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91. 发明授权

US08937093B2 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：US08937093B2
公开(公告)日：2015-01-20
申请号：US13402521
申请日：2012-02-22
申请人： Kurt W. Saionz , Tao Guo , Andrew W. Stamford , Zhaoning Zhu
发明人： Kurt W. Saionz , Tao Guo , Andrew W. Stamford , Zhaoning Zhu
IPC分类号： A61K31/4245 , C07D271/07 , A61K31/5377 , C07D233/46 , C07D233/70 , C07D233/88 , C07D239/22 , C07D239/70 , C07D273/00 , C07D401/04 , C07D401/08 , C07D401/10 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/08 , C07D403/10 , C07D403/12 , C07D405/10 , C07D409/04 , C07D409/10 , C07D409/14 , C07D413/10 , C07D413/12 , C07D417/06 , A61K31/4168 , A61K31/4178 , A61K31/4184 , A61K31/4439 , A61K31/454 , A61K45/06 , C07D295/15 , C07D401/06 , C07D405/06 , C07D409/06
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, X, U, R1, R2, R3, and R4, are as defined herein, 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合物，其中W，X，U，R 1，R 2，R 3和R 4如本文所定义，以及包含式 I.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拮抗剂组合来治疗认知或神经变性疾病的方法。

92. 发明授权

US08809318B2 Gamma secretase modulators 有权
标题翻译：伽玛分泌酶调节剂
公开(公告)号：US08809318B2
公开(公告)日：2014-08-19
申请号：US13128316
申请日：2009-11-11
申请人： Zhaoning Zhu , William J. Greenlee , Hongmei Li , Monica L. Vicarel , Jun Qin , Pawan Kumar Dhondi , Xianhai Huang , Anandan Palani , Xiaoxiang Liu , Zhong-Yue Sun , Hubert B. Josien , Ruo Xu , David James Cole , Duane A. Burnett , Chad E. Bennett , Troy McCracken , Malcolm MacCoss
发明人： Zhaoning Zhu , William J. Greenlee , Hongmei Li , Monica L. Vicarel , Jun Qin , Pawan Kumar Dhondi , Xianhai Huang , Anandan Palani , Xiaoxiang Liu , Zhong-Yue Sun , Hubert B. Josien , Ruo Xu , David James Cole , Duane A. Burnett , Chad E. Bennett , Troy McCracken , Malcolm MacCoss
IPC分类号： A61K31/553 , C07D498/04 , C07D498/14 , C07D498/20
CPC分类号： C07D498/04 , C07D409/14 , C07D413/10 , C07D498/14 , C07D498/20
摘要： In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more disease associated with the central nervous system using such compounds or pharmaceutical compostions.
摘要翻译：在其许多实施方案中，本发明提供了一类新颖的下式杂环化合物：作为γ-分泌酶的调节剂，制备此类化合物的方法，含有一种或多种此类化合物的药物组合物，制备包含一种或多种这样的化合物的药物制剂的方法化合物，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与中枢神经系统相关的一种或多种疾病的方法。

93. 发明授权

US08557798B2 Macrocyclic heterocyclic aspartyl protease inhibitors 有权
标题翻译：大环杂环天门冬酰胺蛋白酶抑制剂
公开(公告)号：US08557798B2
公开(公告)日：2013-10-15
申请号：US12620291
申请日：2009-11-17
申请人： Ulrich Iserloh , Zhaoning Zhu , Andrew Stamford , Johannes H. Voigt
发明人： Ulrich Iserloh , Zhaoning Zhu , Andrew Stamford , Johannes H. Voigt
IPC分类号： A61K31/33 , C07D245/00
CPC分类号： C07D487/08
摘要： Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt, solvate or ester thereof, wherein U, W, X, L, Y, M, Z, c, d, e, f, g, h, s, t, R1, R2, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17 and R18 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. 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，溶剂化物或酯，其中U，W，X，L，Y，M，Z，c，d，e，f，g， s，t，R1，R2，R7，R8，R9，R10，R11，R12，R13，R14，R15，R16，R17和R18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。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。

