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11. 发明授权

US09150603B2 2′-cyano substituted nucleoside derivatives and methods of use thereof useful for the treatment of viral diseases 有权
标题翻译： 2'-氰基取代的核苷衍生物及其用于治疗病毒性疾病的方法
公开(公告)号：US09150603B2
公开(公告)日：2015-10-06
申请号：US14111688
申请日：2012-04-11
申请人： Vinay Girijavallabhan , F. George Njoroge , Stephane Bogen , Angela Kerekes , Frank Bennett , Ying Huang , Latha Nair , Dmitri Pissarnitski , Vishal Verma , Qun Dang , Ian Davies , David B. Olsen , Andrew Stamford , Joseph P. Vacca
发明人： Vinay Girijavallabhan , F. George Njoroge , Stephane Bogen , Angela Kerekes , Frank Bennett , Ying Huang , Latha Nair , Dmitri Pissarnitski , Vishal Verma , Qun Dang , Ian Davies , David B. Olsen , Andrew Stamford , Joseph P. Vacca
IPC分类号： C07H19/06 , C07H19/20 , C07H19/10 , C07H19/12 , C07H19/16 , C07H19/04 , C07H19/207 , C07H19/11 , C07H19/213 , A61K31/7056 , A61K31/7068 , A61K31/7076 , A61K45/06
CPC分类号： C07H19/16 , A61K31/7056 , A61K31/7068 , A61K31/7076 , A61K45/06 , C07H19/06 , C07H19/10 , C07H19/11 , C07H19/20 , C07H19/207 , C07H19/213 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/395
摘要： The present invention relates to 2′-Cyano Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, R1, R2 and R3 are as defined herein. The present invention also relates to compositions comprising at least one 2′-Cyano Substituted Nucleoside Derivative, and methods of using the 2′-Cyano Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.
摘要翻译：本发明涉及式（I）的2'-氰基取代的核苷衍生物及其药学上可接受的盐，其中B，X，R 1，R 2和R 3如本文所定义。本发明还涉及包含至少一种2'-氰基取代的核苷衍生物的组合物，以及使用2'-氰基取代的核苷衍生物治疗或预防患者HCV感染的方法。

12. 发明授权

US09032368B2 Dynamic configuration system 有权
标题翻译：动态配置系统
公开(公告)号：US09032368B2
公开(公告)日：2015-05-12
申请号：US12771807
申请日：2010-04-30
申请人： Sarabhaiah Polakam , Darin Michael DeFer , John Andres Lozes , Christopher Alan Moore , Peter Anthony Tavormina , Ying Huang
发明人： Sarabhaiah Polakam , Darin Michael DeFer , John Andres Lozes , Christopher Alan Moore , Peter Anthony Tavormina , Ying Huang
IPC分类号： G06F9/44 , G06F9/54
CPC分类号： G06F9/542 , G06F8/70 , G06F2209/543
摘要： Systems and methods are illustrated that relate to a dynamic configuration of rules (e.g., business rules, presentation rules, and the like) in a virtual machine environment. Moreover, the rules may be updated and used with an application that is running on a virtual machine without requiring the virtual machine to be stopped and started (i.e., restarted). Furthermore, aspects of the disclosure describe managing the visibility of dynamic rules to various applications running on the same virtual machine.
摘要翻译：示出了与虚拟机环境中的规则（例如，业务规则，呈现规则等）的动态配置相关的系统和方法。此外，可以更新规则并与虚拟机上运行的应用程序一起使用，而不需要停止并启动虚拟机（即重新启动）。此外，本公开的方面描述了将动态规则的可见性管理到在相同虚拟机上运行的各种应用。

