公开(公告)号：WO2012007868A3

公开(公告)日：2012-01-19

申请号：PCT/IB2011/052940

申请日：2011-07-04

Applicant: PFIZER LIMITED ,  BROWN, Alan, Daniel ,  RAWSON, David, James ,  STORER, Robert, Ian ,  SWAIN, Nigel, Alan

Inventor： BROWN, Alan, Daniel ,  RAWSON, David, James ,  STORER, Robert, Ian ,  SWAIN, Nigel, Alan

IPC: C07C311/51 ,  A61K31/18 ,  A61P25/04

Abstract: The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula (I): or a pharmaceutically acceptable salt thereof, wherein X, Ar 1 , R 1 , R 2 , R 3 , R 4 and R 5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.

公开(公告)号：WO2012004714A2

公开(公告)日：2012-01-12

申请号：PCT/IB2011/052920

申请日：2011-07-01

Applicant: PFIZER LIMITED ,  ICAGEN, INC. ,  GREENER, Benjamin Scott ,  MARRON, Brian Edward ,  MILLAN, David Simon ,  RAWSON, David James ,  STORER, Robert Ian ,  SWAIN, Nigel Alan

Inventor： GREENER, Benjamin Scott ,  MARRON, Brian Edward ,  MILLAN, David Simon ,  RAWSON, David James ,  STORER, Robert Ian ,  SWAIN, Nigel Alan

IPC: C07D285/08 ,  C07D285/135 ,  C07D401/12 ,  C07D417/12 ,  A61K31/433 ,  A61K31/4427 ,  A61K31/501 ,  A61P25/04

CPC classification number: C07D285/135 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/501 ,  A61K45/06 ,  C07D285/08 ,  C07D401/12 ,  C07D417/12

Abstract: The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to new sulfonamide Nav1.7 inhibitors of formula (I) or pharmaceutically acceptable salts thereof, wherein X, Y 1 , Y 2 , Z, R 1 , R 2 and R 3 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.

Abstract translation: 本发明涉及磺酰胺衍生物，其在药物中的用途，含有它们的组合物，其制备方法和用于此类方法的中间体。 更具体地说，本发明涉及式（I）的新的磺酰胺Nav1.7抑制剂或其药学上可接受的盐，其中X，Y 1，Y 2，Z，R 1，R 2和R 3如说明书中所定义。 Nav 1.7抑制剂可用于治疗各种疾病，特别是疼痛。

公开(公告)号：WO2008142550A8

公开(公告)日：2009-12-23

申请号：PCT/IB2008001295

申请日：2008-05-16

Applicant: PFIZER LTD ,  RAWSON DAVID JAMES ,  SWAIN NIGEL ALAN ,  WATSON LESA

Inventor： RAWSON DAVID JAMES ,  SWAIN NIGEL ALAN ,  WATSON LESA

IPC: C07D239/70 ,  A61K31/527 ,  A61P29/00 ,  C07D403/10 ,  C07D403/12 ,  C07D413/12

CPC classification number: C07D239/70 ,  C07D403/10 ,  C07D403/12 ,  C07D413/12

Abstract: This invention relates to spirocyclic derivatives, compositions containing and the uses of, such derivatives. The spirocyclic derivatives of the present invention are PDE7 inhibitors and have a number of therapeutic applications, particularly in the treatment of pain, especially neuropathic pain. The invention provides a compound of formula (I): wherein: X is O. S or N-CN; R1 is halogen or CN; A is a single bond, CH2, 0 or S; B is a single bond, CH2 or OCH2; each R2 is independently halogen, (C1-6)alkyl (optionally substituted by 1 to 3 fluorine atoms), OH, (C1-6)aIkOXy, (C1-6)alkytthio or CN; R3 is selected from the following groups (i) to (x).

