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1.发明公开5-INDOLYL-2,4-PENTADIENOIC ACID DERIVATIVES USEFUL AS INHIBITORS OF BONE RESORPTION 失效5-吲哚基-2,4-戊二烯酸衍生物作为骨吸收抑制剂
公开(公告)号：EP0912511A1
公开(公告)日：1999-05-06
申请号：EP97937473.0
申请日：1997-07-07
发明人： FARINA, Carlo , GAGLIARDI, Stefania , CONSOLANDI, Emanuela , NADLER, Guy, Marguerite, Marie, Gérard , SENECI, Pierfausto SmithKline Beecham Laboratoires
CPC分类号： C07D401/06 , C07D209/18
摘要： A compound of formula (I) or a salt thereof, or a solvate thereof, wherein: R1 represents hydrogen, C1-6 alkyl, halo, azido, C1-6 alkylthio, phnylthio, benzylthio, alkoxyalkyloxy or a group NHR8 wherein R8 represents -CO-R9 or -(CH2)nR11, or R1 represents a group -NR12R13 wherein R12 and R13 each independently represent hydrogen, alkyl or aryl; R2, R3 and R4 each independently represent hydrogen, alkyl, aryl or substituted aryl; R5 and R6 each independently represent hydrogen, hydroxy, amino, alkoxy, optionally substituted aryloxy, optionally substituted benzyloxy, alkylamino, dialkylamino, halo, trifluoromethyl, trifluoromethoxy, nitro, alkyl, carboxy, carbalkoxy, carbamoyl, alkylcarbamoyl, or R5 and R6 together represent methylenedioxy, carbonyldioxy or carbonyldiamino; X represents a hydroxy or an alkoxy group wherein the alkyl group may be substituted or unsubstituted or X represents a group NRsRt wherein Rs and Rt each independently represent hydrogen, alkyl, substituted alkyl, optionally substitued alkenyl, optionally substituted aryl, optionally substituted arylalkyl, an optionally substituted heterocyclic group or an optionally substituted heterocyclylalkyl group, or Rs and Rt together with the nitrogen to which they are attached form a heterocyclic group; R7 represents hydrogen, hydroxy, alkanoyl, alkylaminoalkyl, hydroxyalkyl, carboxyalkyl, carbalkoxyalkyl, carbamoyl or aminosulphonyl; R9 represents R10 or OR10 wherein R10 is C1-6 alkyl, phenyl or benzyl; and R11 represents NR12R13, wherein R12 and R13 are as defined above, or R11 is hydroxy or C1-6 alkoxy; and n represents an integer 1, 2 or 3; a pharmaceutical composition containing such a compound, a process for preparing such a compound and the use of such a compound in medicine.
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公开(公告)号：EP0914321A1
公开(公告)日：1999-05-12
申请号：EP97932778.0
申请日：1997-07-03
CPC分类号： C07D451/02 , C07D209/18 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/12 , C07D451/04 , C07D455/02 , C07D471/04 , C07D471/08
摘要： A compound of formula (I), or a salt thereof, or a solvate thereof, wherein Ra represents a group R5 which is hydrogen, alkyl or optionally substituted aryl and Rb represents a moiety of formula (a), wherein X represents a hydroxy or an alkoxy group wherein the alkyl group may be substitued or unsubstituted or X represents a group NRsRt wherein Rs and Rt each independently represent hydrogen, alkyl, substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted arylalkyl, an optionally substituted heterocyclic group or an optionally substituted heterocyclylalkyl group, or Rs and Rt together with the nitrogen to which they are attached form a heterocyclic group; R1 represents an alkyl or a substituted or unsubstituted aryl group; and R2, R3 and R4 each independently represent hydrogen, alkyl, aryl or substituted aryl; R6 and R7 each independently represent hydrogen, hydroxy, amino, alkoxy, optionally substituted aryloxy, optionally substituted benzyloxy, alkylamino, dialkylamino, halo, trifluoromethyl, trifluoromethoxy, nitro, alkyl, carboxy, carbalkoxy, carbamoyl, alkylcarbamoyl, or R6 and R7 together represent methylenedioxy, carbonyldioxy or carbonyldiamino; and R8 represents hydrogen, hydroxy, alkynoyl, alkyl, aminoalkyl, hydroxyalkyl, carboxyalky, carbalkoxyalkyl, carbamoyl or aminosulphonyl; a process for preparing such a compound, a pharmaceutical composition containing such a compound and the use of such a compound in medecine.
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公开(公告)号：EP0912560A1
公开(公告)日：1999-05-06
申请号：EP97932816.0
申请日：1997-07-07
CPC分类号： C07D403/06 , C07D405/06 , C07D417/06
摘要： A compound of formula (I) or a salt thereof, or a solvate thereof, wherein: R2, R3 and R4 each independently represents hydrogen, alkyl, aryl or substituted aryl; R5 represents hydrogen, alkyl, aryl or substituted aryl; R6 and R7 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 R6 and R7 together represent methylenedioxy, carbonyldioxy or carbonyldiamino; R8 represents hydrogen, hydroxy, alkanoyl, alkyl, aminoalkyl, hydroxyalkyl, carboxyalkyl, carbalkoxyalkyl, carbamoyl or aminosulphonyl; and Z1 and Z2 together with the carbon atom to which they are attached represent a heterocyclic group; a pharmaceutical composition comprising such a compound, a process for preparing such a compound and the use of such compound in medicine.
摘要翻译： 式（I）化合物或其盐或其溶剂化物，其中：R2，R3和R4各自独立地表示氢，烷基，芳基或取代的芳基; R5代表氢，烷基，芳基或取代的芳基; R6和R7各自独立地代表氢，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，烷氧羰基，氨基甲酰基， 亚甲二氧基，羰基二氧基或羰基二氨基; R8代表氢，羟基，烷酰基，烷基，氨基烷基，羟基烷基，羧基烷基，烷氧基烷基，氨基甲酰基或氨基磺酰基; 并且Z 1和Z 2与它们所连接的碳原子一起表示杂环基团; 包含该化合物的药物组合物，制备该化合物的方法以及该化合物在药物中的用途。
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