13. 发明申请

US20140206715A1 PREPARATION AND USE OF COMPOUNDS AS PROTEASE INHIBITORS 审中-公开
标题翻译：化合物作为蛋白酶抑制剂的制备和使用
公开(公告)号：US20140206715A1
公开(公告)日：2014-07-24
申请号：US14226338
申请日：2014-03-26
申请人： Andrew W. Stamford , Guoqing Li , William Greenlee , Zhaoning Zhu , Brian McKittrick , Robert Mazzola , Ying Huang , Tao Guo , Thuy X.E. Le , Gang Qian , Yuefei Shao
发明人： Andrew W. Stamford , Guoqing Li , William Greenlee , Zhaoning Zhu , Brian McKittrick , Robert Mazzola , Ying Huang , Tao Guo , Thuy X.E. Le , Gang Qian , Yuefei Shao
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C07D209/44 , C07D487/04
摘要： Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Q is a bond or —N(R5)—; T is a bond, —O—, —C(O)—; S, —N(R5)—, or —C(R6′R7′); U is a bond or —C(R6)(R7)— Y is C or N; Z is C or N; ring A, including variables Y and Z, is a three to nine membered cycloalkyl, cycloalkenyl, heterocyclyl, heterocyclenyl, aryl, and heteroaryl ring having 0 to 4, preferably 0 to 2, heteroatoms independently selected from the group consisting of O, S, N and —N(R)—, wherein ring A is unsubstituted or substituted with 1 to 5 independently selected R1 moieties and/or oxo when ring A is cycloalkyl, cycloalkenyl, heterocyclyl or heterocyclenyl; and R, R1, R2, R3, R4, R5, R6, R6, R7 and R7′ are as defined in the specification; pharmaceutical compositions comprising the compounds of formula I and the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases.
摘要翻译：公开了式I化合物或其立体异构体，互变异构体或其药学上可接受的盐或溶剂合物，其中Q是键或-N（R 5） - ; T是键，-O - ， - C（O） - ; S，-N（R 5） - 或-C（R 6'R 7'）; U是键或-C（R6）（R7）-Y是C或N; Z是C或N; 环A包括变量Y和Z是具有0至4个，优选0至2个杂原子的3至9元环烷基，环烯基，杂环基，杂环烯基，芳基和杂芳基环，其独立地选自O，S， N和-N（R） - ，其中当环A是环烷基，环烯基，杂环基或杂环烯基时，环A是未取代的或被1至5个独立选择的R 1部分和/或氧代取代。并且R，R 1，R 2，R 3，R 4，R 5，R 6，R 6，R 7和R 7'如本说明书中所定义; 包含式I化合物的药物组合物和抑制天冬氨酰蛋白酶的方法，特别是治疗心血管疾病，认知和神经变性疾病的方法。

