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公开(公告)号：US6004549A
公开(公告)日：1999-12-21
申请号：US355585
申请日：1994-12-14
IPC分类号： A61K9/00 , A61K38/00 , A61K38/21 , A61K38/28 , A61K47/10 , A61K47/44 , C07K14/56 , C07K14/00
CPC分类号： A61K47/44 , A61K38/212 , A61K38/28 , A61K47/10 , A61K9/0019 , C07K14/56
摘要： A pharmaceutical composition comprised of a crystalline protein and polyethylene glycol or vegetable oil and a process for producing the same.
摘要翻译： 由结晶蛋白质和聚乙二醇或植物油组成的药物组合物及其制造方法。
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公开(公告)号：US07968683B1
公开(公告)日：2011-06-28
申请号：US12437116
申请日：2009-05-07
申请人： Brian M. Beyer , Alan W. Hruza , Richard N. Ingram , Vincent S. Madison , Andrew J. Prongay , Paul Reichert
发明人： Brian M. Beyer , Alan W. Hruza , Richard N. Ingram , Vincent S. Madison , Andrew J. Prongay , Paul Reichert
CPC分类号： C12Q1/56 , A61K38/00 , C07K2299/00 , C12N9/644 , C12Y304/21022 , G01N2500/04
摘要： The present invention relates to factor IXa complexes and crystals thereof as well as methods for identifying inhibitors of factor IXa.
摘要翻译： 本发明涉及因子IXa复合物及其晶体，以及鉴定因子IXa抑制剂的方法。
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公开(公告)号：US08679472B1
公开(公告)日：2014-03-25
申请号：US11973362
申请日：2007-10-05
申请人： Paul Reichert , Marianna Marshall Long , Alan W. Hruza , Peter Orth , Tattanahalli L. Nagabhushan
发明人： Paul Reichert , Marianna Marshall Long , Alan W. Hruza , Peter Orth , Tattanahalli L. Nagabhushan
CPC分类号： A61K38/212
摘要： This application covers a novel PEGylated interferon and a novel crystalline form of interferon which are useful, inter alia, for detailed structural analysis of interferon as well as treatment and prevention of viral infections and hyperproliferative diseases such as leukemia.
摘要翻译： 该应用涵盖了新型聚乙二醇化干扰素和干扰素的新型结晶形式，其特别用于干扰素的详细结构分析以及病毒感染和过度增殖性疾病如白血病的治疗和预防。
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公开(公告)号：US08710188B2
公开(公告)日：2014-04-29
申请号：US13149011
申请日：2011-05-31
申请人： Brian M. Beyer , Alan W. Hruza , Richard N. Ingram , Vincent S. Madison , Andrew J. Prongay , Paul Reichert
发明人： Brian M. Beyer , Alan W. Hruza , Richard N. Ingram , Vincent S. Madison , Andrew J. Prongay , Paul Reichert
CPC分类号： C12Q1/56 , A61K38/00 , C07K2299/00 , C12N9/644 , C12Y304/21022 , G01N2500/04
摘要： The present invention relates to factor IXa complexes and crystals thereof as well as methods for identifying inhibitors of factor IXa.
摘要翻译： 本发明涉及因子IXa复合物及其晶体，以及鉴定因子IXa抑制剂的方法。
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公开(公告)号：US20160376272A1
公开(公告)日：2016-12-29
申请号：US15116547
申请日：2015-02-06
申请人： Santhosh F. NEELAKAVIL , Scott D. EDMONDSON , Alan W. HRUZA , Zahid HUSSAIN , Charles LESBURG , Remond MONINGKA , Merck Sharp & Dohme Corp.
