Research Materials & Patents
Patents, materials, and other research resources appear below. Some resources may be available for use through Material Transfer Agreements (MTAs) or licensing agreements.
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A3 Adenosine receptor allosteric modulators (U.S. Patent Number 20090054476 A1)
The present invention relates to allosteric modulation of A3 adenosine receptor (A3AR) and provides for the use of an A3 adenosine receptor modulator (A3RM), for the preparation of pharmaceutical compositions for modulating the A3AR in a subject, as… -
A3 Adenosine Receptor Antagonists & Partial Agonists (U.S. Patent Application Number 13/056,997)
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… -
A3 Adenosine Receptor Antagonists (U.S. Patent Number 6,376,521)
This invention relates to a method of decreasing intraocular pressure by administrating an A3 subtype adenosine receptor antagonist, a calmodulin antagonist or an antiestrogen such as tamoxifen -
A3 Adenosine Receptor Positive Allosteric Modulators
Selective A3AR agonists are sought as potential agents for treating inflammatory diseases, chronic pain, cancer and non-alcoholic steatohepatitis (NASH). NIDDK investigators have invented new chemical composition as positive allosteric modulators…E-067-2022-1
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Adenosine receptor agonists, partial agonists, & antagonists (U.S. Patent Number 13/479,973)
NIDDK announces the availability of a highly selective A1 adenosine receptor (AR) agonist. This receptor is neuroprotective in ischemic and epileptic models. The A1AR-selective full agonist MRS5474 displayed anticonvulsant activity in vivo in a model… -
Dendrimer Conjugates of Agonists & Antagonists of the GPCR Superfamily (U.S. Patent Number 8,153,781)
Disclosed are conjugates comprising a dendrimer and a ligand, which is a functionalized congener of an agonist or antagonist of a receptor of the G-protein coupled receptor (GPCR) superfamily, for example, wherein the functionalized congener is an A1… -
Dihydropyridine-, pyridine-, Benzopyran-4-one- & Triazoloquinazoline Derivative, Their Preparation, & Their Use as Adenosine Receptor Antagonists (U.S. Patent Number 6,066,642)
The present invention provides a method of identifying CFTR-binding compounds for treating cells having a reduced apical Cl.sup.- conductance, such as cystic fibrosis cells. This identification method involves the use of polypeptide I.alpha., which… -
Heterocyclic P2Y14 Antagonists for the Treatment of Various Conditions
The technology discloses composition of compounds that are highly selective P2Y14 receptor antagonists, with moderate affinity with insignificant antagonism of other P2Y receptors. These compounds might provide a treatment for patients for various…E-051-2021-0
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Methanocarba cycloalkyl Nucleoside Analogues (U.S. Patent Number 7,790,735)
The present invention provides novel nucleoside and nucleotide derivatives that are useful agonist or antagonists of P1 and P2 receptors. For example, the present invention provides a compound of formula A-M, wherein A is modified adenine or uracil… -
Method of Treating Cystic Fibrosis Using 8-Cyclopentyl-1,3-Dipropylxanthine or Xanthine Amino Congeners (U.S. Patent Number 6,083,954)
A method of treating cells having a reduced apical Cl.sup.- conductance, such as that characteristic of cystic fibrosis cells, by contacting cells having a reduced apical Cl.sup.- conductance with a therapeutically effective quantity of a compound… -
Methods for reducing Intraocular Pressure using A3 Adenosine Receptor Antagonists (U.S. Patent Number 6,528,516)
This invention relates to a method of decreasing intraocular pressure by administrating an A3 subtype adenosine receptor antagonist, a calmodulin antagonist or an antiestrogen such as tamoxifen -
(N)-Methanocarba Adenosine Derivatives & Their Dendrimer Conjugates as A3 Receptor Agonists (U.S. Patent Application Number 61/313,961)
Disclosed are (N)-methanocarba adenine nucleosides, e.g., of the formula (I): as A3 adenosine receptor agonists, pharmaceutical compositions comprising such nucleosides, and a method of use of these nucleosides, wherein A, a, R2, and R3 are as… -
Potent Nucleotide Inhibitors of Ecto-5'-Nucleotidase (CD73)
Novel, small molecule nucleotide derivatives have been developed containing either a purine or pyrimidine nucleobase that competitively block the enzyme CD73, or ecto-5'-nucleotidase. CD73 converts extracellular AMP to adenosine, the native activator…E-132-2018
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Purine Derivatives as A3 Receptor-selective Agonists (U.S. Patent Application Number 13/371,081)
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… -
Triazole Derivatives of 4,7-disubstituted 2 naphthoic acid (PPTN) as P2Y14 Receptor Antagonists
Disclosed are novel small molecules that serve as potent and selective antagonist ligands of the P2Y14 receptor for UDP-glucose, which is a G protein-coupled receptor (GPCR). Blocking this receptor has been shown to be useful in models of asthma…E-213-2015-0