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1. 发明授权

US07465743B2 Pyrazolo[3,4-b]pyridine compounds, and their use as PDE4 inhibitors 失效
标题翻译：吡唑并[3,4-b]吡啶化合物及其作为PDE4抑制剂的用途
公开(公告)号：US07465743B2
公开(公告)日：2008-12-16
申请号：US10598944
申请日：2005-03-15
申请人： Diane Mary Coe , Caroline Mary Cook , Anthony William James Cooper , Christopher David Edlin , Julie Nicole Hamblin , Martin Redpath Johnson , Paul Spencer Jones , Mika Kristian Lindvall , Charlotte Jane Mitchell , Alison Judith Redgrave , John Edward Robinson
发明人： Diane Mary Coe , Caroline Mary Cook , Anthony William James Cooper , Christopher David Edlin , Julie Nicole Hamblin , Martin Redpath Johnson , Paul Spencer Jones , Mika Kristian Lindvall , Charlotte Jane Mitchell , Alison Judith Redgrave , John Edward Robinson
IPC分类号： A01N43/42 , A61K31/44 , C07D471/02 , C07D491/02 , C07D498/02 , C07D513/02 , C07D515/02
CPC分类号： C07D471/04
摘要： The invention relates to a compound of formula (I) or a salt thereof: wherein: R1 is Et, n-Pr, i-Pr, C2fluoroalkyl, or —CH2CH2OH; R2 is H, Me, Et, n-Pr, i-Pr, C1-2fluoroalkyl, cyclopropyl or (cyclopropyl)methyl-; and NHR3 has the sub-formula (nhr3): wherein R3a is methyl or ethyl; R3b is H, methyl or ethyl; R3c is H, methyl or ethyl, R3d is H, methyl or ethyl, and R3e is H or methyl, provided that: (a) R3b is methyl or ethyl; and/or (b) R3c and R3d are independently methyl or ethyl; and provided that: (c) when R3c is ethyl and/or when R3d is ethyl and/or when R3e is methyl, then: R3a is methyl and/or R3b is hydrogen or methyl. These compounds are PDE4 inhibitors.
摘要翻译：本发明涉及式（I）化合物或其盐：其中：R 1为Et，n-Pr，i-Pr，C 2 F 2烷基或-CH 2 CH 2 OH; R2是H，Me，Et，n-Pr，i-Pr，C1-2氟烷基，环丙基或（环丙基）甲基; 和NHR 3具有子式（nhr3）：其中R3a是甲基或乙基; R3b是H，甲基或乙基; R3c是H，甲基或乙基，R3d是H，甲基或乙基，R3e是H或甲基，条件是：（a）R3b是甲基或乙基; 和/或（b）R3c和R3d独立地是甲基或乙基; 并且条件是：（c）当R3c是乙基和/或当R3d是乙基和/或当R3e是甲基时，则：R3a是甲基和/或R3b是氢或甲基。这些化合物是PDE4抑制剂。

2. 发明授权

US07528148B2 Pyrazolo[3,4-B]pyridine compounds, and their use as phosphodiesterase inhibitors 失效
标题翻译：吡唑并[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：US07528148B2
公开(公告)日：2009-05-05
申请号：US10540371
申请日：2003-12-19
申请人： David George Allen , Diane Mary Coe , Caroline Mary Cook , Anthony William James Cooper , Michael Dennis Dowle , Christopher David Edlin , Julie Nicole Hamblin , Martin Redpath Johnson , Paul Spencer Jones , Mika Kristian Lindvall , Charlotte Jane Mitchell , Alison Judith Redgrave
发明人： David George Allen , Diane Mary Coe , Caroline Mary Cook , Anthony William James Cooper , Michael Dennis Dowle , Christopher David Edlin , Julie Nicole Hamblin , Martin Redpath Johnson , Paul Spencer Jones , Mika Kristian Lindvall , Charlotte Jane Mitchell , Alison Judith Redgrave
IPC分类号： C07D471/02 , C07D491/02 , C07D498/02 , C07D513/02 , C07D515/02 , A01N43/42 , A61K31/44
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 or —(CH2)2OH; R2 is a hydrogen atom (H), methyl or C1fluoroalkyl; R3a is a hydrogen atom (H) or C1-3alkyl; R3 is optionally substituted branched C3-6alkyl, optionally substituted C3-8cycloalkyl, optionally substituted mono-unsaturated-C5-7cycloalkenyl, optionally substituted phenyl, or an optionally substituted heterocyclic group of sub-formula (aa), (bb) or (cc): in which n1 and n2 independently are 1 or 2; and Y is O, S, SO2, or NR4; and wherein Het is of sub-formula (i), (ii), (iii), (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：其中：R 1为C 1-4烷基，C 1-3氟烷基或 - （CH 2）2 OH; R2是氢原子（H），甲基或C1-4烷基; R3a是氢原子（H）或C1-3烷基; R 3是任选取代的支链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），（bb）或（cc）其中n1和n2独立地为1或2; Y是O，S，SO 2或NR 4; 并且其中Het为亚式（i），（ii），（iii），（iv）或（v）：所述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。

