公开(公告)号：EP1651608A1

公开(公告)日：2006-05-03

申请号：EP04744013.6

申请日：2004-07-13

申请人： Pfizer Limited ,  PFIZER INC.

发明人： MATHIAS, John Paul

IPC分类号： C07D213/82 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12 ,  A61K31/455 ,  A61P37/00

CPC分类号： C07D213/82 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12

摘要： This invention relates to nicotinamide derivatives of general formuala (I) in which R1, R2, and R3 have the meanings defined herein, and to compositions containing and the uses of such derivatives as PDE4 inhibitors.

公开(公告)号：EP1778686B1

公开(公告)日：2008-10-29

申请号：EP05772546.7

申请日：2005-08-09

申请人： Pfizer Limited ,  Pfizer, Inc.

发明人： MATHIAS, John Paul ,  MILLAN, David Simon ,  LEWTHWAITE, Russell Andrew ,  PHILLIPS, Christopher

IPC分类号： C07D471/04 ,  C07C321/28 ,  A61P29/00 ,  A61K31/437 ,  A61K31/4745

CPC分类号： C07D471/04

摘要： A compound of formula (I), or a pharmaceutically acceptable salt and/or solvate (including hydrate) thereof; Forumla (I) and the use of a compound of formula (I) in the treatment of a TNF-mediated disease, disorder, or condition, or a p38-mediated disease, disorder, or condition, in particular the allergic and non-allergic airways diseases, more particularly obstructive or inflammatory airways diseases, preferably chronic obstructive pulmonary disease.

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：EP1778686B9

公开(公告)日：2009-08-12

申请号：EP05772546.7

申请日：2005-08-09

申请人： Pfizer Limited ,  Pfizer, Inc.

发明人： MATHIAS, John Paul ,  MILLAN, David Simon ,  LEWTHWAITE, Russell Andrew ,  PHILLIPS, Christopher

IPC分类号： C07D471/04 ,  C07C321/28 ,  A61P29/00 ,  A61K31/437 ,  A61K31/4745

CPC分类号： C07D471/04

公开(公告)号：EP1651647A1

公开(公告)日：2006-05-03

申请号：EP04744024.3

申请日：2004-07-13

申请人： Pfizer Limited ,  PFIZER INC.

发明人： MATHIAS, John Paul

IPC分类号： C07D471/04 ,  C07D401/12 ,  A61K31/455 ,  A61P37/00

CPC分类号： A61K31/455 ,  C07D401/12 ,  C07D471/04

摘要： This invention relates to nicotinamide derivatives of general formula (I) in which R1, R2, and R3 have the meanings defined herein, and to compositions containing and the uses of such derivatives as PDE4 inhibitors.

摘要翻译： 本发明涉及通式（I）的烟酰胺衍生物，其中R 1，R 2和R 3具有本文定义的含义，并且涉及含有这些衍生物和PDE 4抑制剂的用途的组合物。

公开(公告)号：EP1778686A2

公开(公告)日：2007-05-02

申请号：EP05772546.7

申请日：2005-08-09

申请人： Pfizer Limited ,  Pfizer, Inc.

发明人： MATHIAS, John Paul ,  MILLAN, David Simon ,  LEWTHWAITE, Russell Andrew ,  PHILLIPS, Christopher

IPC分类号： C07D471/04 ,  C07C321/28 ,  A61P29/00 ,  A61K31/437 ,  A61K31/4745

CPC分类号： C07D471/04

摘要： A compound of formula (I), or a pharmaceutically acceptable salt and/or solvate (including hydrate) thereof; Forumla (I) and the use of a compound of formula (I) in the treatment of a TNF-mediated disease, disorder, or condition, or a p38-mediated disease, disorder, or condition, in particular the allergic and non-allergic airways diseases, more particularly obstructive or inflammatory airways diseases, preferably chronic obstructive pulmonary disease.

摘要翻译： 式（I）化合物或其药学上可接受的盐和/或溶剂化物（包括其水合物）; （I）化合物和式（I）化合物在治疗TNF介导的疾病，病症或病症或p38介导的疾病，病症或病症中的用途，特别是过敏性和非变应性 气道疾病，更特别是阻塞性或炎性气道疾病，优选慢性阻塞性肺病。

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。

公开(公告)号：EP1651640A1

公开(公告)日：2006-05-03

申请号：EP04744026.8

申请日：2004-07-13

申请人： Pfizer Limited ,  Barber, Christopher Gordon

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：EP3303303A1

公开(公告)日：2018-04-11

申请号：EP16724127.2

申请日：2016-05-16

申请人： Pfizer Inc.

发明人： CASIMIRO-GARCIA, Agustin ,  CONDON, Jeffrey Scott ,  FLICK, Andrew Christopher ,  GOPALSAMY, Ariamala ,  KIRINCICH, Steven J. ,  MATHIAS, John Paul ,  STROHBACH, Joseph Walter ,  XIANG, Jason Shaoyun ,  XING, Li Huang ,  WANG, Xiaolun

IPC分类号： C07D239/28 ,  C07D241/14 ,  A61K31/505 ,  A61P29/00

CPC分类号： C07D239/42 ,  A61K31/505 ,  A61P1/00 ,  A61P1/04 ,  A61P35/00 ,  C07D239/28 ,  C07D241/14 ,  C07D401/12 ,  C07D403/12 ,  C07D405/10

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