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1. 发明申请

WO2005030212A1 4-AMINOQUINOLINE-3-CARBOXAMIDE DERIVATIVES AS PDE4 INHIBITORS 审中-公开
标题翻译：作为PDE4抑制剂的4-氨基喹啉-3-羧酰胺衍生物
公开(公告)号：WO2005030212A1
公开(公告)日：2005-04-07
申请号：PCT/EP2004/010844
申请日：2004-09-23
申请人： GLAXO GROUP LIMITED , EDLIN, Christopher, D , ELDRED, Colin, David , KEELING, Steven, Philip , LUNNISS, Christopher, James , REDFERN, Tracy, Jane , REDGRAVE, Alison, Judith , WOODROW, Michael
发明人： EDLIN, Christopher, D , ELDRED, Colin, David , KEELING, Steven, Philip , LUNNISS, Christopher, James , REDFERN, Tracy, Jane , REDGRAVE, Alison, Judith , WOODROW, Michael
IPC分类号： A61K31/4706
CPC分类号： C07D215/54 , C04B35/632 , C07D401/12 , C07D405/12 , C07D405/14
摘要： Compounds of formula (I) or pharmaceutically acceptable salts thereof: (I) are inhibitors of phosphodiesterase type IV (PDE4) and are of use in the treatment of inflammatory and/or allergic diseases.
摘要翻译：式（I）化合物或其药学上可接受的盐：（I）是IV型磷酸二酯酶（PDE4）的抑制剂，可用于治疗炎性和/或过敏性疾病。

2. 发明申请

WO2004103998A1 QUINOLINE DERIVATIVES AS PHOSPHODIESTERASE INHIBITORS 审中-公开
标题翻译：喹啉衍生物作为磷酸二酯酶抑制剂
公开(公告)号：WO2004103998A1
公开(公告)日：2004-12-02
申请号：PCT/EP2004/005494
申请日：2004-05-19
申请人： GLAXO GROUP LIMITED , BALDWIN, Ian, Robert , BARKER, Michael, David , DEAN, Anthony, William , ELDRED, Colin, David , EVANS, Brian , GOUGH, Sharon, Lisa , GUNTRIP, Stephen, Barry , HAMBLIN, Julie, Nicole , HOLMAN, Stuart , JONES, Paul , LINDVALL, Mika, Kristian , LUNNISS, Christopher, James , REDFERN, Tracy, Jane , REDGRAVE, Alison, Judith , ROBINSON, John, Edward , WOODROW, Michael
发明人： BALDWIN, Ian, Robert , BARKER, Michael, David , DEAN, Anthony, William , ELDRED, Colin, David , EVANS, Brian , GOUGH, Sharon, Lisa , GUNTRIP, Stephen, Barry , HAMBLIN, Julie, Nicole , HOLMAN, Stuart , JONES, Paul , LINDVALL, Mika, Kristian , LUNNISS, Christopher, James , REDFERN, Tracy, Jane , REDGRAVE, Alison, Judith , ROBINSON, John, Edward , WOODROW, Michael
IPC分类号： C07D417/12
CPC分类号： C07D401/12 , C07D215/54 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D453/02
摘要： There are provided according to the invention novel compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R19, R20 and R34 are as described in the specification, processes for preparing them, formulations containing them and their use in therapy for the treatment of inflammatory diseases.
摘要翻译：根据本发明提供新的式（I）化合物或其药学上可接受的盐，其中R1，R2，R19，R20和R34如说明书中所述，其制备方法，含有它们的制剂及其在治疗中的用途用于治疗炎性疾病。

