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1. 发明申请

WO2009050227A1 PYRIDAZINE DERIVATIVES FOR INHIBITING BETA AMYLOID PEPTIDE PRODUCTION 审中-公开
标题翻译：抑制β-淀粉样肽生产的吡啶衍生物
公开(公告)号：WO2009050227A1
公开(公告)日：2009-04-23
申请号：PCT/EP2008/063950
申请日：2008-10-16
申请人： GLAXO GROUP LIMITED , EATHERTON, Andrew, John , GIBLIN, Gerard, Martin, Paul , HALL, Adrian , JOHNSON, Matthew, Russell , LE, Joelle , MITCHELL, William, Leonard , MYATT, James , NORTON, David , PRICE, Helen, Susanne
发明人： EATHERTON, Andrew, John , GIBLIN, Gerard, Martin, Paul , HALL, Adrian , JOHNSON, Matthew, Russell , LE, Joelle , MITCHELL, William, Leonard , MYATT, James , NORTON, David , PRICE, Helen, Susanne
IPC分类号： C07D403/10 , A61K31/501
CPC分类号： C07D403/10
摘要： The present invention relates to novel compounds that inhibit the production of β- amyloid peptide (1-42), processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by elevated β-amyloid levels or β-amyloid deposits, particularly Alzheimer's disease.
摘要翻译：本发明涉及抑制β-淀粉样蛋白肽（1-42）的制备，其制备方法，含有它们的组合物及其用于治疗特征在于β-淀粉样蛋白升高或β- 淀粉样沉积物，特别是阿尔茨海默氏病。

2. 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。}

3. 发明申请

WO2014013076A1 HEXAHYDROPYRROLOTHIAZINE COMPOUNDS 审中-公开
标题翻译：十六氢吡咯化合物
公开(公告)号：WO2014013076A1
公开(公告)日：2014-01-23
申请号：PCT/EP2013/065352
申请日：2013-07-19
申请人： EISAI R&D MANAGEMENT CO., LTD. , HALL, Adrian , FARTHING, Christopher Neil , EATHERTON, Andrew John
发明人： HALL, Adrian , FARTHING, Christopher Neil , EATHERTON, Andrew John
IPC分类号： C07D513/04 , A61K31/542 , A61P25/28
CPC分类号： C07D513/04
摘要： A compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R 1 to R 9 are as defined in the specification and which compound has an Αβ production inhibitory effect and may be useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Αβ and typified by Alzheimer-type dementia (AD) or Down's syndrome.
摘要翻译：式（I）化合物或其药学上可接受的盐，其中R 1至R 9如说明书中所定义，并且该化合物具有字母表生产抑制作用，并且可用作由由字母表引起的神经变性疾病的预防或治疗剂并以阿尔茨海默氏型痴呆（AD）或唐氏综合征为特征。

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

WO2008098978A3 BENZOFURAN COMPOUNDS USEFUL IN THE TREATMENT OF CONDITIONS MEDIATED BY THE ACTION OF PGE2 AT THE EP1 RECEPTOR 审中-公开
标题翻译：苯并呋喃化合物可用于治疗EP1受体中PGE2的作用介导的病症
公开(公告)号：WO2008098978A3
公开(公告)日：2008-10-09
申请号：PCT/EP2008051766
申请日：2008-02-14
申请人： GLAXO GROUP LTD , EATHERTON ANDREW JOHN , GIBLIN GERARD MARTIN PAUL , GIBSON MAIRI , HALL ADRIAN , HURST DAVID NIGEL
发明人： EATHERTON ANDREW JOHN , GIBLIN GERARD MARTIN PAUL , GIBSON MAIRI , HALL ADRIAN , HURST DAVID NIGEL
IPC分类号： C07D405/06 , A61P25/00 , C07D405/14 , C07D407/06
CPC分类号： C07D407/06 , C07D405/06 , C07D405/14 , C07D409/14 , C07D417/14
摘要： A compound of formula (I), wherein R 1 , R 2 , and R 3 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，其中R 1，R 2和R 3如本说明书中所定义，这些化合物的制备，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。

