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1. 发明申请

WO2016049586A2 NON-BETA LACTAM ANTIBIOTICS 审中-公开
标题翻译：非β-内酰胺类抗生素
公开(公告)号：WO2016049586A2
公开(公告)日：2016-03-31
申请号：PCT/US2015/052474
申请日：2015-09-25
申请人： UNIVERSITY OF NOTRE DAME DU LAC
发明人： CHANG, Mayland , MOBASHERY, Shahriar , SPINK, Edward , DING, Derong , TESTERO, Sebastian , LEEMANS, Erika , BOUDERAU, Mark
IPC分类号： A61K31/4439 , C07D413/04
CPC分类号： C07D413/04 , C07D271/06 , C07D471/04
摘要： The invention provides a newly discovered oxadiazole class of antibiotics. The oxadiazoles impair cell-wall biosynthesis and exhibit activities against the Gram-positive bacteria such as the bacterium Staphylococcus aureus, including methicillin-resistant S. aureus (MRSA) and vancomycin-resistant and linezolid-resistant S. aureus. For example, 5-(1H-indol-5-yl)-3-(4-(4-(trifluoromethyl)phenoxy)phenyl)-1,2,4-oxadiazole (antibiotic 75b) was efficacious in a mouse model of MRSA infection, exhibiting a long half-life, a high volume of distribution, and low clearance. Antibiotic 75b antibiotic is bactericidal and is orally bioavailable. This class of antibiotics can be used as a therapeutic agent against infections by Gram-positive bacteria such as MRSA.
摘要翻译：本发明提供了新发现的恶二唑类抗生素。恶二唑损害细胞壁生物合成并展现针对革兰氏阳性菌如金黄色葡萄球菌（包括耐甲氧西林金黄色葡萄球菌（MRSA）和万古霉素耐药和耐利奈唑胺金黄色葡萄球菌）的活性。例如，5-（1H-吲哚-5-基）-3-（4-（4-（三氟甲基）苯氧基）苯基）-1,2,4-恶二唑（抗生素75b）在MRSA小鼠模型中有效感染，表现出很长的半衰期，高分布和低清除率。抗生素75b抗生素是杀菌的，可口服生物利用。这类抗生素可用作抗革兰氏阳性菌如MRSA感染的治疗剂。

2. 发明公开

EP3197888A2 NON-BETA LACTAM ANTIBIOTICS 无效
标题翻译：非β-内酰胺类抗生素
公开(公告)号：EP3197888A2
公开(公告)日：2017-08-02
申请号：EP15843566.9
申请日：2015-09-25
申请人： University of Notre Dame du Lac
发明人： CHANG, Mayland , MOBASHERY, Shahriar , SPINK, Edward , DING, Derong , TESTERO, Sebastian , LEEMANS, Erika , BOUDREAU, Mark A.
IPC分类号： C07D413/04
CPC分类号： C07D413/04 , C07D271/06 , C07D471/04
摘要： The invention provides a newly discovered oxadiazole class of antibiotics. The oxadiazoles impair cell-wall biosynthesis and exhibit activities against the Gram-positive bacteria such as the bacterium Staphylococcus aureus, including methicillin-resistant S. aureus (MRSA) and vancomycin-resistant and linezolid-resistant S. aureus. For example, 5-(1H-indol-5-yl)-3-(4-(4-(trifluoromethyl)phenoxy)phenyl)-1,2,4-oxadiazole (antibiotic 75b) was efficacious in a mouse model of MRSA infection, exhibiting a long half-life, a high volume of distribution, and low clearance. Antibiotic 75b antibiotic is bactericidal and is orally bioavailable. This class of antibiotics can be used as a therapeutic agent against infections by Gram-positive bacteria such as MRSA.
摘要翻译：本发明提供了一种新发现的恶二唑类抗生素。恶二唑损害细胞壁生物合成并展现针对革兰氏阳性菌如金黄色葡萄球菌（包括耐甲氧西林金黄色葡萄球菌（MRSA）和万古霉素耐药和耐利奈唑胺金黄色葡萄球菌）的活性。例如，5-（1H-吲哚-5-基）-3-（4-（4-（三氟甲基）苯氧基）苯基）-1,2,4-恶二唑（抗生素75b）在MRSA小鼠模型中有效感染，表现出很长的半衰期，高分布和低清除率。抗生素75b抗生素是杀菌的，可口服生物利用。这类抗生素可用作抗革兰氏阳性细菌如MRSA感染的治疗剂。

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