3. 发明申请

WO2005030725A1 DERIVATIVES OF 3-AMINOCARBONYLQUINOLINE, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND PROCESSES AND INTERMEDIATES FOR THEIR PREPARATION 审中-公开
标题翻译： 3-氨基羰基喹啉衍生物，含有它们的药物组合物及其制备方法及其制备中间体
公开(公告)号：WO2005030725A1
公开(公告)日：2005-04-07
申请号：PCT/GB2004/004106
申请日：2004-09-27
申请人： GLAXO GROUP LIMITED , EDLIN, Christopher , ELDRED, Colin, David , LUNNISS, Christopher, James , REDGRAVE, Alison, Judith , ROBINSON, John, Edward , WOODROW, Michael
发明人： EDLIN, Christopher , ELDRED, Colin, David , LUNNISS, Christopher, James , REDGRAVE, Alison, Judith , ROBINSON, John, Edward , WOODROW, Michael
IPC分类号： C07D215/44
CPC分类号： C04B35/632 , C07D215/44 , C07D401/12 , C07D405/12 , C07D411/12 , C07D417/12
摘要： Compounds of formula (I) or pharmaceutically acceptable salts thereof are inhibitors of phosphodiesterase type IV (PDE4) and are of use in the treatment of inflammatory and/or allergic diseases.
摘要翻译：式（I）化合物或其药学上可接受的盐是IV型磷酸二酯酶（PDE4）的抑制剂，并且可用于治疗炎性和/或过敏性疾病。

4. 发明申请

WO2003035237A2 COMPOUNDS FOR USE AS SURFACTANTS 审中-公开
标题翻译：用作表面活性剂的化合物
公开(公告)号：WO2003035237A2
公开(公告)日：2003-05-01
申请号：PCT/EP2002/011635
申请日：2002-10-17
申请人： GLAXO GROUP LIMITED , LOOKER, Brian, Edgar , LUNNISS, Christopher, James , REDGRAVE, Alison, Judith
发明人： LOOKER, Brian, Edgar , LUNNISS, Christopher, James , REDGRAVE, Alison, Judith
IPC分类号： B01F17/00
CPC分类号： A61K9/008 , B01F17/0028 , B01F17/0035
摘要： There are provided according to the invention compounds of formula (I) or salts or solvate thereof, wherein:n and N independently represent an integer 2 to 12;m1 and m2 independently represent an integer 1 to 15; and R1 and R2 independently represent -(CO)xC1-9 alkyl or -(CO)xC1-9 fluoroalkyl, which fluoroalkyl moiety contains at least 1 fluorine atom and not more than 3 consecutive perfluorocarbon atoms wherein x represents 0 or 1. The invention includes uses of said compounds and processes for their preparation.
摘要翻译：根据本发明提供了式（I）的化合物或其盐或溶剂合物，其中：n和N独立地表示2至12的整数; m 1和m 2独立地表示1至15的整数 ; 并且R 1和R 2独立地表示 - （CO）x C 1-9烷基或 - （CO）x C 1-9氟代烷基，其中氟代烷基部分含有至少1个氟原子和不多于3个连续的全氟化碳原子，其中x代表0或1。包括所述化合物的用途及其制备方法。

5. 发明申请

WO2003013610A3 SURFACTANT COMPOUNDS AND USES THEREOF 审中-公开
公开(公告)号：WO2003013610A3
公开(公告)日：2003-02-20
申请号：PCT/GB2002/003586
申请日：2002-08-02
申请人： GLAXO GROUP LIMITED , KALDOR, Istvan , LOOKER, Brian, Edgar , LUNNISS, Christopher, James , REDGRAVE, Alison, Judith
发明人： KALDOR, Istvan , LOOKER, Brian, Edgar , LUNNISS, Christopher, James , REDGRAVE, Alison, Judith
IPC分类号： A61K9/12
摘要： A pharmaceutical aerosol formulation comprising a particulate medicament, one or more fluorocarbon or hydrogen-containing fluorocarbon propellants and a compound of the general formula (I) or a salt or solvate thereof, wherein A represents a straight chain C 1 - 16 alkylene substituted by n groups of formula B; n represents an integer 1 to 3; and B independently represents C 1 - 4 fluoroalkylC 0 - 6 alkylene-, C 1 - 4 fluoroalkylC 0 - 6 alkylene-O-, or C 1 - 4 alkylC 0 - 6 alkylene-O- wherein at least one substituent of formula B contains at least one fluorine atom and each C 1 - 4 fluoroalkyl- moiety contains one or more fluorine atoms but not more than 3 consecutive perfluorinated carbon atoms. The invention also extends to uses of compounds of formula (I) and certain novel compounds within the definition of formula (I).

