57 results about "Adenosine receptor" patented technology

The invention provides an anti-aging repair composition containing PDRN, and lipid nanoparticles and application thereof. The composition provided by the invention is prepared from polydeoxyribonucleotide, micro-current tetrapeptide-1 and palmitoyl tripeptide-5. According to the application, the polydeoxyribonucleotide, the micro-current tetrapeptide-1 and the palmitoyl tripeptide-5 are compounded for use, so that the composition has a synergistic effect in the aspects of promoting cell proliferation, inhibiting an intracellular ROS (reactive oxygen species) level and the like, and has remarkable antioxidant, anti-inflammatory, anti-aging, soothing and repairing effects. The PDRN-containing composition is prepared into the lipid nanoparticles, so that the stability of the PDRN-containing composition is improved, the permeability of the PDRN-containing composition on the skin surface is improved, the bioavailability of the PDRN-containing composition is improved, the cell survival rate and cell uptake are promoted, the expression of adenosine A2A receptors, the synthesis of collagen, angiogenesis and the inhibition of anti-inflammatory factors are promoted, and a remarkable anti-aging effect is achieved.

The invention relates to an anti-fatigue refreshing functional chewing gum containing natural active ingredients, which relates to the technical field of food, and comprises a gum base, a natural sweetening agent and an active ingredient mixture, the mustard extract and coffee are innovatively combined to form a dual-channel nerve activation mechanism, the mustard extract realizes instant refreshing through a targeted oral trigeminal nerve TRPA1 ion channel, caffeine maintains continuous excitation through antagonism of a central adenosine receptor, and the space-time cooperation of the mustard extract and the coffee breaks through the limitation of a single path. Meanwhile, a rhodiola rosea extract, a sea-buckthorn extract, an American ginseng extract and astragalus polysaccharide are compounded, so that a triple anti-fatigue physiological barrier with functions of nerve regulation, oxidative stress inhibition and energy metabolism optimization is formed. In the preparation process, a microcapsule embedding technology is adopted to control slow release of mustard active ingredients, menthol flavor is combined to synergistically trigger TRP channel dual activation, and unification of efficacy and palatability is achieved.

The invention belongs to the technical field of biological medicines, and particularly relates to application of an adenosine A2a / A2b receptor dual antagonist in preparation of an anti-depression medicine and a medicine for preventing or treating depression. The invention provides a new application of the adenosine A2aR / A2bR double antagonist, animal experiments prove that the adenosine A2aR / A2bR double antagonist AB928 can effectively treat depression of mice, does not have obvious toxic or side effects, increases indications of the AB928, and has a prospect of being applied as an anti-depression drug in practice, so that the medical application of the adenosine A2aR / A2bR double antagonist AB928 is further expanded.

The present invention concerns an A3 adenosine receptor (A3AR) ligand for use in the treatment of an advanced solid tumor, e.g., hepatocellular carcinoma (HCC) in a mammalian subject.

The present invention provides anti-A2aR antigen binding molecules, including antibodies and the antigen binding fragment thereof, and methods for using the same for treating a variety of diseases associated with aberrant adenosine signaling, including cancers, chronic diseases, chronic infections, autoimmune diseases, inflammatory diseases, neurodegenerative diseases, and fibrotic diseases.

The present invention relates to macrocyclic diamine derivatives of Formula II, including pharmaceutically acceptable salts and solvates thereof. The compounds of the present invention are inhibitors of ENT family transporters, particularly ENT1, and are useful as therapeutic compounds for the treatment of cancer. The present invention also relates to the combination of a macrocyclic diamine derivative with an adenosine receptor antagonist for the treatment of cancer. JPEG2023521351000310.jpg36123

The present invention relates to compounds having the formula I: wherein R0, R1, R2, R3 and A are each as defined in the application. The invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of diseases or conditions associated with adenosine A2a receptor activity, such as cancer.

The invention discloses a research method for influence on a post-TBI impulse behavior, and relates to the technical field of traumatic brain injury treatment. The method comprises the following steps: S1, preparing experimental animals, instruments and equipment, reagents and solutions, and grouping the experimental animals; s2, establishing a mouse TBI model by adopting a controllable cortex attack (CCI) mode, and judging the injury severity of the mouse TBI model through nerve function defect scoring (NSS); according to the method, by adopting an immune western blot method, immunofluorescent staining and real-time fluorescent quantitative PCR, the change of lipid droplet metabolism and neuronal functions after TBI can be deeply analyzed from protein and gene levels, multi-level data support is provided, transcranial direct current stimulation and adenosine A2a receptor regulation are used as intervention means, and the method has the advantages that the method is simple and convenient to operate, and the application prospect is wide. The improvement effect of the tDCS on the impulse behavior after the TBI is explored, and particularly, a mechanism that the tDCS regulates A2AR and Plin2 to inhibit lipid droplet accumulation provides a new thought for TBI treatment.