7. 发明申请

WO2005080350A1 PYRIMIDINE DERIVATIVES AS CANNABINOID RECEPTOR MODULATORS 审中-公开
标题翻译：作为CANNABINOID受体调节剂的吡嗪衍生物
公开(公告)号：WO2005080350A1
公开(公告)日：2005-09-01
申请号：PCT/EP2005/001939
申请日：2005-02-21
申请人： GLAXO GROUP LIMITED , EATHERTON, Andrew, John , GIBLIN, Gerard, Martin, Paul , MITCHELL, William, Leonard , NAYLOR, Alan
发明人： EATHERTON, Andrew, John , GIBLIN, Gerard, Martin, Paul , MITCHELL, William, Leonard , NAYLOR, Alan
IPC分类号： C07D239/42
CPC分类号： C07D239/42 , C07D401/12
摘要： The present invention relates to novel pyrimidine 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：本发明涉及新颖的嘧啶衍生物，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。

8. 发明申请

WO2005080342A1 PYRIDINE DERIVATIVES AND THEIR USE AS CB2 RECEPTOR MODULATORS 审中-公开
标题翻译：吡啶衍生物及其作为CB2受体调节剂的用途
公开(公告)号：WO2005080342A1
公开(公告)日：2005-09-01
申请号：PCT/EP2005/001938
申请日：2005-02-22
申请人： GLAXO GROUP LIMITED , EATHERTON, Andrew, John , GIBLIN, Gerard, Martin, Paul , MITCHELL, William, Leonard , NAYLOR, Alan
发明人： EATHERTON, Andrew, John , GIBLIN, Gerard, Martin, Paul , MITCHELL, William, Leonard , NAYLOR, Alan
IPC分类号： C07D213/74
CPC分类号： C07D213/74 , C07D401/06 , 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：本发明涉及新型吡啶衍生物，例如式（I）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受体活性介导的疾病，特别是疼痛中的用途。

9. 发明申请

WO2004018433A1 PYRIMIDINE DERIVATIVES AND THEIR USE AS CB2 MODULATORS 审中-公开
标题翻译：吡啶衍生物及其作为CB2调节剂的用途
公开(公告)号：WO2004018433A1
公开(公告)日：2004-03-04
申请号：PCT/EP2003/009217
申请日：2003-08-19
申请人： GLAXO GROUP LIMITED , EATHERTON, Andrew, John , GIBLIN, Gerard, Martin, Paul , GREEN, Richard, Howard (Deceased) , MITCHELL, William, Leonard , NAYLOR, Alan , RAWLINGS, Derek, Anthony , SLINGSBY, Brian, Peter , WHITTINGTON, Andrew, Richard
发明人： EATHERTON, Andrew, John , GIBLIN, Gerard, Martin, Paul , GREEN, Richard, Howard (Deceased) , MITCHELL, William, Leonard , NAYLOR, Alan , RAWLINGS, Derek, Anthony , SLINGSBY, Brian, Peter , WHITTINGTON, Andrew, Richard
IPC分类号： C07D239/42
CPC分类号： C07D239/42 , C07D401/06 , C07D401/12 , C07D403/06 , C07D405/12 , C07D409/12
摘要： This 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：这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在治疗疾病特别是疼痛中的用途，所述疾病通过大麻素受体的活性的增加或减少而直接或间接引起。

10. 发明申请

WO2011012622A1 BENZOXAZINONE DERIVATIVES FOR THE TREATMENT OF GLYTL MEDIATED DISORDERS 审中-公开
标题翻译：用于治疗GLYTL介导的疾病的苯唑西汀衍生物
公开(公告)号：WO2011012622A1
公开(公告)日：2011-02-03
申请号：PCT/EP2010/060886
申请日：2010-07-27
申请人： GLAXO GROUP LIMITED , BLUNT, Richard , EATHERTON, Andrew John , GARZYA, Vincenzo , HEALY, Mark Patrick , MYATT, James , PORTER, Roderick Alan
发明人： BLUNT, Richard , EATHERTON, Andrew John , GARZYA, Vincenzo , HEALY, Mark Patrick , MYATT, James , PORTER, Roderick Alan
IPC分类号： C07D413/06 , C07D419/06 , C07D471/04 , C07D487/04 , C07D493/04 , C07D495/04 , C07D498/04 , C07D513/04 , A61K31/5377 , A61P25/18
CPC分类号： C07D413/06 , C07D419/06 , C07D471/04 , C07D487/04 , C07D493/04 , C07D495/04 , C07D498/04 , C07D513/04
摘要： The present invention relates to benzoxazinone derivatives, processes for their preparation, pharmaceutical compositions and medicaments containing them and to their use in treating disorders mediated by GlyT1, including neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder.
摘要翻译：本发明涉及苯并恶嗪酮衍生物，其制备方法，药物组合物和含有它们的药物及其用于治疗由GlyT1介导的疾病，包括神经和神经精神障碍，特别是精神病，痴呆或注意力缺陷障碍。

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