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1. 发明申请

WO2005090353A1 PYRAZOLO[3,4-b]PYRIDINE COMPOUNDS, AND THEIR USE AS PDE4 INHIBITORS 审中-公开
标题翻译：吡咯并[3,4-b]吡啶化合物，并且作为PDE4抑制剂使用
公开(公告)号：WO2005090353A1
公开(公告)日：2005-09-29
申请号：PCT/GB2005/000976
申请日：2005-03-15
申请人： GLAXO GROUP LIMITED , COE, Diane, Mary , COOK, Caroline, Mary , COOPER, Anthony, William, James , EDLIN, Christopher, David , HAMBLIN, Julie, Nicole , JOHNSON, Martin, Redpath , JONES, Paul, Spencer , LINDVALL, Mika, Kristian , MITCHELL, Charlotte, Jane , REDGRAVE, Alison, Judith , ROBINSON, John, Edward
发明人： COE, Diane, Mary , COOK, Caroline, Mary , COOPER, Anthony, William, James , EDLIN, Christopher, David , HAMBLIN, Julie, Nicole , JOHNSON, Martin, Redpath , JONES, Paul, Spencer , LINDVALL, Mika, Kristian , MITCHELL, Charlotte, Jane , REDGRAVE, Alison, Judith , ROBINSON, John, Edward
IPC分类号： C07D487/04
CPC分类号： C07D471/04
摘要： The invention relates to a compound of formula (I) or a salt thereof: formula (I) wherein: R 1 is Et, n-Pr, i-Pr, C 2 fluoroalkyl, or -CH 2 CH 2 OH; R 2 is H, Me, Et, n-Pr, i-Pr, C 1-2 fluoroalkyl, cyclopropyl or (cyclopropyl)methyl-; and NHR 3 has the sub-formula (nhr3): formula (nhr3) wherein R 3a is methyl or ethyl; R 3b is H, methyl or ethyl; R 3c is H, methyl or ethyl, R 3d is H, methyl or ethyl, and R 3e is H or methyl, provided that: (a) R 3b is methyl or ethyl; and/or (b) R 3c and R 3d are independently methyl or ethyl; and provided that: (c) when R 3c is ethyl and/or when R 3d is ethyl and/or when R 3e is methyl, then: R 3a is methyl and/or R 3b is a hydrogen atom (H) or methyl. NHR 3 can for example be [(1S)-1,2-dimethylpropyl]amino or t-butylamino. The invention also relates to the use of these pyrazolo[3,4 b]pyridine compounds in therapy, as inhibitors of phosphodiesterase type IV (PDE4), and relates to their use in the treatment and/or prophylaxis of inflammatory and/or allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rheumatoid arthritis or allergic rhinitis.
摘要翻译：本发明涉及式（I）化合物或其盐：式（I）其中：R 1是Et，n-Pr，i-Pr，C 2 F 2烷基或-CH 2 CH 2 OH; R 2是H，Me，Et，n-Pr，i-Pr，C 1-12氟烷基，环丙基或（环丙基）甲基; 和NHR 3具有其中R 3a是甲基或乙基的子式（nhr3）：式（nhr3） R 3b是H，甲基或乙基; R 3c是H，甲基或乙基，R 3d是H，甲基或乙基，R 3e是H或甲基，条件是：（a）R 3b是甲基或乙基; 和/或（b）R 3c和R 3d独立地是甲基或乙基; 并且条件是：（c）当R 3c为乙基和/或当R 3d为乙基时，和/或当R 3e为甲基时，R 3a为甲基和/或R 3b，是氢原子（H）或甲基。 NHR 3可以例如是[（1S）-1,2-二甲基丙基]氨基或叔丁基氨基。本发明还涉及这些吡唑并[3,4b]吡啶化合物在治疗中作为IV型磷酸二酯酶抑制剂（PDE4）的用途，并且涉及它们在治疗和/或预防炎性和/或过敏性疾病中的用途如慢性阻塞性肺疾病（COPD），哮喘，类风湿关节炎或过敏性鼻炎。

