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40 results about "Apelin" patented technology

Apelin (also known as APLN) is a peptide that in humans is encoded by the APLN gene. Apelin is the endogenous ligand for the G-protein-coupled APJ receptor that is expressed at the surface of some cell types. It is widely expressed in various organs such as the heart, lung, kidney, liver, adipose tissue, gastrointestinal tract, brain, adrenal glands, endothelium, and human plasma.

Synthetic apelin mimetics for the treatment of heart failure

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.
Owner:NOVARTIS AG

Apj receptor compounds

The invention relates generally to compounds which are allosteric modulators (e.g., negative and positive allosteric modulators, allosteric agonists, and ago-allosteric modulators) of the G protein coupled receptor apelin, also known as the APJ receptor. The APJ receptor compounds are derived from the intracellular loops and domains of the the APJ receptor. The invention also relates to the use of these APJ receptor compounds and pharmaceutical compositions comprising the APJ receptor compounds in the treatment of diseases and conditions associated with APJ receptor modulation, such as heart diseases (e.g., hypertension and tension and heart failure, such as congestive heart failure), cancer, diabetes, stem cell trafficking, fluid homeostasis, cell proliferation, immune function, obesity, metastatic disease, and HIV infection.
Owner:ANCHOR THERAPEUTICS

Synthetic apelin mimetics for the treatment of heart failure

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.
Owner:NOVARTIS AG

Compositions and methods for treating cardiovascular and pulmonary diseases and disorders with apelin

Compositions and methods for treating cardiovascular and pulmonary diseases and disorders with apelin are disclosed. In particular, the invention relates to formulations comprising apelin encapsulated in liposome nanocarriers conjugated with polyethylene glycol (PEG) and their use in treatment of cardiovascular and pulmonary diseases and disorders. Encapsulation of apelin in PEG-conjugated liposomes significantly enhances efficacy, improves cellular uptake of apelin, and allows for sustained and extended release of apelin under physiological conditions.
Owner:RAJADAS JAYAKUMAR +2

Methods for detecting atrial fibrillation and related conditions

Methods for detecting disorders associated with atrial fibrillation, and, thus, at risk for stroke and / or heart failure) in a subject based on a monitoring plasma levels of apelin are provided. Diagnostic compositions for the detection of such disorders are additionally provided.
Owner:THE GENERAL HOSPITAL CORP

Synthetic linear apelin mimetics for the treatment of heart failure

The invention provides a synthetic polypeptide of Formula I′ (SEQ ID NO: 1):X1-X2-X3-R—X5-X6-X7-X8-X9-X10-X11-X12-X13  Ior an amide, an ester or a salt thereof, wherein X1, X2, X3, 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.
Owner:NOVARTIS AG

Apelin and uses thereof

The invention provides a method of treating or preventing heart failure or a disease or condition associated with heart failure comprising administering an effective dose of an apelin peptide or APJ receptor ligand to the subject. According to certain embodiments of the invention the apelin peptide is administered chronically. In certain embodiments of the invention the apelin peptide is administered in an amount effective to improve at least one hemodynamic parameter or prognostic variable for heart failure. Clinical conditions associated with heart failure include, but are not limited to, atherosclerosis, restenosis, ischemic cardiovascular diseases, idiopathic or viral cardiomyopathy, and the like.
Owner:THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIV

Bioconjugates of synthetic apelin polypeptides

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.
Owner:NOVARTIS AG

Use of compounds inhibiting apelin / apj / gp130 signaling for treating cancer

Today, despite current advances in combinatorial therapies such as surgery, radiotherapy and chemotherapy, aggressive cancers remain fatal. Cancer stem-like cells (CSCs) may account for chemotherapy resistance and thus represent a promising therapeutic target. In this context, the present inventors identified essential intracellular pathways favoring the self-renewal and survival of CSCs. More precisely, the present inventors showed that the cytokine co-receptor GP130 acts as a co-receptor for Apelin / APJ signaling and that the interaction of Apelin with APJ / GP130 activates a dual signaling pathway involving the Akt / mTOR and STAT3 transcription factor, thereby promoting CSCs survival and self-renewal. They therefore propose to block these pathways in order to treat patients suffering from tumors containing CSCs, such as glioblastomas. In another aspect, the invention relates to the use of the Apelin expression level for evaluating the survival probability of a subject suffering from glioblastoma.
Owner:CENT NAT DE LA RECHERCHE SCI +2

