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公开(公告)号：EP0700385A1
公开(公告)日：1996-03-13
申请号：EP94918376.0
申请日：1994-05-24
发明人： NADLER, Guy, Marguerite, Marie, Gérard SmithKline , MORVAN, Marcel, Jean-Marie SmithKline Beecham
CPC分类号： C07D401/06 , C07D211/58 , C07D401/12 , C07D405/12 , C07D409/12
摘要： A compound of formula (I) or a salt thereof, or a solvate thereof, wherein A represents (CH2)n wherein n represents zero or an integer 1 or 2; B represents a C2-4n-alkylene group wherein each carbon is optionally substituted by a C1-6alkyl group; Z represents a bond (CH2)m wherein m is an integer in the range of from 1 to 4 or X-CH2-CH2 wherein X represents O or S; D represents CO, SO2, NH-CO, NH-SO2, -CH=CH- or P(O)OR4 wherein R4 is C1-6alkyl; Q represents aryl, aralkyl, aralkenyl or aralkynyl, wherein the aryl moiety may be substituted or unsubstituted with 1 to 5 substituents selected from the list consisting of nitro, halogen, alkylsulfonamide, 1-imidazo, alkyl or haloalkyl, or Q represents substituted furanyl, substituted thienyl or substituted or unsubstituted: pyranyl, thiazolyl, imidazolyl, triazolyl or the benzo fused equivalents of furanyl, pyranyl, thienyl, thiazolyl, imidazolyl or triazolyl, indolyl, oxoindolyl, indenyl, isoindenyl, indazolyl, indolizinyl or pyridinyl or cycloalkyl optionally fused to an aryl group; R1, R2 and R3 each independently represent H, alkyl, OH or alkoxy or, if attached to adjacent carbon atoms, any two of R1, R2 or R3 together with the carbon atoms to which they are attached may form a fused heterocyclic ring of four to six atoms wherein one, two or three of the said atoms are oxygen or nitrogen; and Ar represents substituted or unsubstituted aryl, wherein the optional substituents are the above defined R1, R2 and R3 or Ar represents a substituted or unsubstituted heteroaryl group; a process for preparing such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.
摘要翻译： 式（I）化合物或其盐或其溶剂合物，其中A代表（CH 2）n，其中n代表零或1或2的整数; B表示其中每个碳任选被C 1-6烷基取代的C 2-4正亚烷基; Z表示键（CH 2）m，其中m是1至4的整数或X-CH 2 -CH 2，其中X表示O或S; D表示CO，SO 2，NH-CO，NH-SO 2，-CH = CH-或P（O）OR 4，其中R 4为C 1-6烷基; Q代表芳基，芳烷基，芳烯基或芳炔基，其中芳基部分可被1至5个选自硝基，卤素，烷基磺酰胺，1-咪唑基，烷基或卤代烷基的取代基取代或未取代，或Q代表取代的呋喃基， 呋喃基，噻吩基，噻唑基，咪唑基或三唑基，吲哚基，氧代吲哚基，茚基，异茚基，吲唑基，吲嗪基或吡啶基或环烷基的吡喃基，噻唑基，咪唑基，三唑基或苯并稠合的等价物， 芳基; R 1，R 2和R 3各自独立地表示H，烷基，OH或烷氧基，或者如果连接到相邻的碳原子上，则R 1，R 2或R 3中的任意两个与它们所连接的碳原子一起可以形成四 至六个原子，其中所述原子中的一个，两个或三个是氧或氮; Ar表示取代或未取代的芳基，其中任选的取代基为上述定义的R1，R2和R3或Ar表示取代或未取代的杂芳基; 制备这些化合物的方法，包含这些化合物的药物组合物以及这些化合物在医学中的用途。
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2.发明公开
公开(公告)号：EP0719263A1
公开(公告)日：1996-07-03
申请号：EP94926240.0
申请日：1994-09-05
IPC分类号： C07D233 , A61K31 , A61P9 , C07C217 , C07D235 , C07D271 , C07D277 , C07D307 , C07D333 , C07D521
CPC分类号： C07D271/12 , C07C217/84 , C07D307/73 , C07D333/42
