Abstract: Novel mutant A1 adenosine receptor cDNA sequences and plasmids. Novel mutant A1 adenosine receptor cDNA sequences and plasmids which can improve immune cells ability to kill cancer cells.

Abstract: The present invention relates to methods for treating and preventing renal impairment by administering to a subject a therapeutically effective amount of an A1 adenosine receptor antagonist alone or in combination with at least one additional therapeutic agent. The invention further encompasses pharmaceutical compositions comprising an A1 adenosine receptor antagonist alone or with, at least, one additional therapeutic agent in a pharmaceutically acceptable carrier. The pharmaceutical compositions of the invention find use in methods for treating and preventing renal impairment.

Abstract: The present invention relates to methods for treating and preventing renal impairment by administering to a subject a therapeutically effective amount of an A1 adenosine receptor antagonist alone or in combination with at least one additional therapeutic agent. The invention further encompasses pharmaceutical compositions comprising an A1 adenosine receptor antagonist alone or with, at least, one additional therapeutic agent in a pharmaceutically acceptable carrier. The pharmaceutical compositions of the invention find use in methods for treating and preventing renal impairment.

Abstract: This invention relates to compounds of formula (I): wherein R1 is a branched or straight chain C1-C6 alkyl; R2 is of the formula (II), wherein n is an integer ranging from 1 to 8; R5 is H or (CH2)pCH3, and R6 is H or (CH2)mOH, wherein p is an integer ranging from 1 to 7 and m is an integer ranging from 1 to 8; R3 is of the formula (III), wherein q is an integer ranging from 1 to 8; and R7 is selected from the group consisting of H, OH, NH2, (CH2)tOH, and R9COOH; wherein R9 is a straight or branched chain alkylene or alkenylene group having 1 to 8 carbon atoms, and t is an integer ranging from 1 to 8; R4 is of the formula (IV), wherein r is an integer ranging from 1 to 8 and R8 is selected from the group consisting of H, OH, (CH2)fNH2, (CH2)sOH, and R10COOH; wherein f is 0 or f and s are independently integers ranging from 1 to 8; and, R10 is a C1-C8 straight or branched chain alkylene or alkenylene; and; salts, solvates, and hydrates thereof.

Abstract: Methods for treating and preventing tissue injury and sepsis associated with a Yersinia pestis infection, particularly pneumonic plague, are provided. The methods of the invention comprise administering to a subject a therapeutically effective amount of an A1 adenosine receptor antagonist alone or in combination with at least one additional therapeutic agent, including an antibiotic agent. The present methods find use in biodefense as a means of preventing and treating tissue injury and sepsis associated with Y. pestis infection, particularly pneumonic plague, in the event of a bioterrorist attack with this deadly bacterium.

Abstract: Compounds of the general formula (I) are described: wherein A is a 5- or 6-membered aromatic or heteroaromatic ring. Compositions comprising such compounds and methods of use thereof are also described.

Abstract: Compounds of the general formula (I) are described: wherein A is a 5- or 6-membered aromatic or heteroaromatic ring. Compositions comprising such compounds and methods of use thereof are also described.

Abstract: wherein R3 is Alk14ArR16, and wherein Alk14 is C1-8 straight or branched alkylene or alkenylene. The present invention provides novel adenosine receptor antagonists, more particularly, A1 adenosine receptor antagonists of formula (I). Pharmaceutical compositions comprising an A1 adenosine receptor antagonist of formula (I) and a pharmaceutically acceptable carrier are further provided. Compositions also include diagnostic assay-type probes comprising a novel A1 adenosine receptor antagonist of formula (I) that is labeled or conjugated with radioactive or non-radioactive material. Methods for treating A1 adenosine receptor related disorders comprising administering an A1 adenosine receptor antagonist of formula (I) are also disclosed. The novel A1 adenosine receptor antagonist compositions of formula (I) find further use in diagnostic and imaging methods.

Abstract: This invention relates to compounds of formula (I): wherein R1 is a branched or straight chain C1-C6 alkyl; R2 is of the formula (II), wherein n is an integer ranging from 1 to 8; R5 is H or (CH2)pCH3, and R6 is H or (CH2)mOH, wherein p is an integer ranging from 1 to 7 and m is an integer ranging from 1 to 8; R3 is of the formula (III), wherein q is an integer ranging from 1 to 8; and R7 is selected from the group consisting of H, OH, NH2, (CH2)tOH, and R9COOH; wherein R9 is a straight or branched chain alkylene or alkenylene group having 1 to 8 carbon atoms, and t is an integer ranging from 1 to 8; R4 is of the formula (IV), wherein r is an integer ranging from 1 to 8 and R8 is selected from the group consisting of H, OH, (CH2)fNH2, (CH2)sOH, and R10COOH; wherein f is 0 or f and s are independently integers ranging from 1 to 8; and, R10 is a C1-C8 straight or branched chain alkylene or alkenylene; and; salts, solvates, and hydrates thereof.

