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1. 发明申请

WO2002074780A1 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO2002074780A1
公开(公告)日：2002-09-26
申请号：PCT/GB2002/001317
申请日：2002-03-19
申请人： GLAXO GROUP LIMITED , HALL, Adrian , JANDU, Karamjit, Singh , LUNNIS, Christopher, James , VINADER, Maria, Victoria , WEST, Robert, Ian
发明人： HALL, Adrian , JANDU, Karamjit, Singh , LUNNIS, Christopher, James , VINADER, Maria, Victoria , WEST, Robert, Ian
IPC分类号： C07H19/16
CPC分类号： C07H19/16 , C07D473/34
摘要： The present invention is concerned with pharmaceutical compositions containing certain adenosine derivatives having an acetylene group in the 4' position, which are adenosine A1 agonists, and to their use in therapy.
摘要翻译：本发明涉及含有腺苷A1激动剂的4'位具有乙炔基的某些腺苷衍生物及其在治疗中的用途的药物组合物。

2. 发明申请

WO1995008549A1 3-(5-TETRAZOLYL-BENZYL)AMINO-PIPERIDINE DERIVATIVES AND ANTAGONISTS OF TACHYKININS 审中-公开
标题翻译： 3-（5-四羧基 - 苄基）氨基哌啶衍生物和TACHYKININS的拮抗剂
公开(公告)号：WO1995008549A1
公开(公告)日：1995-03-30
申请号：PCT/EP1994003129
申请日：1994-09-20
申请人： GLAXO GROUP LIMITED , ARMOUR, Duncan, Robert , EVANS, Brian , GIBLIN, Gerard, Martin, Paul , HANN, Michael, Menteith , HUBBARD, Tania , LEWELL, Xiao-Qing , MIDDLEMISS, David , NAYLOR, Alan , PEGG, Neil, Anthony , VINADER, Maria, Victoria , WATSON, Stephen, Paul
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D401/10
CPC分类号： C07D401/12
摘要： The present invention relates to piperidine derivatives of formula (I), wherein R is a C1-4alkoxy group; R is formula (a); R is a hydrogen or halogen atom; R and R may each independently represent a hydrogen or halogen atom, or a C1-4alkyl, C1-4alkoxy or trifluoromethyl group; R is a hydrogen atom, a C1-4alkyl, (CH2)mcyclopropyl, -S(O)nC1-4alkyl, phenyl, NR R , CH2C(O)CF3 or trifluoromethyl group; R and R may each independently represent a hydrogen atom, or a C1-4alkyl or acyl group; x represents zero or 1; n represents zero, 1 or 2; m represents zero or 1; and pharmaceutically acceptable salts and solvates thereof; to processes for their preparation; and their use in the treatment of conditions mediated by tachykinins.
摘要翻译：本发明涉及式（I）的哌啶衍生物，其中R 1是C 1-4烷氧基; R 2是式（a）; R 3是氢或卤素原子; R 4和R 5各自独立地表示氢或卤素原子，或C 1-4烷基，C 1-4烷氧基或三氟甲基; R 6是氢原子，C 1-4烷基，（CH 2）m环丙基，-S（O）n C 1-4烷基，苯基，NR 7 R 8，CH 2 C（O）CF 3或三氟甲基; R 7和R 8可各自独立地表示氢原子或C 1-4烷基或酰基; x表示零或1; n表示0，1或2; m表示0或1; 及其药学上可接受的盐和溶剂合物; 进行准备; 及其用于治疗由速激肽介导的病症。

