38 results about "Adenosine A2A Receptor Antagonists" patented technology

This invention provides a method of mitigating / ameliorating one or more components of addictive behavior associated with chronic consumption of a substance of abuse, or withdrawal therefrom. The method typically involves administering to a subject in need thereof an adenosine A2A receptor antagonist in an amount sufficient to ameliorate said one or more components of addictive behavior.

There is disclosed a method for the treatment or prevention of Extra Pyramidal syndrome (EPS), dystonia, restless legs syndrome (RLS) or periodic leg movement in sleep (PLMS) comprising the administration of an adenosine A2a receptor antagonist, alone or in combination with other agents useful for treating EPS, dystonia, RLS or PLMS; also claimed are pharmaceutical compositions consisting of an adenosine A2a receptor antagonist in combination with an antipsychotic agent, an anticonvulsant agent, lithium or an opioid.

Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is R1-isoxazolyl, R1-oxadiazolyl, R1-dihydrofuranyl, R1-pyrazolyl, R1-imidazolyl, R1-pyrazinyl or R1-pyrimidinyl; R1 is 1, 2 or 3 substituents selected from H, alkyl, alkoxy and halo; Z is optionally substituted-aryl, or optionally substituted-heteroaryl; are disclosed, as well as their use in the treatment of central nervous system diseases, in particular Parkinson's disease and Extra Pyramidal Syndrome, pharmaceutical compositions comprising them, and combinations with other agents.

There is disclosed a method for the treatment of Extra Pyramidal syndrome (EPS) comprising the administration of an adenosine A2a receptor antagonist, alone or in combination with other agents useful for treating EPS.

N-pyrazole substituted 2-adenosine compounds and methods for using the compounds as A2A-adenosine receptor agonists useful to stimulate mammalian coronary vasodilation for therapeutic purposes and as adjuncts in cardiological imaging.

The invention discloses a substituted pyrimidine compound, and a preparation method, an intermediate and application thereof. The invention provides a substituted pyrimidine compound as shown in a formula I or pharmaceutically acceptable salt thereof. The substituted pyrimidine compound disclosed by the invention can be used as an adenosine A2A receptor antagonist or a histone deacetylase HDAC inhibitor. Furthermore, the substituted pyrimidine compound provided by the invention can simultaneously have adenosine A2A receptor antagonistic activity and histone deacetylase HDAC inhibitory activity. The substituted pyrimidine compound provided by the invention can be used for treating and / or preventing diseases related to adenosine A2A receptor and / or histone deacetylase HDAC, such as tumors and central nervous system diseases.

There is disclosed a method for the treatment or prevention of Extra Pyramidal syndrome (EPS), dystonia, restless legs syndrome (RLS) or periodic leg movement in sleep (PLMS) comprising the administration of an adenosine A2a receptor antagonist, alone or in combination with other agents useful for treating EPS, dystonia, RLS or PLMS.

The invention discloses a 8-substituted aromatic ring vinyl xanthine derivative and application thereof, and particularly relates to a novel 8-substituted aromatic ring vinyl xanthine derivative and apharmaceutical composition containing the compound, which can be used as a selective adenosine A2A receptor antagonist. The invention also relates to a method for preparing the compound and the pharmaceutical composition, and application of the compound and the pharmaceutical composition in preparation of drugs for treating adenosine A2A receptor related diseases, especially Parkinson's disease.

Methods for treating sepsis or septic shock in a patient comprising administering to said patient a therapeutically effective amount of a composition containing an adenosine A2a receptor antagonist.

Compounds having the structural formula Ior a pharmaceutically acceptable salt thereof, whereinR is R1-isoxazolyl, R1-oxadiazolyl, R1-dihydrofuranyl, R1-pyrazolyl, R1-imidazolyl, R1-pyrazinyl or R1-pyrimidinyl;R1 is 1, 2 or 3 substituents selected from H, alkyl, alkoxy and halo;Z is optionally substituted-aryl, or optionally substituted-heteroaryl;are disclosed, as well as their use in the treatment of central nervous system diseases, in particular Parkinson's disease and Extra Pyramidal Syndrome, pharmaceutical compositions comprising them, and combinations with other agents.

The invention relates to antagonists of the adenosine A2A receptor, which can be used for the preparation of medicaments for auricular fibrillation in mammals, including humans. It has been found that the A2A adenosine receptor is present in human auricular cardiomyocytes and involved in the basic pathological mechanisms of auricular fibrillation. The use of A2A antagonists is advantageous over other known agents in that A2A antagonists are directed specifically to patients with auricular fibrillation.

The invention belongs to the technical field of medicines, particularly relates to A2A-targeting benzimidazopyrazine-3-formamide and a tumor immune function thereof, and discloses a subtype selective adenosine A2A receptor antagonist, namely a 1-amino-N-(pyridine-2-yl methyl) benzo [4, 5] imidazopyrazine-3-formamide small molecule compound, of which the structure is shown as a formula (I). Researches find that the small molecule compound can specifically target A2AR, inhibit cAMP accumulation, promote release of immune cell cytokines, enhance killing of immune cells on tumor cells in co-culture and enhance the tumor immunotherapy effect. The polypeptide shows an obvious tumor immunoenhancement effect in molecular level, cellular level and cancer mouse models, and is expected to be applied to tumor immunotherapy.

The disclosure provides, inter alia, compositions, oral formulations, amorphous solid dispersions, extrudates, crystalline nanoparticles, and microprecipitated bulk powders containing adenosine A2A receptor antagonists, and methods of using the compositions, oral formulations, amorphous solid dispersions, extrudates, crystalline nanoparticles, and microprecipitated bulk powder to treat cancer.

