BIOCONJUGATES OF SYNTHETIC APELIN POLYPEPTIDES
    4.
    发明公开
    BIOCONJUGATES OF SYNTHETIC APELIN POLYPEPTIDES 审中-公开
    BIOKONJUGATE VON SYNTHETISCHEN APELINPOLYPEPTIDDEN

    公开(公告)号:EP3024492A2

    公开(公告)日:2016-06-01

    申请号:EP14747491.0

    申请日:2014-07-21

    申请人: Novartis AG

    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.

    摘要翻译: 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以及半衰期延长的部分,其中肽和半衰期延长部分任选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。

    SYNTHETIC APELIN MIMETICS FOR THE TREATMENT OF HEART FAILURE
    5.
    发明公开
    SYNTHETIC APELIN MIMETICS FOR THE TREATMENT OF HEART FAILURE 有权
    SYNTHETISCHE APELIN-MIMETIKA ZUR BEHANDLUNG VON HERZINSUFFIZIENZ

    公开(公告)号:EP2807183A2

    公开(公告)日:2014-12-03

    申请号:EP13711953.3

    申请日:2013-01-25

    申请人: Novartis AG

    IPC分类号: C07K7/56 C07K14/47 A61K38/12

    摘要: A pressure support system that comprises a patient circuit, a docking assembly, and a tank. The patient circuit delivers a pressurized flow of breathable gas to a patient. The docking assembly has an inlet and an outlet that is adapted to receive the pressurized flow of breathable gas, and is also adapted to be connected with the patient circuit. The tank is constructed and arranged to be removably connected with the docking assembly, and enables the pressurized flow of breathable gas to pass therethrough. The tank is also adapted to contain a liquid such that a humidity level of the pressurized flow of breathable gas is elevated as the pressurized flow of breathable gas passes therethrough.

    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X 1,X 2,X 3,X 4,X 5,X 6,X 7,X 8,X 9,X 10,X 11,X 12和X 13 于此。 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,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 APELIN DERIVATIVES FOR THE TREATMENT OF HEART FAILURE
    7.
    发明公开
    CYCLIC APELIN DERIVATIVES FOR THE TREATMENT OF HEART FAILURE 审中-公开
    循环APELINDERIVATE心脏衰竭的治疗

    公开(公告)号:EP3024846A1

    公开(公告)日:2016-06-01

    申请号:EP14750267.8

    申请日:2014-07-21

    申请人: Novartis AG

    IPC分类号: C07K14/47 A61K38/17 A61P9/04

    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.

    CYCLIC POLYPEPTIDES FOR THE TREATMENT OF HEART FAILURE
    8.
    发明公开
    CYCLIC POLYPEPTIDES FOR THE TREATMENT OF HEART FAILURE 审中-公开
    CYCLISCHE POLYPEPTIDE ZUR BEHANDLUNG VON HERZINSUFFIZIENZ

    公开(公告)号:EP3024845A1

    公开(公告)日:2016-06-01

    申请号:EP14747284.9

    申请日:2014-07-21

    申请人: Novartis AG

    IPC分类号: C07K14/47 A61K38/17 A61P9/04

    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,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。