公开(公告)号：WO2010125082A1

公开(公告)日：2010-11-04

申请号：PCT/EP2010/055666

申请日：2010-04-28

Applicant: GLAXO GROUP LIMITED ,  HAMBLIN, Julie, Nicole ,  JONES, Paul, Spencer ,  KEELING, Suzanne, Elaine ,  LE, Joelle ,  MITCHELL, Charlotte, Jane ,  PARR, Nigel, James

Inventor： HAMBLIN, Julie, Nicole ,  JONES, Paul, Spencer ,  KEELING, Suzanne, Elaine ,  LE, Joelle ,  MITCHELL, Charlotte, Jane ,  PARR, Nigel, James

IPC: C07D413/14 ,  A61K31/422 ,  A61K31/4439 ,  A61P35/00 ,  A61P37/00 ,  A61P11/00 ,  A61P31/12

CPC classification number: A61K31/5377 ,  A61K31/496 ,  A61K31/497 ,  A61K31/535 ,  A61K45/06 ,  C07B2200/13 ,  C07D413/14 ,  Y02A50/409

Abstract: 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 kinase activity, in particular PI3-kinase activity.

Abstract translation: 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。 本发明的化合物是激酶活性抑制剂，特别是PI3-激酶活性。

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

Applicant: 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

Inventor： 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: A61K31/416 ,  A61P11/00 ,  C07D403/04 ,  C07D403/14

CPC classification number: C07D403/04 ,  C07D401/14 ,  C07D403/14 ,  C07D413/14 ,  C07D471/04

Abstract: 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.

Abstract translation: 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。

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

Applicant: 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

Inventor： 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: C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04 ,  A61K31/416 ,  A61P11/00

CPC classification number: C07D487/04 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D417/04 ,  C07D471/04

Abstract: 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.

Abstract translation: 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。

公开(公告)号：WO2005073232A1

公开(公告)日：2005-08-11

申请号：PCT/GB2005/000274

申请日：2005-01-27

Applicant: SMITHKLINE BEECHAM CORPORATION ,  BARKER, Michael, David ,  HAMBLIN, Julie, Nicole ,  JONES, Katherine, Louise ,  PATEL, Vipulkumar, Kantibhai ,  SWANSON, Stephen ,  WALKER, Ann, Louise

Inventor： BARKER, Michael, David ,  HAMBLIN, Julie, Nicole ,  JONES, Katherine, Louise ,  PATEL, Vipulkumar, Kantibhai ,  SWANSON, Stephen ,  WALKER, Ann, Louise

IPC: C07D471/04

CPC classification number: C07D471/04

Abstract: Compounds of Formula: (I) are inhibitors of p38 kinase and are useful in the treatment of conditions or disease states mediated by p38 kinase activity or mediated by cytokines produced by the activity of p38.

Abstract translation: 式（I）化合物是p38激酶的抑制剂，可用于治疗由p38激酶活性介导的或由p38活性产生的细胞因子介导的病状或疾病状态。

公开(公告)号：WO2004024728A3

公开(公告)日：2004-10-21

申请号：PCT/EP0311814

申请日：2003-09-12

Applicant: GLAXO GROUP LTD ,  ALLEN DAVID GEORGE ,  COE DIANE MARY ,  COOK CAROLINE MARY ,  DOWLE MICHAEL DENNIS ,  EDLIN CHRISTOPHER DAVID ,  HAMBLIN JULIE NICOLE ,  JOHNSON MARTIN REDPATH ,  JONES PAUL SPENCER ,  KNOWLES RICHARD GRAHAM ,  LINDVALL MIKA KRISTIAN ,  MITCHELL CHARLOTTE JANE ,  REDGRAVE ALISON JUDITH ,  TRIVEDI NAIMISHA ,  WARD PETER

Inventor： ALLEN DAVID GEORGE ,  COE DIANE MARY ,  COOK CAROLINE MARY ,  DOWLE MICHAEL DENNIS ,  EDLIN CHRISTOPHER DAVID ,  HAMBLIN JULIE NICOLE ,  JOHNSON MARTIN REDPATH ,  JONES PAUL SPENCER ,  KNOWLES RICHARD GRAHAM ,  LINDVALL MIKA KRISTIAN ,  MITCHELL CHARLOTTE JANE ,  REDGRAVE ALISON JUDITH ,  TRIVEDI NAIMISHA ,  WARD PETER

