Abstract:
R3 is Alk14ArR16, wherein Alk14 is C1-8 straight or branched alkylene or alkenylene, Ar is a 5- or 6-member aromatic ring containing 0 to 4 heteroato ms selected from N, O, and S, or is a bicyclic 9- or 11-member aromatic ring containing 0 to 6 heteroatoms selected from N, O, and S; R4 is --((CH2)r- Phenyl-R20 wherein r is 1 to 20, R20 is SO3H, PO3H2, halogen, OR13c, COOR13d , NO2, NR21R22, and other choices. The compound optionally has one or more radioactive or non-radioactive label moieties wherein the label moieties are optionally connected to the compound through one or more spacer moiety. The present invention also provides for their use as therapeutic agents and diagnostic agents.
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 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 A 1 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 A 1 adenosine receptor antagonist salts described herein are further provided. The invention further encompasses pharmaceutical compositions comprising a pharmaceutically acceptable salt of an A 1 adenosine receptor antagonist in a pharmaceutically acceptable carrier. The compositions of the invention find use in methods for treating and preventing respiratory disorders.
Abstract:
This invention relates to compounds of formula (I): wherein R1 is a branched or straight chain C1-C8 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; R 4 is of the formula (IV), wherein r is an integer ranging from 1 to 8 and R8 i s selected from the group consisting of H, OH, (CH2)fNH2, (CH2)sOH, and R10COO H; wherein f is 0 or f and s are independently integers ranging from 1 to 8; an d, R10 is a C1-C8 straight or branched chain alkylene or alkenylene; and; salts , solvates, and hydrates thereof. The present invention further provides metho ds of preparing the compounds of formula (I) and their use as therapeutic agent s and diagnostic agents.
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 A 1 adenosine receptors in cells of the subject, and increasing the affinity of cells of the subject for A 1 adenosine receptor ligands. The preventative and diagnostic methods of the present invention may be carried out with kits and pharmaceutical liposomal formulations.
Abstract:
Glycolipids are useful for enhancing the affinity of A1 adenosine receptor ligands for the A1 adenosine receptor. Glycolipids are accordingly useful in diagnostic and therapeutic methods that require the delivery or administrati on of A1 adenosine ligands.
Abstract:
The present invention relates to the methods of use for measurement of lipopolysaccharide (LPS) and methods of use for diagnosis of sepsis and LPS-related conditions. Specifically the present invention relates to a time resolved fluorescence (TRF) based assay for the measurement of LPS and methods of use for the measurement of LPS to diagnose sepsis, Gram-negative bacterial infections, and LPS-related conditions.
Abstract:
The present invention relates to the methods of use for measurement of lipopolysaccharide (LPS) and methods of use for diagnosis of sepsis and LPS-related conditions. Specifically the present invention relates to a time resolved fluorescence (TRF) based assay for the measurement of LPS and methods of use for the measurement of LPS to diagnose sepsis, Gram-negative bacterial infections, and LPS-related conditions.
Abstract:
This invention relates to compounds of formula (I), Wherein R 1 - R 4 are defined in the Specification, their uses in the practice of medicine, their medicinal formulations, their use in medical diagnosis, and their preparation.