30 results about "Formyl peptide receptor" patented technology

Provided is a compound having a formyl peptide receptor like 1 (FPRL1) agonist effect.The present invention relates to a compound represented by the general formula (I) or a pharmacologically acceptable salt thereof. The present invention also relates to a pharmaceutical composition containing the compound represented by the general formula (I) or a pharmacologically acceptable salt thereof.

Disclosed are peptides having SEQ ID NOs: 1 to 24 that induce superoxide generation by human monocytes or neutrophils; that induce an intracellular calcium increase by human peripheral blood monocytes or neutrophils; binds to formyl peptide receptor or formyl peptide receptor-like 1; that induce chemotactic migration of human monocytes or neutrophils in vitro; that induce degranulation in formyl peptide receptor expressing cells or formyl peptide receptor-like 1 expressing cells; that stimulate extracellular signal regulated protein kinase phosphorylation via activation of formyl peptide receptor or formyl peptide receptor-like 1; or that stimulate Akt phosphorylation via activation of formyl peptide receptor or formyl peptide receptor-like 1.

The invention provides novel application of proanthocyanidin oligomer F2 and a polymer F3 in preparing anti-tumor health care food and medicine, in particular novel application in preparing health care food and medicine for treating glioma. The application researches inhibiting function of F2 on brain tumor, blood system tumor, alimentary canal tumor, respiratory system tumor and urinary genital system tumor. Firstly, F2 and F3 are discovered to have the inhibiting functions on glioma cell strains U-87 and U251, humanized leukemia HL-60 cell strains, humanized liver cancer Hep3B cell strains, humanized colon cancer Colon-205 cell strains, humanized prostate cancer Du-145 cell strains and humanized A549 lung cancer cell strains, and the inhibiting function is improved along with progressive increase of dosage. In addition, the F2 can also remarkably inhibit chemotaxis of human malignant glioma U-87 cells induced by formyl peptide and expression of formyl peptide receptor (FPR) in the cells. The receptor has important function on mediating migration, survival, growth and vasculogenesis of the human malignant glioma cells.

The present invention relates to imidazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor.

The invention features a transgenic mouse that expresses human formyl peptide receptor and methods for producing this mouse. The invention also features methods for the measurement of an inflammatory response, particularly that associated with cystic fibrosis. The methods of the invention also feature methods for determining whether a compound inhibits or prevents the recruitment of neutrophils.

The present application relates to a pharmaceutical preparation to be administered into respiratory organs for treating or preventing inflammatory respiratory diseases, comprising a peptide which acts on formyl peptide receptors (FPRs) or receptors analogous thereto, in an amount which is effective in suppressing respiratory inflammation. The present application also relates to a method for treating or preventing inflammatory respiratory diseases by using the preparation, and to a kit containing the preparation. As compared with systemic administration of the peptide by injection, direct administration of the peptide to respiratory organs remarkedly improves the effect in suppressing respiratory inflammation.

A compound that comprises Met-Leu-Phe or Nle-Leu-Phe serving as the leukocyte-binding site of a formyl peptide receptor (FPR), a binding part comprising Ser or Thr that increases the binding ratio to monocytes and lymphocytes in all leukocytes, a group that can be labeled with a radioactive metal or a paramagnetic metal, and spacers binding the three moieties together shows binding properties specific to all leukocytes, i.e., neutrophils, monocytes and lymphocytes both in vivo and in vitro. Owing to this characteristic, this compound is highly useful in SPECT image diagnosis, PET image diagnosis, MRI image diagnosis and the like, for imaging sites of inflammation.

The invention discloses anti-inflammation compounds and a preparation method thereof. The structural formula of the anti-inflammation compounds is cFLFFX1X2, which is tetradecanoyl-phenylalanyl-(D)-lencyl-phenylalanyl-(D)-lencyl-phenylalanyl- or cinnamoyl-phenylalanyl-(D)-lencyl-phenylalanyl-(D)-lencyl-phenylalanine. The antagonist compounds are targeting formyl peptide receptors and have an anti-inflammation effect. The compounds are composed of two parts: a formyl peptide receptor targeting small molecule peptide and an anti-oxidation group and are used to treat bacterium-free inflammation or bacterial inflammation in clinic. Through the formyl peptide receptor, the leukocyte activation time, process and degree can be regulated and controlled directly, thus the whole treatment process has the advantages that the spectrum is wider, the treatment is more reliable, and the side effect is weaker; the patients can be recovered more quickly; the inflammation can be removed more quickly; and at the same time, the patients do not need to eat steroid anti-inflammation drugs or non-steroid anti-inflammation drugs and do not need to worry about side effects and drug resistance.

