基本信息:
- 专利标题： BIOCONJUGATES OF SYNTHETIC APELIN POLYPEPTIDES
- 专利标题（中）：合成APELIN多肽的生物活性
- 申请号：PCT/US2014047378 申请日：2014-07-21
- 公开(公告)号：WO2015013169A3 公开(公告)日：2015-03-19
- 发明人： CAPLAN SHARI L , GOLOSOV ANDREI , GROSCHE PHILIPP , GUIMARAES CARLA , KANTER AARON , LOU CHANGGANG , PARKER DAVID THOMAS , PETERS ERIC C , USERA AIMEE RICHARDSON , YASOSHIMA KAYO , YUAN JUN , ZECRI FREDERIC , ZHAO HONGJUAN
- 申请人： NOVARTIS AG , CAPLAN SHARI L , GOLOSOV ANDREI , GROSCHE PHILIPP , GUIMARAES CARLA , KANTER AARON , LOU CHANGGANG , PARKER DAVID THOMAS , PETERS ERIC C , USERA AIMEE RICHARDSON , YASOSHIMA KAYO , YUAN JUN , ZECRI FREDERIC , ZHAO HONGJUAN
- 专利权人： NOVARTIS AG,CAPLAN SHARI L,GOLOSOV ANDREI,GROSCHE PHILIPP,GUIMARAES CARLA,KANTER AARON,LOU CHANGGANG,PARKER DAVID THOMAS,PETERS ERIC C,USERA AIMEE RICHARDSON,YASOSHIMA KAYO,YUAN JUN,ZECRI FREDERIC,ZHAO HONGJUAN
- 当前专利权人： NOVARTIS AG,CAPLAN SHARI L,GOLOSOV ANDREI,GROSCHE PHILIPP,GUIMARAES CARLA,KANTER AARON,LOU CHANGGANG,PARKER DAVID THOMAS,PETERS ERIC C,USERA AIMEE RICHARDSON,YASOSHIMA KAYO,YUAN JUN,ZECRI FREDERIC,ZHAO HONGJUAN
- 优先权： US201361858303 2013-07-25; US201462015848 2014-06-23
- 主分类号： A61K47/48
- IPC分类号： A61K47/48
摘要：
The invention provides a bioconjugates comprising a synthetic polypeptide of Formula I': 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 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.
摘要（中）：
本发明提供了包含式I'的合成多肽：I'或其酰胺，其酯或其盐的生物缀合物，其中X 1，X 2，X 3，X 4，X 5，X 6，X 7，X 8，X 9，X 10，X 11， X12和X13在本文中定义和半衰期延长部分，其中肽和半衰期延长部分任选地经由连接体共价连接或融合。 多肽是APJ受体的激动剂。 本发明还涉及本发明的生物缀合物的制备方法及其治疗用途，例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，布鲁加达综合征，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，保水，糖尿病（包括妊娠糖尿病），肥胖，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，肌萎缩性侧索硬化，烧伤（ 包括晒伤）和先兆子痫。 本发明还提供药理活性剂和药物组合物的组合。
公开/授权文献:
- WO2015013169A9 BIOCONJUGATES OF SYNTHETIC APELIN POLYPEPTIDES 公开/授权日：2016-10-20
IPC结构图谱:
| A | 人类生活必需 |
| --A61 | 医学或兽医学；卫生学 |
| ----A61K | 医用、牙科用或梳妆用的配制品 |
| ------A61K47/00 | 以所用的非有效成分为特征的医用配制品，如载体、惰性添加剂 |
| --------A61K47/48 | .非有效成分被化学键键合到有效成分上，例如聚合物药物轭合物 |