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1. 发明申请

WO2011067366A1 INDAZOLE DERIVATIVES AS PI 3 - KINASE INHIBITORS 审中-公开
标题翻译：作为PI 3 - 激酶抑制剂的吲哚衍生物
公开(公告)号：WO2011067366A1
公开(公告)日：2011-06-09
申请号：PCT/EP2010/068798
申请日：2010-12-03
申请人： GLAXO GROUP LIMITED , BALDWIN, Ian Robert , DOWN, Kenneth David , FAULDER, Paul , GAINES, Simon , HAMBLIN, Julie Nicole , JONES, Katherine Louise , LE, Joelle , LUNNISS, Christopher James , PARR, Nigel James , RITCHIE, Timothy John , ROBINSON, John Edward , SMETHURST, Christian Alan Paul
发明人： BALDWIN, Ian Robert , DOWN, Kenneth David , FAULDER, Paul , GAINES, Simon , HAMBLIN, Julie Nicole , JONES, Katherine Louise , LE, Joelle , LUNNISS, Christopher James , PARR, Nigel James , RITCHIE, Timothy John , ROBINSON, John Edward , SMETHURST, Christian Alan Paul
IPC分类号： C07D417/12 , C07D417/14 , C07D471/04 , A61K31/416 , A61P11/00 , A61P29/00 , A61P37/00 , A61P25/00 , A61P9/00
CPC分类号： C07D417/14 , C07D417/12 , C07D471/04
摘要： The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.
摘要翻译：本发明涉及某些新化合物。具体地，本发明涉及式（I）的化合物及其盐。本发明的化合物是PI3-激酶活性的抑制剂。

2. 发明申请

WO2011067365A1 BENZPYRAZOLE DERIVATIVES AS INHIBITORS OF P13 KINASES 审中-公开
标题翻译：作为P13激酶抑制剂的苯并噻唑衍生物
公开(公告)号：WO2011067365A1
公开(公告)日：2011-06-09
申请号：PCT/EP2010/068797
申请日：2010-12-03
申请人： GLAXO GROUP LIMITED , BALDWIN, Ian Robert , DOWN, Kenneth David , FAULDER, Paul , GAINES, Simon , HAMBLIN, Julie Nicole , JONES, Katherine Louise , JONES, Paul Spencer , LE, Joelle , LUNNISS, Christopher James , PARR, Nigel James , RITCHIE, Timothy John , ROBINSON, John Edward , SIMPSON, Juliet Kay , SMETHURST, Christian Alan Paul
发明人： BALDWIN, Ian Robert , DOWN, Kenneth David , FAULDER, Paul , GAINES, Simon , HAMBLIN, Julie Nicole , JONES, Katherine Louise , JONES, Paul Spencer , LE, Joelle , LUNNISS, Christopher James , PARR, Nigel James , RITCHIE, Timothy John , ROBINSON, John Edward , SIMPSON, Juliet Kay , SMETHURST, Christian Alan Paul
IPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D417/04 , C07D471/04 , C07D487/04 , A61K31/416 , A61P11/00
CPC分类号： C07D487/04 , C07D401/04 , C07D401/14 , C07D405/14 , C07D417/04 , C07D471/04
摘要： The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.
摘要翻译：本发明涉及某些新化合物。具体地，本发明涉及式（I）的化合物及其盐。本发明的化合物是PI3-激酶活性的抑制剂。

3. 发明申请

WO2006053784A3 1,7-NAPHTHYRIDINES AS PDE4 INHIBITORS 审中-公开
标题翻译：作为PDE4抑制剂的1,7-萘啶
公开(公告)号：WO2006053784A3
公开(公告)日：2006-07-06
申请号：PCT/EP2005012462
申请日：2005-11-17
申请人： GLAXO GROUP LTD , ELDRED COLIN DAVID , ROBINSON JOHN EDWARD , STEEL ALISON JUDITH
发明人： ELDRED COLIN DAVID , ROBINSON JOHN EDWARD , STEEL ALISON JUDITH
IPC分类号： C07D471/04 , A61K31/4375 , A61P29/00
CPC分类号： C07D471/04
摘要： There are provided according to the invention novel compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof: (I) wherein: R 1 is phenyl which may be unsubstituted or substituted by one or two substituents selected from fluorine, chlorine, C 1-2 alkoxy-, -CN; phenyl fused to a 5-membered saturated ring containing one oxygen atom; pyridinyl which may be unsubstituted or substituted by one or two substituents selected from fluorine or chlorine; or C-linked pyrazolyl which may be unsubstituted or substituted by the substituent C 1-2 alkyl; R 2 is C 1-4 alkyl; R 3 is C 1-2 alkyl; and n is 0, 1 or 2.
摘要翻译：根据本发明提供新的式（I）化合物及其药学上可接受的盐和溶剂化物：（I）其中：R 1是可以是未取代的或被一个或两个取代基所取代的苯基由氟，氯，C 1-2烷氧基 - ，-CN; 与含有一个氧原子的5元饱和环稠合的苯基; 吡啶基，其可以是未取代的或被一个或两个选自氟或氯的取代基取代; 或C连接的吡唑基，其可以是未取代的或被取代基C 1-12烷基取代; R 2是C 1-4烷基; R 3是C 1-12烷基; n为0,1或2。

