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1. 发明申请

WO2015043995A1 PROCESS FOR PREPARING BENZISOTHIAZOLINONES 审中-公开
标题翻译：制备苯并噻唑啉酮的方法
公开(公告)号：WO2015043995A1
公开(公告)日：2015-04-02
申请号：PCT/EP2014/069614
申请日：2014-09-15
申请人： TITAN CHEMICALS LIMITED , MARSH, Ian Roger
发明人： MARSH, Ian Roger
IPC分类号： C07D275/04
CPC分类号： C07D275/04 , C07D277/64
摘要： N-alkylated 1,2-benzisothiazolin-3-ones can be prepared in good yield and good selectivity by reaction of the lithium salt of l,2-benzisothiazolin-3-one with an electrophilic alkylating agent.
摘要翻译： N-烷基化的1,2-苯并异噻唑啉-3-酮可以通过1,2-苯并异噻唑啉-3-酮的锂盐与亲电烷基化剂的反应以良好的产率和良好的选择性制备。

2. 发明申请

WO2014173716A1 PROCESS FOR PREPARING 1,2-BENZISOTHIAZOLIN-3-ONES 审中-公开
标题翻译：制备1,2-苯并噻唑啉-3-酮的方法
公开(公告)号：WO2014173716A1
公开(公告)日：2014-10-30
申请号：PCT/EP2014/057508
申请日：2014-04-14
申请人： TITAN CHEMICALS LIMITED , BERG, Carsten , SINGH, Sangita , MARSH, Ian Roger
发明人： BERG, Carsten , SINGH, Sangita , MARSH, Ian Roger
IPC分类号： C07D275/04
CPC分类号： C07D275/04
摘要： Sodium sulfide hydrate is at least partially dehydrated by heating with N-methyl 2- pyrrolidone. 2-Chlorobenzamide is added to the mixture which is heated further. The mixture is cooled and treated with aqueous hydrogen peroxide to give the sodium salt of 1,2-benzisothiazolin-3-one in good yield. Acidification if desired gives rise to the free 1,2- benzisothiazolin-3-one.
摘要翻译：硫化钠水合物通过用N-甲基2-吡咯烷酮加热至少部分脱水。将2-氯苯甲酰胺加入到进一步加热的混合物中。将混合物冷却并用过氧化氢水溶液处理，得到1,2-苯并异噻唑啉-3-酮的钠盐，产率良好。如果需要，酸化产生游离1,2-苯并异噻唑啉-3-酮。

3. 发明申请

WO2005097799A1 PYRAZOLO`4,3-D! PYRIMIDINES 审中-公开
标题翻译： PYRAZOLO`4,3-D！嘧啶类
公开(公告)号：WO2005097799A1
公开(公告)日：2005-10-20
申请号：PCT/IB2005/000891
申请日：2005-03-30
申请人： PFIZER LIMITED , PFIZER INC. , BELL, Andrew, Simon , BROWN, David, Graham , FOX, David, Nathan, Abraham , LU, Hwang-Fun , MARSH, Ian, Roger , MORRELL, Andrew, Ian , OWEN, Dafydd, Rhys , PALMER, Michael, John , ROGERS, Thomas, Edward , WINDSLOW, Carol, Ann
发明人： BELL, Andrew, Simon , BROWN, David, Graham , FOX, David, Nathan, Abraham , LU, Hwang-Fun , MARSH, Ian, Roger , MORRELL, Andrew, Ian , OWEN, Dafydd, Rhys , PALMER, Michael, John , ROGERS, Thomas, Edward , WINDSLOW, Carol, Ann
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： This invention relates to compounds of formula (I).
摘要翻译：本发明涉及式（I）化合物。

4. 发明申请

WO2012007883A1 SULFONAMIDE DERIVATIVES AS NAV1.7 INHIBITORS FOR THE TREATMENT OF PAIN 审中-公开
标题翻译：作为NAV1.7的磺胺衍生物用于治疗疼痛的抑制剂
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
申请人： 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
发明人： 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分类号： C07C311/00 , A61P29/00
CPC分类号： C07C311/51 , C07C2601/02 , C07D231/12 , C07D233/60 , C07D237/08
摘要： 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.
摘要翻译：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。

5. 发明申请

WO2012007861A1 N-SULFONYLBENZAMIDE DERIVATIVES USEFUL AS VOLTAGE GATED SODIUM CHANNEL INHIBITORS 审中-公开
标题翻译： N-磺酰苯胺衍生物作为电压门式通道抑制剂有用
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
申请人： 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
发明人： 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分类号： 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分类号： 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
摘要： 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.
摘要翻译：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。

