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公开(公告)号：US06608087B1
公开(公告)日：2003-08-19
申请号：US10198407
申请日：2002-07-18
申请人： Paul Charifson , Dean Stamos , Michael Badia , Anne-Laure Grillot , Steven Ronkin , Martin Trudeau
发明人： Paul Charifson , Dean Stamos , Michael Badia , Anne-Laure Grillot , Steven Ronkin , Martin Trudeau
IPC分类号： C07D21302
CPC分类号： A61K31/4155 , A61K31/421 , A61K31/422 , A61K31/427 , C07D417/04 , C07D417/14 , Y02A50/473 , Y02A50/475 , Y02A50/481
摘要： The present invention relates to compounds of the formula I: where Ring A is a thiazole, oxazole, imidazole or pyrazole and the substituents are as described in the specification, and pharmaceutically acceptable salts thereof. The compounds inhibit bacterial gyrase activity and therefore are useful for treating bacterial infections in mammals.
摘要翻译： 本发明涉及式I化合物：其中环A是噻唑，恶唑，咪唑或吡唑，取代基如说明书中所述，及其药学上可接受的盐。 该化合物抑制细菌的促旋酶活性，因此可用于治疗哺乳动物的细菌感染。
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公开(公告)号：US06930116B2
公开(公告)日：2005-08-16
申请号：US10395331
申请日：2003-03-24
申请人： Paul Charifson , Dean Stamos , Michael Badia , Anne Laure Grillot , Steven Ronkin , Martin Trudeau
发明人： Paul Charifson , Dean Stamos , Michael Badia , Anne Laure Grillot , Steven Ronkin , Martin Trudeau
IPC分类号： C07D231/38 , A61K31/4155 , A61K31/421 , A61K31/422 , A61K31/427 , A61K31/454 , A61K31/5377 , A61P1/00 , A61P11/00 , A61P13/02 , A61P13/08 , A61P17/00 , A61P17/02 , A61P19/02 , A61P19/08 , A61P25/00 , A61P31/04 , A61P31/06 , A61P43/00 , C07D403/04 , C07D413/04 , C07D417/04 , C07D417/14 , C07D277/32
CPC分类号： A61K31/4155 , A61K31/421 , A61K31/422 , A61K31/427 , C07D417/04 , C07D417/14 , Y02A50/473 , Y02A50/475 , Y02A50/481
摘要： The present invention relates to compounds of the formula I: where Ring A is a thiazole, oxazole, imidazole or pyrazole and the substituents are as described in the specification, and pharmaceutically acceptable salts thereof. The compounds inhibit bacterial gyrase activity and therefore are useful for treating bacterial infections in mammals.
摘要翻译： 本发明涉及式I化合物：其中环A是噻唑，恶唑，咪唑或吡唑，取代基如说明书中所述，及其药学上可接受的盐。 该化合物抑制细菌的促旋酶活性，因此可用于治疗哺乳动物的细菌感染。
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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：US07414046B2
公开(公告)日：2008-08-19
申请号：US10444588
申请日：2003-05-23
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： 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.
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公开(公告)号：US07087642B2
公开(公告)日：2006-08-08
申请号：US10287405
申请日：2002-11-04
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： A61K47/00 , A61K31/27 , C07C229/00 , C07C255/00
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.
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公开(公告)号：US20050148644A1
公开(公告)日：2005-07-07
申请号：US10997810
申请日：2004-11-24
申请人： Dean Stamos , Martin Trudeau , Randy Bethiel , Steven Ronkin , Michael Badia , Jeffrey Saunders
发明人： Dean Stamos , Martin Trudeau , Randy Bethiel , Steven Ronkin , Michael Badia , Jeffrey Saunders
IPC分类号： C07D307/20 , A61K31/27 , A61K31/275 , A61K31/341 , A61K31/421 , A61K31/422 , A61K31/454 , A61K31/5377 , A61K31/541 , A61K45/00 , A61P1/18 , A61P9/10 , A61P11/06 , A61P19/02 , A61P29/00 , A61P31/12 , A61P35/00 , A61P37/02 , A61P43/00 , C07C275/40 , C07C275/42 , C07D263/32 , C07D413/12 , C07D417/12 , C07F9/653 , A61K31/325 , C07D263/34
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：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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公开(公告)号：US20050282876A1
公开(公告)日：2005-12-22
申请号：US11192657
申请日：2005-07-29
申请人： David Armistead , Michael Badia , Guy Bemis , Randy Bethiel , Catharine Frank , Perry Novak , Steven Ronkin , Jeffrey Saunders
发明人： David Armistead , Michael Badia , Guy Bemis , Randy Bethiel , Catharine Frank , Perry Novak , Steven Ronkin , Jeffrey Saunders
IPC分类号： A61K31/17 , A61K31/18 , A61K31/404 , A61K31/42 , A61K31/421 , A61K31/422 , A61P9/14 , A61P29/00 , A61P31/12 , A61P35/00 , A61P37/06 , A61P43/00 , C07C275/42 , C07D263/18 , C07D263/32 , C07D277/18 , C07D413/12
CPC分类号： C07D413/12 , A61K31/404 , A61K31/42 , A61K31/422 , C07C275/42 , C07D263/32 , Y02P20/55
摘要： The present invention relates to a novel class of compounds which are IMPDH inhibitors. 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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