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    SYNTHETIC APELIN MIMETICS FOR THE TREATMENT OF HEART FAILURE
    1.
    发明申请
    SYNTHETIC APELIN MIMETICS FOR THE TREATMENT OF HEART FAILURE 有权
    用于治疗心脏衰竭的合成APELINMIMT

    公开(公告)号：US20130196899A1

    公开(公告)日：2013-08-01

    申请号：US13747621

    申请日：2013-01-23

    申请人： Frédéric ZECRI ,  Andrei GOLOSOV ,  Philipp GROSCHE ,  Kayo YASOSHIMA ,  Hongjuan ZHAO ,  Qi-Ying HU ,  Hidetomo IMASE ,  David Thomas PARKER

    发明人： Frédéric ZECRI ,  Andrei GOLOSOV ,  Philipp GROSCHE ,  Kayo YASOSHIMA ,  Hongjuan ZHAO ,  Qi-Ying HU ,  Hidetomo IMASE ,  David Thomas PARKER

    IPC分类号： C07K7/08 ,  C07K7/60 ,  C07K7/56

    CPC分类号： A61M16/0816 ,  A61K38/00 ,  A61K38/10 ,  A61M16/0066 ,  A61M16/201 ,  A61M2016/0027 ,  A61M2016/003 ,  A61M2205/35 ,  A61M2205/502 ,  C07K7/08 ,  C07K7/56 ,  C07K7/60

    摘要： 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.

    摘要翻译： 本发明提供式I'的合成多肽：或其酰胺，酯或其盐，其中X1，X2，X3，X4，X5，X6，X7，X8，X9，X10，X11，X12和X13被定义 这里。 多肽是APJ受体的激动剂。 本发明还涉及制备本发明多肽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，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。

    SYNTHETIC APELIN MIMETICS FOR THE TREATMENT OF HEART FAILURE
    2.
    发明申请
    SYNTHETIC APELIN MIMETICS FOR THE TREATMENT OF HEART FAILURE 审中-公开
    用于治疗心脏衰竭的合成APELINMIMT

    公开(公告)号：US20140142022A1

    公开(公告)日：2014-05-22

    申请号：US14165680

    申请日：2014-01-28

    申请人： Frederic ZECRI ,  Andrei GOLOSOV ,  Philipp GROSCHE ,  Kayo YASOSHIMA ,  Hongjuan ZHAO ,  Qi-Ying HU ,  Hidetomo IMASE ,  David Thomas PARKER

    发明人： Frederic ZECRI ,  Andrei GOLOSOV ,  Philipp GROSCHE ,  Kayo YASOSHIMA ,  Hongjuan ZHAO ,  Qi-Ying HU ,  Hidetomo IMASE ,  David Thomas PARKER

    IPC分类号： C07K7/08

    CPC分类号： A61M16/0816 ,  A61K38/00 ,  A61K38/10 ,  A61M16/0066 ,  A61M16/201 ,  A61M2016/0027 ,  A61M2016/003 ,  A61M2205/35 ,  A61M2205/502 ,  C07K7/08 ,  C07K7/56 ,  C07K7/60

    摘要： 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.

    摘要翻译： 本发明提供式I'的合成多肽：或其酰胺，酯或其盐，其中X1，X2，X3，X4，X5，X6，X7，X8，X9，X10，X11，X12和X13被定义 这里。 多肽是APJ受体的激动剂。 本发明还涉及制备本发明多肽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，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。

    SYNTHETIC APELIN MIMETICS FOR THE TREATMENT OF HEART FAILURE
    3.
    发明申请
    SYNTHETIC APELIN MIMETICS FOR THE TREATMENT OF HEART FAILURE 有权
    用于治疗心脏衰竭的合成APELINMIMT

    公开(公告)号：US20150252076A1

    公开(公告)日：2015-09-10

    申请号：US14714914

    申请日：2015-05-18

    申请人： Frederic ZECRI ,  Andrei GOLOSOV ,  Philipp GROSCHE ,  Hongjuan ZHAO ,  Qi-Ying HU ,  Hidetomo IMASE

    发明人： Frederic ZECRI ,  Andrei GOLOSOV ,  Philipp GROSCHE ,  Hongjuan ZHAO ,  Qi-Ying HU ,  Hidetomo IMASE

    IPC分类号： C07K7/08 ,  A61K38/10

    CPC分类号： A61M16/0816 ,  A61K38/00 ,  A61K38/10 ,  A61M16/0066 ,  A61M16/201 ,  A61M2016/0027 ,  A61M2016/003 ,  A61M2205/35 ,  A61M2205/502 ,  C07K7/08 ,  C07K7/56 ,  C07K7/60

    摘要： 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.