14. 发明授权

US08722708B2 Substituted isoindolines as aspartyl protease inhibitors 有权
标题翻译：取代的异吲哚啉作为天冬氨酰蛋白酶抑制剂
公开(公告)号：US08722708B2
公开(公告)日：2014-05-13
申请号：US11451065
申请日：2006-06-12
申请人： Andrew Stamford , Guoqing Li , William Greenlee , Zhaoning Zhu , Brian McKittrick , Robert Mazzola , Ying Huang , Tao Guo , Thuy X. H. Le , Gang Qian , Yuefei Shao
发明人： Andrew Stamford , Guoqing Li , William Greenlee , Zhaoning Zhu , Brian McKittrick , Robert Mazzola , Ying Huang , Tao Guo , Thuy X. H. Le , Gang Qian , Yuefei Shao
IPC分类号： C07D487/04 , A61K31/519 , A61K31/4035 , A61K31/4406 , C07D487/14 , A61K31/437 , A61P25/28 , A61P9/00 , A61P31/14
CPC分类号： C07D471/04 , C07D209/44 , C07D487/04
摘要： Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Q is a bond or —N(R5)—; T is a bond, —O—, —C(O)—; S, —N(R5)—, or —C(R6′R7′); U is a bond or —C(R6)(R7)— Y is C or N; Z is C or N; ring A, including variables Y and Z, is a three to nine membered cycloalkyl, cycloalkenyl, heterocyclyl, heterocyclenyl, aryl, and heteroaryl ring having 0 to 4, preferably 0 to 2, heteroatoms independently selected from the group consisting of O, S, N and —N(R)—, wherein ring A is unsubstituted or substituted with 1 to 5 independently selected R1 moieties and/or oxo when ring A is cycloalkyl, cycloalkenyl, heterocyclyl or heterocyclenyl; and R, R1, R2, R3, R4, R5, R6, R6, R7 and R7′ are as defined in the specification; pharmaceutical compositions comprising the compounds of formula I and the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases.
摘要翻译：公开了式I化合物或其立体异构体，互变异构体或其药学上可接受的盐或溶剂合物，其中Q是键或-N（R 5） - ; T是键，-O - ， - C（O） - ; S，-N（R 5） - 或-C（R 6'R 7'）; U是键或-C（R6）（R7）-Y是C或N; Z是C或N; 环A包括变量Y和Z是具有0至4个，优选0至2个杂原子的3至9元环烷基，环烯基，杂环基，杂环烯基，芳基和杂芳基环，其独立地选自O，S， N和-N（R） - ，其中当环A是环烷基，环烯基，杂环基或杂环烯基时，环A是未取代的或被1至5个独立选择的R 1部分和/或氧代取代。并且R，R 1，R 2，R 3，R 4，R 5，R 6，R 6，R 7和R 7'如本说明书中所定义; 包含式I化合物的药物组合物和抑制天冬氨酰蛋白酶的方法，特别是治疗心血管疾病，认知和神经变性疾病的方法。

15. 发明授权

US08691833B2 Heterocyclic aspartyl protease inhibitors 有权
标题翻译：杂环天门冬氨酰蛋白酶抑制剂
公开(公告)号：US08691833B2
公开(公告)日：2014-04-08
申请号：US13415404
申请日：2012-03-08
申请人： Zhaoning Zhu , Brian McKittrick , Zhong-Yue Sun , Yuanzan C. Ye , Johannes H. Voight , Corey O. Strickland , Elizabeth M. Smith , Andrew W. Stamford , William J. Greenlee , Robert D. Mazzola, Jr. , John P. Caldwell , Jared N. Cumming , Lingyan Wang , Yusheng Wu , Ulrich Iserloh , Xiaoiang Liu , Tao Guo , Thuy X.E. Le , Kurt W. Saionz , Suresh D. Babu , Rachael C. Hunter , Michelle L. Morris , Huizhong Gu , Gang Qian , Dawit Tadesse , Ying Huang , Guoqing Li , Jianping Pan , Jeffrey A. Misiaszek , Gaifa Lai , Jingqi Duo , Chuanxing Qu , Yuefei Shao
发明人： Zhaoning Zhu , Brian McKittrick , Zhong-Yue Sun , Yuanzan C. Ye , Johannes H. Voight , Corey O. Strickland , Elizabeth M. Smith , Andrew W. Stamford , William J. Greenlee , Robert D. Mazzola, Jr. , John P. Caldwell , Jared N. Cumming , Lingyan Wang , Yusheng Wu , Ulrich Iserloh , Xiaoiang Liu , Tao Guo , Thuy X.E. Le , Kurt W. Saionz , Suresh D. Babu , Rachael C. Hunter , Michelle L. Morris , Huizhong Gu , Gang Qian , Dawit Tadesse , Ying Huang , Guoqing Li , Jianping Pan , Jeffrey A. Misiaszek , Gaifa Lai , Jingqi Duo , Chuanxing Qu , Yuefei Shao
IPC分类号： A01N43/54 , A61K31/505 , C07D239/02
CPC分类号： C07D233/88 , A61K31/4168 , A61K31/4178 , C07D239/22 , C07D401/06 , C07D401/10 , C07D403/06 , C07D409/04 , C07D409/14 , C07D413/04 , C07D417/10 , C07D417/14 , C07D495/10
摘要： Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein each variable in Formula 1 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.
摘要翻译：公开了式I化合物或其立体异构体，互变异构体或其药学上可接受的盐或溶剂化物，其中式1中的每个变量如说明书中所定义; 以及包含式I化合物的药物组合物。还公开了抑制天冬氨酰蛋白酶的方法，特别是治疗心血管疾病，认知和神经退行性疾病的方法，以及抑制人类免疫缺陷病毒，plasmepins，组织蛋白酶D和原生动物酶。还公开了使用式I化合物与胆碱酯酶抑制剂或毒蕈碱m1激动剂或m2拮抗剂组合治疗认知或神经变性疾病的方法。

