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1. 发明授权

US08202889B2 Inhibitors of bacterial IMPDH 失效
标题翻译：细菌IMPDH抑制剂
公开(公告)号：US08202889B2
公开(公告)日：2012-06-19
申请号：US11517755
申请日：2006-09-08
申请人： Paul Charifson , Trudy Grossman , Emanuele Perola
发明人： Paul Charifson , Trudy Grossman , Emanuele Perola
IPC分类号： A61K31/44 , A61K31/41 , A61K31/425
CPC分类号： A61K31/444 , A61K31/41 , A61K31/4184 , A61K31/426 , A61K31/428 , A61K31/433 , A61K31/44
摘要： The present invention relates to methods of inhibiting bacterial IMPDH comprising administering compounds of formula I: or pharmaceutically acceptable salts thereof. The present invention also relates to pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infections.
摘要翻译：本发明涉及抑制细菌IMPDH的方法，其包括施用式I化合物或其药学上可接受的盐。本发明还涉及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。

2. 发明申请

US20120010222A1 Gyrase Inhibitors and Uses Thereof 失效
标题翻译：促旋酶抑制剂及其用途
公开(公告)号：US20120010222A1
公开(公告)日：2012-01-12
申请号：US13234634
申请日：2011-09-16
申请人： Paul Charifson , David Deininger , Anne-Laure Grillot , Yusheng Liao , Steven Ronkin , Dean Stamos , Emanuele Perola , Tiansheng Wang , Arnaud Le Tiran , Joseph Drumm
发明人： Paul Charifson , David Deininger , Anne-Laure Grillot , Yusheng Liao , Steven Ronkin , Dean Stamos , Emanuele Perola , Tiansheng Wang , Arnaud Le Tiran , Joseph Drumm
IPC分类号： A61K31/506 , A61K31/4184 , A61P31/04 , A61K31/4439
CPC分类号： C07D413/14 , A61K31/4439 , A61K31/506 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/04
摘要： The present invention relates to methods of treating, preventing, or lessening the severity of resistant bacterial infections in mammals, utilizing compounds of formula I or formula VII or pharmaceutically salts thereof. The present invention also relates to methods of using compounds of formula I or formula VII in combination with one or more additional antibacterial agents and/or one or more additional therapeutic agents that increase the susceptibility of bacterial organisms to antibiotics.
摘要翻译：本发明涉及使用式I或式VII化合物或其药学上可接受的方法治疗，预防或减轻哺乳动物中抗性细菌感染的严重性。本发明还涉及使用式I或式VII化合物与一种或多种另外的抗菌剂和/或一种或多种增加细菌生物体对抗生素敏感性的其它治疗剂的组合的方法。

3. 发明授权

US08426426B2 Gyrase inhibitors and uses thereof 失效
标题翻译：促旋酶抑制剂及其用途
公开(公告)号：US08426426B2
公开(公告)日：2013-04-23
申请号：US12761576
申请日：2010-04-16
申请人： Paul Charifson , David Deininger , Joseph Drumm , Anne-Laure Grillot , Yusheng Liao , Patricia Oliver-Shaffer , Dean Stamos
发明人： Paul Charifson , David Deininger , Joseph Drumm , Anne-Laure Grillot , Yusheng Liao , Patricia Oliver-Shaffer , Dean Stamos
IPC分类号： C07D239/42 , C07D239/00 , C07D401/00 , A61K31/505 , A61K31/44
CPC分类号： C07D401/04 , A61K31/4439 , A61K31/444 , A61K31/506 , A61K45/06 , C07C275/06 , C07D401/14 , C07D403/04 , Y02A50/473 , Y02A50/478 , A61K2300/00
摘要： The present invention relates to compounds which inhibit bacterial gyrase 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. The present invention also relates to a method for preparing these compounds.
摘要翻译：本发明涉及抑制细菌促旋酶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。本发明还涉及一种制备这些化合物的方法。

