166 results about "Adenosine receptor antagonist" patented technology

Disclosed are prodrugs of A2B adenosine receptor antagonists, having the following structureand their use in treating mammals for various disease states.

Disclosed are novel A2B adenosine receptor antagonists having the structure of Formula I or Formula II:The compounds are particularly useful for treating asthma, inflammatory gastrointestinal tract disorders, cardiovascular diseases, neurological disorders, and diseases related to undesirable angiogenesis.

The present invention relates generally to compounds of the formula (I):wherein:X is a five or six-membered heteroaromatic ring, containing one to four heteroatoms, selected from nitrogen, oxygen, or sulfur, provided that at least one heteroatom is nitrogen; andG1 and G2 are independently CH or N.The present invention also relates to the preparation of the compounds, pharmaceutical formulations thereof, and their use in medicine as potent or selective A2B adenosine receptor antagonists and their uses for treating asthma, autoimmune diseases and retinal vascular diseases.

A compound useful as an A1 adenosine receptor antagonist has formula (I), wherein R1 is selected from the group consisting of C1-C8alkyl; R2 is of formula (II), wherein n is an integer ranging from 1 to 8; R5 is H or CH3(CH2)p, wherein p is an integer ranging from 1 to 7; and R6 is H; (CH2)mH; or (CH2)mOH, wherein m is an integer ranging from 1 to 8; R3 is selected from the group consisting of: (a), (b), (c) and (d), wherein q is an integer ranging from 1 to 8; D is selected from the group consisting of NH, S, and O; wherein R7 is selected from the group consisting of H, OH, NH2, R9COOH, wherein R9 is an alkylene or alkenylene group having 1 to 8 carbon atoms, and (CH2)tOH, wherein t is an integer ranging from 1 to 8; R11 is selected from the group consisting of -CH2COOH and -CH2-CONH(CH2)wNHZ, wherein w is an integer ranging from 1 to 2 and Z is selected from the group consisting of hydrogen and acetate; and R4 is of formula (III), wherein R8 is selected from the group consisting of H; OH; (CH2)fNH2 wherein f is selected from the group consisting of 0 and an integer ranging from 1 to 8; (CH2)5OH, wherein s is an integer ranging from 1 to 8; and R10COOH, wherein R10 is an alkylene or alkenylene group having 1 to 8 carbon atoms; and r is an integer ranging from 1 to 8.

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.

The present invention relates to the use of adenosine receptor antagonists, preferably A3 receptor antagonists, either alone or in combination with other agents for the treatment, prevention and / or management of diseases or disorders associated with overexpression of HIF-1α and / or increased HIF-1α activity (e.g., cancer, respiratory disease). The methods and compositions of the invention are particularly useful for preventing, treating, or ameliorating symptoms associated with a cancer, disease or disorder associated with hypoxia-inducible factor 1α (HIF-1α) using the A3 receptor antagonists of the invention. The present invention provides methods to inhibit the growth of tumors, particularly solid tumors and more particularly hypoxic tumors.

The invention is related to methods of treating hepatic fibrosis using A2B adenosine receptor antagonists and utility in the treatment of liver damage caused by alcohol abuse, surgical intervention, viral hepatitis, the ingestion of hepatotoxic drugs, or other hepatic diseases.

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.

Disclosed are methods for making novel A2B adenosine receptor antagonists having the structure of formula I or Formula II:The compounds are particularly useful for treating asthma, inflammatory gastrointestinal tract disorders, cardiovascular diseases, neurological disorders, and diseases related to undesirable angiogenesis.

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.