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1. 发明授权

US06897207B2 Azaindoles 失效
标题翻译：楝树
公开(公告)号：US06897207B2
公开(公告)日：2005-05-24
申请号：US10177804
申请日：2002-06-21
申请人： Paul J. Cox , Tahir N. Majid , Justine Yeun Quai Lai , Andrew D. Morley , Shelley Amendola , Stephanie D. Deprets , Christopher Edlin , Charles J. Gardner , Dorothea Kominos , Brian L. Pedgrift , Frank Halley , Timothy A. Gillespy , Michael Edwards , Francois F. Clerc , Conception Nemecek , Olivier Houille , Dominique Damour , Herve Bouchard , Daniel N. A. Bezard , Chantal Carrez
发明人： Paul J. Cox , Tahir N. Majid , Justine Yeun Quai Lai , Andrew D. Morley , Shelley Amendola , Stephanie D. Deprets , Christopher Edlin , Charles J. Gardner , Dorothea Kominos , Brian L. Pedgrift , Frank Halley , Timothy A. Gillespy , Michael Edwards , Francois F. Clerc , Conception Nemecek , Olivier Houille , Dominique Damour , Herve Bouchard , Daniel N. A. Bezard , Chantal Carrez
IPC分类号： A61K20060101 , A61K31/437 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/4985 , A61K31/5355 , A61K31/5377 , A61K31/541 , A61P20060101 , A61P9/00 , A61P11/00 , A61P11/02 , A61P11/06 , A61P13/08 , A61P17/00 , A61P17/02 , A61P17/06 , A61P19/02 , A61P27/14 , A61P29/00 , A61P35/00 , A61P37/08 , A61P43/00 , C07D20060101 , C07D209/00 , C07D221/00 , C07D241/00 , C07D471/04 , C07D487/04 , C07D519/00 , A61K31/33 , A61K31/66 , C07D417/02
CPC分类号： C07D519/00 , C07D471/04 , C07D487/04
摘要： The invention is directed to physiologically active compounds of general formula (I): and compositions containing such compounds; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (I). Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases.
摘要翻译：本发明涉及通式（I）的生理活性化合物：和含有这些化合物的组合物; 及其前药，以及这些化合物及其前药的药学上可接受的盐和溶剂合物，以及式（I）范围内的新化合物。这些化合物和组合物具有有价值的药物特性，特别是抑制激酶的能力。

2. 发明授权

US07943616B2 Azaindoles for inhibiting aurora2 and other kinases 失效
标题翻译：抑制极光2和其他激酶的阿魏酸
公开(公告)号：US07943616B2
公开(公告)日：2011-05-17
申请号：US10995103
申请日：2004-11-23
申请人： Paul J. Cox , Tahir N. Majid , Justine Yeun Quai Lai , Andrew D. Morley , Shelley Amendola , Stephanie D. Deprets , Christopher Edlin , Charles J. Gardner , Dorothea Kominos , Brian L. Pedgrift , Frank Halley , Timothy A. Gillespy , Michael Edwards , Francois F. Clerc , Conception Nemecek , Olivier Houille , Dominique Damour , Herve Bouchard , Daniel N. A. Bezard , Chantal Carrez
发明人： Paul J. Cox , Tahir N. Majid , Justine Yeun Quai Lai , Andrew D. Morley , Shelley Amendola , Stephanie D. Deprets , Christopher Edlin , Charles J. Gardner , Dorothea Kominos , Brian L. Pedgrift , Frank Halley , Timothy A. Gillespy , Michael Edwards , Francois F. Clerc , Conception Nemecek , Olivier Houille , Dominique Damour , Herve Bouchard , Daniel N. A. Bezard , Chantal Carrez
IPC分类号： C07D487/04 , A61K31/5025 , A61P29/00 , A61P35/00 , A61P19/02
CPC分类号： C07D519/00 , C07D471/04 , C07D487/04
摘要： The invention is directed to physiologically active compounds of general formula (I):— and compositions containing such compounds; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (I). Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases.
摘要翻译：本发明涉及通式（I）的生理活性化合物： - 含有这些化合物的组合物; 及其前药，以及这些化合物及其前药的药学上可接受的盐和溶剂合物，以及式（I）范围内的新化合物。这些化合物和组合物具有有价值的药物特性，特别是抑制激酶的能力。