2. 发明申请

WO2005090352A1 PYRAZOLO[3,4-B]PYRIDINE COMPOUND, AND ITS USE AS A PDE4 INHIBITOR 审中-公开
标题翻译：吡咯并[3,4-B]吡啶化合物，并且用作PDE4抑制剂
公开(公告)号：WO2005090352A1
公开(公告)日：2005-09-29
申请号：PCT/EP2005/003038
申请日：2005-03-15
申请人： GLAXO GROUP LIMITED , CHRISTENSEN IV, Siegfried, Benjamin , COOK, Caroline, Mary , EDLIN, Christopher, David , JOHNSON, Martin, Redpath , JONES, Paul, Spencer , LINDVALL, Mika, Kristian , SAYANI, Amyn, Pyarali , TRIVEDI, Naimisha , TROTTET, Lionel
发明人： CHRISTENSEN IV, Siegfried, Benjamin , COOK, Caroline, Mary , EDLIN, Christopher, David , JOHNSON, Martin, Redpath , JONES, Paul, Spencer , LINDVALL, Mika, Kristian , SAYANI, Amyn, Pyarali , TRIVEDI, Naimisha , TROTTET, Lionel
IPC分类号： C07D487/04
CPC分类号： C07D471/04
摘要： The invention provides 4-{[1-(aminocarbonyl)-4-piperidinyl]amino}-N-[(3,4-dimethylphenyl)methyl]-1-ethyl-1H-pyrazolo[3,4-b]pyridine-5-carb oxamide, which is the compound of formula (I), or a salt thereof. The invention also provides the use of said compound or a pharmaceutically acceptable salt thereof as an inhibitor of phosphodiesterase type IV (PDE4), for example in the treatment and/or prophylaxis of an inflammatory and/or allergic disease, cognitive impairment or depression in a mammal. In particular, the invention provides the use of the compound or pharmaceutically acceptable salt in the treatment and/or prophylaxis of atopic dermatitis in a mammal, for example by external topical administration to the mammal such as a human. Pharmaceutical compositions containing said compound or salt, in particular suitable for external topical administration, are also provided.
摘要翻译：本发明提供4 - {[1-（氨基羰基）-4-哌啶基]氨基} -N - [（3,4-二甲基苯基）甲基] -1-乙基-1H-吡唑并[3,4-b]吡啶-5 - 肟酰胺，其为式（I）化合物或其盐。本发明还提供了所述化合物或其药学上可接受的盐作为IV型磷酸二酯酶抑制剂（PDE4）的用途，例如用于治疗和/或预防炎性和/或过敏性疾病，认知障碍或抑郁症哺乳动物。特别地，本发明提供了化合物或药学上可接受的盐在哺乳动物治疗和/或预防特应性皮炎中的用途，例如通过外用局部施用于哺乳动物如人。还提供了含有所述化合物或盐的药物组合物，特别适用于外用局部给药。

