The title compds. I [R1, R2 = (un)substituted alkyl; R3 = H, halo; R4, R5 = H or alkyl; R6 = (un)substituted (hetero)aryl] which are adenosine A2B receptor antagonists and, thus, may be employed for the treatment of conditions and diseases mediated by the adenosine A2B receptor activity, were prepd. Such conditions and diseases include, but are not limited to, chronic and acute inflammatory diseases involving degranulation of mast cells, e.g., asthma, allergic rhinitis and allergic dermatitis; impaired sensitivity to insulin, e.g., type 2 diabetes, non-insulin dependent diabetes, pre-diabetic state, and impaired glucose tolerance; diseases in which angiogenesis is a key component of pathogenesis, e.g., solid tumors and angiogenic retinopathies; apnea of preterm infants; myocardial reperfusion injury; inflammatory bowel disease; autoimmune diseases, such as rheumatoid arthritis, multiple sclerosis, and lupus erythematosus; diseases involving microvascular abnormalities of the retina that are mediated by adenosine A2B receptors, e.g., retinopathy of prematurity, macular degeneration, and diabetic retinopathy; and cardiac diseases including hyperplasia consequent to hypertension, arteriosclerosis, and heart attack. E.g., a multi-step synthesis of II, starting from aniline, was described. Exemplified compds. I were tested in adenosine A2B receptor binding and functional assays (data given). Pharmaceutical compn. comprising the compd. I is disclosed.
Preparation of substituted purinylpyrazolylacetamides as adenosine A2B receptor antagonists.
BARALDI, Pier Giovanni;BOREA, Pier Andrea;AGHAZADEH TABRIZI, Mojgan
2008
Abstract
The title compds. I [R1, R2 = (un)substituted alkyl; R3 = H, halo; R4, R5 = H or alkyl; R6 = (un)substituted (hetero)aryl] which are adenosine A2B receptor antagonists and, thus, may be employed for the treatment of conditions and diseases mediated by the adenosine A2B receptor activity, were prepd. Such conditions and diseases include, but are not limited to, chronic and acute inflammatory diseases involving degranulation of mast cells, e.g., asthma, allergic rhinitis and allergic dermatitis; impaired sensitivity to insulin, e.g., type 2 diabetes, non-insulin dependent diabetes, pre-diabetic state, and impaired glucose tolerance; diseases in which angiogenesis is a key component of pathogenesis, e.g., solid tumors and angiogenic retinopathies; apnea of preterm infants; myocardial reperfusion injury; inflammatory bowel disease; autoimmune diseases, such as rheumatoid arthritis, multiple sclerosis, and lupus erythematosus; diseases involving microvascular abnormalities of the retina that are mediated by adenosine A2B receptors, e.g., retinopathy of prematurity, macular degeneration, and diabetic retinopathy; and cardiac diseases including hyperplasia consequent to hypertension, arteriosclerosis, and heart attack. E.g., a multi-step synthesis of II, starting from aniline, was described. Exemplified compds. I were tested in adenosine A2B receptor binding and functional assays (data given). Pharmaceutical compn. comprising the compd. I is disclosed.I documenti in SFERA sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