4. 发明申请

WO2009147189A1 NOVEL COMPOUNDS 审中-公开
标题翻译：新型化合物
公开(公告)号：WO2009147189A1
公开(公告)日：2009-12-10
申请号：PCT/EP2009/056840
申请日：2009-06-03
申请人： GLAXO GROUP LIMITED , BALDWIN, Ian, Robert , DOWN, Kenneth, David , FAULDER, Paul , GAINES, Simon , HAMBLIN, Julie, Nicole , JONES, Paul, Spencer , LE, Joelle , PARR, Nigel, James , RITCHIE, Timothy, John , ROBINSON, John, Edward , SIMPSON, Juliet, Kay , SMETHURST, Christian, Alan, Paul
发明人： BALDWIN, Ian, Robert , DOWN, Kenneth, David , FAULDER, Paul , GAINES, Simon , HAMBLIN, Julie, Nicole , JONES, Paul, Spencer , LE, Joelle , PARR, Nigel, James , RITCHIE, Timothy, John , ROBINSON, John, Edward , SIMPSON, Juliet, Kay , SMETHURST, Christian, Alan, Paul
IPC分类号： A61K31/416 , A61P11/00 , C07D403/04 , C07D403/14
CPC分类号： C07D403/04 , C07D401/14 , C07D403/14 , C07D413/14 , C07D471/04
摘要： The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.
摘要翻译：本发明涉及某些新化合物。具体地，本发明涉及式（I）的化合物及其盐。本发明的化合物是PI3-激酶活性的抑制剂。

5. 发明申请

WO2009050244A1 INDAZOLES AS GLUCOCORTICOID RECEPTOR LIGANDS 审中-公开
标题翻译： INDAZOLES作为糖皮质激素受体配体
公开(公告)号：WO2009050244A1
公开(公告)日：2009-04-23
申请号：PCT/EP2008/063986
申请日：2008-10-16
申请人： GLAXO GROUP LIMITED , BIGGADIKE, Keith , COOPER, Anthony, William, James , HOUSE, David , MCLAY, Iain, McFarlane , ROBINSON, John, Edward , WEINGARTEN, Gordon, Gad
发明人： BIGGADIKE, Keith , COOPER, Anthony, William, James , HOUSE, David , MCLAY, Iain, McFarlane , ROBINSON, John, Edward , WEINGARTEN, Gordon, Gad
IPC分类号： C07D231/56 , C07D401/12 , A61K31/416 , A61P11/06
CPC分类号： C07D231/56 , C07D401/12
摘要： The present invention provides compounds of formula (I), a process for their preparation, to pharmaceutical compositions comprising the compounds and the preparation of said compositions, to intermediates, and to use of the compounds for the manufacture of a medicament for therapeutic treatment, particularly for the treatment of inflammation and/or allergic conditions.
摘要翻译：本发明提供了式（I）的化合物，其制备方法，包含所述化合物和所述组合物的制备的药物组合物，中间体以及所述化合物用于制造用于治疗性治疗的药物，特别是用于治疗炎症和/或过敏性疾病。

