公开(公告)号：EP3126330A1

公开(公告)日：2017-02-08

申请号：EP15717250.3

申请日：2015-03-26

申请人： Pfizer Inc.

发明人： ANDERSON, David Randolph ,  BUNNAGE, Mark Edward ,  CURRAN, Kevin Joseph ,  DEHNHARDT, Christoph Martin ,  GAVRIN, Lori Krim ,  GOLDBERG, Joel Adam ,  HAN, Seungil ,  HEPWORTH, David ,  HUANG, Horng-Chih ,  LEE, Arthur ,  LEE, Katherine Lin ,  LOVERING, Frank Eldridge ,  LOWE, Michael Dennis ,  MATHIAS, John Paul ,  PAPAIOANNOU, Nikolaos ,  PATNY, Akshay ,  PIERCE, Betsy Susan ,  SAIAH, Eddine ,  STROHBACH, Joseph Walter ,  TRZUPEK, John David ,  VARGAS, Richard ,  WANG, Xiaolun ,  WRIGHT, Stephen Wayne ,  ZAPF, Christoph Wolfgang

IPC分类号： C07D207/26 ,  C07D207/273 ,  C07D209/52 ,  C07D215/48 ,  C07D217/02 ,  C07D217/22 ,  C07D217/24 ,  C07D239/86 ,  C07D239/88 ,  C07D263/24 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12

CPC分类号： C07D491/056 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06 ,  C07C69/94 ,  C07D207/08 ,  C07D207/26 ,  C07D207/267 ,  C07D207/273 ,  C07D209/52 ,  C07D215/48 ,  C07D217/02 ,  C07D217/22 ,  C07D217/24 ,  C07D239/86 ,  C07D239/88 ,  C07D263/24 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D407/14 ,  C07D413/12 ,  C07D417/12 ,  C07D487/04 ,  C07D498/04 ,  C07F7/1804

摘要： Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

摘要翻译： 公开了化合物的化合物，互变异构体和药学上可接受的盐，其中化合物具有如说明书中定义的式Ia结构。 还公开了相应的药物组合物，治疗方法，合成方法和中间体。

公开(公告)号：EP1624868B9

公开(公告)日：2009-08-12

申请号：EP04730338.3

申请日：2004-04-29

申请人： Pfizer Limited ,  Pfizer Inc.

发明人： BUNNAGE, Mark Edward ,  GLOSSOP, Paul, Alan ,  LANE, Charlotte Alice Louise ,  LEWTHWAITE, Russell Andrew

IPC分类号： A61K31/4402 ,  C07C237/20 ,  C07D213/40 ,  C07C311/16 ,  A61K31/164 ,  C07D217/02 ,  C07D209/44 ,  A61K31/4035 ,  A61K31/472

CPC分类号： C07C237/20 ,  C07C237/22 ,  C07C311/46 ,  C07C2602/08 ,  C07D209/44 ,  C07D213/40 ,  C07D217/06

摘要： The invention relates to compounds of formula (1), and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.

公开(公告)号：EP1624868B1

公开(公告)日：2008-11-12

申请号：EP04730338.3

申请日：2004-04-29

申请人： Pfizer Limited ,  Pfizer Inc.

发明人： BUNNAGE, Mark Edward ,  GLOSSOP, Paul, Alan ,  LANE, Charlotte Alice Louise ,  LEWTHWAITE, Russell Andrew

IPC分类号： A61K31/4402 ,  C07C237/20 ,  C07D213/40 ,  C07C311/16 ,  A61K31/164 ,  C07D217/02 ,  C07D209/44 ,  A61K31/4035 ,  A61K31/472

CPC分类号： C07C237/20 ,  C07C237/22 ,  C07C311/46 ,  C07C2602/08 ,  C07D209/44 ,  C07D213/40 ,  C07D217/06

摘要： The invention relates to compounds of formula (1), and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.

公开(公告)号：EP1651640B1

公开(公告)日：2007-02-14

申请号：EP04744026.8

申请日：2004-07-13

申请人： Pfizer Limited ,  PFIZER INC.

