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1. 发明申请

US20120245176A1 NOVEL PIPERAZINE ANALOGS WITH SUBSTITUTED HETEROARYL GROUPS AS BROAD-SPECTRUM INFLUENZA ANTIVIRALS 审中-公开
标题翻译：具有替代性荧光素酶的新型哌嗪类似物作为广谱流感病毒
公开(公告)号：US20120245176A1
公开(公告)日：2012-09-27
申请号：US13242676
申请日：2011-09-23
申请人： Christopher W. Cianci , Samuel Gerritz , Sean Kim , David R. Langley , Guo Li , Bradley C. Pearce , Annapurna Pendri , Shuhao Shi , Weixu Zhai , Shirong Zhu
发明人： Christopher W. Cianci , Samuel Gerritz , Sean Kim , David R. Langley , Guo Li , Bradley C. Pearce , Annapurna Pendri , Shuhao Shi , Weixu Zhai , Shirong Zhu
IPC分类号： A61K31/496 , C07D413/14 , A61K31/506 , A61P31/16 , C07D403/06 , C07D401/14 , C07D417/06 , A61P31/12 , C07D413/06 , A61K31/498
CPC分类号： C07D413/06 , C07D403/06 , C07D413/14
摘要： A compound of Formula I is set forth, including pharmaceutically acceptable salts thereof: wherein Het is a 5 or 6-membered heterocycle with —N, —O, or —S adjacent to the —Ar substituent or adjacent to the point of attachment for the —Ar substituent; Ar is aryl or heteroaryl; R is —CH3, —CH2F, —CHF2 or —CH═CH2; V is —H, —CH3 or ═O; W is —NO2, —Cl, —Br, —CH2OH, or —CN; X is —Cl, —Br, —F, —CH3, —OCH3, or —CN; Y is —CH or —N; and Z is —CH or —N. This compound is useful in compositions for the prevention and treatment of influenza virus.
摘要翻译：提出了式I的化合物，包括其药学上可接受的盐：其中Het是与-Ar取代基相邻的具有-N，-O或-S的5或6元杂环，或邻近-Ar取代基的连接点 -Ar取代基; Ar是芳基或杂芳基; R是-CH 3，-CH 2 F，-CHF 2或-CH = CH 2; V是-H，-CH 3或= O; W是-NO 2，-Cl，-Br，-CH 2 OH或-CN; X是-Cl，-Br，-F，-CH 3，-OCH 3或-CN; Y是-CH或-N; 并且Z是-CH或-N。该化合物可用于预防和治疗流感病毒的组合物。

2. 发明申请

US20060287287A1 Aminoacetamide acyl guanidines as beta-secretase inhibitors 有权
标题翻译：氨基乙酰胺酰基鸟苷作为β-分泌酶抑制剂
公开(公告)号：US20060287287A1
公开(公告)日：2006-12-21
申请号：US11471104
申请日：2006-06-20
申请人： Samuel Gerritz , Shuhao Shi , Shirong Zhu
发明人： Samuel Gerritz , Shuhao Shi , Shirong Zhu
IPC分类号： A61K31/55 , A61K31/454 , A61K31/4439 , A61K31/496 , A61K31/425 , A61K31/42 , A61K31/416
CPC分类号： C07D275/03 , C07D231/14 , C07D261/18 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： There is provided a series of substituted acyl guanidines of Formula (Ik) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R2, R3, R4, R5, R25, R26 and R27 as defined herein, their pharmaceutical compositions and methods of use. These compounds inhibit the processing of amyloid precursor protein (APP) by β-secretase and, more specifically, inhibit the production of Aβ-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to β-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
摘要翻译：提供一系列式（Ik）的取代酰基胍或立体异构体; 或其药学上可接受的盐，其中R 2，R 3，R 4，R 5，R 5，如本文所定义的其药物组合物和使用方法。这些化合物通过β-分泌酶抑制淀粉样蛋白前体蛋白（APP）的加工，更具体地抑制Aβ-肽的产生。本公开涉及可用于治疗与β-淀粉样蛋白产生相关的神经系统疾病的化合物，例如阿尔茨海默病和受抗淀粉样蛋白活性影响的其它病症。