6. 发明申请

WO2009050220A1 INDAZOLES AS GLUCOCORTICOID RECEPTOR LIGANDS 审中-公开
公开(公告)号：WO2009050220A1
公开(公告)日：2009-04-23
申请号：PCT/EP2008/063924
申请日：2008-10-16
申请人： GLAXO GROUP LIMITED , BIGGADIKE, Keith , COOPER, Anthony, William, James , HOUSE, David , MCLAY, Iain, McFarlane , ROBINSON, John, Edward , WELLER, Victoria
发明人： BIGGADIKE, Keith , COOPER, Anthony, William, James , HOUSE, David , MCLAY, Iain, McFarlane , ROBINSON, John, Edward , WELLER, Victoria
IPC分类号： C07D231/56 , C07D403/12 , C07D405/12 , C07D409/12 , A61K31/416 , A61P11/06
CPC分类号： C07D231/56 , C07D403/12 , C07D405/12 , C07D409/12
摘要： The present invention provides compounds of formula (I): a process for their preparation, to pharmaceutical compositions comprising the compounds and the preparation of said compositions, to intermediates, and to use of the compounds for the manufacture of a medicament for therapeutic treatment, particularly for the treatment of inflammation and/or allergic conditions.

7. 发明申请

WO2006097340A1 1,7-NAPHTHYRIDINES AS PDE4 INHIBITORS 审中-公开
标题翻译：作为PDE4抑制剂的1,7-萘啶
公开(公告)号：WO2006097340A1
公开(公告)日：2006-09-21
申请号：PCT/EP2006/002543
申请日：2006-03-16
申请人： GLAXO GROUP LIMITED , ELDRED, Colin, David , ROBINSON, John, Edward
发明人： ELDRED, Colin, David , ROBINSON, John, Edward
IPC分类号： C07D471/04 , A61K31/4375 , A61P29/00
CPC分类号： C07D471/04
摘要： There are provided according to the invention novel compounds of formula (I) and pharmaceutically acceptable salts and solvates thereof, wherein: R 1 is selected from the group consisting of C 1-4 alkyl, C 4-6 cycloalkyl(CH 2 ) m -, methoxyC 2-4 alkyl, HOCH 2 CH 2 -, R 3 (O) 2 S(CH 2 ) 2 -, R 5 R 4 NCO(CH 2 ) n -, and heterocyclyl(CH 2 ) m - wherein any nitrogen heteroatom of the heterocyclyl radical may be unsubstituted or substituted by methyl; R 2 is hydrogen or methyl; R 3 is methyl or NH 2 ; R 4-5 independently represent methyl; m is 0, 1 or 2; and n is 1 or 2; or R 1 and R 2 together with the nitrogen atom to which they are attached may form a heterocyclyl ring, which may be unsubstituted or substituted by one or two substituents selected from the group consisting of: methyl, =O and (CH 3 ) 2 N-.
摘要翻译：根据本发明提供新的式（I）化合物及其药学上可接受的盐和溶剂化物，其中：R 1选自C 1-4烷基烷基，C 4-6环烷基（CH 2）2 - ，甲氧基C 2-4 - 烷基，HOCH （O 2）2（CH 2）2， - - - - （CH 2））2 R 2 - ， - - - - - - - - - - - - - - - - - 和杂环基（CH 2 CH 2）m - ，其中杂环基的任何氮杂原子可以是未取代的或被甲基取代; R 2是氢或甲基; R 3是甲基或NH 2; R 4-5独立地表示甲基; m为0,1或2; n为1或2; 或R 1和R 2与它们所连接的氮原子一起可以形成杂环基环，其可以是未取代的或被一个或两个选自以下的取代基取代：由以下组成的组：甲基，= O和（CH 3 3）2 N。

8. 发明申请

WO2006053784A2 1,7-NAPHTHYRIDINES 审中-公开
标题翻译： 1,7-萘啶
公开(公告)号：WO2006053784A2
公开(公告)日：2006-05-26
申请号：PCT/EP2005/012462
申请日：2005-11-17
申请人： GLAXO GROUP LIMITED , ELDRED, Colin, David , ROBINSON, John, Edward , STEEL, Alison, Judith
发明人： ELDRED, Colin, David , ROBINSON, John, Edward , STEEL, Alison, Judith
IPC分类号： C07D471/04 , A61K31/4375 , A61P29/00
CPC分类号： C07D471/04
摘要： There are provided according to the invention novel compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof: (I) wherein: R 1 is phenyl which may be unsubstituted or substituted by one or two substituents selected from fluorine, chlorine, C 1-2 alkoxy-, -CN; phenyl fused to a 5-membered saturated ring containing one oxygen atom; pyridinyl which may be unsubstituted or substituted by one or two substituents selected from fluorine or chlorine; or C-linked pyrazolyl which may be unsubstituted or substituted by the substituent C 1-2 alkyl; R 2 is C 1-4 alkyl; R 3 is C 1-2 alkyl; and n is 0, 1 or 2.
摘要翻译：根据本发明提供新的式（I）化合物及其药学上可接受的盐和溶剂化物：（I）其中：R 1是可以是未被取代的或被一个或两个取代基所取代的苯基由氟，氯，C 1-2烷氧基 - ，-CN; 与含有一个氧原子的5元饱和环稠合的苯基; 吡啶基，其可以是未取代的或被一个或两个选自氟或氯的取代基取代; 或C连接的吡唑基，其可以是未取代的或被取代基C 1-12烷基取代; R 2是C 1-4烷基; R 3是C 1-12烷基; n为0,1或2。

