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    • 2. 发明申请
    • ALKYLIDINE SUBSTITUTED HETEROCYCLYL DERIVATIVES AS ANTI-BACTERIAL AGENTS
    • 作为抗菌剂的烷基取代的杂环衍生物
    • WO2015071780A1
    • 2015-05-21
    • PCT/IB2014/061104
    • 2014-04-30
    • AURIGENE DISCOVERY TECHNOLOGIES LIMITEDUM PHARMAUJI SDN. BHD
    • MOHAMED, TakhiHOSAHALLI, SubramanyaPANIGRAHI, Sunil Kumar
    • A61K31/00
    • C07D471/04
    • The present invention relates to alkylidine substituted heterocyclyl derivatives of formula (1) which may be therapeutically useful as as anti-bacterial agents, more particulalrly FabI inhibitors; I in which P, Q, Ri, R2, R3 and "n" have the same meanings given in the specification, and pharmaceutically acceptable salts or pharmaceutically acceptable stereoisomers thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage in inhibiting Enoyl-ACP reductase enzyme (FABI) activity. The present invention also provides methods for synthesizing and administering the FabI inhibitory compounds. The present invention also provides pharmaceutical formulations comprising at least one of the FabI inhibitory compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
    • 本发明涉及式(1)的烷基胺取代的杂环基衍生物,其可以作为抗细菌剂,更特别是FabI抑制剂; 其中P,Q,R 1,R 2,R 3和“n”具有与说明书中给出的相同的含义及其药学上可接受的盐或药学上可接受的立体异构体,其可用于治疗和预防疾病或病症, 用于抑制Enoyl-ACP还原酶(FABI)活性有优势的疾病或病症。 本发明还提供了合成和施用FabI抑制化合物的方法。 本发明还提供了包含至少一种FabI抑制化合物及其药学上可接受的载体,稀释剂或赋形剂的药物制剂。