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：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：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.