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1. 发明申请

WO2004103998A1 QUINOLINE DERIVATIVES AS PHOSPHODIESTERASE INHIBITORS 审中-公开
标题翻译：喹啉衍生物作为磷酸二酯酶抑制剂
公开(公告)号：WO2004103998A1
公开(公告)日：2004-12-02
申请号：PCT/EP2004/005494
申请日：2004-05-19
申请人： GLAXO GROUP LIMITED , BALDWIN, Ian, Robert , BARKER, Michael, David , DEAN, Anthony, William , ELDRED, Colin, David , EVANS, Brian , GOUGH, Sharon, Lisa , GUNTRIP, Stephen, Barry , HAMBLIN, Julie, Nicole , HOLMAN, Stuart , JONES, Paul , LINDVALL, Mika, Kristian , LUNNISS, Christopher, James , REDFERN, Tracy, Jane , REDGRAVE, Alison, Judith , ROBINSON, John, Edward , WOODROW, Michael
发明人： BALDWIN, Ian, Robert , BARKER, Michael, David , DEAN, Anthony, William , ELDRED, Colin, David , EVANS, Brian , GOUGH, Sharon, Lisa , GUNTRIP, Stephen, Barry , HAMBLIN, Julie, Nicole , HOLMAN, Stuart , JONES, Paul , LINDVALL, Mika, Kristian , LUNNISS, Christopher, James , REDFERN, Tracy, Jane , REDGRAVE, Alison, Judith , ROBINSON, John, Edward , WOODROW, Michael
IPC分类号： C07D417/12
CPC分类号： C07D401/12 , C07D215/54 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D453/02
摘要： There are provided according to the invention novel compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R19, R20 and R34 are as described in the specification, processes for preparing them, formulations containing them and their use in therapy for the treatment of inflammatory diseases.
摘要翻译：根据本发明提供新的式（I）化合物或其药学上可接受的盐，其中R1，R2，R19，R20和R34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用于治疗炎性疾病。

2. 发明申请

WO2007036733A1 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]吡啶化合物及其用作PDE4抑制剂
公开(公告)号：WO2007036733A1
公开(公告)日：2007-04-05
申请号：PCT/GB2006/003626
申请日：2006-09-29
申请人： GLAXO GROUP LIMITED , EDLIN, Christopher, David , HOLMAN, Stuart , JONES, Paul, Spencer , KEELING, Suzanne, Elaine , LINDVALL, Mika, Kristian , MITCHELL, Charlotte, Jane , TRIVEDI, Naimisha
发明人： EDLIN, Christopher, David , HOLMAN, Stuart , JONES, Paul, Spencer , KEELING, Suzanne, Elaine , LINDVALL, Mika, Kristian , MITCHELL, Charlotte, Jane , TRIVEDI, Naimisha
IPC分类号： C07D471/04 , C07D519/00 , A61K31/437 , A61P29/00
CPC分类号： C07D471/04
摘要： The invention provides a compound of formula (I) or a salt thereof: wherein R 2 is H, C 1-3 alkyl, n butyl, C1-2fluoroalkyl, cyclopropyl, cyclobutyl, (cyclopropyl)methyl , CN, or CH 2 OH; R 3 is inter alia optionally substituted C 4-7 cycloalkyl or an optionally substituted heterocyclic group (aa), (bb) or (cc); R a is H, methyl or ethyl; R b is H or methyl; R 4 is H, methyl, ethyl, n propyl, C(O) Me, or C(O) C1fluoroalkyl; and R 5 is: C(O) (CH2) n Ar, C(O) Het, C(O) C 1 6alkyl, C(O) C1fluoroalkyl, C(O) (CH 2 ) 2 C(O) NR 15b NR 15b , C(O) CH 2 C(O) NR 15b NR 15 b, C(O) NR 15b (CH2)m 1 Ar, C(O) NR 15b Het, C(O) NR 15b C 1-6 alkyl, C(O) NR 5a R 5b , S(O) 2 (CH 2 )m 2 - Ar , S(O) 2 Het, S(O) 2 -C 1 - 6 alkyl, or CH 2 Ar; or R 4 and R 5 taken together are -(CH 2 ) p 1 -, (CH 2 ) 2 X 5 (CH 2 ) 2 , C(O) (CH 2 )p 2 ,-C(O)-N(R 15 ) (CH 2 )p 3 ; or NR 4 R 5 is of sub-formula (y), (y1), (y2) or (y3). 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, psoriasis or atopic dermatitis.
摘要翻译：本发明提供式（I）化合物或其盐：其中R 2为H，C 1-3烷基，正丁基，C 1-2 - 氟烷基，环丙基，环丙基，（环丙基）甲基，CN或CH 2 OH; 特别是任选取代的C 4-7环烷基或任选取代的杂环基团（aa），（bb）或（cc）; R a是H，甲基或乙基; R b是H或甲基; R 4是H，甲基，乙基，正丙基，C（O）Me或C（O） R 5是C（O）（CH 2）n Ar Ar，C（O）Het，C（O）C 1-6烷基， C（O）C 1-4烷基，C（O）（CH 2）2 C（O）NR 15b R 15 >，C（O）CH 2 C（O）NR 15b -NR 15 B，C（O）NR 15b，（CH2）m 1 Ar，C（O）NR 15b Het，C（O）NR 15b C 1〜 C 1 -C 6烷基，C（O）NR 5a R 5b，S（O）2（CH 2） S（O）2 Het，S（O）2 -C（O）2 -C C 1 -C 6烷基或CH 2 Ar; 或R 4和R 5合在一起是 - （CH 2）2 -

