公开(公告)号：WO2003082861A3

公开(公告)日：2003-10-09

申请号：PCT/EP2003/003335

申请日：2003-03-27

Applicant: GLAXO GROUP LIMITED ,  ANCLIFF, Rachael, Ann ,  COOK, Caroline, Mary ,  ELDRED, Colin, David ,  GORE, Paul, Martin ,  HARRISON, Lee, Andrew ,  HAYES, Martin, Alistair ,  HODGSON, Simon, Teanby ,  JUDD, Duncan, Bruce ,  KEELING, Suzanne, Elaine ,  LEWELL, Xiao, Qing ,  MILLS, Gail ,  ROBERTSON, Graeme, Michael ,  SWANSON, Stephen ,  WALKER, Andrew, John ,  WILKINSON, Mark

Inventor： ANCLIFF, Rachael, Ann ,  COOK, Caroline, Mary ,  ELDRED, Colin, David ,  GORE, Paul, Martin ,  HARRISON, Lee, Andrew ,  HAYES, Martin, Alistair ,  HODGSON, Simon, Teanby ,  JUDD, Duncan, Bruce ,  KEELING, Suzanne, Elaine ,  LEWELL, Xiao, Qing ,  MILLS, Gail ,  ROBERTSON, Graeme, Michael ,  SWANSON, Stephen ,  WALKER, Andrew, John ,  WILKINSON, Mark

IPC: C07D413/12

Abstract: Compounds of formula (I) wherein: R1 represents substituted or unsubstituted heteroaryl; Y represents -(CRnaRnb)n-; Rna and Rnb are each independently hydrogen or C1-6alkyl; n is an integer from 0 to 5;R2 represents unsubstituted or substituted aryl or unsubstituted or substituted heteroaryl; R3 and R4 each independently represent hydrogen or C1-6alkyl; R7 represents hydrogen or C1-6alkyl; R8 represents hydrogen or C1-6alkyl;and salts and solvates thereof;are CCR3 antagonists and are thus indicated to be useful in therapy.

公开(公告)号：WO2003082295A1

公开(公告)日：2003-10-09

申请号：PCT/EP2003/003349

申请日：2003-03-27

Applicant: GLAXO GROUP LIMITED ,  ANCLIFF, Rachael, Ann ,  COOK, Caroline, Mary ,  ELDRED, Colin, David ,  GORE, Paul, Martin ,  HARRISON, Lee, Andrew ,  HAYES, Martin, Alistair ,  HODGSON, Simon, Teanby ,  JUDD, Duncan, Bruce ,  KEELING, Suzanne, Elaine ,  LEWELL, Xiao, Qing ,  MILLS, Gail ,  ROBERTSON, Graeme, Michael ,  SWANSON, Stephen ,  WALKER, Andrew, John ,  WILKINSON, Mark

Inventor： ANCLIFF, Rachael, Ann ,  COOK, Caroline, Mary ,  ELDRED, Colin, David ,  GORE, Paul, Martin ,  HARRISON, Lee, Andrew ,  HAYES, Martin, Alistair ,  HODGSON, Simon, Teanby ,  JUDD, Duncan, Bruce ,  KEELING, Suzanne, Elaine ,  LEWELL, Xiao, Qing ,  MILLS, Gail ,  ROBERTSON, Graeme, Michael ,  SWANSON, Stephen ,  WALKER, Andrew, John ,  WILKINSON, Mark

IPC: A61K31/5377

CPC classification number: C07D265/30 ,  C07D413/12

Abstract: Certain compounds of formula (I): wherein: R 1 represents substituted or unsubstituted heterocyciyl; Y represents -(CR na R nb ) n -; R na and R nb are each independently hydrogen or C 1-6 alkyl; n is an integer from 1 to 5; R 2 represents unsubstituted or substituted aryl or unsubstituted or substituted, heteroaryl; R 3 and R 4 each independently represent hydrogen or C 1-6 alkyl; and salts and solvates thereof are CCR-3. antagonists and thus are indicated to be useful in therapy of inflammatory conditions.

