , Philipp Grosche , Hongjuan Zhao , Qi-Ying Hu , Hidetomo Imase
CPC classification number: A61M16/0816 , A61K38/00 , A61K38/10 , A61M16/0066 , A61M16/201 , A61M2016/0027 , A61M2016/003 , A61M2205/35 , A61M2205/502 , C07K7/08 , C07K7/56 , C07K7/60
Abstract: The invention provides a synthetic polypeptide of Formula I′: or an amide, an ester or a salt thereof, wherein X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, X11, X12 and X13 are defined herein. The polypeptides are agonist of the APJ receptor. The invention also relates to a method for manufacturing the polypeptides of the invention, and its therapeutic uses such as treatment or prevention of acute decompensated heart failure (ADHF), chronic heart failure, pulmonary hypertension, atrial fibrillation, Brugada syndrome, ventricular tachycardia, atherosclerosis, hypertension, restenosis, ischemic cardiovascular diseases, cardiomyopathy, cardiac fibrosis, arrhythmia, water retention, diabetes (including gestational diabetes), obesity, peripheral arterial disease, cerebrovascular accidents, transient ischemic attacks, traumatic brain injuries, amyotrophic lateral sclerosis, burn injuries (including sunburn) and preeclampsia. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
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公开(公告)号：US11813306B2
公开(公告)日：2023-11-14
申请号：US17200471
申请日：2021-03-12
Applicant: NOVARTIS AG
Inventor： Karin Briner , Brian Addison Dechristopher , Alec Nathanson Flyer , Andrei Alexandrovich Golosov , Philipp Grosche , Eugene Yuejin Liu , Justin Yik Ching Mao , Lauren Gilchrist Monovich , Tajesh Jayprakash Patel , Liansheng Su , Lihua Yang , Rui Zheng
Abstract: The disclosure relates to inhibitors of PCSK9 useful in the treatment of cholesterol lipid metabolism, and other diseases in which PCSK9 plays a role, having the Formula (I):
or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, N-oxide, or tautomer thereof, wherein R1, R1, R1, R1, R1, R1, R1, R1, R1, X1, X2, and X3 are described herein.-
公开(公告)号：US11026993B2
公开(公告)日：2021-06-08
申请号：US16695843
申请日：2019-11-26
Applicant: NOVARTIS AG
Inventor： Karin Briner , Brian Addison Dechristopher , Alec Nathanson Flyer , Andrei Alexandrovich Golosov , Philipp Grosche , Eugene Yuejin Liu , Justin Yik Ching Mao , Lauren Gilchrist Monovich , Tajesh Jayprakash Patel , Carina Cristina Sanchez , Liansheng Su , Lihua Yang , Rui Zheng
Abstract: The disclosure relates to inhibitors of PCSK9 useful in the treatment of cholesterol lipid metabolism, and other diseases in which PCSK9 plays a role, having the Formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, N-oxide, or tautomer thereof, wherein R1, R1, R1, R1, R1, R1, R1, R1, R1, X1, X2, and X3 are described herein.
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公开(公告)号：US09908919B2
公开(公告)日：2018-03-06
申请号：US14905333
申请日：2014-07-21
Applicant: Novartis AG
Inventor： Frederic Zecri , Philipp Grosche , Kayo Yasoshima , Hongjuan Zhao , Jun Yuan
IPC: A61K38/10 , A61K38/04 , C07K5/00 , C07K7/00 , C07K16/00 , C07K17/00 , C07K14/47 , A61K38/17 , A61K45/06 , A61K47/64 , A61K47/68
CPC classification number: C07K14/47 , A61K38/10 , A61K38/1709 , A61K45/06 , A61K47/643 , A61K47/6811
Abstract: The invention provides a synthetic polypeptide of Formula I (SEQ ID NO: 1): X1-R-X3-R-L-X6-X7-K-X9-P-X11-X12-X13 I or an amide, an ester, a salt thereof, or a bioconjugate thereof, wherein X1, X3, X6, X7, X9, X11, X12 and X13 are defined herein. The polypeptides and bioconjugates are agonist of the APJ receptor. The invention also relates to a method for manufacturing the polypeptides and bioconjugates of the invention, and its therapeutic uses such as treatment or prevention of acute decompensated heart failure (ADHF), chronic heart failure, pulmonary hypertension, atrial fibrillation, Brugada syndrome, ventricular tachycardia, atherosclerosis, hypertension, restenosis, ischemic cardiovascular diseases, cardiomyopathy, cardiac fibrosis, arrhythmia, water retention, diabetes (including gestational diabetes), obesity, peripheral arterial disease, cerebrovascular accidents, transient ischemic attacks, traumatic brain injuries, amyotrophic lateral sclerosis, burn injuries (including sunburn) and preeclampsia. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
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