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41 results about "A3 ADENOSINE RECEPTOR" patented technology
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The adenosine A3 receptor is a member of the adenosine receptor group of G-protein-coupled receptors that also includes A1, A2A and A2B. They display high expression levels in the testes and mast cells of rats, with low expression levels in the thyroid, liver, kidney and heart.
Compounds specific to adenosine A1 and A3 receptors and uses thereof
This invention pertains to compounds having the structure:whereinm is 0, 1, 2, or 3;R2 is a substituted or unsubstituted imidazole or pyrazole wherein the point of attachment of R2 to the alkyl chain is not N;R5 is a hydrogen atom or a substituted or unsubstituted alkyl, aryl, or alkylaryl moiety; andR7 is a halogen atom, C1-C4 alkyl, OH, O-alkyl(C1-C4), NH2, or NH-alkyl(C1-C4),which specifically inhibit the adenosine A1 and A3 receptors and the use of these compounds to treat a disease associated with A3 adenosine receptor in a subject, comprising administering to the subject a therapeutically effective amount of the compound.
Owner:OSI PHARMA INC
Pharmaceutical compositions comprising an adenosine receptor agonist or antagonist
InactiveUS7064112B1Prevent proliferationInhibit proliferation and growth of tumor cellBiocideSugar derivativesSide effectLeukopenia
Adenosine receptor agonists, particularly an agonist which binds to the A3 adenosine receptor, are used for induction of production or secretion of G-CSF within the body, prevention or treatment of toxic side effects of a drug or prevention or treatment of leukopenia, particularly drug-induced leukopenias; and inhibition of abnormal cell growth and proliferation.
Owner:CAN-FITE BIOPHARMA LTD
Purine derivatives as a3 adenosine receptor-selective agonists
Disclosed are (N)-methanocarba adenine nucleosides, e.g., of formula (I) as highly potent A3 adenosine receptor agonists, pharmaceutical compositions comprising such nucleosides, and a method of use of these nucleosides, wherein R1-R6 are as defined in the specification. These nucleosides exhibit similar selectivities as agonists of the A3 versus the A1 receptor for both human and mouse adenosine receptors, and are contemplated for use in the treatment a number of diseases, for example, inflammation, cardiac ischemia, stroke, asthma, diabetes, and cardiac arrhythmias.
Owner:UNITED STATES OF AMERICA
A3 adenosine receptor antagonists and partial agonists
InactiveUS20110171130A1High potencyHighly selectiveBiocideSenses disorderHypersensitive responseArthritis
Disclosed are A3 adenosine receptor antagonists and / or partial agonists of formula (I): wherein R1 to R5 are as described herein, as well as pharmaceutical compositions thereof and methods of use thereof. The antagonists or partial agonists find use in treating a number of diseases including cancer, glaucoma, inflammatory diseases, asthma, stroke, myocardial infarction, allergic reactions, rhinitis, poison ivy induced responses, urticaria, scleroderma, arthritis, brain arteriole diameter constriction, bronchoconstriction, and myocardial ischemia, as well as in preventing cardiac ischemia. Also disclosed are radiolabeled compounds of formula (I) and the use thereof in diagnostic imaging of tissues and organs.
Owner:UNITED STATES OF AMERICA
Therapeutic Treatment of Accelerated Bone Resorption
InactiveUS20080051364A1Avoid actionReduce deliveryBiocideAntipyreticTherapeutic treatmentInflammation
The present invention concerns the use of an A3 adenosine receptor agonist (A3AR agonist) for treatment of accelerated bone resorption, particularly, inflammation induced bone resorption. Specifically, there is provided by the present invention a method and pharmaceutical composition for treatment of said condition, the A3AR agonist being formulated as a pharmaceutical composition which is administered to a subject having accelerated bone resorption.The invention also provides the use of A3AR agonist in the preparation of said pharmaceutical composition.
