-
公开(公告)号:US08604024B2
公开(公告)日:2013-12-10
申请号:US13477143
申请日:2012-05-22
申请人: Lorin A. Thompson, III , Jianliang Shi , Yong-Jin Wu , Lawrence R. Marcin , Ramkumar Rajamani , Mendi A. Higgins
发明人: Lorin A. Thompson, III , Jianliang Shi , Yong-Jin Wu , Lawrence R. Marcin , Ramkumar Rajamani , Mendi A. Higgins
IPC分类号: C07D279/08 , C07D513/04 , C07D417/10
CPC分类号: C07D279/08 , C07D417/04 , C07D417/10 , C07D417/12 , C07D513/04
摘要: Compounds of formula (I), including pharmaceutically acceptable salts thereof, are set forth herein: wherein X is selected from the group of CH2, O, and NR2; m=0 or 1; R1 at each instance is selected from the group of halogen, hydroxy, amino, C1-4alkylamino, C1-4dialkylamino, haloC1-4 alkyl, CN, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, and C2-C4 alkynyl; L is a bond, —NHCO—, —NH—, or L and Z together can be absent; Z is a C6-C10-aryl group or a 5-10 membered heterocyclic group which can be further substituted with from 0-3 substituents selected from the group of halogen, haloC1-4 alkoxy, 4-methoxyphenyl, hydroxy, amino, C1-4alkylamino, C1-4dialkylamino, haloC1-4 alkyl, CN, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, and C2-C4 alkynyl; R2 is selected from the group of hydrogen, benzyl, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, acetyl, and methanesulfonyl; and R3, R4 and R5 are independently selected from hydrogen or C1-4alkyl.
摘要翻译: 包括其药学上可接受的盐的式(I)化合物在本文中阐述:其中X选自CH 2,O和NR 2; m = 0或1; 每个实例的R 1选自卤素,羟基,氨基,C 1-4烷基氨基,C 1-4二烷基氨基,卤代C 1-4烷基,CN,C 1 -C 6烷基或环烷基,C 1 -C 6烷氧基和C 2 -C 4炔基; L是键,-NHCO-,-NH-或L和Z可以不存在; Z是可以被0-3个选自卤素,卤代C 1-4烷氧基,4-甲氧基苯基,羟基,氨基,C 1 -C 10 - 芳基的取代基取代的C 6 -C 10 - 芳基或5-10元杂环基, C 1-4烷基氨基,卤代C 1-4烷基,CN,C 1 -C 6烷基或环烷基,C 1 -C 6烷氧基和C 2 -C 4炔基; R 2选自氢,苄基,C 1 -C 6烷基或环烷基,C 1 -C 6烷氧基,乙酰基和甲磺酰基; 并且R 3,R 4和R 5独立地选自氢或C 1-4烷基。
-
公开(公告)号:US20130131051A1
公开(公告)日:2013-05-23
申请号:US13477143
申请日:2012-05-22
申请人: LORIN A. THOMPSON, III , Jianliang Shi , Yong-Jin Wu , Lawrence R. Marcin , Ramkumar Rajamani , Mendi A. Higgins
发明人: LORIN A. THOMPSON, III , Jianliang Shi , Yong-Jin Wu , Lawrence R. Marcin , Ramkumar Rajamani , Mendi A. Higgins
IPC分类号: C07D279/08 , C07D513/04 , C07D417/10
CPC分类号: C07D279/08 , C07D417/04 , C07D417/10 , C07D417/12 , C07D513/04
摘要: Compounds of formula (I), including pharmaceutically acceptable salts thereof, are set forth herein: wherein X is selected from the group of CH2, O, and NR2; m=0 or 1; R1 at each instance is selected from the group of halogen, hydroxy, amino, C1-4alkylamino, C1-4dialkylamino, haloC1-4 alkyl, CN, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, and C2-C4 alkynyl; L is a bond, —NHCO—, —NH—, or L and Z together can be absent; Z is a C6-C10-aryl group or a 5-10 membered heterocyclic group which can be further substituted with from 0-3 substituents selected from the group of halogen, haloC1-4 alkoxy, 4-methoxyphenyl, hydroxy, amino, C1-4alkylamino, C1-4dialkylamino, haloC1-4 alkyl, CN, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, and C2-C4 alkynyl; R2 is selected from the group of hydrogen, benzyl, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, acetyl, and methanesulfonyl; and R3, R4 and R5 are independently selected from hydrogen or C1-4alkyl.
