166 results about "Adenosine receptor antagonist" patented technology

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.

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 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.

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.

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.