Owner:CAN-FITE BIOPHARMA LTD
Use of A3 Adenosine Receptor Agonist in Osteoarthritis Treatment
The present invention provides the use of an A3 adenosine receptor agonist (A3AR agonist) for the preparation of a pharmaceutical composition for the treatment of a mammal subject having osteoarthritis (OA), as well as to a method for the treatment of OA in a mammal subject, the method comprises administering to said subject in need of said treatment an amount of an A3AR agonist, the amount being effective to treat or prevent the development of OA. Preferred but not exclusive A3AR agonists in accordance with the invention are IB-MECA and Cl—IB-MECA. The A3AR agonist may be administered in combination with another drug, such as, Methotrexate (MTX). The invention also provides pharmaceutical compositions for treatment of osteoarthritis comprising an amount of an A3AR agonist.
Owner:CAN-FITE BIOPHARMA LTD
A3 adenosine receptor agonists and antagonists
Disclosed are (N)-methanocarba adenine nucleosides of formulas (I)-(V), for example, of formula (V):as highly potent A3 adenosine receptor agonists, pharmaceutical compositions comprising such nucleosides, and a method of use of these nucleosides, wherein R1-R6 are as defined in the specification. These nucleosides exhibit similar selectivities as agonists of the A3 versus the A1 receptor for both human and mouse adenosine receptors, and are contemplated for use in the treatment a number of diseases, for example, inflammation, cardiac ischemia, stroke, asthma, diabetes, and cardiac arrhythmias.
Owner:US DEPT OF HEALTH & HUMAN SERVICES
Effective delivery of cross-species a3 adenosine-receptor antagonists to reduce intraocular pressure
InactiveUS20090258836A1Good curative effectImprove actionBiocideSenses disorderPyridiniumNK1 receptor antagonist
Provided are methods for reducing intraocular pressure in an individual having an ocular disorder causing elevated intraocular pressure, such as glaucoma. The method comprises administering to the individual an effective intraocular pressure-reducing amount of a pharmaceutical composition comprising an A3 subtype adenosine receptor (A3AR) antagonist, including dihydropyridine, pyridine, pyridinium salt or triazoloquinazoline, and derivatives thereof expressly having A3AR antagonist activity, including, e.g., the nucleoside-based A3AR antagonist, MRS-3820. Further provided is a method for ensuring the delivery of a topically administered therapeutic composition for reducing intraocular pressure, wherein the method expressly requires physically opening a channel through the corneal barrier of the patient's eye by a microneedle or micropipette to permit transport of the topical composition to the anterior chamber of the eye.
Owner:HEALTH & HUMAN SERVICES GOVERNMENT OF THE US SEC DEPT OF THE +1
Adenosine derivatives, method for the synthesis thereof, and the pharmaceutical compositions for the prevention and treatment of the inflammatory diseases containing the same as an active ingredient
ActiveUS20100137577A1High affinityHigh selectivitySugar derivativesAntipyreticMedicineBULK ACTIVE INGREDIENT
Disclosed are adenosine derivatives, methods for the synthesis thereof, and pharmaceutical compositions for the prevention and treatment of inflammatory diseases, comprising the same as an active ingredient. The adenosine derivatives have high binding affinity and selectivity for adenosine receptors, especially for A3 adenosine receptors and act as A3 adenosine receptor antagonists, and exhibit anti-inflammatory activity. Thus, the adenosine derivatives are useful in the prevention and treatment of inflammatory diseases.
Owner:GOVERNMENT OF THE US REPRESENTED BY THE SEC +1
Adenosine receptor agonists, partial agonists, and antagonists
Disclosed are A3 adenosine receptor antagonists and / or partial agonists and A1 adenosine receptor agonists and / or partial agonists of formula (I):wherein R1 to R5 are as described herein, as well as pharmaceutical compositions thereof and methods of use thereof. The A3 AR antagonists or partial agonists find use in treating a number of diseases such as cancer, glaucoma, and inflammatory diseases, as well as in preventing cardiac ischemia. Also disclosed are radiolabeled compounds of formula (I) and the use thereof in diagnostic imaging of tissues and organs. The A1 AR agonists and partial agonists find use in treating diseases such as seizures, convulsion, stroke, diabetes, pain, arrhythmias, depression, and anxiety and in cardioprotection or neuroprotection.
