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1. 发明申请

WO2007093578A1 BENZOISOINDOLE DERIVATIVES AND THEIR USE AS EP4 RECEPTOR LIGANDS 审中-公开
标题翻译：苯并噻唑衍生物及其作为EP4受体配体使用
公开(公告)号：WO2007093578A1
公开(公告)日：2007-08-23
申请号：PCT/EP2007/051348
申请日：2007-02-12
申请人： GLAXO GROUP LIMITED , HEALY, Mark Patrick , GIBLIN, Gerard, Martin, Paul , MILLER, Neil Derek
发明人： HEALY, Mark Patrick , GIBLIN, Gerard, Martin, Paul , MILLER, Neil Derek
IPC分类号： C07D209/64 , C07D209/66 , A61K31/4035
CPC分类号： C07D209/66 , C07D209/64
摘要： A compound of formula (I) or a pharmaceutically acceptable derivative thereof, wherein, R 1 to R 8 , X and Y are as defined in the specification; a process for preparing such compounds; a pharmaceutical composition comprising such compounds; and the use of such compounds in medicine.
摘要翻译：式（I）化合物或其药学上可接受的衍生物，其中R 1至R 8，X和Y如说明书中所定义; 制备这种化合物的方法; 包含这些化合物的药物组合物; 并在药物中使用这些化合物。

2. 发明申请

WO2005054191A1 PYRROLE COMPOUNDS 审中-公开
标题翻译：吡咯化合物
公开(公告)号：WO2005054191A1
公开(公告)日：2005-06-16
申请号：PCT/EP2004/013744
申请日：2004-11-30
申请人： GLAXO GROUP LIMITED , GIBLIN, Gerard, Martin, Paul , HALL, Adrian , HEALY, Mark, Patrick , LEWELL, Xiao, Qing , MILLER, Neil, Derek , NOVELLI, Riccardo , KING, Francis, David , NAYLOR, Alan
发明人： GIBLIN, Gerard, Martin, Paul , HALL, Adrian , HEALY, Mark, Patrick , LEWELL, Xiao, Qing , MILLER, Neil, Derek , NOVELLI, Riccardo , KING, Francis, David , NAYLOR, Alan
IPC分类号： C07D207/32
CPC分类号： C07D207/333 , C07D401/04
摘要： Compounds of formula (I) or a derivative thereof: wherein A, B, Z, R1, R2a, R2b, Rx, R8, and R9 are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.
摘要翻译：式（I）化合物或其衍生物：其中A，B，Z，R 1，R 2a，R 2b，R x，R 8和R 9如本说明书中所定义，制备这些化合物的方法，化合物和这些化合物在医药中的应用。

3. 发明申请

WO2003101959A1 PYRROLE COMPOUNDS FOR THE TREATMENT OF PROSTAGLANDIN MEDIATED DISEASES 审中-公开
标题翻译：用于治疗PROSTAGLANDIN介导的疾病的吡咯类化合物
公开(公告)号：WO2003101959A1
公开(公告)日：2003-12-11
申请号：PCT/EP2003/005790
申请日：2003-05-30
申请人： GLAXO GROUP LIMITED , GIBLIN, Gerard, Martin, Paul , HALL, Adrian , HEALY, Mark, Patrick , LEWELL, Xiao, Qing , MILLER, Neil, Derek , NOVELLI, Riccardo
发明人： GIBLIN, Gerard, Martin, Paul , HALL, Adrian , HEALY, Mark, Patrick , LEWELL, Xiao, Qing , MILLER, Neil, Derek , NOVELLI, Riccardo
IPC分类号： C07D207/32
CPC分类号： C07D207/333 , C07D401/04 , C07D401/10 , C07D401/12 , C07D403/04 , C07D403/10 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/10 , C07D413/12 , C07D417/10
摘要： Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein A, R 1 , R 2a , R 2b , R x , R 8 , and R 9 are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine, in particular their use in the treatment of prostaglandin mediated diseases such as pain, inflammatory, immunological, bone, neurodegenerative or renal disorder.
摘要翻译：式（I）化合物或其药学上可接受的衍生物：其中A，R 1，R 2a，R 2b，R x，R 8和R 9如说明书，制备这些化合物的方法，包含这些化合物的药物组合物和这些化合物在医药中的用途，特别是它们在治疗前列腺素介导的疾病如疼痛，炎症，免疫学，骨骼，神经变性或肾脏中的用途紊乱。

