신규한 1-[1-(3,4-디알콕시아릴)-피리딜메틸]-1H-피라졸화합물, 이의 제조방법 및 이를 포함하는 약제학적 조성물
    11.
    发明授权
    신규한 1-[1-(3,4-디알콕시아릴)-피리딜메틸]-1H-피라졸화합물, 이의 제조방법 및 이를 포함하는 약제학적 조성물 失效
    1- [1-(3,4-二甲氧基乙基) - 吡咯烷基] -1H-吡唑化合物,其制备方法和包含该化合物的药物组合物

    公开(公告)号:KR100833799B1

    公开(公告)日:2008-05-30

    申请号:KR1020070002725

    申请日:2007-01-10

    Abstract: 1-[1-(3,4-Dialkoxyaryl)-pyridylmethyl]-1H-pyrazole compounds are provided to inhibit activity of PDE-4(phosphodiesterase-4) with high activity and selectivity without side effects, so that the compounds are useful for treating inflammation diseases, neurodegenerative disease and cancers. 1-[1-(3,4-Dialkoxyaryl)-pyridylmethyl]-1H-pyrazole compounds represented by the formula(1) are provided, wherein A is N or CH; R1 is linear or branched, saturated or unsaturated (C1-C7)alkyl or halogen-substituted linear or branched, saturated or unsaturated (C1-C7)alkyl; R2 is hydrogen atom, (C3-C7)cycloalkyl or (C3-C8)cycloalkylmethyl; R3, R4 and R5 are each independently hydrogen atom, phenyl, pyridinyl, N-oxypyridinyl, linear or branched, saturated or unsaturated (C1-C7)alkyl, (C3-C7)cycloalkyl, (C3-C10)cycloalkyl(C1-C7)alkyl, halogen atom, cyano, nitro, amino, mono- or di(C1-C7)alkylamino, mono- or di(C1-C7)alkylaminocarbonyl, (C3-C7)cycloalkylamino, 3- to 7-membered saturated or unsaturated hetero ring containing oxygen, nitrogen or sulfur in hetero ring, guanidinyl, ureido, benzyl, benzyloxy, formyl, (C1-C7)alkanoyl, (C1-C7)alkoxy, (C1-C7)alkoxy(C1-C7)alkyl, hydroxy(C1-C7)alkyl, carboxyl or (C1-C7)alkoxycarbonyl; and R6 is pyridinyl or N-oxypyridinyl group.

    Abstract translation: 提供1- [1-(3,4-二烷氧基芳基) - 吡啶基甲基] -1H-吡唑化合物以抑制具有高活性和选择性的PDE-4(磷酸二酯酶-4)的活性而没有副作用,使得该化合物可用于 治疗炎症疾病,神经退行性疾病和癌症。 提供由式(1)表示的1- [1-(3,4-二烷氧基芳基) - 吡啶基甲基] -1H-吡唑化合物,其中A是N或CH; R1是直链或支链饱和或不饱和(C1-C7)烷基或卤素取代的直链或支链饱和或不饱和(C1-C7)烷基; R2是氢原子,(C3-C7)环烷基或(C3-C8)环烷基甲基; R 3,R 4和R 5各自独立地为氢原子,苯基,吡啶基,N-氧代吡啶基,直链或支链,饱和或不饱和的(C1-C7)烷基,(C3-C7)环烷基,(C3-C10)环烷基 )(C 1 -C 7)烷基氨基羰基,(C 3 -C 7)环烷基氨基,3至7元饱和或不饱和的(C 1 -C 7)烷基氨基, 杂环中含氧,氮或硫的杂环,胍基,脲基,苄基,苄氧基,甲酰基,(C1-C7)烷酰基,(C1-C7)烷氧基,(C1-C7)烷氧基(C1-C7) (C 1 -C 7)烷基,羧基或(C 1 -C 7)烷氧基羰基; R6是吡啶基或N-氧代吡啶基。

    약물에 의한 HERG 칼륨 채널의 억제 정도를 측정하는방법
    15.
    发明公开
    약물에 의한 HERG 칼륨 채널의 억제 정도를 측정하는방법 有权
    用于测量药物对草药通道的抑制的方法

    公开(公告)号:KR1020050029375A

    公开(公告)日:2005-03-28

    申请号:KR1020030065623

    申请日:2003-09-22

    Abstract: A method for measuring inhibition of a HERG potassium channel by drugs is provided, which inhibition of a HERG (human ether-a-go--go-related gene) potassium channel by drugs causes long QT syndrom(LQTS) that results in heart arrhythmia. The method for measuring inhibition of a HERG potassium channel by drugs comprises the steps of: (1) transforming a cell with a HERG gene; (2) treating the transformed cell with a drug; and (3) measuring the electric current from the HERG potassium channel expressed from the transformed cell using an extracellular solution and intracellular solution, wherein the gene HERG is isolated from a cDNA library of sea horse(Hippocampus sp.); the cell is a mammal cell; the extracellular solution comprises NaCl, KCl, HEPES, NaH2PO4, MgCl2, glucose and CaCl2; and the intracellular solution comprises KCl, MgCl2, EGTA, MgATP and HEPES.

    Abstract translation: 提供了一种通过药物测量HERG钾通道抑制的方法,药物导致的HERG(人类醚转运相关基因)钾通道的抑制导致长期QT综合征(LQTS),导致心律失常 。 测量药物对HERG钾通道抑制的方法包括以下步骤:(1)用HERG基因转化细胞; (2)用药物处理转化细胞; 和(3)使用细胞外溶液和细胞内溶液测量从转化细胞表达的HERG钾通道的电流,其中基因HERG从海马cDNA文库(Hippocampus sp。)中分离; 细胞是哺乳动物细胞; 细胞外溶液包含NaCl,KCl,HEPES,NaH2PO4,MgCl2,葡萄糖和CaCl2; 并且细胞内溶液包含KCl,MgCl 2,EGTA,MgATP和HEPES。

    항암활성을 가지는 아크리딘 유도체
    16.
    发明授权
    항암활성을 가지는 아크리딘 유도체 失效
    항암활성을가지는아크리딘유도체

    公开(公告)号:KR100381716B1

    公开(公告)日:2003-04-26

    申请号:KR1020000059346

    申请日:2000-10-09

    Abstract: PURPOSE: Provided are acridine derivatives having an anticancer activity, their pharmaceutically acceptable salts, their manufacturing method and their use for an anticancer agent. CONSTITUTION: The acridine derivative is represented by the formula(1) and has an anticancer activity and low toxicity, wherein X1 and X2 are the same or different from each other and represent methylene(CH2) or hetero atom; R1, R2 and R3 are the same or different from each other and represent hydrogen atom or C1-6 linear, branched or circular alkyl; and R4 and R3 are the same or different from each other and represent hydrogen atom, C1-6 linear, branched or circular alkyl, phenyl or hetero aromatic group including a hetero atom.

    Abstract translation: 用途:提供具有抗癌活性的吖啶衍生物,其药学上可接受的盐,其制备方法和它们在抗癌剂中的用途。 构成:吖啶衍生物由式(1)表示,具有抗癌活性和低毒性,其中X1和X2彼此相同或不同,代表亚甲基(CH2)或杂原子; R1,R2和R3彼此相同或不同,并且表示氢原子或C1-6直链,支链或环状烷基; R4和R3彼此相同或不同,并且表示氢原子,C1-6直链,支链或环状烷基,苯基或包含杂原子的杂芳族基团。

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