公开(公告)号：US20220387602A1

公开(公告)日：2022-12-08

申请号：US17642285

申请日：2020-09-14

Applicant: NOVARTIS AG

Inventor： 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: A61K47/55 ,  A61K47/54

Abstract: 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

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.

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.

公开(公告)号：US20180111932A1

公开(公告)日：2018-04-26

申请号：US15788248

申请日：2017-10-19

Applicant: NOVARTIS AG

Inventor： Guillaume BARBE ,  Gregory Raymond BEBERNITZ ,  Sicong GENG ,  Hatice Belgin GULGEZE EFTHYMIOU ,  Lv LIAO ,  Fupeng MA ,  Ruowei MO ,  David Thomas PARKER ,  Yunshan PENG ,  Stefan PEUKERT ,  Ken YAMADA ,  Kayo YASOSHIMA

IPC: C07D471/04 ,  A61K31/4375 ,  A61K45/06 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/541 ,  C07F9/6561 ,  A61K31/675

CPC classification number: C07D471/04 ,  A61K31/4375 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/675 ,  A61K45/06 ,  A61P9/06 ,  C07B2200/13 ,  C07F9/6561

Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; Wherein R1, R3-R6, X2 and X3 are as defined herein, a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

公开(公告)号：US20240183076A1

公开(公告)日：2024-06-06

申请号：US18550004

申请日：2022-03-09

Applicant: Novartis AG

Inventor： Asitha Adrian ABEYWARDANE ,  Tushar Dattu APSUNDE ,  Gianluca Nicolas ETIENNE ,  Alessia GAMBARDELLA ,  James Kevin MAINQUIST ,  Andrew J. MEYER ,  Brian MINIE ,  Steven PAULA ,  Dwayne A. L. VICKERS ,  Ken YAMADA

IPC: C40B40/06 ,  B01L3/00 ,  C08L87/00

CPC classification number: C40B40/06 ,  B01L3/502761 ,  B01L3/502784 ,  C08L87/005 ,  B01L2200/0652 ,  B01L2300/0829 ,  B01L2400/0415

Abstract: The present disclosure generally relates to compositions, methods, sorters, systems, devices and uses for screening for bioactive substances in emulsion droplets. In some embodiments, the compositions are a continuous phase formulation for stable emulsions, In some embodiments, the methods are for preparing a monodisperse polyethylene glycol acrylamide (PEGA) co-polymer resin, or for preparing a core-shell bead. In some embodiments, the systems and devices include a sorter, comprising an inlet channel, first and second outlet channels meeting the inlet channel at a junction, and first and second electrodes proximate respective first and second sides of the junction sorter. In some embodiments, the systems and devices include a sorter, comprising a microwell array plate configured to host one microdroplet per microwell, a fluorescence microscope, an imager configured to automatically image assay droplets and identify desired droplets, and an automated microcapillary-based droplet sampling device configured to continuously deposit desired droplets to hit wells.

公开(公告)号：US20210284635A1

公开(公告)日：2021-09-16

申请号：US17071311

申请日：2020-10-15

Applicant: NOVARTIS AG

Inventor： Guillaume BARBE ,  Gregory Raymond BEBERNITZ ,  Sicong GENG ,  Hatice Belgin GULGEZE EFTHYMIOU ,  Lv LIAO ,  Fupeng MA ,  Ruowei MO ,  David Thomas PARKER ,  Yunshan PENG ,  Stefan PEUKERT ,  Nichola Smith ,  Ken YAMADA ,  Kayo YASOSHIMA

IPC: C07D471/04 ,  A61P9/06 ,  A61K31/4375 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/675 ,  A61K45/06 ,  C07F9/6561

Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; Wherein R1, R3-R6, X2 and X3 are as defined herein, a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

公开(公告)号：US20190263803A1

公开(公告)日：2019-08-29

申请号：US16290313

申请日：2019-03-01

Applicant: NOVARTIS AG

Inventor： Guillaume BARBE ,  Gregory Raymond BEBERNITZ ,  Sicong GENG ,  Hatice Belgin GULGEZE EFTHYMIOU ,  Lv LIAO ,  Fupeng MA ,  Ruowei MO ,  David Thomas PARKER ,  Yunshan PENG ,  Stefan PEUKERT ,  Ken YAMADA ,  Kayo YASOSHIMA

IPC: C07D471/04 ,  A61P9/06 ,  A61K31/675 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/4375 ,  C07F9/6561 ,  A61K45/06 ,  A61K31/541

Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; Wherein R1, R3-R6, X2 and X3 are as defined herein, a method for manufacturing the compounds of the invention, and its therapeutic uses. 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

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：US20220363671A1

公开(公告)日：2022-11-17

申请号：US17642292

申请日：2020-09-16

Applicant: NOVARTIS AG

Inventor： Jake AXFORD ,  Rohan Eric John BECKWITH ,  Simone BONAZZI ,  Nicole BUSCHMANN ,  Artiom CERNIJENKO ,  Janetta DEWHURST ,  Aleem FAZAL ,  Matthew James HESSE ,  Lauren HOLDER ,  Viktor HORNAK ,  Hidetomo IMASE ,  Rama JAIN ,  Xianming JIN ,  John Ryan KERRIGAN ,  Julie LACHAL ,  Fupeng MA ,  Hasnain Ahmed MALIK ,  James R. MANNING ,  Daniel MCKAY ,  Robert Joseph MOREAU ,  Pierre NIMSGERN ,  Gary O'BRIEN ,  Anna VULPETTI ,  Ken YAMADA ,  Junping ZHAO

IPC: C07D405/04 ,  A61K31/513 ,  C07D471/04 ,  C07D413/04 ,  C07D401/14

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