3. 发明申请

WO2007107499A1 QUINOLINE DERIVATIVES USEFUL AS PDE4 INHIBITORS 审中-公开
标题翻译：喹啉衍生物作为PDE4抑制剂有用
公开(公告)号：WO2007107499A1
公开(公告)日：2007-09-27
申请号：PCT/EP2007/052478
申请日：2007-03-15
申请人： GLAXO GROUP LIMITED , EDLIN, Christopher David , HOLMAN, Stuart
发明人： EDLIN, Christopher David , HOLMAN, Stuart
IPC分类号： C07D401/12 , A61K31/4709 , A61P19/00 , A61P11/00 , A61P29/00 , A61P37/00
CPC分类号： C07D401/12
摘要： There is provided according to the invention novel compounds of formula (I) or pharmaceutically acceptable salts or solvates thereof. The invention also relates to the use of said compounds, compositions and medicaments, for example as inhibitors of phosphodiesterases and/or for the treatment and/or prophylaxis of diseases or conditions for which a PDE4 inhibitor is indicated, in particular inflammatory and/or allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rheumatoid arthritis and allergic rhinitis.
摘要翻译：根据本发明提供新颖的式（I）化合物或其药学上可接受的盐或溶剂化物。本发明还涉及所述化合物，组合物和药物的用途，例如作为磷酸二酯酶的抑制剂和/或用于治疗和/或预防指示PDE4抑制剂的疾病或病症，特别是炎性和/或过敏性疾病疾病如慢性阻塞性肺疾病（COPD），哮喘，类风湿性关节炎和过敏性鼻炎。

4. 发明申请

WO2007036734A1 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：WO2007036734A1
公开(公告)日：2007-04-05
申请号：PCT/GB2006/003627
申请日：2006-09-29
申请人： GLAXO GROUP LIMITED , CHRISTENSEN, Siegfried, Benjamin, IV , HOLMAN, Stuart , KEELING, Suzanne, Elaine , SAYANI, Amyn, Pyarali
发明人： CHRISTENSEN, Siegfried, Benjamin, IV , HOLMAN, Stuart , KEELING, Suzanne, Elaine , SAYANI, Amyn, Pyarali
IPC分类号： C07D471/04 , A61K31/437 , A61P29/00
CPC分类号： C07D471/04
摘要： The invention provides N -{[1,6-diethyl-4-(tetrahydro-2H-pyran-4-ylamino)-1 H -pyrazolo[3,4-b]pyridin-5-yl]methyl}-3-methyl-5-isoxazolecarboxamide Formula (I): or a salt thereof, such as the compound or a pharmaceutically acceptable salt thereof. The invention also provides the use of the compound or salt as an inhibitor of phosphodiesterase type IV (PDE4) and/or for the treatment and/or prophylaxis of an inflammatory and/or allergic disease, especially an inflammatory and/or allergic skin disease such as atopic dermatitis, in a mammal such as a human. External topical administration, e.g. topical administration to the skin, of the compound or salt is preferred, and external-topical pharmaceutical compositions are provided
摘要翻译：本发明提供了N - {[1,6-二乙基-4-（四氢-2H-吡喃-4-基氨基）-1H-吡唑并[3,4-b]吡啶-5-基]甲基} -3-甲基 - 式（I）的5-异恶唑酰胺或其盐，例如化合物或其药学上可接受的盐。本发明还提供了化合物或盐作为IV型磷酸二酯酶（PDE4）的抑制剂和/或用于治疗和/或预防炎症和/或过敏性疾病，特别是炎性和/或过敏性皮肤病，例如作为特应性皮炎，在哺乳动物如人中。外用局部给药，例如优选局部施用于皮肤，化合物或盐，并提供外用 - 外用药物组合物

