公开(公告)号：US09982017B2

公开(公告)日：2018-05-29

申请号：US14714914

申请日：2015-05-18

Applicant: Novartis AG

Inventor： Frederic Zecri ,  Andrei Golosov ,  Philipp Grosche ,  Hongjuan Zhao ,  Qi-Ying Hu ,  Hidetomo Imase

IPC: A61K38/10 ,  C07K7/08 ,  C07K7/56 ,  C07K7/60 ,  A61K38/00

CPC classification number: A61M16/0816 ,  A61K38/00 ,  A61K38/10 ,  A61M16/0066 ,  A61M16/201 ,  A61M2016/0027 ,  A61M2016/003 ,  A61M2205/35 ,  A61M2205/502 ,  C07K7/08 ,  C07K7/56 ,  C07K7/60

Abstract: The invention provides a synthetic polypeptide of Formula I′: or an amide, an ester or a salt thereof, wherein X1, X2, X3, X4, X5, X6, 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, and its 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：US09908919B2

公开(公告)日：2018-03-06

申请号：US14905333

申请日：2014-07-21

Applicant: Novartis AG

Inventor： Frederic Zecri ,  Philipp Grosche ,  Kayo Yasoshima ,  Hongjuan Zhao ,  Jun Yuan

IPC: A61K38/10 ,  A61K38/04 ,  C07K5/00 ,  C07K7/00 ,  C07K16/00 ,  C07K17/00 ,  C07K14/47 ,  A61K38/17 ,  A61K45/06 ,  A61K47/64 ,  A61K47/68

CPC classification number: C07K14/47 ,  A61K38/10 ,  A61K38/1709 ,  A61K45/06 ,  A61K47/643 ,  A61K47/6811

Abstract: The invention provides a synthetic polypeptide of Formula I (SEQ ID NO: 1): X1-R-X3-R-L-X6-X7-K-X9-P-X11-X12-X13  I or an amide, an ester, a salt thereof, or a bioconjugate thereof, wherein X1, X3, X6, X7, X9, X11, X12 and X13 are defined herein. The polypeptides and bioconjugates are agonist of the APJ receptor. The invention also relates to a method for manufacturing the polypeptides and bioconjugates of the invention, and its 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：US10005829B2

公开(公告)日：2018-06-26

申请号：US14440198

申请日：2013-11-19

Applicant: Novartis AG

Inventor： Frederic Zecri ,  Kayo Yasoshima ,  Philipp Grosche ,  Jun Yuan ,  Hongjuan Zhao

IPC: A61K38/10 ,  C07K14/765 ,  C07K14/47 ,  A61K45/06 ,  A61K38/38

CPC classification number: C07K14/765 ,  A61K38/385 ,  A61K45/06 ,  C07K14/47 ,  A61K38/1709 ,  A61K2300/00

Abstract: The invention relates to novel compositions comprising modified apelin-13 peptide sequences designed to treat cardiovascular disease in subjects to whom they are administered, and which exhibit greater resistance to degradation, and equivalent or greater bioactivity than their wild type counterparts. The invention also relates to methods of making said compositions and using said compositions as pharmaceutically active agents to treat cardiovascular disease.