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    • 65. 发明授权
    • 신규한 퀴놀론계 항균제 및 이의 제조방법
    • 신규한퀴놀론계항균제및이의제조방법
    • KR100463993B1
    • 2004-12-30
    • KR1020010088822
    • 2001-12-31
    • 한국화학연구원
    • 박태호이상호한철
    • C07D471/04
    • PURPOSE: Quinolone type antimicrobial agents and a preparation process thereof are provided, which compounds have improved antimicrobial activity and wide range of antimicrobial spectrum. CONSTITUTION: Quinolone type antimicrobial agents are represented by the formula 1, wherein R1 is C1-4 alkyl, halogen substituted or unsubstituted phenyl, or halogen substituted or unsubstituted C3-6 cycloalkyl; R2 is hydrogen, amino or C1-4 alkyl; R5 is hydrogen, C1-4 alkyl, C1-4 alkyl substituted or unsubstituted amino, or C1-4 alkyl substituted or unsubstituted aminomethyl or aminoethyl; W is nitrogen, CH or CY; Y is halogen, or halogen substituted or unsubstituted C1-4 alkyl or C1-4 alkoxy; and Pyr is 2-, 3- or 4-pyridyl, provided that W and R1 form COCH2CH(CH3), CCH2CH2CH(CH3) or CSCH2CH(CH3) together when W is CH. A process for preparing the quinolone type antimicrobial agents comprises condensation reacting a compound of the formula 2 with a compound of the formula 3, wherein X is halogen; and HA is hydrogen chloride or trifluoroacetic acid.
    • 目的:提供喹诺酮类抗菌剂及其制备方法,该化合物具有改善的抗微生物活性和广泛的抗微生物谱。 构成:喹诺酮类抗微生物剂由式1表示,其中R 1是C 1-4烷基,卤素取代或未取代的苯基或卤素取代或未取代的C 3-6环烷基; R2是氢,氨基或C1-4烷基; R5为氢,C1-4烷基,C1-4烷基取代或未取代的氨基或C1-4烷基取代或未取代的氨基甲基或氨基乙基; W是氮,CH或CY; Y是卤素或卤素取代或未取代的C 1-4烷基或C 1-4烷氧基; 并且Pyr是2-,3-或4-吡啶基,条件是当W是CH时,W和R1一起形成COCH2CH(CH3),CCH2CH2CH(CH3)或CSCH2CH(CH3)。 制备喹诺酮类抗微生物剂的方法包括使式2化合物与式3化合物缩合反应,其中X是卤素; HA是氯化氢或三氟乙酸。
    • 66. 发明公开
    • 신규한 퀴놀론계 항균제 및 이의 제조방법
    • 喹诺酮类抗微生物剂及其制备方法
    • KR1020030058394A
    • 2003-07-07
    • KR1020010088822
    • 2001-12-31
    • 한국화학연구원
    • 박태호이상호한철
    • C07D471/04
    • PURPOSE: Quinolone type antimicrobial agents and a preparation process thereof are provided, which compounds have improved antimicrobial activity and wide range of antimicrobial spectrum. CONSTITUTION: Quinolone type antimicrobial agents are represented by the formula 1, wherein R1 is C1-4 alkyl, halogen substituted or unsubstituted phenyl, or halogen substituted or unsubstituted C3-6 cycloalkyl; R2 is hydrogen, amino or C1-4 alkyl; R5 is hydrogen, C1-4 alkyl, C1-4 alkyl substituted or unsubstituted amino, or C1-4 alkyl substituted or unsubstituted aminomethyl or aminoethyl; W is nitrogen, CH or CY; Y is halogen, or halogen substituted or unsubstituted C1-4 alkyl or C1-4 alkoxy; and Pyr is 2-, 3- or 4-pyridyl, provided that W and R1 form COCH2CH(CH3), CCH2CH2CH(CH3) or CSCH2CH(CH3) together when W is CH. A process for preparing the quinolone type antimicrobial agents comprises condensation reacting a compound of the formula 2 with a compound of the formula 3, wherein X is halogen; and HA is hydrogen chloride or trifluoroacetic acid.
    • 目的:提供喹诺酮类抗微生物剂及其制备方法,该化合物具有改善的抗菌活性和广泛的抗菌谱。 组成:喹诺酮类抗微生物剂由式1表示,其中R1为C1-4烷基,卤素取代或未取代的苯基或卤素取代或未取代的C3-6环烷基; R2是氢,氨基或C1-4烷基; R5是氢,C1-4烷基,C1-4烷基取代或未取代的氨基或C1-4烷基取代或未取代的氨基甲基或氨基乙基; W是氮,CH或CY; Y是卤素,或卤素取代或未取代的C 1-4烷基或C 1-4烷氧基; 并且Pyr是2-,3-或4-吡啶基,条件是当W是CH时,W和R 1一起形成COCH 2 CH(CH 3),CCH 2 CH 2 CH(CH 3)或CSCH 2 CH(CH 3)。 制备喹诺酮型抗微生物剂的方法包括使式2化合物与式3化合物缩合反应,其中X为卤素; HA是氯化氢或三氟乙酸。