发明人： BARBER, Christopher Gordon ,  BUNNAGE, Mark Edward ,  HARVEY, John Wilson ,  MATHIAS, John Paul

IPC分类号： C07D409/12 ,  A61P11/00 ,  A61P37/00 ,  A61K31/4436 ,  C07D409/14 ,  C07D471/04 ,  C07D417/14 ,  C07D413/14

CPC分类号： A61K31/4436 ,  A61K9/2018 ,  A61K9/2866 ,  A61K31/4523 ,  A61K31/454 ,  A61K31/519 ,  C07D213/82 ,  C07D409/12 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04 ,  Y02A50/411

摘要： This invention relates to nicotinamide derivatives of general formula (I): in which R1, Z and R2 have the meanings defined herein, and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of such derivatives.

公开(公告)号：EP3126330B1

公开(公告)日：2019-02-27

申请号：EP15717250.3

申请日：2015-03-26

申请人： Pfizer Inc.

发明人： ANDERSON, David Randolph ,  BUNNAGE, Mark Edward ,  CURRAN, Kevin Joseph ,  DEHNHARDT, Christoph Martin ,  GAVRIN, Lori Krim ,  GOLDBERG, Joel Adam ,  HAN, Seungil ,  HEPWORTH, David ,  HUANG, Horng-Chih ,  LEE, Arthur ,  LEE, Katherine Lin ,  LOVERING, Frank Eldridge ,  LOWE, Michael Dennis ,  MATHIAS, John Paul ,  PAPAIOANNOU, Nikolaos ,  PATNY, Akshay ,  PIERCE, Betsy Susan ,  SAIAH, Eddine ,  STROHBACH, Joseph Walter ,  TRZUPEK, John David ,  VARGAS, Richard ,  WANG, Xiaolun ,  WRIGHT, Stephen Wayne ,  ZAPF, Christoph Wolfgang

IPC分类号： C07D207/26 ,  C07D207/273 ,  C07D209/52 ,  C07D215/48 ,  C07D217/02 ,  C07D217/22 ,  C07D217/24 ,  C07D239/86 ,  C07D239/88 ,  C07D263/24 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12

公开(公告)号：EP1624868A1

公开(公告)日：2006-02-15

申请号：EP04730338.3

申请日：2004-04-29

申请人： Pfizer Limited ,  PFIZER INC.

发明人： BUNNAGE, Mark Edward ,  GLOSSOP, Paul, Alan ,  LANE, Charlotte Alice Louise ,  LEWTHWAITE, Russell Andrew

IPC分类号： A61K31/4402 ,  C07C237/20 ,  C07D213/40 ,  C07C311/16 ,  A61K31/164 ,  C07D217/02 ,  C07D209/44 ,  A61K31/4035 ,  A61K31/472

CPC分类号： C07C237/20 ,  C07C237/22 ,  C07C311/46 ,  C07C2602/08 ,  C07D209/44 ,  C07D213/40 ,  C07D217/06

摘要： The invention relates to compounds of formula (1), and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.

摘要翻译： 本发明涉及式（1）的化合物＆lt; CHEM＆gt;以及制备用于制备含有这些衍生物的组合物和用途的中间体的方法。 根据本发明的化合物可用于许多疾病，病症和病症，特别是炎性，过敏和呼吸道疾病，病症和病症。

公开(公告)号：EP1467732A1

公开(公告)日：2004-10-20

申请号：EP03700057.7

申请日：2003-01-13

申请人： Pfizer Limited ,  PFIZER INC.

发明人： ALLERTON, Charlotte Moira Norfor ,  BUNNAGE, Mark Edward ,  STEELE, John,UK Patent Department,Pfizer Limited

IPC分类号： A61K31/4178 ,  A61P7/02 ,  C07D403/06 ,  C07D401/06

CPC分类号： C07D401/06 ,  C07D403/06

摘要： Compounds according to formula (I) wherein n is 1-4, R1 is optionally substituted C1-6alkyl, C2-6alkenyl, or C2-6alkynyl, Heterocycle, Aromatic heterocycle, Aryl or hydrogen and R2, R3, R4, R5, R6, R7 and R8 are each independently selected from hydrogen and optionally substituted C1-6 alkyl are novel. They are useful in the treatment of thrombotic conditions and other pathologies associated with fibrin deposition. (1).