3. 发明申请

WO2004071389A3 NON-STEROIDAL INFALMMATION INHIBITORS 审中-公开
标题翻译：非立体感染抑制剂
公开(公告)号：WO2004071389A3
公开(公告)日：2004-12-02
申请号：PCT/EP2004001507
申请日：2004-02-13
申请人： GLAXO GROUP LTD , BARKER MICHAEL DAVID , DEMAINE DEREK ANTHONY , HOUSE DAVID , INGLIS GRAHAM GEORGE ADAM , JOHNSTON MICHAEL JOHN , JONES HAYDN TERENCE , MACDONALD SIMON JOHN FAWCETT , MCLAY IAIN MCFARLANE , SHANAHAN STEPHEN , SKONE PHILIP ALAN , VINADER MARIA VICTORIA
发明人： BARKER MICHAEL DAVID , DEMAINE DEREK ANTHONY , HOUSE DAVID , INGLIS GRAHAM GEORGE ADAM , JOHNSTON MICHAEL JOHN , JONES HAYDN TERENCE , MACDONALD SIMON JOHN FAWCETT , MCLAY IAIN MCFARLANE , SHANAHAN STEPHEN , SKONE PHILIP ALAN , VINADER MARIA VICTORIA
IPC分类号： A61P29/00 , C07D265/02 , C07D413/12 , A61K31/536
CPC分类号： C07D265/02 , C07D413/12
摘要： A compound of formula (I) wherein: n represents an integer 0, 1 or 2; X represents, O, S, NR , or CHR ; R represents hydrogen, halogen such as F, Cl or Br, NO2, hydroxy, cyano, -OC1-6 alkoxy such as methoxy, C1-6 alkyl such as methyl, NR R such as NH2, NR COR such as -NHCHO or -NHCOCH3, COOR or CONR R ; R represents hydrogen, halogen such as F, Cl, Br, NO2, hydroxy, cyano, -OC1-6 alkoxy such as methoxy, C1-6 alkyl such as methyl, NR R such as NH2, NR COR such as -NHCHO or -NHCOCH3, COOR or CONR R ; R represents hydrogen, halogen such as F, Cl, Br, NO2, hydroxy, cyano, -OC1-6 alkoxy such as methoxy, C1-6 alkyl such as methyl, NR R such as NH2, NR COR such as -NHCHO or -NHCOCH3, COOR , CONR R ; R represents hydrogen, halogen such as F, Cl, Br, NO2, hydroxy, cyano, -OC1-6 alkoxy such as methoxy, C1-6 alkyl such as methyl, NR R such as NH2, NR COR such as -NHCHO or -NHCOCH3, COOR or CONR R ; R represents H, C1-6 alkyl, or C1-6 alkenyl; R represents hydrogen, C1-6 alkyl, CO2C1-3 alkyl, COC1-3 alkyl or SO2C1-3 alkyl; R represents hydrogen, or C1-6 alkyl; R represents hydrogen, C1-6 alkyl, C1-3 alkyleneSiC1-3 alkyl such as -CH2CH2Si(CH3)3; R and R independently represent hydrogen or C1-6 alkyl; including pharmaceutically acceptable esters, amides and carbamates thereof, salts thereof, solvates thereof, and solvates of such pharmaceutically acceptable esters, amides, carbamates and salts.
摘要翻译：式（I）的化合物，其中：n表示整数0,1或2; X表示O，S，NR 6a或CHR 6b; R 1表示氢，卤素如F，Cl或Br，NO 2，羟基，氰基，-OC 1-6烷氧基如甲氧基，C 1-6烷基如甲基，NR 8 R 9如NH 2 NR 8 COR 9如-NHCHO或-NHCOCH 3，COOR 7或CONR 8 R 9; R 2表示氢，卤素如F，Cl，Br，NO 2，羟基，氰基，-OC 1-6烷氧基如甲氧基，C 1-6烷基如甲基，NR 8 R 9如NH 2 NR 8 COR 9如-NHCHO或-NHCOCH 3，COOR 7或CONR 8 R 9; R 3表示氢，卤素如F，Cl，Br，NO 2，羟基，氰基，-OC 1-6烷氧基如甲氧基，C 1-6烷基如甲基，NR 8 R 9如NH 2 NR 8 COR 9如-NHCHO或-NHCOCH 3，COOR 7，CONR 8 R 9; R 4表示氢，卤素如F，Cl，Br，NO 2，羟基，氰基，-OC 1-6烷氧基如甲氧基，C 1-6烷基如甲基，NR 8 R 9如NH 2 NR 8 COR 9如-NHCHO或-NHCOCH 3，COOR 7或CONR 8 R 9; R 5表示H，C 1-6烷基或C 1-6烯基; R 6a表示氢，C 1-6烷基，CO 2 C 1-3烷基，COC 1-3烷基或SO 2 C 1-3烷基; R 6b表示氢或C 1-6烷基; R 7表示氢，C 1-6烷基，C 1-3亚烷基，C 1-3烷基如-CH 2 CH 2 Si（CH 3）3; R 8和R 9独立地表示氢或C 1-6烷基; 包括其药学上可接受的酯，酰胺和氨基甲酸酯，其盐，溶剂合物和这些药学上可接受的酯，酰胺，氨基甲酸酯和盐的溶剂合物。

