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1. 发明申请

WO2004016578A3 ARYLETHANOLAMINE BETA2-ADRENORECEPTOR AGONIST COMPOUNDS 审中-公开
标题翻译：氨基乙酰胺BETA2-腺苷二磷酸激动剂化合物
公开(公告)号：WO2004016578A3
公开(公告)日：2004-06-10
申请号：PCT/EP0308264
申请日：2003-07-24
申请人： GLAXO GROUP LTD , BIGGADIKE KEITH , COE DIANE MARY , HOLMES DUNCAN STUART , LOOKER BRIAN EDGAR
发明人： BIGGADIKE KEITH , COE DIANE MARY , HOLMES DUNCAN STUART , LOOKER BRIAN EDGAR
IPC分类号： C07D215/24 , A61K31/18 , A61K31/428 , A61K31/44 , A61K31/4704 , A61K31/538 , A61P11/00 , A61P11/06 , A61P11/08 , A61P25/02 , C07C303/40 , C07C311/29 , C07C311/37 , C07D213/65 , C07D215/26 , C07D265/36 , C07D277/68 , C07C217/10 , C07C213/00
CPC分类号： C07D277/68 , C07C311/29 , C07D213/65 , C07D215/26 , C07D265/36
摘要： The present invention concerns compounds of formula (I) and salts, solvates, and physiologically functional derivatives thereof, wherein: R is hydrogen or -XSO2NR R ; R and R are independently selected from hydrogen, C1-6 alkyl, C1-6 alkoxy, halo, phenyl and C1-6 haloalkyl and Ar is a group selected from and. Processes for preparing said compounds and pharmaceutical formulations containing them are also described. Compounds of formula (I) are useful in the treatment of respiratory diseases
摘要翻译：本发明涉及式（I）化合物及其盐，溶剂化物和生理功能衍生物，其中：R 1是氢或-XSO 2 NR 6 R 7; R 2和R 3独立地选自氢，C 1-6烷基，C 1-6烷氧基，卤素，苯基和C 1-6卤代烷基，Ar是选自和。还描述了制备所述化合物的方法和含有它们的药物制剂。式（I）化合物可用于治疗呼吸系统疾病

2. 发明申请

WO0224623A2 NOVEL ALKANOIC ACID DERIVATIVES 审中-公开
标题翻译：新型酸性衍生物
公开(公告)号：WO0224623A2
公开(公告)日：2002-03-28
申请号：PCT/GB0104226
申请日：2001-09-21
申请人： GLAXO GROUP LTD , 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： A61K9/12 , A61K47/06 , A61K47/32 , A61P11/00 , C07C51/09 , C07C51/367 , C07C59/125 , C07C59/135 , C07C69/708 , C07C31/18 , C07C31/42 , C07C67/333 , C07C69/34
CPC分类号： C07C69/708 , C07C51/09 , C07C59/125 , C07C59/135 , Y10S514/958
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 represents (CO)xC1-9alkyl or (CO)xC1-9fluoroalkyl, 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 and R independently represent C1-3alkyl or hydrogen. There are also provided pharmaceutical aerosol formulations employing said compounds as suspension stabilising agents.
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：n表示1至6的整数; N表示1〜15的整数， R 1表示（CO）x C 1-9烷基或（CO）x C 1-9氟烷基，该氟烷基部分含有至少1个氟原子和不多于3个连续的全氟化碳原子，其中x表示0或1; R 2和R 3独立地表示C 1-3烷基或氢。还提供了使用所述化合物作为悬浮稳定剂的药物气溶胶制剂。

3. 发明申请

WO2009047336A1 PHTHALAZINE AND PYRIDO [3,4-D] PYRIDAZ INE COMPOUNDS AS H1 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：苯丙氨酸和吡咯并[3,4-D]吡嗪类化合物作为H1受体拮抗剂
公开(公告)号：WO2009047336A1
公开(公告)日：2009-04-16
申请号：PCT/EP2008/063642
申请日：2008-10-10
申请人： GLAXO GROUP LIMITED , GORE, Paul, Martin , LOOKER, Brian, Edgar , PROCOPIOU, Panayiotis, Alexandrou , VILE, Sadie
发明人： GORE, Paul, Martin , LOOKER, Brian, Edgar , PROCOPIOU, Panayiotis, Alexandrou , VILE, Sadie
IPC分类号： C07D403/06 , C07D471/04 , A61K31/502 , A61K31/5025 , A61P29/00 , A61P37/08
CPC分类号： C07D403/06 , C07D471/04
摘要： The present invention relates to compounds of formula (I), and salts thereof, processes for their preparation, to compositions containing them and to their use in the treatment of various diseases, such as allergic rhinitis.
摘要翻译：本发明涉及式（I）化合物及其盐，其制备方法，含有它们的组合物及其在治疗各种疾病如过敏性鼻炎中的用途。

