公开(公告)号：EP3209669A1

公开(公告)日：2017-08-30

申请号：EP15787313.4

申请日：2015-09-16

申请人： Council of Scientific and Industrial Research

发明人： YEMPALLA, Kushalava Reddy ,  MUNAGALA, Gurunadham ,  SINGH, Samsher ,  SHARMA, Sumit ,  KHAN, Inshad Ali ,  VISHWAKARMA, Ram Asrey ,  SINGH, Parvinder Pal

IPC分类号： C07D498/04 ,  A61K31/424 ,  A61P31/06

CPC分类号： C07D498/04

摘要： The present invention relates to new generation of triazole functionality containing 6-nitro-2,3-dihydroimidazooxazole agents for general formula I, their method of preparation and their use as drugs for treatment of tuberculosis, MDR-TB and XDR-TB either alone or in combination with other anti-tubercular agents. In general formula l, X is selected from a group (CH2)nor a direct bond, where n is any number from 1-6,Y is selected from O, S or direct bond, R1 is selected from the group consisting of H, alkyl, substituted alkyl, aryl, substituted aryl, biaryl, substituted biaryl, heterocyclic and substituted heterocyclic, wherein the substituted heterocyclic is selected from any of the following rings consisting of piperazinyl, morpholinyl, piperidyl, pyridyl, triazolyl, triazinyl, pyrimidinyl, pyridazinyl, oxazolyl, furanyl, benzofuranyl, thiophenyl, pyrrolyl, imidazoyl, thiazoyl, quinolinyl, isoquinolinyl, benzooxazolyl and benzothiazolyl and the substitution on aryl and biaryl is selected from the group consisting of F, CI, Br, I, CF3, OCF3, OR11, NO2 and alkyl chain from C1 to C14, wherein R11 is selected from the group consisting of H, alkyl, phenyl and substituted phenyl.

摘要翻译： 本发明涉及新一代含有用于通式I的6-硝基-2,3-二氢咪唑并恶唑试剂的三唑官能团，其制备方法及其作为药物用于治疗结核病，MDR-TB和XDR-TB的药物，其单独或 与其他抗结核药物组合。 在通式1中，X选自基团（CH 2）或直接键，其中n是1-6的任何数，Y选自O，S或直接键，R 1选自H， 烷基，取代的烷基，芳基，取代的芳基，联芳基，取代的联芳基，杂环和取代的杂环，其中取代的杂环选自任何由哌嗪基，吗啉基，哌啶基，吡啶基，三唑基，三嗪基，嘧啶基，哒嗪基， 呋喃基，苯并呋喃基，噻吩基，吡咯基，咪唑基，噻唑基，喹啉基，异喹啉基，苯并恶唑基和苯并噻唑基，并且芳基和联芳基上的取代基选自F，Cl，Br，I，CF3，OCF3，OR11，NO2 和C1至C14的烷基链，其中R11选自H，烷基，苯基和取代的苯基。