Abstract translation: 本发明涉及螺环衍生物，含有这些衍生物的组合物和用途。 本发明的螺环衍生物是PDE7抑制剂，并且具有许多治疗应用，特别是治疗疼痛，特别是神经性疼痛。 本发明提供式（I）化合物：其中：X为O.S或N-CN; R1是卤素或CN; A是单键，CH2，O或S; B是单键，CH2或OCH2; 每个R 2独立地为卤素，（C 1-6）烷基（任选被1至3个氟原子取代），OH，（C 1-6）烷氧基，（C 1-6）烷硫基或CN; R3选自以下组（i）至（x）。

公开(公告)号：WO2007063391A2

公开(公告)日：2007-06-07

申请号：PCT/IB2006003388

申请日：2006-11-23

Applicant: PFIZER LTD ,  RAWSON DAVID JAMES ,  SWAIN NIGEL ALAN

Inventor： RAWSON DAVID JAMES ,  SWAIN NIGEL ALAN

IPC: C07D239/80 ,  A61K31/522 ,  A61P25/00 ,  A61P25/02

CPC classification number: A61K31/522 ,  C07D239/80

Abstract: The invention provides compounds of formula (I): (I) wherein: m is 0, 1 or 2; X is O, S or N-CN; R is F, Cl or CN; A is a C 3-6 cycloalkylene group optionally substituted with a C 1-4 alkyl group; and B is a single bond or a C 1-2 alkylene group; or a pharmaceutically acceptable salt, solvate, polymorph or prodrug thereof. The compounds are PDE7 inhibitors and have a number of therapeutic applications, particularly in the treatment of pain, especially neuropathic pain.

Abstract translation: 本发明提供式（I）化合物：（I）其中：m为0,1或2; X是O，S或N-CN; R是F，Cl或CN; A是任选被C 1-4烷基取代的C 3-6亚烷基; 和B是单键或C 1-12亚烷基; 或其药学上可接受的盐，溶剂合物，多晶型物或前药。 这些化合物是PDE7抑制剂，并且具有许多治疗应用，特别是治疗疼痛，特别是神经性疼痛。

公开(公告)号：WO2006120544A1

公开(公告)日：2006-11-16

申请号：PCT/IB2006/001209

申请日：2006-04-24

Applicant: PFIZER LIMITED ,  CRAWFORD, Terry, Dale ,  RAWSON, David, James ,  THORPE, Andrew, John

Inventor： CRAWFORD, Terry, Dale ,  RAWSON, David, James ,  THORPE, Andrew, John

IPC: C07C229/34 ,  A61K31/195 ,  A61P29/02

CPC classification number: C07C323/63 ,  C07B2200/07 ,  C07C229/34 ,  C07D317/60

Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 , R 2 , R 3 , R 8 and R 9 are as defined herein, as well as to compositions containing such a compound and the uses of such a compound. Compounds of formula (I) are especially useful in the treatment of pain.

Abstract translation: 本发明涉及式（I）化合物或其药学上可接受的盐或溶剂合物，其中R 1，R 2，R 3， >，R 8和R 9如本文所定义，以及含有这种化合物的组合物和这种化合物的用途。 式（I）的化合物特别可用于治疗疼痛。

公开(公告)号：WO2006011050A3

公开(公告)日：2006-10-05

申请号：PCT/IB2005002214

申请日：2005-07-12

Applicant: PFIZER LTD ,  PFIZER ,  LANE CHARLOTTE ALICE LOUISE ,  MAW GRAHAM NIGEL ,  RAWSON DAVID JAMES ,  THOMPSON LISA ROSEMARY

Inventor： LANE CHARLOTTE ALICE LOUISE ,  MAW GRAHAM NIGEL ,  RAWSON DAVID JAMES ,  THOMPSON LISA ROSEMARY

IPC: C07D213/81 ,  A61K31/44 ,  A61K31/4439 ,  A61P29/00 ,  C07D401/12

CPC classification number: C07D213/81 ,  C07D401/12

Abstract: The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts and solvates thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds for the treatment of pain.

