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：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.

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：US20220064164A1

公开(公告)日：2022-03-03

申请号：US17101510

申请日：2020-11-23

Applicant: NOVARTIS AG

Inventor： Kelly D. BOSS ,  Yi FAN ,  Alec Nathanson FLYER ,  Declan HARDY ,  Zhihong HUANG ,  Kathryn Taylor LINKENS ,  Jon Christopher LOREN ,  Fupeng MA ,  Valentina MOLTENI ,  Duncan SHAW ,  Jeffrey SMITH ,  Catherine Fooks SOLOVAY

IPC: C07D471/10 ,  C07D413/14 ,  C07D413/06 ,  C07D491/107 ,  A61P27/04

Abstract: Provided herein are compounds and pharmaceutical compositions useful for treating meibomian gland dysfunction (MGD), comprising administering to a subject in need thereof a therapeutically effective amount of a compound of Formula (I) or a compound of Formula (I′), or pharmaceutical composition described herein.

公开(公告)号：US20230037639A1

公开(公告)日：2023-02-09

申请号：US17493055

申请日：2021-10-04

Applicant: Novartis AG

Inventor： Rohan Eric John BECKWITH ,  Simone BONAZZI ,  Artiom CERNIJENKO ,  Fupeng MA ,  Nathaniel F. WARE

IPC: A61K31/454 ,  A61P35/00 ,  A61K31/4545 ,  A61K31/498 ,  C07D401/04 ,  C07D401/14

Abstract: The present disclosure provides a compound of Formula (IT or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, wherein Ra, Rb, Rx, R1, R2, X2, and q are as defined herein, and methods of making and using same.

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：US20220340573A1

公开(公告)日：2022-10-27

申请号：US17805487

申请日：2022-06-06

Applicant: Novartis AG

Inventor： Kelly D. BOSS ,  Yi FAN ,  Alec Nathanson FLYER ,  Declan HARDY ,  Zhihong HUANG ,  Kathryn Taylor LINKENS ,  Jon Christopher LOREN ,  Fupeng MA ,  Valentina MOLTENI ,  Duncan SHAW ,  Jeffrey SMITH ,  Catherine Fooks SOLOVAY

IPC: C07D471/10 ,  A61P27/04 ,  C07D413/06 ,  C07D413/14 ,  C07D491/107

Abstract: Provided herein are compounds and pharmaceutical compositions useful for treating meibomian gland dysfunction (MGD), comprising administering to a subject in need thereof a therapeutically effective amount of a compound of Formula (I) or a compound of Formula (I′), or pharmaceutical composition described herein.

公开(公告)号：US20200016143A1

公开(公告)日：2020-01-16

申请号：US16504376

申请日：2019-07-08

Applicant: Novartis AG

Inventor： Rohan Eric John BECKWITH ,  Simone BONAZZI ,  Artiom CERNIJENKO ,  Fupeng MA ,  Nathaniel F. WARE

IPC: A61K31/454 ,  C07D401/14 ,  C07D401/04 ,  A61K31/4545 ,  A61P35/00 ,  A61K31/498

Abstract: The present disclosure provides a compound of Formula (I′): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, wherein Ra, Rb, Rx, R1, R2, X2, and q are as defined herein, and methods of making and using same.