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公开(公告)号:US20160108091A1
公开(公告)日:2016-04-21
申请号:US14963391
申请日:2015-12-09
申请人: Frederic ZECRI , Philipp GROSCHE , Kayo YASOSHIMA , Hongjuan ZHAO , Jun YUAN , Aimee Richardson USERA , Changgang LOU , Aaron KANTER , Alexandra Marshall BRUCE , Carla GUIMARAES
发明人: Frederic ZECRI , Philipp GROSCHE , Kayo YASOSHIMA , Hongjuan ZHAO , Jun YUAN , Aimee Richardson USERA , Changgang LOU , Aaron KANTER , Alexandra Marshall BRUCE , Carla GUIMARAES
IPC分类号: C07K7/64 , C07K14/765
CPC分类号: C07K14/47 , A61K38/12 , A61K38/1709 , A61K45/06 , A61K47/542 , A61K47/60 , A61K47/643 , A61K47/6811 , C07K7/64 , C07K14/765 , C07K16/461 , C07K2319/30 , C07K2319/31
摘要: The invention provides a cyclic polypeptide of Formula I (SEQ ID NO: 1): X1-R-X3-X4-L-S-X7-X8-X9-X10-X11-X12-X13 I 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.
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公开(公告)号:US20160166634A1
公开(公告)日:2016-06-16
申请号:US15053316
申请日:2016-02-25
申请人: Shari Lynn CAPLAN , Andrei GOLOSOV , Philipp GROSCHE , Carla GUIMARAES , Aaron KANTER , Changgang LOU , David Thomas PARKER , Eric C. Peters , Aimee Richardson USERA , Kayo YASOSHIMA , Jun YUAN , Federic ZECRI , Hongjuan ZHAO
发明人: Shari Lynn CAPLAN , Andrei GOLOSOV , Philipp GROSCHE , Carla GUIMARAES , Aaron KANTER , Changgang LOU , David Thomas PARKER , Eric C. Peters , Aimee Richardson USERA , Kayo YASOSHIMA , Jun YUAN , Federic ZECRI , Hongjuan ZHAO
CPC分类号: A61K38/10 , A61K38/00 , A61K45/06 , A61K47/542 , A61K47/643 , A61K47/68 , A61K47/6811 , C07K14/47 , C07K14/765 , C07K2319/30 , C07K2319/31
摘要: The invention provides a bioconjugates comprising a synthetic polypeptide of Formula I′ (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.
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