6. 发明申请

WO2002024623A3 NOVEL ALKANOIC ACID DERIVATIVES 审中-公开
公开(公告)号：WO2002024623A3
公开(公告)日：2002-03-28
申请号：PCT/GB2001/004226
申请日：2001-09-21
申请人： GLAXO GROUP LIMITED , LOOKER, Brian, Edgar , REDGRAVE, Alison, Judith , LUNNISS, Christopher, James , REYNOLDS, Derek, Peter
发明人： LOOKER, Brian, Edgar , REDGRAVE, Alison, Judith , LUNNISS, Christopher, James , REYNOLDS, Derek, Peter
IPC分类号： C07C51/09
摘要： There are provided according to the invention compounds of the formula (I) or a salt or solvate thereof, wherein: n represents an integer 1 to 6; N represents an integer 1 to 15; R 1 represents (CO) x C 1-9 alkyl or (CO) x C 1-9 fluoroalkyl, which fluoroalkyl moiety contains at least 1 fluorine atom and not more than 3 consecutive perfluorocarbon atoms wherein x represents 0 or 1; and R 2 and R 3 independently represent C 1-3 alkyl or hydrogen. There are also provided pharmaceutical aerosol formulations employing said compounds as suspension stabilising agents.

7. 发明申请

WO2003074537A1 COMPOUNDS FOR USE AS SURFACTANTS 审中-公开
标题翻译：用作表面活性剂的化合物
公开(公告)号：WO2003074537A1
公开(公告)日：2003-09-12
申请号：PCT/GB2003/000876
申请日：2003-03-04
申请人： GLAXO GROUP LIMITED , LOOKER, Brian, Edgar , LUNNISS, Christopher, James , REDGRAVE, Alison, Judith
发明人： LOOKER, Brian, Edgar , LUNNISS, Christopher, James , REDGRAVE, Alison, Judith
IPC分类号： C07F9/10
CPC分类号： A61K9/008 , C07F9/10
摘要： There are provided according to the invention compounds of formula (I)or a salt or solvate thereof wherein: m, n, p and q independently represent an integer 1 to 12; R 1a , R 1b and R 1c independently represent C 1-3 alkyl or hydrogen; R 2 and R 3 independently represent C 1-4 alkyl optionally substituted with up to 5 fluorine atoms or -COC 1-2 alkyl optionally substituted with up to 5 fluorine atoms; R 4 and R 5 independently represent -CH 3 or hydrogen. X 1 and X 2 independently represent -(CH 2 ) 2 -, -(CH 2 ) 3 -, -CH(CH 3 )CH 2 -, -CH 2 CH(CH 3 )-, -CH(CH 3 )CH 2 CH 2 , -CH 2 CH(CH 3 )CH 2 -, CH 2 CH 2 CH(CH 3 ) or -COCH(CH 3 )-; and Y 1 and Y 2 independently represent -CH 2 - or carbonyl; with the proviso that when: p and q represent 1; m and n independently represent an integer between 1 to 12; R 4 and R 5 represent hydrogen; X 1 and X 2 represent -(CH 2 ) 2 -; and Y 1 and Y 2 represent -CH 2 -; then R 2 and R 3 may only represent C 1-2 alkyl optionally substituted with up to 5 fluorine atoms or -COC 1-2 alkyl optionally substituted with up to 5 fluorine atoms.
摘要翻译：根据本发明提供式（I）化合物或其盐或溶剂化物，其中：m，n，p和q独立地表示1至12的整数; R1a，R1b和R1c独立地表示C1-3烷基或氢; R2和R3独立地表示任选被至多5个氟原子取代的C 1-4烷基或任选被至多5个氟原子取代的-COC1-2烷基; R4和R5独立地表示-CH3或氢。 X1和X2独立地表示 - （CH2）2-， - （CH2）3-，-CH（CH3）CH2-，-CH2CH（CH3） - ， - CH（CH3）CH2CH2，-CH2CH（CH3）CH2-，CH2CH2CH （CH 3）或-COCH（CH 3） - ; Y 1和Y 2独立地表示-CH 2 - 或羰基; 条件是当：p和q表示1; m和n独立地表示1〜12的整数， R4和R5代表氢; X1和X2表示 - （CH2）2-; Y1和Y2表示-CH2-; 那么R 2和R 3可以仅表示任选被至多5个氟原子取代的C 1-2烷基或任选被至多5个氟原子取代的-COC1-2烷基。

