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公开(公告)号：US20080153817A1
公开(公告)日：2008-06-26
申请号：US10566844
申请日：2004-07-29
申请人： Dirk Beher , Michela Bettati , Graham David Checksfield , Ian Churcher , Victoria Alexandra Doughty , Paul Joseph Oakley , Abdul Quddus , Martin Richard Teall , Jonathan David Wrigley
发明人： Dirk Beher , Michela Bettati , Graham David Checksfield , Ian Churcher , Victoria Alexandra Doughty , Paul Joseph Oakley , Abdul Quddus , Martin Richard Teall , Jonathan David Wrigley
IPC分类号： A61K31/5377 , C07D209/82 , A61K31/403 , C07D295/00 , A61P25/28 , C07D209/96
CPC分类号： C07D401/04 , A61K31/403 , A61K31/4439 , C07D209/86 , C07D209/88 , C07D209/96 , C07D409/04
摘要： Compounds of formula (I): are useful in the treatment of diseases associated with deposition of β-amyloid in the brain.
摘要翻译： 式（I）化合物：可用于治疗与脑中β-淀粉样蛋白沉积相关的疾病。
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公开(公告)号：US08203004B2
公开(公告)日：2012-06-19
申请号：US12084814
申请日：2006-11-03
申请人： Frank Burkamp , Graham David Checksfield , Stephen Robert Fletcher , Stephen John Lewis , Edward Giles Mciver , Paul Joseph Oakley , Martin Richard Teall
发明人： Frank Burkamp , Graham David Checksfield , Stephen Robert Fletcher , Stephen John Lewis , Edward Giles Mciver , Paul Joseph Oakley , Martin Richard Teall
IPC分类号： C07D209/02 , C07D209/52
CPC分类号： C07D209/30 , C07D209/08 , C07D209/10 , C07D209/12 , C07D209/42 , C07D209/86 , C07D231/56 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04
摘要： Tetrahydroindole derivatives of formula (I): are disclosed. These compounds modulate the activity of gamma-secretase and hence find use in treatment or prevention of Alzheimer's disease.
摘要翻译： 公开了式（I）的四氢吲哚衍生物： 这些化合物调节γ-分泌酶的活性，因此可用于治疗或预防阿尔茨海默氏病。
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公开(公告)号：US20100016308A1
公开(公告)日：2010-01-21
申请号：US12084814
申请日：2006-11-03
申请人： Frank Burkamp , Graham David Checksfield , Stephen Robert Fletcher , Stephen John Lewis , Edward Giles Meiver , Paul Joseph Oakley , Martin Richard Teall
发明人： Frank Burkamp , Graham David Checksfield , Stephen Robert Fletcher , Stephen John Lewis , Edward Giles Meiver , Paul Joseph Oakley , Martin Richard Teall
IPC分类号： A61K31/5377 , C07D209/52 , A61K31/403 , C07D401/04 , A61K31/4439 , C07D413/02
CPC分类号： C07D209/30 , C07D209/08 , C07D209/10 , C07D209/12 , C07D209/42 , C07D209/86 , C07D231/56 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04
摘要： Tetrahydroindole derivatives of formula (I): are disclosed. These compounds modulate the activity of gamma-secretase and hence find use in treatment or prevention of Alzheimer's disease.