发明人： Santhosh F. Neelamkavil , Scott D. Edmondson , Alan W. Hruza , Zahid Hussain , Charles Lesburg , Remond Moningka
IPC分类号： C07D471/08 , C07D487/08
CPC分类号： C07D471/08 , C07D487/08
摘要： The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
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公开(公告)号：US08546404B2
公开(公告)日：2013-10-01
申请号：US11810282
申请日：2007-06-05
申请人： Alan B. Cooper , Yongqi Deng , Gerald W. Shipps, Jr. , Neng-Yang Shih , Hugh Y. Zhu , Robert Sun , Joseph M. Kelly , Ronald J. Doll , Yang Nan , Tong Wang , Jagdish A. Desai , James J-S Wang , Youhao Dong , Vincent S. Madison , Li Xiao , Alan W. Hruza , M. Arshad Siddiqui , Ahmed A. Samatar , Sunil Paliwal , Hon-Chung Tsui , Azim Alan Celebi , Yiji Wu , Sobhana Babu Boga , Abdul-Basit Alhassan , Xiaolei Gao , Liang Zhu , Mehul Patel
发明人： Alan B. Cooper , Yongqi Deng , Gerald W. Shipps, Jr. , Neng-Yang Shih , Hugh Y. Zhu , Robert Sun , Joseph M. Kelly , Ronald J. Doll , Yang Nan , Tong Wang , Jagdish A. Desai , James J-S Wang , Youhao Dong , Vincent S. Madison , Li Xiao , Alan W. Hruza , M. Arshad Siddiqui , Ahmed A. Samatar , Sunil Paliwal , Hon-Chung Tsui , Azim Alan Celebi , Yiji Wu , Sobhana Babu Boga , Abdul-Basit Alhassan , Xiaolei Gao , Liang Zhu , Mehul Patel
IPC分类号： A01N43/54 , C07D239/42 , C07D401/04
CPC分类号： C07D231/56 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/14
摘要： Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts, esters and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.
摘要翻译： 公开了式1.0的ERK抑制剂及其药学上可接受的盐，酯和溶剂化物。 Q是可以具有桥或稠合环的哌啶或哌嗪环。 哌啶环可以在环中具有双键。 所有其他取代基如本文所定义。 还公开了使用式1.0化合物治疗癌症的方法。
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公开(公告)号：US07511063B2
公开(公告)日：2009-03-31
申请号：US11504869
申请日：2006-08-16
申请人： Yongqi Deng , Patrick J. Curran , Gerald W. Shipps, Jr. , Lianyun Zhao , M. Arshad Siddiqui , Janeta Popovici-Muller , Jose S. Duca , Alan W. Hruza , Thierry O. Fischmann , Vincent S. Madison , Rumin Zhang , Charles W. McNemar , Todd W. Mayhood , William T. Windsor , Emma M. Lees , David A. Parry
发明人： Yongqi Deng , Patrick J. Curran , Gerald W. Shipps, Jr. , Lianyun Zhao , M. Arshad Siddiqui , Janeta Popovici-Muller , Jose S. Duca , Alan W. Hruza , Thierry O. Fischmann , Vincent S. Madison , Rumin Zhang , Charles W. McNemar , Todd W. Mayhood , William T. Windsor , Emma M. Lees , David A. Parry
IPC分类号： A61K31/47 , C07D215/14
CPC分类号： C07D409/04 , C07D215/48 , C07D215/50 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/04 , C07D409/12 , C07D409/14 , C07D413/10 , C07D413/12 , C07D417/04 , C07D417/06 , C07D417/10
摘要： Quinoline-based inhibitors of cyclin dependent kinase 2, compositions including the inhibitors, and methods of using the inhibitors and inhibitor compositions are described. The inhibitors and compositions including them are useful for treating disease or disease symptoms. The invention also provides for methods of making CDK-2 inhibitor compounds, methods of inhibiting CDK-2, and methods for treating disease or disease symptoms.