8. 发明申请

WO2003013610A2 SURFACTANT COMPOUNDS AND USES THEREOF 审中-公开
标题翻译：表面活性剂化合物及其用途
公开(公告)号：WO2003013610A2
公开(公告)日：2003-02-20
申请号：PCT/GB2002/003586
申请日：2002-08-02
申请人： GLAXO GROUP LIMITED , KALDOR, Istvan , LOOKER, Brian, Edgar , LUNNISS, Christopher, James , REDGRAVE, Alison, Judith
发明人： KALDOR, Istvan , LOOKER, Brian, Edgar , LUNNISS, Christopher, James , REDGRAVE, Alison, Judith
IPC分类号： A61K47/00
CPC分类号： A61K9/008 , A61K31/137 , A61K31/56 , A61K47/12 , C07C59/135 , C07C69/63 , C07C69/708 , C09K3/30
摘要： A pharmaceutical aerosol formulation comprising a particulate medicament, one or more fluorocarbon or hydrogen-containing fluorocarbon propellants and a compound of the general formula (I) or a salt or solvate thereof, wherein A represents a straight chain C 1 - 16 alkylene substituted by n groups of formula B; n represents an integer 1 to 3; and B independently represents C 1 - 4 fluoroalkylC 0 - 6 alkylene-, C 1 - 4 fluoroalkylC 0 - 6 alkylene-O-, or C 1 - 4 alkylC 0 - 6 alkylene-O- wherein at least one substituent of formula B contains at least one fluorine atom and each C 1 - 4 fluoroalkyl- moiety contains one or more fluorine atoms but not more than 3 consecutive perfluorinated carbon atoms. The invention also extends to uses of compounds of formula (I) and certain novel compounds within the definition of formula (I).
摘要翻译：包含微粒药物，一种或多种氟碳或含氢氟碳推进剂和通式（I）的化合物或其盐或溶剂化物的药物气雾剂制剂，其中A表示直链被式B的n个基团取代的C 1 -C 16 - 亚烷基; n表示1至3的整数; 和B独立地代表C 1 -C 4 - 氟代烷基C 0 -C 6亚烷基 - ，C 1 -C 1 - 低级烷氧基，低级烷氧基低级烷氧基，低级烷氧基低级烷氧基低级烷氧基，其中至少一个式B的取代基含有至少一个氟原子，并且每个C 1〜C 6亚烷基具有至少一个氟原子， - 氟代烷基 - 部分含有一个或多个氟原子但不超过3个连续的全氟化碳原子。本发明还扩展至式（I）化合物和式（I）定义内的某些新化合物的用途。