The invention discloses an 8-substituted styryl xanthine derivative and application thereof, and particularly relates to a novel 8-substituted styryl xanthine derivative and a pharmaceutical composition containing the 8-substituted styryl xanthine derivative. The 8-substituted styryl xanthine derivative can be used as a selective adenosine A2A receptor antagonist. The invention also relates to a method for preparing the 8-substituted styryl xanthine derivative and the pharmaceutical composition, and application of the 8-substituted styryl xanthine derivative and the pharmaceutical compositionin preparation of drugs for treating adenosine A2A receptor related diseases, especially Parkinson's disease.

The invention discloses a nitrogen-containing fused tricyclic derivative and application thereof, and particularly relates to a novel nitrogen-containing fused tricyclic derivative and a pharmaceutical composition containing the nitrogen-containing fused tricyclic derivative, and the nitrogen-containing fused tricyclic derivative can be used as a selective adenosine A2A receptor antagonist. The invention also relates to a method for preparing the compound and the pharmaceutical composition and application of the compound and the pharmaceutical composition in preparation of drugs for treating adenosine A2A receptor related diseases, especially Parkinson's disease.

The invention discloses a nitrogen-containing fused tricyclic derivative and application thereof, and particularly relates to a novel nitrogen-containing fused tricyclic derivative and a pharmaceutical composition containing the nitrogen-containing fused tricyclic derivative, and the nitrogen-containing fused tricyclic derivative can be used as a selective adenosine A2A receptor antagonist. The invention also relates to a method for preparing the compound and the pharmaceutical composition and application of the compound and the pharmaceutical composition in preparation of drugs for treating adenosine A2A receptor related diseases, especially Parkinson's disease.

The disclosure provides, inter alia, pharmaceutical compositions comprising micronized drug particles of adenosine A2A receptor antagonists, and methods of treating cancer using the pharmaceutical compositions.

The present invention provides methods of treating restless legs syndrome or related disorders, comprising administering an effective amount of at least one adenosine A2A receptor antagonist to a patient in need thereof. More preferably the adenosine A2A receptor antagonist is a xanthine derivative or a pharmaceutically acceptable salt thereof.

Provided herein are, inter alia, methods of treating a cancer tumor in a subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of an adenosine A2A receptor antagonist, wherein the subject comprises an elevated level of CD8+ tumor infiltrating lymphocytes relative to a control, the subject comprises an elevated level of T-effector gene signature relative to a control, the subject comprises an increased cancer tumor T cell receptor diversity or blood T cell receptor diversity relative to a control, the cancer tumor comprises an elevated level of PD-L1 relative to a control, and / or the cancer tumor or the blood of the subject comprises an elevated level of CD73 relative to a control. Further provided are, inter alia, methods for determining whether a subject is likely to, is, or has responded to anti-cancer therapy comprising an A2A receptor antagonist.

The invention discloses a 3H-[1, 2, 3] triazolo [4, 5-d] pyrimidine-5-amine derivative and application thereof and particularly relates to the novel 3H-[1, 2, 3] triazolo [4, 5-d] pyrimidine-5-amine derivative and a pharmaceutical composition containing the compound, and the derivative can be used as a selective adenosine A2A receptor antagonist. The invention also relates to a method for preparing the compound and the pharmaceutical composition and the application of the compound and the pharmaceutical composition in preparation of drugs for treating adenosine A2A receptor related diseases, especially Parkinson's disease.

This invention relates to a novel arylindenopyrimidine, A, and its therapeutic and prophylactic uses as an antagonist of Adenosine A2a receptors. Disorders treated ans / or prevented include Parkinson's Disease.

Provided herein are, inter alia, methods of treating a cancer tumor in a subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of an adenosine A2A receptor antagonist, wherein the subject comprises an elevated level of CD8+ tumor infiltrating lymphocytes relative to a control, the subject comprises an elevated level of T-effector gene signature relative to a control, the subject comprises an increased cancer tumor T cell receptor diversity or blood T cell receptor diversity relative to a control, the cancer tumor comprises an elevated level of PD-L1 relative to a control, and / or the cancer tumor or the blood of the subject comprises an elevated level of CD73 relative to a control. Further provided are, inter alia, methods for determining whether a subject is likely to, is, or has responded to anti-cancer therapy comprising an A2A receptor antagonist.

The disclosure provides, inter alia, pharmaceutical compositions comprising micronized drug particles of adenosine A2A receptor antagonists, and methods of treating cancer using the pharmaceutical compositions.

The invention relates to a new application of an adenosine A2A receptor antagonist drug, and particularly relates to an application of the adenosine A2A receptor antagonist drug in promotion of brain-computer interface learning. Experiments prove that the adenosine A2A receptor antagonist drug can promote brain-computer interface learning and increase the success rate of brain-computer interface behavioral model construction.

This invention relates to novel arylindenopyrimidines A, B, and C, and their therapeutic and prophylactic uses. Disorders treated and / or prevented using these compounds include Parkinson's Disease.Formula (I).

There is disclosed a method for the treatment or prevention of Extra Pyramidal syndrome (EPS), dystonia, restless legs syndrome (RLS) or periodic leg movement in sleep (PLMS) comprising the administration of an adenosine A2a receptor antagonist, alone or in combination with other agents useful for treating EPS, dystonia, RLS or PLMS; also claimed are pharmaceutical compositions consisting of an adenosine A2a receptor antagonist in combination with an antipsychotic agent, an anticonvulsant agent, lithium or an opioid.