摘要翻译： 公开了式（I）的四氢吲哚衍生物： 这些化合物调节γ-分泌酶的活性，因此可用于治疗或预防阿尔茨海默氏病。
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公开(公告)号：US07598386B2
公开(公告)日：2009-10-06
申请号：US11788888
申请日：2007-04-23
申请人： Jose Luis Castro Pineiro , Ian Churcher , Kevin Dinnell , Timothy Harrison , Sonia Kerrad , Alan John Nadin , Paul Joseph Oakley , Andrew Pate Owens , Duncan Edward Shaw , Martin Richard Teall , Susannah William , Brian John Williams
发明人： Jose Luis Castro Pineiro , Ian Churcher , Kevin Dinnell , Timothy Harrison , Sonia Kerrad , Alan John Nadin , Paul Joseph Oakley , Andrew Pate Owens , Duncan Edward Shaw , Martin Richard Teall , Susannah William , Brian John Williams
IPC分类号： C07D211/00 , C07D211/68 , C07D211/40 , C07D211/70 , C07D309/00
CPC分类号： C07D207/27 , C07C317/14 , C07C317/20 , C07C317/24 , C07C317/30 , C07C317/46 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07D207/12 , C07D207/404 , C07D211/18 , C07D211/42 , C07D211/46 , C07D211/54 , C07D211/60 , C07D211/62 , C07D213/40 , C07D213/64 , C07D213/65 , C07D231/12 , C07D233/32 , C07D233/40 , C07D233/56 , C07D233/64 , C07D241/18 , C07D249/04 , C07D249/08 , C07D249/12 , C07D257/04 , C07D263/38 , C07D263/44 , C07D271/06 , C07D277/26 , C07D285/12 , C07D295/088 , C07D295/096 , C07D295/182 , C07D307/52 , C07D309/08 , C07D309/10 , C07D317/48 , C07D317/72 , C07D491/10 , C07F7/0812
摘要： Novel sulphones of Formula I are disclosed: wherein A completes a 4-7 membered ring optionally comprising up to two heteroatoms. The compounds modulate the action of γ-secretase and are therefore useful in the treatment or prevention of Alzheimer's disease.
摘要翻译： 公开了式I的新型砜：其中A完成任选包含最多两个杂原子的4-7元环。 该化合物调节γ-分泌酶的作用，因此可用于治疗或预防阿尔茨海默氏病。
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公开(公告)号：US07304094B2
公开(公告)日：2007-12-04
申请号：US11261365
申请日：2005-10-28
申请人： Ian Churcher , Kevin Dinnell , Timothy Harrison , Sonia Kerrad , Alan John Nadin , Paul Joseph Oakley , Duncan Edward Shaw , Martin Richard Teall , Susannah Williams , Brian John Williams
发明人： Ian Churcher , Kevin Dinnell , Timothy Harrison , Sonia Kerrad , Alan John Nadin , Paul Joseph Oakley , Duncan Edward Shaw , Martin Richard Teall , Susannah Williams , Brian John Williams
IPC分类号： A61K31/165 , C07C321/24
CPC分类号： C07D213/40 , C07C317/20 , C07C317/24 , C07C317/30 , C07C317/44 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D207/27 , C07D207/404 , C07D211/44 , C07D211/46 , C07D211/60 , C07D211/62 , C07D213/36 , C07D213/64 , C07D213/65 , C07D231/12 , C07D233/32 , C07D233/56 , C07D233/60 , C07D233/61 , C07D233/64 , C07D233/72 , C07D249/04 , C07D249/08 , C07D249/12 , C07D257/04 , C07D263/44 , C07D271/06 , C07D271/10 , C07D277/26 , C07D285/12 , C07D295/096 , C07D295/185
摘要： Novel sulphones of formula I are disclosed: The compounds modulate the processing of amyloid precursor protein by gamma-secretase, and hence are useful in the treatment or prevention of Alzheimer's disease.
摘要翻译： 公式I的新型手机被公开：
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公开(公告)号：US07101895B2
公开(公告)日：2006-09-05
申请号：US10679557
申请日：2003-10-06
申请人： Ian Churcher , Timothy Harrison , Sonia Kerrad , Paul Joseph Oakley , Duncan Edward Shaw , Martin Richard Teall , Susannah Williams
发明人： Ian Churcher , Timothy Harrison , Sonia Kerrad , Paul Joseph Oakley , Duncan Edward Shaw , Martin Richard Teall , Susannah Williams
IPC分类号： A01N43/40 , A61K31/445
CPC分类号： C07D213/70 , C07C317/14 , C07C317/18 , C07C317/20 , C07C317/22 , C07C317/24 , C07C317/44 , C07C331/04 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D205/04 , C07D207/48 , C07D211/96 , C07D213/71 , C07D213/89 , C07D233/84 , C07D239/38 , C07D249/12 , C07D257/04 , C07D277/36 , C07D285/125 , C07D295/088 , C07D295/26 , C07D307/38 , C07D307/46 , C07D307/52 , C07D307/64 , C07D307/68 , C07D317/46 , C07D333/18 , C07D333/48 , C07D491/08
摘要： Compounds of formula I: wherein Ar1 and Ar2 are optionally substituted aryl or heteroaryl, L is a bond, ═CH— or —(CHRa)n—, and X is SCN, SR1, S(O)R1, (CRaRb)mSO2R1, SO2N(R2)2, SO2NHCOR1, SO2NHN(R2)2, OSO2N(R2)2, OS(O)N(R2)2, OSO2NHCOR1, COR4, NHCOR1, NHCO2R1, NHCON(R2)2, NHSO2R1 or NHSO2N(R2)2, inhibit the processing of APP by gamma secretase, and hence are useful in treatment of Alzheimer's disease.
