申请人:ZECRI Frédéric
公开号:US20130196899A1
公开(公告)日:2013-08-01
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.
本发明提供了公式I'的合成多肽:
或其酰胺、酯或盐,其中X1、X2、X3、X4、X5、X6、X7、X8、X9、X10、X11、X12和X13在此定义。这些多肽是APJ受体的激动剂。本发明还涉及制造所述多肽的方法,以及其治疗用途,如治疗或预防急性失代偿性心力衰竭(ADHF)、慢性心力衰竭、肺动脉高压、心房颤动、布氏综合症、室性心动过速、动脉粥样硬化、高血压、再狭窄、缺血性心血管疾病、心肌病、心脏纤维化、心律失常、水潴留、糖尿病(包括妊娠期糖尿病)、肥胖症、外周动脉疾病、脑血管意外、短暂性脑缺血发作、创伤性脑损伤、肌萎缩性脊髓侧索硬化、烧伤(包括晒伤)和妊娠高血压综合症。本发明还提供了药理活性剂的组合和制药组合物。