Cyclic apelin derivatives for the treatment of heart failure

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.
Owner:NOVARTIS AG

Cyclic apelin derivatives for the treatment of heart failure

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  Ior 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.
Owner:NOVARTIS AG

APJ Receptor Compounds

The invention relates generally to compounds which are allosteric modulators (e.g., negative and positive allosteric modulators, allosteric agonists, and ago-allosteric modulators) of the G protein coupled receptor apelin, also known as the APJ receptor. The APJ receptor compounds are derived from the it intracellular loop and domain of the APJ receptor. The invention also relates to the use of these APJ receptor compounds and pharmaceutical compositions comprising the APJ receptor compounds in the treatment of diseases and conditions associated with APJ receptor modulation, such as cardiovascular diseases, (e.g., hypertension and heart failure, such as congestive heart failure), cancer, diabetes, stem cell trafficking, fluid homeostasis, cell proliferation, immune function, obesity, metastatic disease, and HIV infection.
Owner:ANCHOR THERAPEUTICS

Freeze-dried powder for treating focal cerebral ischemia reperfusion inflammation reaction and preparation method thereof

InactiveCN104399064AReduce releaseReduce MPO activityPowder deliveryPeptide/protein ingredientsCytotoxic substancesTreatment effect
The invention discloses a freeze-dried powder for treating focal cerebral ischemia reperfusion inflammation reaction and a preparation method thereof. The freeze-dried powder is composed of Apelin-13, human serum albumin, mannitol, dextran and arginine. The freeze-dried powder is prepared by steps of raw materials mixing, activated carbon adsorption, filtering, micro-filtration and freeze drying. The freeze-dried powder can obviously reduce cerebral infarction volume and has good treatment effect for treating focal cerebral ischemia reperfusion inflammation injury; the freeze-dried powder can reduce MPO activity in hippocampus, performs up-regulation of expression level of APJ protein, decreases Iba1, GFAP and HMGB1 protein expression level; inhibits activation, adhesion and aggregation of neutral granulocyte in a cerebral ischemia zone, minimizes release of cytotoxic substances, mitigates inflammation reaction in an ischemic zone and performs neuroprotection effect.
Owner:JINING MEDICAL UNIV

Device for treating diabetic nephropathy by using Apelin-13

InactiveCN108421129AImprove protectionProtective film for easy protectionInfusion syringesInfusion needlesApelinEngineering
The invention discloses a device for treating diabetic nephropathy by using Apelin-13. The device comprises an injection needle, a threaded rod mounting post and a syringe casing; the upper end of thesyringe casing has a syringe baffle, and a piston drawing rod is arranged inside the syringe casing; a piston pressing head is disposed on an end of the piston drawing rod near the user's hand; a drawing rod limiting buckle is disposed on an end of the piston drawing rod near the piston pressing head; a syringe piston is arranged on one end of the piston drawing rod away from the piston pressinghead; dosage marking scales are arranged on a front surface of the syringe casing; a syringe threaded rod is arranged under the syringe casing; a needle sealing protective film can protect the injection needle, can prevent the needle from being polluted by external pathogenic bacteria, can improve the use safety, can protect the needle, and can avoid the problem that the needle is damaged during transportation.
Owner:胥小鹏

Synthetic linear apelin mimetics for the treatment of heart failure

The invention relates to novel compositions comprising modified apelin-13 peptide sequences designed to treat cardiovascular disease in subjects to whom they are administered, and which exhibit greater resistance to degradation, and equivalent or greater bioactivity than their wild type counterparts. The invention also relates to methods of making said compositions and using said compositions as pharmaceutically active agents to treat cardiovascular disease.
Owner:NOVARTIS AG

Application of Apelin in preparation of medicine for treating silicosis

The invention belongs to the technical field of active peptides of medicines, and discloses application of Apelin in preparation of medicines for treating silicosis. Tests show that Apelin has a good curative effect on relieving diseases of silicosis, has a good medicinal value prospect, and can be developed into a novel medicine for treating silicosis.
Owner:广东省职业病防治院 +1