16. 发明授权

US08629155B2 Aspartyl protease inhibitors 有权
标题翻译：天冬氨酰蛋白酶抑制剂
公开(公告)号：US08629155B2
公开(公告)日：2014-01-14
申请号：US13421396
申请日：2012-03-15
申请人： Yusheng Wu , Ulrich Iserloh , Jared N. Cumming , Xiaoxiang Liu , Robert D. Mazzola , Zhong-Yue Sun , Ying Huang , Andrew Stamford , Brian McKittrick , Zhaoning Zhu
发明人： Yusheng Wu , Ulrich Iserloh , Jared N. Cumming , Xiaoxiang Liu , Robert D. Mazzola , Zhong-Yue Sun , Ying Huang , Andrew Stamford , Brian McKittrick , Zhaoning Zhu
IPC分类号： C07D239/70 , C07D513/20 , A01N43/54 , A61P31/18 , A61P25/28 , A61P9/00
CPC分类号： C07D239/20 , C07D401/04 , C07D401/10 , C07D403/04 , C07D405/04 , C07D409/14 , C07D411/04 , C07D417/04 , C07D417/14 , C07D495/20
摘要： Disclosed are compounds of formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, U, W, X, R1, R2, R6, R7, R30 and R31 are as described above in the specification. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.
摘要翻译：公开了式I化合物或其立体异构体，互变异构体或其药学上可接受的盐或溶剂合物，U，W，X，R 1，R 2，R 6，R 7，R 30和R 31如上文在说明书中所述。还公开了抑制天冬氨酰蛋白酶的方法，特别是治疗心血管疾病，认知和神经变性疾病的方法。还公开了使用式I化合物与胆碱酯酶抑制剂或毒蕈碱m1激动剂或m2拮抗剂组合治疗认知或神经变性疾病的方法。

17. 发明授权

US08488025B2 Sub-frame tapered reset 有权
标题翻译：子框架锥形复位
公开(公告)号：US08488025B2
公开(公告)日：2013-07-16
申请号：US12582316
申请日：2009-10-20
申请人： Ying Huang , Giuseppe Rossi , Lester Joseph Kozlowski , Laurent Blanquart , Qianjiang Mao , Gregory Chow
发明人： Ying Huang , Giuseppe Rossi , Lester Joseph Kozlowski , Laurent Blanquart , Qianjiang Mao , Gregory Chow
IPC分类号： H04N5/217 , H04N5/335
CPC分类号： H04N5/363 , H04N5/343 , H04N5/3532 , H04N5/374 , H04N5/3765
摘要： Systems and methods are provided that facilitate employing a plurality of independent reset buses for a column of pixels in a pixel array of a CMOS sensor imager. Utilization of the plurality of independent reset buses for the column of pixels can enable independent reset to be effectuated when employing sub-frame integration. For example, rows to be read and reset during a given readout time interval can be selected based upon one or more criteria. Further, each of the rows selected during the given readout time interval can be associated with a respective distinct reset bus. By leveraging the plurality of independent reset buses, uniformity in pixel operation can be maintained whether operating in full frame integration mode or sub-frame integration mode. Thus, noise resultant from changing between integration modes can be mitigated by using the plurality of independent reset buses.
摘要翻译：提供了系统和方法，其便于对CMOS传感器成像器的像素阵列中的像素列采用多个独立的复位总线。对于像素列，多个独立复位总线的利用可以使得在采用子帧集成时能够实现独立的复位。例如，可以基于一个或多个标准来选择在给定的读出时间间隔期间要读取和复位的行。此外，在给定读出时间间隔期间选择的每行都可以与相应的不同的复位总线相关联。通过利用多个独立的复位总线，无论是在全帧集成模式还是子帧集成模式下操作，都可以保持像素操作的均匀性。因此，可以通过使用多个独立复位总线来减轻由积分模式之间变化引起的噪声。

