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1. 发明申请

WO2007085540A1 1H-INDAZ0L-4-YL-2 , 4-PYRIMIDINEDIAMINE DERIVATIVES 审中-公开
标题翻译： 1H-INDAZ0L-4-YL-2，4-PYRIMININEDIAMINE DERIVATIVES
公开(公告)号：WO2007085540A1
公开(公告)日：2007-08-02
申请号：PCT/EP2007/050309
申请日：2007-01-12
申请人： GLAXO GROUP LIMITED , ATKINSON, Francis, Louis , CAMPOS, Sebastien, Andre , HARRISON, Lee, Andrew , PARR, Nigel, James , PATEL, Vipulkumar, Kantibhai , VITULLI, Giovanni
发明人： ATKINSON, Francis, Louis , CAMPOS, Sebastien, Andre , HARRISON, Lee, Andrew , PARR, Nigel, James , PATEL, Vipulkumar, Kantibhai , VITULLI, Giovanni
IPC分类号： C07D417/14 , A61K31/506 , C07D403/14 , C07D413/14 , C07D401/14 , C07D405/14 , C07D409/14
CPC分类号： C07D417/14 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要： Compounds of formula (I): or a salt or solvate, preferably a pharmaceutically acceptable salt or solvate, thereof; are useful as inhibitors of Syk kinase and thus useful in treating diseases resulting from inappropriate mast cell activation, for instance allergic and inflammatory diseases.
摘要翻译：式（I）化合物或其盐或溶剂合物，优选其药学上可接受的盐或溶剂合物; 可用作Syk激酶的抑制剂，因此可用于治疗由不适当的肥大细胞活化引起的疾病，例如过敏性和炎性疾病。

2. 发明申请

WO2003082861A3 MORPHOLINYL-UREA DERIVATIVES FOR USE OF THE TREATMENT OF INFLAMMATORY DISEASES 审中-公开
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
申请人： 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
发明人： 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分类号： C07D413/12
摘要： 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.

3. 发明申请

WO2003082295A1 MORPHOLINE DERIVATIVES SUBSTITUTED AT THE 2-POSITION BY A HETEROCYCLYLALKYLUREA GROUP FOR USE AS CCR-3 ANTAGONISTS IN THE TREATMENT OF INFLAMMATORY CONDITIONS 审中-公开
标题翻译：通过在治疗炎症条件下作为CCR-3拮抗剂使用的间苯二酚基团在2位置取代的吗啉衍生物
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
申请人： 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
发明人： 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分类号： A61K31/5377
CPC分类号： C07D265/30 , C07D413/12
摘要： 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.
摘要翻译：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。

4. 发明申请

WO2007028445A1 6-INDOLYL-4-YL-AMINO-5-HALOGENO-2-PYRIMIDINYL-AMINO DERIVATIVES 审中-公开
标题翻译： 6-吲哚基-4-氨基氨基-5-苯基-2-吡啶基氨基衍生物
公开(公告)号：WO2007028445A1
公开(公告)日：2007-03-15
申请号：PCT/EP2006/006952
申请日：2006-07-13
申请人： GLAXO GROUP LIMITED , ATKINSON, Francis, Louis , BARKER, Michael, David , CAMPOS, Sebastien, Andre , HARRISON, Lee, Andrew , PARR, Nigel, James , PATEL, Vipulkumar, Kantibhai
发明人： ATKINSON, Francis, Louis , BARKER, Michael, David , CAMPOS, Sebastien, Andre , HARRISON, Lee, Andrew , PARR, Nigel, James , PATEL, Vipulkumar, Kantibhai
IPC分类号： C07D403/14 , C07D413/14 , C07D403/12 , C07D409/14 , C07D417/14 , C07D401/14 , A61K31/506
CPC分类号： C07D401/14 , C07D403/12 , C07D403/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： Bis Anilinopyrimidine compounds of formula (I) are useful as inhibitors of Syk kinase and thus useful in treating diseases resulting from inappropriate mast cell activation, for instance allergic and inflammatory diseases.
摘要翻译：式（I）的双苯胺基嘧啶化合物可用作Syk激酶的抑制剂，因此可用于治疗由不适当的肥大细胞活化引起的疾病，例如过敏性和炎性疾病。

