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1. 发明申请

WO2007017264A3 PYRROLOPYRIDINEDERIVATIVES AS MODULATORS OF THE CANNABINOID RECEPTOR FOR THE TREATMENT OF IMMUNE AND INFLAMMATORY DISORDERS 审中-公开
标题翻译：作为用于治疗免疫和炎症疾病的CANNABINOID受体的调节剂的吡咯烷酮
公开(公告)号：WO2007017264A3
公开(公告)日：2007-04-12
申请号：PCT/EP2006007875
申请日：2006-08-07
申请人： GLAXO GROUP LTD , EATHERTON ANDREW JOHN , GIBLIN GERARD MARTIN PAUL , JANDU KARAMJIT SINGH , JOHNSON MATTHEW RUSSELL , MITCHELL WILLIAM LEONARD , NAYLOR ALAN , SWEETING JENNIFER ANNE
发明人： EATHERTON ANDREW JOHN , GIBLIN GERARD MARTIN PAUL , JANDU KARAMJIT SINGH , JOHNSON MATTHEW RUSSELL , MITCHELL WILLIAM LEONARD , NAYLOR ALAN , SWEETING JENNIFER ANNE
IPC分类号： C07D471/04 , A61K31/437 , A61P19/02 , A61P29/00 , A61P37/02
CPC分类号： C07D471/04
摘要： The present invention relates to novel pyrrolopyridine derivatives of formula (I), pharmaceutical compositions containing these compounds and their use in the treatment of diseases, particularly pain, which diseases are caused directly or indirectly by an increase or decrease-in activity of the cannabinoid receptor, wherein: X 1 is NH and X 2 and X 3 together form a -CR 13 =CR 11 -group or X 3 is NR 12 and X 2 and X 1 together form a -CR 13 =CR 11 - group; X 4 is O, SO 2 , S, or a bond, or X 4 is -NHCO or -NHCH 2 such that R 6 X 4 is R 6 CONH or R 6 CH 2 NH; R 1 is selected from hydrogen, C 1-6 alkyl, C 3-6 cycloalkyl and halosubstituted C 1-6 alkyl; R 2 is hydrogen or (CH 2 )mR 3 where m is 0 or 1; or R 1 and R 2 together with N to which they are attached form an optionally substituted 4- to 8- membered non-aromatic heterocyclyl ring; R 3 is a 4- to8- membered non-aromatic heterocyclyl group, a C 3-8 cycloalkyl group, a straight or branched C 1-10 alkyl, a C 2-10 alkenyl, a C 3-8 cycloalkenyl, a C 2-10 alkynyl, a C 3-8 cycloalkynyl or phenyl group, any of which can be unsubstituted or substituted, or R 5 ; wherein p is 0, 1 or 2, and X is CH 2 . O, S, or SO 2 ; R 6 is phenyl, C 3-6 cycloalkyl, a straight or branched C 1-6 alkyl group, -CH 2 -C 3-6 cycloalkyl, -CH 2 -phenyl, 4- to 8- membered non-aromatic heterocyclyl group, or a bicyclic group any of which can be unsubstituted or substituted, however when X 4 is a bond R 6 is substituted phenyl; R 7 is OH, C 1-6 alkoxy, NR 8a R 8b , NHCOR 9 , NHSO 2 R 9 or SOqR 9 ; R 8a is H or C 1-6 alkyl; R 8b is Hor C 1-6 alkyl; R 9 is C 1-6 alkyl; R 10 is hydrogen, substituted or unsubstituted (C 1-6 )alkyl or chloro; R 11 is hydrogen or C 1-6 alkyl; R 12 is hydrogen or C 1-6 alkyl; R 13 is hydrogen or C 1-6 alkyl; q is 0, 1 or 2.
摘要翻译：本发明涉及式（I）的新型吡咯并吡啶衍生物，含有这些化合物的药物组合物及其在治疗疾病尤其是疼痛中的用途，所述疾病是由大麻素受体直接或间接引起的活性增加或减少引起的，其中：X 1是NH且X 2和X 3一起形成-CR 13 = CR 3， SUP> 11 - 组或X 3是NR 12和X 2和X 1一起形成一个-CR = CR 11 - 组; X 4是O，SO 2，S或键，或X 4是-NHCO或-NHCH 2， SUB>使得R 6 X 4是R 6 CONH或R 6 CH 2， SUB> NH; R 1选自氢，C 1-6烷基，C 3-6环烷基和卤素取代的C 1-6烷基， SUB>烷基; R 2是氢或（CH 2 CH 2）m R 3，其中m是0或1; 或R 1和R 2与它们所连接的N一起形成任选取代的4-至8-元非芳族杂环基环; R 3是4-至8-元非芳族杂环基，C 3-8环烷基，直链或支链C 1-10烷基，亚烷基，C 2-10链烯基，C 3-8环烯基，C 2-10炔基，C _{3-8环炔基或苯基，其中任何一个可以是未取代的或取代的，或R 5; 其中p是0,1或2，X是CH 2。 O，S或SO 2; R 6是苯基，C 3-6环烷基，直链或支链C 1-6 - 烷基，-CH 2， C 3-6环烷基，-CH 2 - 苯基，4-至8-元非芳族杂环基，或双环基，任何一个可以未取代或取代的，但是当X 4为键时，R 6为取代的苯基; R 7是OH，C 1-6烷氧基，NR 8a R 8b，NHCOR 9， / SO 2，NHSO 2 R 9或SO 3 R 9; R 8a是H或C 1-6烷基; R 8b是Hor C 1-6烷基; R 9是C 1-6烷基; R 10是氢，取代或未取代的（C 1-6 - ）烷基或氯; R 11是氢或C 1-6烷基; R 12是氢或C 1-6烷基; R 13是氢或C 1-6烷基; q是0,1或2。}

