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公开(公告)号：US07321059B2
公开(公告)日：2008-01-22
申请号：US10492606
申请日：2002-10-17
CPC分类号： A61K9/008 , B01F17/0028 , B01F17/0035
摘要： Compounds of formula (I): or salts or solvate thereof, wherein: n and N independently represent an integer 2 to 12; m1 and m2 independently represent an integer 1 to 15; and R1 and R2 independently represent —(CO)xC1-9 alkyl or —(CO)xC1-9 fluoroalkyl, which fluoroalkyl moiety contains at least 1 fluorine atom and not more than 3 consecutive perfluorocarbon atoms wherein x represents 0 or 1, as well as pharmaceutical formulations containing such compounds and processes for the manufacture of such compounds are disclosed. Intermediates of such compounds and processes for the manufacture of such intermediates are also disclosed.
摘要翻译： 式（I）化合物或其盐或溶剂合物，其中：n和n独立地表示2-12的整数; m 1和m 2独立地表示1〜15的整数， 且R 1和R 2独立地表示 - （CO）1 -C 12烷基或 - （CO ）氟烷基部分含有至少1个氟原子和不多于3个连续的全氟化碳原子，其中x表示0或1，以及药物 公开了含有这些化合物的制剂和制备这些化合物的方法。 还公开了这些化合物的中间体和制备这种中间体的方法。
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公开(公告)号：US06528494B2
公开(公告)日：2003-03-04
申请号：US10025678
申请日：2001-12-19
申请人： Brian Cox , Suzanne Elaine Keeling , David George Allen , Alison Judith Redgrave , Michael David Barker , Heather Hobbs , Thomas Davis Roper, IV , Joanna Victoria Geden
发明人： Brian Cox , Suzanne Elaine Keeling , David George Allen , Alison Judith Redgrave , Michael David Barker , Heather Hobbs , Thomas Davis Roper, IV , Joanna Victoria Geden
IPC分类号： A01N4304
CPC分类号： C07D473/00 , C07H19/16 , Y10S514/826 , Y10S514/851 , Y10S514/885 , Y10S514/921 , Y10S514/925
摘要： There are provided according to the invention novel compounds of formula I wherein R1, R2 and R3 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，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炎性疾病中的应用。
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公开(公告)号：US07195752B2
公开(公告)日：2007-03-27
申请号：US10485595
申请日：2002-08-02
CPC分类号： A61K9/008 , A61K31/137 , A61K31/56 , A61K47/12 , C07C59/135 , C07C69/63 , C07C69/708 , C09K3/30
摘要： A pharmaceutical aerosol formulation that includes a particulate medicament, one or more fluorocarbon or hydrogen-containing fluorocarbon propellants and a compound of the general formula (I) or a salt or solvate thereof is disclosed, wherein A represents a straight chain C1-16 alkylene substituted by n groups of formula B; n represents an integer 1 to 3; and B independently represents C1-4 fluoroalkylC0-6 alkylene-, C1-4 fluoroalkylC0-6 alkylene-O—, or C1-4 alkylC0-6 alkylene-O— wherein at least one substituent of formula B contains at least one fluorine atom and each C1-4 fluoroalkyl- moiety contains one or more fluorine atoms but not more than 3 consecutive perfluorinated carbon atoms. Compounds of formula (I) and uses of such compounds are also disclosed.