摘要翻译： 描述了基于喹啉的细胞周期蛋白依赖性激酶2抑制剂，包括抑制剂的组合物，以及使用抑制剂和抑制剂组合物的方法。 包括它们的抑制剂和组合物可用于治疗疾病或疾病症状。 本发明还提供了制备CDK-2抑制剂化合物的方法，抑制CDK-2的方法以及治疗疾病或疾病症状的方法。
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公开(公告)号：US20080045568A1
公开(公告)日：2008-02-21
申请号：US11504869
申请日：2006-08-16
申请人： Yongqi Deng , Patrick J. Curran , Gerald W. Shipps , Lianyun Zhao , M. Arshad Siddiqui , Janeta Popovici-Muller , Jose S. Duca , Alan W. Hruza , Thierry O. Fischmann , Vincent S. Madison , Rumin Zhang , Charles W. McNemar , Todd W. Mayhood , William T. Windsor , Emma M. Lees , David A. Parry
发明人： Yongqi Deng , Patrick J. Curran , Gerald W. Shipps , Lianyun Zhao , M. Arshad Siddiqui , Janeta Popovici-Muller , Jose S. Duca , Alan W. Hruza , Thierry O. Fischmann , Vincent S. Madison , Rumin Zhang , Charles W. McNemar , Todd W. Mayhood , William T. Windsor , Emma M. Lees , David A. Parry
IPC分类号： A61K31/4709 , A61K31/4706 , C07D215/38
CPC分类号： C07D409/04 , C07D215/48 , C07D215/50 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/04 , C07D409/12 , C07D409/14 , C07D413/10 , C07D413/12 , C07D417/04 , C07D417/06 , C07D417/10
摘要： Quinoline-based inhibitors of cyclin dependent kinase 2, compositions including the inhibitors, and methods of using the inhibitors and inhibitor compositions are described. The inhibitors and compositions including them are useful for treating disease or disease symptoms. The invention also provides for methods of making CDK-2 inhibitor compounds, methods of inhibiting CDK-2, and methods for treating disease or disease symptoms.
摘要翻译： 描述了基于喹啉的细胞周期蛋白依赖性激酶2抑制剂，包括抑制剂的组合物，以及使用抑制剂和抑制剂组合物的方法。 包括它们的抑制剂和组合物可用于治疗疾病或疾病症状。 本发明还提供了制备CDK-2抑制剂化合物的方法，抑制CDK-2的方法以及治疗疾病或疾病症状的方法。
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公开(公告)号：US20090118284A1
公开(公告)日：2009-05-07
申请号：US11810282
申请日：2007-06-05
申请人： Alan B. Cooper , Yongqi Deng , Gerald W. Shipps, JR. , Neng-Yang Shih , Hugh Y. Zhu , Robert Sun , Joseph M. Kelly , Ronald J. Doll , Yang Nan , Tong Wang , Jagdish A. Desai , James J-S Wang , Youhao Dong , Vincent S. Madison , Li Xiao , Alan W. Hruza , M. Arshad Siddiqui , Ahmed A. Samatar , Sunil Paliwal , Hon-Chung Tsui , Azim Alan Celebi , Yiji Wu , Sobhana Babu Boga , Abdul-Basit Alhassan , Xiaolei Gao , Liang Zhu , Mehul Patel
发明人： Alan B. Cooper , Yongqi Deng , Gerald W. Shipps, JR. , Neng-Yang Shih , Hugh Y. Zhu , Robert Sun , Joseph M. Kelly , Ronald J. Doll , Yang Nan , Tong Wang , Jagdish A. Desai , James J-S Wang , Youhao Dong , Vincent S. Madison , Li Xiao , Alan W. Hruza , M. Arshad Siddiqui , Ahmed A. Samatar , Sunil Paliwal , Hon-Chung Tsui , Azim Alan Celebi , Yiji Wu , Sobhana Babu Boga , Abdul-Basit Alhassan , Xiaolei Gao , Liang Zhu , Mehul Patel
IPC分类号： A61K31/496 , C07D403/14 , C07D413/14 , A61K31/506 , A61P35/00 , A61P35/02 , A61K31/4439 , A61K31/5377 , C07D401/14
CPC分类号： C07D231/56 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/14
摘要： Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts, esters and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.
摘要翻译： 公开了式1.0的ERK抑制剂及其药学上可接受的盐，酯和溶剂化物。 Q是可以具有桥或稠合环的哌啶或哌嗪环。 哌啶环可以在环中具有双键。 所有其他取代基如本文所定义。 还公开了使用式1.0化合物治疗癌症的方法。
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公开(公告)号：US09944643B2
公开(公告)日：2018-04-17
申请号：US15116547
申请日：2015-02-06
申请人： MERCK SHARP & DOHME CORP. , Santhosh F. Neelamkavil , Scott D. Edmondson , Alan W. Hruza , Zahid Hussain , Charles Lesburg , Remond Moningka
发明人： Santhosh F. Neelamkavil , Scott D. Edmondson , Alan W. Hruza , Zahid Hussain , Charles Lesburg , Remond Moningka
IPC分类号： C07D471/08 , C07D487/08
CPC分类号： C07D471/08 , C07D487/08
摘要： The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
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