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1. 发明授权

US08003663B2 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：US08003663B2
公开(公告)日：2011-08-23
申请号：US11831325
申请日：2007-07-31
申请人： David George Allen , Rodger Phillip Barnett , Reshma Manesh Chudasama , Caroline Jane Day , Christopher David Edlin , Leanda Jane Kindon
发明人： David George Allen , Rodger Phillip Barnett , Reshma Manesh Chudasama , Caroline Jane Day , Christopher David Edlin , Leanda Jane Kindon
IPC分类号： A61K31/437 , C07D471/04
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}-4-({8-[(2-hydroxyethyl) (methyl)amino]octanoyl}amino)benzamide, whose formula is or a salt thereof, such as the monohydrochloride salt thereof. The invention also provides the use of the compound or salt 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, or rhinitis (e.g. allergic and/or non-allergic rhinitis).
摘要翻译：本发明提供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} -4 - （{ 8 - [（2-羟乙基）（甲基）氨基]辛酰基}氨基）苯甲酰胺，其为其盐或其盐，例如其一盐酸盐。本发明还提供了化合物或盐作为磷酸二酯酶IV（PDE4）的抑制剂和/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疾病（COPD），哮喘或鼻炎（例如过敏性和/或非过敏性鼻炎）。

2. 发明申请

US20090325952A1 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：US20090325952A1
公开(公告)日：2009-12-31
申请号：US12375685
申请日：2007-07-31
申请人： David George Allen , Nicola Mary Aston , Rodger Phillip Barnett , Reshma Manesh Chudasama , Caroline Jane Day , Christopher David Edlin , Leanda Jane Kindon , Naimisha Trivedi
发明人： David George Allen , Nicola Mary Aston , Rodger Phillip Barnett , Reshma Manesh Chudasama , Caroline Jane Day , Christopher David Edlin , Leanda Jane Kindon , Naimisha Trivedi
IPC分类号： A61K31/437 , C07D471/04 , A61K31/5377 , A61P29/00 , A61P37/08 , A61P11/00
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): as defined herein, and the use of the compounds as inhibitors of PDE4.
摘要翻译：本发明提供式（I）化合物或其盐：其中Ar具有如下定义的亚式（x）：以及该化合物作为PDE4抑制剂的用途。

3. 发明申请

US20090326003A1 PYRAZOLO (3, 4-B) PYRIDINE DERIVATIVES AS PDE4 INHIBITORS 审中-公开
标题翻译： PYRAZOLO（3，4-B）吡啶衍生物作为PDE4抑制剂
公开(公告)号：US20090326003A1
公开(公告)日：2009-12-31
申请号：US12374331
申请日：2007-07-19
申请人： David George Allen , Michael Dennis Dowle , Christopher David Edlin , Leanda Jane Kindon
发明人： David George Allen , Michael Dennis Dowle , Christopher David Edlin , Leanda Jane Kindon
IPC分类号： A61K31/437 , C07D471/04 , A61P11/06 , A61P17/06
CPC分类号： C07D519/00
摘要： The present invention provides a compound of formula (I) or a salt thereof (in particular, a pharmaceutically acceptable salt thereof): The invention also provides the use of the compounds or salts as inhibitors of phosphodiesterase type IV (PDE4) for the treatment or prophylaxis of inflammatory or allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rhinitis, atopic dermatitis or psoriasis, e.g. in a mammal such as a human.
摘要翻译：本发明提供式（I）化合物或其盐（特别是其药学上可接受的盐）：本发明还提供了化合物或盐作为IV型磷酸二酯酶抑制剂（PDE4）用于治疗或预防炎症或过敏性疾病如慢性阻塞性肺疾病（COPD），哮喘，鼻炎，特应性皮炎或牛皮癣，例如在哺乳动物如人中。

4. 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。

5. 发明授权

US07709497B2 Pyrazolo[3,4-b]pyridine compound, and its use as a PDE4 inhibitor 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：US07709497B2
公开(公告)日：2010-05-04
申请号：US10598838
申请日：2005-03-15
申请人： Siegfried Benjamin Christensen, IV , Caroline Mary Cook , Christopher David Edlin , Martin Redpath Johnson , Paul Spencer Jones , Mika Kristian Lindvall , Amyn Pyarali Sayani , Naimisha Trivedi , Lionel Trottet
发明人： Siegfried Benjamin Christensen, IV , Caroline Mary Cook , Christopher David Edlin , Martin Redpath Johnson , Paul Spencer Jones , Mika Kristian Lindvall , Amyn Pyarali Sayani , Naimisha Trivedi , Lionel Trottet
IPC分类号： A61K31/44 , A01N43/42 , C07D471/02 , C07D491/02 , C07D498/02
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-carboxamide, which is the compound of formula (I): or a salt thereof.
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 甲酰胺，其为式（I）的化合物或其盐。

6. 发明申请

US20090318494A1 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：US20090318494A1
公开(公告)日：2009-12-24
申请号：US12375695
申请日：2007-08-01
申请人： David George Allen , Nicola Mary Aston , Naimisha Trivedi , Christopher David Edlin
发明人： David George Allen , Nicola Mary Aston , Naimisha Trivedi , Christopher David Edlin
IPC分类号： A61K31/437 , C07D471/04 , A61P29/00 , A61P11/00
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 (w), (y), (z1) or (z2): wherein the several groups are defined herein below, and the use of these compounds as inhibitors of phosphodiesterase type IV (PDE4).
摘要翻译：本发明提供式（I）化合物或其盐：其中Ar具有下式（w），（y），（z1）或（z2）：其中数个基团如下文所定义，的这些化合物作为磷酸二酯酶IV（PDE4）的抑制剂。

7. 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。

8. 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。

9. 发明申请

US20080275078A1 Pyrazolo[3,4-B] Pyridine Compounds and Their Use as Pde4 Inhibitors 审中-公开
标题翻译：吡唑并[3,4-B]吡啶化合物及其用作Pde4抑制剂
公开(公告)号：US20080275078A1
公开(公告)日：2008-11-06
申请号：US10598973
申请日：2005-03-15
申请人： Caroline Mary Cook , Michael Dennis Dowle , Christopher David Edlin , Martin Redpath Johnson , Paul Spencer Jones , Mika Kristian Lindvall , Naimisha Trivedi , Alison Judith Redgrave
发明人： Caroline Mary Cook , Michael Dennis Dowle , Christopher David Edlin , Martin Redpath Johnson , Paul Spencer Jones , Mika Kristian Lindvall , Naimisha Trivedi , Alison Judith Redgrave
IPC分类号： A61K31/437 , C07D487/04 , A61P11/06
CPC分类号： C07D471/04
摘要： The invention provides a compound of formula (I) or a salt thereof: wherein: R1 is C1-3alkyl, C1-3fluoroalkyl, or —CH2CH2OH; R2 is hydrogen, methyl or C1fluoroalkyl; R3 is of sub-formula (aa) or (bb): wherein Y is NCONH2 and n1 is 0 or 1; R4 is H; and R5 is a group of the sub-formula (x), (y), (y1) or (z): These compounds are PDE4 inhibitors.
摘要翻译：本发明提供式（I）化合物或其盐：其中：R 1是C 1-3烷基，C 1-3 氟代烷基或-CH 2 CH 2 OH; R 2是氢，甲基或C 1氟代烷基; R 3是亚式（aa）或（bb）：其中Y是NCONH 2和n 1是0或1; R 4是H; 和R 5是子式（x），（y），（y1）或（z）的一组：这些化合物是PDE4抑制剂。

10. 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。

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