摘要翻译： 一种药物气溶胶制剂，其包含颗粒药物，一种或多种含氟碳或含氢碳氟化合物推进剂和通式（I）的化合物，
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公开(公告)号：US07566786B2
公开(公告)日：2009-07-28
申请号：US10557079
申请日：2004-05-19
申请人： Ian Robert Baldwin , Michael David Barker , Anthony William Dean , Colin David Eldred , Brian Evans , Sharon Lisa Gough , Stephen Barry Guntrip , Julie Nicole Hamblin , Stuart Holman , Paul Jones , Mika Kristian Lindvall , Christopher James Lunniss , Tracy Jane Redfern , Alison Judith Redgrave , John Edward Robinson , Michael Woodrow
发明人： Ian Robert Baldwin , Michael David Barker , Anthony William Dean , Colin David Eldred , Brian Evans , Sharon Lisa Gough , Stephen Barry Guntrip , Julie Nicole Hamblin , Stuart Holman , Paul Jones , Mika Kristian Lindvall , Christopher James Lunniss , Tracy Jane Redfern , Alison Judith Redgrave , John Edward Robinson , Michael Woodrow
IPC分类号： C07D215/38 , C07D215/44
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 治疗炎症性疾病。
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![PYRAZOLO [3,4-B] PYRIDINE COMPOUNDS, AND THEIR USE AS PDE4 INHIBITORS](/abs-image/US/2008/06/05/US20080132536A1/abs.jpg.150x150.jpg)
15.发明申请PYRAZOLO [3,4-B] PYRIDINE COMPOUNDS, AND THEIR USE AS PDE4 INHIBITORS 审中-公开吡咯并[3,4-B]吡啶化合物及其用作PDE4抑制剂公开(公告)号：US20080132536A1
公开(公告)日：2008-06-05
申请号：US12022372
申请日：2008-01-30
申请人： David George Allen , Diane Mary Coe , Caroline Mary Cook , Michael Dennis Dowle , Christopher David Edlin , Julie Nicole Hamblin , Martin Redpath Johnson , Paul Spencer Jones , Mika Kristian Lindvall , Charlotte Jane Mitchell , Alison Judith Redgrave , John Edward Robinson , Naimisha Trivedi
发明人： David George Allen , Diane Mary Coe , Caroline Mary Cook , Michael Dennis Dowle , Christopher David Edlin , Julie Nicole Hamblin , Martin Redpath Johnson , Paul Spencer Jones , Mika Kristian Lindvall , Charlotte Jane Mitchell , Alison Judith Redgrave , John Edward Robinson , Naimisha Trivedi
IPC分类号： A61K31/437 , A61P11/00 , A61P19/02 , A61P37/08 , A61P17/00 , C07D471/04 , A61K31/4545 , C07D487/04
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 R3 is optionally substituted C3-8cycloalkyl, optionally substituted C5-7cycloalkenyl, an optionally substituted heterocyclic group (aa), (bb) or (cc), or a bicyclic group (ee); and wherein R4 is H, C1-3alkyl, C1-2fluoroalkyl, cyclopropyl, —CH2OR4a, —CH(Me)OR4a, or —CH2CH2OR4a; and R5 is inter alia H, C1-8alkyl, C1-3fluoroalkyl, C3-8cycloalkyl, certain substituted alkyl groups, —(CH2)n13-Het, or optionally substituted phenyl or —CH2-Ph; or R4 and R5 taken together are —(CH2)p1— or —(CH2)p3—X5—(CH2)p4—; provided that at least one of R4 and R5 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个环烷基，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为H，C 1-3烷基，C 1-12氟代烷基，环丙基，-CH 2， -CH（Me）OR 4a或-CH 2 H 2 CH 2或-O SUP > 4a ; 且R 5特别是H，C 1-8烷基，C 1-3烷基，C 3-8 - 某些取代的烷基， - （CH 2）n - ，或任选取代的苯基或-CH 2 - 2 - 或 - （CH 2）2 - - - - （CH 2） 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病（COPD），哮喘，类风湿性关节炎， 过敏性鼻炎或特应性皮炎。
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公开(公告)号：US07217833B2
公开(公告)日：2007-05-15
申请号：US10504252
申请日：2003-02-12
摘要： Compounds of formula (I) or a salt or solvate thereof, wherein: x represents 0 or 1; y represents 0 or 1; R1 and R2 independently represent —C1-9 alkyleneC1-6 fluoroalkyl, which fluoroalkyl moiety contains at least 1 fluorine atom and not more than 3 consecutive perfluorocarbon atoms and wherein the R1 and/or R2 moiety is optionally interrupted by an ether link, processes for their preparation, use of the compounds in the preparation of pharmaceutical formulations and the formulations are described.
摘要翻译： 式（I）化合物或其盐或溶剂合物，其中：x表示0或1; y表示0或1; R 1和R 2独立地代表-C 1-6 - 亚烷基C 1-6 - 氟代烷基，该氟烷基部分含有 至少1个氟原子和不超过3个连续的全氟化碳原子，其中R 1和/或R 2 O 2部分任选地被醚键中断，其制备方法 描述了制备药物制剂和制剂中化合物的用途。
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