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1. 发明申请

US20090270444A1 1,7-Naphthyridines 审中-公开
标题翻译： 1,7-萘啶
公开(公告)号：US20090270444A1
公开(公告)日：2009-10-29
申请号：US11718892
申请日：2005-11-17
申请人： Colin David Eldred , John Edward Robinson , Alison Judith Steel
发明人： Colin David Eldred , John Edward Robinson , Alison Judith Steel
IPC分类号： A61K31/4375 , C07D471/04 , A61P37/08
CPC分类号： C07D471/04
摘要： There are provided according to the invention novel compounds of formula (I) and pharmaceutically acceptable salts and solvates thereof, wherein: R1 is phenyl which may be unsubstituted or substituted by one or two substituents selected from fluorine, chlorine, C1-2alkoxy-, —CN; phenyl fused to a 5-membered saturated ring containing one oxygen atom; pyridinyl which may be unsubstituted or substituted by one or two substituents selected from fluorine or chlorine; or C-linked pyrazolyl which may be unsubstituted or substituted by the substituent C1-2alkyl; R2 is C1-4alkyl; R3 is C1-2alkyl; and n is 0, 1 or 2.
摘要翻译：根据本发明，提供新的式（I）化合物及其药学上可接受的盐和溶剂化物，其中：R1是可以是未取代的或被一个或两个选自氟，氯，C 1-2烷氧基 - ， - CN; 与含有一个氧原子的5元饱和环稠合的苯基; 吡啶基，其可以是未取代的或被一个或两个选自氟或氯的取代基取代; 或C连接的吡唑基，其可以是未取代的或被取代基C 1-2烷基取代; R2是C1-4烷基; R3是C1-2烷基; n为0,1或2。

2. 发明申请

US20090312325A1 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：US20090312325A1
公开(公告)日：2009-12-17
申请号：US12474324
申请日：2009-05-29
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： A61K31/4709 , C07D401/12 , C07D417/12 , C07D403/12 , C07D215/38 , A61K31/47 , A61K31/5377 , A61P29/00 , A61P37/08
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。

3. 发明申请

US20080146563A1 1,7-Naphthyridines as Pde4 Inhibitors 审中-公开
标题翻译： 1,7-萘乙酸作为Pde4抑制剂
公开(公告)号：US20080146563A1
公开(公告)日：2008-06-19
申请号：US11908188
申请日：2006-03-16
申请人： Colin David Eldred , John Edward Robinson
发明人： Colin David Eldred , John Edward Robinson
IPC分类号： A61K31/5377 , C07D221/04 , A61K31/4375 , A61K31/496 , A61P37/08 , A61P29/00 , C07D295/00
CPC分类号： C07D471/04
摘要： There are provided according to the invention novel compounds of formula (I) and pharmaceutically acceptable salts and solvates thereof: wherein R1 is selected from the group consisting of C1-4alkyl, C4-6cycloalkyl(CH2)m—, methoxyC2-4alkyl, HOCH2CH2—, R3(O)2S(CH2)2—, R5R4NCO(CH2)n—, and heterocyclyl(CH2)m— wherein any nitrogen heteroatom of the heterocyclyl radical may be unsubstituted or substituted by methyl; R2 is hydrogen or methyl; R3 is methyl or NH2; R4-5 independently represent methyl, m is 0, 1 or 2; and n is 1 or 2; or R1 and R2 together with the nitrogen atom to which they are attached may form a heterocyclyl ring, which may be unsubstituted or substituted by one or two substituents selected from the group consisting of; methyl, ═O and (CH3)2N—.
摘要翻译：根据本发明提供新的式（I）化合物及其药学上可接受的盐和溶剂合物：其中R 1选自C 1-4烷基，烷基，C 4-6环烷基（CH 2 CH 2）m - ，甲氧基C 2-4烷基，（O）2 S 2（CH 2）2 - - - - （CH 2） R 2，R 5，R 5，R 5，N 2，N 2，和杂环基（CH 2 CH 2）m - ，其中杂环基的任何氮杂原子可以是未取代的或被甲基取代; R 2是氢或甲基; R 3是甲基或NH 2; R 4-5独立地表示甲基，m是0,1或2; n为1或2; 或R 1和R 2与它们所连接的氮原子一起可以形成杂环基环，其可以是未取代的或被一个或两个选自以下的取代基取代：组成; 甲基，-O和（CH 3）2 N - 。

4. 发明授权

US07566786B2 Quinoline derivatives as phosphodiesterase inhibitors 失效
标题翻译：喹啉衍生物作为磷酸二酯酶抑制剂
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。