4. 发明申请

WO2004083185A2 IMIDAZOLE COMPOUNDS 审中-公开
标题翻译：苯基取代的咪唑衍生物
公开(公告)号：WO2004083185A2
公开(公告)日：2004-09-30
申请号：PCT/EP2004/002831
申请日：2004-03-17
申请人： GLAXO GROUP LIMITED , GIBLIN, Gerard, Martin, Paul , HALL, Adrian , LEWELL, Xiao, Qing , MILLER, Neil, Derek
发明人： GIBLIN, Gerard, Martin, Paul , HALL, Adrian , LEWELL, Xiao, Qing , MILLER, Neil, Derek
IPC分类号： C07D233/54
CPC分类号： C07D233/64
摘要： Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein A, B, Z, R1, R2a, R2b, Rx, R8, R9, Q, and T are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.
摘要翻译：式（I）化合物或其药学上可接受的衍生物：其中A，B，Z，R1，R2a，R2b，Rx，R8，R9，Q和T如说明书中所定义，化合物，包含这些化合物的药物组合物以及这些化合物在医药中的用途。

5. 发明申请

WO2007039219A1 QUINOLINE COMPOUNDS CAPABLE OF BINDING THE CB2 AND/OR THE 5-HT6 RECEPTOR 审中-公开
标题翻译：可结合CB2和/或5-HT6受体的喹啉化合物
公开(公告)号：WO2007039219A1
公开(公告)日：2007-04-12
申请号：PCT/EP2006/009416
申请日：2006-09-26
申请人： GLAXO GROUP LIMITED , AHMED, Mahmood , GIBLIN, Gerard, Martin, Paul , JOHNSON, Christopher, Norbert , LIVERMORE, David, George, Hubert , MILLER, Neil, Derek , MOSS, Stephen, Frederick , WITTY, David, R
发明人： AHMED, Mahmood , GIBLIN, Gerard, Martin, Paul , JOHNSON, Christopher, Norbert , LIVERMORE, David, George, Hubert , MILLER, Neil, Derek , MOSS, Stephen, Frederick , WITTY, David, R
IPC分类号： C07D401/06 , C07D215/36 , C07D491/10 , A61K31/4709 , A61P25/00
CPC分类号： C07D491/10 , C07D215/36 , C07D401/06
摘要： The present invention relates to novel quinoline derivatives such as compounds of the formula (I) which possess antagonist potency for the 5-HT 6 receptor and/or are capable of selectively modulating the cannabinoid 2 receptor and the use of such compounds or pharmaceutical compositions thereof in the treatment of CNS disorders.
摘要翻译：本发明涉及新颖的喹啉衍生物，例如式（I）化合物，其具有5-HT 6受体的拮抗剂效能和/或能够选择性调节大麻素2受体和使用的这些化合物或其药物组合物用于治疗CNS障碍。