IPC: A61K31/437 ,  A61P11/00 ,  A61P29/00 ,  C07D221/00 ,  C07D231/00 ,  C07D471/04

CPC classification number: C07D471/04

Abstract: The invention relates to a compound of formula (I) or a salt thereof: wherein:R1 is C1-4alkyl, C1-3fluoroalkyl, -CH2CH2OH or -CH2CH2CO2C1-2alkyl;R2 is a hydrogen atom (H), methyl or C1fluoroalkyl;R3 is optionally substituted C3-8cycloalkyl or optionally substituted mono-unsaturated-C5-7cycloalkenyl or an optionally substituted heterocyclic group of sub-formula (aa), (bb) or (cc); in which n1 and n2 independently are 1 or 2; and in which Y is O, S, SO2, or NR10; or R3 is a bicyclic group (dd) or (ee): ; and wherein X is NR4R5 or OR5a. The compounds are phosphodiesterase (PDE) inhibitors, in particular PDE4 inhibitors. Also provided is the use of a compound of formula (I), or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for the treatment and/or prophylaxis of an inflammatory and/or allergic disease in a mammal such as a human, for example chronic obstructive pulmonary disease (COPD), asthma, or allergic rhinitis.

Abstract translation: 本发明涉及式（I）化合物或其盐：其中：R 1为C 1-4烷基，C 1-3氟烷基，-CH 2 CH 2 OH或-CH 2 CH 2 CO 2 C 1-2烷基; R 2为氢原子（H），甲基或C 1-3氟烷基; （aa），（bb）或（cc）的任选取代的C 3-8环烷基或任选取代的单不饱和-C 5-7环烯基或任选取代的杂环基; 其中n1和n2独立地为1或2; 并且其中Y是O，S，SO 2或NR 10; 或R3是双环基团（dd）或（ee）： 并且其中X是NR 4 R 5或OR 5 a。 这些化合物是磷酸二酯酶（PDE）抑制剂，特别是PDE4抑制剂。 还提供了式（I）化合物或其药学上可接受的盐在制备用于治疗和/或预防哺乳动物例如人的炎症和/或过敏性疾病的药物中的用途， 例如慢性阻塞性肺病（COPD），哮喘或过敏性鼻炎。

公开(公告)号：WO2003022841A1

公开(公告)日：2003-03-20

申请号：PCT/AU2002/001187

申请日：2002-08-30

Applicant: BIOTA SCIENTIFIC MANAGEMENT PTY LTD ,  JUDKINS, Brian, David ,  MACDONALD, Simon, John Fawcett ,  DEMAINE, Derek, Anthony ,  INGLIS, Graham, George Adam ,  HAMBLIN, Julie, Nicole

Inventor： JUDKINS, Brian, David ,  MACDONALD, Simon, John Fawcett ,  DEMAINE, Derek, Anthony ,  INGLIS, Graham, George Adam ,  HAMBLIN, Julie, Nicole

IPC: C07D407/06

CPC classification number: C07D407/06 ,  C07D309/28 ,  Y02P20/55

Abstract: Compounds of formula (I), methods for their preparation and their use in the manufacture of neuraminidase inhibitor conjugates. Wherein R represents as carboxylic acid protecting group; P 1 and P 2 can be the same or different and are selected from amine protecting groups; P 3 represents a protecting group for 1, 2 diols; and LG represents a leaving group.

Abstract translation: 式（I）的化合物，其制备方法及其在制备神经氨酸酶抑制剂缀合物中的用途。 其中R表示羧酸保护基; P1和P2可以相同或不同，并且选自胺保护基; P3表示1,2二醇的保护基; LG代表离职团体。

公开(公告)号：WO2002100830A1

公开(公告)日：2002-12-19

申请号：PCT/GB2002/002721

申请日：2002-06-06

Applicant: GLAXO GROUP LIMITED ,  CHAN, Chuen ,  HAMBLIN, Julie, Nicole ,  KELLY, Henry, Anderson ,  KING, Nigel, Paul ,  MASON, Andrew, McMurtrie ,  PATEL, Vipulkumar, Kantibhai ,  SENGER, Stefan ,  SHAH, Gita, Punjabhai ,  WATSON, Nigel, Stephen ,  WESTON, Helen, Elisabeth ,  WHITWORTH, Caroline ,  YOUNG, Robert, John

Inventor： CHAN, Chuen ,  HAMBLIN, Julie, Nicole ,  KELLY, Henry, Anderson ,  KING, Nigel, Paul ,  MASON, Andrew, McMurtrie ,  PATEL, Vipulkumar, Kantibhai ,  SENGER, Stefan ,  SHAH, Gita, Punjabhai ,  WATSON, Nigel, Stephen ,  WESTON, Helen, Elisabeth ,  WHITWORTH, Caroline ,  YOUNG, Robert, John

IPC: C07D207/26

CPC classification number: C07D413/14 ,  A61K31/5377 ,  C07D207/12 ,  C07D413/06 ,  C07D417/14 ,  C07D495/04

Abstract: The invention relates to compounds of formula (I) which processes for their preparation, pharmaceutical compositions containing them and to their use in medicine, particularly use in the amelioration of a clinical condition for which a Factor Xa inhibitor is indicated.