18. 发明授权

US08367712B2 Substituted amide beta secretase inhibitors 有权
标题翻译：取代的酰胺β分泌酶抑制剂
公开(公告)号：US08367712B2
公开(公告)日：2013-02-05
申请号：US12861347
申请日：2010-08-23
申请人： Ying Huang , Guoqing Li , Andrew W. Stamford
发明人： Ying Huang , Guoqing Li , Andrew W. Stamford
IPC分类号： A01N43/50 , A61K31/415
CPC分类号： C07D401/12 , C07D241/04 , C07D241/08 , C07D401/10 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R4 and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I.Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease.Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula I and at least one compound selected from the group consisting of β-secretase inhibitors other than those of formula I, HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.
摘要翻译：公开了下式的新化合物或其药学上可接受的盐或溶剂化物，其中R1，R2，R3，R4和X如说明书中所定义。还公开了包含式I化合物的药物组合物。还公开了治疗认知或神经变性疾病如阿尔茨海默病的方法。还公开了治疗认知或神经退行性疾病的方法，包括向需要这种治疗的患者施用至少一种式I化合物和至少一种选自除了那些的那些之外的其他化合物式I，HMG-CoA还原酶抑制剂，γ-分泌酶抑制剂，非甾体抗炎剂，N-甲基-D-天冬氨酸受体拮抗剂，胆碱酯酶抑制剂和抗淀粉样蛋白抗体。

19. 发明申请

US20130004518A1 CYCLIC AMINE BACE-1 INHIBITORS HAVING A BENZAMIDE SUBSTITUENT 有权
标题翻译：具有苯甲酸替代物的循环胺BACE-1抑制剂
公开(公告)号：US20130004518A1
公开(公告)日：2013-01-03
申请号：US13610162
申请日：2012-09-11
申请人： Jared N. Cumming , Ulrich Iserloh , Andrew Stamford , Corey Strickland , Johannes H. Voight , Yusheng Wu , Ying Huang , Yan Xia , Samuel Chackalamannil , Tao Guo , Douglas W. Hobbs , Thuy X.H. Le , Jeffrey F. Lowrie , Kurt W. Saionz , Suresh D. Babu
发明人： Jared N. Cumming , Ulrich Iserloh , Andrew Stamford , Corey Strickland , Johannes H. Voight , Yusheng Wu , Ying Huang , Yan Xia , Samuel Chackalamannil , Tao Guo , Douglas W. Hobbs , Thuy X.H. Le , Jeffrey F. Lowrie , Kurt W. Saionz , Suresh D. Babu
IPC分类号： C07D207/09 , C07F9/572 , A61K31/675 , C07D217/18 , A61K31/472 , C07F9/62 , C07D207/12 , A61K31/4025 , C07D401/14 , A61K31/4439 , C07D205/04 , A61K31/397 , C07D211/26 , A61K31/4458 , C07D211/46 , A61K31/445 , C07D413/12 , A61K31/5377 , C07D401/12 , A61K31/454 , C07D401/04 , A61K31/451 , A61K31/4545 , C07D241/08 , A61K31/495 , C07D403/12 , A61K31/496 , C07D241/24 , C07D413/06 , C07D243/08 , A61K31/551 , A61K39/395 , A61K31/5415 , A61K31/505 , A61P25/00 , A61P25/28 , A61P29/00 , A61K31/40
CPC分类号： C07D243/08 , C07D205/04 , C07D207/08 , C07D207/09 , C07D207/12 , C07D207/26 , C07D209/52 , C07D211/26 , C07D211/46 , C07D217/18 , C07D233/32 , C07D241/04 , C07D241/08 , C07D401/06 , C07D401/10 , C07D401/12 , C07D403/12 , C07D403/14 , C07D409/06 , C07D409/12 , C07D413/06
摘要： Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, whereinR1 is R is —C(O)—N(R27)(R28) or and the remaining variables are as defined in the specification.Also disclosed are pharmaceutical compositions comprising the compounds of formula I.Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease.Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a β-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.
摘要翻译：公开了下式的化合物或其药学上可接受的盐或溶剂化物，其中R1是R是-C（O）-N（R27）（R28），或其余的变量如说明书中所定义。还公开了包含式I化合物的药物组合物。还公开了治疗认知或神经变性疾病如阿尔茨海默病的方法。还公开了治疗认知或神经变性疾病的药物组合物和方法，其包含式I化合物与除式I以外的分泌抑制剂抑制剂，HMG-CoA还原酶抑制剂，γ-分泌酶抑制剂，非 - 甾族抗炎药，N-甲基-D-天冬氨酸受体拮抗剂，胆碱酯酶抑制剂或抗淀粉样蛋白抗体。