摘要： A compound of formula (I), or a salt thereof, or a solvate thereof, wherein A and B each independently represents a C1-4 n-alkylene group wherein each carbon is optionally substituted by a C1-6 alkyl group; D represents CO, SO2, NH-CO or CH2CO; T represents hydrogen, alkyl, alkene or cycloalkyl; and Het represents substituted or unsubstituted: furanyl, pyranyl, thienyl, thiazolyl, imidazolyl, triazolyl or the benzo fused equivalents of furanyl, pyranyl, thienyl, thiazolyl, imidazolyl, or triazolyl, indolyl, oxoindolyl, indenyl, isoindenyl, indazolyl, indolizinyl, or benzofurazanyl; optional substituents for the moiety Het include 1 to 5 substituents selected from the list consisting of nitro, halogen, alkylsulfonamido, alkylamido, 1H-imidazolyl, alkyl and haloalkyl; R1, R2 and R3 each independently represent H, alkyl, OH or alkoxy or, if attached to adjacent carbon atoms, any two of R1, R2 or R3 together with the carbon atoms to which they are attached may form a fused heterocyclic ring of five to six atoms wherein one, two or three of the said atoms are oxygen or nitrogen; Z represents a bond, CH2, (CH2)2 or X-CH2-CH2 wherein X represents O or S; and Ar represents substituted or unsubstituted aryl, wherein the optional substituents are the above defined R1, R2 and R3; a composition containing such compound, a process for the preparation of such a compound and the use of such a compound in medicine.
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公开(公告)号：EP0700389A1
公开(公告)日：1996-03-13
申请号：EP94918377.0
申请日：1994-05-24
发明人： NADLER, Guy, Marguerite, Marie, Gérard SmithKline , MARTIN, Michel, Jean, Roger SmithKline Beecham
IPC分类号： A61K31 , A61P9 , C07D217 , C07D223 , C07D401 , C07D403 , C07D405 , C07D409 , C07D521 , C07F9
CPC分类号： C07D223/16 , C07D217/04 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07F9/6558
摘要： A compound of formula (I) or a salt thereof, or a solvate thereof, wherein A represents CH2, (CH2)2, CO, COCH2, CH2CO, CSCH2 or CH=CH; B represents CH2 or CO; Z represents a bond, CH2, (CH2)2 or X-CH2-CH2 wherein X represents O or S; D represents CO, SO2, NH-CO, NH-SO2, CH=CH or P(O)OR6 wherein R6 is C1-6 alkyl; Q represents aryl, aralkyl, aralkenyl or aralkynyl, wherein the aryl moiety may be substituted or unsubstituted with 1 to 5 substituents selected from the list consisting of nitro, halogen, alkylsulfonamide, amino, 1-imidazo, alkyl or haloalkyl, or Q represents substituted or unsubstituted: furanyl, pyranyl, thienyl, thiazolyl, imidazolyl, triazolyl or the benzo fused equivalents of furanyl, pyranyl, thienyl, thiazolyl, imidazolyl or triazolyl, indolyl, oxoindolyl, indenyl, isoindenyl, indazolyl, indolizinyl or pyridinyl or cycloalkyl optionally fused to an aryl group; R1, R2, R3, R4 and R5 each independently represent H, alkyl, OH or alkoxy or, if attached to adjacent carbon atoms, any two of R1, R2, R3, R4 and R5 together with the carbon atoms to which they are attached may form a fused heterocyclic ring of four to six atoms wherein one, two or three of the said atoms are oxygen or nitrogen; and E represents C2-4 n-alkylene group wherein each carbon is optionally substituted by R6; a process for preparing such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.
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