6. 发明申请

WO2002064564A1 BENZO'F!ISOINDOLE DERIVATIVES WITH AFFINITY TO THE EP4 RECEPTOR 审中-公开
标题翻译： BENZO'F！具有对EP4受体的亲和力的ISOINDOLE衍生物
公开(公告)号：WO2002064564A1
公开(公告)日：2002-08-22
申请号：PCT/GB2002/000522
申请日：2002-02-07
申请人： GLAXO GROUP LIMITED , CONGREVE, Miles, Stuart , GIBLIN, Gerard, Martin, Paul , MASON, Andrew, McMurtrie , MILLER, Neil, Derek , ROOMANS, Susan , WALKER, Ann, Louise
发明人： CONGREVE, Miles, Stuart , GIBLIN, Gerard, Martin, Paul , MASON, Andrew, McMurtrie , MILLER, Neil, Derek , ROOMANS, Susan , WALKER, Ann, Louise
IPC分类号： C07D209/64
CPC分类号： C07D209/66 , C07D209/64
摘要： A compound of formula (I) wherein R 1 and R 3 are the same or different and represent =O, hydrogen, C 1-6 alkyl, C 1-6 dialkyl, =CHC 1 -C 5 alkyl, =S, or a 5- or 6-membered anyl; R 4 to R 9 are the same or different and represent hydrogen, C 1-6 alkoxy, OCF 3 , OCH 2 CF 3 , O-cyclopropyl, OCH 2 -cyclopropyl, C 1 -C 6 alkyl, S-alkyl, NR 2 10¿ where R 10 is hydrogen or C 1-6 alkyl, halogen, NO 2 , OH, CH 2 OC 1 -C 6 alkly, CH 2 OH, or CF 3 ; Q 1 is hydrogen, C 1-6 alkyl, C 1-6 dialkyl, C 1-6 alkoxy, NHAc, NR 2 10¿ where R 10 is hydrogen is hydrogen or C 1-6 alkyl, difluoro, fluoro, =O, or OH; Q 2 , Q 3 , Q 4 and Q 5 are the same or different and represent hydrogen, C 1-6 alkoxy, OCF 3 , OCH 2 CF 3 , O-cyclopropyl, OCH 2 -cyclopropyl, C 1 -C 6 alkyl, S-alkyl, NR 2 10¿ where R 10 is hydrogen or C 1-6 alkyl, halogen, NO 2 , OH, CH 2 OC 1 -C 6 alkyl, CH 2 OH, or a 5-or 6-membered aryl; with the proviso that the compounds [4-(1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl)phenyl]-2-propionic acid, sodium salt and [4-(4,9-diethoxy-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl)phenyl]acetic acid are excluded; and pharmaceutically acceptable derivatives thereof.
摘要翻译：式（I）化合物，其中R 1和R 3相同或不同，表示= O，氢，C 1-6烷基，C 1-6二烷基，= CHCl-C 5烷基，= S或5-或 6元芳基; R 4至R 9相同或不同，表示氢，C 1-6烷氧基，OCF 3，OCH 2 CF 3，O-环丙基，OCH 2 - 环丙基，C 1 -C 6烷基，S-烷基，NR 2 10，其中R 10为氢或C1- 6烷基，卤素，NO 2，OH，CH 2 OC 1 -C 6烷基，CH 2 OH或CF 3; Q 1是氢，C 1-6烷基，C 1-6二烷基，C 1-6烷氧基，NHAc，NR 2 10，其中R 10是氢或C 1-6烷基，二氟，氟，= O或OH; Q 2，Q 3，Q 4和Q 5相同或不同，表示氢，C 1-6烷氧基，OCF 3，OCH 2 CF 3，O-环丙基，OCH 2 - 环丙基，C 1 -C 6烷基，烷基，NR210，其中R10是氢或C1-6烷基，卤素，NO2，OH，CH2OC1-C6烷基，CH2OH或5-或6-元芳基; 条件是化合物[4-（1-氧代-1,3-二氢-2H-苯并[f]异吲哚-2-基）苯基] -2-丙酸钠盐和[4-（4,9 - 二乙氧基-1-氧代-1,3-二氢-2H-苯并[f]异吲哚-2-基）苯基]乙酸; 及其药学上可接受的衍生物。

7. 发明申请

WO2008061955A1 BENZOISOINDOLE DERIVATIVES AND THEIR USE AS EP4 RECEPTOR AGONISTS 审中-公开
标题翻译：苯并噻唑衍生物及其作为EP4受体激动剂的用途
公开(公告)号：WO2008061955A1
公开(公告)日：2008-05-29
申请号：PCT/EP2007/062497
申请日：2007-11-19
申请人： GLAXO GROUP LIMITED , GIBLIN, Gerard, Martin, Paul , HEALY, Mark, Patrick , PRICE, Helen, Susanne
发明人： GIBLIN, Gerard, Martin, Paul , HEALY, Mark, Patrick , PRICE, Helen, Susanne
IPC分类号： C07D209/64 , C07D209/66 , A61K31/403 , A61P25/00
CPC分类号： C07D209/64 , C07D209/66
摘要： The present invention relates to benzoisoindole phenylacetic acid derivatives, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medicine as EP4 receptor organists.
摘要翻译：本发明涉及苯并异吲哚苯乙酸衍生物，其制备方法，含有它们的药物组合物及其作为EP4受体器官的医药用途。

8. 发明申请

WO2005037786A1 HETEROCYCLYL COMPOUNDS 审中-公开
标题翻译：杂环化合物
公开(公告)号：WO2005037786A1
公开(公告)日：2005-04-28
申请号：PCT/EP2004/011366
申请日：2004-10-06
申请人： GLAXO GROUP LIMITED , GIBLIN, Gerard, Martin, Paul , HALL, Adrian , KILFORD, Ian, Reginald , LEWELL, Xiao, Qing , MILLER, Neil, Derek , NAYLOR, Alan
发明人： GIBLIN, Gerard, Martin, Paul , HALL, Adrian , KILFORD, Ian, Reginald , LEWELL, Xiao, Qing , MILLER, Neil, Derek , NAYLOR, Alan
IPC分类号： C07D207/337
CPC分类号： C07D207/337 , C07D213/55 , C07D213/56 , C07D231/12 , C07D241/12 , C07D307/46 , C07D401/04
摘要： Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein A, B, D, Z, R 1 , R 2a , R 2b , and R x are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in treating conditions mediated by the action of PGE 2 at EP 1 receptors. Such conditions include pain, or inflammatory, immunological, bone, neurodegenerative or renal disorders.
摘要翻译：式（I）化合物或其药学上可接受的衍生物：其中A，B，D，Z，R 1，R 2a，R 2b和R x如说明书中所定义，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治疗由EP1受体的PGE2作用介导的病症中的用途。这些病症包括疼痛或炎症，免疫学，骨骼，神经变性或肾脏疾病。