2. 发明申请

WO2006114313A1 PYRAZOLE COMPOUNDS AS PROSTAGLANDIN RECEPTORS LIGANDS 审中-公开
标题翻译：作为PROSTAGLANDIN受体配体的吡咯化合物
公开(公告)号：WO2006114313A1
公开(公告)日：2006-11-02
申请号：PCT/EP2006/003919
申请日：2006-04-24
申请人： GLAXO GROUP LIMITED , CONWAY, Elizabeth, Ann , GIBLIN, Gerard, Martin, Paul , GIBSON, Mairi , HALL, Adrian , HAYHOW, Thomas, George, Christopher , HEALY, Mark, Patrick , HURST, David, Nigel , KILFORD, Ian, Reginald , MCKEOWN, Stephen, Carl , NAYLOR, Alan , PRICE, Helen Susanne , RAWLINGS, Derek Anthony
发明人： CONWAY, Elizabeth, Ann , GIBLIN, Gerard, Martin, Paul , GIBSON, Mairi , HALL, Adrian , HAYHOW, Thomas, George, Christopher , HEALY, Mark, Patrick , HURST, David, Nigel , KILFORD, Ian, Reginald , MCKEOWN, Stephen, Carl , NAYLOR, Alan , PRICE, Helen Susanne , RAWLINGS, Derek Anthony
IPC分类号： A61K31/4155 , C07D231/14 , C07D231/20 , C07D231/40 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/04 , C07D409/12 , C07D413/04 , C07D413/12 , C07D417/12
CPC分类号： C07D231/40 , C07D231/14 , C07D231/20 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/04 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04
摘要： Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein Z, R 1 ,R 2a , R 2b , R 10 , R 11 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 medicine.
摘要翻译：式（I）化合物或其药学上可接受的衍生物：其中Z，R 1，R 2a，R 2b，R 2b， 10，R 11和R x如本说明书中所定义，制备这些化合物的方法，包含这些化合物的药物组合物和使用药物中的这种化合物。

3. 发明申请

WO2005080349A1 PYRIMIDINE DERIVATIVES 审中-公开
标题翻译：吡嗪衍生物
公开(公告)号：WO2005080349A1
公开(公告)日：2005-09-01
申请号：PCT/EP2005/001937
申请日：2005-02-22
申请人： GLAXO GROUP LIMITED , GIBLIN, Gerard, Martin, Paul , MITCHELL, William, Leonard , NAYLOR, Alan , WALL, Ian, David
发明人： GIBLIN, Gerard, Martin, Paul , MITCHELL, William, Leonard , NAYLOR, Alan , WALL, Ian, David
IPC分类号： C07D239/42
CPC分类号： C07D239/42
摘要： The present invention relates to novel pyrimidine derivatives, pharmaceutical compositions containing these compounds and their use in the treatment of diseases, particularly pain, which diseases are caused directly or indirectly by an increase or decrease in activity of the cannabinoid receptor.
摘要翻译：本发明涉及新颖的嘧啶衍生物，含有这些化合物的药物组合物及其用于治疗由大麻素受体的活性增加或减少而直接或间接引起的疾病，特别是疼痛的疾病。

