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36 条记录 (耗时 0.019 秒)

    5-INDOLYL-2,4-PENTADIENOIC ACID DERIVATIVES USEFUL AS INHIBITORS OF BONE RESORPTION
    4.
    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

    申请人： Smithkline Beecham S.p.A. ,  SMITHKLINE BEECHAM LABORATOIRES PHARMACEUTIQUES

    发明人： FARINA, Carlo ,  GAGLIARDI, Stefania ,  CONSOLANDI, Emanuela ,  NADLER, Guy, Marguerite, Marie, Gérard ,  SENECI, Pierfausto SmithKline Beecham Laboratoires

    IPC分类号： C07D401 ,  A61K31 ,  A61P19 ,  C07D209

    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.

    HETEROCYCLIC CARBOXAMIDE DERIVATIVES WITH ANTIARRHYTHMIC ACTIVITY
    8.
    发明公开
    HETEROCYCLIC CARBOXAMIDE DERIVATIVES WITH ANTIARRHYTHMIC ACTIVITY 失效
    WITH影响ANTIARRYTHMISCHER杂环甲酰胺

    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

    申请人： SMITHKLINE BEECHAM LABORATOIRES PHARMACEUTIQUES

    发明人： NADLER, Guy, Marguerite, Marie, Gérard SmithKline

    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.

    AZALICYCLOOCTANE DERIVATIVES AS ANTI-ARRHYTHMIC AGENTS
    9.
    发明公开
    AZALICYCLOOCTANE DERIVATIVES AS ANTI-ARRHYTHMIC AGENTS 失效
    AZALICYCLOOCTANE衍生物作为抗心律失常药物

    公开(公告)号：EP0710236A1

    公开(公告)日：1996-05-08

    申请号：EP94924752.0

    申请日：1994-07-11

    申请人： SMITHKLINE BEECHAM LABORATOIRES PHARMACEUTIQUES

    发明人： NADLER, Guy M. M. G., Smithkline ,  SOUCHET, Michel L., Smithkline

    IPC分类号： C07D453 ,  A61K31 ,  A61P9 ,  C07D451

    CPC分类号： C07D451/04

    摘要： A compound of formula (I) or a salt thereof, or a solvate thereof, wherein B represents a C1-4 n-alkylene group wherein each carbon is optionally substituted by a C1-6 alkyl group; Z represents a bond, CH2, (CH2)2 or X-CH2-CH2 wherein X represents O or S; D represents CO, SO2, NH-CO or NH-SO2; T represents a bond and U represents CH2 or T represents CH2 and U represents a bond; Q represents aryl, aralkyl, aralkenyl or aralkynyl, wherein the aryl moiety may be unsubstituted or substituted with 1 to 5 substituents selected from the list consisting of nitro, halogen, alkylsulfonamido, acylamido, 1H-imidazolyl, 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, 1H-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 represents 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 or six atoms wherein one, two or three of the said atoms are oxygen or nitrogen; 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 the preparation of such a compound and the use of such a compound in medicine.

    摘要翻译： 式（I）化合物或其盐或其溶剂化物，其中B表示其中每个碳任选被C1-6烷基取代的C1-4正亚烷基; Z表示键，CH 2，（CH 2）2或X-CH 2 -CH 2，其中X表示O或S; D代表CO，SO2，NH-CO或NH-SO2; T表示键并且U表示CH 2或T表示CH 2并且U表示键; Q代表芳基，芳烷基，芳烯基或芳炔基，其中芳基部分可以未被取代或被1至5个选自硝基，卤素，烷基磺酰氨基，酰基酰氨基，1H-咪唑基，烷基或卤代烷基的取代基取代，或Q代表取代 噻吩基，噻唑基，1H-咪唑基或三唑基，吲哚基，氧代吲哚基，茚基，异茚基，吲唑基，中氮茚基或吡啶基或​​环烷基，呋喃基，噻吩基，噻唑基，咪唑基，三唑基或苯并稠合的等价物 与芳基稠合; 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五 或六个原子，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，其中任选取代基为上述定义的R1，R2和R3或者Ar表示取代或未取代的杂芳基; 制备这种化合物的方法以及这种化合物在药物中的用途。

    ANTI-ARRHYTHMIC N-SUBSTITUTED 3-BENZAZEPINES OR ISOQUINOLINES
    10.
    发明公开
    ANTI-ARRHYTHMIC N-SUBSTITUTED 3-BENZAZEPINES OR ISOQUINOLINES 失效
    抗心律失常的N-取代的3-苯并吖庚因或异喹啉

    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

    申请人： SMITHKLINE BEECHAM LABORATOIRES PHARMACEUTIQUES

    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.