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公开(公告)号：US06498178B2
公开(公告)日：2002-12-24
申请号：US09955626
申请日：2001-09-19
申请人： Dean Stamos , Martin Trudeau , Scott Bethiel , Steven Ronkin , Michael Badia , Jeffrey Saunders
发明人： Dean Stamos , Martin Trudeau , Scott Bethiel , Steven Ronkin , Michael Badia , Jeffrey Saunders
IPC分类号： A61K31277
CPC分类号： C07C275/40 , C07B2200/07 , C07C275/42 , C07D263/32 , C07F9/653
摘要： The present invention relates to compounds which inhibit IMPDH. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH-mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.
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12.发明申请PROCESS FOR MAKING MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR 有权CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR制造调制器的工艺公开(公告)号：US20100267768A1
公开(公告)日：2010-10-21
申请号：US12728173
申请日：2010-03-19
申请人： John DeMattei , Adam R. Looker , Bobbianna Neubert-Langille , Martin Trudeau , Stefanie Roeper , Michael P. Ryan , Dahrika Milfred Lao Yap , Brian R. Krueger , Peter D.J. Grootenhuis , Fredrick F. van Goor , Martyn C. Botfield , Gregor Zlokarnik
发明人： John DeMattei , Adam R. Looker , Bobbianna Neubert-Langille , Martin Trudeau , Stefanie Roeper , Michael P. Ryan , Dahrika Milfred Lao Yap , Brian R. Krueger , Peter D.J. Grootenhuis , Fredrick F. van Goor , Martyn C. Botfield , Gregor Zlokarnik
IPC分类号： A61K31/47 , C07D215/233 , C07C69/96 , C07D307/77 , A61P11/06 , A61P1/18 , A61P15/10 , A61P37/08 , A61P1/16 , A61P3/00 , A61P25/28 , A61P3/10 , A61P37/00 , A61P7/12 , C12N5/07 , C12Q1/02
CPC分类号： C07C205/43 , C07C68/02 , C07C69/96 , C07C201/08 , C07C213/02 , C07C229/66 , C07D215/233 , C07D215/56 , G01N33/5041 , G01N33/6872 , Y02P20/55
摘要： The invention provides a process for the preparation of a compound of Formula 1, comprising coupling a carboxylic acid of Formula 2 with an aniline of Formula 3 in the presence of a coupling agent.
摘要翻译： 本发明提供了制备式1化合物的方法，包括在偶联剂存在下将式2的羧酸与式3的苯胺偶联。
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公开(公告)号：US20100105914A1
公开(公告)日：2010-04-29
申请号：US12630350
申请日：2009-12-03
申请人： Jean-Damien Charrier , Steven Durrant , Michael Mortimore , Michael O'Donnell , Alistair Rutherford , Sharn Ramaya , John R. Studley , Martin Trudeau , Adam Looker
发明人： Jean-Damien Charrier , Steven Durrant , Michael Mortimore , Michael O'Donnell , Alistair Rutherford , Sharn Ramaya , John R. Studley , Martin Trudeau , Adam Looker
IPC分类号： C07D405/14 , C07D417/14 , C07D405/12
CPC分类号： C07D405/12 , A61K38/06 , C07D207/16 , C07D209/52 , C07D401/12 , C07D401/14 , C07D417/06 , C07D417/12 , C07K5/0202 , Y02A50/385 , Y02A50/387 , Y02A50/389
摘要： The present invention provides a compound of formula I: wherein the variables are as defined herein. The present invention also provides processes for preparing the compounds of formula I, and intermediates thereof, pharmaceutical compositions comprising those compounds, and methods of using the compounds and compositions.
摘要翻译： 本发明提供式I化合物：其中变量如本文所定义。 本发明还提供制备式I化合物的方法及其中间体，包含这些化合物的药物组合物，以及使用该化合物和组合物的方法。
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公开(公告)号：US07381827B2
公开(公告)日：2008-06-03
申请号：US11078147
申请日：2005-03-11
申请人： Gerald J. Tanoury , Minzhang Chen , Andrew D. Jones , Philip L. Nyce , Martin Trudeau , David J. Guerin , John R. Snoonian
发明人： Gerald J. Tanoury , Minzhang Chen , Andrew D. Jones , Philip L. Nyce , Martin Trudeau , David J. Guerin , John R. Snoonian
IPC分类号： C07D207/06 , C07D295/02 , C07D305/00 , C07C239/00
CPC分类号： C07D207/16 , C07D209/52 , C07D211/60 , C07D405/12 , C07D417/06 , C07D417/12 , C07D417/14 , Y02P20/55
摘要： The invention relates to processes and compounds useful for producing modified aspartic acid derivatives, such as aspartic acid aldehyde moieties. Aspartic acid derivatives are useful for preparing caspase inhibitors and/or prodrugs thereof.
