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：US20250090699A1

公开(公告)日：2025-03-20

申请号：US18802972

申请日：2024-08-13

Applicant: Novartis AG

Inventor： Salvatore BONGARZONE ,  Davide CAMPORESE ,  Gonçalo dos Santos CLEMENTE ,  Takeru EHARA ,  Matteo FISCHER ,  Andrei Alexandrovich GOLOSOV ,  Philipp GROSCHE ,  Philipp HOLZER ,  Alexei KARPOV ,  Marion LACAUD-BAUMLIN ,  Lukas LEDER ,  Rafael Bermeo MALO ,  Andreas MARZINZIK ,  Yoshihide MIZUKOSHI ,  Charlie MUNSCH ,  Markus Oliver RESCHKE ,  Holger SELLNER ,  Therese-Marie STACHYRA

IPC: A61K51/08 ,  A61P35/00 ,  C07B59/00

Abstract: Described herein are cyclic peptides targeting fibroblast activation protein (FAP), and their incorporation into compounds for radioligand imaging and therapies, as well as methods and/or uses of such compounds for the imaging, treatment and/or prevention of FAP-implicated diseases and disorders.

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：US20170233443A1

公开(公告)日：2017-08-17

申请号：US15497135

申请日：2017-04-25

Applicant: NOVARTIS AG

Inventor： Alexandra Marshall BRUCE ,  Philipp GROSCHE ,  Carla GUIMARAES ,  Aaron KANTER ,  Changgang LOU ,  Aimee Richardson USERA ,  Kayo YASOSHIMA ,  Jun YUAN ,  Frederic Zecri ,  Hongjuan ZHAO

IPC: C07K14/47 ,  A61K45/06 ,  A61K38/17

CPC classification number: C07K14/47 ,  A61K38/12 ,  A61K38/1709 ,  A61K45/06 ,  A61K47/542 ,  A61K47/60 ,  A61K47/643 ,  A61K47/6811 ,  C07K7/64 ,  C07K14/765 ,  C07K16/461 ,  C07K2319/30 ,  C07K2319/31

Abstract: The invention provides a cyclic polypeptide of Formula I (SEQ ID NO: 1): X1-R-X3-X4-L-S-X7-X8-X9-X10-X11-X12-X13  I or an amide, an ester or a salt thereof, or a bioconjugate thereof, wherein X1, X3, X4, X7, X8, X9, X10, X11, X12 and X13 are defined herein. The polypeptides are agonist of the APJ receptor. The invention also relates to a method for manufacturing the polypeptides of the invention or bioconjugates thereof, and their therapeutic uses such as treatment or prevention of acute decompensated heart failure (ADHF), chronic heart failure, pulmonary hypertension, atrial fibrillation, Brugada syndrome, ventricular tachycardia, atherosclerosis, hypertension, restenosis, ischemic cardiovascular diseases, cardiomyopathy, cardiac fibrosis, arrhythmia, water retention, diabetes (including gestational diabetes), obesity, peripheral arterial disease, cerebrovascular accidents, transient ischemic attacks, traumatic brain injuries, amyotrophic lateral sclerosis, burn injuries (including sunburn) and preeclampsia. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

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.