公开(公告)号：US20190002393A1

公开(公告)日：2019-01-03

申请号：US16135116

申请日：2018-09-19

Applicant: Novartis AG

Inventor： Rohan Eric John BECKWITH ,  Luis BRITO ,  Brian Addison DECHRISTOPHER ,  Gabriel Grant GAMBER ,  Andrew GEALL ,  Thomas ZABAWA

IPC: C07C219/06 ,  C07D211/34 ,  A61K47/18 ,  C07D207/08 ,  C07C217/58 ,  C07C219/16 ,  C07D211/62 ,  C07C229/12 ,  A61K31/713 ,  A61K31/711 ,  A61K31/7105 ,  A61K9/51 ,  A61K9/127 ,  A61K47/22 ,  C07D295/15

Abstract: This invention provides for a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein RA, RB, R2 and R4 are defined herein. The compounds of formula (I) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.

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：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.

公开(公告)号：US20170275243A1

公开(公告)日：2017-09-28

申请号：US15505282

申请日：2015-09-04

Applicant: Novartis AG

Inventor： Rohan Eric John BECKWITH ,  Luis BRITO ,  Brian Addison DECHRISTOPHER ,  Gabriel Grant GAMBER ,  Andrew GEALL ,  Thomas ZABAWA

IPC: C07C219/06 ,  A61K9/127 ,  C07D295/15 ,  C07C219/16 ,  C07C229/12 ,  C07D207/08 ,  A61K47/22 ,  C07C217/58

CPC classification number: C07C219/06 ,  A61K9/1272 ,  A61K9/5123 ,  A61K31/7105 ,  A61K31/711 ,  A61K31/713 ,  A61K47/18 ,  A61K47/22 ,  C07C217/58 ,  C07C219/16 ,  C07C229/12 ,  C07D207/08 ,  C07D211/34 ,  C07D211/62 ,  C07D295/15

Abstract: This invention provides for a compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein RA, RB, R2 and R4 are defined herein. The compounds of formula (I) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.