5. 发明授权

EP1940835B1 PYRAZOLO[3,4-B]PYRIDINE COMPOUNDS, AND THEIR USE AS PDE4 INHIBITORS 有权
标题翻译：吡唑并[3,4-B]吡啶类化合物及其作为PDE4抑制剂的用途
公开(公告)号：EP1940835B1
公开(公告)日：2011-03-30
申请号：EP06779578.1
申请日：2006-09-29
申请人： GLAXO GROUP LIMITED
发明人： EDLIN, Christopher, David , HOLMAN, Stuart , JONES, Paul, Spencer , KEELING, Suzanne, Elaine , LINDVALL, Mika, Kristian , MITCHELL, Charlotte, Jane , TRIVEDI, Naimisha
IPC分类号： C07D471/04 , C07D519/00 , A61K31/437 , A61P29/00
CPC分类号： C07D471/04
摘要： The invention provides a compound of formula (I) or a salt thereof: wherein R2 is H, C1-3alkyl, n butyl, C1-2fluoroalkyl, cyclopropyl, cyclobutyl, (cyclopropyl)methyl , CN, or CH2OH; R3 is inter alia optionally substituted C4-7cycloalkyl or an optionally substituted heterocyclic group (aa), (bb) or (cc); Ra is H, methyl or ethyl; Rb is H or methyl; R4 is H, methyl, ethyl, n propyl, C(O) Me, or C(O) C1fluoroalkyl; and R5 is: C(O) (CH2)n Ar, C(O) Het, C(O) C1 6alkyl, C(O) C1fluoroalkyl, C(O) (CH2)2 C(O) NR15bNR15b, C(O) CH2 C(O) NR15bNR15b, C(O) NR15b (CH2)m1 Ar, C(O) NR15b Het, C(O) NR15b C1-6 alkyl, C(O) NR5aR5b, S(O)2 (CH2)m2-Ar, S(O)2 Het, S(O)2-C1-6alkyl, or CH2 Ar; or R4 and R5 taken together are -(CH2)p1-, (CH2)2 X5 (CH2)2 , C(O) (CH2)p2 ,-C(O)-N(R15) (CH2)p3 ; or NR4R5 is of sub-formula (y), (y1), (y2) or (y3). 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, psoriasis or atopic dermatitis.
摘要翻译：本发明提供了式（I）化合物或其盐：其中R2是H，C1-3烷基，正丁基，C1-2氟烷基，环丙基，环丁基，（环丙基）甲基，CN或CH2OH; R 3特别是任选取代的C 4-7环烷基或任选取代的杂环基（aa），（bb）或（cc）; Ra是H，甲基或乙基; Rb是H或甲基; R4是H，甲基，乙基，正丙基，C（O）Me或C（O）C1氟烷基; （O）（CH 2）n Ar，C（O）Het，C（O）C 1-6烷基，C（O）C 1氟烷基，C（O）（CH 2）2 C（O）NR 15b NR 15b，C （O）NR15bNR15b，C（O）NR15b（CH2）m1Ar，C（O）NR15bHet，C（O）NR15bCl6烷基，C（O）NR5aR5b，S（O）2（CH2）（O）2 Het，S（O）2 -C 1-6烷基或CH 2 Ar; （CH 2）2（CH 2）2，C（O）（CH 2）p2，-C（O）-N（R 15）（CH 2）p3;或者R 4和R 5一起为 - 或NR 4 R 5具有子式（y），（y 1），（y 2）或（y 3）。本发明还提供了所述化合物作为IV型磷酸二酯酶（PDE4）抑制剂和/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。