9. 发明申请

WO2003097618A1 MORPHOLINYLMETHYLUREAS CCR-3 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：吗啉代甲基CCR-3受体拮抗剂
公开(公告)号：WO2003097618A1
公开(公告)日：2003-11-27
申请号：PCT/EP2003/005446
申请日：2003-05-20
申请人： GLAXO GROUP LIMITED , DOWLE, Michael, Dennis , GORE, Paul, Martin , HODGSON, Simon, Teanby , JOHNSON, Martin, Redpath , JUDD, Duncan, Bruce , REDFERN, Tracy, Jane , ROBINSON, John, Edward , SWANSON, Stephen , TRIVEDI, Naimisha
发明人： DOWLE, Michael, Dennis , GORE, Paul, Martin , HODGSON, Simon, Teanby , JOHNSON, Martin, Redpath , JUDD, Duncan, Bruce , REDFERN, Tracy, Jane , ROBINSON, John, Edward , SWANSON, Stephen , TRIVEDI, Naimisha
IPC分类号： C07D265/30
CPC分类号： C07D265/30 , C07D265/36 , C07D267/10 , C07D279/12 , C07D417/12
摘要： Compounds of formula (I'): (I); wherein: R 1 represents substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl; X represents -(CR ka R kb ) k -; R ka and R kb are each independently hydrogen or C 1-6 alkyl; k is 0-5; Y represents -NR 3 - or a bond; R 3 represents hydrogen or C 1-6 alkyl; Z represents a moiety of formula (ZA), (ZB), (ZC), (ZD), (ZE), or (ZF); A represents -(CR ja R jb ) j -; R ja and R jb are each independently hydrogen or C 1-6 alkyl; j is 0, 1 or 2, and; R 2 represents unsubstituted or substituted aryl; and salts and solvates thereof are CCR3 receptor antagonists and are thus indicated to be useful in therapy.
摘要翻译：式（I'）化合物：（I）; 其中：R 1表示取代或未取代的芳基或取代或未取代的杂芳基; X表示 - （CRkaRkb）k-; Rka和Rkb各自独立地为氢或C 1-6烷基; k为0-5; Y表示-NR 3 - 或键; R 3表示氢或C 1-6烷基; Z表示式（ZA），（ZB），（ZC），（ZD），（ZE）或（ZF）的部分; A表示 - （CRjaRjb）j-; Rja和Rjb各自独立地为氢或C 1-6烷基; j为0,1或2， R2表示未取代或取代的芳基; 其盐和溶剂化物是CCR3受体拮抗剂，因此被认为可用于治疗。

10. 发明申请

WO1995007910A1 ANTIVIRAL INDOLE DERIVATIVES 审中-公开
标题翻译：抗病毒药物衍生物
公开(公告)号：WO1995007910A1
公开(公告)日：1995-03-23
申请号：PCT/GB1994002016
申请日：1994-09-16
申请人： THE WELLCOME FOUNDATION LIMITED , SLATER, Martin, John , COCKERILL, George, Stuart , ROBINSON, John, Edward
发明人： THE WELLCOME FOUNDATION LIMITED
IPC分类号： C07D471/22
CPC分类号： C07D471/22
摘要： Compounds of formula (I), in which R and R , which may be the same or different, each together with the carbon atoms to which they are attached form an unsaturated 6-membered carbocyclic ring in which from 1 to 3 carbon atom(s) may be replaced by nitrogen atom(s), providing that at least one ring structure contains at least one nitrogen atom, and their use for the treatment or prophylaxis of viral infections.
摘要翻译：其中R 8和R 9可以相同或不同的式（I）化合物与它们所连接的碳原子一起形成不饱和的6-元碳环，其中1 至少3个碳原子可被氮原子取代，条件是至少一个环结构含有至少一个氮原子，以及它们用于治疗或预防病毒感染的用途。

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