3. 发明授权

US07732434B2 Macrocyclic acyl guanidines as beta-secretase inhibitors 有权
标题翻译：大环酰基鸟苷作为β-分泌酶抑制剂
公开(公告)号：US07732434B2
公开(公告)日：2010-06-08
申请号：US12099334
申请日：2008-04-08
申请人： Shuhao Shi , Samuel Gerritz , Shirong Zhu
发明人： Shuhao Shi , Samuel Gerritz , Shirong Zhu
IPC分类号： C07D267/22 , A61K31/33
CPC分类号： C07D513/04 , C07D498/04
摘要： There is provided a series of heterocyclic-containing macrocyclic acyl guanidines of Formula (I) or a stereoisomer; or a nontoxic pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, n and X as defined herein, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein (APP) by β-secretase and, more specifically, inhibit the production of Aβ-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to β-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
摘要翻译：提供一系列式（I）的含杂环的大环酰基胍或立体异构体; 或其无毒的药学上可接受的盐，其中如本文所定义的R 1，R 2，R 3，R 4，R 5，n和X，其药物组合物和使用方法。这些新化合物通过分泌酶抑制淀粉样蛋白前体蛋白（APP）的加工，更具体地，抑制Aβ的生成。本公开涉及可用于治疗与淀粉样蛋白产生相关的神经系统疾病的化合物，例如阿尔茨海默病和受抗淀粉样蛋白活性影响的其它病症。

4. 发明授权

US07612069B2 Acyl guanidines as beta-secretase inhibitors 有权
标题翻译：酰基胍作为β-分泌酶抑制剂
公开(公告)号：US07612069B2
公开(公告)日：2009-11-03
申请号：US11471125
申请日：2006-06-20
申请人： Samuel Gerritz , Weixu Zhai , Shuhao Shi , Shirong Zhu , Andrew C. Good , Lorin A. Thompson, III
发明人： Samuel Gerritz , Weixu Zhai , Shuhao Shi , Shirong Zhu , Andrew C. Good , Lorin A. Thompson, III
IPC分类号： A61K31/5377 , A61K31/55 , A61K31/416 , C07D231/12
CPC分类号： C07D275/03 , C07D231/14 , C07D261/18 , C07D413/12
摘要： There is provided a series of substituted acyl guanidines of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4 and R5 as defined herein, their pharmaceutical compositions and methods of use. These compounds inhibit the processing of amyloid precursor protein (APP) by β-secretase and, more specifically, inhibit the production of Aβ-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to β-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
摘要翻译：提供一系列式（I）的取代酰基胍或立体异构体; 或其药学上可接受的盐，其中如本文所定义的R 1，R 2，R 3，R 4和R 5，其药物组合物和使用方法。这些化合物通过β-分泌酶抑制淀粉样蛋白前体蛋白（APP）的加工，更具体地抑制Aβ-肽的产生。本公开涉及可用于治疗与β-淀粉样蛋白产生相关的神经系统疾病的化合物，例如阿尔茨海默病和受抗淀粉样蛋白活性影响的其它病症。

5. 发明授权

US08362004B2 Piperazine analogs as broad-spectrum influenza antivirals 有权
标题翻译：哌嗪类似物作为广谱流感病毒抗生素
公开(公告)号：US08362004B2
公开(公告)日：2013-01-29
申请号：US13225851
申请日：2011-09-06
申请人： Christopher W. Cianci , Samuel Gerritz , Guo Li , Bradley C. Pearce , Annapurna Pendri , Shuhao Shi , Weixu Zhai , Shirong Zhu
发明人： Christopher W. Cianci , Samuel Gerritz , Guo Li , Bradley C. Pearce , Annapurna Pendri , Shuhao Shi , Weixu Zhai , Shirong Zhu
IPC分类号： A61K31/397 , A61K31/496 , C07D403/04 , C07D403/14 , C07D413/04 , C07D413/14
CPC分类号： C07D261/18 , C07D207/327 , C07D231/14 , C07D233/90 , C07D249/06 , C07D403/12 , C07D413/12 , C07D417/12
摘要： A compound of Formula I is set forth, including pharmaceutically acceptable salts thereof: wherein Het is a 5 or 6-membered heterocycle with —N, —O, or —S adjacent to the —Ar substituent or adjacent to the point of attachment for the —Ar substituent; Ar is aryl or heteroaryl; R is —CH3, —CH2F, or —CH═CH2; W is —NO2, —Cl, —Br, —CHO, —CH═CH2, or —CN; X is —Cl, —CH3, or —CN; Y is —CH or —N; and Z is C1-C6 alkyl, C3-C6 cycloalkyl, substituted aryl, substituted heteroaryl, OR1, or NHR1, wherein R1 is selected from the group of H, aryl, heteroaryl, C1-C6 alkyl and C3-C6 cycloalkyl. This compound is useful in compositions for the prevention and treatment of influenza virus.
摘要翻译：提出了式I的化合物，包括其药学上可接受的盐：其中Het是与-Ar取代基相邻的具有-N，-O或-S的5或6元杂环，或邻近-Ar取代基的连接点 -Ar取代基; Ar是芳基或杂芳基; R是-CH 3，-CH 2 F或-CH = CH 2; W是-NO 2，-Cl，-Br，-CHO，-CH = CH 2或-CN; X是-Cl，-CH 3或-CN; Y是-CH或-N; 并且Z是C 1 -C 6烷基，C 3 -C 6环烷基，取代的芳基，取代的杂芳基，OR 1或NHR 1，其中R 1选自H，芳基，杂芳基，C 1 -C 6烷基和C 3 -C 6环烷基。该化合物可用于预防和治疗流感病毒的组合物。

