公开(公告)号：US20100092443A1

公开(公告)日：2010-04-15

申请号：US12535865

申请日：2009-08-05

申请人： Premavathy Levasseur ,  John Lee Pace ,  Kenneth Coleman ,  John Lowther

发明人： Premavathy Levasseur ,  John Lee Pace ,  Kenneth Coleman ,  John Lowther

IPC分类号： A61K35/74 ,  A61K31/551 ,  A61K31/70 ,  A61K31/43 ,  A61K31/65 ,  A61K38/14 ,  A61K31/397 ,  A61K31/545 ,  A61P31/04

CPC分类号： C07D471/18

摘要： The invention relates to the combination of nitrogenated heterocyclic antibacterial compounds of formula (I) with other antibacterial compounds and the use of same as drugs.The nitrogenated heterocyclic compounds are of general formula (I) wherein R1 represents a (CH2)n-NH2 or (CH2)n—NHR radical, where R is a (C1-C6) alkyl and n is equal to 1 or 2; R2 represents a hydrogen atom; R3 and R4 together form an aromatic nitrogenated heterocycle with 5 apexes with 1, 2 or 3 nitrogen atoms optionally substituted by one or several R′ groups, R′ being selected in the group composed of a hydrogen atom and the alkyl radicals with 1 to 6 carbon atoms, in free form, as zwitterions, and in the form of salts of pharmaceutically acceptable inorganic or organic bases and acids. The other antibacterial compound is selected among the group comprised of beta-lactams, monobactams or penicillins, if needed combined with a beta lactamases inhibitor, aminoglycosides, glycylcyclines, tetracyclines, quinolones, glycopeptides, lipopeptides, macrolides, ketolides, lincosamides, streptogramins, oxazolidinones, polymyxins and other compounds known to have therapeutic activity on Pseudomonas aeruginosa and Enterobacteriaceae.

摘要翻译： 本发明涉及式（I）的氮化杂环抗菌化合物与其它抗菌化合物的组合及其与药物的用途。 氮化杂环化合物具有通式（I），其中R 1表示（CH 2）n -NH 2或（CH 2）n -NHR基，其中R是（C 1 -C 6）烷基，n等于1或2; R2表示氢原子; R3和R4一起形成具有5个具有1,2或3个氮原子的顶点的芳族氮杂环，任选被一个或几个R'基团取代，R'选自由氢原子组成的组，并且具有1至6个 游离形式的碳原子作为两性离子，并且为药学上可接受的无机或有机碱和酸的盐的形式。 如果需要与β-内酰胺酶抑制剂，氨基糖苷类，甘氨酰环素，四环素，喹诺酮类，糖肽，脂肽，大环内酯类，酮内酯，林可素，链霉素，恶唑烷酮类， 已知对铜绿假单胞菌和肠杆菌科具有治疗活性的多粘菌素和其它化合物。