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公开(公告)号:US20080021019A1
公开(公告)日:2008-01-24
申请号:US11729020
申请日:2007-03-28
申请人: Tin-Yau Chan , Brian McKittrick , Haiyan Pu , Liwu Hong , Andrew Prongay , Li Xiao , Mark McCoy
发明人: Tin-Yau Chan , Brian McKittrick , Haiyan Pu , Liwu Hong , Andrew Prongay , Li Xiao , Mark McCoy
IPC分类号: A61K31/496 , A61K31/497 , A61K31/551 , A61P11/00 , A61P25/16 , A61P25/28 , A61P3/00 , A61P3/10 , A61P35/00 , A61P37/04 , C07D241/04 , C07D241/20 , C07D243/08
CPC分类号: C07D403/14 , C07D401/14 , C07D403/04
摘要: Disclosed is a compound of the formula: and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating protein kinase mediated diseases using the compound of formula 1.0. Also disclosed are methods of treating cancer using a compound of formula 1.0. The disclosed methods also include combination therapies wherein the compound of formula 1.0 is administered in combination with at least one addition pharmaceutically active ingredient.
摘要翻译: 公开了下式的化合物及其药学上可接受的盐。 还公开了使用式1.0化合物治疗蛋白激酶介导的疾病的方法。 还公开了使用式1.0化合物治疗癌症的方法。 所公开的方法还包括联合治疗,其中式1.0化合物与至少一种加成药物活性成分组合施用。
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公开(公告)号:US20080004257A1
公开(公告)日:2008-01-03
申请号:US11338501
申请日:2006-01-24
申请人: Tin-Yau Chan , Thierry Fischmann , Mark McCoy , Brian McKittrick , Andrew Prongay , Haiyan Pu , Li Wang , Li Xiao
发明人: Tin-Yau Chan , Thierry Fischmann , Mark McCoy , Brian McKittrick , Andrew Prongay , Haiyan Pu , Li Wang , Li Xiao
IPC分类号: A61K31/53 , A61K31/551 , A61P25/00 , A61P3/00 , A61P35/00 , A61P37/00 , A61P5/00 , A61P9/00 , C07D403/14
CPC分类号: C07D403/04
摘要: A compound having the general structure of Formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, are useful in treating diseases, disorders, or conditions such as immunodeficiencies, cancers, cardiovascular diseases, endocrine disorders, Parkinson's disease, metabolic diseases, tumorigenesis, Alzheimer's disease, heart disease, diabetes, neurodegeneration, inflammation, kidney disease, atherosclerosis and airway disease.
摘要翻译: 具有式(I)的通式结构的化合物或其药学上可接受的盐,溶剂化物或酯可用于治疗疾病,病症或病症,例如免疫缺陷,癌症,心血管疾病,内分泌紊乱,帕金森病,代谢 疾病,肿瘤发生,阿尔茨海默病,心脏病,糖尿病,神经变性,炎症,肾脏疾病,动脉粥样硬化和气道疾病。
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公开(公告)号:US20080076750A1
公开(公告)日:2008-03-27
申请号:US11854738
申请日:2007-09-13
申请人: Robert Aslanian , Tin-Yau Chan , Joel Harris , Brian McKittrick , Bernard Neustadt , Anandan Palani , Tony Priestley , Elizabeth Smith , Andrew Stamford , Henry Vaccaro , Dong Xiao
发明人: Robert Aslanian , Tin-Yau Chan , Joel Harris , Brian McKittrick , Bernard Neustadt , Anandan Palani , Tony Priestley , Elizabeth Smith , Andrew Stamford , Henry Vaccaro , Dong Xiao
IPC分类号: A61K31/397 , A61P25/04 , A61P3/00
CPC分类号: A61K31/4427 , C07D471/10 , C07D519/00
摘要: The present invention relates to methods for treating or preventing a disorder of lipid metabolism, pain, diabetes, a vascular condition, demyelination or nonalcoholic fatty liver disease, comprising administering a compound having the formula or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof, wherein: R1 and R2 are defined in Tables 1-6 herein, and R3 is -phenyl, -4-chlorophenyl, -2-pyridyl, or -3-pyridyl.