Abstract translation: 本发明涉及式（I）化合物及其药学上可接受的盐和溶剂合物，制备用于制备中间体的方法和含有这些化合物的组合物以及这些化合物用于治疗疼痛的用途 。

公开(公告)号：WO1994027990A1

公开(公告)日：1994-12-08

申请号：PCT/EP1994001760

申请日：1994-05-26

Applicant: PFIZER LIMITED ,  PFIZER INC. ,  PFIZER RESEARCH AND DEVELOPMENT COMPANY, N.V./S.A. ,  MAW, Graham, Nigel ,  BLAGG, Julian ,  RAWSON, David, James

Inventor： PFIZER LIMITED ,  PFIZER INC. ,  PFIZER RESEARCH AND DEVELOPMENT COMPANY, N.V./S.A.

IPC: C07D405/06

CPC classification number: C07D405/06

Abstract: The present invention provides compounds of formula (I) and the pharmaceutically acceptable base salts thereof, wherein R is -CO2H or tetrazol-5-yl; R is C3-C8alkyl optionally substituted by fluoro; and R is C2-C4alkyl, together with compositions containing, uses of, processes for the preparation of and intermediates used in the preparation of, such compounds. The compounds have steroid 5 alpha -reductase inhibitory activity and are useful for treating a disease such as benign prostatic hypertrophy.

Abstract translation: 本发明提供式（I）化合物及其药学上可接受的碱盐，其中R是-CO 2 H或四唑-5-基; R 1是任选被氟取代的C 3 -C 8烷基; 和R 2是C 2 -C 4烷基，以及含有用于制备所用化合物的制备方法和中间体的组合物。 该化合物具有类固醇5α-还原酶抑制活性，可用于治疗良性前列腺肥大等疾病。

公开(公告)号：WO2012007883A1

公开(公告)日：2012-01-19

申请号：PCT/IB2011/053030

申请日：2011-07-07

Applicant: PFIZER LIMITED ,  BELL, Andrew, Simon ,  BROWN, Alan, Daniel ,  DE GROOT, Marcel, John ,  LEWTHWAITE, Russell, Andrew ,  MARSH, Ian, Roger ,  MILLAN, David, Simon ,  PEREZ PACHECO, Manuel ,  RAWSON, David, James ,  SCIAMMETTA, Nunzio ,  STORER, Robert, Ian ,  STUPPLE, Paul, Anthony ,  SWAIN, Nigel, Alan

Inventor： BELL, Andrew, Simon ,  BROWN, Alan, Daniel ,  DE GROOT, Marcel, John ,  LEWTHWAITE, Russell, Andrew ,  MARSH, Ian, Roger ,  MILLAN, David, Simon ,  PEREZ PACHECO, Manuel ,  RAWSON, David, James ,  SCIAMMETTA, Nunzio ,  STORER, Robert, Ian ,  STUPPLE, Paul, Anthony ,  SWAIN, Nigel, Alan

IPC: C07C311/00 ,  A61P29/00

CPC classification number: C07C311/51 ,  C07C2601/02 ,  C07D231/12 ,  C07D233/60 ,  C07D237/08

Abstract: The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula (I):or a pharmaceutically acceptable salt thereof, wherein Ar 1 , X, R 1 , R 2 , R 3 , R 4 and R 5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.

Abstract translation: 本发明涉及磺酰胺衍生物，其在医学上的用途，含有它们的组合物，其制备方法以及在这些方法中使用的中间体。 更具体地，本发明涉及式（I）的新的磺酰胺Nav1.7抑制剂：或其药学上可接受的盐，其中Ar1，X，R1，R2，R3，R4和R5如说明书中所定义。 Nav 1.7抑制剂可用于治疗各种疾病，特别是疼痛。