摘要翻译： 式I的化合物：其中Ar 1和Ar 2是任选取代的芳基或杂芳基，L是键，-CH-或 - （CHR） S（O）R 1，S（O）R 1，...，S（O）R 1， SO 2 SO 2 SO 2，SO 2 N（N，N） R 2，N 2，NH 2，NH 2，NH 2（R 2） 2 O 2，OSO 2 N（R 2）2，OS（ O）N（R 2）2，OSO 2，NHCOR 1，COR 4， ，NHCOR 1，NHCO 2 R 1，NHCON（R 2）2，/ SUB >，NHSO 2 R 1，或NHSO 2 N（R 2）2， ，通过γ分泌酶抑制APP的处理，因此可用于治疗阿尔茨海默氏病。
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公开(公告)号：US06984663B2
公开(公告)日：2006-01-10
申请号：US10223993
申请日：2002-08-20
申请人： Ian Churcher , Kevin Dinnell , Timothy Harrison , Sonia Kerrad , Alan John Nadin , Paul Joseph Oakley , Duncan Edward Shaw , Martin Richard Teall , Susannah Williams , Brian John Williams
发明人： Ian Churcher , Kevin Dinnell , Timothy Harrison , Sonia Kerrad , Alan John Nadin , Paul Joseph Oakley , Duncan Edward Shaw , Martin Richard Teall , Susannah Williams , Brian John Williams
IPC分类号： A61K31/19 , C07C317/12 , C07C317/14
CPC分类号： C07D213/40 , C07C317/20 , C07C317/24 , C07C317/30 , C07C317/44 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D207/27 , C07D207/404 , C07D211/44 , C07D211/46 , C07D211/60 , C07D211/62 , C07D213/36 , C07D213/64 , C07D213/65 , C07D231/12 , C07D233/32 , C07D233/56 , C07D233/60 , C07D233/61 , C07D233/64 , C07D233/72 , C07D249/04 , C07D249/08 , C07D249/12 , C07D257/04 , C07D263/44 , C07D271/06 , C07D271/10 , C07D277/26 , C07D285/12 , C07D295/096 , C07D295/185
摘要： Novel sulphones of formula I are disclosed: The compounds modulate the processing of amyloid precursor protein by gamma-secretase, and hence are useful in the treatment or prevention of Alzheimer's disease.