3. 发明申请

WO2005090348A1 PYRAZOLO ’3,4-B! PYRIDINE COMPOUNDS, AND THEIR USE AS PHOSPHODIESTERASE TYPE 4 (PDE4) INHIBITORS 审中-公开
标题翻译： PYRAZOLO'3,4-B！吡啶化合物及其作为磷酸二酯酶4（PDE4）抑制剂的用途
公开(公告)号：WO2005090348A1
公开(公告)日：2005-09-29
申请号：PCT/GB2005/000983
申请日：2005-03-15
申请人： GLAXO GROUP LIMITED , ALLEN, David, George , COE, Diane, Mary , COOK, Caroline, Mary , DOWLE, Michael, Dennis , EDLIN, Christopher, David , HAMBLIN, Julie, Nicole , JOHNSON, Martin, Redpath , JONES, Paul, Spencer , LINDVALL, Mika, Kristian , MITCHELL, Charlotte, Jane , REDGRAVE, Alison, Judith , TRIVEDI, Naimisha
发明人： ALLEN, David, George , COE, Diane, Mary , COOK, Caroline, Mary , DOWLE, Michael, Dennis , EDLIN, Christopher, David , HAMBLIN, Julie, Nicole , JOHNSON, Martin, Redpath , JONES, Paul, Spencer , LINDVALL, Mika, Kristian , MITCHELL, Charlotte, Jane , REDGRAVE, Alison, Judith , TRIVEDI, Naimisha
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： The invention provides a compound of formula (I) or a salt thereof: formula (I) wherein W is Ar, -CR 4 R 5 Ar or a group (y) or (y1), wherein Ar is (x) or (z): formulae (x), (z), (y), (y1) R 1 is C 1-4 alkyl, C 1-3 fluoroalkyl or CH 2 CH 2 OH. R 2 is C 2-6 alkyl, C 3-6 cycloalkyl or -(CH 2 ) n 4 -C 3-6 cycloalkyl; and R 3 is optionally substituted C 3-8 cycloalkyl, optionally substituted mono unsaturated C 5-7 cycloalkenyl, an optionally substituted heterocyclic group (aa), (bb) or (cc) (in which Y is O, S, SO 2 , or NR 10 ), or a bicyclic group (ee): formulae (aa), (bb), (cc), (ee). The invention also relates to the use of the compounds in therapy as inhibitors of phosphodiesterase type IV (PDE4), and/or for the treatment and/or prophylaxis of inflammatory and/or allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rheumatoid arthritis or allergic rhinitis.
摘要翻译：本发明提供式（I）化合物或其盐：其中W是Ar，-CR 4 R 5 Ar或式（y）或（y1）的式（I），其中Ar是（x ）或（z）：式（x），（z），（y），（y1）R 1为C 1-4烷基，C 1-3氟烷基或CH 2 CH 2 OH。 R 2是C 2-6烷基，C 3-6环烷基或 - （CH 2）n 4 -C 3-6环烷基; 任选取代的单不饱和C 5-7环烯基，任选取代的杂环基（aa），（bb）或（cc）（其中Y是O，S，SO2或NR） 10），或双环基（ee）：式（aa），（bb），（cc），（ee）。本发明还涉及该化合物在治疗中作为IV型磷酸二酯酶抑制剂（PDE4）和/或用于治疗和/或预防炎性和/或过敏性疾病如慢性阻塞性肺疾病（COPD），哮喘的用途，类风湿关节炎或过敏性鼻炎。

4. 发明申请

WO2003082862A1 ANTI-INFLAMMATORY MORPHOLIN-ACETAMIDE DERIVATIVES 审中-公开
标题翻译：抗炎性吗啉 - 乙酰胺衍生物
公开(公告)号：WO2003082862A1
公开(公告)日：2003-10-09
申请号：PCT/EP2003/003347
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： C07D265/30 , C07D413/12 , C07D413/14 , C07D417/14
摘要： Certain compounds of formula (I): wherein: R 1 represents substituted or unsubstituted heteroaryl; 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：某些式（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是1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表示氢或C 1-6烷基;其盐和溶剂化物是CCR-3拮抗剂，因此被认为可用于治疗。