摘要翻译: 包括其药学上可接受的盐的式(I)化合物在本文中阐述:其中X选自CH 2,O和NR 2; m = 0或1; 每个实例的R 1选自卤素,羟基,氨基,C 1-4烷基氨基,C 1-4二烷基氨基,卤代C 1-4烷基,CN,C 1 -C 6烷基或环烷基,C 1 -C 6烷氧基和C 2 -C 4炔基; L是键,-NHCO-,-NH-或L和Z可以不存在; Z是可以被0-3个选自卤素,卤代C 1-4烷氧基,4-甲氧基苯基,羟基,氨基,C 1 -C 10 - 芳基的取代基取代的C 6 -C 10 - 芳基或5-10元杂环基, C 1-4烷基氨基,卤代C 1-4烷基,CN,C 1 -C 6烷基或环烷基,C 1 -C 6烷氧基和C 2 -C 4炔基; R 2选自氢,苄基,C 1 -C 6烷基或环烷基,C 1 -C 6烷氧基,乙酰基和甲磺酰基; 并且R 3,R 4和R 5独立地选自氢或C 1-4烷基。
-
3.
公开(公告)号:US08349880B2
公开(公告)日:2013-01-08
申请号:US12683791
申请日:2010-01-07
申请人: Lawrence R. Marcin , Lorin A. Thompson, III , Kenneth M. Boy , Jason M. Guernon , Mendi A. Higgins , Jianliang Shi , Yong-Jin Wu , Yunhui Zhang , John E. Macor
发明人: Lawrence R. Marcin , Lorin A. Thompson, III , Kenneth M. Boy , Jason M. Guernon , Mendi A. Higgins , Jianliang Shi , Yong-Jin Wu , Yunhui Zhang , John E. Macor
IPC分类号: A61K31/41 , A61K31/425 , C07D249/00 , C07D277/82
CPC分类号: C07D487/04 , C07D417/12 , C07D471/04 , C07D513/10
摘要: The present disclosure provides a series of compounds of the formula (I) which reduce β-amyloid peptide (β-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by β-amyloid peptide (β-AP) production.
摘要翻译: 本公开提供了一系列式(I)的化合物,其减少β-淀粉状蛋白肽(&bgr--AP)产生,并且可用于治疗阿尔茨海默氏病和其它受β-淀粉状蛋白肽(&bgr; -AP)生产。
-
4.
公开(公告)号:US20110015175A1
公开(公告)日:2011-01-20
申请号:US12683791
申请日:2010-01-07
申请人: Lawrence R. Marcin , Lorin A. Thompson, III , Kenneth M. Boy , Jason M. Guernon , Mendi A. Higgins , Jianliang Shi , Yong-Jin Wu , Yunhui Zhang , John E. Macor
发明人: Lawrence R. Marcin , Lorin A. Thompson, III , Kenneth M. Boy , Jason M. Guernon , Mendi A. Higgins , Jianliang Shi , Yong-Jin Wu , Yunhui Zhang , John E. Macor
IPC分类号: A61K31/55 , C07D487/04 , C07D417/12 , C07D491/20 , A61K31/437 , A61K31/428 , A61K31/4439 , A61P25/28 , A61P25/00 , A61P27/02 , A61P35/00
CPC分类号: C07D487/04 , C07D417/12 , C07D471/04 , C07D513/10
摘要: The present disclosure provides a series of compounds of the formula (I) which reduce β-amyloid peptide (β-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by β-amyloid peptide (β-AP) production.
