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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：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：US20180037623A1
公开(公告)日：2018-02-08
申请号：US15532634
申请日：2015-12-02
Applicant: Novartis AG
Inventor： Donglin GUO , Chikwendu IBEBUNJO
CPC classification number: C07K14/50 , A61K38/00 , C07K2319/00 , C07K2319/30 , C12N9/2402 , C12N15/62 , C12Y302/01031
Abstract: The present disclosure is directed to compositions and methods related to an alpha sKlotho variant or fragment, in which 1 to up to about 20 amino acids have been deleted from the C-terminus, optionally also having mutations at V563 and/or K795. The present disclosure also pertains to an alpha sKlotho polypeptide variant or fragment, having mutations at V563 and/or K795, wherein the polypeptide variant or fragment is full-length, or optionally 1 to up to about 20 amino acids have been deleted from the C-terminus. The present disclosure also pertains to fusion polypeptides comprising: (a) an alpha sKlotho, in which 1 to up to about 20 amino acids have been deleted from the C-terminus, optionally also having mutations at V563 and/or K795; (b) a linker; and (c) FGF23, optionally having a mutation at R179, C206 and/or C244, or (c) serum albumin.
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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.
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