5. 发明申请

WO2003099798A1 MORPHOLINYLMETHYLUREAS CCR-3 RECEPTOR ANTAGONIST 审中-公开
公开(公告)号：WO2003099798A1
公开(公告)日：2003-08-14
申请号：PCT/EP2003/005597
申请日：2003-05-26
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： C07D265/30
摘要： Compounds of formula (I): wherein:R 1 represents C 3-8 cycloalkyl-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 -, R 22 R 23 N-Y 1 -, R 22 R 23 N-CO-Y 1 - or R 24 -CONR 22 -Y 1 -; Q represents -(CR 19 R 20 )(CR 19a R 20a )t-, wherein t represents an integer from 0 to 3;R 2 and R 3 independently represent 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 4 and R 5 independently represent hydrogen or C 1-4 alkyl; Z represents a bond, CO, SO 2 , CR 10 R 7 (CH 2 ) n , (CH 2 ) n CR 10 R 7 , CR 10 R 7 (CH 2 ) n O, CR 10 R 7 (CH 2 ) n S, CR 10 R 7 (CH 2 ) n CO, COCR 10 R 7 (CH 2 ) n or SO 2 CR 10 R 7 (CH 2 ) n ; R 6 represents aryl, heteroaryl or aryl-C 2-6 alkenyl-; R 7 represents hydrogen, C 1-4 alkyl, CONR 8 R 9 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 21 , -NR 21 SO 2 or -NR 21 -; n represents an integer from 0 to 4; J 1 independently represents a moiety of formula (K): wherein X 1 represents oxygen, NR 11 or sulphur, X 2 represents CH 2 , oxygen, NR 12 or sulphur, m 1 represents an integer from 1 to 3, m 2 represents an integer from 1 to 3, provided that m 1 +m 2 is in the range from 3 to 5, also provided that when both X 1 and X 2 represent oxygen, NR 11 , NR 12 or sulphur, m 1 and m 2 must both not equal less than 2, wherein K is optionally substituted by one or more (eg. 1 or 2) -Y 3 -aryl, -Y 3 -heteroaryl, -Y 3 -CO-aryl, -Y 3 -CO-heteroaryl, -C 1-6 alkyl, -Y 3 -COOC 1-6 alkyl, -Y 3 -COC 1-6 alkyl, -Y 3 -W, -Y 3 -CO-W, -Y 3 -NR 15 R 16 , -Y 3 -CONR 15 R 16 , hydroxy, oxo, -Y 3 -SO 2 NR 15 R 16 , -Y 3 -SO 2 C 1-6 alkyl, -Y 3 -SO 2 aryl, -Y 3 -SO 2 heteroaryl, -Y 3 -NR 13 C 1-6 alkyl, -Y 3 -NR 13 SO 2 C 1-6 alkyl, -Y 3 -NR 13 CONR 15 R 16 , -Y 3 -NR 13 COOR 14 or -Y 3 -OCONR 15 R 16 groups, and is optionally fused to a monocyclic aryl or heteroaryl ring;R 8 , R 9 , R 10 , R 11 , R 12 , R 13 and R 14 independently represent hydrogen or C 1-6 alkyl; R 15 and R 16 independently represent hydrogen or C 1-6 alkyl or R 15 and R 16 together with the nitrogen atom to which they are attached may form a morpholine, piperidine or pyrrolidine ring; R 17 , R 18 , R 19 , R 20 , R 19a , R 20a , and R 21 independently represent hydrogen or C 1-4 alkyl; R 22 and R 23 independently represent hydrogen, C 1-6 alkyl, C 3-8 cycloalkyl or C 3-8 cycloalkylC1-6alkyl; R 24 represents C 1-6 alkyl, C 3-8 cycloalkyl, aryl or heteroaryl; W represents a saturatedor unsaturated, non-aromatic 5-7 membered ring containing between 1 and 3 heteroatoms selected from nitrogen, oxygen or sulphur, optionally substituted with one or more C 1-6 alkyl, halogen or hydroxy groups; Y 1 and Y 3 independently represent a bond or a group of formula - (CH 2 ) p CR c R d (CH 2 ) q - wherein R c and R d independently represent hydrogen or C 1-4 alkyl or R c and R d may together with the carbon atom to which they are attached form a C 3-8 cycloalkyl group, and p and q independently represent an integer from 0 to 5 wherein p + q is an integer from 0 to 5; and salts and solvates thereof are CCR3 receptor antagonists and thus are indicated to be useful in therapy.