5. 发明申请

WO2003099287A1 MORPHOLIN-ACETAMIDE DERIVATIVES FOR THE TREATMENT OF INFLAMMATORY DISEASES 审中-公开
标题翻译：用于治疗炎症性疾病的吗啉 - 乙酰胺衍生物
公开(公告)号：WO2003099287A1
公开(公告)日：2003-12-04
申请号：PCT/EP2003/005717
申请日：2003-05-27
申请人： GLAXO GROUP LIMITED , COOK, Caroline, Mary , ELDRED, Colin, David , HARRISON, Lee, Andrew
发明人： COOK, Caroline, Mary , ELDRED, Colin, David , HARRISON, Lee, Andrew
IPC分类号： A61K31/5375
CPC分类号： C07D265/30
摘要： Compounds of formula I: (I) wherein:R 1 represents C 3-8 cycloalky l -Y 1 -, aryl-Y 1 -, heteroaryl-Y 1 -, aryl- G-Y 1 -, heteroaryl-G-Y 1 -, C 1-6 alkyl-G-Y 1 -, J 1 -Y 1 -, NR 21 R 22 -Y 1 -, NR 21 R 22 -CO-Y 1 - or R 23 -CONR 21 -Y 1 -;Q represents -(CR 16 R 19 )(CR 18a R 19a ) t -, wherein t represents an integer from 0 to 3; R 2 represents hydrogen or C 1-6 alkyl; X represents ethylene or a group of formula CR e R f wherein R e and R f independently represent hydrogen or C 1-4 alkyl or R e and R f may together with the carbon atom to which they are attached form a C 3-8 cycloalkyl group; R 3 and R 4 independently represent hydrogen or C 1-4 alkyl; Z represents a bond, CO, SO 2 , CR 9 R 6 (CH 2 ) n , (CH 2 ) n CR 9 R 6 , CR 9 R 6 (CH 2 ) n O, CR 9 R 6 (CH 2 ) n S, CR 9 R 6 (CH 2 ) n CO, COCR 9 R 6 (CH 2 ) n or SO 2 CR 9 R 6 (CH 2 ) n ; R 5 represents aryl, heteroaryl or aryl-C 2-6 alkenyl-; R 6 represents hydrogen, C 1-4 alkyl, CONR 7 R 8 or COOC 1-6 alkyl; a and b represent 1 or 2, such that a+b represents 2 or 3; G represents -S-, -SO 2 -, -SO 2 NR 20 , -NR 20 SO 2 or -NR 20 -; n represents an integer from 0 to 4; 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C 3-8环烷基-Y 1 - ，芳基Y 1 - ，杂芳基Y 1 - ，芳基-GY 1 - ， - 杂芳基-GY 1 - ，C 1-6烷基-GY 1 - ，J 1 -Y 1 - ，NR 21 R 22 -Y 1 - ，NR 21 - 21 R 22 -CO-Y 1 - 或R 23 -CONR 21 -Y 1 - ; Q表示 - （CR 16 R 19）（CR 18 R 19） t-，其中t表示0至3的整数; R 2表示氢或C 1-6烷基; X表示亚乙基或式CR e R f的基团，其中R e和R f独立地表示氢或C 1-4烷基或R e和R f可与碳原子一起它们连接在其上形成C 3-8环烷基; R 3和R 4独立地表示氢或C 1-4烷基; Z表示键，CO，SO 2，CR 9 R 6（CH 2）n，（CH 2）n CR 9 R 6，CR 9 R 6（CH 2）n O，CR 9 R 6（CH 2）n S，CR 9 R 6（CH 2）n CO，COCR 9 R 6（CH 2）n或SO 2 CR 9 R 6（CH 2）n; R 5表示芳基，杂芳基或芳基-C 2-6烯基 - ; R 6表示氢，C 1-4烷基，CONR 7 R 8或COOC 1-6烷基; a和b表示1或2，使得a + b表示2或3; G表示-S - ， - SO 2 - ， - SO 2 NR 20，-NR 20 SO 2或-NR 20 - 。 n表示0〜4的整数，其盐和溶剂化物是CCR3受体拮抗剂，因此被认为可用于治疗。

6. 发明申请

WO2003082863A1 N-(MORPHOLIN-2YL) METHYL ACETAMIDE DERIVATIVES AS CCR-3 ANTAGONISTS USEFUL IN THE TREATMENT OF INFLAMMATORY DISEASES 审中-公开
标题翻译： N-（MORPHOLIN-2YL）甲基乙酰胺衍生物作为用于治疗炎症疾病的CCR-3拮抗剂
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
申请人： 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
发明人： 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分类号： C07D413/12
CPC分类号： C07D413/12
摘要： 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.
摘要翻译：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。