4. 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。

5. 发明申请

WO2002096427A1 PYRIMIDINE DERIVATIVES AS SELECTIVE INHIBITORS OF COX-2 审中-公开
标题翻译：作为COX-2的选择性抑制剂的吡嗪衍生物
公开(公告)号：WO2002096427A1
公开(公告)日：2002-12-05
申请号：PCT/GB2002/002414
申请日：2002-05-23
申请人： GLAXO GROUP LIMITED , HARTLEY, Charles, David , NAYLOR, Alan , PAYNE, Jeremy, John , PEGG, Neil, Anthony
发明人： HARTLEY, Charles, David , NAYLOR, Alan , PAYNE, Jeremy, John , PEGG, Neil, Anthony
IPC分类号： A61K31/505
CPC分类号： C07D239/42
摘要： The invention thus provides the compounds of formula (I) and pharmaceutically acceptable salts thereof, in which: R 1 and R 2 are independently selected from the group consisting of H, C 1-6 alkyl, C 2-6 alkenyl, C 3-6 alkynyl, C 3-10 cycloalkylC 0-6 alkyl and C 4-12 bridged cycloalkyl; R 3 is selected from the group consisting of C 1-6 alkyl, NH 2 and R 5 CONH; R 4 is selected from the group consisting of CH 2 F, CHF 2 , CF 3 CH 2 , CF 3 CHF and CF 3 CF 2 ; and R 5 is selected from the group consisting of H, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 alkylOC 1-6 alkyl, phenyl, HO¿ 2 CC 1-6?alkyl, C 1-6 alkylOCOC 1-6 alkyl, C 1-6 alkylOCO, H 2 NC 1-6 alkyl, C 1-6 alkylOCONHC 1-6 alkyl and C 1-6 alkylCONHC 1-6 alkyl. Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever, inflammation of a variety of conditions and diseases.
摘要翻译：因此，本发明提供式（I）化合物及其药学上可接受的盐，其中：R 1和R 2独立地选自H，C 1-6烷基，C 2-6烯基，C 3-6炔基，C 3-10环烷基C 1-6烷基和C 4-12桥环烷基; R 3选自C 1-6烷基，NH 2和R 5 CONH; R 4选自CH 2 F，CHF 2，CF 3 CH 2，CF 3 CHF和CF 3 CF 2; 和R 5选自H，C 1-6烷基，C 1-6烷氧基，C 1-6烷基C 1-6烷基，苯基，HO 2 CCl 1-6烷基，C 1-6烷基COOC 1-6烷基，C 1-6烷基COO，H 2 NC 1-6烷基，C 1 1-6烷基OCONHC 1-6烷基和C 1-6烷基CONHC 1-6烷基。式（I）化合物是COX-2的有效和选择性抑制剂，可用于治疗疼痛，发热，各种病症和疾病的炎症。

6. 发明申请

WO0156555A3 USE OF COX-2 INHIBITORS FOR THE TREATMENT OF CONSTIPATION 审中-公开
标题翻译：使用COX-2抑制剂治疗组织
公开(公告)号：WO0156555A3
公开(公告)日：2002-08-08
申请号：PCT/GB0100416
申请日：2001-02-01
申请人： GLAXO GROUP LTD , MANGEL ALLEN WAYNE , NAYLOR ALAN
发明人： MANGEL ALLEN WAYNE , NAYLOR ALAN
IPC分类号： C07D239/42 , A61K31/00 , A61K31/18 , A61K31/196 , A61K31/365 , A61K31/405 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/437 , A61K31/444 , A61K31/5025 , A61K31/505 , A61K45/00 , A61P1/10 , A61P1/14 , A61P43/00 , C07D209/32 , C07D231/12 , C07D487/04
CPC分类号： A61K31/00 , A61K31/18 , A61K31/196 , A61K31/365 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/437 , A61K31/444 , A61K31/5025 , A61K31/505
摘要： The invention provides a COX-2 inhibitor or a pharmaceutically acceptable derivative thereof for use in the treatment of constipation.
摘要翻译：本发明提供了一种用于治疗便秘的COX-2抑制剂或其药学上可接受的衍生物。