6. 发明申请

WO2005090354A1 PYRAZOLO[3,4-b] PYRIDINE COMPOUNDS, AND THEIR USE AS PDE4 INHIBITORS 审中-公开
标题翻译：吡咯并[3,4-b]吡啶化合物，并且作为PDE4抑制剂使用
公开(公告)号：WO2005090354A1
公开(公告)日：2005-09-29
申请号：PCT/GB2005/000987
申请日：2005-03-15
申请人： GLAXO GROUP LIMITED , COOK, Caroline, Mary , DOWLE, Michael, Dennis , EDLIN, Christopher, David , JOHNSON, Martin, Redpath , JONES, Paul, Spencer , LINDVALL, Mika, Kristian , TRIVEDI, Naimisha , REDGRAVE, Alison, Judith
发明人： COOK, Caroline, Mary , DOWLE, Michael, Dennis , EDLIN, Christopher, David , JOHNSON, Martin, Redpath , JONES, Paul, Spencer , LINDVALL, Mika, Kristian , TRIVEDI, Naimisha , REDGRAVE, Alison, Judith
IPC分类号： C07D487/04
CPC分类号： C07D471/04
摘要： The invention provides a compound of formula (I) or a salt thereof: formula (I) wherein: R 1 is C 1-3 alkyl, C 1-3 fluoroalkyl, or -CH 2 CH 2 OH; R 2 is a hydrogen atom (H), methyl or C 1 fluoroalkyl; R 3 is of sub-formula (aa) or (bb): formulae (aa), (bb) wherein Y is NCONH 2 and n 1 is 0 or 1; R 4 is H; and R 5 is a group of the sub-formula (x), (y), (y1) or (z): formulae (x), (y), (y1), (z). The invention also relates to the use of these compounds or salts in therapy as inhibitors of phosphodiesterase type IV (PDE4). For example, it relates to their use in the treatment and/or prophylaxis of inflammatory and/or allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rheumatoid arthritis, allergic rhinitis, psoriasis or atopic dermatitis in a mammal such as a human.
摘要翻译：本发明提供式（I）化合物或其盐：式（I）其中：R 1为C 1-3烷基，C 1-3氟烷基或-CH 2 CH 2 OH; R 2是氢原子（H），甲基或C 1-6烷基; （aa）或（bb）：式（aa），（bb）其中Y为NCONH2且n为0或1; R 4是H; 并且R 5是式（x），（y），（y1）或（z）的子集：式（x），（y），（y1），（z）。本发明还涉及这些化合物或盐在治疗中作为IV型磷酸二酯酶抑制剂（PDE4）的用途。例如，它涉及其用于治疗和/或预防哺乳动物例如慢性阻塞性肺疾病（COPD），哮喘，类风湿性关节炎，过敏性鼻炎，牛皮癣或特应性皮炎的炎性和/或过敏性疾病人类。

