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1. 发明授权

US06506758B2 Indole derivatives useful A.O. for the treatment of osteoporosis 失效
标题翻译：吲哚衍生物有用A.O. 用于治疗骨质疏松症
公开(公告)号：US06506758B2
公开(公告)日：2003-01-14
申请号：US09975347
申请日：2001-10-11
申请人： Stefania Gagliardi , Guy Marguerite Marie Gerard Nadler , Pietro A T Novella
发明人： Stefania Gagliardi , Guy Marguerite Marie Gerard Nadler , Pietro A T Novella
IPC分类号： C07D40112
CPC分类号： C07D401/12 , C07D209/18
摘要： A compound of formula (I): or a salt thereof, or a solvate thereof, wherein: A represents an optionally substituted aryl group or an optionally substituted heterocyclyl group; Ra represents —CO—NRsRt wherein Rs and Rt each independently represent hydrogen, alkyl, substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heterocyclyl or an optionally substituted heterocyclylalkyl group, or Rs and Rt together with the nitrogen to which they are attached form a heterocyclyl group; R1 and R2 each independently represents hydrogen, hydroxy, amino, alkoxy, optionally substituted aryloxy, optionally substituted benzyloxy, alkylamino, dialkylamino, halo, trifluoromethyl, trifluoromethoxy, nitro, alkyl, carboxy, carbalkoxy, carbamoyl, alkylcarbamoyl, or R1 and R2 together represent methylenedioxy, carbonyldioxy or carbonyldiamino; and R3 represents hydrogen, alkanoyl, alkyl, aminoalkyl, hydroxyalkyl, carboxyalkyl, carbalkoxyalkyl, carbamoyl or alkylsulphonyl and arylsulphonyl; a process for the preparation of such a compound, a pharmaceutical composition containing such a compound and the use of such a compound or composition in medicine.
摘要翻译：式（I）化合物或其盐或其溶剂化物，其中：A表示任选取代的芳基或任选取代的杂环基; Ra表示-CO-NRsRt，其中R 5和R 5各自独立地表示氢，烷基取代的烷基，任选取代的烯基，任选取代的芳基，任选取代的芳基烷基，任选取代的杂环基或任选取代的杂环基烷基，或R 5和R 5与它们所连接的氮一起形成杂环基; R 1和R 2各自独立地表示氢，羟基，氨基，烷氧基，任选取代的芳氧基，任选取代的苄氧基，烷基氨基，二烷基氨基，卤素，三氟甲基，三氟甲氧基，硝基，烷基，羧基，烷氧基，氨基甲酰基，烷基氨基甲酰基，或R1和R2一起代表亚甲二氧基，羰基二氧基或羰基二氨基; 烷基，氨基烷基，羟基烷基，羧基烷基，烷氧基烷基，氨基甲酰基或烷基磺酰基和芳基磺酰基; 制备这种化合物的方法，含有这种化合物的药物组合物和这种化合物或组合物在医药中的用途。

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