4. 发明授权

US08193352B2 Gyrase inhibitors and uses thereof 失效
标题翻译：促旋酶抑制剂及其用途
公开(公告)号：US08193352B2
公开(公告)日：2012-06-05
申请号：US12552430
申请日：2009-09-02
申请人： Paul Charifson , David Deininger , Anne-Laure Grillot , Yusheng Liao , Steven Ronkin , Dean Stamos , Emanuele Perola , Tiansheng Wang , Arnaud LeTiran , Joseph Drumm
发明人： Paul Charifson , David Deininger , Anne-Laure Grillot , Yusheng Liao , Steven Ronkin , Dean Stamos , Emanuele Perola , Tiansheng Wang , Arnaud LeTiran , Joseph Drumm
IPC分类号： C07D401/14 , C07D403/14 , A61K31/506 , A61K31/4439
CPC分类号： C07D401/14 , C07D403/14
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。

5. 发明申请

US20090176771A1 GYRASE INHIBITORS AND USES THEREOF 失效
标题翻译： GYRASE抑制剂及其用途
公开(公告)号：US20090176771A1
公开(公告)日：2009-07-09
申请号：US12246778
申请日：2008-10-07
申请人： Paul Charifson , David Deininger , Anne-Laure Grillot , Yusheng Liao , Steven Ronkin , Dean Stamos , Emanuele Perola , Tiansheng Wang , Arnaud Le Tiran , Joseph Drumm
发明人： Paul Charifson , David Deininger , Anne-Laure Grillot , Yusheng Liao , Steven Ronkin , Dean Stamos , Emanuele Perola , Tiansheng Wang , Arnaud Le Tiran , Joseph Drumm
IPC分类号： A61K31/55 , C07D243/12 , A61P31/04
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 which 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促旋酶和/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。

6. 发明申请

US20070191434A1 Inhibitors of bacterial IMPDH 失效
标题翻译：细菌IMPDH抑制剂
公开(公告)号：US20070191434A1
公开(公告)日：2007-08-16
申请号：US11517755
申请日：2006-09-08
申请人： Paul Charifson , Trudy Grossman , Emanuele Perola
发明人： Paul Charifson , Trudy Grossman , Emanuele Perola
IPC分类号： A61K31/44 , A61K31/41
CPC分类号： A61K31/444 , A61K31/41 , A61K31/4184 , A61K31/426 , A61K31/428 , A61K31/433 , A61K31/44
摘要： The present invention relates to methods of inhibiting bacterial IMPDH comprising administering compounds of formula I: or pharmaceutically acceptable salts thereof. The present invention also relates to pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infections.
摘要翻译：本发明涉及抑制细菌IMPDH的方法，其包括施用式I化合物或其药学上可接受的盐。本发明还涉及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。

7. 发明授权

US06930116B2 Gyrase inhibitors and uses thereof 失效
标题翻译：促旋酶抑制剂及其用途
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。

8. 发明授权

US06426413B1 Inhibitors of caspases 失效
标题翻译：胱天蛋白酶抑制剂
公开(公告)号：US06426413B1
公开(公告)日：2002-07-30
申请号：US09654855
申请日：2000-09-05
申请人： Marion W. Wannamaker , Paul Charifson , David J. Lauffer , Michael D. Mullican
发明人： Marion W. Wannamaker , Paul Charifson , David J. Lauffer , Michael D. Mullican
IPC分类号： C07D24302
CPC分类号： C07D401/12 , C07D243/02 , C07D401/14 , C07D405/12
摘要： The present invention relates to novel classes of compounds which are caspase inhibitors, in particular interleukin-1&bgr; converting enzyme (“ICE”) 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 caspase activity and consequently, may be advantageously used as agents against interleukin-1-(“IL-1”), apoptosis-, interferon-&ggr; inducing factor-(IGIF), or interferon-&ggr;-(“IFN-&ggr;”) mediated diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases. This invention also relates to methods for inhibiting caspase activity and decreasing IGIF production and IFN-&ggr; production and methods for treating interleukin-1, apoptosis-, and interferon-&ggr;-mediated diseases using the compounds and compositions of this invention. This invention also relates to methods of preparing the compounds of this invention.
摘要翻译：本发明涉及新型的化合物，其是胱天蛋白酶抑制剂，特别是白细胞介素-1β转换酶（“ICE”）抑制剂。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胱天蛋白酶活性，因此可有利地用作抗白细胞介素-1-（“IL-1”），细胞凋亡，干扰素-γ诱导因子（IGIF）或“干扰素-γ”（“IFN-γ”）介导的疾病，包括炎性疾病，自身免疫性疾病，破坏性骨病，增殖性疾病，感染性疾病和退行性疾病。本发明还涉及使用本发明的化合物和组合物来抑制胱天蛋白酶活性和降低IGIF产生和IFN-γ产生的方法以及用于治疗白介素-1，细胞凋亡和干扰素-γ介导的疾病的方法。本发明还涉及制备本发明化合物的方法。