7. 发明申请

WO2003082294A1 MORPHOLINE DERIVATIVES WITH A SUBSTITUTED ACETAMIDE GROUP IN THE 2-POSITION FOR USE AS CCR-3 ANTAGONISTS FOR THE TREATMENT OF INFLAMMATORY DISEASES 审中-公开
标题翻译：在用于治疗炎症疾病的CCR-3拮抗剂的2位置中具有取代的乙酰胺基团的吗啉衍生物
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
申请人： 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
发明人： 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分类号： A61K31/5377
CPC分类号： C07D209/48 , C07D265/30 , C07D413/06 , C07D413/12
摘要： 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.
摘要翻译：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。

8. 发明申请

WO2010146105A1 S1P1 AGONISTS COMPRISING A BICYCLIC N-CONTAINING RING 审中-公开
标题翻译： S1P1包含双相包含N型环的激光
公开(公告)号：WO2010146105A1
公开(公告)日：2010-12-23
申请号：PCT/EP2010/058515
申请日：2010-06-17
申请人： GLAXO GROUP LIMITED , BAILEY, James, Matthew , BIT, Rino, Antonio , DEMONT, Emmanuel, Hubert , HARRISON, Lee, Andrew , JONES, Katherine, Louise , SMETHURST, Christian, Alan, Paul , WITHERINGTON, Jason
发明人： BAILEY, James, Matthew , BIT, Rino, Antonio , DEMONT, Emmanuel, Hubert , HARRISON, Lee, Andrew , JONES, Katherine, Louise , SMETHURST, Christian, Alan, Paul , WITHERINGTON, Jason
IPC分类号： C07D413/04 , C07D413/14 , C07D417/04 , A61K31/4245 , A61P17/06
CPC分类号： C07D413/04 , C07D413/14 , C07D417/04
摘要： The present invention relates to novel compounds of formula (I) having S1P1 agonist activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.
摘要翻译：本发明涉及具有S1P1激动剂活性的新型式（I）化合物，其制备方法，含有它们的药物组合物及其在治疗各种疾病中的用途。

9. 发明申请

WO2003082292A1 MORPHOLINE DERIVATIVES SUBSTITUTED AT THE 2-POSITION BY AN ARYLALKYLUREA GROUP FOR USE AS CCR-3 ANTAGONISTS IN THE TREATMENT OF INFLAMMATORY CONDITIONS 审中-公开
标题翻译：通过ARYLALKYLUREA集团在2位置取代的多环芳烃衍生物用作治疗炎症条件下的CCR-3拮抗剂
公开(公告)号：WO2003082292A1
公开(公告)日：2003-10-09
申请号：PCT/EP2003/003340
申请日：2003-03-27
申请人： 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
发明人： 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分类号： A61K31/5377
CPC分类号： C07D265/30 , C07D413/12
摘要： Certain compounds of formula (I); wherein R 1 represents unsubstituted or substituted aryl; Y represents -(CR na R nb ) n -; R na and R nb are each independently hydrogen or C1-6 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 CCR3-antagonists and are thus indicated to be useful in therapy of inflammatory conditions.
摘要翻译：某些式（I）化合物; 其中R 1表示未取代或取代的芳基; 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; 其盐和溶剂化物是CCR3-拮抗剂，因此被认为可用于治疗炎性病症。

10. 发明申请

WO1997036903A1 PYRROLOPYRROLONE DERIVATIVES AS INHIBITORS OF NEUTROPHIL ELASTASE 审中-公开
标题翻译：作为中性粒细胞酶抑制剂的吡咯烷酮衍生物
公开(公告)号：WO1997036903A1
公开(公告)日：1997-10-09
申请号：PCT/EP1997001530
申请日：1997-03-26
申请人： GLAXO GROUP LIMITED , DOWLE, Michael, Dennis , FINCH, Harry , HARRISON, Lee, Andrew , INGLIS, Graham, George, Adam , JOHNSON, Martin, Redpath , MACDONALD, Simon, John, Fawcett , SHAH, Pritom , SMITH, Robin, Andrew
发明人： GLAXO GROUP LIMITED
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , C07D207/14
摘要： There are described according to the invention compounds of formula (I) (relative stereochemistry indicated), wherein R1, R2, R3 and X are as defined in the specification, together with processes for preparing them, compositions containing them and their use as pharmaceuticals. Compounds of formula (I) are indicated inter alia for the treatment of chronic bronchitis.
摘要翻译：根据本发明描述了式（I）化合物（所示的相对立体化学），其中R1，R2，R3和X如说明书中所定义，以及其制备方法，含有它们的组合物及其作为药物的用途。式（I）的化合物尤其用于治疗慢性支气管炎。

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