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31. 发明申请

US20050085506A1 Novel gamma secretase inhibitors 失效
标题翻译：新型γ分泌酶抑制剂
公开(公告)号：US20050085506A1
公开(公告)日：2005-04-21
申请号：US10941440
申请日：2004-09-15
申请人： Dmitri Pissarnitski , Hubert Josien , Elizabeth Smith , John Clader , Theodros Asberom , Tao Guo , Douglas Hobbs
发明人： Dmitri Pissarnitski , Hubert Josien , Elizabeth Smith , John Clader , Theodros Asberom , Tao Guo , Douglas Hobbs
IPC分类号： A61K31/445 , C07D211/60 , C07D43/02
CPC分类号： C07D401/14 , C07D211/96 , C07D401/04 , C07D401/12 , C07D405/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D451/06 , C07D471/04 , C07D471/10 , C07D491/10
摘要： This invention discloses novel gamma secretase inhibitors of the formula: wherein: R1 is a substituted aryl or substituted heteroaryl group; R2 is an R1 group, alkyl, —XC(O)Y, alkylene-XC(O)Y, cycloalkylene-X—C(O)—Y, —CH—X—C(O)—NR3—Y or —CH—X—C(O)—Y, wherein X and Y are as defined herein; each R3 and each R3A are independently H, or alkyl; R11 is aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, or alkoxyalkyl. Also disclosed is a method of treating Alzheimer's Disease using one or more compounds of the invention.
摘要翻译：本发明公开了下式的新型γ分泌酶抑制剂：其中：R 1是取代的芳基或取代的杂芳基; R 2是R 1基团，烷基，-XC（O）Y，亚烷基-XC（O）Y，亚环烷基-XC（O）-Y，-CH -XC（O）-NR 3 -Y或-CH-XC（O）-Y，其中X和Y如本文所定义; 每个R 3和R 3各自独立地为H或烷基; R 11是芳基，杂芳基，烷基，环烷基，芳基烷基，芳基环烷基，杂芳基烷基，杂芳基环烷基，芳基杂环烷基或烷氧基烷基。还公开了使用一种或多种本发明化合物治疗阿尔茨海默病的方法。

32. 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。

33. 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。

34. 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。

35. 发明授权

US08666170B2 Computer system and method of matching for images and graphs 有权
标题翻译：计算机系统和匹配图像和图形的方法
公开(公告)号：US08666170B2
公开(公告)日：2014-03-04
申请号：US13030428
申请日：2011-02-18
申请人： Tao Guo
发明人： Tao Guo
IPC分类号： G06K9/62 , G06K9/74 , G06K9/64 , G06K9/32
CPC分类号： G06K9/6212 , G06K9/6204
摘要： It is provided a computer system for matching between images/graphs comprising a processing unit, a storage unit, an input unit and a data recording unit, wherein the computer system includes a feature pattern generating unit for generating a set of feature patterns of the image and the graph from the received image and the received graph, segmenting each of the image and the graph into a plurality of regions centered on a sample point, and determining characteristics of the plurality of regions; a correspondence computing unit for computing correspondence between the image and the graph to be matched by comparing the generated feature patterns; a transform unit for transforming a coordinate system of at least one of the image and the graph to be matched; and a combination unit for combining the image and the graph that have been subjected to the transform of the coordinate system.
摘要翻译：提供了一种用于在包括处理单元，存储单元，输入单元和数据记录单元的图像/图形之间进行匹配的计算机系统，其中计算机系统包括特征图案生成单元，用于生成图像的特征图案集合以及来自接收图像和接收图的曲线图，将图像和图形中的每一个分割成以采样点为中心的多个区域，并且确定多个区域的特征; 对应计算单元，用于通过比较所生成的特征图案来计算图像和要匹配的图形之间的对应关系; 用于变换要匹配的图像和图形中的至少一个的坐标系的变换单元; 以及用于组合已经经过坐标系变换的图像和图形的组合单元。