3. 发明申请

US20080132536A1 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：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。

4. 发明申请

US20080175914A1 Pyrazolo[3,4-b]Pyridine Compounds, and their Use as Phosphodiesterase Inhibitors 审中-公开
标题翻译：吡唑并[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：US20080175914A1
公开(公告)日：2008-07-24
申请号：US12013529
申请日：2008-01-14
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 , Richard Graham Knowles , Mika Kristian Lindvall , Charlotte Jane Mitchell , Alison Judith Redgrave , Peter Ward
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 , Richard Graham Knowles , Mika Kristian Lindvall , Charlotte Jane Mitchell , Alison Judith Redgrave , Peter Ward
IPC分类号： A61K9/14 , C07D487/04 , A61P29/00 , A61P11/00 , A61P37/08 , A61K31/437
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是C 1-4烷基，C 1-3烷基，氟代烷基，-CH 2 CH 2 OH或-CH 2 CH 2 CO 2， C 1-12烷基; R 2是氢原子（H），甲基或C 1氟代烷基; R 3是任选取代的C 3-8环烷基或任选取代的单不饱和C 5〜5-7环烯基或任选取代的杂环基子公式（aa），（bb）或（cc）; 其中n 1和n 2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）：其中X是NR 4 R 5或OR 5a 。化合物是磷酸二酯酶（PDE）抑制剂，特别是PDE 4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。

5. 发明申请

US20090131431A1 Pyrazolo[3,4-b]pyridine compounds, and their use as a PDE4 inhibitors 审中-公开
标题翻译：吡唑并[3,4-b]吡啶化合物，以及它们作为PDE4抑制剂的用途
公开(公告)号：US20090131431A1
公开(公告)日：2009-05-21
申请号：US12067990
申请日：2006-09-29
申请人： Christopher David Edlin , Stuart Holman , Paul Spencer Jones , Suzanne Elaine Keeling , Mika Kristian Lindvall , Charlotte Jane Mitchell , Naimisha Trivedi
发明人： Christopher David Edlin , Stuart Holman , Paul Spencer Jones , Suzanne Elaine Keeling , Mika Kristian Lindvall , Charlotte Jane Mitchell , Naimisha Trivedi
IPC分类号： A61K31/5377 , C07D471/04 , A61P17/06 , A61K31/496 , A61K31/437
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)—C1 fluoroalkyl, —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—C1-6alkyl, —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 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 COPD and the like.
摘要翻译：本发明提供式（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; R3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）; Ra是H，甲基或乙基; Rb是H或甲基; R 4是H，甲基，乙基，正丙基，-C（O）-Me或-C（O）-C 1-6氟烷基; 并且R 5是：-C（O） - （CH 2）n -Ar，-C（O）-Het，-C（O）-C 1-6烷基，-C（O）-C 1氟代烷基，-C（O）（CH 2）2 -C（O）-NR 15 b N R 15 b，-C（O）-CH 2 -C（O）-NR 15 b NR 15 b，-C（O）-NR 15 b - （CH 2）m -Ar，-C（O） C（O）-NR 15 b -C 1-6烷基，-C（O）-NR 5 R 5a，-S（O）2 - （CH 2）m -Ar，-S（O）2 -Het，-S（O） 2-C 1-6烷基或-CH 2 -Ar; 或（R 4）和R 5和R 5一起为 - （CH 2）p1 - ， - （CH 2）2 -X 5 - （CH 2）2 - ， - - （CH 2）p3-; 或NR4R5为子式（y），（y1），（y2）或（y3）。本发明提供了化合物作为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COPD等的用途。