Owner:US DEPT OF HEALTH & HUMAN SERVICES
Treatment for dry eye conditions
The present invention provides a method for treating dry eye condition in an individual comprising administrating to said individual an amount of A3 adenosine receptor (A3AR) agonist, the amount being effective to ameliorate symptoms of dry eye in the individual. In accordance with one embodiment, the dry eye condition is manifested by one or more opthalmologic clinical symptoms selected from foreign body sensation, burning, itching, irritation, redness, eye pain, blurred vision, degraded vision and excessive tearing. A preferred A3RAg in accordance with the invention is N6-(3-iodobenzyl)-adenosine-5′-N-methyluronamide (IB-MECA).
Owner:CAN-FITE BIOPHARMA LTD
A3 adenosine receptors as targets for the modulation of central serotonergic signaling
InactiveUS20090088403A1Reducing SERT activityEnhance SERT activityBiocideCarbohydrate active ingredientsSerotonin transporterIn vivo
The present invention relates to the use of adenosine type 3 receptor (A3R) modulators to modulate serotonin transporter (SERT) function in vivo. In particular, antagonists of A3R can be used to inhibit A3R-dependent upregulation of SERT, for example, as antidepressants.
Owner:VANDERBILT UNIV
A3 adenosine receptor agonists and antagonists
Disclosed are (N)-methanocarba adenine nucleosides of formulas (I)-(V), for example, of formula (V):as highly potent A3 adenosine receptor agonists, pharmaceutical compositions comprising such nucleosides, and a method of use of these nucleosides, wherein R1-R6 are as defined in the specification. These nucleosides exhibit similar selectivities as agonists of the A3 versus the A1 receptor for both human and mouse adenosine receptors, and are contemplated for use in the treatment a number of diseases, for example, inflammation, cardiac ischemia, stroke, asthma, diabetes, and cardiac arrhythmias.
Owner:UNITED STATES OF AMERICA
Purine derivatives as A3 adenosine receptor-selective agonists
Disclosed are (N)-methanocarba adenine nucleosides, e.g., of formula (I) as highly potent A3 adenosine receptor agonists, pharmaceutical compositions comprising such nucleosides, and a method of use of these nucleosides, wherein R1-R6 are as defined in the specification. These nucleosides exhibit similar selectivities as agonists of the A3 versus the A1 receptor for both human and mouse adenosine receptors, and are contemplated for use in the treatment a number of diseases, for example, inflammation, cardiac ischemia, stroke, asthma, diabetes, and cardiac arrhythmias.
Owner:UNITED STATES OF AMERICA
Pharmaceutical compositions comprising an adenosine receptor agonist or antagonist
InactiveUS20060084626A1Prevent proliferationCounter toxic sideBiocideAntinoxious agentsSide effectLeukopenia
Adenosine receptor agonists, particularly an agonist which binds to the A3 adenosine receptor, are used for induction of production or secretion of G-CSF within the body, prevention or treatment of toxic side effects of a drug or prevention or treatment of leukopenia, particularly drug-induced leukopenias; and inhibition of abnormal cell growth and proliferation.
Owner:CAN-FITE BIOPHARMA LTD
A3 adenosine receptor agonists
ActiveUS20170002007A1Treating and preventing neuropathic painConfer oral bioavailabilityAntipyreticAnalgesicsDiseaseNeuropathic pain
Disclosed are compounds of the formula (I) and (II) which are A3 adenosine receptor agonists, pharmaceutical compositions comprising such compounds, and a method of use of these compounds, wherein X, Y, Z, R2-R6, and R103-R106 are as defined in the specification. These compounds are selective to the A3 receptor, and are contemplated for use in the treatment or prevention of a number of diseases or conditions, for example, neuropathic pain.
Owner:US DEPT OF HEALTH & HUMAN SERVICES +1
A3 adenosine receptor agonists
ActiveUS9963450B2Favorable for crossing blood-brain barrierOral bioavailabilityAntipyreticAnalgesicsDiseaseNeuropathic pain
Disclosed are compounds of the formula (I) and (II) which are A3 adenosine receptor agonists, pharmaceutical compositions comprising such compounds, and a method of use of these compounds, wherein X, Y, Z, R2-R6, and R103-R106 are as defined in the specification. These compounds are selective to the A3 receptor, and are contemplated for use in the treatment or prevention of a number of diseases or conditions, for example, neuropathic pain.