3. 发明申请

US20050267304A1 Azaindoles 失效
标题翻译：楝树
公开(公告)号：US20050267304A1
公开(公告)日：2005-12-01
申请号：US10995103
申请日：2004-11-23
申请人： Paul Cox , Tahir Majid , Justine Lai , Andrew Morley , Shelley Amendola , Stephanie Deprets , Christopher Edlin , Charles Gardner , Dorothea Kominos , Brian Pedgrift , Frank Halley , Timothy Gillespy , Michael Edwards , Francois Clerc , Conception Nemecek , Olivier Houille , Dominique Damour , Herve Bouchard , Daniel Bezard , Chantal Carrez
发明人： Paul Cox , Tahir Majid , Justine Lai , Andrew Morley , Shelley Amendola , Stephanie Deprets , Christopher Edlin , Charles Gardner , Dorothea Kominos , Brian Pedgrift , Frank Halley , Timothy Gillespy , Michael Edwards , Francois Clerc , Conception Nemecek , Olivier Houille , Dominique Damour , Herve Bouchard , Daniel Bezard , Chantal Carrez
IPC分类号： A61K20060101 , A61K31/437 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/4985 , A61K31/5355 , A61K31/5377 , A61K31/541 , A61P20060101 , A61P9/00 , A61P11/00 , A61P11/02 , A61P11/06 , A61P13/08 , A61P17/00 , A61P17/02 , A61P17/06 , A61P19/02 , A61P27/14 , A61P29/00 , A61P35/00 , A61P37/08 , A61P43/00 , C07D20060101 , C07D209/00 , C07D221/00 , C07D241/00 , C07D471/04 , C07D487/04 , C07D519/00 , C07D487/02 , A61K31/4745 , A61K31/498 , C07D471/02
CPC分类号： C07D519/00 , C07D471/04 , C07D487/04
摘要： The invention is directed to physiologically active compounds of general formula (I):— and compositions containing such compounds; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (I). Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases.
摘要翻译：本发明涉及通式（I）的生理活性化合物： - 和含有这些化合物的组合物; 及其前药，以及这些化合物及其前药的药学上可接受的盐和溶剂合物，以及式（I）范围内的新化合物。这些化合物和组合物具有有价值的药物特性，特别是抑制激酶的能力。

4. 发明授权

US06770643B2 Azaindoles 有权
标题翻译：楝树
公开(公告)号：US06770643B2
公开(公告)日：2004-08-03
申请号：US10178667
申请日：2002-06-24
申请人： Paul J Cox , Tahir N. Majid , Justine Y. Q. Lai , Andrew D. Morley , Shelley Amendola , Stephanie D. Deprets , Christopher Edlin
发明人： Paul J Cox , Tahir N. Majid , Justine Y. Q. Lai , Andrew D. Morley , Shelley Amendola , Stephanie D. Deprets , Christopher Edlin
IPC分类号： C07D47104
CPC分类号： A61K31/4985 , A61K31/437 , C07D471/04 , C07D487/04
摘要： The invention is directed to compositions containing physiologically active compounds of general formula (I): wherein R1 is aryl or heteroaryl; R2 represents hydrogen, acyl, cyano, halo, lower alkenyl or lower alkyl optionally substituted by a substituent selected from cyano, heteroaryl, heterocycloalkyl, —Z1R8, —C(═O)—NY3Y4, —CO2R8, —NY3Y4, —N(R6)—C(═O)—R7, —N(R6)—C(═O)—NY3Y4, —N(R6)—C(═O)—OR7, —N(R6)—SO2—R7, —N(R6)—SO2—NY3Y4 and one or more halogen a toms ; R3 represents hydrogen, aryl, cyano, halo, heteroaryl, lower alkyl, —C(═O)—OR5 or —C(═O)—NY3Y; and X1 represents N, CH, C-halo, C—CN, C—R7, C—NY3Y4, C—OH, C—Z2R7, C—C(═O)—OR5, C—C(═O)—NY3Y4, C—N(R8)—C(═O)—R7, C—SO2—NY3Y4, C—N(R8)—SO2—R7, C-alkenyl, C-alkynyl or C—NO2; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (I). Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit protein kinases.
摘要翻译：本发明涉及含有通式（I）的生理活性化合物的组合物：其中R 1是芳基或杂芳基; R 2表示氢，酰基，氰基，卤素，低级烯基或任选被选自氰基，杂芳基，杂环烷基，-Z 1 R 8，-C（= O）-NY 3，Y 4，-CO 2 R 8，-NY 3 Y 4，-N（R 6）-C（= O）-R 7，-N（R 6））-C（= O）-NY 3 Y 4，-N（R 6）-C（= O）-OR 7，-N（R 6）-SO 2 -R 7，-N（R 6）-SO 2 -NY 3 Y 4和一个或多个卤素; R 3表示氢，芳基，氰基，卤素，杂芳基，低级烷基，-C（= O）-OR 5或-C（= O）-NY 3 Y; 并且X 1表示N，CH，C - 卤素，C-CN，CR 7，C-NY 3 Y 4，C-OH，CZ 2 R 7，CC（= O）-OR 5，CC（= O）-NY 3 Y 4，CN（R 8）-C（= O）-R 7，C-SO 2 -YN 3， Y 4，CN（R 8）-SO 2 -R 7，C-烯基，C - 炔基或C-NO 2; 和它们的前药，以及这些化合物及其前药的药学上可接受的盐和溶剂合物，以及式（I）范围内的新化合物。这些化合物和组合物具有有价值的药物性质，特别是抑制蛋白激酶的能力。