摘要翻译: 本公开提供了一系列式(I)的化合物,其减少β-淀粉状蛋白肽(&bgr--AP)产生,并且可用于治疗阿尔茨海默氏病和其它受β-淀粉状蛋白肽(&bgr; -AP)生产。
-
公开(公告)号:US08486952B2
公开(公告)日:2013-07-16
申请号:US12845045
申请日:2010-07-28
申请人: Kenneth M. Boy , Jason M. Guernon , John E. Macor , Richard E. Olson , Jianliang Shi , Lorin A. Thompson, III , Yong-Jin Wu , Li Xu , Yunhui Zhang , Dmitry S. Zuev
发明人: Kenneth M. Boy , Jason M. Guernon , John E. Macor , Richard E. Olson , Jianliang Shi , Lorin A. Thompson, III , Yong-Jin Wu , Li Xu , Yunhui Zhang , Dmitry S. Zuev
IPC分类号: A01N43/54 , A01N43/90 , A61K31/517 , A61K31/519 , A61K31/52 , A61K31/497 , A61K31/00 , A61K31/535 , C07D239/70 , C07D491/00 , C07D495/00 , C07D471/00 , C07D413/00
CPC分类号: C07D403/12 , A61K31/517 , A61K31/519 , A61K31/5377 , C07D239/70 , C07D401/12 , C07D401/14 , C07D403/14 , C07D407/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D491/048 , C07D491/052 , C07D491/08 , C07D491/107 , C07D491/113
摘要: The present disclosure provides a series of compounds of the formula (I) which modulate β-amyloid peptide (β-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by β-amyloid peptide (β-AP) production.
摘要翻译: 本公开提供了一系列调节β-淀粉样肽(β-AP)产生的式(I)化合物,并且可用于治疗阿尔茨海默病和其它受β-淀粉样蛋白肽(β-AP)产生影响的病症 。
-
公开(公告)号:US08710061B2
公开(公告)日:2014-04-29
申请号:US13358822
申请日:2012-01-26
申请人: Kenneth M. Boy , Jason M. Guernon , John E. Macor , Richard E. Olson , Jianliang Shi , Lorin A. Thompson, III , Yong-Jin Wu , Li Xu , Yunhui Zhang , Dmitry S. Zuev
发明人: Kenneth M. Boy , Jason M. Guernon , John E. Macor , Richard E. Olson , Jianliang Shi , Lorin A. Thompson, III , Yong-Jin Wu , Li Xu , Yunhui Zhang , Dmitry S. Zuev
IPC分类号: A61K31/497 , A01N43/54 , A01N43/90
CPC分类号: C07D239/70 , A61K31/517 , A61K31/519 , C07D401/04 , C07D471/04 , C07D487/10 , C07D491/048 , C07D491/10
摘要: The present disclosure provides a series of compounds of the formula (I) which modulate β-amyloid peptide (β-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by β-amyloid peptide (β-AP) production.
摘要翻译: 本公开提供了一系列式(I)的化合物,其调节和淀粉样蛋白肽(&bgr; -AP)产生,并且可用于治疗阿尔茨海默氏病和其它受β-淀粉状蛋白肽(&bgr; -AP)生产。
-
公开(公告)号:US20130030011A1
公开(公告)日:2013-01-31
申请号:US13358822
申请日:2012-01-26
申请人: KENNETH M. BOY , Jason M. Guernon , John E. Macor , Richard E. Olson , Jianliang Shi , Lorin A. Thompson, III , Yong-Jin Wu , Li Xu , Yunhui Zhang , Dmitry S. Zuev
发明人: KENNETH M. BOY , Jason M. Guernon , John E. Macor , Richard E. Olson , Jianliang Shi , Lorin A. Thompson, III , Yong-Jin Wu , Li Xu , Yunhui Zhang , Dmitry S. Zuev
IPC分类号: A61K31/517 , C07D491/052 , A61P35/00 , A61P25/28 , A61P25/00 , A61P27/02 , C07D239/70 , C07D471/04
CPC分类号: C07D239/70 , A61K31/517 , A61K31/519 , C07D401/04 , C07D471/04 , C07D487/10 , C07D491/048 , C07D491/10
摘要: The present disclosure provides a series of compounds of the formula (I) which modulate β-amyloid peptide (β-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by β-amyloid peptide (β-AP) production.