9. 发明申请

US20130030004A1 Gyrase inhibitors and uses thereof 失效
标题翻译：促旋酶抑制剂及其用途
公开(公告)号：US20130030004A1
公开(公告)日：2013-01-31
申请号：US11593418
申请日：2006-11-06
申请人： Paul Charifson , David Deininger , Joseph Drumm , Anne-Laure Grillot , Arnaud LeTiran , Yusheng Liao , Emanuele Perola , Steven Ronkin , Dean Stamos , Tiansheng Wang
发明人： Paul Charifson , David Deininger , Joseph Drumm , Anne-Laure Grillot , Arnaud LeTiran , Yusheng Liao , Emanuele Perola , Steven Ronkin , Dean Stamos , Tiansheng Wang
IPC分类号： A61K31/506 , C07D403/10 , A61K31/4184 , A61P31/04 , A61K31/4439 , C07D401/14 , A61K31/4545 , C07D403/14 , C07D401/10
CPC分类号： C07D403/04 , C07D401/04 , C07D403/14
摘要： The present invention relates to compounds of formula I: or a pharmaceutically acceptable salt thereof, that inhibit bacterial gyrase and/or TopoIV 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促旋酶和/或TopoIV的式I化合物或其药学上可接受的盐以及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。

10. 发明申请

US20110104207A1 GYRASE INHIBITORS AND USES THEREOF 失效
标题翻译： GYRASE抑制剂及其用途
公开(公告)号：US20110104207A1
公开(公告)日：2011-05-05
申请号：US12761576
申请日：2010-04-16
申请人： Paul CHARIFSON , David DEININGER , Joseph DRUMM , Anne-Laure GRILLOT , Yusheng LIAO , Patricia OLIVER-SHAFFER , Dean STAMOS
发明人： Paul CHARIFSON , David DEININGER , Joseph DRUMM , Anne-Laure GRILLOT , Yusheng LIAO , Patricia OLIVER-SHAFFER , Dean STAMOS
IPC分类号： A61K39/085 , C07D401/10 , C07D401/14 , C07D403/10 , A61K31/513 , A61K31/506 , A61K31/4545 , A61K31/4439 , A61K31/444 , A61K38/18 , C12N9/99 , A61K39/09 , A61K39/108 , A61K39/02 , A61K39/07 , A61K39/102 , A61K39/118 , C07C255/24 , A61P29/00 , A61P37/06 , A61P37/02 , A61P35/00 , A61P31/12 , A61P31/04
CPC分类号： C07D401/04 , A61K31/4439 , A61K31/444 , A61K31/506 , A61K45/06 , C07C275/06 , C07D401/14 , C07D403/04 , Y02A50/473 , Y02A50/478 , A61K2300/00
摘要： The present invention relates to compounds which inhibit bacterial gyrase 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. The present invention also relates to a method for preparing these compounds.
摘要翻译：本发明涉及抑制细菌促旋酶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。本发明还涉及一种制备这些化合物的方法。

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