36 results about "Apelin" patented technology

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.

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.

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.

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  I

• • or 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.

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.

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.

The invention relates to a pharmaceutical composition for treating cerebral apoplexy and acute cerebral infarction. The pharmaceutical composition takes active peptide Apelin as an active ingredient,and the structure of the active peptide Apelin is 2-(4-chlorphenyl)-2, 2-difluoroacetic acid-QRPRLSHKGPMPF. The pharmaceutical composition disclosed by the invention has a bidirectional treatment effect on cerebral arterial thrombosis, and can relieve neurological dysfunction of the cerebral arterial thrombosis and reduces the cerebral infarction volume.

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.

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.

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.

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.

The invention discloses an application of Apelin protein in preparation of a reagent for diagnosing respiratory system diseases. What is found for the first time is that the combination of Apelin-13, especially Apelin-13, GP73 (Golgi Transmembrane Glycoprotein) and Cys-C (cystatin C), can be used as a diagnostic marker for diagnosing respiratory system diseases, especially acute lung injury, and the detection specificity of acute lung injury can be effectively improved.