Owner:UNITED STATES OF AMERICA +1
Compounds antagonizing A3 adenosine receptor, method for preparing them, and medical-use thereof
ActiveUS10196396B2Preventing and ameliorating and treating glaucomaBiocideSenses disorderDiseaseGlaucoma
The present disclosure provides compounds useful in the amelioration, prevention or treatment of A3 adenosine receptor mediated diseases, such as glaucoma and glaucoma-related ocular disorders, having the structure of Formula I as defined in the detailed description; pharmaceutical compositions comprising at least one of the compounds; and methods for ameliorating, preventing or treating A3 adenosine receptor mediated diseases using the compound.
Owner:HANDOK INC
Small-molecular antagonist for A3 adenosine receptor
ActiveCN108017584AOrganic active ingredientsSenses disorderAdenosine A1 receptorAdenosine A2A receptor
The invention discloses a small-molecular antagonist for an A3 adenosine receptor, and an application thereof in medicine synthesis, and concretely relates to a use of the small-molecular antagonist for the A3 adenosine receptor and pharmacologically available salts of the small-molecular antagonist for the A3 adenosine receptor as medicines for treating or preventing A3 adenosine receptor-mediated related diseases or symptoms.
Owner:NANKAI UNIV
Pharmaceutical composition including an A3 adenosine receptor agonist 1-deooxy-1-[N6-(3-idobenzyl)-adenin-9-yl]-N-methyl-β-D-ribofuronamide(IB-MECA/CF-101) for treatment of psoriasis
Clinical finding shows that twice daily administrations of 2 mg of 1-deoxy-1-[N6-(3-iodobenzyl)-adenin-9-yl]-N-methyl-β-D-ribofuronamide (IB-MECA) (total daily administration of 4 mg) to subjects having moderate to severe psoriasis, was significantly more effective in treatment of the psoriatic plaques than treatment of psoriasis at two administration doses of 1 mg or 4 mg (total daily doses of 2 or 8 mg, respectively). A pharmaceutical composition for the treatment of psoriasis includes as the active ingredient IB-MECA in an amount suitable for a total daily dose administration of about 4 mg. In one preferred embodiment, IB-MECA is administered twice a day to a subject in need of psoriasis treatment, the pharmaceutical composition including an administration dose of 2 mg.
![Pharmaceutical composition including an A3 adenosine receptor agonist 1-deooxy-1-[N<sup>6</sup>-(3-idobenzyl)-adenin-9-yl]-N-methyl-β-D-ribofuronamide(IB-MECA/CF-101) for treatment of psoriasis](https://images-eureka-patsnap-com.libproxy1.nus.edu.sg/patent_img/5fb339b5-408b-49ef-8e0f-f037f80e93c6/US08987228-20150324-D00001.PNG "Pharmaceutical composition including an A3 adenosine receptor agonist 1-deooxy-1-[N<sup>6</sup>-(3-idobenzyl)-adenin-9-yl]-N-methyl-β-D-ribofuronamide(IB-MECA/CF-101) for treatment of psoriasis")
Owner:CAN-FITE BIOPHARMA LTD
Adenosine A3 receptor agonists
Disclosed are novel compounds that are A3 adenosine receptor agonists, useful for treating various disease states, including cancer, cardiac ischemia, leukopenia, and neutropennia.
Owner:GILEAD PALO ALTO
Adenosine receptor
InactiveUS20070112177A1Cell receptors/surface-antigens/surface-determinantsDepsipeptidesAntigen Binding FragmentAntigen binding
The present invention provides an isolated mammalian adenosine receptor, isolated or recombinant nucleic acids and recombinant vectors encoding the same, host cells comprising the nucleic acids and vectors, and methods of making the receptor using the host cells. This invention further provides antibodies and antigen binding fragments thereof which specifically bind to the receptor and are useful for treating medical conditions caused or mediated by adenosine. Also provided are screening methods for identifying specific agonists and antagonists of the mammalian adenosine receptor.
