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38 results about "Adenosine A2A Receptor Antagonists" patented technology

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SYN115 (Tozadenant) is a orally-available, benzothiazole-based, antagonist of the Adenosine A2A receptor for the treatment of Parkinson's disease and other CNS-related conditions.

Antagonizing an adenosine A2A receptor to ameliorate one or more components of addictive behavior

InactiveUS20060128708A1Many componentReduce the impactBiocideNervous disorderAddictive behaviorAdenosine A2A Receptor Antagonists

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.

Antagonizing an adenosine A2A receptor to ameliorate one or more components of addictive behavior

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Owner:RGT UNIV OF CALIFORNIA

Adenosine a2a receptor antagonists for the treatment of extra-pyramidal syndrome and other movement disorders

InactiveUS20090029967A1BiocideNervous disorderPyramidal syndromeAdenosine A2A Receptor Antagonists

There is disclosed a method for the treatment or prevention of Extra Pyramidal syndrome (EPS), dystonia, restless leg 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.

Adenosine a2a receptor antagonists for the treatment of extra-pyramidal syndrome and other movement disorders

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Owner:SCHERING CORP

Adenosine A2a receptor antagonists for the treatment of extra-pyramidal syndrome and other movement disorders

InactiveUS20060128694A1BiocideNervous disorderPyramidal syndromeAnticonvulsant Agent

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.

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Owner:SCHERING CORP

2-Heteroaryl-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A2a receptor antagonists

ActiveUS20070066620A1Organic active ingredientsBiocideArylPyramidal syndrome

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.

2-Heteroaryl-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A2a receptor antagonists

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Owner:MERCK SHARP & DOHME LLC

Adenosine A2a receptor antagonists for the treatment of extra-pyramidal syndrome and other movement disorders

InactiveUS7414058B2BiocideNervous disorderPyramidal syndromeAdenosine A2A Receptor Antagonists

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.

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Owner:MERCK SHARP & DOHME CORP

2-(N-pyrazolo)adenosines with application as adenosine A_2Areceptor agonists

InactiveUSRE47351E1Facilitate coronary imagingEasy to useSugar derivativesAgonistArterial Vasodilation

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.

2-(N-pyrazolo)adenosines with application as adenosine A<sub>2A </sub>receptor agonists

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Owner:GILEAD SCI INC

Substituted pyrimidine compound, and preparation method, intermediate and application thereof

ActiveCN113387938AOrganic active ingredientsNervous disorderDiseaseDepressant

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.

Substituted pyrimidine compound, and preparation method, intermediate and application thereof

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Owner:SHANGHAI TECH UNIV

Adenosine A2a receptor antagonists for the treatment of extra-pyramidal syndrome and other movement disorders

InactiveUS20060106040A1BiocideNervous disorderPyramidal syndromeAdenosine A2A Receptor Antagonists

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Owner:SCHERING CORP

8-substituted aromatic ring vinyl xanthine derivative and application thereof

ActiveCN111333648ANervous disorderOrganic chemistryAdenosine a2a receptorsXanthine

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.

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Owner:DONGGUAN HEC NEW DRUG R&D CO LTD +1

Sepsis Prevention Through Adenosine Receptor Modulation

InactiveUS20090041751A1Avoid dysfunctionReduce mortalityBiocidePeptide/protein ingredientsAdenosine aAdenosine A2A Receptor Antagonists

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.

Sepsis Prevention Through Adenosine Receptor Modulation

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Owner:UNIV OF MEDICINE & DENTISTRY OF NEW JERSEY

8-substituted styryl xanthine derivative and application thereof

ActiveCN110981876AStable in natureImprove securityNervous disorderOrganic chemistryAdenosine a2a receptorsXanthine

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 compound, and 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 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.

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Owner:SUNSHINE LAKE PHARM CO LTD

2-heteroaryl-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A2a receptor antagonists

ActiveUS7465740B2Organic active ingredientsBiocideArylMedicine

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.

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Owner:MERCK SHARP & DOHME LLC

Compounds for the treatment of auricular fibrillation

InactiveCN101325956ACardiovascular disorderHeterocyclic compound active ingredientsCardiac muscleAuricular fibrillation

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.