7. 发明申请

WO0145714A3 FORMULATIONS OF ADENOSINE A1 AGONISTS 审中-公开
标题翻译：腺苷A1激动剂的配方
公开(公告)号：WO0145714A3
公开(公告)日：2002-02-28
申请号：PCT/GB0004892
申请日：2000-12-19
申请人： GLAXO GROUP LTD , BOUNTRA CHARANJIT , CLAYTON NICHOLAS MAUGHAN , NAYLOR ALAN
发明人： BOUNTRA CHARANJIT , CLAYTON NICHOLAS MAUGHAN , NAYLOR ALAN
IPC分类号： A61K45/00 , A61K31/195 , A61K31/197 , A61K31/52 , A61K31/7076 , A61K45/06 , A61P1/00 , A61P3/10 , A61P19/00 , A61P19/02 , A61P21/00 , A61P25/04 , A61P25/06 , A61P29/00 , A61P35/00 , A61P25/00
CPC分类号： A61K31/7076 , A61K31/195 , A61K31/70 , A61K45/06 , A61K2300/00
摘要： The present invention provides a method of treating conditions associated with pain and alleviating the symptoms associated therewith which comprises administering to a mammal, including man, (i) an adenosine A1 agonist or a physiologically acceptable salt or solvate thereof and (ii) gabapentin or pregabalin or a physiologically acceptable salt or solvate thereof. The present invention also provides pharmaceutical formulations and patient packs comprising said combinations.
摘要翻译：本发明提供了一种治疗与疼痛相关的病症并减轻与之相关的症状的方法，其包括对包括人在内的哺乳动物施用（i）腺苷A1激动剂或其生理学上可接受的盐或溶剂合物和（ii）加巴喷丁或普瑞巴林或其生理上可接受的盐或溶剂合物。本发明还提供包含所述组合的药物制剂和患者包装。

8. 发明申请

WO0145685A3 FORMULATIONS OF ADENOSINE A1 AGONISTS 审中-公开
标题翻译：腺苷A1激动剂的配方
公开(公告)号：WO0145685A3
公开(公告)日：2002-02-28
申请号：PCT/GB0004902
申请日：2000-12-19
申请人： GLAXO GROUP LTD , BOUNTRA CHARANJIT , CLAYTON NICHOLAS MAUGHAN , NAYLOR ALAN
发明人： BOUNTRA CHARANJIT , CLAYTON NICHOLAS MAUGHAN , NAYLOR ALAN
IPC分类号： A61K45/00 , A61K31/40 , A61K31/4184 , A61K31/437 , A61K31/4375 , A61K31/46 , A61K31/517 , A61K31/52 , A61K31/7076 , A61P25/04 , A61P43/00 , A61K45/06 , A61P25/00
CPC分类号： A61K31/517 , A61K31/46 , A61K31/52 , A61K31/7076
摘要： The present invention provides a method of treating conditions associated with pain and alleviating the symptoms associated therewith which comprises administering to a mammal, including man, an adenosine A1 agonist or a physiologically acceptable salt or solvate thereof and a 5HT3 antagonist or a physiologically acceptable salt or solvate thereof. The present invention also provides pharmaceutical formulations and patient packs comprising said combinations.
摘要翻译：本发明提供了一种治疗与疼痛相关的病症并减轻与之相关的症状的方法，其包括对哺乳动物，包括人，腺苷A1激动剂或其生理学上可接受的盐或溶剂合物和5HT3拮抗剂或生理上可接受的盐或其溶剂合物。本发明还提供包含所述组合的药物制剂和患者包装。