Abstract: Subjects at risk for developing cancer may be identified by obtaining samples of diagnostic cells from the subjects and determining a measure of cytotoxicity of the cells, the measure of cytotoxicity correlating negatively with the risk of developing cancer. The development of cancer may be prevented in subjects determined to be at risk for developing cancer by administering priming and activating agents to the subject, by increasing the expression of A1 adenosine receptors in cells of the subject, and increasing the affinity of cells of the subject for A1 adenosine receptor ligands. The preventative and diagnostic methods of the present invention may be carried out with kits and pharmaceutical liposomal formulations.

Abstract: Methods and compositions for treating and preventing respiratory disorders are provided. The methods of the invention comprise administering to a subject a therapeutically effective amount of a pharmaceutically acceptable salt of an A1 adenosine receptor antagonist, particularly 1-hydroxy-2-naphthoic acid salts or 3-hydroxy-2-naphthoic acid salts, more particularly a 1-hydroxy-2-naphthoic acid salt of 3-[2-(4-aminophenyl)ethyl]-8-benzyl-7-{2-[ethyl-(2-hydroxyethyl)amino]ethyl}-1-propyl-3,7-dihydropurine-2,6-dione (i.e., an L-97-1 xinafoic acid salt). Hydrates of the A1 adenosine receptor antagonist salts described herein are further provided. The invention further encompasses pharmaceutical compositions comprising a pharmaceutically acceptable salt of an A1 adenosine receptor antagonist in a pharmaceutically acceptable carrier. The compositions of the invention find use in methods for treating and preventing respiratory disorders.

Abstract: The present invention provides novel adenosine receptor antagonists, more particularly, A1 adenosine receptor antagonists of formula (I). Pharmaceutical compositions comprising an A1 adenosine receptor antagonist of formula (I) and a pharmaceutically acceptable carrier are further provided. Compositions also include diagnostic assay-type probes comprising a novel A1 adenosine receptor antagonist of formula (I) that is labeled or conjugated with radioactive or non-radioactive material. Methods for treating A1 adenosine receptor related disorders comprising administering an A1 adenosine receptor antagonist of formula (I) are also disclosed. The novel A1 adenosine receptor antagonist compositions of formula (I) find further use in diagnostic and imaging methods. wherein R3 is Alk14ArR16, and wherein Alk14 is C1-8 straight or branched alkylene or alkenylene.

Abstract: Compounds of the general formula (I) are described: wherein A is a 5- or 6-membered aromatic or heteroaromatic ring. Compositions comprising such compounds and methods of use thereof are also described.

Abstract: Compounds of the general formula (I) are described: wherein A is a 5- or 6-membered aromatic or heteroaromatic ring. Compositions comprising such compounds and methods of use thereof are also described.

Abstract: Methods and compositions for treating and preventing sepsis are provided. The methods of the invention comprise administering to a subject a therapeutically effective amount of an A1 adenosine receptor antagonist in combination with an antibiotic agent. The invention further encompasses pharmaceutical compositions comprising a combination of an A1 adenosine receptor antagonist and an antibiotic agent in a pharmaceutically acceptable carrier. The pharmaceutical compositions of the invention find use in methods for treating and preventing sepsis.

Abstract: Methods of treating and/or imaging tumors utilize A1 adenosine-receptor activated cells (such as monocytes and macrophages) are described. Activated cells may be administered systemically or locally, and may be radiolabelled to provide imaging and diagnostic functions. Macrophages resident in tissues may be primed and activated for use in treating and imaging tumors.

Abstract: A compound useful as an A1 adenosine receptor antagonist has the formula: wherein R1 is selected from the group consisting of C1-C8 alkyl; R2 is of the formula: R3 is of the formula: —(CH2)qC6H4—R7 R4 is of the formula:

Abstract: A compound useful as an A1 adenosine receptor antagonist has the formula: wherein R1 is selected from the group consisting of C1-C8 alkyl; R2 is of the formula:  wherein is an integer ranging from 1 to 8; R5 is H or (CH2)p, wherein p is an integer ranging from 1 to 8 and R6 is H or (CH2)mOH, wherein m is an integer ranging from 1 to 8; R3 is of the formula: —(CH2)qC6H4—R7  wherein q is an integer ranging from 1 to 8; and wherein R7 is selected from the group consisting of H, NH2, (CH2)tOH, wherein t is an integer ranging from 1 to 8; and R9COOH, wherein R9 is an alkyl or alkylidene group having 1 to 8 carbon atoms; and R4 is of the formula:  wherein Rs is selected from the group consisting of H; NH2; (CH2)rOH, wherein s is an integer ranging from 1 to 8; and R10COOH wherein R10 is an alkyl or alkylidene group having 1 to 8 carbon atoms; and r is an integer ranging from 1 to 8.