POLIPÉPTIDOS CÍCLICOS PARA EL TRATAMIENTO DE LA INSUFICIENCIA CARDIACA

• Main Authors: YASOSHIMA, KAYO, GROSCHE, PHILIPP, LOU, CHANGGANG, BRUCE, ALEXANDRA MARSHALL, USERA, AIMEE RICHARDSON, ZECRI, FREDERIC, KANTER, AARON, GUIMARAES, CARLA, YUAN, JUN, ZHAO, HONGJUAN
• Format: Patent
• Language: Spanish
• Published: 17.06.2016
• Subjects: CHEMISTRY; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PEPTIDES; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

La invención proporciona un polipéptido cíclico de la Fórmula I' (SEQ ID NO: 1):X1-R-X3-X4-L-S-X7-X8-X9-X10-X11-X12-X13 o una amida, un éster o una sal del mismo, o un bioconjugado del mismo, en donde X1, X3, X4, X7, X8, X9, X10, X11, X12 y X13 se definen en la presente. Los polipéptidos son agonistas del receptor APJ. 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.