摘要翻译： 公开了式I的新型砜：该化合物通过γ-分泌酶调节淀粉样蛋白前体蛋白的加工，因此可用于治疗或预防阿尔茨海默氏病。
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公开(公告)号：US07595344B2
公开(公告)日：2009-09-29
申请号：US12151296
申请日：2008-05-06
申请人： Jose Luis Castro Pineiro , Ian Churcher , Kevin Dinnell , Timothy Harrison , Sonia Kerrad , Alan John Nadin , Paul Joseph Oakley , Andrew Pate Owens , Duncan Edward Shaw , Martin Richard Teall , Susannah William , Brian John Williams
发明人： Jose Luis Castro Pineiro , Ian Churcher , Kevin Dinnell , Timothy Harrison , Sonia Kerrad , Alan John Nadin , Paul Joseph Oakley , Andrew Pate Owens , Duncan Edward Shaw , Martin Richard Teall , Susannah William , Brian John Williams
IPC分类号： A61K31/65
CPC分类号： C07D207/27 , C07C317/14 , C07C317/20 , C07C317/24 , C07C317/30 , C07C317/46 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07D207/12 , C07D207/404 , C07D211/18 , C07D211/42 , C07D211/46 , C07D211/54 , C07D211/60 , C07D211/62 , C07D213/40 , C07D213/64 , C07D213/65 , C07D231/12 , C07D233/32 , C07D233/40 , C07D233/56 , C07D233/64 , C07D241/18 , C07D249/04 , C07D249/08 , C07D249/12 , C07D257/04 , C07D263/38 , C07D263/44 , C07D271/06 , C07D277/26 , C07D285/12 , C07D295/088 , C07D295/096 , C07D295/182 , C07D307/52 , C07D309/08 , C07D309/10 , C07D317/48 , C07D317/72 , C07D491/10 , C07F7/0812
摘要： Disclosed are sulphones which modulate the action of gamma-secretase. The compounds are useful in the treatment or prevention of Alzheimer's disease.
摘要翻译： 公开了调节γ-分泌酶作用的唾液。 该化合物可用于治疗或预防阿尔茨海默病。
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公开(公告)号：US20090131419A1
公开(公告)日：2009-05-21
申请号：US12151296
申请日：2008-05-06
申请人： Jose Luis Castro Pineiro , Ian Churcher , Kevin Dinnell , Timothy Harrison , Sonia Kerrad , Alan John Nadin , Paul Joseph Oakley , Andrew Pate Owens , Duncan Edward Shaw , Martin Richard Teall , Susannah William , Brian John Williams
发明人： Jose Luis Castro Pineiro , Ian Churcher , Kevin Dinnell , Timothy Harrison , Sonia Kerrad , Alan John Nadin , Paul Joseph Oakley , Andrew Pate Owens , Duncan Edward Shaw , Martin Richard Teall , Susannah William , Brian John Williams
IPC分类号： A61K31/54 , C07C317/14 , A61K31/10 , C07D295/14 , A61P25/28 , C07D241/04 , A61K31/495
CPC分类号： C07D207/27 , C07C317/14 , C07C317/20 , C07C317/24 , C07C317/30 , C07C317/46 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07D207/12 , C07D207/404 , C07D211/18 , C07D211/42 , C07D211/46 , C07D211/54 , C07D211/60 , C07D211/62 , C07D213/40 , C07D213/64 , C07D213/65 , C07D231/12 , C07D233/32 , C07D233/40 , C07D233/56 , C07D233/64 , C07D241/18 , C07D249/04 , C07D249/08 , C07D249/12 , C07D257/04 , C07D263/38 , C07D263/44 , C07D271/06 , C07D277/26 , C07D285/12 , C07D295/088 , C07D295/096 , C07D295/182 , C07D307/52 , C07D309/08 , C07D309/10 , C07D317/48 , C07D317/72 , C07D491/10 , C07F7/0812
摘要： Disclosed are sulphones which modulate the action of gamma-secretase. The compounds are useful in the treatment or prevention of Alzheimer's disease.
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公开(公告)号：US07276637B2
公开(公告)日：2007-10-02
申请号：US10522261
申请日：2003-07-30
申请人： Karel Marie Joseph Brands , Antony John Davies , Paul Joseph Oakley , Jeremy Peter Scott , Duncan Edward Shaw , Martin Richard Teall
发明人： Karel Marie Joseph Brands , Antony John Davies , Paul Joseph Oakley , Jeremy Peter Scott , Duncan Edward Shaw , Martin Richard Teall
IPC分类号： C07C15/00
CPC分类号： C07C315/04 , C07C2601/14 , C07C317/24 , C07C317/44
摘要： A novel process for preparing cyclohexanone derivatives of formula (I) is described. The products are useful as gamma secretase inhibitors, or as intermediates in the synthesis of other gamma secretase inhibitors.
摘要翻译： 描述了制备式（I）的环己酮衍生物的新方法。 该产物可用作γ分泌酶抑制剂，或作为合成其它γ分泌酶抑制剂的中间体。
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