9. 发明申请

WO0068463A3 ELECTRODE STRUCTURE 审中-公开
标题翻译：电极结构
公开(公告)号：WO0068463A3
公开(公告)日：2001-04-12
申请号：PCT/GB0001645
申请日：2000-04-28
申请人： ICI PLC , REVILL BRIAN KENNETH , DUTTON MICHAEL FREDERICK , STANLEY KEITH ALBERT , NAYLOR ALAN ROBERT
发明人： REVILL BRIAN KENNETH , DUTTON MICHAEL FREDERICK , STANLEY KEITH ALBERT , NAYLOR ALAN ROBERT
IPC分类号： C25B9/00 , C25B9/08 , C25B9/20 , C25B11/02 , H01M4/86 , H01M8/02 , H01M8/18 , C25B9/06
CPC分类号： H01M4/8626 , C25B9/08 , C25B9/206 , C25B11/02 , H01M8/0273
摘要： An electrode structure for use, for example, in a bipolar electrolyser comprising (i) a pan with a dished recess and a flange around the periphery thereof for supporting gasket means for sealing a separator between the flanges in adjacent electrode structures, which separator is disposed between the surface of the anode of a first electrode structure and the cathode of a second electrode structure such that the anode surface is substantially parallel to and faces but is insulated and spaced apart from the cathode surface by the separator and is hermetically-sealed to the separator, (ii) an electrically conductive plate spaced from the pan, (iii) a plurality of electrically-conductive members to which the electrically conductive plate is electroconductively attached and which provide electrically-conductive pathways between the pan and the electrically conductive plate, (iv) inlet for electrolyte and (v) outlets for liquids and gases wherein where the electrode structure is an anode structure the dished recess is provided with a plurality of inwardly projecting projections and where the electrode structure is a cathode structure the dished recess is provided with a plurality of outwardly projecting projections such that the inwardly projecting projections in the dished recess of the pan of the anode structure mate with the outwardly projecting projections in the dished recess of the pan of an adjacent cathode structure in a bipolar electrolyser comprising a plurality of the electrode structures.
摘要翻译：一种电极结构，例如在双极电解槽中使用的电极结构，该电极结构包括：（i）具有碟形凹槽的盘和围绕其圆周的凸缘，用于支撑用于将隔板密封在相邻电极结构中的凸缘之间的垫片装置，在第一电极结构的阳极的表面和第二电极结构的阴极之间，使得阳极表面基本上平行于并面对，但是通过隔板绝缘并与阴极表面隔开，并且密封到分离器，（ii）与所述盘间隔开的导电板，（iii）多个导电构件，所述导电板被导电地连接到所述导电构件上，并且在所述盘和所述导电板之间提供导电通路（ iv）电解质入口和（v）用于液体和气体的出口，其中电极结构是阳极结构碟形凹部的结构设置有多个向内突出的突出物，并且其中电极结构是阴极结构，碟形凹部设置有多个向外突出的突起，使得阳极盘的凹槽中的向内突出的突起结构与包括多个电极结构的双极电解器中的相邻阴极结构的盘的凹槽中的向外突出的突起配合。

10. 发明申请

WO1996031509A1 IMIDAZO[1,2-a]PYRIDINE DERIVATIVES 审中-公开
标题翻译：咪唑并[1,2-a]吡啶衍生物
公开(公告)号：WO1996031509A1
公开(公告)日：1996-10-10
申请号：PCT/EP1996001438
申请日：1996-04-02
申请人： GLAXO GROUP LIMITED , BESWICK, Paul, John , CAMPBELL, Ian, Baxter , NAYLOR, Alan
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： The invention provides the compounds of formula (I) and pharmaceutically acceptable derivatives thereof in which: R represents halogen; R and R are independently selected from H, halogen, C1-4alkyl, C1-4alkyl substituted by one or more fluorine atoms, C1-4alkoxy, C1-4hydroxyalkyl, SC1-4alkyl, C(O)H or C(O)C1-4alkyl; and R represents C1-4alkyl. Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever, inflammation of a variety of conditions and diseases.
摘要翻译：本发明提供式（I）化合物及其药学上可接受的衍生物，其中：R 0表示卤素; R 1和R 2独立地选自H，卤素，C 1-4烷基，被一个或多个氟原子取代的C 1-4烷基，C 1-4烷氧基，C 1-4羟烷基，SC 1-4烷基，C（O）H或 C（O）C 1-4烷基; 且R 3表示C 1-4烷基。式（I）化合物是COX-2的有效和选择性抑制剂，可用于治疗疼痛，发热，各种病症和疾病的炎症。

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