公开(公告)号：EP3536685A1

公开(公告)日：2019-09-11

申请号：EP19157789.9

申请日：2015-03-26

申请人： Pfizer Inc.

发明人： ANDERSON, David Randolph ,  BUNNAGE, Mark Edward ,  CURRAN, Kevin Joseph ,  DEHNHARDT, Christoph Martin ,  GAVRIN, Lori Krim ,  GOLDBERG, Joel Adam ,  HAN, Seungil ,  HEPWORTH, David ,  HUANG, Horng-Chih ,  LEE, Arthur ,  LEE, Katherine Lin ,  LOVERING, Frank Eldridge ,  LOWE, Michael Dennis ,  MATHIAS, John Paul ,  PAPAIOANNOU, Nikolaos ,  PATNY, Akshay ,  PIERCE, Betsy Susan ,  SAIAH, Eddine ,  STROHBACH, Joseph Walter ,  TRZUPEK, John David ,  VARGAS, Richard ,  WANG, Xiaolun ,  WRIGHT, Stephen Wayne ,  ZAPF, Christoph Wolfgang

IPC分类号： C07D207/26

摘要： Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia ,

as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment of autoimmune and inflammatory diseases associated with Interleukin-1 Receptor Associated Kinase (IRAK), methods of synthesis, and intermediates are also disclosed.

公开(公告)号：EP1220856B1

公开(公告)日：2004-12-08

申请号：EP00966347.7

申请日：2000-10-11

申请人： Pfizer Limited ,  Pfizer Inc.

发明人： BUNNAGE, Mark Edward ,  DEVRIES, Keith Michael ,  HARRIS, Laurence James ,  LEVETT, Philip Charles ,  MATHIAS, John Paul ,  NEGRI, Joanna Teresa ,  STREET, Stephen Derek Albert ,  WOOD, Albert Shaw

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P15/10 ,  C07D401/12 ,  C07D231/38 ,  C07D213/80

CPC分类号： C07D213/80 ,  A61K31/519 ,  C07D231/38 ,  C07D401/12 ,  C07D487/04

摘要： Compounds of formula (I) wherein R?1, R2, R4 and R13¿ are as defined or a pharmaceutically or veterinarily acceptable salt or polymorph thereof, or a pharmaceutically or veterinarily acceptable solvate or pro-drug thereof: are potent and selective inhibitors of type 5 cyclic guanosine 3', 5'-monophosphate phosphodiesterase (cGMP PDE5) and have utility in the treatment of, inter alia, male erectile dysfunction (MED) and female sexual dysfunction (FSD).

公开(公告)号：EP1220856A2

公开(公告)日：2002-07-10

申请号：EP00966347.7

申请日：2000-10-11

申请人： Pfizer Limited ,  Pfizer Inc.

发明人： BUNNAGE, Mark Edward ,  DEVRIES, Keith Michael ,  HARRIS, Laurence James ,  LEVETT, Philip Charles ,  MATHIAS, John Paul ,  NEGRI, Joanna Teresa ,  STREET, Stephen Derek Albert ,  WOOD, Albert Shaw

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P15/10 ,  C07D401/12 ,  C07D231/38 ,  C07D213/80

CPC分类号： C07D213/80 ,  A61K31/519 ,  C07D231/38 ,  C07D401/12 ,  C07D487/04

摘要： Compounds of formula (I) wherein R?1, R2, R4 and R13¿ are as defined or a pharmaceutically or veterinarily acceptable salt or polymorph thereof, or a pharmaceutically or veterinarily acceptable solvate or pro-drug thereof: are potent and selective inhibitors of type 5 cyclic guanosine 3', 5'-monophosphate phosphodiesterase (cGMP PDE5) and have utility in the treatment of, inter alia, male erectile dysfunction (MED) and female sexual dysfunction (FSD).

摘要翻译： 式（I）的化合物：其中R 1，R 2，R 4和R 13均为 定义的或其药学上或兽医学上可接受的盐或其多晶型物，或其药学上或兽医学上可接受的溶剂合物或前体药物：是5型环鸟嘌呤3'，5'-单磷酸磷酸二酯酶（cGMP PDE5）的有效和选择性抑制剂， 在治疗男性勃起功能障碍（MED）和女性性功能障碍（FSD）方面。