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公开(公告)号：US20180326079A1
公开(公告)日：2018-11-15
申请号：US15985060
申请日：2018-05-21
Applicant: NOVARTIS AG
Inventor： David Weninger BARNES , Avirup BOSE , Alexandra Marshall BRUCE , Alokesh DUTTAROY , Chikwendu IBEBUNJO , Aaron KANTER , Louise Clare KIRMAN , Changgang LOU , Aimee Richardson USERA , Ken YAMADA , Jun YUAN , Frederic ZECRI
IPC: A61K47/54 , C07C55/02 , A61K38/08 , C12N15/113 , C07C59/245 , C07C57/18 , C07C57/02 , C07C55/22 , A61K45/06 , A61K38/22 , A61K38/18 , A61K38/17 , A61K38/16
Abstract: The invention provides a conjugate comprising a biomolecule linked to a fatty acid via a linker wherein the fatty acid has the following Formulae A1, A2 or A3: wherein R1, R2, R3, R4, Ak, n, m and p are defined herein. The invention also relates to a method for manufacturing the conjugate of the invention such as GDF15 conjugate, and its therapeutic uses such as treatment or prevention of metabolic disorders or diseases, type 2 diabetes mellitus, obesity, pancreatitis, dyslipidemia, alcoholic and nonalcoholic fatty liver disease/steatohepatitis and other progressive liver diseases, insulin resistance, hyperinsulinemia, glucose intolerance, hyperglycemia, metabolic syndrome, hypertension, cardiovascular disease, atherosclerosis, peripheral arterial disease, stroke, heart failure, coronary heart disease, diabetic complications (including but not limited to chronic kidney disease), neuropathy, gastroparesis and other metabolic disorders. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
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公开(公告)号：US20210000964A1
公开(公告)日：2021-01-07
申请号：US16889201
申请日：2020-06-01
Applicant: NOVARTIS AG
Inventor： David Weninger BARNES , Avirup BOSE , Alexandra Marshall BRUCE , Alokesh DUTTAROY , Chikwendu IBEBUNJO , Aaron KANTER , Louise Clare KIRMAN , Changgang LOU , Aimee Richardson USERA , Ken YAMADA , Jun YUAN , Frederic ZECRI
IPC: A61K47/54 , A61K38/095 , A61K38/08 , A61K38/16 , A61K38/17 , A61K38/18 , A61K38/22 , A61K45/06 , C07C55/02 , C07C55/22 , C07C57/02 , C07C57/18 , C07C59/245 , C12N15/113
Abstract: The invention provides a conjugate comprising a biomolecule linked to a fatty acid via a linker wherein the fatty acid has the following Formulae A1, A2 or A3: wherein R1, R2, R3, R4, Ak, n, m and p are defined herein. The invention also relates to a method for manufacturing the conjugate of the invention such as GDF15 conjugate, and its therapeutic uses such as treatment or prevention of metabolic disorders or diseases, type 2 diabetes mellitus, obesity, pancreatitis, dyslipidemia, alcoholic and nonalcoholic fatty liver disease/steatohepatitis and other progressive liver diseases, insulin resistance, hyperinsulinemia, glucose intolerance, hyperglycemia, metabolic syndrome, hypertension, cardiovascular disease, atherosclerosis, peripheral arterial disease, stroke, heart failure, coronary heart disease, diabetic complications (including but not limited to chronic kidney disease), neuropathy, gastroparesis and other metabolic disorders. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
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公开(公告)号：US20220249614A1
公开(公告)日：2022-08-11
申请号：US17720555
申请日：2022-04-14
Applicant: NOVARTIS AG
Inventor： William CHUTKOW , John Richard Neville HADCOCK , Kurt Alex HELDWEIN , Aimee Richardson USERA
Abstract: The disclosure relates to the treatment of non-alcoholic fatty liver disease (NAFLD) and non-alcoholic steatohepatitis (NASH), as well as end-stage liver disease, hepatic steatosis (fatty liver), liver fibrosis, liver inflammation, liver cirrhosis, primary biliary cirrhosis (PBC), and hepatocellular carcinoma (HCC), by administering to a subject in need a GDF15 protein or a functional variant, mutation, fusion, or conjugate thereof, and to pharmaceutical compositions that contain the same.
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Patent Agency Ranking
公开(公告)号：US20220089639A1
公开(公告)日：2022-03-24
申请号：US17228284
申请日：2021-04-12
Applicant: Novartis AG
Inventor： Aimee Richardson USERA , Zachary Hayes ROBINSON , Jennifer Stroka COBB
IPC: C07K5/103 , C07K5/083 , C07K5/062 , A61K49/00 , C07C271/22 , C07C317/28 , C07K1/13 , C07K5/072 , A61K47/64 , C07D229/02 , C07D257/08 , C07D209/42 , C07K7/02
Abstract: The present invention relates to methods and reagents for use in site-selective modification of proteins having lysine residues with functionalized peptides using a chemoenzymatic microbial transglutaminase-mediated reaction. The functionalized proteins may be used for study or therapeutic uses.
