Publication number: 20230089867
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 X1, R1, R2, R3, R4, R5, R6, R6?, R7, R7?, R8, R9, R9?, R10, R11, R12, and n are described herein.
Type:
Application
Filed:
November 26, 2019
Publication date:
March 23, 2023
Inventors:
Christopher BECKER, Brian Addison DECHRISTOPHER, Alec Nathanson FLYER, Adam FRIEDMAN, Christian GAMPE, Andrei Alexandrovich GOLOSOV, Philipp GROSCHE, Tyler HARRISON, Qian LIU, Eugene Yuejin LIU, I, Justin Yik Ching MAO, Lauren Gilchrist MONOVICH, Tajesh Jayprakash PATEL, Carina Cristina SANCHEZ, Liansheng SU, Lihua YANG, Rui ZHENG
Publication number: 20220024981
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.
Type:
Application
Filed:
November 26, 2019
Publication date:
January 27, 2022
Inventors:
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
Publication number: 20210252103
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.
Type:
Application
Filed:
March 12, 2021
Publication date:
August 19, 2021
Inventors:
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
Patent number: 11026993
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.
Type:
Grant
Filed:
November 26, 2019
Date of Patent:
June 8, 2021
Assignee:
Novartis AG
Inventors:
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
Publication number: 20200164024
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.
Type:
Application
Filed:
November 26, 2019
Publication date:
May 28, 2020
Inventors:
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
Patent number: 9982017
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.
Type:
Grant
Filed:
May 18, 2015
Date of Patent:
May 29, 2018
Assignee:
NOVARTIS AG
Inventors:
Frederic Zecri, Andrei Golosov, Philipp Grosche, Hongjuan Zhao, Qi-Ying Hu, Hidetomo Imase
Publication number: 20160159871
Abstract: The invention provides a synthetic polypeptide of Formula I?: X1-R-X3-R-L-X6-X7-K-X9-P-X11-X12-X13 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.
Type:
Application
Filed:
July 21, 2014
Publication date:
June 9, 2016
Applicant:
Novartis AG
Inventors:
Frédéric ZECRI, Philipp GROSCHE, Kayo YASOSHIMA, Hongjuan ZHAO, Jun YUAN
Publication number: 20160145309
Abstract: The invention provides a synthetic polypeptide of Formula I?: X1-R-P-R-X5-X6-X7-K-X9-P-X11-X12-X13 or an amide, an ester, a salt or a bioconjugate thereof, wherein X1, X5, X6, X7, X9 and X11 to 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 or 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.
Type:
Application
Filed:
July 21, 2014
Publication date:
May 26, 2016
Applicant:
NOVARTIS AG
Inventors:
Frédéric ZECRI, Philipp GROSCHE, Kayo YASOSHIMA, Hongjuan ZHAO, Jun YUAN