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    Bioconjugates of synthetic apelin polypeptides
    2.
    发明授权
    Bioconjugates of synthetic apelin polypeptides 有权
    合成apelin多肽的生物缀合物

    公开(公告)号：US09340582B2

    公开(公告)日：2016-05-17

    申请号：US14336290

    申请日：2014-07-21

    Applicant: Jun Yuan ,  Frederic Zecri ,  Philipp Grosche ,  Hongjuan Zhao ,  Eric Peters ,  Shari Lynn Caplan ,  Changgang Lou

    Inventor： Jun Yuan ,  Frederic Zecri ,  Philipp Grosche ,  Hongjuan Zhao ,  Eric Peters ,  Shari Lynn Caplan ,  Changgang Lou

    IPC: C07K14/47 ,  C07K7/08 ,  A61K47/48 ,  A61K45/06 ,  A61K38/10 ,  C07K16/00 ,  A61K39/395

    CPC classification number: A61K38/10 ,  A61K38/00 ,  A61K45/06 ,  A61K47/542 ,  A61K47/643 ,  A61K47/68 ,  A61K47/6811 ,  C07K14/47 ,  C07K14/765 ,  C07K2319/30 ,  C07K2319/31

    Abstract: 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.

    Abstract translation: 本发明提供包含式I'（SEQ ID NO：1）的合成多肽的生物缀合物或其酰胺，其酯或其盐，其中X 1，X 2，X 3，X 4，X 5，X 6，X 7，X 8，X 9 ，X10，X11，X12和X13在本文中定义并且半衰期延长部分，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。

    CYCLIC POLYPEPTIDES FOR THE TREATMENT OF HEART FAILURE
    3.
    发明申请
    CYCLIC POLYPEPTIDES FOR THE TREATMENT OF HEART FAILURE 有权
    治疗心力衰竭的循环多糖

    公开(公告)号：US20150031604A1

    公开(公告)日：2015-01-29

    申请号：US14336262

    申请日：2014-07-21

    Applicant: Frederic ZECRI ,  Philipp GROSCHE ,  Kayo YASOSHIMA ,  Hongjuan ZHAO ,  Jun Yuan ,  Aimee Richardson USERA ,  Changgang LOU ,  Aaron KANTER ,  Alexandra Marshall BRUCE ,  Carla Giumaraes

    Inventor： Frederic ZECRI ,  Philipp GROSCHE ,  Kayo YASOSHIMA ,  Hongjuan ZHAO ,  Jun Yuan ,  Aimee Richardson USERA ,  Changgang LOU ,  Aaron KANTER ,  Alexandra Marshall BRUCE ,  Carla Giumaraes

    IPC: C07K7/64 ,  A61K38/12 ,  A61K45/06 ,  C07K16/46

    CPC classification number: 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

    Abstract: 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.

    Abstract translation: 本发明提供式I（SEQ ID NO：1）的环状多肽：X1-R-X3-X4-LS-X7-X8-X9-X10-X11-X12-X13I或酰胺，酯或盐 或其生物缀合物，其中X1，X3，X4，X7，X8，X9，X10，X11，X12和X13在本文中定义。 多肽是APJ受体的激动剂。 本发明还涉及制备本发明多肽或其生物缀合物的方法及其治疗用途，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，Brugada综合征，心室 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，潴留，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。

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