6. 发明公开

EP1940835A1 PYRAZOLO[3,4-B]PYRIDINE COMPOUNDS, AND THEIR USE AS PDE4 INHIBITORS 有权
标题翻译：吡唑并[3,4-b]吡啶化合物和它们作为PDE4抑制剂的用途
公开(公告)号：EP1940835A1
公开(公告)日：2008-07-09
申请号：EP06779578.1
申请日：2006-09-29
申请人： GLAXO GROUP LIMITED
发明人： EDLIN, Christopher, David , HOLMAN, Stuart , JONES, Paul, Spencer , KEELING, Suzanne, Elaine , LINDVALL, Mika, Kristian , MITCHELL, Charlotte, Jane , TRIVEDI, Naimisha
IPC分类号： C07D471/04 , C07D519/00 , A61K31/437 , A61P29/00
CPC分类号： C07D471/04
摘要： The invention provides a compound of formula (I) or a salt thereof: wherein R2 is H, C1-3alkyl, n butyl, C1-2fluoroalkyl, cyclopropyl, cyclobutyl, (cyclopropyl)methyl , CN, or CH2OH; R3 is inter alia optionally substituted C4-7cycloalkyl or an optionally substituted heterocyclic group (aa), (bb) or (cc); Ra is H, methyl or ethyl; Rb is H or methyl; R4 is H, methyl, ethyl, n propyl, C(O) Me, or C(O) C1fluoroalkyl; and R5 is: C(O) (CH2)n Ar, C(O) Het, C(O) C1 6alkyl, C(O) C1fluoroalkyl, C(O) (CH2)2 C(O) NR15bNR15b, C(O) CH2 C(O) NR15bNR15b, C(O) NR15b (CH2)m1 Ar, C(O) NR15b Het, C(O) NR15b C1-6 alkyl, C(O) NR5aR5b, S(O)2 (CH2)m2-Ar, S(O)2 Het, S(O)2-C1-6alkyl, or CH2 Ar; or R4 and R5 taken together are -(CH2)p1-, (CH2)2 X5 (CH2)2 , C(O) (CH2)p2 ,-C(O)-N(R15) (CH2)p3 ; or NR4R5 is of sub-formula (y), (y1), (y2) or (y3). 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, psoriasis or atopic dermatitis.

7. 发明公开

EP1940836A1 PYRAZOLO[3,4-B]PYRIDINE COMPOUND, AND ITS USE AS A PDE4 INHIBITOR 审中-公开
标题翻译：吡唑并[3,4-b]吡啶和它们作为PDE4抑制剂
公开(公告)号：EP1940836A1
公开(公告)日：2008-07-09
申请号：EP06779579.9
申请日：2006-09-29
申请人： GLAXO GROUP LIMITED
发明人： CHRISTENSEN, Siegfried, Benjamin, IV , HOLMAN, Stuart , KEELING, Suzanne, Elaine , SAYANI, Amyn, Pyarali
IPC分类号： C07D471/04 , A61K31/437 , A61P29/00
CPC分类号： C07D471/04
摘要： The invention provides N-{[1,6-diethyl-4-(tetrahydro-2H-pyran-4-ylamino)-1H-pyrazolo[3,4-b]pyridin-5-yl]methyl}-3-methyl-5-isoxazolecarboxamide Formula (I): or a salt thereof, such as the compound or a pharmaceutically acceptable salt thereof. The invention also provides the use of the compound or salt as an inhibitor of phosphodiesterase type IV (PDE4) and/or for the treatment and/or prophylaxis of an inflammatory and/or allergic disease, especially an inflammatory and/or allergic skin disease such as atopic dermatitis, in a mammal such as a human. External topical administration, e.g. topical administration to the skin, of the compound or salt is preferred, and external-topical pharmaceutical compositions are provided

8. 发明公开

EP1289539A1 PHARMACEUTICAL ANTI-INFLAMMATORY AEROSOL FORMULATION 审中-公开
标题翻译：具有消炎作用的药物气雾剂
公开(公告)号：EP1289539A1
公开(公告)日：2003-03-12
申请号：EP01938435.3
申请日：2001-06-15
申请人： GLAXO GROUP LIMITED
发明人： ARMOUR, Duncan, RobertDiscovery Chemistry , BROWN, DavidRoche Products Limited , CONGREVE, Miles, StuartGlaxoSmithKline , GORE, Paul, Martin , GREEN, Darren, Victor, Steven , HOLMAN, Stuart , JACK, Torquil, Iain, Maclean , MASON, Andrew, McMurtrie , MORRISS, Karen , RAMSDEN, Nigel, Grahame , THOMAS, Marian , WARD, Peter
IPC分类号： A61K38/05 , A61K9/00
CPC分类号： A61K9/008
摘要： The present invention relates to a pharmaceutical aerosol formulation comprising a hydrofluoroalkane (HFA) propellant having dissolved therein particulate (2S)-3-[4-({[4-(aminocarbonyl)-1-piperidinyl]carbonyl}oxy)phenyl]-2-[((2S)-4-methyl-2-{[2-(2-methylphenoxy)acetyl]amino}pentanoyl)amino] propanoic acid or a salt or solvate thereof. Methods and uses of the formulation in the treatment of respiratory disorders are also described, as are canisters and metered dose inhalers containing said formulation.

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