公开(公告)号：WO2012007868A2

公开(公告)日：2012-01-19

申请号：PCT/IB2011052940

申请日：2011-07-04

Applicant: PFIZER LTD ,  BROWN ALAN DANIEL ,  RAWSON DAVID JAMES ,  STORER ROBERT IAN ,  SWAIN NIGEL ALAN

Inventor： BROWN ALAN DANIEL ,  RAWSON DAVID JAMES ,  STORER ROBERT IAN ,  SWAIN NIGEL ALAN

IPC: C07C311/51

CPC classification number: C07C311/04 ,  A61K31/18 ,  A61K31/277 ,  A61K31/415 ,  A61K31/4245 ,  A61K31/451 ,  A61K31/495 ,  A61K31/50 ,  A61K45/06 ,  C07C311/51 ,  C07D211/22 ,  C07D231/12 ,  C07D237/08 ,  C07D241/04 ,  C07D271/06

Abstract: The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula (I): or a pharmaceutically acceptable salt thereof, wherein X, Ar1, R1, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.

Abstract translation: 本发明涉及磺酰胺衍生物，其在医学上的用途，含有它们的组合物，其制备方法以及在这些方法中使用的中间体。 更具体地，本发明涉及式（I）的新的磺酰胺Nav1.7抑制剂：或其药学上可接受的盐，其中X，Ar1，R1，R2，R3，R4和R5如说明书中所定义。 Nav 1.7抑制剂可用于治疗各种疾病，特别是疼痛。

公开(公告)号：WO2012007861A1

公开(公告)日：2012-01-19

申请号：PCT/IB2011/052797

申请日：2011-06-24

Applicant: PFIZER LIMITED ,  BELL, Andrew, Simon ,  BROWN, Alan, Daniel ,  DE GROOT, Marcel, John ,  GAULIER, Steven, Matthieu ,  LEWTHWAITE, Russell, Andrew ,  MARSH, Ian, Roger ,  MILLAN, David, Simon ,  PEREZ PACHECO, Manuel ,  RAWSON, David, James ,  SCIAMMETTA, Nunzio ,  STORER, Robert, Ian ,  SWAIN, Nigel, Alan

Inventor： BELL, Andrew, Simon ,  BROWN, Alan, Daniel ,  DE GROOT, Marcel, John ,  GAULIER, Steven, Matthieu ,  LEWTHWAITE, Russell, Andrew ,  MARSH, Ian, Roger ,  MILLAN, David, Simon ,  PEREZ PACHECO, Manuel ,  RAWSON, David, James ,  SCIAMMETTA, Nunzio ,  STORER, Robert, Ian ,  SWAIN, Nigel, Alan

IPC: C07D213/63 ,  C07D213/64 ,  C07D213/65 ,  C07D213/69 ,  C07D213/70 ,  C07D213/74 ,  C07D213/85 ,  C07D215/20 ,  C07D231/56 ,  C07D239/47 ,  C07D401/04 ,  C07D405/12 ,  C07D487/04 ,  C07B59/00 ,  A61K31/44

CPC classification number: C07D213/69 ,  C07D213/63 ,  C07D213/64 ,  C07D213/65 ,  C07D213/70 ,  C07D213/74 ,  C07D213/85 ,  C07D215/20 ,  C07D231/56 ,  C07D239/47 ,  C07D401/04 ,  C07D405/12 ,  C07D487/04

Abstract: The invention relates to sulfonamide derivatives, to their use i n medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula (I): or a pharmaceutically acceptable salt thereof, wherein Het 1 , X, R 1 , R 2 , R 3 , R 4 and R 5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.

Abstract translation: 本发明涉及磺酰胺衍生物，其药物用途，含有它们的组合物，其制备方法和用于此类方法的中间体。 更具体地，本发明涉及式（I）的新的磺酰胺Nav1.7抑制剂：或其药学上可接受的盐，其中Het1，X，R1，R2，R3，R4和R5如说明书中所定义。 Nav 1.7抑制剂可用于治疗各种疾病，特别是疼痛。