7. 发明申请

WO2005058892A1 PYRAZOLO [3,4-B] PYRIDINE COMPOUNDS, AND THEIR USE AS PHOSPHODIESTERASE INHIBITORS 审中-公开
标题翻译：吡咯并[3,4-B]吡啶化合物及其作为磷酸二酯酶抑制剂的用途
公开(公告)号：WO2005058892A1
公开(公告)日：2005-06-30
申请号：PCT/EP2004/014490
申请日：2004-12-17
申请人： GLAXO GROUP LIMITED , ALLEN, David, George , COE, Diane, Mary , COOK, Caroline, Mary , DOWLE, Michael, Dennis , EDLIN, Christopher, David , HAMBLIN, Julie, Nicole , JOHNSON, Martin, Redpath , JONES, Paul, Spencer , LINDVALL, Mika, Kristian , MITCHELL, Charlotte, Jane , REDGRAVE, Alison, Judith , ROBINSON, John Edward , TRIVEDI, Naimisha
发明人： ALLEN, David, George , COE, Diane, Mary , COOK, Caroline, Mary , DOWLE, Michael, Dennis , EDLIN, Christopher, David , HAMBLIN, Julie, Nicole , JOHNSON, Martin, Redpath , JONES, Paul, Spencer , LINDVALL, Mika, Kristian , MITCHELL, Charlotte, Jane , REDGRAVE, Alison, Judith , ROBINSON, John Edward , TRIVEDI, Naimisha
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： The invention provides a compound of formula (I) or a salt thereof, wherein Ar has the sub-formula (x) or (z) and wherein R 3 is optionally substituted C 3-8 cycloalkyl, optionally substituted C 5-7 cycloalkenyl, an optionally substituted heterocyclic group (aa), (bb) or (cc), or a bicyclic group (ee); and wherein R 4 is H, C 1-3 alkyl, C 1-2 fluoroalkyl, cyclopropyl, CH 2 OR 4a , CH(Me)OR 4a , or CH2CH2OR 4a ; and R 5 is inter alia H, C 1-8 alkyl, C 1-8 fluoroalkyl, C 3-8 cycloalkyl, certain substituted alkyl groups, -(CH2) n 13 - Het, or optionally substituted phenyl or CH 2 -Ph; or R 4 and R 5 taken together are -(CH 2 )p 1 - or (CH 2 )p3 X 5 (CH2)p 4 - ; provided that at least one of R 4 and R 5 is not a hydrogen atom (H). The invention also provides the use of the compounds as inhibitors of phosphodiesterase type IV (PDE4) and/or for the treatment and/or prophylaxis of inflammatory and/or allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rheumatoid arthritis, allergic rhinitis or atopic dermatitis.
摘要翻译：本发明提供式（I）化合物或其盐，其中Ar具有亚式（x）或（z），其中R 3是任选取代的C 3-8环烷基，任选取代的C 5-7环烯基，任选取代的杂环基（aa），（bb）或（cc）或双环基（ee）; 并且其中R 4是H，C 1-3烷基，C 1-2 - 氟烷基，环丙基，CH 2 OH 4a，CH（Me）OR 4a或CH 2 CH 2OR 4a。和R 5尤其是H，C 1-8烷基，C 1-8氟烷基，C 3-8环烷基，某些取代的烷基， - （CH 2）n 13 - 或任选取代的苯基或CH 2 -Ph; 或R 4和R 5一起是 - （CH 2）p - 或（CH 2）p 3 X 5（CH 2）p 4 - ; 条件是R 4和R 5中的至少一个不是氢原子（H）。本发明还提供了化合物作为IV型磷酸二酯酶抑制剂（PDE4）和/或用于治疗和/或预防炎性和/或过敏性疾病如慢性阻塞性肺疾病（COPD），哮喘，类风湿性关节炎，过敏性鼻炎或特应性皮炎。