36. 发明申请

US20140057910A1 HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS 审中-公开
标题翻译：异源ASPARTYL蛋白酶抑制剂
公开(公告)号：US20140057910A1
公开(公告)日：2014-02-27
申请号：US13402521
申请日：2012-02-22
申请人： Zhaoning Zhu , Brian McKittrick , Zhong-Yue Sun , Yuanzan C. Ye , Johannes H. Voight , Corey Strickland , Elizabeth M. Smith , Andrew W. Stamford , William J. Greenlee , Robert Mazzola , John Caldwell , Jared N. Cumming , Lingyan Wang , Yusheng Wu , Ulrich Iserloh , Tao Guo , Thuy X.H. Le , Kurt W. Saionz , Suresh D. Babu , Rachael C. Hunter
发明人： Zhaoning Zhu , Brian McKittrick , Zhong-Yue Sun , Yuanzan C. Ye , Johannes H. Voight , Corey Strickland , Elizabeth M. Smith , Andrew W. Stamford , William J. Greenlee , Robert Mazzola , John Caldwell , Jared N. Cumming , Lingyan Wang , Yusheng Wu , Ulrich Iserloh , Tao Guo , Thuy X.H. Le , Kurt W. Saionz , Suresh D. Babu , Rachael C. Hunter
IPC分类号： A61K31/5377 , A61K31/4168 , C07D405/06 , A61K31/4178 , C07D401/04 , A61K45/06 , A61K31/454 , C07D409/06 , C07D401/06 , C07D295/15 , A61K31/4184 , C07D233/88 , A61K31/4439
CPC分类号： C07D233/88 , A61K31/4168 , A61K31/4178 , A61K31/4184 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4725 , A61K31/5377 , A61K31/655 , A61K45/06 , C07D233/46 , C07D233/70 , C07D235/02 , C07D239/22 , C07D239/70 , C07D271/07 , C07D273/00 , C07D295/15 , C07D401/04 , C07D401/06 , C07D401/08 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/08 , C07D403/10 , C07D403/12 , C07D405/06 , C07D405/10 , C07D405/14 , C07D407/06 , C07D409/04 , C07D409/06 , C07D409/10 , C07D409/14 , C07D413/10 , C07D413/12 , C07D417/06 , Y02A50/411
摘要： Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(═S)—, —S(O)—, —S(O)2—, —C(═O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(═N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(═O)— or —C(═NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(═NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method 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 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W为键，-C（= S） - ， - S（O） - ， - S（O） -C（= O） - ， - O - ， - C（R6）（R7） - ， - N（R5） - 或-C（= N（R5） X是-O - ， - N（R 5） - 或-C（R 6）（R 7） - ; 条件是当X是-O-时，U不是-O-，-S（O） - ， - S（O）2 - ， - C（= O） - 或-C（= NR5） - ; U是一个键，-S（O） - ， - S（O）2 - ， - C（O） - ， - O - ， - O（OR）（C（R6）（R7））b-或-N（R5） - ; 其中b为1或2; 条件是当W是-S（O） - ， - S（O）2 - ， - O-或-N（R 5） - 时，U不是-S（O） - ， - S（O） -O-或-N（R 5） - ; 条件是当X为-N（R5） - 且W为-S（O） - ， - S（O）2 - ， - O-或-N（R5） - 时，则U不为键; 并且R1，R2，R3，R4，R5，R6和R7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，认知和神经变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拮抗剂组合来治疗认知或神经变性疾病的方法。

37. 发明授权

US08359156B2 Map generation system and map generation method by using GPS tracks 有权
标题翻译：使用GPS轨迹的地图生成系统和地图生成方法
公开(公告)号：US08359156B2
公开(公告)日：2013-01-22
申请号：US12068296
申请日：2008-02-05
申请人： Tao Guo , Masashi Koga
发明人： Tao Guo , Masashi Koga
IPC分类号： G06F19/00
CPC分类号： G01C21/32
摘要： A map generation system comprising: a mobile device for acquiring location data of a vehicle and a status of the vehicle at a time of acquisition of the location; and a server for processing the acquired location data of the vehicle. The server comprises an input interface, a first storage unit, a processor and a second storage unit. The server includes a management unit for collecting a plurality of pieces of the track data obtained by a motion of the vehicle, an extraction unit for extracting feature points of the plurality of pieces of the track data on a road from which the plurality of pieces of the track data are collected to calculate a Spline curve satisfying the extracted feature points, and an update unit for adding the calculated Spline curve as a lane central line to the digital road map to update map data.
摘要翻译：一种地图生成系统，包括：在获取所述位置时获取车辆的位置数据和所述车辆的状态的移动装置; 以及用于处理所获取的车辆位置数据的服务器。服务器包括输入接口，第一存储单元，处理器和第二存储单元。服务器包括：管理单元，用于收集通过车辆的运动获得的多条轨道数据;提取单元，用于从道路上提取多条轨迹数据的特征点，该道路上的多条收集轨道数据以计算满足所提取的特征点的样条曲线，以及更新单元，用于将所计算的样条曲线作为车道中心线添加到数字路线图以更新地图数据。

38. 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。

39. 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.

40. 发明申请

US20120130076A1 Synthetic Multimerizing Agents 失效
标题翻译：合成多元化剂
公开(公告)号：US20120130076A1
公开(公告)日：2012-05-24
申请号：US13361082
申请日：2012-01-30
申请人： Dennis A. Holt , Terence P. Keenan , Tao Guo , Edgardo Laborde , Wu Yang
发明人： Dennis A. Holt , Terence P. Keenan , Tao Guo , Edgardo Laborde , Wu Yang
IPC分类号： C07D401/12
CPC分类号： C07D401/14 , C07D207/16 , C07D211/60 , C07D401/12 , C07D405/12
摘要： New compounds are disclosed for multimerizing immunophilins and proteins containing immunophilin or immunophilin-related domains. The compounds are of the formula M-L-Q where M is a synthetic ligand for an FKBP protein.
摘要翻译：公开了用于多聚化免疫亲和素和含有免疫亲和素相关结构域的蛋白质的新化合物。该化合物具有式M-L-Q，其中M是FKBP蛋白质的合成配体。

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