4. 发明申请

WO2004071389A2 COMPOUNDS 审中-公开
标题翻译：化合物
公开(公告)号：WO2004071389A2
公开(公告)日：2004-08-26
申请号：PCT/EP2004/001507
申请日：2004-02-13
申请人： GLAXO GROUP LIMITED , BARKER, Michael, David , DEMAINE, Derek, Anthony , HOUSE, David , INGLIS, Graham, George, Adam , JOHNSTON, Michael, John , JONES, Haydn, Terence , MACDONALD, Simon, John, Fawcett , MCLAY, Iain McFarlane , SHANAHAN, Stephen , SKONE, Philip, Alan , VINADER, Maria, Victoria
发明人： BARKER, Michael, David , DEMAINE, Derek, Anthony , HOUSE, David , INGLIS, Graham, George, Adam , JOHNSTON, Michael, John , JONES, Haydn, Terence , MACDONALD, Simon, John, Fawcett , MCLAY, Iain McFarlane , SHANAHAN, Stephen , SKONE, Philip, Alan , VINADER, Maria, Victoria
IPC分类号： A61K
CPC分类号： C07D265/02 , C07D413/12
摘要： A compound of formula (I) wherein: n represents an integer 0, 1 or 2; X represents, O, S, NR 6a , or CHR 6b ; R 1 represents hydrogen, halogen such as F, Cl or Br, NO 2 , hydroxy, cyano, -OC 1-6 alkoxy such as methoxy, C 1-6 alkyl such as methyl, NR 8 R 9 such as NH 2 , NR 8 COR 9 such as -NHCHO or -NHCOCH 3 , COOR 7 or CONR 8 R 9 ; R 2 represents hydrogen, halogen such as F, Cl, Br, NO 2 , hydroxy, cyano, -OC 1-6 alkoxy such as methoxy, C 1-6 alkyl such as methyl, NR 8 R 9 such as NH 2 , NR 8 COR 9 such as -NHCHO or -NHCOCH 3 , COOR 7 or CONR 8 R 9 ; R 3 represents hydrogen, halogen such as F, Cl, Br, NO 2 , hydroxy, cyano, -OC 1-6 alkoxy such as methoxy, C 1-6 alkyl such as methyl, NR 8 R 9 such as NH 2 , NR 8 COR 9 such as -NHCHO or -NHCOCH 3 , COOR 7 , CONR 8 R 9 ; R 4 represents hydrogen, halogen such as F, Cl, Br, NO 2 , hydroxy, cyano, -OC 1-6 alkoxy such as methoxy, C 1-6 alkyl such as methyl, NR 8 R 9 such as NH 2 , NR 8 COR 9 such as -NHCHO or -NHCOCH 3 , COOR 7 or CONR 8 R 9 ; R 5 represents H, C 1-6 alkyl, or C 1-6 alkenyl; R 6a represents hydrogen, C 1-6 alkyl, CO 2 C 1-3 alkyl, COC 1-3 alkyl or SO 2 C 1-3 alkyl; R 6b represents hydrogen, or C 1-6 alkyl; R 7 represents hydrogen, C 1-6 alkyl, C 1-3 alkyleneSiC 1-3 alkyl such as -CH 2 CH 2 Si(CH 3 ) 3 ; R 8 and R 9 independently represent hydrogen or C 1-6 alkyl; including pharmaceutically acceptable esters, amides and carbamates thereof, salts thereof, solvates thereof, and solvates of such pharmaceutically acceptable esters, amides, carbamates and salts.
摘要翻译：式（I）的化合物，其中：n表示整数0,1或2; X表示O，S，NR 6a或CHR 6b; R 1表示氢，卤素如F，Cl或Br，NO 2，羟基，氰基，-OC 1-6烷氧基如甲氧基，C 1-6烷基如甲基，NR 8 R 9如NH 2 NR 8 COR 9如-NHCHO或-NHCOCH 3，COOR 7或CONR 8 R 9; R 2表示氢，卤素如F，Cl，Br，NO 2，羟基，氰基，-OC 1-6烷氧基如甲氧基，C 1-6烷基如甲基，NR 8 R 9如NH 2 NR 8 COR 9如-NHCHO或-NHCOCH 3，COOR 7或CONR 8 R 9; R 3表示氢，卤素如F，Cl，Br，NO 2，羟基，氰基，-OC 1-6烷氧基如甲氧基，C 1-6烷基如甲基，NR 8 R 9如NH 2 ，NR 8 COR 9如-NHCHO或-NHCOCH 3，COOR 7，CONR 8 R 9; R 4表示氢，卤素如F，Cl，Br，NO 2，羟基，氰基，-OC 1-6烷氧基如甲氧基，C 1-6烷基如甲基，NR 8 R 9如NH 2 NR 8 COR 9如-NHCHO或-NHCOCH 3，COOR 7或CONR 8 R 9; R 5表示H，C 1-6烷基或C 1-6烯基; R 6a表示氢，C 1-6烷基，CO 2 C 1-3烷基，COC 1-3烷基或SO 2 C 1-3烷基; R 6b表示氢或C 1-6烷基; R 7表示氢，C 1-6烷基，C 1-3亚烷基，C 1-3烷基如-CH 2 CH 2 Si（CH 3）3; R 8和R 9独立地表示氢或C 1-6烷基; 包括其药学上可接受的酯，酰胺和氨基甲酸酯，其盐，溶剂化物，和这些药学上可接受的酯，酰胺，氨基甲酸酯和盐的溶剂合物。

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