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1. 发明申请

WO2005074939A1 COMBINATION OF CB2 MODULATORS AND PDE4 INHIBITORS FOR USE IN MEDICINE 审中-公开
标题翻译： CB2调节剂和PDE4抑制剂在医学中的组合
公开(公告)号：WO2005074939A1
公开(公告)日：2005-08-18
申请号：PCT/GB2005/000348
申请日：2005-02-01
申请人： GLAXO GROUP LIMITED , DOUGHTY, Jennifer, Margaret , BROWN, Andrew, James , CONNOR, Helen, Elizabeth , EATHERTON, Andrew, John , GIBLIN, Gerard, Martin, Paul , JANDU, Karamjit, Singh , KNOWLES, Richard, Graham , MITCHELL, William, Leonard , NAYLOR, Alan , O'SHAUGHNESSY, Celestine, Theresa , PALOMBI, Giovanni , RAWLINGS, Derek, Anthony , SLINGSBY, Brian, Peter , TRALAU-STEWART, Catherine, Jane , WHITTINGTON, Andrew, Richard , WILLIAMSON, Richard, Alexander
发明人： BROWN, Andrew, James , CONNOR, Helen, Elizabeth , EATHERTON, Andrew, John , GIBLIN, Gerard, Martin, Paul , JANDU, Karamjit, Singh , KNOWLES, Richard, Graham , MITCHELL, William, Leonard , NAYLOR, Alan , O'SHAUGHNESSY, Celestine, Theresa , PALOMBI, Giovanni , RAWLINGS, Derek, Anthony , SLINGSBY, Brian, Peter , TRALAU-STEWART, Catherine, Jane , WHITTINGTON, Andrew, Richard , WILLIAMSON, Richard, Alexander
IPC分类号： A61K31/505
CPC分类号： A61K31/505 , A61K2300/00
摘要： Combination of one or more CB2 modulators such as a compound of formula (I), (II) and (III); and one more PDE4 inhibitors are useful of treating conditions which are mediated by the activity of CB2 receptors or conditions which are mediated by PDE4, such as an immune disorder, an inflamatory disorder, pain, rheumatoid.
摘要翻译：一种或多种CB 2调节剂如式（I），（II）和（III）的化合物的组合; 另外还有一种PDE4抑制剂可用于治疗由CB2受体的活性介导的病症或由PDE4介导的病症，例如免疫疾病，炎症性疾病，疼痛，类风湿病。

2. 发明申请

WO2009083526A1 NOVEL COMPOUNDS 审中-公开
标题翻译：新型化合物
公开(公告)号：WO2009083526A1
公开(公告)日：2009-07-09
申请号：PCT/EP2008/068150
申请日：2008-12-22
申请人： SMITHKLINE BEECHAM CORPORATION , BLANC, Jean-Baptiste, Emmanuel , ALLAN, Amanda, Claire , FIELDHOUSE, Charlotte , GIBLIN, Gerard, Martin, Paul , GIBSON, Mairi , HEALY, Mark, Patrick , JANDU, Karamjit, Singh , LAMBERT III, Millard, Hurst , PRICE, Helen Susanne , SHEARER, Barry, George
发明人： BLANC, Jean-Baptiste, Emmanuel , ALLAN, Amanda, Claire , FIELDHOUSE, Charlotte , GIBLIN, Gerard, Martin, Paul , GIBSON, Mairi , HEALY, Mark, Patrick , JANDU, Karamjit, Singh , LAMBERT III, Millard, Hurst , PRICE, Helen Susanne , SHEARER, Barry, George
IPC分类号： C07D235/06 , C07D235/08 , C07D235/10 , C07D401/06 , C07D401/12 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D413/06 , C07D417/06 , C07D417/12 , A61K31/4184 , A61P3/10 , A61P25/28
CPC分类号： C07D235/10 , C07D235/06 , C07D235/08 , C07D401/06 , C07D401/12 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D413/06 , C07D417/06 , C07D417/12
摘要： The invention relates to novel benzimidazole compounds of formula (I) wherein R 1 to R 1 are as defined in the specification, pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing them and their use in medicine. In particular, the invention relates to compounds that are agonists of peroxisome proliferators-activated receptorγ (PPARγ).
摘要翻译：本发明涉及式（I）的新型苯并咪唑化合物，其中R 1至R 1如本说明书中所定义，其药学上可接受的盐，含有它们的药物组合物及其在药物中的用途。特别地，本发明涉及作为过氧化物酶体增殖物激活受体的激动剂的化合物（PPAR？）。