-
公开(公告)号:US20120028994A1
公开(公告)日:2012-02-02
申请号:US13013373
申请日:2011-01-25
申请人: Kenneth M. Boy , Jason M. Guernon , John E. Macor , Richard E. Olson , Jianliang Shi , Lorin A. Thompson, III , Yong-Jin Wu , Li Xu , Yunhui Zhang , Dmitry S. Zuev
发明人: Kenneth M. Boy , Jason M. Guernon , John E. Macor , Richard E. Olson , Jianliang Shi , Lorin A. Thompson, III , Yong-Jin Wu , Li Xu , Yunhui Zhang , Dmitry S. Zuev
IPC分类号: A61K31/517 , C07D401/14 , A61P35/00 , A61P25/28 , A61P25/00 , A61P27/02 , C07D403/12 , C07D401/12
CPC分类号: A61K31/517 , A61K31/519 , A61K31/5377 , C07D239/70 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D407/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D491/052 , C07D491/08 , C07D491/107 , C07D491/113
摘要: The present disclosure provides a series of compounds of the formula (I) which modulate β-amyloid peptide (β-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by β-amyloid peptide (β-AP) production.
摘要翻译: 本公开提供了一系列式(I)的化合物,其调节和淀粉样蛋白肽(&bgr; -AP)产生,并且可用于治疗阿尔茨海默氏病和其它受β-淀粉状蛋白肽(&bgr; -AP)生产。
-
公开(公告)号:US08637525B2
公开(公告)日:2014-01-28
申请号:US13013373
申请日:2011-01-25
申请人: Kenneth M. Boy , Jason M. Guernon , John E. Macor , Richard E. Olson , Jianliang Shi , Lorin A. Thompson, III , Yong-Jin Wu , Li Xu , Yunhui Zhang , Dmitry S. Zuev
发明人: Kenneth M. Boy , Jason M. Guernon , John E. Macor , Richard E. Olson , Jianliang Shi , Lorin A. Thompson, III , Yong-Jin Wu , Li Xu , Yunhui Zhang , Dmitry S. Zuev
IPC分类号: A01N43/54 , A01N43/90 , A61K31/517 , A61K31/519 , A01N43/64 , A61K31/41
CPC分类号: A61K31/517 , A61K31/519 , A61K31/5377 , C07D239/70 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D407/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D491/052 , C07D491/08 , C07D491/107 , C07D491/113
摘要: The present disclosure provides a series of compounds of the formula (I) which modulate β-amyloid peptide (β-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by β-amyloid peptide (β-AP) production.
摘要翻译: 本公开提供了一系列调节β-淀粉样肽(β-AP)产生的式(I)化合物,并且可用于治疗阿尔茨海默病和其它受β-淀粉样蛋白肽(β-AP)产生影响的病症 。
-
公开(公告)号:US20110212937A1
公开(公告)日:2011-09-01
申请号:US12845045
申请日:2010-07-28
申请人: Kenneth M. Boy , Jason M. Guernon , John E. Macor , Richard E. Olson , Jianliang Shi , Lorin A. Thompson, III , Yong-Jin Wu , Li Xu , Yunhui Zhang , Dmitry S. Zuev
发明人: Kenneth M. Boy , Jason M. Guernon , John E. Macor , Richard E. Olson , Jianliang Shi , Lorin A. Thompson, III , Yong-Jin Wu , Li Xu , Yunhui Zhang , Dmitry S. Zuev
IPC分类号: A61K31/397 , C07D401/12 , A61K31/517 , C07D239/70 , C07D403/12 , C07D403/14 , C07D471/04 , A61K31/519 , C07D491/052 , C07D413/14 , A61K31/5377 , A61K31/496 , A61K31/5386 , A61P25/28
CPC分类号: C07D403/12 , A61K31/517 , A61K31/519 , A61K31/5377 , C07D239/70 , C07D401/12 , C07D401/14 , C07D403/14 , C07D407/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D491/048 , C07D491/052 , C07D491/08 , C07D491/107 , C07D491/113
摘要: The present disclosure provides a series of compounds of the formula (I) which modulate β-amyloid peptide (β-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by β-amyloid peptide (β-AP) production.
摘要翻译: 本公开提供了一系列式(I)的化合物,其调节和淀粉样蛋白肽(&bgr; -AP)产生,并且可用于治疗阿尔茨海默氏病和其它受β-淀粉状蛋白肽(&bgr; -AP)生产。
-
-
-
-
-
-
-
-
-