    摘要翻译： 本发明提供式I'的合成多肽：或其酰胺，酯或其盐，其中X1，X2，X3，X4，X5，X6，X7，X8，X9，X10，X11，X12和X13被定义 这里。 多肽是APJ受体的激动剂。 本发明还涉及制备本发明多肽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，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 APELIN DERIVATIVES FOR THE TREATMENT OF HEART FAILURE
    6.
    发明申请
    CYCLIC APELIN DERIVATIVES FOR THE TREATMENT OF HEART FAILURE 有权
    用于治疗心力衰竭的循环APELIN衍生物

    公开(公告)号：US20160159871A1

    公开(公告)日：2016-06-09

    申请号：US14905333

    申请日：2014-07-21

    申请人： Frédéric ZECRI ,  Philipp GROSCHE ,  Kayo YASOSHIMA ,  Hongjuan ZHAO ,  Jun YUAN

    发明人： Frederic ZECRI ,  Philipp GROSCHE ,  Kayo YASOSHIMA ,  Hongjuan ZHAO ,  Jun YUAN

    IPC分类号： C07K14/47 ,  A61K38/17 ,  A61K47/48 ,  A61K45/06

    CPC分类号： C07K14/47 ,  A61K38/10 ,  A61K38/1709 ,  A61K45/06 ,  A61K47/643 ,  A61K47/6811

    摘要： The invention provides a synthetic polypeptide of Formula I′: X1-R-X3-R-L-X6-X7-K-X9-P-X11-X12-X13 or an amide, an ester, a salt thereof, or a bioconjugate thereof, wherein X1, X3, X6, X7, X9, X11, X12 and X13 are defined herein. The polypeptides and bioconjugates are agonist of the APJ receptor. The invention also relates to a method for manufacturing the polypeptides and 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.

    摘要翻译： 本发明提供式I'的合成多肽：X1-R-X3-RL-X6-X7-K-X9-P-X11-X12-X13或其酰胺，酯，其盐或其生物缀合物， 其中X1，X3，X6，X7，X9，X11，X12和X13在本文中定义。 多肽和生物缀合物是APJ受体的激动剂。 本发明还涉及本发明的多肽和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，Brugada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 受伤（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。

    DISULFIDE CYCLIC POLYPEPTIDES FOR THE TREATMENT OF HEART FAILURE
    7.
    发明申请
    DISULFIDE CYCLIC POLYPEPTIDES FOR THE TREATMENT OF HEART FAILURE 有权
    用于治疗心力衰竭的解决循环多糖

    公开(公告)号：US20160145309A1

    公开(公告)日：2016-05-26

    申请号：US14905338

    申请日：2014-07-21

    申请人： Frédéric ZECRI ,  Philipp GROSCHE ,  Kayo YASOSHIMA ,  Hongjuan ZHAO ,  Jun YUAN

    发明人： Frederic ZECRI ,  Philipp GROSCHE ,  Kayo YASOSHIMA ,  Hongjuan ZHAO ,  Jun YUAN

    IPC分类号： C07K7/08 ,  A61K45/06 ,  A61K38/10 ,  C07K7/06 ,  A61K38/08

    CPC分类号： C07K7/08 ,  A61K38/08 ,  A61K38/10 ,  A61K45/06 ,  C07K7/06 ,  C07K14/47

    摘要： The invention provides a synthetic polypeptide of Formula I′: X1-R-P-R-X5-X6-X7-K-X9-P-X11-X12-X13 or an amide, an ester, a salt or a bioconjugate thereof, wherein X1, X5, X6, X7, X9 and X11 to X13 are defined herein. The polypeptides and bioconjugates are agonist of the APJ receptor. The invention also relates to a method for manufacturing the polypeptides or 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.

    摘要翻译： 本发明提供式I'的合成多肽：X1-RPR-X5-X6-X7-K-X9-P-X11-X12-X13或其酰胺，酯，盐或生物缀合物，其中X1，X5 ，X6，X7，X9，X11〜X13。 多肽和生物缀合物是APJ受体的激动剂。 本发明还涉及制备本发明的多肽或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，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 受伤（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
    8.
    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

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

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

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

    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.

    摘要翻译： 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。