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5.发明申请公开(公告)号：US20190000923A1
公开(公告)日：2019-01-03
申请号：US16064054
申请日：2016-12-20
Applicant: NOVARTIS AG
Inventor： William CHUTKOW , John Richard Neville HADCOCK , Kurt Alex HELDWEIN , Aimee Richardson USERA
Abstract: The disclosure relates to the treatment of non-alcoholic fatty liver disease (NAFLD) and non-alcoholic steatohepatitis (NASH), as well as end-stage liver disease, hepatic steatosis (fatty liver), liver fibrosis, liver inflammation, liver cirrhosis, primary biliary cirrhosis (PBC), and hepatocellular carcinoma (HCC), by administering to a subject in need a GDF15 protein or a functional variant, mutation, fusion, or conjugate thereof, and to pharmaceutical compositions that contain the same.
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公开(公告)号：US20240066132A1
公开(公告)日：2024-02-29
申请号：US18352345
申请日：2023-07-14
Applicant: NOVARTIS AG
Inventor： David Weninger BARNES , Avirup BOSE , Alexandra Marshall BRUCE , Alokesh DUTTAROY , Chikwendu IBEBUNJO , Aaron KANTER , Louise Clare KIRMAN , Changgang LOU , Aimee Richardson USERA , Ken YAMADA , Jun YUAN , Frederic ZECRI
IPC: A61K47/54 , A61K38/095 , A61K38/16 , A61K38/17 , A61K38/18 , A61K38/22 , A61K45/06 , C07C55/02 , C07C55/22 , C07C57/02 , C07C57/18 , C07C59/245 , C12N15/113
CPC classification number: A61K47/543 , A61K47/542 , A61K38/095 , A61K38/164 , A61K38/1709 , A61K38/1825 , A61K38/1841 , A61K38/2221 , A61K45/06 , C07C55/02 , C07C55/22 , C07C57/02 , C07C57/18 , C07C59/245 , C12N15/113 , C12N2310/14 , C12N2310/351
Abstract: The invention provides a conjugate comprising a biomolecule linked to a fatty acid via a linker wherein the fatty acid has the following Formulae A1, A2 or A3:
wherein R1, R2, R3, R4, Ak, n, m and p are defined herein. The invention also relates to a method for manufacturing the conjugate of the invention such as GDF15 conjugate, and its therapeutic uses such as treatment or prevention of metabolic disorders or diseases, type 2 diabetes mellitus, obesity, pancreatitis, dyslipidemia, alcoholic and nonalcoholic fatty liver disease/steatohepatitis and other progressive liver diseases, insulin resistance, hyperinsulinemia, glucose intolerance, hyperglycemia, metabolic syndrome, hypertension, cardiovascular disease, atherosclerosis, peripheral arterial disease, stroke, heart failure, coronary heart disease, diabetic complications (including but not limited to chronic kidney disease), neuropathy, gastroparesis and other metabolic disorders. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.-
公开(公告)号：US20170233443A1
公开(公告)日：2017-08-17
申请号：US15497135
申请日：2017-04-25
Applicant: NOVARTIS AG
Inventor： Alexandra Marshall BRUCE , Philipp GROSCHE , Carla GUIMARAES , Aaron KANTER , Changgang LOU , Aimee Richardson USERA , Kayo YASOSHIMA , Jun YUAN , Frederic Zecri , Hongjuan ZHAO
CPC classification number: C07K14/47 , A61K38/12 , A61K38/1709 , A61K45/06 , A61K47/542 , A61K47/60 , A61K47/643 , A61K47/6811 , C07K7/64 , C07K14/765 , C07K16/461 , C07K2319/30 , C07K2319/31
Abstract: The invention provides a cyclic polypeptide of Formula I (SEQ ID NO: 1): X1-R-X3-X4-L-S-X7-X8-X9-X10-X11-X12-X13 I or an amide, an ester or a salt thereof, or a bioconjugate thereof, wherein X1, X3, X4, 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 or bioconjugates thereof, and their 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：US20170107248A1
公开(公告)日：2017-04-20
申请号：US15318191
申请日：2015-06-18
Applicant: NOVARTIS AG
Inventor： Changgang LOU , Aimee Richardson USERA , Jun YUAN
IPC: C07K1/13 , C07K14/475 , C07K16/00 , C07K1/107
CPC classification number: C07K1/13 , A61K47/542 , A61K47/60 , A61K47/64 , A61K47/68 , A61K51/088 , C07K1/1075 , C07K1/1077 , C07K14/475 , C07K14/705 , C07K16/00 , C07K2319/21 , C07K2319/30 , C07K2319/50
Abstract: The present invention relates to method and reagents for use in site-selective modification of protein and peptide. The site selective modification is a selective derivation of the amino functionality at the N-terminus of the protein or the polypeptide using the presence of a neighboring histidine amino acid to increase the reactivity of the N-terminal amino functionality. The modified proteins or peptides obtained by method of the invention may be used for imaging study or therapeutic uses.
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