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1. 发明授权

US06949573B2 Nicotinamide derivatives useful as PDE4 inhibitors 失效
标题翻译：可用作PDE4抑制剂的烟酰胺衍生物
公开(公告)号：US06949573B2
公开(公告)日：2005-09-27
申请号：US10361062
申请日：2003-02-06
申请人： Simon Bailey , Elisabeth C. L. Gautier , Alan J. Henderson , Thomas V. Magee , Anthony Marfat , John P. Mathias , Dale G. McLeod , Sandra M. Monaghan , Blanda L. C. Stammen
发明人： Simon Bailey , Elisabeth C. L. Gautier , Alan J. Henderson , Thomas V. Magee , Anthony Marfat , John P. Mathias , Dale G. McLeod , Sandra M. Monaghan , Blanda L. C. Stammen
IPC分类号： A61K31/44 , A61K31/443 , A61K31/4433 , A61K31/4545 , A61K31/455 , A61K31/46 , A61K31/537 , A61K45/06 , A61P1/00 , A61P1/04 , A61P1/16 , A61P1/18 , A61P3/10 , A61P7/06 , A61P9/12 , A61P11/00 , A61P11/06 , A61P11/08 , A61P13/12 , A61P17/02 , A61P17/04 , A61P17/06 , A61P19/00 , A61P19/02 , A61P19/10 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/24 , A61P25/28 , A61P25/30 , A61P27/02 , A61P29/00 , A61P31/16 , A61P31/22 , A61P35/00 , A61P37/00 , A61P37/02 , A61P43/00 , C07D213/82 , C07D401/12 , C07D405/12 , C07D451/04 , C07D451/10 , C07D213/643
CPC分类号： C07D213/82 , A61K31/4433 , A61K31/455 , A61K31/46 , A61K31/537 , A61K45/06 , C07D401/12 , C07D405/12 , C07D451/04 , C07D451/10 , Y02A50/411 , A61K2300/00
摘要： The invention relates to nicotinamide derivatives and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The nicotinamide derivatives according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic, respiratory diseases, disorders and conditions, as well as wounds.
摘要翻译：本发明涉及烟酰胺衍生物以及制备用于制备含有这些衍生物的组合物和用途的中间体的方法。根据本发明的烟酰胺衍生物可用于许多疾病，病症和病症，特别是炎性，过敏性，呼吸道疾病，病症和病症以及伤口。

2. 发明授权

US07060717B2 Nicotinamide derivatives useful as PDE4 inhibitors 失效
公开(公告)号：US07060717B2
公开(公告)日：2006-06-13
申请号：US10865263
申请日：2004-06-09
申请人： Simon Bailey , Elisabeth C. L. Gautier , Alan J. Henderson , Thomas V. Magee , Anthony Marfat , John P. Mathias , Dale G. McLeod , Sandra M. Monaghan , Blanda L. C. Stammen
发明人： Simon Bailey , Elisabeth C. L. Gautier , Alan J. Henderson , Thomas V. Magee , Anthony Marfat , John P. Mathias , Dale G. McLeod , Sandra M. Monaghan , Blanda L. C. Stammen
IPC分类号： A61K31/445 , C07D211/72
CPC分类号： C07D213/82 , A61K31/4433 , A61K31/455 , A61K31/46 , A61K31/537 , A61K45/06 , C07D401/12 , C07D405/12 , C07D451/04 , C07D451/10 , Y02A50/411 , A61K2300/00
摘要： The invention relates to nicotinamide derivatives and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The nicotinamide derivatives according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic, respiratory diseases, disorders and conditions, as well as wounds.

3. 发明授权

US07795243B2 Penem prodrugs 有权
公开(公告)号：US07795243B2
公开(公告)日：2010-09-14
申请号：US11769849
申请日：2007-06-28
申请人： Katherine E. Brighty , Anthony Marfat , Dale G. McLeod , John P. O'Donnell
发明人： Katherine E. Brighty , Anthony Marfat , Dale G. McLeod , John P. O'Donnell
IPC分类号： C07D499/887 , A61K31/431 , A61P31/04
CPC分类号： C07D499/887
摘要： Orally bioavailable prodrugs of sulopenem, e.g., and solvates and hydrates thereof, preparation thereof, formulation thereof, and use to treat and prevent infection in mammals such as humans. This abstract is not limiting to the invention.

4. 发明申请

US20080009474A1 PENEM PRODRUGS 有权
公开(公告)号：US20080009474A1
公开(公告)日：2008-01-10
申请号：US11769849
申请日：2007-06-28
申请人： Katherine E. BRIGHTY , Anthony Marfat , Dale G. McLeod , John P. O'Donnell
发明人： Katherine E. BRIGHTY , Anthony Marfat , Dale G. McLeod , John P. O'Donnell
IPC分类号： A61K31/43 , C07D501/14
CPC分类号： C07D499/887
摘要： Orally bioavailable prodrugs of sulopenem, e.g., and solvates and hydrates thereof, preparation thereof, formulation thereof, and use to treat and prevent infection in mammals such as humans. This abstract is not limiting to the invention.
摘要翻译：口服生物可利用的磺脲类前体药物，例如及其溶剂化物和水合物，其制备，其制剂，以及治疗和预防哺乳动物如人类感染的用途。该摘要不限于本发明。

5. 发明授权

US07091197B2 Beta-lactamase inhibitor prodrug 失效
标题翻译： β-内酰胺酶抑制剂前药
公开(公告)号：US07091197B2
公开(公告)日：2006-08-15
申请号：US10648408
申请日：2003-08-25
申请人： Anthony Marfat , Dale G. McLeod
发明人： Anthony Marfat , Dale G. McLeod
IPC分类号： C07D499/861 , A61K31/43 , A61P31/04
CPC分类号： C07D499/00
摘要： Prodrugs of 6-β-hydroxymethylpenicillanic acid sulfone having the structure wherein R is H or methyl, and solvates thereof, are disclosed. Also disclosed are pharmaceutical compositions comprising a prodrug of the present invention or a solvate thereof, an optional beta-lactam antibiotic and a pharmaceutically acceptable excipient. Further disclosed is a method for increasing the therapeutic effectiveness of a beta-lactam antibiotic in a mammal by administering an effective amount of a beta-lactam antibiotic and an effectiveness-increasing amount of a prodrug of the present invention, or a solvate thereof.Additionally disclosed is a method for treating a bacterial infection in a mammal by administering a therapeutically effective amount of a pharmaceutical composition of the present invention to a mammal in need thereof.
摘要翻译：公开了具有其中R为H或甲基的结构及其溶剂合物的6-β-羟甲基青霉烷酸砜的前药。还公开了包含本发明的前药或其溶剂合物，任选的β-内酰胺抗生素和药学上可接受的赋形剂的药物组合物。进一步公开的是通过施用有效量的β-内酰胺抗生素和增加有效量的本发明的前药或其溶剂化物来增加哺乳动物中β-内酰胺抗生素的治疗有效性的方法。另外公开了通过向有需要的哺乳动物施用治疗有效量的本发明药物组合物来治疗哺乳动物细菌感染的方法。

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