摘要翻译: 本发明涉及治疗或预防脂质代谢紊乱,疼痛,糖尿病,血管病症,脱髓鞘或非酒精性脂肪性肝病的方法,包括给予具有下式的化合物或其药学上可接受的盐,溶剂合物,酯,前药或 其中:R 1和R 2在本文的表1-6中定义,R 3是 - 苯基, 氯苯基,-2-吡啶基或-3-吡啶基。
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公开(公告)号:US20080076751A1
公开(公告)日:2008-03-27
申请号:US11854754
申请日:2007-09-13
申请人: Robert Aslanian , Chad Bennett , Duane Burnett , Tin-Yau Chan , Eugenia Kiselgof , Chad Knutson , Joel Harris , Brian McKittrick , Anandan Palani , Elizabeth Smith , Henry Vaccaro , Dong Xiao , Hyunjin Kim
发明人: Robert Aslanian , Chad Bennett , Duane Burnett , Tin-Yau Chan , Eugenia Kiselgof , Chad Knutson , Joel Harris , Brian McKittrick , Anandan Palani , Elizabeth Smith , Henry Vaccaro , Dong Xiao , Hyunjin Kim
IPC分类号: A61K31/397 , A61P25/04 , A61P3/00 , C07D471/10
CPC分类号: C07D471/10
摘要: The present invention relates to Azetidinone Derivatives, compositions comprising an Azetidinone Derivative and methods for treating or preventing a disorder of lipid metabolism, pain, diabetes, a vascular condition, demyelination or nonalcoholic fatty liver disease, comprising administering to a patient an effective amount of an Azetidinone Derivative.
摘要翻译: 本发明涉及氮杂环丁酮衍生物,包含氮杂环丁酮衍生物的组合物和用于治疗或预防脂质代谢紊乱,疼痛,糖尿病,血管病症,脱髓鞘或非酒精性脂肪性肝病的方法,包括向患者施用有效量的 氮杂环丁酮衍生物。
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公开(公告)号:US07652020B2
公开(公告)日:2010-01-26
申请号:US11142601
申请日:2005-06-01
申请人: Zhuyan Guo , Peter Orth , Zhaoning Zhu , Robert D. Mazzola , Tin-Yau Chan , Henry A. Vaccaro , Brian McKittrick , Joseph A. Kozlowski , Brian J. Lavey , Guowei Zhou , Sunil Paliwal , Shing-Chun Wong , Neng-Yang Shih , Pauline C. Ting , Kristin E. Rosner , Gerald W. Shipps, Jr. , M. Arshad Siddiqui , David B. Belanger , Chaoyang Dai , Dansu Li , Vinay M. Girijavallabhan , Janeta Popovici-Muller , Wensheng Yu , Lianyun Zhao
发明人: Zhuyan Guo , Peter Orth , Zhaoning Zhu , Robert D. Mazzola , Tin-Yau Chan , Henry A. Vaccaro , Brian McKittrick , Joseph A. Kozlowski , Brian J. Lavey , Guowei Zhou , Sunil Paliwal , Shing-Chun Wong , Neng-Yang Shih , Pauline C. Ting , Kristin E. Rosner , Gerald W. Shipps, Jr. , M. Arshad Siddiqui , David B. Belanger , Chaoyang Dai , Dansu Li , Vinay M. Girijavallabhan , Janeta Popovici-Muller , Wensheng Yu , Lianyun Zhao
IPC分类号: A61K31/519 , A61K31/506 , A61K31/4709 , A61K31/43 , A61K31/4245 , C07D413/00 , C07D241/36 , C07D471/00 , C07D295/00 , C07D471/02 , C07D401/00 , C07D513/00 , C07D277/22 , C07D277/62 , C07D263/30 , C07D261/06 , C07D235/00 , C07D209/04 , C07D207/00 , C07D205/00 , C07D409/00 , C07D307/00
CPC分类号: C07D409/14 , C07C235/06 , C07C235/08 , C07C235/10 , C07C2601/08 , C07D207/20 , C07D207/26 , C07D209/44 , C07D215/14 , C07D217/06 , C07D263/32 , C07D295/185 , C07D307/52 , C07D333/20 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D513/04
摘要: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, TNF-α or combinations thereof.