The invention discloses a synthetic method for a quinazolinone FPR2 formyl peptide receptor agonist. The method is specifically implemented according to the following steps of: weighing isatoic anhydride, an aromatic hydrazide compound and an aromatic aldehyde compound with the ratio of amount of substance of 1:1:1 as raw materials; after mixing the raw materials in a solvent, performing a one-pot synthetic reaction by taking a nano metal oxide as a catalyst; and separating and purifying a reaction product after the reaction by virtue of column chromatography to obtain the quinazolinone FPR2 formyl peptide receptor agonist. The synthetic method disclosed by the invention reduces the complexity of preparation by simplifying the preparation process, and moreover, the reaction condition is mild, the raw materials are low in price and are easily available, the product is high in yield, and the solvent in the preparation process is non-toxic, so that the synthetic method has a good industrial application prospect.

The present invention describes methods of inhibiting the pro-inflammatory response of human peripheral blood mononuclear cells or polymorphonuclear cells, or fixed tissue cells. Contacting cells with pro-inflammatory agents stimulates a pro-inflammatory response. The cells are then contacted with a G protein kinase signaling pathway modifier, thereby inhibiting the G protein-mediated inflammatory response signaling pathway. The present invention describes receptor complexes in which G protein kinase signaling pathway modifiers bind to cell surface receptors of human peripheral blood mononuclear cells or polymorphonuclear cells stimulated with pro-inflammatory agents.

The present invention is directed to modulators of eosinophilic and neutrophilic function and the use of such modulators for treatment of eosinophil-associated and neutrophil-associated diseases.

The invention provides a microfluidic chip group used for screening a formyl peptide receptor agonist and a screening method. The microfluidic chip group consists of three microfluidic chip units, i.e. a cell chemotaxis detection unit, a receptor endocytosis detection unit and a calcium ion transient flow process monitoring unit. The invention designs a group of chips by aiming to the characteristics of different cell function analytical experiments, can respectively carry out cell chemotaxis, receptor endocytosis detection and calcium ion transient flow (release) process monitoring, and judges biologic activity thereof by comprehensively evaluating influence on the formyl peptide receptor signal conduction path by an alternative compound. Compared with the traditional technology, the invention realizes real-time monitoring of the intracellular calcium ion releasing process and saves a series of complex operations, such as film laying, film obtaining, cell doctoring, fixing, dying andthe like, thereby greatly saving the analysis time and lowering the detection cost.

The present disclosure relates to methods and applications for detecting the content of formyl peptide or formyl peptide receptor-1 ligand. Specifically, the present disclosure relates to the use of reagents for detecting FPR1 ligands in the preparation of reagents or kits for detecting acute brain injury or changes in brain edema, and methods for evaluating and predicting changes in brain edema after acute brain injury such as cerebral hemorrhage method. Through the above application and method, it can be determined that the level of N-formylphthalein or FPR1 ligand in peripheral blood is positively correlated with the progress of perihematoma edema after cerebral hemorrhage, and is used to evaluate and predict acute brain injury such as changes in perihematoma brain edema after cerebral hemorrhage , to provide a biomarker basis for judging the evolution of brain damage.

The present invention provides a urea derivative or a pharmacologically acceptable salt thereof that has a formyl peptide receptor like 1 (hereinafter may be abbreviated as FPRL1) agonist effect, a pharmaceutical composition containing the urea derivative or the pharmacologically acceptable salt thereof, and a pharmaceutical use thereof. It has been found that a urea derivative represented by the general formula (I) below or a pharmacologically acceptable salt thereof has a superior FPRL1 agonist effect. Compound (I) or a pharmacologically acceptable salt thereof is highly useful for treatment, prevention, or suppression of inflammatory diseases, chronic airway diseases, cancers, septicemia, allergic symptoms, HIV retrovirus infection, circulatory disorders, neuroinflammation, nervous disorders, pains, prion diseases, amyloidosis, immune disorders and the like.

The present invention provides a urea compound or a pharmacologically acceptable salt thereof that has a formyl peptide receptor like 1 (hereinafter may be abbreviated as FPRL1) agonist effect, a pharmaceutical composition containing the urea compound or the pharmacologically acceptable salt thereof and a pharmaceutical use thereof. It has been found that a urea derivative represented by the general formula (I) below or a pharmacologically acceptable salt thereof has a superior FPRL1 agonist effect. Compound (I) or a pharmacologically acceptable salt thereof is highly useful for treatment, prevention, or suppression of inflammatory diseases, chronic airway diseases, cancers, septicemia, allergic symptoms, HIV retrovirus infection, circulatory disorders, neuroinflammation, nervous disorders, pains, prion diseases, amyloidosis, immune disorders and the like.

The present invention relates to N-phenyl carbamate derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide 2 receptor.

The present invention is directed to modulators of eosinophilic and neutrophilic function and the use of such modulators for treatment of eosinophil-associated and neutrophil-associated diseases.