Owner:SCHERING CORP
Adenosine a3 receptor agonists for the treatment of dry eye disorders
The present invention concerns methods and compositions for treating dry eye. The method comprises providing an individual exhibiting ophthalmologic clinical symptoms and signs of dry eye with an A3 adenosine receptor (A3AR) agonist. The A3AR agonist is preferably administered to the subject either topically or orally.
Owner:CAN-FITE BIOPHARMA LTD
Treatment for inflammation
Inflammatory state in a subject is assayed by determining the level of expression of A3 adenosine receptor (A3AR) in white blood cells (WBC), e.g. circulating WBCs, from the subject. A high level of expression of A3AR is indicative of an inflammatory state in the subject. This assay can be used for determining the severity of inflammation in a subject and monitoring the efficacy of anti-inflammatory treatment. Also, the level of expression may be used for selecting patients to receive an anti-inflammatory treatment that comprises an A3AR agonist.
Owner:CAN-FITE BIOPHARMA LTD
Pharmaceutical composition containing a3 adenosine receptor agonist
InactiveUS20120322815A1Good anti-inflammatory effectEnhanced inhibitory effectBiocideNervous disorderProstate cancer cellThio-
The present invention relates to a pharmaceutical composition for preventing or treating inflammatory disease, colorectal cancer and prostate cancer, which contains an A3 adenosine receptor agonist, 2-chloro-N6-(3-iodobenzyl)-4′-thioadenosine-5′-N-methyluronamide (thio-Cl-IB-MECA), N6-(3-iodobenzyl)-4′-thioadenosine-5′-N-methyluronamide (thio-IB-MECA), or a pharmaceutically acceptable salt thereof. The pharmaceutical composition of the invention is significantly less toxic than conventional A3 adenosine agonists, and thus is useful for prevention or treatment of inflammatory disease. In addition, it more selectively inhibits the growth of androgen receptor-dependent or independent prostate cancer cells than other A3 adenosine receptor agonists and thus is useful for prevention or treatment of colorectal cancer or prostate cancer.
Owner:EWHA UNIV IND COLLABORATION FOUND
Use of a3 adenosine receptor agonist in osteoarthritis treatment
ActiveUS20160263142A1Avoid developmentOrganic active ingredientsAntipyreticSubject matterOsteoarthritis
Provided is an A3 adenosine receptor agonist (A3AR agonist) for the preparation of a pharmaceutical composition for the treatment of a mammal subject having osteoarthritis (OA), as well as to a method for the treatment of OA in a mammal subject, the method includes administering to said subject in need of said treatment an amount of A3AR agonist, the amount being effective to treat or prevent the development of OA. Preferred but not exclusive A3AR agonists in accordance with the present subject matter are IB-MECA and Cl-IB-MECA. The A3AR agonist may be administered in combination with another drug, such as Methotrexate (MTX). Also provided are pharmaceutical compositions for treatment of osteoarthritis including an amount of an A3AR agonist.
Owner:CAN-FITE BIOPHARMA LTD
A3 adenosine receptor ligands for modulation of pigmentation
ActiveUS9199102B2Treating and ameliorating skin hypo-pigmentationBiocideCosmetic preparationsPigmentationsSecretion
The present invention relates to compositions and methods for modulating melanin production, secretion and / or accumulation in human skin cells. In particular, the present invention relates to the use of A3 adenosine receptor antagonists in compositions and methods for the treatment and amelioration of hyper-pigmentation conditions and for the lightening of skin, and to the use of A3 adenosine receptor agonists in compositions and methods for the treatment and amelioration of hypo-pigmentation conditions and for the tanning of skin.
Owner:ORADIN PHARMA
Adenosine receptor
InactiveUS7465789B2Cell receptors/surface-antigens/surface-determinantsDepsipeptidesAntigen Binding FragmentAntigen binding
The present invention provides an isolated mammalian adenosine receptor, isolated or recombinant nucleic acids and recombinant vectors encoding the same, host cells comprising the nucleic acids and vectors, and methods of making the receptor using the host cells. This invention further provides antibodies and antigen binding fragments thereof which specifically bind to the receptor and are useful for treating medical conditions caused or mediated by adenosine. Also provided are screening methods for identifying specific agonists and antagonists of the mammalian adenosine receptor.
Owner:SCHERING CORP
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