Apelin liposome and preparation method thereof

The present invention provides a kind of Apelin liposome and preparation method thereof, this Apelin liposome comprises Apelin, phosphatidylglycerol, phosphatidylcholine, cholesterol, phosphatidylethanolamine-polyethylene glycol derivative, and Apelin and phosphatidylglycerol The molar ratio is 1:2~1:10. The Apelin liposome of the invention realizes high-efficiency encapsulation of Apelin, with an encapsulation rate of more than 90%, and at the same time significantly prolongs the half-life of Apelin in a living body.
Owner:KUNMING JIDA PHARMA

Application of [pyr1]‑apelin‑13 as a rescue drug for cardiac arrest caused by long-acting amide local anesthetic poisoning

The invention discloses an application of (Pyr<1>)-Apelin-13 as a salvage drug for cardiac arrest caused by long-term amide class local anesthetics toxicity. The technical scheme includes that the salvage drug comprises (Pyr1)-Apelin-13 with the sequence to be: Glp-Arg-Pro-Arg-Leu-Ser-His-Lys-Gly-Pro-Met-Pro-Phe. The application has the advantages that the salvage drug on the basis of the (Pyr<1>)-Apelin-13 can be used for effectively saving cardiac arrest caused by local anesthetic toxicity, and recovery rate is increased; secondary mortality is lower as compared with recognized use of lipid emulsion with epinephrine, and 60-minute survival rate is higher.
Owner:THE FIRST AFFILIATED HOSPITAL OF WENZHOU MEDICAL UNIV

Preparation method of active peptide Apelin

The invention relates to a preparation method of an active peptide Apelin, which comprises the steps of preparing Apelin by adopting a solid-phase synthesis method, and further connecting 2-(4-chlorphenyl)-2,2-difluoroacetic acid by adopting the solid-phase synthesis method. The active peptide Apelin (2-(4-chlorphenyl)-2,2-difluoroacetic acid-QRPRLSHKGPMPF) is obtained through the solid-phase synthesis method, and the activity of the active peptide Apelin obtained on the basis of the method can be further improved while the half-life period of the active peptide Apelin can be prolonged.
Owner:温州医科大学慈溪生物医药研究院 +1

Pharmaceutical composition containing Apelin-12 and application of pharmaceutical composition

PendingCN109395057AThe ideal effect of promoting platelet aggregationAvoid formingPeptide/protein ingredientsBlood disorderMedicineApelin
The invention relates to an endogenous ligand Apelin-12. The endogenous ligand can promote platelet aggregation and thrombosis by acting on an APJ receptor and can cooperate ADP and collagen induced platelet aggregation and thrombosis promoting functions. The Apelin-12 is used as a novel drug for promoting platelet aggregation and thrombosis in fundamental research of hemorrhagic diseases.
Owner:NANHUA UNIV

Synthetic apelin fatty acid conjugates with improved half-life

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.
Owner:NOVARTIS AG

A pharmaceutical composition for treating cerebral apoplexy and acute cerebral infarction

The invention relates to a pharmaceutical composition for treating cerebral apoplexy and acute cerebral infarction, which uses active peptide Apelin as an active ingredient, and the structure of the active peptide Apelin is 2-(4-chlorophenyl)-2,2- Difluoroacetic acid‑QRPRLSHKGPMPF. The pharmaceutical composition of the present invention has bidirectional therapeutic effects on ischemic stroke, can relieve ischemic stroke neurological dysfunction, and reduce cerebral infarction volume.
Owner:温州医科大学慈溪生物医药研究院 +1

Preparation method of active peptide apelin

The invention relates to a preparation method of the active peptide Apelin, which comprises the step of linking 2-(4-chlorophenyl)-2,2-difluoroacetic acid through a solid-phase synthesis method after preparing Apelin by a solid-phase synthesis method. The present invention obtains the active peptide Apelin (2-(4-chlorophenyl)-2,2-difluoroacetic acid-QRPRLSHKGPMPF) through a solid-phase synthesis method, and the active peptide Apelin obtained based on this method can prolong the half-life while further improving its activity.
Owner:温州医科大学慈溪生物医药研究院 +1
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