9. 发明申请

WO2004039753A2 PHENYL COMPOUNDS 审中-公开
标题翻译：苯乙烯化合物
公开(公告)号：WO2004039753A2
公开(公告)日：2004-05-13
申请号：PCT/EP2003/012181
申请日：2003-10-30
申请人： GLAXO GROUP LIMITED , BIT, Rino, Antonio , GIBLIN, Gerard, Martin, Paul , HALL, Adrian , HURST, David, Nigel , KILFORD, Ian, Reginald , MILLER, Neil, Derek , SCOCCITTI, Tiziana
发明人： BIT, Rino, Antonio , GIBLIN, Gerard, Martin, Paul , HALL, Adrian , HURST, David, Nigel , KILFORD, Ian, Reginald , MILLER, Neil, Derek , SCOCCITTI, Tiziana
IPC分类号： C07C
CPC分类号： C07D333/38 , C07C65/03 , C07C65/24 , C07C69/734 , C07C69/94 , C07C229/64 , C07C233/54 , C07C235/42 , C07C311/08 , C07C311/51 , C07D211/60 , C07D211/62 , C07D213/30 , C07D213/38 , C07D213/61 , C07D213/64 , C07D213/79 , C07D213/80 , C07D241/24 , C07D241/26 , C07D257/04 , C07D261/18 , C07D333/16
摘要： Compounds of formula (I) or derivatives thereof: wherein A, B, Z, R 1 , R 2a , R 2b , R x , R 8 , and R 9 are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.
摘要翻译：式（I）化合物或其衍生物：其中A，B，Z，R 1，R 2a，R 2b，R x，R 8和R 9如上所定义在说明书中，制备这种化合物的方法，包含这些化合物的药物组合物和这些化合物在医药中的用途。

10. 发明申请

WO2009019281A1 BENZOISOINDOLE DERIVATIVES AND THEIR USE AS EP4 RECEPTOR AGONISTS FOR THE TREATMENT OF PAIN 审中-公开
标题翻译：苯并噻唑衍生物及其用作治疗疼痛的EP4受体激动剂
公开(公告)号：WO2009019281A1
公开(公告)日：2009-02-12
申请号：PCT/EP2008/060313
申请日：2008-08-06
申请人： GLAXO GROUP LIMITED , CHILDS, Amanda, Claire , GIBLIN, Gerard, Martin, Paul , HEALY, Mark, Patrick
发明人： CHILDS, Amanda, Claire , GIBLIN, Gerard, Martin, Paul , HEALY, Mark, Patrick
IPC分类号： C07D209/64 , C07D209/66 , A61K31/4035 , A61P25/00 , A61P35/00
CPC分类号： C07D209/66 , C07D209/64
摘要： A compound of formula (I) wherein R 1 represents C 1-4 alkyl or C 1-4 alkoxy; R 2 represents C 1-4 alkyl or C 1-4 alkenyl; R 3 represents H, F, Cl, methyl, methoxy or CF 3 ; R 4 represents H or F; X represents CH 2 or C=O; and Y represents CH 2 or C=O, provided that at least one of X and Y represents C=O and at least one of R 3 and R 4 is H; and pharmaceutically acceptable derivatives thereof, processes for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds in medicine.
摘要翻译：式（I）的化合物，其中R 1表示C 1-4烷基或C 1-4烷氧基; R 2表示C 1-4烷基或C 1-4烯基; R3表示H，F，Cl，甲基，甲氧基或CF3; R4表示H或F; X表示CH 2或C = O; 并且Y表示CH 2或C = O，条件是X和Y中的至少一个表示C = O，并且R 3和R 4中的至少一个为H; 和其药学上可接受的衍生物，制备这些化合物的方法，包含这些化合物的药物组合物和这些化合物在医药中的用途。

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