34 results about "Adenosine receptor" patented technology

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 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 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.

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.

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.

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.

To provide a method for treating a disease. [Solution] A 2B Compounds, compositions, formulations, and methods for modulating adenosine receptors are disclosed in this specification. The specification includes compounds, methods for producing such compounds, pharmaceutical compositions and formulations containing such compounds, and somatostatin A 2B Methods of using such compounds in the treatment of diseases, disorders, or conditions for which adenosine receptor activity is to be beneficial are described.

The invention discloses application of an adenosine receptor stimulant in preparation of a medicine for improving multiple organ injuries, and belongs to the technical field of medicines. In-vivo and in-vitro experiments prove that the adenosine receptor stimulant can improve multiple organ injuries, especially multiple organ injuries caused by sepsis and syndromes after cardiac arrest. Further, the adenosine receptor stimulant is proved to be capable of improving the organ function recovery level of a patient with sepsis multi-organ function impairment; the clinical prognosis of the patient with the post-cardiac arrest syndrome is improved, especially the brain and heart function recovery is improved, and the survival rate of the patient with the multi-organ function impairment is improved. Meanwhile, starting from the core ATP of human body energy metabolism, the purpose of improving multiple organ injuries is achieved by regulating adenosine and adenosine receptors, and the method has a protection effect on the heart, brain, lung and the like of the important organs of the human body, and is safe and free of toxic and side effects. Therefore, the application way of the invention can increase treatment means and strategies, and further promote continuous improvement of the treatment technology.

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.

The present disclosure relates to a method of preventing, treating, or ameliorating a release apoptosis (NETosis)-mediated disease in a subject, the method comprises administering to the individual an active agent selected from the group consisting of adenosine receptor (AR)-specific antagonist or inhibitor, protein arginine deiminase 4 (PAD4)-specific antagonist or inhibitor, and elastin-specific antagonist or inhibitor.

The present invention relates to new agents useful for in the treatment of cancers, in particular by immunotherapy, as well as pharmaceutically acceptable salts thereof. In particular, this invention provides new A2AR modulators, pharmaceutical compositions and uses thereof.

The present disclosure provides a compound of Formula I or its pharmaceutically acceptable salts, complexes, hydrates, solvates, tautomers, polymorphs, stereoisomers, racemates, pharmaceutically active derivatives thereof. The compounds of Formula I act as antagonists to adenosine receptors. The present disclosure also provides a process for preparation of compounds of Formula I and pharmaceutical composition thereof.

In its many embodiments, the invention provides compounds of structural Formula (I): (I), and pharmaceutically acceptable salts thereof, wherein, ring A, R1, R2 and R3 are as defined herein, and pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutically active agents). The invention further provides methods for the preparation and use of the compounds of the invention, or a pharmaceutically acceptable salt thereof, alone and in combination with other therapeutic agents, as antagonists of A2a and / or A2b receptors, and in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2a receptor and / or the adenosine A2b receptor.

The invention discloses a bionic nano-carrier capable of reversibly regulating and controlling a blood brain barrier and application of the bionic nano-carrier. The bionic nano-carrier is of a core-shell structure, a lecithin surface modified inorganic nano-material serves as a core, a cell membrane of brain metastatic cancer cells coats the surface of the core to serve as a shell, and an A2A adenosine receptor agonist is loaded in a cell membrane coating layer. The blood brain barrier crossing efficiency is further improved; wherein the lecithin surface modified inorganic nano-material is obtained by using an oleic acid modified inorganic nano-material as a matrix and carrying out surface modification through amphiphilic ligand lecithin. The bionic nano-carrier regulates and controls the blood-brain barrier permeability in a reversible mode, the problems that the brain transfer efficiency of a brain metastatic cell membrane bionic carrier through a cell bypass path is limited, potential safety hazards exist in a traditional blood-brain barrier permeability regulation and control open means and the like are solved, and a new strategy is provided for efficient brain delivery.

Adenosine receptor (e.g., A2A and / or A1 receptor) antagonist compounds and compositions including the adenosine receptor antagonist compounds are disclosed. Methods of using the compounds and compositions for modulating (e.g., inhibiting or antagonizing) A2A and / or A1 receptor in a biological system are also disclosed. The compounds and compositions find use in various therapeutic applications including the treatment of cancer and in immuno-oncology. The compounds and compositions find use in various therapeutic applications including the treatment of central nervous system or neurodegenerative diseases, such as Parkinson's disease.

The invention provides a compound of formula (I), or pharmaceutically acceptable ester, amide, carbamate, solvate or salt thereof, including a salt of such an ester, amide or carbamate,wherein R1 is an optionally substituted phenyl, or an optionally substituted 5- or 6-membered aromatic heterocycle; and R2 is an optionally substituted 5- or 6-membered aromatic heterocycle. Also provided are pharmaceutical compositions comprising a compound of formula (I).

The present invention relates to a dual-acting ligand that acts on both A2A adenosine receptor and / or A3 adenosine receptor, and a composition including the ligand for the prevention, alleviation, or treatment of obesity, and a method for treating a disease associated with A2A adenosine receptor (AR) and / or A3 adenosine receptor (AR) by using the ligand and a use of the ligand in preparing a drug for the treatment of a disease associated with A2A adenosine receptor (AR) and / or A3 adenosine receptor (AR).