Patent application number | Description | Published |
20090012035 | DENDRIMER CONJUGATES OF AGONISTS AND ANTAGONISTS OF THE GPCR SUPERFAMILY - 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 A | 01-08-2009 |
20090258836 | EFFECTIVE DELIVERY OF CROSS-SPECIES A3 ADENOSINE-RECEPTOR ANTAGONISTS TO REDUCE INTRAOCULAR PRESSURE - 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 A | 10-15-2009 |
20100137577 | 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 - 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. | 06-03-2010 |
20110046166 | PURINE DERIVATIVES AS A3 ADENOSINE RECEPTOR-SELECTIVE AGONISTS - Disclosed are (N)-methanocarba adenine nucleosides, e.g., of formula (I) as highly potent A | 02-24-2011 |
20110171130 | A3 ADENOSINE RECEPTOR ANTAGONISTS AND PARTIAL AGONISTS - Disclosed are A | 07-14-2011 |
20110212924 | COMPOSITIONS AND METHODS TO TREAT CARDIAC DISEASES - Phosphonate and phosphinate N-methanocarba derivatives of AMP including their prodrug analogs are described. MRS2339, a 2-chloro-AMP derivative containing a (N)-methanocarba (bicyclo[3.1.0]hexane) ring system in place of ribose, activates P2X receptors, ligand-gated ion channels. Phosphonate analogues of MRS2339 were synthesized using Michaelis-Arbuzov and Wittig reactions, based on the expectation of increased half-life in vivo due to the stability of the C—P bond. When administered to calsequestrin-overexpressing mice (a genetic model of heart failure) via a mini-osmotic pump (Alzet), some analogues significantly increased intact heart contractile function in vivo, as assessed by echocardiography-derived fractional shortening (FS) as compared to vehicle-infused mice. The range of carbocyclic nucleotide analogues for treatment of heart failure has been expanded. | 09-01-2011 |
20120184569 | A3 ADENOSINE RECEPTOR AGONISTS AND ANTAGONISTS - Disclosed are (N)-methanocarba adenine nucleosides of formulas (I)-(V), for example, of formula (V): | 07-19-2012 |
20120252823 | ADENOSINE RECEPTOR AGONISTS, PARTIAL AGONISTS, AND ANTAGONISTS - Disclosed are A | 10-04-2012 |
20120264769 | METHANOCARBA ADENOSINE DERIVATIVES AND DENDRIMER CONJUGATES THEREOF - Disclosed are (N)-methanocarba adenine nucleosides, e.g., of the formula (I): as A | 10-18-2012 |
20130190335 | FLUORESCENT ANTAGONISTS OF THE A3 ADENOSINE RECEPTOR - Disclosed are compounds of the formula (I) which are fluorescently labeled antagonists of the A | 07-25-2013 |
20150038463 | COMPOSITIONS AND METHODS TO TREAT CARDIAC DISEASES - Phosphonate and phosphinate N-methanocarba derivatives of AMP including their prodrug analogs are described. MRS2339, a 2-chloro-AMP derivative containing a (N)-methanocarba(bicyclo[3.1.0]hexane) ring system in place of ribose, activates P2X receptors, ligand-gated ion channels. Phosphonate analogues of MRS2339 were synthesized using Michaelis-Arbuzov and Wittig reactions, based on the expectation of increased half-life in vivo due to the stability of the C—P bond. When administered to calsequestrin-overexpressing mice (a genetic model of heart failure) via a mini-osmotic pump (Alzet), some analogues significantly increased intact heart contractile function in vivo, as assessed by echocardiography-derived fractional shortening (FS) as compared to vehicle-infused mice. The range of carbocyclic nucleotide analogues for treatment of heart failure has been expanded. | 02-05-2015 |