公开(公告)号：US20180326079A1

公开(公告)日：2018-11-15

申请号：US15985060

申请日：2018-05-21

申请人： NOVARTIS AG

发明人： 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分类号： 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

摘要： 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：US20240066132A1

公开(公告)日：2024-02-29

申请号：US18352345

申请日：2023-07-14

申请人： NOVARTIS AG

发明人： 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分类号： 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分类号： 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

摘要： 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：US20220387602A1

公开(公告)日：2022-12-08

申请号：US17642285

申请日：2020-09-14

申请人： NOVARTIS AG

发明人： Luca ARISTA ,  Valerie BROENNIMANN ,  Pier Luca D'ALESSANDRO ,  Lionel DOUMAMPOUOM-METOUL ,  Marie-Line GOUDE ,  Christina HEBACH ,  Gregory John HOLLINGWORTH ,  Ingrid Karen Jennifer JEULIN ,  Louise Clare KIRMAN ,  Julien LORBER ,  Fupeng MA ,  Anna VULPETTI ,  Ken YAMADA ,  Thomas ZOLLER

IPC分类号： A61K47/55 ,  A61K47/54

摘要： Described herein are bifunctional degrader compounds, their various targets, their preparation, pharmaceutical compositions comprising them, and their use in the treatment of conditions, diseases, and disorders mediated by various target proteins.

公开(公告)号：US20210000964A1

公开(公告)日：2021-01-07

申请号：US16889201

申请日：2020-06-01

申请人： NOVARTIS AG

发明人： 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分类号： 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

摘要： 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.