6. 发明申请

US20130165433A1 Novel Use 有权
标题翻译：小说使用
公开(公告)号：US20130165433A1
公开(公告)日：2013-06-27
申请号：US13821594
申请日：2011-09-06
申请人： Ian Robert Baldwin , Kenneth David Down , Paul Faulder , Simon Gaines , Julie Nicole Hamblin , Zoe Alicia Harrison , Katherine Louise Jones , Paul Spencer Jones , Suzanne Elaine Keeling , Joelle Le , Christopher James Lunniss , Charlotte Jane Mitchell , Nigel James Parr , Timothy John Ritchie , John Edward Robinson , Juliet Kay Simpson , Christopher Alan Paul Smethurst , Yoshiaki Washio
发明人： Ian Robert Baldwin , Kenneth David Down , Paul Faulder , Simon Gaines , Julie Nicole Hamblin , Zoe Alicia Harrison , Katherine Louise Jones , Paul Spencer Jones , Suzanne Elaine Keeling , Joelle Le , Christopher James Lunniss , Charlotte Jane Mitchell , Nigel James Parr , Timothy John Ritchie , John Edward Robinson , Juliet Kay Simpson , Christopher Alan Paul Smethurst , Yoshiaki Washio
IPC分类号： C07D413/14
CPC分类号： A61K31/5377 , A61K31/416 , A61K31/422 , A61K31/4245 , A61K31/427 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/5386 , C07D413/14
摘要： The present invention is directed to compounds for use in the treatment or prevention of influenza virus infection.
摘要翻译：本发明涉及用于治疗或预防流感病毒感染的化合物。

7. 发明授权

US08735390B2 Polymorphs and salts 有权
标题翻译：多晶型物和盐类
公开(公告)号：US08735390B2
公开(公告)日：2014-05-27
申请号：US13821585
申请日：2011-09-06
申请人： Julie Nicole Hamblin , Paul Spencer Jones , Suzanne Elaine Keeling , Joelle Le , Charlotte Jane Mitchell , Nigel James Parr , Robert David Willacy
发明人： Julie Nicole Hamblin , Paul Spencer Jones , Suzanne Elaine Keeling , Joelle Le , Charlotte Jane Mitchell , Nigel James Parr , Robert David Willacy
IPC分类号： A61K31/5377 , C07D413/14
CPC分类号： A61K31/5377 , C07D413/14
摘要： The present invention is directed to novel polymorphs and salts of a compound which is an inhibitor of kinase activity.
摘要翻译：本发明涉及作为激酶活性抑制剂的化合物的新型多晶型物和盐。

8. 发明授权

US08609657B2 Compounds 有权
公开(公告)号：US08609657B2
公开(公告)日：2013-12-17
申请号：US13633230
申请日：2012-10-02
申请人： Julie Nicole Hamblin , Paul Spencer Jones , Suzanne Elaine Keeling , Joelle Le , Charlotte Jane Mitchell , Nigel James Parr
发明人： Julie Nicole Hamblin , Paul Spencer Jones , Suzanne Elaine Keeling , Joelle Le , Charlotte Jane Mitchell , Nigel James Parr
IPC分类号： A61K31/535 , C07D413/14
CPC分类号： A61K31/5377 , A61K31/496 , A61K31/497 , A61K31/535 , A61K45/06 , C07B2200/13 , C07D413/14 , Y02A50/409
摘要： 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.

9. 发明申请

US20130165441A1 Novel Polymorphs and Salts 有权
公开(公告)号：US20130165441A1
公开(公告)日：2013-06-27
申请号：US13821585
申请日：2011-09-06
申请人： Julie Nicole Hamblin , Paul Spencer Jones , Suzanne Elaine Keeling , Joelle Le , Charlotte Jane Mitchell , Nigel James Parr , Robert David Willacy
发明人： Julie Nicole Hamblin , Paul Spencer Jones , Suzanne Elaine Keeling , Joelle Le , Charlotte Jane Mitchell , Nigel James Parr , Robert David Willacy
IPC分类号： C07D413/14
CPC分类号： A61K31/5377 , C07D413/14
摘要： The present invention is directed to novel polymorphs and salts of a compound which is an inhibitor of kinase activity.

10. 发明授权

US09326987B2 Indazole derivatives for use in the treatment of influenza virus infection 有权
标题翻译：用于治疗流感病毒感染的吲唑衍生物
公开(公告)号：US09326987B2
公开(公告)日：2016-05-03
申请号：US13821594
申请日：2011-09-06
申请人： Julie Nicole Hamblin , Paul Spencer Jones , Suzanne Elaine Keeling , Joelle Le , Charlotte Jane Mitchell , Nigel James Parr
发明人： Julie Nicole Hamblin , Paul Spencer Jones , Suzanne Elaine Keeling , Joelle Le , Charlotte Jane Mitchell , Nigel James Parr
IPC分类号： A61K31/535 , A61K31/497 , A61K31/445 , A61K31/55 , A61K31/5377 , C07D413/14 , A61K31/416 , A61K31/422 , A61K31/4245 , A61K31/427 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/5386
CPC分类号： A61K31/5377 , A61K31/416 , A61K31/422 , A61K31/4245 , A61K31/427 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/5386 , C07D413/14
摘要： The present invention is directed to compounds for use in the treatment or prevention of influenza virus infection.
摘要翻译：本发明涉及用于治疗或预防流感病毒感染的化合物。

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