6. 发明申请

WO2005049616A8 5,7-DIAMINOPYRAZOLO [4,3-d] PYRIMIDINES WITH PDE-5 INHIBITING ACTIVITY 审中-公开
标题翻译：具有PDE-5抑制活性的5,7-二氨基吡唑[4,3-d]吡嗪
公开(公告)号：WO2005049616A8
公开(公告)日：2006-06-01
申请号：PCT/IB2004003747
申请日：2004-11-12
申请人： PFIZER LTD , PFIZER , BELL ANDREW SIMON , BROWN DAVID GRAHAM , DACK KEVIN NEIL , FOX DAVID NATHAN ABRAHAM , MARSH IAN ROGER , MORRELL ANDREW IAN , PALMER MICHAEL JOHN , WINSLOW CAROL ANN
发明人： BELL ANDREW SIMON , BROWN DAVID GRAHAM , DACK KEVIN NEIL , FOX DAVID NATHAN ABRAHAM , MARSH IAN ROGER , MORRELL ANDREW IAN , PALMER MICHAEL JOHN , WINSLOW CAROL ANN
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , Y02P20/582
摘要： This invention relates to compounds of formula (I).
摘要翻译：本发明涉及式（I）化合物。

7. 发明申请

WO2005097799A8 PYRAZOLO`4,3-D! PYRIMIDINES 审中-公开
标题翻译： PYRAZOLO`4,3-D！嘧啶类
公开(公告)号：WO2005097799A8
公开(公告)日：2006-02-16
申请号：PCT/IB2005000891
申请日：2005-03-30
申请人： PFIZER LTD , PFIZER , BELL ANDREW SIMON , BROWN DAVID GRAHAM , FOX DAVID NATHAN ABRAHAM , LU HWANG-FUN , MARSH IAN ROGER , MORRELL ANDREW IAN , OWEN DAFYDD RHYS , PALMER MICHAEL JOHN , ROGERS THOMAS EDWARD , WINSLOW CAROL ANN
发明人： BELL ANDREW SIMON , BROWN DAVID GRAHAM , FOX DAVID NATHAN ABRAHAM , LU HWANG-FUN , MARSH IAN ROGER , MORRELL ANDREW IAN , OWEN DAFYDD RHYS , PALMER MICHAEL JOHN , ROGERS THOMAS EDWARD , WINSLOW CAROL ANN
IPC分类号： A61K31/519 , C07D487/04 , A61P9/00
CPC分类号： C07D487/04
摘要： This invention relates to compounds of formula (I).
摘要翻译：本发明涉及式（I）化合物。

8. 发明申请

WO2005049616A1 5,7-DIAMINOPYRAZOLO ‘4,3-D!PYRIMIDINES WITH PDE-5 INHIBITING ACTIVITY 审中-公开
标题翻译：具有PDE-5抑制活性的5,7-二氨基吡唑“4,3-D”嘧啶
公开(公告)号：WO2005049616A1
公开(公告)日：2005-06-02
申请号：PCT/IB2004/003747
申请日：2004-11-12
申请人： PFIZER LIMITED , PFIZER INC. , BELL, Andrew, Simon , BROWN, David, Graham , DACK, Kevin, Neil , FOX, David, Nathan, Abraham , MARSH, Ian, Roger , MORRELL, Andrew, Ian , PALMER, Michael, John , WINSLOW, Carol, Ann
发明人： BELL, Andrew, Simon , BROWN, David, Graham , DACK, Kevin, Neil , FOX, David, Nathan, Abraham , MARSH, Ian, Roger , MORRELL, Andrew, Ian , PALMER, Michael, John , WINSLOW, Carol, Ann
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , Y02P20/582
摘要： This invention relates to compounds of formula (I).
摘要翻译：本发明涉及式（I）化合物。