5. 发明申请

US20060014756A1 Benzimidazoles 有权
标题翻译：苯并咪唑
公开(公告)号：US20060014756A1
公开(公告)日：2006-01-19
申请号：US11029064
申请日：2005-01-04
申请人： Michael Edwards , Paul Cox , Shelley Amendola , Stephanie Deprets , Timothy Gillespy , Christopher Edlin , Andrew Morley , Charles Gardner , Brian Pedgrift , Herve Bouchard , Didier Babin , Laurence Gauzy , Alain Le-Brun , Tahir Majid , John Reader , Lloyd Payne , Nawaz Khan , Michael Cherry
发明人： Michael Edwards , Paul Cox , Shelley Amendola , Stephanie Deprets , Timothy Gillespy , Christopher Edlin , Andrew Morley , Charles Gardner , Brian Pedgrift , Herve Bouchard , Didier Babin , Laurence Gauzy , Alain Le-Brun , Tahir Majid , John Reader , Lloyd Payne , Nawaz Khan , Michael Cherry
IPC分类号： A61K31/496 , A61K31/4184 , C07D43/02
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D471/04 , C07D487/04 , C07D491/04
摘要： The invention is directed to physiologically active compounds of the general formula (Ix) and compositions containing such compounds, and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (Ix), and to processes for their preparation. Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases.
摘要翻译：本发明涉及通式（Ix）的生理活性化合物和含有这些化合物及其前药以及这些化合物及其前药的药学上可接受的盐和溶剂合物的组合物，以及式（Ix）范围内的新化合物 Ix），以及它们的制备过程。这些化合物和组合物具有有价值的药物特性，特别是抑制激酶的能力。

6. 发明授权

US07259154B2 Pyrrolopyrimidines 失效
标题翻译：吡咯并嘧啶
公开(公告)号：US07259154B2
公开(公告)日：2007-08-21
申请号：US10744478
申请日：2003-12-23
申请人： Paul Joseph Cox , Tahir Nadeem Majid , Stephanie Daniele Deprets , Shelley Amendola , Iain McFarlane McLay , Christopher Edlin , David John Aldous , Brian Pedgrift , Frank Halley , Michael Edwards , Bernard Baudoin
发明人： Paul Joseph Cox , Tahir Nadeem Majid , Stephanie Daniele Deprets , Shelley Amendola , Iain McFarlane McLay , Christopher Edlin , David John Aldous , Brian Pedgrift , Frank Halley , Michael Edwards , Bernard Baudoin
IPC分类号： C07D413/04 , C07D487/04 , A61P11/06 , A61K31/5355 , A61K31/519 , A61K31/66 , C07F9/38
CPC分类号： C07D487/04
摘要： Compounds of the formula and N-oxides, prodrugs, acid bioisosteres, pharmaceutically acceptable salts or solvates of such compounds, or N-oxides, prodrugs, or acid bioisosteres of such salts or solvates, to compositions comprising such compounds, and methods of treatment comprising administering, to a patient in need thereof, such compounds and compositions.
摘要翻译：这些化合物的式和N-氧化物，前体药物，酸性生物电子等排物，这些化合物的药学上可接受的盐或溶剂化物，或这些盐或溶剂化物的N-氧化物，前体药物或酸性生物电子等离子体对包含这些化合物的组合物，以及包括向有需要的患者施用此类化合物和组合物。

