FREDERIC ZECRI,SHARI L. CAPLAN,ANDREI GOLOSOV,PHILLIPP GROSCHE,DAVID THOMAS PARKER,KAYO YASOSHIMA,HONGJUAN ZHAO,CARLA GUIMARAES,AARON KANTER,CHANGGANG LOU,ERIC C. PETERS,AIMEE RICHARDSON USERA,JUN YUA
申请号：
CL2016000157
公开号：
CL2016000157A1
申请日:
2016.01.21
申请国别(地区):
CL
年份:
2016
代理人:
摘要：
The invention provides a bioconjugates comprising a synthetic polypeptide of Formula I&prime； (SEQ ID NO: 1): 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 and a half-life extending moiety wherein the peptide and the half-life extending moiety are covalently linked or fuse, optionally via a linker. The polypeptides are agonist of the APJ receptor. The invention also relates to a method for manufacturing the 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.La solicitud se refiere a péptidos conjugados cíclicos análogos de apelina según se describe en la fórmula I´ de la cláusula 1, y la lista que identifica los radicales presentes en cada una de las posiciones del polímero, además de otras especificaciones de interacción entre ellos, y una porción conjugada que enriquece su vida media. Luego, se reivindica el uso terapéutico de dicho producto.
