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    • 1. 发明申请
    • HETEROARYL DERIVATIVES HAVING ANTI-MYCOBACTERIAL ACTIVITY
    • 具有抗真菌活性的异氟烷衍生物
    • WO2006111716A1
    • 2006-10-26
    • PCT/GB2006/001378
    • 2006-04-13
    • ASTON UNIVERSITYPARKER, Katy, JaneRATHBONE, Daniel, LeeLAMBERT, Peter, AnthonyBILLINGTON, David, Charles
    • PARKER, Katy, JaneRATHBONE, Daniel, LeeLAMBERT, Peter, AnthonyBILLINGTON, David, Charles
    • C07D213/54C07D215/12C07D241/12A61K31/44A61K31/47A61K31/4965A61P31/00
    • C07D213/54C07D215/12C07D241/12
    • A compound of formula (I) where Het is selected from (2PY) (3PY) (4PY) (PZ) (QN) and (HD); (A) is formula (1) where X is O or S; R 1 is C 1-6 straight or branched alkyl, C 1-6 straight or branched alkoxy or alkylthio, C 1-6 straight or branched alkylcarbonyloxy, C 1-6 straight or branched alkyloxycarbonyl, phenyl, benzyl or phenyl(C 1-6 )alkyloxy, in each case the phenyl moiety itself being substituted or unsubstituted; and R 2 is H, C 1-6 straight or branched alkyl, C 1-6 alkylcarbonyl, phenyl, benzyl or arylcarbonyl (e.g. benzoyl), in each case the phenyl moiety itself being substituted or unsubstituted, and B is H, hydroxy, C 1-6 straight or branched alkyl, C 1-6 straight or branched alkoxy or alkylthio, C 1-6 straight or branched alkylcarbonyloxy, C 1-6 straight or branched alkyloxycarbonyl, cyano, amino, nitro, halo, phenyl, benzyl or phenyl(C 1-6 )alkyloxy, in each case the phenyl moiety itself being substituted or unsubstituted, and physiologically acceptable salts and complexes (e.g. metal complexes) thereof.
    • 其中Het选自(2PY)(3PY)(4PY)(PZ)(QN)和(HD))的式(I)化合物; (A)为式(1)其中X为O或S; R 1是C 1-6 - 直链或支链烷基,C 1-6 - 直链或支链烷氧基或烷硫基,C 1〜 6直链或支链烷基羰基氧基,C 1-6直链或支链烷氧基羰基,苯基,苄基或苯基(C 1-6 - )烷氧基,在每种情况下 苯基部分本身是取代或未取代的; 和R 2是H,C 1-6直链或支链烷基,C 1-6烷基羰基,苯基,苄基或芳基羰基(例如苯甲酰基 ),在每种情况下,苯基部分本身是取代或未取代的,并且B是H,羟基,C 1-16直链或支链烷基,C 1-6直链或 支链烷氧基或烷硫基,C 1-6直链或支链烷基羰基氧基,C 1-6直链或支链烷氧基羰基,氰基,氨基,硝基,卤素,苯基,苄基或苯基 (C 1-6)烷氧基,在各种情况下,苯基部分本身为取代或未取代的,以及其生理上可接受的盐和络合物(例如金属络合物)。