6. 发明申请

US20120238539A1 NOVEL PIPERAZINE ANALOGS AS BROAD-SPECTRUM INFLUENZA ANTIVIRALS 有权
标题翻译：新型PIPERAZINE模拟物作为广谱流感病毒
公开(公告)号：US20120238539A1
公开(公告)日：2012-09-20
申请号：US13225851
申请日：2011-09-06
申请人： Christopher W. Cianci , Samuel Gerritz , Guo Li , Bradley C. Pearce , Annapurna Pendri , Shuhao Shi , Weixu Zhai , Shirong Zhu
发明人： Christopher W. Cianci , Samuel Gerritz , Guo Li , Bradley C. Pearce , Annapurna Pendri , Shuhao Shi , Weixu Zhai , Shirong Zhu
IPC分类号： A61K31/496 , C07D413/14 , A61P31/16 , A61K31/5355 , C07D403/14 , A61P31/12 , C07D413/06 , C07D417/14
CPC分类号： C07D261/18 , C07D207/327 , C07D231/14 , C07D233/90 , C07D249/06 , C07D403/12 , C07D413/12 , C07D417/12
摘要： A compound of Formula I is set forth, including pharmaceutically acceptable salts thereof: wherein Het is a 5 or 6-membered heterocycle with —N, —O, or —S adjacent to the —Ar substituent or adjacent to the point of attachment for the —Ar substituent; Ar is aryl or heteroaryl; R is —CH3, —CH2F, or —CH═CH2; W is —NO2, —Cl, —Br, —CHO, —CH═CH2, or —CN; X is —Cl, —CH3, or —CN; Y is —CH or —N; and Z is C1-C6 alkyl, C3-C6 cycloalkyl, substituted aryl, substituted heteroaryl, OR1, or NHR1, wherein R1 is selected from the group of H, aryl, heteroaryl, C1-C6 alkyl and C3-C6 cycloalkyl. This compound is useful in compositions for the prevention and treatment of influenza virus.
摘要翻译：提出了式I的化合物，包括其药学上可接受的盐：其中Het是与-Ar取代基相邻的具有-N，-O或-S的5或6元杂环，或邻近-Ar取代基的连接点 -Ar取代基; Ar是芳基或杂芳基; R是-CH 3，-CH 2 F或-CH = CH 2; W是-NO 2，-Cl，-Br，-CHO，-CH = CH 2或-CN; X是-Cl，-CH 3或-CN; Y是-CH或-N; 并且Z是C 1 -C 6烷基，C 3 -C 6环烷基，取代的芳基，取代的杂芳基，OR 1或NHR 1，其中R 1选自H，芳基，杂芳基，C 1 -C 6烷基和C 3 -C 6环烷基。该化合物可用于预防和治疗流感病毒的组合物。

7. 发明申请

US20080262055A1 Macrocyclic Acyl Guanidines as Beta-Secretase Inhibitors 有权
标题翻译：大环酰基胍作为β-分泌酶抑制剂
公开(公告)号：US20080262055A1
公开(公告)日：2008-10-23
申请号：US12099334
申请日：2008-04-08
申请人： Shuhao Shi , Samuel Gerritz , Shirong Zhu
发明人： Shuhao Shi , Samuel Gerritz , Shirong Zhu
IPC分类号： A61K31/425 , C07D291/00 , A61K31/42 , A61P25/28
CPC分类号： C07D513/04 , C07D498/04
摘要： There is provided a series of heterocyclic-containing macrocyclic acyl guanidines of Formula (I) or a stereoisomer; or a nontoxic pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, n and X as defined herein, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein (APP) by β-secretase and, more specifically, inhibit the production of Aβ-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to β-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
摘要翻译：提供一系列式（I）的含杂环的大环酰基胍或立体异构体; 或其无毒的药学上可接受的盐，其中R 1，R 2，R 3，R 4，R 本文定义的N，X和X，它们的药物组合物和使用方法。这些新型化合物通过β-分泌酶抑制淀粉样前体蛋白（APP）的加工，更具体地，抑制Aβ-肽的产生。本公开涉及可用于治疗与β-淀粉样蛋白产生相关的神经系统疾病的化合物，例如阿尔茨海默病和受抗淀粉样蛋白活性影响的其它病症。

