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    • 5. 发明申请
    • ANTIFUNGAL SUBSTITUTED PROPYL TRIAZOLE COMPOUND, ITS SALT, AND PREPARATION METHODS THEREOF
    • 反义替代丙三唑化合物及其盐及其制备方法
    • WO0189447A8
    • 2002-05-23
    • PCT/CN0100862
    • 2001-05-24
    • UNIV PLA 2ND MILITARY MEDICALLIU CHAOMEISUN QINGYAN
    • LIU CHAOMEISUN QINGYAN
    • C07D249/08C07D521/00A61K31/495C07D249/12C07D401/12C07D403/12C07D403/14
    • C07D231/12C07D233/56C07D249/08
    • The substituted propyl triazole compounds of formula (I) and the salts thereof having the structure (II): (I), (II) wherein X is hydrogen or alkyl group; M is hydrogen, hydroxy or ester group; Ar is selected from phenyl, naphthyl, thienyl, furyl, pyridyl and pyrimidinyl substituted by halogen, nitro group, trifluoromethyl or trifluoromethoxy group; L is hydrochloric acid, hydrobromic acid, methyl sulfonic acid, nitric acid, sulfuric acid, phosphoric acid, acetic acid, oxalic acid, maleic acid, citric acid, fumaric acid, gluconic acid, lactic acid, succinic acid, tartaric acid, malic acid: Y is (a) wherein R1-8 is selected from hydrogen, alkyl, cyano or ester group; Z is selected from N or CH; R is selected from (1)formacyl;(2)alkyl group;(3) benzyl or substituted benzyl group;(4)phenyl or substituted phenyl group. The compounds of formula (I) and formula (II) have wide-spectrum potent activity against systemic fungal infections, as well as have low toxicity.
    • 式(I)的取代的丙基三唑化合物及其具有结构(II)的盐:(I),(II)其中X是氢或烷基; M是氢,羟基或酯基; Ar选自被卤素,硝基,三氟甲基或三氟甲氧基取代的苯基,萘基,噻吩基,呋喃基,吡啶基和嘧啶基; L是盐酸,氢溴酸,甲基磺酸,硝酸,硫酸,磷酸,乙酸,草酸,马来酸,柠檬酸,富马酸,葡萄糖酸,乳酸,琥珀酸,酒石酸,苹果酸 :Y是(a)其中R1-8选自氢,烷基,氰基或酯基; Z选自N或CH; R选自(1)甲酰基;(2)烷基;(3)苄基或取代的苄基;(4)苯基或取代的苯基。 式(I)和式(II)的化合物对全身真菌感染具有广谱的有效活性,并具有低毒性。