7. 发明申请

US20070280971A1 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：US20070280971A1
公开(公告)日：2007-12-06
申请号：US10598838
申请日：2005-03-15
申请人： Siegfried Christensen , Caroline Cook , Christopher Edlin , Martin Johnson , Paul Jones , Mika Lindvall , Amyn Sayani , Naimisha Trivedi , Lionel Trottet
发明人： Siegfried Christensen , Caroline Cook , Christopher Edlin , Martin Johnson , Paul Jones , Mika Lindvall , Amyn Sayani , Naimisha Trivedi , Lionel Trottet
IPC分类号： A61K31/437 , A61K9/06 , A61K9/107 , A61P17/00 , A61P29/00 , A61P37/00 , C07D471/04
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。

8. 发明申请

US20070167485A1 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，它们用作pde4抑制剂
公开(公告)号：US20070167485A1
公开(公告)日：2007-07-19
申请号：US10598944
申请日：2005-03-15
申请人： Diane Coe , Caroline Cook , Anthony Cooper , Christopher Edlin , Julie Hamblin , Martin Johnson , Paul Jones , Mika Lindvall , Charlotte Mitchell , Alison Redgrave , John Robinson
发明人： Diane Coe , Caroline Cook , Anthony Cooper , Christopher Edlin , Julie Hamblin , Martin Johnson , Paul Jones , Mika Lindvall , Charlotte Mitchell , Alison Redgrave , John Robinson
IPC分类号： 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 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是Et，n-Pr，i-Pr，C 2氟代烷基，或 -CH 2 CH 2 CH 2 OH; R 2是H，Me，Et，n-Pr，i-Pr，C 1-12氟代烷基，环丙基或（环丙基）甲基; 和NHR 3具有子式（nhr3）：其中R 3a是甲基或乙基; R 3b是H，甲基或乙基; R 3c是H，甲基或乙基，R 3d是H，甲基或乙基，R 3e是H或甲基，条件是：（a）R 3b是甲基或乙基; 和/或（b）R 3c和R 3d独立地是甲基或乙基; 并且条件是：（c）当R 3c为乙基时，和/或当R 3d为乙基时，和/或当R 3e为甲基时，那么：R 3a是甲基，和/或R 3b是氢或甲基。这些化合物是PDE4抑制剂。

9. 发明申请

US20070191426A1 Derivatives of 3-aminocarbonylquinoline, pharmaceutical compositions containing them and processes and intermediates for their preparation 审中-公开
标题翻译： 3-氨基羰基喹啉的衍生物，含有它们的药物组合物及其制备方法和中间体
公开(公告)号：US20070191426A1
公开(公告)日：2007-08-16
申请号：US10572913
申请日：2004-09-27
申请人： Christopher Edlin , Colin Eldred , Christopher Lunniss , Alison Redgrave , John Robinson , Michael Woodrow
发明人： Christopher Edlin , Colin Eldred , Christopher Lunniss , Alison Redgrave , John Robinson , Michael Woodrow
IPC分类号： A61K31/47
CPC分类号： C04B35/632 , C07D215/44 , C07D401/12 , C07D405/12 , C07D411/12 , C07D417/12
摘要： Compounds of formula (I) or pharmaceutically acceptable salts thereof are inhibitors of phosphodiesterase type IV (PDE4) and are of use in the treatment of inflammatory and/or allergic diseases.
摘要翻译：式（I）化合物或其药学上可接受的盐是IV型磷酸二酯酶（PDE4）的抑制剂，并且可用于治疗炎性和/或过敏性疾病。

10. 发明申请

US20080058369A1 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：US20080058369A1
公开(公告)日：2008-03-06
申请号：US11831325
申请日：2007-07-31
申请人： David Allen , Rodger Barnett , Reshma Chudasama , Caroline Day , Christopher Edlin , Leanda Kindon
发明人： David Allen , Rodger Barnett , Reshma Chudasama , Caroline Day , Christopher Edlin , Leanda Kindon
IPC分类号： A61K31/437 , A61P29/00 , A61P37/08 , 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）苯甲酰胺或其盐，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）。

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