摘要翻译： 本发明涉及可用于生产改性天冬氨酸衍生物如天冬氨酸醛部分的方法和化合物。 天冬氨酸衍生物可用于制备半胱天冬酶抑制剂和/或其前药。
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公开(公告)号：USRE40245E1
公开(公告)日：2008-04-15
申请号：US10833995
申请日：2004-04-28
申请人： Anne-Laure Grillot , Paul S. Charifson , Dean Stamos , Yusheng Liao , Michael C. Badia , Martin Trudeau
发明人： Anne-Laure Grillot , Paul S. Charifson , Dean Stamos , Yusheng Liao , Michael C. Badia , Martin Trudeau
IPC分类号： C07D403/04 , C07D413/04 , C07D235/30 , A61K31/55
CPC分类号： C07D403/12 , A61K31/00 , A61K31/4184 , A61K31/423 , A61K31/437 , A61K31/4439 , A61K31/4709 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D231/12 , C07D233/56 , C07D235/30 , C07D249/08 , C07D263/58 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D413/04 , C07D471/04 , C07D471/14 , C07D491/04 , C07F9/65583 , C07F9/6561 , Y02A50/393 , Y02A50/473 , A61K2300/00
摘要： The present invention relates to compounds of the formula I: or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also relates to methods for treating bacterial infections in mammala. The present invention also relates to methods for decreasing bacterial quantity in a biological sample.
摘要翻译： 本发明涉及式I化合物或其药学上可接受的衍生物或前药。 这些化合物可用作细菌回旋酶活性的抑制剂。 本发明还涉及用于治疗哺乳动物细菌感染的方法。 本发明还涉及生物样品中细菌数量减少的方法。
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公开(公告)号：US20050233979A1
公开(公告)日：2005-10-20
申请号：US11069895
申请日：2005-02-28
申请人： Jean-Damien Charrier , Steven Durrant , Michael Mortimore , Michael O'Donnell , Alistair Rutherford , Sharn Ramaya , John Studley , Martin Trudeau , Adam Looker
发明人： Jean-Damien Charrier , Steven Durrant , Michael Mortimore , Michael O'Donnell , Alistair Rutherford , Sharn Ramaya , John Studley , Martin Trudeau , Adam Looker
IPC分类号： A61K38/04 , A61K38/06 , C07D207/16 , C07D209/52 , C07D401/12 , C07D401/14 , C07D405/12 , C07D417/06 , C07D417/12 , C07K5/02 , C07K5/04 , C07D45/14
CPC分类号： C07D405/12 , A61K38/06 , C07D207/16 , C07D209/52 , C07D401/12 , C07D401/14 , C07D417/06 , C07D417/12 , C07K5/0202 , Y02A50/385 , Y02A50/387 , Y02A50/389
摘要： The present invention provides a compound of formula wherein the variables are as defined herein. The present invention also provides processes for preparing the compounds of formula I, and intermediates thereof, pharmaceutical compositions comprising those compounds, and methods of using the compounds and compositions.
摘要翻译： 本发明提供了式的化合物，其中变量如本文所定义。 本发明还提供制备式I化合物的方法及其中间体，包含这些化合物的药物组合物，以及使用该化合物和组合物的方法。
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公开(公告)号：US06632809B2
公开(公告)日：2003-10-14
申请号：US10015332
申请日：2001-12-12
申请人： Anne-Laure Grillot , Paul Charifson , Dean Stamos , Yusheng Liao , Michael Badia , Martin Trudeau
发明人： Anne-Laure Grillot , Paul Charifson , Dean Stamos , Yusheng Liao , Michael Badia , Martin Trudeau
IPC分类号： C07D40304
CPC分类号： C07D403/12 , A61K31/00 , A61K31/4184 , A61K31/423 , A61K31/437 , A61K31/4439 , A61K31/4709 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D231/12 , C07D233/56 , C07D235/30 , C07D249/08 , C07D263/58 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D413/04 , C07D471/04 , C07D471/14 , C07D491/04 , C07F9/65583 , C07F9/6561 , Y02A50/393 , Y02A50/473 , A61K2300/00
摘要： The present invention relates to compounds of the formula I: or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also relates to methods for treating bacterial infections in mammala. The present invention also relates to methods for decreasing bacterial quantity in a biological sample.