3. 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。}

4. 发明申请

WO2007017264A2 COMPOUNDS 审中-公开
标题翻译：化合物
公开(公告)号：WO2007017264A2
公开(公告)日：2007-02-15
申请号：PCT/EP2006/007875
申请日：2006-08-07
申请人： GLAXO GROUP LIMITED , 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
CPC分类号： C07D471/04
摘要： The present invention relates to novel pyrrolopyridine 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：本发明涉及新型吡咯并吡啶衍生物，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。

5. 发明申请

WO2004029026A1 PYRIDINE DERIVATIVES AS CB2 RECEPTOR MODULATORS 审中-公开
标题翻译：吡啶衍生物作为CB2受体调节剂
公开(公告)号：WO2004029026A1
公开(公告)日：2004-04-08
申请号：PCT/EP2003/010930
申请日：2003-09-25
申请人： GLAXO GROUP LIMITED , EATHERTON, Andrew, John , GIBLIN, Gerard, Martin, Paul , JANDU, Karamjit, Singh , MITCHELL, William, Leonard , NAYLOR, Alan , PALOMBI, Giovanni , RAWLINGS, Derek, Anthony , SLINGSBY, Brian, Peter , WHITTINGTON, Andrew, Richard
发明人： EATHERTON, Andrew, John , GIBLIN, Gerard, Martin, Paul , JANDU, Karamjit, Singh , MITCHELL, William, Leonard , NAYLOR, Alan , PALOMBI, Giovanni , RAWLINGS, Derek, Anthony , SLINGSBY, Brian, Peter , WHITTINGTON, Andrew, Richard
IPC分类号： C07D213/82
CPC分类号： C07D213/82 , C07D401/06 , C07D403/06 , C07D405/12 , C07D409/12
摘要： The present invention relates to novel pyridine 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，该疾病通过大麻素受体的活性的增加或减少直接或间接引起。

6. 发明申请

WO2012028629A1 2 - (BENZYLOXY) BENZAMIDES AS LRRK2 KINASE INHIBITORS 审中-公开
标题翻译： 2 - （苄氧基）苯甲酸酯作为LRRK2激酶抑制剂
公开(公告)号：WO2012028629A1
公开(公告)日：2012-03-08
申请号：PCT/EP2011/064943
申请日：2011-08-31
申请人： GLAXO GROUP LIMITED , ANDREOTTI, Daniele , DAI, Xuedong , EATHERTON, Andrew John , JANDU, Karamjit Singh , LIU, Qian , PHILPS, Oliver James
发明人： ANDREOTTI, Daniele , DAI, Xuedong , EATHERTON, Andrew John , JANDU, Karamjit Singh , LIU, Qian , PHILPS, Oliver James
IPC分类号： C07C235/64 , C07D213/75 , C07D231/12 , C07D237/22 , C07D261/14 , C07D401/12 , C07D403/12 , C07D413/12 , C07D295/192 , A61K31/5377 , A61K31/501 , A61K31/4406 , A61K31/4439 , A61K31/4545 , A61K31/42
CPC分类号： C07D403/12 , C07D213/75 , C07D231/12 , C07D237/20 , C07D261/14 , C07D295/192 , C07D401/12 , C07D413/12
摘要： The present invention relates to novel compounds that inhibit LRRK2 kinase activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by LRRK2 kinase activity, for example Parkinson's disease or Alzheimer's disease.
摘要翻译：本发明涉及抑制LRRK2激酶活性的新化合物，其制备方法，含有它们的组合物及其用于治疗以LRRK2激酶活性为特征的疾病，例如帕金森病或阿尔茨海默氏病。

