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    Synthetic apelin fatty acid conjugates with improved half-life
    11.
    发明授权
    Synthetic apelin fatty acid conjugates with improved half-life 有权

    公开(公告)号：US09931372B2

    公开(公告)日：2018-04-03

    申请号：US14996418

    申请日：2016-01-15

    Applicant: Novartis AG

    Inventor： Aaron Kanter ,  Aimee Richardson Usera ,  Frederic Zecri

    IPC: A61K38/12 ,  A61K47/64 ,  A61K51/04 ,  A61K45/06 ,  C07K14/47 ,  A61K47/60 ,  A61K47/54 ,  C07K7/64

    CPC classification number: A61K38/12 ,  A61K45/06 ,  A61K47/542 ,  A61K47/60 ,  A61K47/64 ,  A61K51/0402 ,  C07K7/64 ,  C07K14/47

    Abstract: 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.

    Cyclic apelin derivatives for the treatment of heart failure
    12.
    发明授权
    Cyclic apelin derivatives for the treatment of heart failure 有权

    公开(公告)号：US09908919B2

    公开(公告)日：2018-03-06

    申请号：US14905333

    申请日：2014-07-21

    Applicant: Novartis AG

    Inventor： Frederic Zecri ,  Philipp Grosche ,  Kayo Yasoshima ,  Hongjuan Zhao ,  Jun Yuan

    IPC: A61K38/10 ,  A61K38/04 ,  C07K5/00 ,  C07K7/00 ,  C07K16/00 ,  C07K17/00 ,  C07K14/47 ,  A61K38/17 ,  A61K45/06 ,  A61K47/64 ,  A61K47/68

    CPC classification number: C07K14/47 ,  A61K38/10 ,  A61K38/1709 ,  A61K45/06 ,  A61K47/643 ,  A61K47/6811

    Abstract: The invention provides a synthetic polypeptide of Formula I (SEQ ID NO: 1): X1-R-X3-R-L-X6-X7-K-X9-P-X11-X12-X13  I 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.

    Fatty acids and their use in conjugation to biomolecules
    18.
    发明授权
    Fatty acids and their use in conjugation to biomolecules 有权

    公开(公告)号：US10588980B2

    公开(公告)日：2020-03-17

    申请号：US14738272

    申请日：2015-06-12

    Applicant: Novartis AG

    Inventor： Alexandra Marshall Bruce ,  Aimee Richardson Usera ,  Frederic Zecri ,  Jun Yuan ,  Changgang Lou ,  Aaron Kanter

    IPC: A61K47/54 ,  A61K38/08 ,  A61K38/16 ,  A61K38/17 ,  A61K38/18 ,  A61K38/22 ,  A61K45/06 ,  C07C55/02 ,  C07C55/22 ,  C07C57/02 ,  C07C57/18 ,  C07C59/245 ,  C12N15/113

    Abstract: 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.

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