| abstract |
"INDOL DERIVATIVES AND THEIR USE FOR OSTEOPOROSIS TREATMENT AMONG OTHER APPLICATIONS". A compound of formula (I), or its salt or solvate, wherein: R ~ 1 ~ and R ~ 2 ~ each independently represent C ~ 1-6 ~ alkoxy or halo; R ~ 3 ~ and R ~ 4 ~ each independently represent hydrogen, C ~ 1-6 ~ alkoxy, C ~ 1-6 ~ aryl alkoxy, hydroxy, C ~ 1-6 ~ alkoxy carbonoxy, C ~ 1-6 alkoxy hydroxy ~, C ~ 1-6 ~ alkoxy dihydroxy, mono- and di (C ~ 1-6 ~ alkyl) amino C ~ 1-6 ~ alkoxy, or C ~ 1-6 ~ amino alkoxy, and R ~ 5 ~ represents - NR ~ s ~ R ~ t ~, where R ~ s ~ and R ~ t ~ each independently represent hydrogen, unsubstituted or substituted C ~ 1-6 ~ alkyl, or unsubstituted or substituted heterocyclyl, a process for preparing such compound, pharmaceutical composition containing that compound and the use of the compound or composition in medicine. Particular indole compounds are selective for mammalian osteoclasts, acting in the selective inhibition of their bone resorption activity. These compounds are therefore considered particularly useful for the treatment and / or prophylaxis of diseases associated with loss of bone mass, such as osteoporosis and related osteopenic diseases, Paget's disease, hyperparathyroidism and related diseases. These compounds are also considered to have antitumor activity, antiviral activity (for example, against Semliki Forest, Vesicular Stomatitis, Newcastle Disease, Influenza A and B, HIV), anti-ulcer activity (for example, compounds can be useful for the treatment of chronic gastritis and Helicobacter pylori-induced peptic ulcer), immunosuppressive activity, antilipidemic activity, anti-atherosclerotic activity and useful for the treatment of AIDS and Alzheimer's disease. In addition, these compounds are also considered useful in inhibiting angiogenesis, that is, the formation of new blood vessels that is observed in various types of pathological conditions (angiogenic diseases), such as rheumatoid arthritis, diabetic retinopathy, psoriasis and solid tumors. |