9. 发明申请

WO2003011874A1 COMPOUNDS FOR USE AS SURFACTANTS 审中-公开
标题翻译：用作表面活性剂的化合物
公开(公告)号：WO2003011874A1
公开(公告)日：2003-02-13
申请号：PCT/GB2002/003375
申请日：2002-07-24
申请人： GLAXO GROUP LIMITED , LOOKER, Brian, Edgar , LUNNISS, Christopher, James , REDGRAVE, Alison, Judith
发明人： LOOKER, Brian, Edgar , LUNNISS, Christopher, James , REDGRAVE, Alison, Judith
IPC分类号： C07F9/10
CPC分类号： A61K9/008 , A61K47/24 , C07C69/63 , C07F9/10 , C07F9/14
摘要： A compound of formula (I) or a salt thereof, wherein: R 1a represents C l-3 alkyl; R 1b represents C 1-3 alkyl; R 1c represents C 1-3 alkyl; R 2 represents C 1-5 fluoroalkyl; R 3 represents C 1-5 fluoroalkyl; X represents -C 1-6 alkylene-; Y represents -C 1-6 alkylene-; with the proviso the each C 1-5 fluoroalkyl contains 3 or fewer consecutive perfluorocarbon atoms, methods of preparing said compounds, pharmaceutical aerosol formulation comprising said compounds and uses thereof.
摘要翻译：式（I）化合物或其盐，其中：R 1a表示C 1-3烷基; R 1b表示C 1-3烷基; R 1c表示C 1-3烷基; R 2表示C 1-5氟烷基; R 3表示C 1-5氟烷基; X表示-C 1-6亚烷基 - ; Y表示-C 1-6亚烷基; 条件是每个C 1-5氟代烷基含有3个或更少的连续的全氟化碳原子，制备所述化合物的方法，包含所述化合物的药物气溶胶制剂及其用途。

10. 发明申请

WO2005090354A1 PYRAZOLO[3,4-b] PYRIDINE COMPOUNDS, AND THEIR USE AS PDE4 INHIBITORS 审中-公开
标题翻译：吡咯并[3,4-b]吡啶化合物，并且作为PDE4抑制剂使用
公开(公告)号：WO2005090354A1
公开(公告)日：2005-09-29
申请号：PCT/GB2005/000987
申请日：2005-03-15
申请人： GLAXO GROUP LIMITED , COOK, Caroline, Mary , DOWLE, Michael, Dennis , EDLIN, Christopher, David , JOHNSON, Martin, Redpath , JONES, Paul, Spencer , LINDVALL, Mika, Kristian , TRIVEDI, Naimisha , REDGRAVE, Alison, Judith
发明人： COOK, Caroline, Mary , DOWLE, Michael, Dennis , EDLIN, Christopher, David , JOHNSON, Martin, Redpath , JONES, Paul, Spencer , LINDVALL, Mika, Kristian , TRIVEDI, Naimisha , REDGRAVE, Alison, Judith
IPC分类号： C07D487/04
CPC分类号： C07D471/04
摘要： The invention provides a compound of formula (I) or a salt thereof: formula (I) wherein: R 1 is C 1-3 alkyl, C 1-3 fluoroalkyl, or -CH 2 CH 2 OH; R 2 is a hydrogen atom (H), methyl or C 1 fluoroalkyl; R 3 is of sub-formula (aa) or (bb): formulae (aa), (bb) wherein Y is NCONH 2 and n 1 is 0 or 1; R 4 is H; and R 5 is a group of the sub-formula (x), (y), (y1) or (z): formulae (x), (y), (y1), (z). The invention also relates to the use of these compounds or salts in therapy as inhibitors of phosphodiesterase type IV (PDE4). For example, it relates to their use in the treatment and/or prophylaxis of inflammatory and/or allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rheumatoid arthritis, allergic rhinitis, psoriasis or atopic dermatitis in a mammal such as a human.
摘要翻译：本发明提供式（I）化合物或其盐：式（I）其中：R 1为C 1-3烷基，C 1-3氟烷基或-CH 2 CH 2 OH; R 2是氢原子（H），甲基或C 1-6烷基; （aa）或（bb）：式（aa），（bb）其中Y为NCONH2且n为0或1; R 4是H; 并且R 5是式（x），（y），（y1）或（z）的子集：式（x），（y），（y1），（z）。本发明还涉及这些化合物或盐在治疗中作为IV型磷酸二酯酶抑制剂（PDE4）的用途。例如，它涉及其用于治疗和/或预防哺乳动物例如慢性阻塞性肺疾病（COPD），哮喘，类风湿性关节炎，过敏性鼻炎，牛皮癣或特应性皮炎的炎性和/或过敏性疾病人类。

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