Abstract translation: 某些式（I）化合物：其中：R 1表示取代或未取代的杂环基; Y表示 - （CRnaRnb）n-; Rna和Rnb各自独立地为氢或C 1-6烷基; n为1〜5的整数; R 2表示未取代或取代的芳基或未取代或取代的杂芳基; R 3和R 4各自独立地表示氢或C 1-6烷基; 其盐和溶剂合物是CCR-3。 拮抗剂，因此被认为可用于治疗炎性病症。

公开(公告)号：WO1998028319A1

公开(公告)日：1998-07-02

申请号：PCT/EP1997007197

申请日：1997-12-22

Applicant: GLAXO GROUP LIMITED ,  COX, Brian ,  KEELING, Suzanne, Elaine ,  ALLEN, David, George ,  REDGRAVE, Alison, Judith ,  BARKER, Michael, David ,  HOBBS, Heather ,  ROPER, Thomas, Davis, IV ,  GEDEN, Joanna, Victoria

Inventor： GLAXO GROUP LIMITED

IPC: C07H19/167

CPC classification number: C07D473/00 ,  C07H19/16 ,  Y10S514/826 ,  Y10S514/851 ,  Y10S514/885 ,  Y10S514/921 ,  Y10S514/925

Abstract: There are provided according to the invention novel compounds of formula (I) wherein R , R and R are as described in the specification, processes for preparing them, formulations containing them and their use in therapy for the treatment of inflammatory diseases.

Abstract translation: 根据本发明提供了新的式（I）化合物，其中R 1，R 2和R 3如说明书中所述，其制备方法，含有它们的制剂及其在治疗中的用途 治疗炎症性疾病。

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：WO2003082863A1

公开(公告)日：2003-10-09

申请号：PCT/EP2003/003350

申请日：2003-03-27

Applicant: GLAXO GROUP LIMITED ,  ANCLIFF, Rachael, Ann ,  COOK, Caroline, Mary ,  ELDRED, Colin, David ,  GORE, Paul, Martin ,  HARRISON, Lee, Andrew ,  HAYES, Martin, Alistair ,  HODGSON, Simon, Teanby ,  JUDD, Duncan, Bruce ,  KEELING, Suzanne, Elaine ,  LEWELL, Xiao, Qing ,  MILLS, Gail ,  ROBERTSON, Graeme, Michael ,  SWANSON, Stephen ,  WALKER, Andrew, John ,  WILKINSON, Mark

Inventor： ANCLIFF, Rachael, Ann ,  COOK, Caroline, Mary ,  ELDRED, Colin, David ,  GORE, Paul, Martin ,  HARRISON, Lee, Andrew ,  HAYES, Martin, Alistair ,  HODGSON, Simon, Teanby ,  JUDD, Duncan, Bruce ,  KEELING, Suzanne, Elaine ,  LEWELL, Xiao, Qing ,  MILLS, Gail ,  ROBERTSON, Graeme, Michael ,  SWANSON, Stephen ,  WALKER, Andrew, John ,  WILKINSON, Mark

IPC: C07D413/12

CPC classification number: C07D413/12

Abstract: Compounds of formula (I); wherein: R 1 represents substituted or unsubstituted heterocyclyl; Y represents -(CR na R nb ) n -; R na and R nb are each independently hydrogen or C 1-6 alkyl; n is an integer from 1 to 5; R 2 represents unsubstituted or substituted aryl or unsubstituted or substituted heteroaryl; R 3 represents hydrogen or C 1-6 alkyl; and salts and solvates thereof are CCR-3 antagonists and are thus indicated to be useful in therapy.