94. 发明授权

US08450331B2 Thiophenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as BACE-1 inhibitors, compositions, and their use 有权
标题翻译：噻吩基取代的2-亚氨基-3-甲基吡咯并嘧啶酮化合物作为BACE-1抑制剂，组合物及其用途
公开(公告)号：US08450331B2
公开(公告)日：2013-05-28
申请号：US12988464
申请日：2009-04-21
申请人： Zhaoning Zhu , Andrew Stamford , Mihirbaran Mandal , Xiaoxiang Liu
发明人： Zhaoning Zhu , Andrew Stamford , Mihirbaran Mandal , Xiaoxiang Liu
IPC分类号： C07D487/04 , A61K31/519 , A61P25/28 , A61P3/10
CPC分类号： C07D487/04
摘要： In its many embodiments, the present invention provides certain thiophenyl-substituted 2-imino-3-methyl pyrrolo pyrimidone compounds, including compounds (or tautomers or a pharmaceutically acceptable salts thereof) having the structural Formula (III): wherein R2, R3, R4, R5, R6, R7, R8, and R9 are each selected independently and as defined herein. Pharmaceutical compositions comprising one or more such compounds, and methods for their preparation and use in treating pathologies associated with amyloid beta (Aβ) protein, including Alzheimer's Disease, are also disclosed.
摘要翻译：在其许多实施方案中，本发明提供了具有结构式（III）的化合物（或其互变异构体或其药学上可接受的盐）的某些噻吩基取代的2-亚氨基-3-甲基吡咯烷酮化合物：其中R2，R3，R4 ，R 5，R 6，R 7，R 8和R 9各自独立地并如本文所定义。还公开了包含一种或多种这样的化合物的药物组合物，及其制备和用于治疗与包括阿尔茨海默病在内的淀粉样蛋白β（Abeta）蛋白相关的病理学的方法。

95. 发明授权

US08357682B2 Gamma secretase modulators 有权
标题翻译：伽玛分泌酶调节剂
公开(公告)号：US08357682B2
公开(公告)日：2013-01-22
申请号：US12598704
申请日：2008-05-05
申请人： Zhaoning Zhu , William J. Greenlee , Zhong-Yue Sun , Gioconda Gallo , Theodros Asberom , Xianhai Huang , Xiaohong Zhu , Mark D. McBriar , Dmitri A. Pissarnitski , Zhiqiang Zhao , Ruo Xu , Hongmei Li , Anandan Palani , Johannes H. Voigt , Robert D. Mazzola, Jr. , John Clader , Hubert Josien , Jun Qin
发明人： Zhaoning Zhu , William J. Greenlee , Zhong-Yue Sun , Gioconda Gallo , Theodros Asberom , Xianhai Huang , Xiaohong Zhu , Mark D. McBriar , Dmitri A. Pissarnitski , Zhiqiang Zhao , Ruo Xu , Hongmei Li , Anandan Palani , Johannes H. Voigt , Robert D. Mazzola, Jr. , John Clader , Hubert Josien , Jun Qin
IPC分类号： C07D413/10 , C07D413/14 , C07D498/10 , A61K31/395 , A61K31/4245 , A61K31/4439
CPC分类号： C07D413/10 , C07D413/14 , C07D498/04 , C07D498/10 , C07D498/20
摘要： The present invention provides a novel class of heterocyclic compounds of Formula (I) as modulators of gamma secretase, wherein the definitions of the variables of Formula (I) are defined herein, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
摘要翻译：本发明提供了一类新颖的式（I）杂环化合物作为γ-分泌酶的调节剂，其中式（I）变量的定义在本文中定义，制备此类化合物的方法，含有一种或多种此类化合物的药物组合物制备包含一种或多种此类化合物的药物制剂的方法，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与中枢神经系统相关的一种或多种疾病的方法。