8. 发明申请

WO2004056823A1 PYRAZOLO[3,4-b]PYRIDINE COMPOUNDS, AND THEIR USE AS PHOSPHODIESTERASE INHIBITORS 审中-公开
标题翻译：吡咯并[3,4-b]吡啶化合物及其作为磷酸二酯酶抑制剂的用途
公开(公告)号：WO2004056823A1
公开(公告)日：2004-07-08
申请号：PCT/EP2003/014867
申请日：2003-12-19
申请人： GLAXO GROUP LIMITED , ALLEN, David, George , COE, Diane, Mary , COOK, Caroline, Mary , COOPER, Anthony, William, James , DOWLE, Michael, Dennis , EDLIN, Christopher, David , HAMBLIN, Julie, Nicole , JOHNSON, Martin, Redpath , JONES, Paul, Spencer , LINDVALL, Mika, Kristian , MITCHELL, Charlotte, Jane , REDGRAVE, Alison, Judith
发明人： ALLEN, David, George , COE, Diane, Mary , COOK, Caroline, Mary , COOPER, Anthony, William, James , DOWLE, Michael, Dennis , EDLIN, Christopher, David , HAMBLIN, Julie, Nicole , JOHNSON, Martin, Redpath , JONES, Paul, Spencer , LINDVALL, Mika, Kristian , MITCHELL, Charlotte, Jane , REDGRAVE, Alison, Judith
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： The invention relates to a compound of formula (I) or a salt thereof: Formula (I) wherein: R 1 is C 1-4 alkyl, C 1-3 fluoroalkyl or -(CH 2 ) 2 OH; R 2 is a hydrogen atom (H), methyl or C 1 fluoroalkyl; R 3a is a hydrogen atom (H) or C 1-3 alkyl; R 3 is optionally substituted branched C 3-6 alkyl, optionally substituted C 3-8 cycloalkyl, optionally substituted mono-unsaturated-C 5-7 cycloalkenyl, optionally substituted phenyl, or an optionally substituted heterocyclic group of sub-formula (aa), or (bb) or (cc) in which n 1 and n 2 independently are 1 or 2; and Y is O, S, SO 2 , or NR 4 ; and wherein Het is of sub-formula (i), or (ii), or (iii), or (iv) or (v). 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.
摘要翻译：本发明涉及式（I）化合物或其盐：式（I）其中：R 1为C 1-4烷基，C 1-3氟烷基或 - （CH 2）2 OH; R 2是氢原子（H），甲基或C 1-6烷基; R 3a是氢原子（H）或C 1-3烷基; R 3为任选取代的支链C 3-6烷基，任选取代的C 3-8环烷基，任选取代的单不饱和C 5-7环烯基，任选取代的苯基或任选取代的亚式（aa）杂环基或（bb）或（cc），其中n 1和n 2独立地为1或2; Y是O，S，SO 2或NR 4; 并且其中Het为子式（i），或（ii），或（iii），或（iv）或（v）。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性和/或过敏性疾病的药物中的用途，例如慢性阻塞性肺疾病（COPD），哮喘或过敏性鼻炎。