Abstract translation: 式（I）化合物; 其中：R 1表示取代或未取代的杂环基; Y表示 - （CRnaRnb）n-; Rna和Rnb各自独立地为氢或C 1-6烷基; n为1〜5的整数; R 2表示未取代或取代的芳基或未取代或取代的杂芳基; R 3表示氢或C 1-6烷基; 其盐和溶剂合物是CCR-3拮抗剂，因此被认为可用于治疗。

公开(公告)号：WO2003082294A1

公开(公告)日：2003-10-09

申请号：PCT/EP2003/003348

申请日：2003-03-27

Applicant: GLAXO GROUP LIMITED ,  ANCLIFF, Rachael, Ann ,  COOK, Caroline, Mary ,  ELDRED, Colin, David ,  GORE, Paul, Martin ,  HARRISON, Lee, Andrew ,  HAYES, Martin, Alistair ,  HODGSON, Simon, Teanby ,  JUDD, Duncan, Bruce ,  KEELING, Suzanne, Elaine ,  LEWELL, Xiao, Qing ,  MILLS, Gail ,  ROBERTSON, Graeme, Michael ,  SWANSON, Stephen ,  WALKER, Andrew, John ,  WILKINSON, Mark

Inventor： ANCLIFF, Rachael, Ann ,  COOK, Caroline, Mary ,  ELDRED, Colin, David ,  GORE, Paul, Martin ,  HARRISON, Lee, Andrew ,  HAYES, Martin, Alistair ,  HODGSON, Simon, Teanby ,  JUDD, Duncan, Bruce ,  KEELING, Suzanne, Elaine ,  LEWELL, Xiao, Qing ,  MILLS, Gail ,  ROBERTSON, Graeme, Michael ,  SWANSON, Stephen ,  WALKER, Andrew, John ,  WILKINSON, Mark

IPC: A61K31/5377

CPC classification number: C07D209/48 ,  C07D265/30 ,  C07D413/06 ,  C07D413/12

Abstract: Certain compounds of formula (I); wherein R 1 represents substituted or unsubstituted aryl; X represents -O- or a bond; Y represents -(CR na ,R nb ) n-; R na and R nb are each independently hydrogen or C 1-6 alkyl; n is an integer from 1 to 5; R 2 represents unsubstituted or substituted aryl or unsubstituted or substituted heteroaryl; R 3 represents hydrogen or C 1 - 6 alkyl; R 10 represents hydrogen or C 1-6 alkyl; and salts and solvates thereof are CCR3 antagonists and are therefore indicated to be useful in therapy of inflammatory conditions.

Abstract translation: 某些式（I）化合物; 其中R1表示取代或未取代的芳基; X表示-O-或键; Y表示 - （CRna，Rnb）n-; Rna和Rnb各自独立地为氢或C 1-6烷基; n为1〜5的整数; R 2表示未取代或取代的芳基或未取代或取代的杂芳基; R 3表示氢或C 1-6烷基; R 10表示氢或C 1-6烷基; 其盐和溶剂合物是CCR3拮抗剂，因此被认为可用于治疗炎性病症。

公开(公告)号：WO1996002553A2

公开(公告)日：1996-02-01

申请号：PCT/EP1995002837

申请日：1995-07-14

Applicant: GLAXO GROUP LIMITED ,  AYRES, Diana, Sally +hf ,  GREGSON, Michael ,  EWAN, George, Blanch ,  KEELING, Suzanne, Elaine ,  BELL, Richard

Inventor： GLAXO GROUP LIMITED ,  AYRES, Diana, Sally +hf ,  AYRES, Barry, Edward +di

IPC: C07H19/067

CPC classification number: C07H19/16

Abstract: Amino purine- beta -D-ribofuranuronamide derivatives are described having general formula (I) and salts and solvates thereof, wherein: R is hydrogen, C3-8cycloaklyl or C1-6alkyl; A represents O, S, SO, SO2, a saturated hydrocarbon moiety having from 1 to 4 carbon atoms or an unsaturated hydrocarbon moiety having from 2 to 4 carbon atoms; R is C3-8cycloalkyl, C3-8cycloalkyl C1-6alkyl, Alk1Y, -(CHR )m (Alk2)nZ or appropriately substituted C3-8cycloalkyl, C3-8cycloalkylC1-6alkyl, pyrrolidin-3-yl, 2-oxopyrrolidin-4-yl, 2-oxopyrrolidin-5-yl, piperidin-3-yl or piperidin-4-yl, and Q is oxygen or sulphur with the proviso that when A represents O, S, SO or SO2, Alk1 represents a C2-6alkylene group. Compounds of formula (I) and their salts and solvates have use in medicine as anti-inflammatory agents, particularly in the treatment of patients with inflammatory conditions who are susceptible to leukocyte-induced tissue damage.