摘要翻译： 本发明涉及式I化合物或其药学上可接受的衍生物或前药。 这些化合物可用作细菌回旋酶活性的抑制剂。 本发明还涉及用于治疗哺乳动物细菌感染的方法。 本发明还涉及用于降低生物样品中细菌数量的方法
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公开(公告)号：US08268873B2
公开(公告)日：2012-09-18
申请号：US12221921
申请日：2008-08-07
申请人： Dean Stamos , Martin Trudeau , Randy S. Bethiel , Steven M. Ronkin , Michael C. Badia , Jeffrey O. Saunders
发明人： Dean Stamos , Martin Trudeau , Randy S. Bethiel , Steven M. Ronkin , Michael C. Badia , Jeffrey O. Saunders
IPC分类号： A61K31/42 , A61K31/27 , C07D263/14 , C07D207/00
CPC分类号： C07C275/40 , C07B2200/07 , C07C275/42 , C07D263/32 , C07F9/653
摘要： The present invention relates to compounds which inhibit IMPDH. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH-mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.
摘要翻译： 本发明涉及抑制IMPDH的化合物。 本发明还涉及包含这些化合物的药物组合物。 本发明的化合物和药物组合物特别适用于抑制IMPDH酶活性，因此可有利地用作IMPDH介导的方法的治疗剂。 本发明还涉及使用本发明化合物和相关化合物抑制IMPDH活性的方法。
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公开(公告)号：US07834200B2
公开(公告)日：2010-11-16
申请号：US12074983
申请日：2008-03-07
申请人： Gerald J. Tanoury , Minzhang Chen , Andrew D. Jones , Philip L. Nyce , Martin Trudeau , David J. Guerin , John R. Snoonian
发明人： Gerald J. Tanoury , Minzhang Chen , Andrew D. Jones , Philip L. Nyce , Martin Trudeau , David J. Guerin , John R. Snoonian
IPC分类号： C07D307/56
CPC分类号： C07D207/16 , C07D209/52 , C07D211/60 , C07D405/12 , C07D417/06 , C07D417/12 , C07D417/14 , Y02P20/55
摘要： The invention relates to processes and compounds useful for producing modified aspartic acid derivatives, such as aspartic acid aldehyde moieties. Aspartic acid derivatives are useful for preparing caspase inhibitors and/or prodrugs thereof.
摘要翻译： 本发明涉及可用于生产改性天冬氨酸衍生物如天冬氨酸醛部分的方法和化合物。 天冬氨酸衍生物可用于制备半胱天冬酶抑制剂和/或其前药。
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公开(公告)号：US07652153B2
公开(公告)日：2010-01-26
申请号：US11069895
申请日：2005-02-28
申请人： Jean Damien Charrier , Steven Durrant , Michael Mortimore , Michael O'Donnell , Alistair Rutherford , Sharn Ramaya , John Studley , Martin Trudeau , Adam Looker
发明人： Jean Damien Charrier , Steven Durrant , Michael Mortimore , Michael O'Donnell , Alistair Rutherford , Sharn Ramaya , John Studley , Martin Trudeau , Adam Looker
IPC分类号： A61K31/401 , A61K31/403 , A61K31/4025 , C07D207/09 , C07D209/02
CPC分类号： C07D405/12 , A61K38/06 , C07D207/16 , C07D209/52 , C07D401/12 , C07D401/14 , C07D417/06 , C07D417/12 , C07K5/0202 , Y02A50/385 , Y02A50/387 , Y02A50/389
摘要： The present invention provides a compound of formula I: wherein the variables are as defined herein. The present invention also provides processes for preparing the compounds of formula I, and intermediates thereof, pharmaceutical compositions comprising those compounds, and methods of using the compounds and compositions.
摘要翻译： 本发明提供式I化合物：其中变量如本文所定义。 本发明还提供制备式I化合物的方法及其中间体，包含这些化合物的药物组合物，以及使用该化合物和组合物的方法。
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