摘要翻译: 本发明涉及式(I)化合物或其药学上可接受的盐,溶剂合物或异构体,其可用于治疗由MMP,ADAM,TACE,TNF-α或其组合介导的疾病或病症。
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公开(公告)号:US20100145048A1
公开(公告)日:2010-06-10
申请号:US12582341
申请日:2009-10-20
申请人: Zhuyan Guo , Peter Orth , Zhaoning Zhu , Robert D. Mazzola , Tin-Yau Chan , Henry A. Vaccaro , Brian McKittrick , Joseph A. Kozlowski , Brian J. Lavey , Guowei Zhou , Sunil Paliwal , Shing-Chun Wong , Neng-Yang Shih , Pauline C. Ting , Kristin E. Rosner , Gerald W. Shipps, JR. , M. Arshad Siddiqui , David B. Belanger , Chaoyang Dai , Dansu Li , Vinay M. Girijavallabhan , Janeta Popovici-Muller , Wensheng Yu , Lianyun Zhao
发明人: Zhuyan Guo , Peter Orth , Zhaoning Zhu , Robert D. Mazzola , Tin-Yau Chan , Henry A. Vaccaro , Brian McKittrick , Joseph A. Kozlowski , Brian J. Lavey , Guowei Zhou , Sunil Paliwal , Shing-Chun Wong , Neng-Yang Shih , Pauline C. Ting , Kristin E. Rosner , Gerald W. Shipps, JR. , M. Arshad Siddiqui , David B. Belanger , Chaoyang Dai , Dansu Li , Vinay M. Girijavallabhan , Janeta Popovici-Muller , Wensheng Yu , Lianyun Zhao
IPC分类号: C07D405/12 , C07D417/12 , C07D413/14 , C07D409/12
CPC分类号: C07D409/14 , C07C235/06 , C07C235/08 , C07C235/10 , C07C2601/08 , C07D207/20 , C07D207/26 , C07D209/44 , C07D215/14 , C07D217/06 , C07D263/32 , C07D295/185 , C07D307/52 , C07D333/20 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D513/04
摘要: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, TNF-α or combinations thereof.
摘要翻译: 本发明涉及式(I)化合物或其药学上可接受的盐,溶剂合物或异构体,其可用于治疗由MMP,ADAM,TACE,TNF-α或其组合介导的疾病或病症。
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公开(公告)号:US20060252778A1
公开(公告)日:2006-11-09
申请号:US11142601
申请日:2005-06-01
申请人: Zhuyan Guo , Peter Orth , Zhaoning Zhu , Robert Mazzola , Tin-Yau Chan , Henry Vaccaro , Brian McKittrick , Joseph Kozlowski , Brian Lavey , Guowei Zhou , Sunil Paliwal , Shing-Chun Wong , Neng-Yang Shih , Pauline Ting , Kristin Rosner , Gerald Shipps , M. Siddiqui , David Belanger , Chaoyang Dai , Dansu Li , Vinay Girijavallabhan , Janeta Popovici-Muller , Wensheng Yu , Lianyun Zhao
发明人: Zhuyan Guo , Peter Orth , Zhaoning Zhu , Robert Mazzola , Tin-Yau Chan , Henry Vaccaro , Brian McKittrick , Joseph Kozlowski , Brian Lavey , Guowei Zhou , Sunil Paliwal , Shing-Chun Wong , Neng-Yang Shih , Pauline Ting , Kristin Rosner , Gerald Shipps , M. Siddiqui , David Belanger , Chaoyang Dai , Dansu Li , Vinay Girijavallabhan , Janeta Popovici-Muller , Wensheng Yu , Lianyun Zhao
IPC分类号: C07D471/02 , C07D498/02 , A61K31/519 , A61K31/506 , A61K31/4709 , A61K31/43 , A61K31/4245
CPC分类号: C07D409/14 , C07C235/06 , C07C235/08 , C07C235/10 , C07C2601/08 , C07D207/20 , C07D207/26 , C07D209/44 , C07D215/14 , C07D217/06 , C07D263/32 , C07D295/185 , C07D307/52 , C07D333/20 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D513/04
摘要: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, TNF-α or combinations thereof.