4. 发明申请

WO2008074803A3 4-BENZYL-L ( 2H) -PHTHALAZINONES AS HL RECEPTOR ANTAGONISTS 审中-公开
标题翻译： 4-BENZYL-L（2H）-PHTHALAZINONES作为HL受体拮抗剂
公开(公告)号：WO2008074803A3
公开(公告)日：2008-09-18
申请号：PCT/EP2007064140
申请日：2007-12-18
申请人： GLAXO GROUP LTD , GORE PAUL MARTIN , KRANZ MICHAEL JOACHIM , LOOKER BRIAN EDGAR , VILE SADIE
发明人： GORE PAUL MARTIN , KRANZ MICHAEL JOACHIM , LOOKER BRIAN EDGAR , VILE SADIE
IPC分类号： A61K31/502 , A61K31/5025 , A61P29/00 , A61P37/08 , C07D237/32 , C07D471/04
CPC分类号： C07D471/04 , C07D237/32
摘要： The present invention relates to compounds of formula (I) and salts thereof, processes for their preparation, to compositions containing them and to their use in the treatment of various diseases, such as allergic rhinitis.
摘要翻译：本发明涉及式（I）化合物及其盐，其制备方法，含有它们的组合物及其在治疗各种疾病如过敏性鼻炎中的用途。

5. 发明申请

WO2004071388A3 MEDICINAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2004071388A3
公开(公告)日：2005-01-06
申请号：PCT/EP2004001415
申请日：2004-02-12
申请人： GLAXO GROUP LTD , BIGGADIKE KEITH , BOX PHILIP CHARLES , COE DIANE MARY , HOLMES DUNCAN STUART , LOOKER BRIAN EDGAR , PROCOPIOU PANAYIOTIS ALEXANDRO
发明人： BIGGADIKE KEITH , BOX PHILIP CHARLES , COE DIANE MARY , HOLMES DUNCAN STUART , LOOKER BRIAN EDGAR , PROCOPIOU PANAYIOTIS ALEXANDRO
IPC分类号： A61K20060101 , A61K31/136 , A61K31/167 , A61K31/18 , A61K31/44 , A61P11/06 , C07C217/08 , C07C217/28 , C07C233/43 , C07C311/13 , C07D213/65
CPC分类号： C07D213/65 , C07C217/28
摘要： A compound of formula (I) or a salt, solvate, or physiologically functional derivative thereof, wherein: m is an integer of from 2 to 8; n is an integer of from 2 to 5; with the proviso that m + n is 4 to 10; R and R are independently selected from hydrogen and C1-4 alkyl with the proviso that the total number of carbon atoms in R and R is not more than 4; R and R are independently selected from hydrogen and C1-4alkyl with the proviso that the total number of carbon atoms in R and R is not more than 4, and Ar is a group selected from (a), (b), (c) and (d).
摘要翻译：式（I）化合物或其盐，溶剂合物或生理功能衍生物，其中：m为2至8的整数; n为2〜5的整数，条件是m + n为4至10; R 4和R 5独立地选自氢和C 1-4烷基，条件是R 4和R 5中的碳原子总数不大于4; R 6和R 7独立地选自氢和C 1-4烷基，条件是R 6和R 7中的碳原子总数不大于4，Ar 1是选自（a），（b），（c）和（d）的基团。

6. 发明申请

WO2004071388A2 MEDICINAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2004071388A2
公开(公告)日：2004-08-26
申请号：PCT/EP2004/001415
申请日：2004-02-12
申请人： GLAXO GROUP LIMITED , BIGGADIKE, Keith , BOX, Philip, Charles , COE, Diane, Mary , HOLMES, Duncan, Stuart , LOOKER, Brian, Edgar , PROCOPIOU, Panayiotis, Alexandrou
发明人： BIGGADIKE, Keith , BOX, Philip, Charles , COE, Diane, Mary , HOLMES, Duncan, Stuart , LOOKER, Brian, Edgar , PROCOPIOU, Panayiotis, Alexandrou
IPC分类号： A61K
CPC分类号： C07D213/65 , C07C217/28
摘要： A compound of formula (I) or a salt, solvate, or physiologically functional derivative thereof, wherein: m is an integer of from 2 to 8; n is an integer of from 2 to 5; with the proviso that m + n is 4 to 10; R 4 and R 5 are independently selected from hydrogen and C 1-4 alkyl with the proviso that the total number of carbon atoms in R 4 and R 5 is not more than 4; R 6 and R 7 are independently selected from hydrogen and C 1-4 alkyl with the proviso that the total number of carbon atoms in R 6 and R 7 is not more than 4, and Ar 1 is a group selected from (a), (b), (c) and (d).
摘要翻译：式（I）化合物或其盐，溶剂合物或生理功能衍生物，其中：m为2至8的整数; n为2〜5的整数，条件是m + n为4至10; R 4和R 5独立地选自氢和C 1-4烷基，条件是R 4和R 5中的碳原子总数不大于4; R 6和R 7独立地选自氢和C 1-4烷基，条件是R 6和R 7中的碳原子总数不大于4，Ar 1是选自（a），（b），（c）和（d）的基团。

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

WO03035237A3 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：WO03035237A3
公开(公告)日：2003-08-14
申请号：PCT/EP0211635
申请日：2002-10-17
申请人： GLAXO GROUP LTD , 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： A61K9/12 , A61K9/00 , A61K9/72 , A61K31/137 , A61K31/439 , A61K31/522 , A61K31/56 , A61K31/573 , A61K31/58 , A61K47/06 , A61K47/12 , A61K47/34 , A61P11/02 , A61P11/06 , A61P11/08 , A61P29/00 , A61P37/08 , B01F17/00 , C07C59/125 , C07C59/185
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）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; m1和m2独立地表示1至15的整数; 并且R 1和R 2独立地表示 - （CO）xC1-9烷基或 - （CO）xC1-9氟代烷基，该氟烷基部分含有至少1个氟原子和不超过3个连续的全氟化碳原子，其中x表示0或1.本发明包括所述化合物的用途及其制备方法。

9. 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。

10. 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。

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