The application provides application of an adenosine A2B receptor as a target in a medicine for preventing and / or treating itch, and belongs to the technical field of biological medicines. Based on previously reported single-cell RNA sequencing data of a mouse dorsal root ganglion (DRG), expression of genes encoding main ligand ion channels is detected, Adora2b highly expressed in Neuron_10 is detected, and it is indicated that Adora2b and a receptor (adenosine A2B receptor) of Adora2b can participate in regulating itch. Experiments prove that the activity of the adenosine A2B receptor can be effectively blocked to prevent a histamine-induced scratching behavior of a mouse, and it is indicated that the A2B receptor participates in histamine-induced itch sensation. The application also provides application of a reagent for inhibiting biological functions of the adenosine A2B receptor in preparation of a medicine for preventing and / or treating itch, and provides a new means for prevention and treatment of itch.

Provided herein are methods and compositions relating to an adenosine A2A receptor library having nucleic acids encoding scaffolds comprising adenosine A2A binding domains. The adenosine A2A receptor library described herein encodes immunoglobulins such as antibodies.

The invention relates to the technical field of medicines, and particularly provides application of a 6-(substituted pyridine-4-yl)-5-(substituted phenyl)-1, 2, 4-triazine compound derivative in preparation of an antidepressant drug. A cell experiment proves that the 6-(substituted pyridine-4-yl)-5-(substituted phenyl)-1, 2, 4-triazine compound is an antagonist of an adenosine 2A receptor, and a plurality of animal model experiments prove that the 6-(substituted pyridine-4-yl)-5-(substituted phenyl)-1, 2, 4-triazine compound has a relatively good treatment effect on a plurality of depression models. The compound has an application prospect of being used as an anti-depression treatment drug.

Described herein are cyclic amide-containing pyridyl-xanthines of formula I and pharmaceutical compositions thereof that are useful as antagonists of A2B adenosine receptors.

The present disclosure relates to compositions and methods for the diagnosis and treatment or prevention of cancers, particularly cancers that exhibit elevated expression of FOXA1 and / or FOXA1 gene targets, such as certain breast, liver and / or prostate cancers, including luminal and / or ER-positive forms of breast cancer. Three previously identified adenosine receptor antagonists, CGS-15943, MRS-1220 and SCH-58261, as well as furan ring moiety-possessing derivatives of CGS-15943 are specifically provided for killing cancer cells in a manner that appears to involve activation of the aryl hydrocarbon receptor (AHR) by such compounds. The instant disclosure therefore provides for selecting and / or administering CGS-15943, MRS-1220, SCH-58261 and / or a furan-possessing derivative of CGS-15943, MRS-1220 and / or SCH-58261 as a therapeutic agent to target a cancer cell and / or subject having or at risk of developing a cancer. Methods and compositions for therapies that include such compounds are also provided.

The present invention relates to compounds of formula I shown below:wherein R1, R4, R5 and R6 are each as defined in the application. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of diseases or conditions in which adenosine A2a and / or A2b receptor activity is implicated, such as, for example, cancer.

The present disclosure relates generally to adenosine receptor modulator compounds of formula (I), and methods of using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of A2B adenosine receptor activity.

Use of an adenosine A2B receptor as a target in drugs for prevention and / or treatment of pruritus and belongs to the technical field of biological pharmaceuticals. Expression of genes encoding major l

This disclosure provides a compound of formula I, or a pharmaceutically acceptable salt, complex, hydrate, solvate, tautomer, polymorph, stereoisomer, racemic compound, or a pharmaceutically active derivative thereof. The compound of formula I is used as an adenosine receptor antagonist. This disclosure also provides a method for preparing the compound of formula I and pharmaceutical compositions thereof.

A method, a computer-readable medium and a system for assessment of a hemodynamic response to an Adenosine receptor agonist stimulation for a human patient are disclosed. Starting point for the method are non-invasive pressure data in the resting state. Said data are used in pharmacokinetic / pharmacodynamic modeling to arrive at an individual patient-specific response for an adenosine receptor stimulation by an agonist. This response is used to a calibrate lumped-parameter Windkessel type model of a blood circulation. The calibrated model allows for calculating of hemodynamic parameters for the hyperemic state, in particular to calculate flow and pressure values in both coronary arteries inlets. The hemodynamic parameters allow for in silico coronary vessel diagnostic. The effectiveness of the developed method has been confirmed in multi-center clinical trials.

The invention belongs to the field of platelet differentiation, and particularly relates to application of an adenosine A2a receptor stimulant in induced differentiation of platelets. The invention provides an application of an adenosine A2a receptor agonist in inducing differentiation of hematopoietic stem progenitor cells and / or megakaryocyte progenitor cells to generate platelets. The adenosine A2a receptor agonist contains Redelbrusone; in addition, the invention further provides a culture medium containing the adenosine A2a receptor stimulant and application of the culture medium in preparation of platelets through in-vitro differentiation, and provides an in-vitro differentiation method of the platelets, and the in-vitro differentiation method of the platelets improves the yield of the platelets by nearly one time.