8. 发明授权

US07408071B2 N-aryl pyrrolidine derivatives as beta-secretase inhibitors 有权
标题翻译： N-芳基吡咯烷衍生物作为β-分泌酶抑制剂
公开(公告)号：US07408071B2
公开(公告)日：2008-08-05
申请号：US11693034
申请日：2007-03-29
申请人： Kenneth M. Boy , Shirong Zhu , John E. Macor , Shuhao Shi , Samuel Gerritz
发明人： Kenneth M. Boy , Shirong Zhu , John E. Macor , Shuhao Shi , Samuel Gerritz
IPC分类号： C07D207/04 , C07D207/00 , A01N43/64 , A01N43/36
CPC分类号： C07D207/16 , C07D209/52
摘要： There is provided a series of substituted N-aryl pyrrolidine derivatives of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R5′, R6, R7, and p as defined herein, their pharmaceutical compositions and methods of use. These compounds inhibit the processing of amyloid precursor protein (APP) by β-secretase and, more specifically, inhibit the production of Aβ-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to β-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
摘要翻译：提供一系列式（I）的取代的N-芳基吡咯烷衍生物或立体异构体; 或其药学上可接受的盐，其中R 1，R 2，R 3，R 4，R 4，它们的药物组合物和方法，如本文所定义的，其中R 5，R 5，R 6，R 7，的使用。这些化合物通过β-分泌酶抑制淀粉样蛋白前体蛋白（APP）的加工，更具体地抑制Aβ-肽的产生。本公开涉及可用于治疗与β-淀粉样蛋白产生相关的神经系统疾病的化合物，例如阿尔茨海默病和受抗淀粉样蛋白活性影响的其它病症。

9. 发明申请

US20070232679A1 N-Aryl Pyrrolidine Derivatives as Beta-Secretase Inhibitors 有权
标题翻译： N-芳基吡咯烷衍生物作为β-分泌酶抑制剂
公开(公告)号：US20070232679A1
公开(公告)日：2007-10-04
申请号：US11693034
申请日：2007-03-29
申请人： Kenneth M. Boy , Shirong Zhu , John E. Macor , Shuhao Shi , Samuel Gerritz
发明人： Kenneth M. Boy , Shirong Zhu , John E. Macor , Shuhao Shi , Samuel Gerritz
IPC分类号： A61K31/403 , A61K31/4025 , A61K31/401
CPC分类号： C07D207/16 , C07D209/52
摘要： There is provided a series of substituted N-aryl pyrrolidine derivatives of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R5′, R6, R7, and p as defined herein, their pharmaceutical compositions and methods of use. These compounds inhibit the processing of amyloid precursor protein (APP) by β-secretase and, more specifically, inhibit the production of Aβ-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to β-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
摘要翻译：提供一系列式（I）的取代的N-芳基吡咯烷衍生物或立体异构体; 或其药学上可接受的盐，其中R 1，R 2，R 3，R 4，R 4，它们的药物组合物和方法，如本文所定义的，其中R 5，R 5，R 6，R 7，的使用。这些化合物通过β-分泌酶抑制淀粉样蛋白前体蛋白（APP）的加工，更具体地抑制Aβ-肽的产生。本公开涉及可用于治疗与β-淀粉样蛋白产生相关的神经系统疾病的化合物，例如阿尔茨海默病和受抗淀粉样蛋白活性影响的其它病症。

10. 发明申请

US20070232581A1 Oxime-Containing Acyl Guanidines as Beta-Secretase Inhibitors 有权
标题翻译：含肟的酰基胍作为β-分泌酶抑制剂
公开(公告)号：US20070232581A1
公开(公告)日：2007-10-04
申请号：US11693026
申请日：2007-03-29
申请人： Yong-Jin Wu , Samuel Gerritz , Shuhao Shi , Shirong Zhu
发明人： Yong-Jin Wu , Samuel Gerritz , Shuhao Shi , Shirong Zhu
IPC分类号： A61K31/55 , A61K31/445 , A61K31/40 , A61K31/397 , A61K31/396 , A61K31/165 , C07D211/26 , C07D207/30 , C07D223/04 , C07D203/04
CPC分类号： C07D209/20 , C07C257/20 , C07C279/22
摘要： There is provided a series of substituted oxime-containing acyl guanidines of Formula (I) or a stereoisomer; or a nontoxic pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, and R7 are as defined herein, their pharmaceutical compositions and methods of use. These compounds inhibit the processing of amyloid precursor protein (APP) by β-secretase and, more specifically, inhibit the production of Aβ-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to β-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
摘要翻译：提供了一系列式（I）的取代的含肟基的酰基胍或立体异构体; 或其无毒的药学上可接受的盐，其中R 1，R 2，R 3，R 4，R R 5，R 6和R 7如本文所定义，其药物组合物和使用方法。这些化合物通过β-分泌酶抑制淀粉样蛋白前体蛋白（APP）的加工，更具体地抑制Aβ-肽的产生。本公开涉及可用于治疗与β-淀粉样蛋白产生相关的神经系统疾病的化合物，例如阿尔茨海默病和受抗淀粉样蛋白活性影响的其它病症。

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