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    • 7. 发明授权
    • 피페라진 유도체 및 그 제조방법
    • 피페라진유도체및그제조방법
    • KR100396738B1
    • 2003-09-03
    • KR1020007011876
    • 2000-03-03
    • 삼진제약주식회사
    • 조의환정순간이순환권호석강동욱주정호이영희
    • C07D295/108
    • C07D213/74C07D213/75C07D241/20C07D295/215
    • The present invention relates to a novel compound of the general formula (I) and its pharmaceutically acceptable acid addition salt, and process for the preparation thereof, which have strong antimumor activities and very low toxicity. wherein R1 and R2 are independently hydrogen, C1-C4 alkyl, C1-C4 alkylcarboxyl, C1-C4 alkylcarbonyl, C1-C4 alkoxy, C1-C4 hydroxyalkyl, C1-C4 aminoalkyl or C1-C4 hydroxyiminoalkyl, or R1 and R2 are fused to form C3-C4 unsaturated ring; R3, R4, R5, R6 and R7 are independently hydrogen, halogen, hydroxy, nitro, amino, C1-C4 alkyl, C1-C4 alkylcarboxyl, C1-C4 alkylcarbonyl, C1-C4 alkoxy or C1-C4 thioalkoxy; Y is amino, substituted amino or C1-C4 thioalkyl; Z is C1-C4 alkoxy, C1-C4 alkyl, C1-C4 alkylamino or C1-C4 thioalkoxy; X1 is CH and X2 is nitrogen;
    • 本发明涉及通式(I)的新型化合物及其药学上可接受的酸加成盐及其制备方法,其具有强的抗肿瘤活性和极低的毒性。 < CHEM> 其中R1和R2独立地为氢,C1-C4烷基,C1-C4烷基羧基,C1-C4烷基羰基,C1-C4烷氧基,C1-C4羟烷基,C1- 形成C3-C4不饱和环; R 3,R 4,R 5,R 6和R 7独立地为氢,卤素,羟基,硝基,氨基,C 1 -C 4烷基,C 1 -C 4烷基羧基,C 1 -C 4烷基羰基,C 1 -C 4烷氧基或C 1 -C 4硫代烷氧基; Y是氨基,取代的氨基或C 1 -C 4硫代烷基; Z是C1-C4烷氧基,C1-C4烷基,C1-C4烷基氨基或C1-C4硫代烷氧基; X1是CH且X2是氮;
    • 8. 发明公开
    • 피페라진 유도체 및 그 제조방법
    • 哌嗪衍生物及其制备方法
    • KR1020010043018A
    • 2001-05-25
    • KR1020007011876
    • 2000-03-03
    • 삼진제약주식회사
    • 조의환정순간이순환권호석강동욱주정호이영희
    • C07D295/108
    • C07D213/74C07D213/75C07D241/20C07D295/215
    • PURPOSE: Piperazine derivatives are provided for strong antitumor activities and very low toxicity. CONSTITUTION: Provided are a novel compound of general formula (I) and its pharmaceutically acceptable acid addition salt, and process for the preparation thereof, wherein R1 and R2 are independently hydrogen, C1-C4 alkyl, C1-C4 alkylcarboxyl, C1-C4 alkylcarbonyl, C1-C4 alkoxy, C1-C4 hydroxyalkyl, C1-C4 aminoalkyl or C1-C4 hydroxyiminoalkyl, or R1 and R2 are fused to form C3-C4 unsaturated ring; R3, R4, R5, R6 and R7 are independently hydrogen, halogen, hydroxy, nitro, amino, C1-C4 alkyl, C1-C4 alkylcarboxyl, C1-C4 alkylcarbonyl, C1-C4 alkoxy or C1-C4 thioalkoxy; R8 is C1-C4 alkyl; Y is oxygen, sulphur, amino, substituted amino or C1-C4 thioalkyl; Z is C1-C4 alkoxy, C1-C4 alkyl, C1-C4 alkylamino or C1-C4 thioalkoxy; X1 and X2 are independently carbon or nitrogen; and -N--C- and -C--Y- may form a single bond or a double bond provided that if -N--C- forms a single bond, -C--Y- forms a double bond, and if -C--Y- forms a single bond, -N--C- forms a double bond and R8 is nonexistent.
    • 目的:提供哌嗪衍生物用于强抗肿瘤活性和极低的毒性。 构成:提供通式(I)的新化合物及其药学上可接受的酸加成盐及其制备方法,其中R 1和R 2独立地为氢,C 1 -C 4烷基,C 1 -C 4烷基羧基,C 1 -C 4烷基羰基 C1-C4烷氧基,C1-C4羟烷基,C1-C4氨基烷基或C1-C4羟基亚氨基烷基,或R1和R2稠合形成C3-C4不饱和环; R3,R4,R5,R6和R7独立地是氢,卤素,羟基,硝基,氨基,C1-C4烷基,C1-C4烷基羧基,C1-C4烷基羰基,C1-C4烷氧基或C1-C4硫代烷氧基; R8是C1-C4烷基; Y是氧,硫,氨基,取代的氨基或C 1 -C 4硫代烷基; Z是C 1 -C 4烷氧基,C 1 -C 4烷基,C 1 -C 4烷基氨基或C 1 -C 4硫代烷氧基; X1和X2独立地为碳或氮; 和-N-C-和-C-Y-可以形成单键或双键,条件是如果-N-C-形成单键,则-C-Y-形成双键,如果 -C-Y-形成单键,-N-C-形成双键,并且R 8不存在。