20. 发明申请

US20120231017A1 HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS 有权
公开(公告)号：US20120231017A1
公开(公告)日：2012-09-13
申请号：US13415404
申请日：2012-03-08
申请人： ZHAONING ZHU , Brian McKittrick , Zhong-Yue Sun , Yuanzan C. Ye , Johannes H. Voigt , Corey O. Strickland , Elizabeth M. Smith , Andrew Stamford , William J. Greenlee , Robert D. Mozzola , John P. Caldwell , Jared N. Cumming , Lingyan Wang , Yusheng Wu , Ulrich Iserloh , Xiaoiang Liu , Tao Guo , Thuy X. E. Le , Kurt W. Sainoz , Suresh D. Babu , Rachael C. Hunter , Michelle L. Morris , Huizhong Gu , Gang Qian , Dawit Tadesse , Ying Huang , Guoqing Li , Jianping Pan , Jeffrey A. Misiaszek , Gaifa Lai , Jingqi Duo , Chuanxing Qu , Yuefei Shao
发明人： ZHAONING ZHU , Brian McKittrick , Zhong-Yue Sun , Yuanzan C. Ye , Johannes H. Voigt , Corey O. Strickland , Elizabeth M. Smith , Andrew Stamford , William J. Greenlee , Robert D. Mozzola , John P. Caldwell , Jared N. Cumming , Lingyan Wang , Yusheng Wu , Ulrich Iserloh , Xiaoiang Liu , Tao Guo , Thuy X. E. Le , Kurt W. Sainoz , Suresh D. Babu , Rachael C. Hunter , Michelle L. Morris , Huizhong Gu , Gang Qian , Dawit Tadesse , Ying Huang , Guoqing Li , Jianping Pan , Jeffrey A. Misiaszek , Gaifa Lai , Jingqi Duo , Chuanxing Qu , Yuefei Shao
IPC分类号： A61K39/395 , C07D239/70 , C07F5/02 , C07D403/10 , A61K31/513 , A61K31/506 , C07D409/04 , C07D409/14 , C07D401/04 , C07D405/14 , C07D417/14 , C07D417/04 , C07D413/14 , C07D413/10 , A61K31/5377 , A61P29/00 , A61P9/00 , A61P25/28 , A61P31/10 , A61P33/02 , C07D495/04 , A61P25/00 , A61P31/04 , C07D239/22
CPC分类号： C07D233/88 , A61K31/4168 , A61K31/4178 , C07D239/22 , C07D401/06 , C07D401/10 , C07D403/06 , C07D409/04 , C07D409/14 , C07D413/04 , C07D417/10 , C07D417/14 , C07D495/10
摘要： Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein each variable in Formula 1 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.

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