公开(公告)号：US08741884B2

公开(公告)日：2014-06-03

申请号：US13086704

申请日：2011-04-14

申请人： Tao Wang ,  Zhiwei Yin ,  Zhongxing Zhang ,  Annapurna Pendri ,  Guo Li ,  Samuel Gerritz ,  Weixu Zhai ,  Paul Michael Scola ,  Li-Qiang Sun ,  Eric Mull

发明人： Tao Wang ,  Zhiwei Yin ,  Zhongxing Zhang ,  Annapurna Pendri ,  Guo Li ,  Samuel Gerritz ,  Weixu Zhai ,  Paul Michael Scola ,  Li-Qiang Sun ,  Eric Mull

IPC分类号： A61K31/33 ,  C07D487/00

CPC分类号： C07D498/06

摘要： The disclosure provides compounds of formula I, including pharmaceutically acceptable salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.

公开(公告)号：US20120093767A1

公开(公告)日：2012-04-19

申请号：US13086704

申请日：2011-04-14

申请人： Tao Wang ,  Zhiwei Yin ,  Zhongxing Zhang ,  Annapurna Pendri ,  Guo Li ,  Samuel Gerritz ,  Weixu Zhai ,  Paul Michael Scola ,  Li-Qiang Sun ,  Eric Mull

发明人： Tao Wang ,  Zhiwei Yin ,  Zhongxing Zhang ,  Annapurna Pendri ,  Guo Li ,  Samuel Gerritz ,  Weixu Zhai ,  Paul Michael Scola ,  Li-Qiang Sun ,  Eric Mull

IPC分类号： A61K38/20 ,  C07D487/08 ,  A61P31/14 ,  A61K38/21 ,  A61K38/13 ,  C07D498/08 ,  A61K31/53

CPC分类号： C07D498/06

摘要： The disclosure provides compounds of formula I, including pharmaceutically acceptable salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.

公开(公告)号：US08445490B2

公开(公告)日：2013-05-21

申请号：US13086036

申请日：2011-04-13

申请人： Tao Wang ,  Annapurna Pendri ,  Zhongxing Zhang ,  Weixu Zhai ,  Guo Li ,  Samuel Gerritz ,  Paul Michael Scola ,  Li-Qiang Sun ,  Qian Zhao ,  Eric Mull

发明人： Tao Wang ,  Annapurna Pendri ,  Zhongxing Zhang ,  Weixu Zhai ,  Guo Li ,  Samuel Gerritz ,  Paul Michael Scola ,  Li-Qiang Sun ,  Qian Zhao ,  Eric Mull

IPC分类号： A61K31/53 ,  C07D251/18

CPC分类号： C07D487/08 ,  C07D498/08

摘要： The disclosure provides compounds of formula I, including pharmaceutically acceptable salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.

公开(公告)号：US08586584B2

公开(公告)日：2013-11-19

申请号：US12904264

申请日：2010-10-14

申请人： Tao Wang ,  Annapurna Pendri ,  Zhongxing Zhang ,  Weixu Zhai ,  Guo Li ,  Samuel Gerritz ,  Paul Michael Scola ,  Li-Qiang Sun ,  Qian Zhao ,  Eric Mull

发明人： Tao Wang ,  Annapurna Pendri ,  Zhongxing Zhang ,  Weixu Zhai ,  Guo Li ,  Samuel Gerritz ,  Paul Michael Scola ,  Li-Qiang Sun ,  Qian Zhao ,  Eric Mull

IPC分类号： A61K31/53 ,  C07D251/72 ,  C07D487/00

CPC分类号： C07D487/08 ,  C07D498/08

摘要： The disclosure provides compounds of formula I, including pharmaceutically acceptable salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.

公开(公告)号：US20120093766A1

公开(公告)日：2012-04-19

申请号：US13086036

申请日：2011-04-13

申请人： Tao Wang ,  Annapurna Pendri ,  Zhongxing Zhang ,  Weixu Zhai ,  Guo Li ,  Samuel Gerritz ,  Paul Michael Scola ,  Li-Qiang Sun ,  Qian Zhao ,  Eric Mull

发明人： Tao Wang ,  Annapurna Pendri ,  Zhongxing Zhang ,  Weixu Zhai ,  Guo Li ,  Samuel Gerritz ,  Paul Michael Scola ,  Li-Qiang Sun ,  Qian Zhao ,  Eric Mull

IPC分类号： A61K31/53 ,  C07D498/08 ,  A61K38/13 ,  A61K38/20 ,  A61P31/14 ,  C07D487/08 ,  A61K38/21

CPC分类号： C07D487/08 ,  C07D498/08

摘要： The disclosure provides compounds of formula I, including pharmaceutically acceptable salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.

公开(公告)号：US20110086858A1

公开(公告)日：2011-04-14

申请号：US12904264

申请日：2010-10-14

申请人： Tao Wang ,  Annapurna Pendri ,  Zhongxing Zhang ,  Weixu Zhai ,  Guo Li ,  Samuel Gerritz ,  Paul Michael Scola ,  Li-Qiang Sun ,  Qian Zhao ,  Eric Mull

发明人： Tao Wang ,  Annapurna Pendri ,  Zhongxing Zhang ,  Weixu Zhai ,  Guo Li ,  Samuel Gerritz ,  Paul Michael Scola ,  Li-Qiang Sun ,  Qian Zhao ,  Eric Mull

IPC分类号： A61K31/53 ,  C07D245/00 ,  C07D267/00 ,  A61P31/14

CPC分类号： C07D487/08 ,  C07D498/08

摘要： The disclosure provides compounds of formula I, including pharmaceutically acceptable salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.

摘要翻译： 本公开提供式I化合物，包括药学上可接受的盐，以及使用该化合物的组合物和方法。 该化合物具有抗丙型肝炎病毒（HCV）的活性，可用于治疗HCV感染者。

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。

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。

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。

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。