9. 发明申请

WO2004024728A2 PYRAZOLO[3,4-B]PYRIDINE COMPOUNDS, AND THEIR USE AS PHOSPHODIESTERASE INHIBITORS 审中-公开
标题翻译：吡咯并[3,4-B]吡啶化合物及其作为磷酸酯酶抑制剂的用途
公开(公告)号：WO2004024728A2
公开(公告)日：2004-03-25
申请号：PCT/EP2003/011814
申请日：2003-09-12
申请人： GLAXO GROUP LIMITED , 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
发明人： 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分类号： C07D471/04
CPC分类号： C07D471/04
摘要： 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.
摘要翻译：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 1-6烷基; R 3 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亚式（aa），（bb）或（cc）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R 3是双环基（dd）或（ee）：。并且其中X为NR4R5或OR5a。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性和/或过敏性疾病的药物中的用途，例如慢性阻塞性肺疾病（COPD），哮喘或过敏性鼻炎。

10. 发明申请

WO03099798A8 MORPHOLINYLMETHYLUREAS CCR-3 RECEPTOR ANTAGONIST 审中-公开
标题翻译：吗啉酰吗啉CCR-3受体拮抗剂
公开(公告)号：WO03099798A8
公开(公告)日：2004-01-15
申请号：PCT/EP0305597
申请日：2003-05-26
申请人： GLAXO GROUP LTD , 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： A61P11/06 , C07D265/30 , C07D413/12 , A61K31/5375 , A61K31/5377
CPC分类号： C07D265/30 , C07D413/12
摘要： Compounds of formula (I): wherein:R represents C3-8 cycloalkyl-Y -, aryl-Y -, heteroaryl-Y -, aryl- G-Y -, heteroaryl-G-Y -, C1-6 alkyl-G-Y -, J -Y -, R R N-Y -, R R N-CO-Y - or R -CONR -Y -; Q represents -(CR R )(CR R )t-, wherein t represents an integer from 0 to 3;R and R independently represent hydrogen or C1-6 alkyl;X represents ethylene or a group of formula CR R wherein R and R independently represent hydrogen or C1-4 alkyl or R and R may together with the carbon atom to which they are attached form a C3-8 cycloalkyl group; R and R independently represent hydrogen or C1-4 alkyl; Z represents a bond, CO, SO2, CR R (CH2)n, (CH2)nCR R , CR R (CH2)nO, CR R (CH2)nS, CR R (CH2)nCO, COCR R (CH2)n or SO2CR R (CH2)n; R represents aryl, heteroaryl or aryl-C2-6 alkenyl-; R represents hydrogen, C1-4 alkyl, CONR R or COOC1-6 alkyl;a and b represent 1 or 2, such that a+b represents 2 or 3;G represents -S-, -SO2-, -SO2NR , -NR SO2 or -NR -; n represents an integer from 0 to 4; J independently represents a moiety of formula (K): wherein X represents oxygen, NR or sulphur, X represents CH2, oxygen, NR or sulphur, m represents an integer from 1 to 3, m represents an integer from 1 to 3, provided that m +m is in the range from 3 to 5, also provided that when both X and X represent oxygen, NR , NR or sulphur, m and m must both not equal less than 2, wherein K is optionally substituted by one or more (eg. 1 or 2) -Y -aryl, -Y -heteroaryl, -Y -CO-aryl, -Y -CO-heteroaryl, -C1-6 alkyl, -Y -COOC1-6 alkyl, -Y -COC1-6 alkyl, -Y -W, -Y -CO-W, -Y -NR R , -Y -CONR R , hydroxy, oxo, -Y -SO2NR R , -Y -SO2C1-6 alkyl, -Y -SO2aryl, -Y -SO2heteroaryl, -Y -NR C1-6 alkyl, -Y -NR SO2C1-6 alkyl, -Y -NR CONR R , -Y -NR COOR or -Y -OCONR R groups, and is optionally fused to a monocyclic aryl or heteroaryl ring;R , R , R , R , R , R and R
摘要翻译：式（I）化合物：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 - ，R 22 R 23，NY 22 - ，R 22 R 23 > N-CO-Y 1 - 或R 24 -CONR 22 -Y 1 - ; Q表示 - （CR 19 R 20）（CR 19 R 20）t - ，其中t表示0至3的整数; R 2和R 3独立地表示氢或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可以在一起与它们所连接的碳原子一起形成C 3-8环烷基; R 4和R 5独立地表示氢或C 1-4烷基; Z表示键，CO，SO 2，CR 10 R 7（CH 2）n，（CH 2）n CR 10 R 7，CR 10 R 7（CH 2）n O，CR 10 （CH 2）n C，CR 10 R 7（CH 2）n CO，COCR 10 R 7（CH 2）n或SO 2 CR 10 R 7（CH 2）n; R 6代表芳基，杂芳基或芳基-C 2-6烯基 - ; R 7表示氢，C 1-4烷基，CONR 8 R 9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 21，-NR 21 SO 2或-NR 21 - ; n表示0〜4的整数， J 1独立地表示式（K）的部分：其中X 1表示氧，NR 11或硫，X 2表示CH 2，氧，NR 12或硫，m表示 1〜3的整数，m 2表示1〜3的整数，条件是m 1 + m 2在3〜5的范围内，条件是当X 1和X 2表示氧，NR 11，NR 12或硫，m 1和m 2都必须不小于2，其中K任选被一个或多个（例如1或2个）取代）-Y 3 - 芳基，-Y 3 - 杂芳基，-Y 3 -CO-芳基，-Y 3 -CO-杂芳基，-C 1-6烷基，-Y 3 -COOC 1 -6烷基，-Y 3 -COC 1-6烷基，-Y 3 -W，-Y 3 -CO-W，-Y 3 -NR 15 R 16，-Y -CONR 15，R 16，羟基，氧代，-Y 3 -SO 2 NR 15，-Y 3 -SO 2 C 1-6烷基，-Y 3 -SO 2芳基，-Y 3 -SO 2杂芳基，-Y 3 -NR 13 C 1-6烷基，-Y 3 -NR 13 SO 2 C 1-6烷基，-Y 3 -NR 13 CONR R 15，-Y 3 -NR 13 COOR 14或-Y 3 -CONR 15 R 16基团，并且任选地与单环芳基或杂芳基环稠合 R 8，R 9，R 10，R 11，R 12，R 13和R 10， 14

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