40 results about "Apelin" patented technology

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.

The present invention relates to the preparation method of [Pyr1]-apelin-13, comprising: step (1), the phenylalanine resin is placed in the reaction bottle for swelling treatment; step (2), adding to the reaction bottle containing The mixed solution of the raw material amino acid Fmoc-Pro-OH of the group, coupling agent and DMF carries out the coupling reaction, then deprotects and removes the protecting group Fmoc; step (3), uses Fmoc-Met-OH, Fmoc-Pro in sequence -OH, Fmoc-Gly-OH, Fmoc-Lys(Boc)-OH, Fmoc-His(Trt)-OH, Fmoc-Ser(tBu)-OH, Fmoc-Leu-OH, Fmoc-Arg(Pbf)-OH , Fmoc-Pro-OH, Fmoc-Arg(Pbf)-OH and Boc-Pyr-OH carry out step (2) respectively, do not remove Boc after the Boc-Pyr-OH coupling is completed, and obtain a side chain protecting group [Pyr1]-apelin-13 protected peptide resin; step (4), cleavage to obtain [Pyr1]-apelin-13 crude peptide; step (5), purification to obtain [Pyr1]-apelin-13. The preparation method is safe, environment-friendly, high in yield and high in purity.

The present invention provides compounds of Formula (I): wherein all variables are as defined in the specification. The compounds are apelin and APJ agonists for treating cardiovascular diseases. Preferred compounds are 2-(1,1′-biphe-1H-benzo[d]imidazole derivatives. The invention further provides compositions comprising the compounds and the compounds for use in methods of medical treatment.

The invention discloses the application of Apelin protein in preparing reagents for diagnosing respiratory system diseases. The present invention is the first discovery that Apelin-13, especially the combination of Apelin-13, GP73 (Golgi apparatus transmembrane glycoprotein) and Cys-C (cystatin C) can be used as a diagnosis of respiratory diseases, especially the diagnosis of acute lung injury Markers can effectively improve the detection specificity of acute lung injury.

The invention discloses an application of Golgi apparatus outer membrane protein GOLPH3 as a biomarker in predicting cardiomyocyte hypertrophy, and an application of siRNA-GOLPH3 in preparing a medicine for preventing or treating cardiomyocyte hypertrophy. The Golgi apparatus outer membrane protein GOLPH3 can promote Golgiphagy, the novel selective autophagy can mediate Apelin-13 to promote cardiomyocyte hypertrophy, and the expression of interference GOLPH3 can inhibit Golgiphagy in cardiomyocytes and the effect of increasing diameter and volume of cardiomyocytes by Apelin-13.