发明名称 INDOLE DERIVATIVES AND THEIR USE FOR THE TREATMENT OF OSTEOPOROSIS AMONGST OTHER APPLICATIONS
摘要 A compound of formula (I) or a salt thereof, or a solvate thereof, wherein: R1 and R2 each independently represents C1-6alkoxy or halo; R3 and R4 each independently represents hydrogen, C1-6alkoxy, arylC1-6alkoxy, hydroxy, carboxyC1-6alkoxy, hydroxyC1-6alkoxy, dihydroxyC1-6alkoxy, mono- and di-(C1- 6alkyl)aminoC1-6alkoxy or aminoC1-6alkoxy, and R5 represents -NRsRt wherein Rs and Rt each independently represent hydrogen, unsubstituted or substituted C 1- 6alkyl, or unsubstituted or substituted heterocyclyl, a process for the preparation of such a compound, a pharmaceutical composition containing such a compound and the use of the compound or composition in medicine. Particular indole compounds are selective for mammalian osteoclasts, acting to selectively inhibit their bone resorbing activity. These compounds are therefore considered to be 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 considere d to possess antitumour activity, antiviral activity (for example against Semliki Forest, Vesicular Stomatitis, Newcastle Disease, Influenza A and B, HIVviruses), antiulcer activity (for examplethe compounds may be useful for the treatment of chronic gastritis and peptic ulcer induced by Helicobacter pylori) immunosuppressant activity, antilipidemic activity, antiatherosclerotic activity and to be useful for the treatment of AIDS and Alzheimer's disease. Furthermore, these compounds are also consider ed useful in inhibiting angiogenesis i.e. the formation of new blood vessels which is observed in various types of pathological conditions (angiogenic diseases) such as rheumatoid arthritis, diabetic retinopathy, psoriasis and solid tumours.
申请公布号 CA2376657(A1) 申请公布日期 2001.01.11
申请号 CA20002376657 申请日期 2000.06.16
申请人 GLAXOSMITHKLINE S.P.A. 发明人 FARINA, CARLO;GAGLIARDI, STEFANIA;NOVELLA, PIETRO A. T.
分类号 A61K31/404;A61K31/4439;A61K31/454;A61K31/496;A61K31/506;A61P1/00;A61P1/04;A61P3/06;A61P9/10;A61P11/00;A61P13/12;A61P17/00;A61P17/06;A61P19/02;A61P19/10;A61P25/28;A61P27/02;A61P29/00;A61P31/04;A61P31/12;A61P31/16;A61P31/18;A61P35/00;A61P35/02;A61P37/06;A61P43/00;C07D209/18;C07D401/12;C07D403/12;(IPC1-7):C07D401/12 主分类号 A61K31/404
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