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公开(公告)号:US07989498B2
公开(公告)日:2011-08-02
申请号:US10671967
申请日:2003-09-25
申请人: Jeffrey O Saunders , Daniel Elbaum , Perry M Novak , Douglas Naegele , Randy S Bethiel , Steven M Ronkin , Michael C Badia , Catharine Frank , Dean P Stamos , William Walters , David Pearlman
发明人: Jeffrey O Saunders , Daniel Elbaum , Perry M Novak , Douglas Naegele , Randy S Bethiel , Steven M Ronkin , Michael C Badia , Catharine Frank , Dean P Stamos , William Walters , David Pearlman
IPC分类号: A61K31/165 , A61K31/16
CPC分类号: C07D213/75 , A61K31/4965 , A61K31/53 , C07C217/84 , C07C235/64 , C07C311/21 , C07C311/29 , C07C317/40 , C07C323/42 , C07C333/08 , C07D263/32 , C07D271/06 , C07D307/91 , C07D317/68 , C07D413/12
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介导的过程的治疗剂。 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:US20090093639A1
公开(公告)日:2009-04-09
申请号:US12228164
申请日:2008-08-07
申请人: Dean P. Stamos , Randy S. Bethiel
发明人: Dean P. Stamos , Randy S. Bethiel
IPC分类号: C07D413/12 , C07D233/90
CPC分类号: C07D413/12 , A61K38/00 , C07K5/06017 , C07K5/06026 , C07K5/06165
摘要: The present invention relates to novel compounds, methods of preparing these compounds, and pharmaceutical compositions comprising these compounds. These compounds are carbamate prodrugs that convert to active inhibitors of the IMPDH enzyme in vivo. The compounds and pharmaceutical compositions of this invention are particularly well suited for activation and subsequent inhibition of the IMPDH enzyme activity. Consequently, these prodrugs 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 and compositions of this invention.
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公开(公告)号:US07618974B2
公开(公告)日:2009-11-17
申请号:US10971573
申请日:2004-10-21
申请人: Paul Charifson , David Deininger , Anne-Laure Grillot , Yusheng Liao , Steven M. Ronkin , Dean P. Stamos , Emanuele Perola , Tiansheng Wang , Arnaud LeTiran , Joseph Drumm
发明人: Paul Charifson , David Deininger , Anne-Laure Grillot , Yusheng Liao , Steven M. Ronkin , Dean P. Stamos , Emanuele Perola , Tiansheng Wang , Arnaud LeTiran , Joseph Drumm
IPC分类号: A61K31/506 , C07D403/04
CPC分类号: C07D401/14 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/04
摘要: The present invention relates to compounds that inhibit bacterial gyrase and/or Topo IV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals.
摘要翻译: 本发明涉及抑制细菌回旋酶和/或Topo IV的化合物和包含所述化合物的药学上可接受的组合物。 这些化合物及其组合物可用于治疗细菌感染。 因此,本发明还涉及用于治疗哺乳动物细菌感染的方法。
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公开(公告)号:US06395763B1
公开(公告)日:2002-05-28
申请号:US09602703
申请日:2000-06-23
申请人: Dean P. Stamos , Randy S. Bethiel
发明人: Dean P. Stamos , Randy S. Bethiel
IPC分类号: C07D26332
CPC分类号: C07D413/12 , A61K38/00 , C07K5/06017 , C07K5/06026 , C07K5/06165
摘要: The present invention relates to novel compounds, methods of preparing these compounds, and pharmaceutical compositions comprising these compounds. These compounds are carbamate prodrugs that convert to active inhibitors of the IMPDH enzyme in vivo. The compounds and pharmaceutical compositions of this invention are particularly well suited for activation and subsequent inhibition of the IMPDH enzyme activity. Consequently, these prodrugs 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 and compositions of this invention.