Described herein are triazalone compounds of Formula (I): and pharmaceutically acceptable salts thereof. Methods of making and using compounds of Formula (I) are also described. Compounds of Formula (I) and pharmaceutically acceptable salts thereof can be useful as adenosine receptor antagonists, for example in the treatment of diseases or conditions mediated by the adenosine receptor, such as cancer, movement disorders, or attention disorders.

Provided here are pharmaceutical formulations containing A2B adenosine receptor antagonists and one or more excipients. The method of treating diseases or disorders associated with or would benefit from modulation of A2B adenosine receptor activity, and the combination treatment thereof are also provided.

The present disclosure provides a compound of formula I or its pharma- ceutically acceptable salts, complexes, hydrates, solvates, tautomers, polymorphs, stereoisomers, racemates, and pharma- ceutically active derivatives thereof. The compound of formula I acts as an antagonist to adenosine receptors. The present disclosure also provides processes for the preparation of the compound of formula I and its pharmaceutical compositions. TIFF2024507022000440.tif50163

This application provides an anti-aging and repairing composition containing PDRN, its lipid nanoparticles, and its applications. The composition provided in this application includes polydeoxyribonucleotides, microcurrent tetrapeptide-1, and palmitoyl tripeptide-5. This application combines polydeoxyribonucleotides, microcurrent tetrapeptide-1, and palmitoyl tripeptide-5, exhibiting synergistic effects in promoting cell proliferation and inhibiting intracellular ROS levels, resulting in significant antioxidant, anti-inflammatory, anti-aging, soothing, and repairing effects. This application prepares the PDRN-containing composition into lipid nanoparticles, improving the stability of the PDRN-containing composition and increasing its permeability to the skin surface, thereby enhancing its bioavailability, promoting cell survival and uptake, adenosine A2A receptor expression, collagen synthesis, angiogenesis, and inhibiting anti-inflammatory factors, achieving significant anti-aging effects.

The present invention relates to compounds having the following Formula I: wherein R0, R1, R2, R3 and A are each as defined herein. The invention also relates to processes for preparing these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of diseases or conditions associated with adenosine A2a receptor activity, such as cancer.

This text describes triadimefon compounds of formula (I) and their pharmaceutically acceptable salts. Methods for preparing and using the compounds of formula (I) are also described. The compounds of formula (I) and their pharmaceutically acceptable salts can be used as adenosine receptor antagonists, for example, for treating diseases or disorders mediated by adenosine receptors, such as cancer, movement disorders or attention disorders.

The invention relates to lemon and mint flavored refreshing anti-fatigue chewing gum containing natural active ingredients, and belongs to the technical field of food. Through synergistic compounding of the rhodiola rosea extract, the sea-buckthorn extract, caffeine and the American ginseng extract, central nervous excitation and mitochondrial energy metabolism pathways are synchronously activated in the oral chewing process, and the dual effects of instant refreshing and long-acting fatigue resistance are achieved. Wherein the caffeine blocks an adenosine receptor to realize rapid wakeup, the rhodiola rosea and the American ginseng jointly enhance cell energy synthesis, the sea-buckthorn component protects neurons from oxidative damage, and ginseng and astragalus membranaceus extracts can be selected to improve cerebral blood flow supply. According to the product, lemon and mint flavor is adopted for optimizing experience, all components are selected from a medicinal and edible catalog, the stability of active substances is guaranteed through a fine processing technology, and finally, a functional food which is safe and independent and has instant refreshing and continuous anti-fatigue capabilities is formed.

Cisplatin is a potent chemotherapeutic drug, widely used in the treatment of various solid cancers. However, its clinical effectiveness is strongly limited by frequent severe adverse effects, such as neuropathy. Therefore, there is an urgent medical need to identify novel strategies limiting cisplatin-induced pain. Here, the inventors provide evidence that the FDA-approved adenosine A2A receptor antagonist istradefylline (KW-6002) significantly protects from cisplatin-induced neuropathy in experimental models of sub-chronic cisplatin treatment. In particular, the present invention relates to a method for the treatment of neuropathy (e.g. CIPN) in a subject in need therefore comprising administering to the subject a therapeutically effective amount of a selective A2A Adenosine Receptor (A2AR) antagonist.

The present invention relates to macrocyclic diamine derivatives of formula I, including pharmaceutically acceptable salts and solvates thereof. Compounds of the invention are inhibitors of ENT family transporter, especially of ENT1, and are useful as therapeutic compounds for the treatment of cancers. The invention also relates to the combined use of the macrocyclic diamine derivatives with an adenosine receptor antagonist, for the treatment of cancers.

A compound represented by formula (I) and a pharmaceutical composition thereof. The compound represented by formula (I) can be used as an adenosine receptor inhibitor, in particular, A2A and / or A2B inhibitors, for example, can be used for preventing or treating diseases related to A2A and / or A2B activity or expression level.