Abstract translation: 本发明涉及其制备方法的式（I）化合物，含有它们的药物组合物及其在医药中的用途，特别是用于改善指示因子Xa抑制剂的临床病症。

公开(公告)号：WO2012032065A1

公开(公告)日：2012-03-15

申请号：PCT/EP2011/065417

申请日：2011-09-06

Applicant: GLAXO GROUP LIMITED ,  BALDWIN, Ian Robert ,  DOWN, Kenneth David ,  FAULDER, Paul ,  GAINES, Simon ,  HAMBLIN, Julie Nicole ,  HARRISON, Zoe Alicia ,  JONES, Katherine Louise ,  JONES, Paul Spencer ,  KEELING, Suzanne Elaine ,  LE, Joelle ,  LUNNISS, Christopher James ,  MITCHELL, Charlotte Jane ,  PARR, Nigel James ,  RITCHIE, Timothy John ,  ROBINSON, John Edward ,  SIMPSON, Juliet Kay ,  SMETHURST, Christian Alan Paul ,  WASHIO, Yoshiaki

Inventor： BALDWIN, Ian Robert ,  DOWN, Kenneth David ,  FAULDER, Paul ,  GAINES, Simon ,  HAMBLIN, Julie Nicole ,  HARRISON, Zoe Alicia ,  JONES, Katherine Louise ,  JONES, Paul Spencer ,  KEELING, Suzanne Elaine ,  LE, Joelle ,  LUNNISS, Christopher James ,  MITCHELL, Charlotte Jane ,  PARR, Nigel James ,  RITCHIE, Timothy John ,  ROBINSON, John Edward ,  SIMPSON, Juliet Kay ,  SMETHURST, Christian Alan Paul ,  WASHIO, Yoshiaki

IPC: A61K31/416 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/5386 ,  A61P31/16

CPC classification number: A61K31/5377 ,  A61K31/416 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5386 ,  C07D413/14

Abstract: The present invention is directed to indazole compounds for use in the treatment or prevention of influenza virus infection.

Abstract translation: 本发明涉及用于治疗或预防流感病毒感染的吲唑化合物。

公开(公告)号：WO2010102958A1

公开(公告)日：2010-09-16

申请号：PCT/EP2010/052835

申请日：2010-03-05

Applicant: GLAXO GROUP LIMITED ,  HAMBLIN, Julie, Nicole ,  HARRISON, Zoe, Alicia ,  JONES, Paul, Spencer ,  KEELING, Suzanne, Elaine ,  LE, Joelle ,  LUNNISS, Christopher, James ,  PARR, Nigel, James

Inventor： HAMBLIN, Julie, Nicole ,  HARRISON, Zoe, Alicia ,  JONES, Paul, Spencer ,  KEELING, Suzanne, Elaine ,  LE, Joelle ,  LUNNISS, Christopher, James ,  PARR, Nigel, James

IPC: C07D413/14 ,  C07D487/04 ,  C07D487/08 ,  A61K31/4245 ,  A61P11/06 ,  A61P37/08 ,  A61P19/02 ,  A61P29/00 ,  A61P35/00

CPC classification number: C07D413/14 ,  C07D487/04 ,  C07D487/08

Abstract: 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 kinase activity, in particular PI3-kinase activity.

Abstract translation: 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。 本发明的化合物是激酶活性的抑制剂，特别是PI3-激酶活性。

公开(公告)号：WO2009147190A1

公开(公告)日：2009-12-10

申请号：PCT/EP2009/056841

申请日：2009-06-03

Applicant: GLAXO GROUP LIMITED ,  BALDWIN, Ian, Robert ,  DOWN, Kenneth, David ,  FAULDER, Paul ,  GAINES, Simon ,  HAMBLIN, Julie, Nicole ,  LE, Joelle ,  LUNNISS, Christopher, James ,  PARR, Nigel, James ,  RITCHIE, Timothy, John ,  SIMPSON, Juliet, Kay ,  SMETHURST, Christian, Alan, Paul

Inventor： BALDWIN, Ian, Robert ,  DOWN, Kenneth, David ,  FAULDER, Paul ,  GAINES, Simon ,  HAMBLIN, Julie, Nicole ,  LE, Joelle ,  LUNNISS, Christopher, James ,  PARR, Nigel, James ,  RITCHIE, Timothy, John ,  SIMPSON, Juliet, Kay ,  SMETHURST, Christian, Alan, Paul

IPC: C07D401/14 ,  C07D471/04 ,  A61K31/404 ,  A61K31/437 ,  A61P11/06

CPC classification number: C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04

Abstract: 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.

Abstract translation: 本发明涉及某些新型化合物。 具体而言，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。