摘要翻译: 本发明涉及新化合物,制备这些化合物的方法和包含这些化合物的药物组合物。 这些化合物是在体内转化为IMPDH酶的活性抑制剂的氨基甲酸酯前药。 本发明的化合物和药物组合物特别适用于IMPDH酶活性的活化和随后的抑制。 因此,这些前药可以有利地用作IMPDH介导的过程的治疗剂。 本发明还涉及使用本发明的化合物和组合物来抑制IMPDH的活性的方法。
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公开(公告)号:US07777069B2
公开(公告)日:2010-08-17
申请号:US12228164
申请日:2008-08-07
申请人: Dean P. Stamos , Randy S. Bethiel
发明人: Dean P. Stamos , Randy S. Bethiel
IPC分类号: C07D263/32 , C07C271/00
CPC分类号: C07D413/12 , A61K38/00 , C07K5/06017 , C07K5/06026 , C07K5/06165
摘要: The present invention relates to novel compounds, methods of preparing these compounds, and pharmaceutical compositions comprising these compounds. These compounds are carbamate prodrugs that convert to active inhibitors of the IMPDH enzyme in vivo. The compounds and pharmaceutical compositions of this invention are particularly well suited for activation and subsequent inhibition of the IMPDH enzyme activity. Consequently, these prodrugs 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 and compositions of this invention.
摘要翻译: 本发明涉及新化合物,制备这些化合物的方法和包含这些化合物的药物组合物。 这些化合物是在体内转化为IMPDH酶的活性抑制剂的氨基甲酸酯前药。 本发明的化合物和药物组合物特别适用于IMPDH酶活性的活化和随后的抑制。 因此,这些前药可以有利地用作IMPDH介导的过程的治疗剂。 本发明还涉及使用本发明的化合物和组合物来抑制IMPDH的活性的方法。
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公开(公告)号:US06825224B2
公开(公告)日:2004-11-30
申请号:US10125617
申请日:2002-04-17
申请人: Dean P. Stamos , Randy S. Bethiel
发明人: Dean P. Stamos , Randy S. Bethiel
IPC分类号: A61K3142
CPC分类号: C07D413/12 , A61K38/00 , C07K5/06017 , C07K5/06026 , C07K5/06165
摘要: The present invention relates to novel compounds, methods of preparing these compounds, and pharmaceutical compositions comprising these compounds. These compounds are carbamate prodrugs that convert to active inhibitors of the IMPDH enzyme in vivo. The compounds and pharmaceutical compositions of this invention are particularly well suited for activation and subsequent inhibition of the IMPDH enzyme activity. Consequently, these prodrugs 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 and compositions of this invention.
摘要翻译: 本发明涉及新化合物,制备这些化合物的方法和包含这些化合物的药物组合物。 这些化合物是在体内转化为IMPDH酶的活性抑制剂的氨基甲酸酯前药。 本发明的化合物和药物组合物特别适用于IMPDH酶活性的活化和随后的抑制。 因此,这些前药可以有利地用作IMPDH介导的过程的治疗剂。 本发明还涉及使用本发明的化合物和组合物来抑制IMPDH的活性的方法。
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公开(公告)号:US06653309B1
公开(公告)日:2003-11-25
申请号:US09702991
申请日:2000-10-30
申请人: Jeffrey O. Saunders , Daniel Elbaum , Perry M. Novak , Douglas Naegele , Randy S. Bethiel , Steven M. Ronkin , Michael C. Badia , Catharine Frank , Dean P. Stamos , William Walters , David Pearlman
发明人: Jeffrey O. Saunders , Daniel Elbaum , Perry M. Novak , Douglas Naegele , Randy S. Bethiel , Steven M. Ronkin , Michael C. Badia , Catharine Frank , Dean P. Stamos , William Walters , David Pearlman
IPC分类号: C07D25102
CPC分类号: C07D213/75 , A61K31/4965 , A61K31/53 , C07C217/84 , C07C235/64 , C07C311/21 , C07C311/29 , C07C317/40 , C07C323/42 , C07C333/08 , C07D263/32 , C07D271/06 , C07D307/91 , C07D317/68 , C07D413/12
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合于抑制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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