9. 发明申请

WO2006111856A1 PYRAZOLE DERIVATIVES AS PROGESTERONE RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为孕激素受体拮抗剂的吡唑衍生物
公开(公告)号：WO2006111856A1
公开(公告)日：2006-10-26
申请号：PCT/IB2006/001096
申请日：2006-04-10
申请人： PFIZER LIMITED , BRADLEY, Paul, Anthony , DACK, Kevin, Neil , MARSH, Ian, Roger
发明人： BRADLEY, Paul, Anthony , DACK, Kevin, Neil , MARSH, Ian, Roger
IPC分类号： C07D231/18 , C07D403/06 , C07D417/06 , A61K31/415 , A61P15/00
CPC分类号： C07D231/28 , C07D231/18 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D413/06 , C07D417/06
摘要： Compounds of formula (I), or pharmaceutically acceptable derivatives thereof, wherein: R 1 represents H, C 1-6 alkyl, C 1-6 alkyloxy, C 3-8 cycloalkyl, or halo; R 2 represents H, C 1-6 alkyl (optionally substituted by R 3 ), phenyl (optionally substituted by CN), or Het; R 3 represents OH, CN, Het, -R 4 - C 1-6 alkyl, or CONR 5 R 6 ; R 4 represents ―CO 2 -, or ―O-; R 5 and R 6 independently represent H, C 1-6 alkyl (optionally substituted by OR 7 ) or C 3-8 cycloalkyl; R 7 represents H or C 1-6 alkyl; Het represents a five or six membered aromatic heterocyclic group containing (i) from one to four nitrogen heteroatom(s) or (ii) one or two nitrogen heteroatom(s) and one oxygen or one sulphur heteroatom or (iii) one or two oxygen or sulphur heteroatom (s), said heterocyclic group being optionally substituted by one or more groups selected from CN and C 1-6 alkyl; R 8 represents C 1-6 alkyl, C 1-6 alkyloxy, C 3-8 cycloalkyl, or halo; R 9 and R 10 independently represent H, C 1-6 alkyl, C 1-6 alkyloxy, CN, CF 3 or halo; may be useful for treating endometriosis, uterine fibroids (leiomyomata), menorrhagia, adenomyosis, primary and secondary dysmenorrhoea (including symptoms of dyspareunia, dyschexia and chronic pelvic pain), or chronic pelvic pain syndrome.
摘要翻译：式（I）化合物或其药学上可接受的衍生物，其中：R 1表示H，C 1-6烷基，C 1-6 烷氧基，C 3-8环烷基或卤素; R 2表示H，C 1-6烷基（任选被R 3 O 3取代），苯基（任选被CN取代）或Het; R 3表示OH，CN，Het，-R 4，C 1-6烷基或CONR 5 [R ^{6 ; R 4表示2 CO 2 - 或αO-; R 5和R 6独立地表示H，C 1-6烷基（任选被OR 7取代）或 ç_{3-8 环烷基; R 7表示H或C 1-6烷基; Het表示含有（i）1-4个氮杂原子或（ii）一个或两个氮杂原子和一个氧或一个硫杂原子的五元或六元芳族杂环基，或（iii）一个或两个氧或硫杂原子，所述杂环基团任选被一个或多个选自CN和C 1-6烷基的基团取代; R 8表示C 1-6烷基，C 1-6烷氧基，C 3-8环烷基，或光环; R 9和R 10独立地代表H，C 1-6烷基，C 1-6烷氧基，CN CF 3或卤素; 可能有助于治疗子宫内膜异位症，子宫肌瘤（平滑肌瘤），月经过多，子宫腺肌症，原发性和继发性痛经（包括性交疼痛，dyschexia和慢性盆腔疼痛症状）或慢性盆腔疼痛综合征。}}

10. 发明申请

WO2004096810A1 5,7-DIAMINOPYRAZOLO`4,3-D!PYRIMIDINES USEFUL IN THE TREATMENT OF HYPERTENSION 审中-公开
标题翻译：用于治疗高血压的5,7-二氨基吡唑并[4,3-D]吡啶
公开(公告)号：WO2004096810A1
公开(公告)日：2004-11-11
申请号：PCT/IB2004/001433
申请日：2004-04-22
申请人： PFIZER LIMITED , PFIZER INC. , BELL, Andrew, Simon , BROWN, David, Graham , FOX, David, Nathan, Abraham , MARSH, Ian, Roger , MORRELL, Andrew, Ian , PALMER, Michael, John , WINSLOW, Carol, Ann
发明人： BELL, Andrew, Simon , BROWN, David, Graham , FOX, David, Nathan, Abraham , MARSH, Ian, Roger , MORRELL, Andrew, Ian , PALMER, Michael, John , WINSLOW, Carol, Ann
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： This invention relates to compounds of formula (I).
摘要翻译：本发明涉及式（I）化合物。

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