Abstract translation: 描述了具有通式（I）的氨基嘌呤-β-D-呋喃核糖脲衍生物及其盐和溶剂化物，其中：R 1是氢，C 3-8环基或C 1-6烷基; A表示O，S，SO，SO 2，具有1至4个碳原子的饱和烃部分或具有2至4个碳原子的不饱和烃部分; R 2是C 3-8环烷基，C 3-8环烷基C 1-6烷基，Alk 1 Y， - （CHR 5）m（Alk 2）n Z或适当取代的C 3-8环烷基，C 3-8环烷基C 1-6烷基，吡咯烷-3-基，2 - 氧代吡咯烷-4-基，2-氧代吡咯烷-5-基，哌啶-3-基或哌啶-4-基，Q为氧或硫，条件是当A表示O，S，SO或SO 2时，Alk1表示 C2-6亚烷基。 式（I）化合物及其盐和溶剂合物在药物中用作抗炎剂，特别是在治疗易受白细胞诱导的组织损伤的炎性病症的患者中。

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：WO2003082861A2

公开(公告)日：2003-10-09

申请号：PCT/EP2003/003335

申请日：2003-03-27

Applicant: GLAXO GROUP LIMITED ,  ANCLIFF, Rachael, Ann ,  COOK, Caroline, Mary ,  ELDRED, Colin, David ,  GORE, Paul, Martin ,  HARRISON, Lee, Andrew ,  HAYES, Martin, Alistair ,  HODGSON, Simon, Teanby ,  JUDD, Duncan, Bruce ,  KEELING, Suzanne, Elaine ,  LEWELL, Xiao, Qing ,  MILLS, Gail ,  ROBERTSON, Graeme, Michael ,  SWANSON, Stephen ,  WALKER, Andrew, John ,  WILKINSON, Mark

Inventor： ANCLIFF, Rachael, Ann ,  COOK, Caroline, Mary ,  ELDRED, Colin, David ,  GORE, Paul, Martin ,  HARRISON, Lee, Andrew ,  HAYES, Martin, Alistair ,  HODGSON, Simon, Teanby ,  JUDD, Duncan, Bruce ,  KEELING, Suzanne, Elaine ,  LEWELL, Xiao, Qing ,  MILLS, Gail ,  ROBERTSON, Graeme, Michael ,  SWANSON, Stephen ,  WALKER, Andrew, John ,  WILKINSON, Mark

IPC: C07D413/12

CPC classification number: C07D413/12 ,  C07D413/14 ,  C07D417/12

Abstract: Compounds of formula (I) wherein: R1 represents substituted or unsubstituted heteroaryl; Y represents -(CRnaRnb)n-; Rna and Rnb are each independently hydrogen or C1-6alkyl; n is an integer from 0 to 5;R2 represents unsubstituted or substituted aryl or unsubstituted or substituted heteroaryl; R3 and R4 each independently represent hydrogen or C1-6alkyl; R7 represents hydrogen or C1-6alkyl; R8 represents hydrogen or C1-6alkyl;and salts and solvates thereof;are CCR3 antagonists and are thus indicated to be useful in therapy.

Abstract translation: 式（I）化合物，其中：R 1表示取代或未取代的杂芳基; Y表示 - （CRnaRnb）n-; Rna和Rnb各自独立地为氢或C 1-6烷基; n为0至5的整数; R 2表示未取代或取代的芳基或未取代或取代的杂芳基; R 3和R 4各自独立地表示氢或C 1-6烷基; R 7表示氢或C 1-6烷基; R8表示氢或C1-6烷基;其盐和溶剂合物;是CCR3拮抗剂，因此被认为可用于治疗。