5. 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。

6. 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。

7. 发明授权

US08658635B2 Benzpyrazol derivatives as inhibitors of PI3 kinases 有权
标题翻译：苯并吡唑衍生物作为PI3激酶的抑制剂
公开(公告)号：US08658635B2
公开(公告)日：2014-02-25
申请号：US12994250
申请日：2009-06-03
申请人： Ian Robert Baldwin , Kenneth David Down , Paul Faulder , Simon Gaines , Julie Nicole Hamblin , Joelle Le , Christopher James Lunniss , Nigel James Parr , Timothy John Ritchie , John Edward Robinson , Juliet Kay Simpson , Christian Alan Paul Smethurst
发明人： Ian Robert Baldwin , Kenneth David Down , Paul Faulder , Simon Gaines , Julie Nicole Hamblin , Joelle Le , Christopher James Lunniss , Nigel James Parr , Timothy John Ritchie , John Edward Robinson , Juliet Kay Simpson , Christian Alan Paul Smethurst
IPC分类号： A61K31/55 , A61K31/5377 , A61K31/501 , A61K31/496 , A61K31/497 , A61K31/50 , A61K31/505 , A61K31/4523 , A61K31/4427 , A61K31/427 , A61K31/425 , C07D267/02 , C07D279/12 , C07D295/00 , C07D265/30 , C07D413/14 , C07D487/12 , C07D417/12 , C07D211/00 , C07D277/20 , C07D235/00 , C07D233/54 , C07D403/14
CPC分类号： C07D231/56
摘要： The invention is directed to certain novel compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.
摘要翻译：本发明涉及某些新的式（I）化合物及其盐。本发明的化合物是PI3-激酶活性的抑制剂。

8. 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。

9. 发明申请

US20120245171A1 BENZPYRAZOLE DERIVATIVES AS INHIBITORS OF PI3 KINASES 审中-公开
标题翻译：作为PI3 KINASES的抑制剂的苯并噻唑衍生物
公开(公告)号：US20120245171A1
公开(公告)日：2012-09-27
申请号：US13513063
申请日：2010-12-03
申请人： Ian Robert Baldwin , Kenneth David Down , Paul Faulder , Simon Gaines , Julie Nicole Hamblin , Katherine Louise Jones , Paul Spencer Jones , Joelle Le , Christopher James Lunniss , Nigel James Parr , Timothy John Ritchie , John Edward Robinson , Juliet Kay Simpson , Christian Alan Paul Smethurst
发明人： Ian Robert Baldwin , Kenneth David Down , Paul Faulder , Simon Gaines , Julie Nicole Hamblin , Katherine Louise Jones , Paul Spencer Jones , Joelle Le , Christopher James Lunniss , Nigel James Parr , Timothy John Ritchie , John Edward Robinson , Juliet Kay Simpson , Christian Alan Paul Smethurst
IPC分类号： A61K31/4985 , C07D417/14 , A61K31/496 , C07D413/14 , A61K31/5377 , C07D471/04 , A61P37/00 , A61P29/00 , A61P9/00 , A61P35/00 , A61P25/28 , A61P1/18 , A61P13/12 , A61P7/04 , A61P15/08 , A61P37/06 , A61P11/00 , A61P25/00 , A61P11/06 , A61P37/08 , A61P17/00 , A61P1/00 , A61P7/02 , A61P9/10 , C07D487/04
CPC分类号： C07D487/04 , C07D401/04 , C07D401/14 , C07D405/14 , C07D417/04 , C07D471/04
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 PI3-kinase activity.
摘要翻译：本发明涉及某些新化合物。具体地，本发明涉及式（I）的化合物及其盐。本发明的化合物是PI3-激酶活性的抑制剂。

10. 发明申请

US20110183973A1 Novel Compounds 有权
标题翻译：新型化合物
公开(公告)号：US20110183973A1
公开(公告)日：2011-07-28
申请号：US12994254
申请日：2009-06-03
申请人： Ian Robert Baldwin , Kenneth David Down , Paul Faulder , Simon Gaines , Julie Nicole Hamblin , Paul Spencer Jones , Joelle Le , Nigel James Parr , Timothy John Ritchie , John Edward Robinson , Juliet Kay Simpson , Christian Alan Paul Smethurst
发明人： Ian Robert Baldwin , Kenneth David Down , Paul Faulder , Simon Gaines , Julie Nicole Hamblin , Paul Spencer Jones , Joelle Le , Nigel James Parr , Timothy John Ritchie , John Edward Robinson , Juliet Kay Simpson , Christian Alan Paul Smethurst
IPC分类号： A61K31/5377 , C07D231/56 , A61K31/416 , C07D401/14 , A61K31/454 , C07D413/14 , A61K31/4439 , A61P35/00 , A61P3/00 , A61P7/00 , A61P11/00 , A61P19/00 , A61P25/04 , A61P29/00 , A61P37/06
CPC分类号： C07D403/04 , C07D401/14 , C07D403/14 , C07D413/14 , C07D471/04
摘要： The invention is directed to certain novel compounds directed to compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.
摘要翻译：本发明涉及针对式（I）化合物及其盐的某些新化合物。本发明的化合物是PI3-激酶活性的抑制剂。

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