96. 发明申请

US20120232064A1 ASPARTYL PROTEASE INHIBITORS 有权
标题翻译： ASPARTYL PROTEASE抑制剂
公开(公告)号：US20120232064A1
公开(公告)日：2012-09-13
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： A61K31/506 , C07D403/04 , A61K31/497 , A61P29/00 , A61K31/551 , A61P9/00 , A61P25/28 , C07D409/14 , C07D401/04
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。

97. 发明授权

US08202854B2 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：US08202854B2
公开(公告)日：2012-06-19
申请号：US13191978
申请日：2011-07-27
申请人： Zhaoning Zhu , Andrew W. Stamford , Brian McKittrick
发明人： Zhaoning Zhu , Andrew W. Stamford , Brian McKittrick
IPC分类号： C07D409/04 , C07D487/04 , C07D498/04 , A61K31/395
CPC分类号： C07D409/04 , C07D487/04
摘要： Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Ar, R1, R2, R3, R4 and R5 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. 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Ar，R 1，R 2，R 3，R 4和R 5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。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。

98. 发明申请

US20100298359A1 GAMMA SECRETASE MODULATORS 审中-公开
标题翻译： GAMMA秘密调节器
公开(公告)号：US20100298359A1
公开(公告)日：2010-11-25
申请号：US12746313
申请日：2008-12-04
申请人： Xianhai Huang , Anandan Palani , Jun Qin , Robert Aslanian , Zhaoning Zhu , William Greenlee
发明人： Xianhai Huang , Anandan Palani , Jun Qin , Robert Aslanian , Zhaoning Zhu , William Greenlee
IPC分类号： A61K31/517 , C07D401/10 , A61K31/4725 , A61P29/00 , A61K39/395 , A61P25/28 , C07D403/10
CPC分类号： C07D471/04 , C07D401/10 , C07D403/10 , C07D491/04 , C07D498/04
摘要： This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I) wherein R2 is a fused bicyclic ring of the formula (II). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's disease using the compounds of formula (I).
摘要翻译：本发明提供了作为γ分泌酶调节剂的新型化合物。所述化合物具有式（I），其中R 2是式（II）的稠合双环。还公开了使用式（I）的化合物调节γ-分泌酶活性和治疗阿尔茨海默病的方法的方法。

99. 发明申请

US20100292203A1 HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS 有权
公开(公告)号：US20100292203A1
公开(公告)日：2010-11-18
申请号：US12693874
申请日：2010-01-26
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. Mazzola , John P. Caldwell , Jared N. Cumming , Lingyan Wang , Yusheng Wu , Ulrich Iserloh , Xiaoxiang Liu , Dawit Tadesse , Ying Huang , Guoqing Li , Jianping Pan
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. Mazzola , John P. Caldwell , Jared N. Cumming , Lingyan Wang , Yusheng Wu , Ulrich Iserloh , Xiaoxiang Liu , Dawit Tadesse , Ying Huang , Guoqing Li , Jianping Pan
IPC分类号： A61K31/505 , C07D239/22 , A61K31/55 , A61K31/397
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 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 m1 agonist or m2 antagonist.

100. 发明授权

US07812013B2 Macrocyclic heterocyclic aspartyl protease inhibitors 有权
标题翻译：大环杂环天门冬酰胺蛋白酶抑制剂
公开(公告)号：US07812013B2
公开(公告)日：2010-10-12
申请号：US11451064
申请日：2006-06-12
申请人： Ulrich Iserloh , Zhaoning Zhu , Andrew Stamford , Johannes H. Voigt
发明人： Ulrich Iserloh , Zhaoning Zhu , Andrew Stamford , Johannes H. Voigt
IPC分类号： A01N43/00 , A61K31/33 , C07D498/00
CPC分类号： C07D487/08
摘要： Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt, solvate or ester thereof, wherein U, W, X, L, Y, M, Z, c, d, e, f, g, h, s, t, R1, R2, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17 and R18 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. 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，溶剂化物或酯，其中U，W，X，L，Y，M，Z，c，d，e，f，g， s，t，R1，R2，R7，R8，R9，R10，R11，R12，R13，R14，R15，R16，R17和R18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。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。

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