7. 发明申请

WO2011038572A1 NOVEL COMPOUNDS 审中-公开
标题翻译：新型化合物
公开(公告)号：WO2011038572A1
公开(公告)日：2011-04-07
申请号：PCT/CN2010/001501
申请日：2010-09-27
申请人： GLAXO GROUP LIMITED , GLAXOSMITHKLINE (CHINA) R&D COMPANY LIMITED , NICHOLS, Paula Louise , EATHERTON, Andrew John , BAMBOROUGH, Paul , JANDU, Karamjit Singh , PHILPS, Oliver James , ANDREOTTI, Daniele
发明人： NICHOLS, Paula Louise , EATHERTON, Andrew John , BAMBOROUGH, Paul , JANDU, Karamjit Singh , PHILPS, Oliver James , ANDREOTTI, Daniele
IPC分类号： C07D265/30 , C07D261/14 , C07D241/04 , C07D237/20 , C07D231/12 , C07C233/00 , C07C223/00 , A61K31/5375 , A61K31/4965 , A61K31/495 , A61K31/44 , A61K31/42 , A61K31/4155 , A61P25/16 , A61P25/28 , A61P25/00
CPC分类号： C07C235/64 , C07D213/75 , C07D231/40 , C07D237/20 , C07D261/14 , C07D263/48 , C07D401/12 , C07D403/12 , C07D413/12
摘要： The present invention discloses novel compounds inhibiting LRRK2 kinase activity, the preparation processes thereof, the compositions containing them, as well as the use in treating diseases characterized by LRRK2 kinase activity, particularly Parkinson's disease and Alzheimer's disease.
摘要翻译：本发明公开了抑制LRRK2激酶活性的新化合物，其制备方法，含有它们的组合物，以及用于治疗以LRRK2激酶活性为特征的疾病，特别是帕金森病和阿尔茨海默氏病。

8. 发明申请

WO2005075464A1 PYRIDINE DERIVATIVES AS CONNABINOID RECEPTOR MODULATORS 审中-公开
标题翻译：吡啶衍生物作为稳定蛋白受体调节剂
公开(公告)号：WO2005075464A1
公开(公告)日：2005-08-18
申请号：PCT/GB2005/000350
申请日：2005-02-01
申请人： GLAXO GROUP LIMITED , GIBLIN, Gerard, Martin, Paul , JANDU, Karamjit, Singh , MITCHELL, William, Leonard , WALL, Ian, David
发明人： GIBLIN, Gerard, Martin, Paul , JANDU, Karamjit, Singh , MITCHELL, William, Leonard , WALL, Ian, David
IPC分类号： C07D407/12
CPC分类号： C07D213/82 , C07D405/12 , C07D409/12
摘要： The present invention relates to novel pyridine derivatives such as compounds of the formula (I): and the use of such compounds or pharmaceutical compositions thereof in the treatment of diseases, particularly pain, which are mediated by the activity of the cannabinoid 2 receptor.
摘要翻译：本发明涉及新的吡啶衍生物，例如式（I）的化合物：以及这些化合物或其药物组合物在治疗由大麻素2受体的活性介导的疾病，特别是疼痛中的用途。

9. 发明申请

WO2004029027A1 PYRIDINE DERIVATIVES AS CB2 RECEPTOR MODULATORS 审中-公开
标题翻译：吡啶衍生物作为CB2受体调节剂
公开(公告)号：WO2004029027A1
公开(公告)日：2004-04-08
申请号：PCT/EP2003/010935
申请日：2003-09-25
申请人： GLAXO GROUP LIMITED , EATHERTON, Andrew, John , GIBLIN, Gerard, Martin, Paul , JANDU, Karamjit, Singh , MITCHELL, William, Leonard , NAYLOR, Alan , PALOMBI, Giovanni , RAWLINGS, Derek, Anthony , SLINGSBY, Brian, Peter , WHITTINGTON, Andrew, Richard
发明人： EATHERTON, Andrew, John , GIBLIN, Gerard, Martin, Paul , JANDU, Karamjit, Singh , MITCHELL, William, Leonard , NAYLOR, Alan , PALOMBI, Giovanni , RAWLINGS, Derek, Anthony , SLINGSBY, Brian, Peter , WHITTINGTON, Andrew, Richard
IPC分类号： C07D213/82
CPC分类号： C07D213/82 , C07D401/12 , C07D413/12
摘要： The present invention relates to novel pyridine 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.
摘要翻译：本发明涉及式（I）的新型吡啶衍生物，其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的增加或减少直接或间接引起的疾病，特别是疼痛的疾病。

10. 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。

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