Compounds for the treatment of auricular fibrillation

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Owner:PROYECTO DE BIOMEDICINA CIMA

Benzimidazopyrazine-3-carboxamide targeting A2A and tumor immune function thereof

ActiveCN114539265AAvoid accumulationFacilitated releaseOrganic active ingredientsOrganic chemistryPyrazineAdenosine

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.

Benzimidazopyrazine-3-carboxamide targeting A2A and tumor immune function thereof

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Owner:SUN YAT SEN UNIV +1

Pharmaceutical formulations

InactiveUS20190231783A1Organic active ingredientsPowder deliveryNanoparticleMedicine

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.

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Owner:CORVUS PHARMACEUTICALS INC

8-substituted styryl xanthine derivative and application thereof

ActiveCN111018856AStable in natureImprove securityNervous disorderOrganic chemistryAdenosine a2a receptorsXanthine

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.

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Owner:SUNSHINE LAKE PHARM CO LTD

Nitrogen-containing fused tricyclic derivatives and application thereof

ActiveCN111072676AStable in natureImprove securityOrganic active ingredientsNervous disorderAdenosine a2a receptorsPharmaceutical drug

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.

Nitrogen-containing fused tricyclic derivatives and application thereof

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Owner:SUNSHINE LAKE PHARM CO LTD

Nitrogen-containing fused tricyclic derivative and application thereof

InactiveCN111072675AStable in natureImprove securityOrganic active ingredientsNervous disorderAdenosine a2a receptorsPharmaceutical drug

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Owner:SUNSHINE LAKE PHARM CO LTD

Pharmaceutical formulations

ActiveUS11266649B2Maintain good propertiesImprove bioavailabilityPowder deliveryOrganic active ingredientsMedicineAdenosine

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.

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Owner:CORVUS PHARMACEUTICALS INC

Adenosine A2A receptor antagonists for treating restless legs syndrome or nocturnal myoclonus

InactiveUS7759355B2BiocideNervous disorderXanthineAdenosine a

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.

Adenosine A2A receptor antagonists for treating restless legs syndrome or nocturnal myoclonus

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Owner:KYOWA HAKKO KIRIN CO LTD

Methods of treating cancer

ActiveUS11040040B2Enhance anti-tumor immune responseIncreasing the amount of CD8-positive cellsOrganic active ingredientsImmunoglobulins against cell receptors/antigens/surface-determinantsAdenosineOncology

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.

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Owner:CORVUS PHARMACEUTICALS INC

3H-[1, 2, 3] triazolo [4, 5-d] pyrimidine-5-amine derivative and application thereof

ActiveCN110922408AStable in natureImprove securityOrganic active ingredientsNervous disorderPharmaceutical drugCombinatorial chemistry

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.

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Owner:SUNSHINE LAKE PHARM CO LTD

Arylindenopyrimidines and their use as adenosine A2a receptor antagonists

InactiveCN101835759AOrganic active ingredientsNervous disorderDiseaseMedicine

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.

Arylindenopyrimidines and their use as adenosine A2a receptor antagonists

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Owner:JANSSEN PHARMA NV

Methods of treating cancer

ActiveUS20200297728A1Enhance anti-tumor immune responseEnhancing anti-tumor immune memoryOrganic active ingredientsImmunoglobulins against cell receptors/antigens/surface-determinantsAdenosineOncology

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Owner:CORVUS PHARMACEUTICALS INC

Adenosine a2a receptor antagonists for the treatment of extra-pyramidal syndrome and other movement disorders

InactiveCN101312731ANervous disorderMuscular disorderPyramidal syndromeAdenosine A2A Receptor Antagonists

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Owner:SCHERING AG

Pharmaceutical formulations

ActiveUS20210060020A1Maintain good propertiesImprove bioavailabilityPowder deliveryOrganic active ingredientsAdenosineAdenosine A2A Receptor Antagonists

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Owner:CORVUS PHARMACEUTICALS INC

New application of adenosine A2A receptor antagonist drug

PendingCN111407763AIncrease success rateShorten completion timeNervous disorderHeterocyclic compound active ingredientsAdenosineAdenosine A2A Receptor Antagonists

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.