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1. 发明授权

EP3247405B1 SYNTHETIC APELIN FATTY ACID CONJUGATES WITH IMPROVED HALF-LIFE 有权
公开(公告)号：EP3247405B1
公开(公告)日：2019-07-17
申请号：EP16701560.1
申请日：2016-01-15
申请人： Novartis AG
发明人： KANTER, Aaron , USERA, Aimee Richardson , ZECRI, Frederic
IPC分类号： A61K47/54 , A61K47/60 , A61K38/12 , A61K45/06 , C07K14/47

2. 发明公开

EP3247405A1 SYNTHETIC APELIN FATTY ACID CONJUGATES WITH IMPROVED HALF-LIFE 有权
标题翻译：具有改善的半衰期的合成APELIN脂肪酸缀合物
公开(公告)号：EP3247405A1
公开(公告)日：2017-11-29
申请号：EP16701560.1
申请日：2016-01-15
申请人： Novartis AG
发明人： KANTER, Aaron , USERA, Aimee Richardson , ZECRI, Frederic
IPC分类号： A61K47/50 , A61K45/06 , A61P9/04
CPC分类号： A61K38/12 , A61K45/06 , A61K47/542 , A61K47/60 , A61K47/64 , A61K51/0402 , C07K7/64 , C07K14/47
摘要： The invention provides a conjugate, or a pharmaceutically acceptable salt thereof, comprising a synthetic polypeptide of Formula I: Q-R-P-R-L-C*-H-K-G-P-(Nle)-C*-F (I) or a amide or ester thereof; and a fatty acid selected from: wherein said fatty acid is covalently linked to the N-terminus of the peptide via one of its carboxylic acid functionality, optionally via a polyethylene glycol linker; and wherein the two cysteine amino acids labeled with “*” form a disulfide bond between the thiol functionalities of their side chain. The conjugates are agonist of the APJ receptor. The invention also relates to a method for manufacturing the conjugates 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.

3. 发明公开

EP3024492A2 BIOCONJUGATES OF SYNTHETIC APELIN POLYPEPTIDES 审中-公开
标题翻译： 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
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
IPC分类号： A61K47/48
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': 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。

4. 发明公开

EP3988170A1 FATTY ACIDS AND THEIR USE IN CONJUGATION TO BIOMOLECULES 审中-公开
公开(公告)号：EP3988170A1
公开(公告)日：2022-04-27
申请号：EP21206196.4
申请日：2015-06-18
申请人： Novartis AG
发明人： BARNES, David Weninger , YAMADA, Ken , IBEBUNJO, Chikwendu , DUTTAROY, Alokesh , KIRMAN, Louise Clare , BRUCE, Alexandra Marshall , USERA, Aimee Richardson , ZECRI, Frederic , YUAN, Jun , LOU, Changgang , KANTER, Aaron , BOSE, Avirup
IPC分类号： A61P1/00 , A61P3/00 , A61P5/48 , A61P9/00 , A61P25/18
摘要： The invention provides a conjugate comprising a biomolecule linked to a fatty acid via a linker wherein the fatty acid has the following Formula A1:

wherein R 1 , R 2 , R 3 , n and m are defined herein. The invention also relates to uses of the fatty acids in providing said conjuage. The invention also relates to a method for manufacturing the conjugate of the invention such as GDF15 conjugate, and its therapeutic uses such as treatment or prevention of metabolic disorders or diseases, type 2 diabetes mellitus, obesity, pancreatitis, dyslipidemia, alcoholic and nonalcoholic fatty liver disease/steatohepatitis and other progressive liver diseases, insulin resistance, hyperinsulinemia, glucose intolerance, hyperglycemia, metabolic syndrome, hypertension, cardiovascular disease, atherosclerosis, peripheral arterial disease, stroke, heart failure, coronary heart disease, diabetic complications (including but not limited to chronic kidney disease), neuropathy, gastroparesis and other metabolic disorders. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

5. 发明公开

EP3157571A1 FATTY ACIDS AND THEIR USE IN CONJUGATION TO BIOMOLECULES 有权
标题翻译：达赖喇嘛在德累斯顿的VENBIOMOLEKÜLEN
公开(公告)号：EP3157571A1
公开(公告)日：2017-04-26
申请号：EP15732508.5
申请日：2015-06-18
申请人： Novartis AG
发明人： BARNES, David Weninger , YAMADA, Ken , IBEBUNJO, Chikwendu , DUTTAROY, Alokesh , KIRMAN, Louise Clare , BRUCE, Alexandra Marshall , USERA, Aimee Richardson , ZECRI, Frederic , YUAN, Jun , LOU, Changgang , KANTER, Aaron , BOSE, Avirup
IPC分类号： A61K47/50 , A61P3/00 , C07K14/475
CPC分类号： A61K47/48038 , A61K38/08 , A61K38/164 , A61K38/1709 , A61K38/1825 , A61K38/1841 , A61K38/2221 , A61K45/06 , A61K47/542 , C07C55/02 , C07C55/22 , C07C57/02 , C07C57/18 , C07C59/245 , C12N15/113 , C12N2310/14 , C12N2310/351
摘要： The invention provides a conjugate comprising a biomolecule linked to a fatty acid via a linker wherein the fatty acid has the following Formulae A1, A2 or A3: wherein R1, R2, R3, R4, Ak, n, m and p are defined herein. The invention also relates to a method for manufacturing the conjugate of the invention such as GDF15 conjugate, and its therapeutic uses such as treatment or prevention of metabolic disorders or diseases, type 2 diabetes mellitus, obesity, pancreatitis, dyslipidemia, alcoholic and nonalcoholic fatty liver disease/steatohepatitis and other progressive liver diseases, insulin resistance, hyperinsulinemia, glucose intolerance, hyperglycemia, metabolic syndrome, hypertension, cardiovascular disease, atherosclerosis, peripheral arterial disease, stroke, heart failure, coronary heart disease, diabetic complications (including but not limited to chronic kidney disease), neuropathy, gastroparesis and other metabolic disorders. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
摘要翻译：本发明提供了一种缀合物，其包含通过接头与脂肪酸连接的生物分子，其中脂肪酸具有下列式A1，A2或A3：其中R1，R2，R3，R4，Ak，n，m和p如本文所定义。本发明还涉及制备本发明缀合物如GDF15缀合物的方法及其治疗用途，例如治疗或预防代谢紊乱或疾病，2型糖尿病，肥胖症，胰腺炎，血脂异常，酒精和非酒精性脂肪肝疾病/脂肪性肝炎和其他进行性肝病，胰岛素抵抗，高胰岛素血症，葡萄糖不耐受，高血糖症，代谢综合征，高血压，心血管疾病，动脉粥样硬化，外周动脉疾病，中风，心力衰竭，冠心病，糖尿病并发症（包括但不限于慢性肾脏疾病），神经病，胃轻瘫等代谢紊乱。本发明还提供药理活性剂和药物组合物的组合。

6. 发明公开

EP3024845A1 CYCLIC POLYPEPTIDES FOR THE TREATMENT OF HEART FAILURE 审中-公开
标题翻译： 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
发明人： BRUCE, Alexandra Marshall , GROSCHE, Philipp , GUIMARAES, Carla , KANTER, Aaron , LOU, Changgang , USERA, Aimee Richardson , YASOSHIMA, Kayo , YUAN, Jun , ZECRI, Frederic , ZHAO, Hongjuan
IPC分类号： C07K14/47 , A61K38/17 , A61P9/04
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，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。

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