公开(公告)号：US20220024981A1

公开(公告)日：2022-01-27

申请号：US17296679

申请日：2019-11-26

Applicant: Novartis AG

Inventor： Alec Nathanson FLYER ,  Andrei Alexandrovich GOLOSOV ,  Philipp GROSCHE ,  Ian LEWIS ,  Eugene Yuejin LIU ,  Andreas MARZINZIK ,  Lauren Gilchrist MONOVICH ,  Johannes OTTL ,  Tajesh Jayprakash PATEL ,  Patrick Crawford REID ,  Mohindra SEEPERSAUD

IPC: C07K7/64 ,  A61K38/12 ,  A61K45/06

Abstract: The disclosure relates to inhibitors of PCSK9 useful in the treatment of lipid metabolism, and other diseases in which PCSK9 plays a role, having the Formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, stereoisomer, or tautomer thereof, wherein R1, X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, X11, X12, and X13 are described herein.

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：US20200164024A1

公开(公告)日：2020-05-28

申请号：US16695843

申请日：2019-11-26

Applicant: NOVARTIS AG

Inventor： Karin BRINER ,  Brian Addison DECHRISTOPHER ,  Alec Nathanson FLYER ,  Andrei Alexandrovich GOLOSOV ,  Philipp GROSCHE ,  Eugene Yuejin LIU ,  Justin Yik Ching MAO ,  Lauren Gilchrist MONOVICH ,  Tajesh Jayprakash PATEL ,  Carina Cristina SANCHEZ ,  Liansheng SU ,  Lihua YANG ,  Rui ZHENG

IPC: A61K38/12 ,  A61K45/06 ,  C07K5/12

Abstract: The disclosure relates to inhibitors of PCSK9 useful in the treatment of cholesterol lipid metabolism, and other diseases in which PCSK9 plays a role, having the Formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, N-oxide, or tautomer thereof, wherein R1, R1, R1, R1, R1, R1, R1, R1, R1, X1, X2, and X3 are described herein.

公开(公告)号：US20230089867A1

公开(公告)日：2023-03-23

申请号：US17296895

申请日：2019-11-26

Applicant: Novartis AG

Inventor： Christopher BECKER ,  Brian Addison DECHRISTOPHER ,  Alec Nathanson FLYER ,  Adam FRIEDMAN ,  Christian GAMPE ,  Andrei Alexandrovich GOLOSOV ,  Philipp GROSCHE ,  Tyler HARRISON ,  Qian LIU ,  Eugene Yuejin LIU, I ,  Justin Yik Ching MAO ,  Lauren Gilchrist MONOVICH ,  Tajesh Jayprakash PATEL ,  Carina Cristina SANCHEZ ,  Liansheng SU ,  Lihua YANG ,  Rui ZHENG

IPC: C07K7/56

Abstract: The disclosure relates to inhibitors of PCSK9 useful in the treatment of cholesterol lipid metabolism, and other diseases in which PCSK9 plays a role, having the Formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, N-oxide, or tautomer thereof, wherein X1, R1, R2, R3, R4, R5, R6, R6′, R7, R7′, R8, R9, R9′, R10, R11, R12, and n are described herein.

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：US20210252103A1

公开(公告)日：2021-08-19

申请号：US17200471

申请日：2021-03-12

Applicant: NOVARTIS AG

Inventor： Karin BRINER ,  Brian Addison DECHRISTOPHER ,  Alec Nathanson FLYER ,  Andrei Alexandrovich GOLOSOV ,  Philipp GROSCHE ,  Eugene Yuejin LIU ,  Justin Yik Ching MAO ,  Lauren Gilchrist MONOVICH ,  Tajesh Jayprakash PATEL ,  Liansheng SU ,  Lihua YANG ,  Rui ZHENG

IPC: A61K38/12 ,  A61K45/06 ,  C07K5/12

Abstract: The disclosure relates to inhibitors of PCSK9 useful in the treatment of cholesterol lipid metabolism, and other diseases in which PCSK9 plays a role, having the Formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, N-oxide, or tautomer thereof, wherein R1, R1, R1, R1, R1, R1, R1, R1, R1, X1, X2, and X3 are described herein.