摘要翻译: 本发明涉及式(I)化合物或其药学上可接受的盐,溶剂化物或异构体,其可用于治疗由MMP,ADAM,TACE,TNF-α或其组合介导的疾病或病症。
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公开(公告)号:US08178513B2
公开(公告)日:2012-05-15
申请号:US12480391
申请日:2009-06-08
申请人: Zhaoning Zhu , Brian McKittrick , Zhong-Yue Sun , Yuanzan C. Ye , Johannes H. Voigt , Corey O. Strickland , Elizabeth M. Smith , Andrew W. Stamford , William J. Greenlee , Robert D. Mazzola, Jr. , 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. Voigt , Corey O. Strickland , Elizabeth M. Smith , Andrew W. Stamford , William J. Greenlee , Robert D. Mazzola, Jr. , 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: A01N57/00 , A01N43/54 , A01N43/40 , A61K31/675 , A61K31/44 , A61K31/445 , C07D239/02 , C07D233/00 , C07D239/24 , C07D401/00
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, U, X, R1, R2, R3, and R4 are as defined herein, and pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of using such compounds to inhibit aspartyl protease and to treat a variety of disease or disorders, including 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 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,U,X,R 1,R 2,R 3和R 4如本文所定义,并且药物组合物包含式I化合物 还公开了使用这些化合物抑制天冬氨酰蛋白酶和治疗各种疾病或病症(包括心血管疾病,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拮抗剂组合治疗认知或神经变性疾病的方法
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公开(公告)号:US08168641B2
公开(公告)日:2012-05-01
申请号:US11759336
申请日:2007-06-07
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: C07D239/20 , C07D239/22 , A61K31/497 , A61K31/513 , A61K31/506 , A61P9/00 , A61P25/28 , A61P31/18 , C07D495/20 , A61K31/527
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。
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公开(公告)号:US20110009392A1
公开(公告)日:2011-01-13
申请号:US12671806
申请日:2008-08-04
申请人: Zhaoning Zhu , William J. Greenlee , John P. Caldwell , Robert D. Mazzola, JR. , Brian McKittrick , Chad E. Bennett , Xianhai Huang , Hubert B. Josien , Duane A. Burnett
发明人: Zhaoning Zhu , William J. Greenlee , John P. Caldwell , Robert D. Mazzola, JR. , Brian McKittrick , Chad E. Bennett , Xianhai Huang , Hubert B. Josien , Duane A. Burnett
IPC分类号: A61K31/55 , C07D487/04 , C07D235/02 , C07D498/04 , C07D491/04 , A61K31/4188 , A61K31/519 , A61K31/535 , A61K31/4353 , A61K31/435 , A61K31/47 , A61K31/505 , A61K31/397 , A61K31/4406 , A61K38/16 , A61P25/28
CPC分类号: C07D487/04 , C07D217/24 , C07D498/04
摘要: In its many embodiments, the present invention provides a novel class of heterocyclic compounds 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 diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
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