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    • 55. 发明公开
    • 신규 다중치환 벤즈옥사졸로 치환된 피리딘 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 이상세포 성장 질환의 예방 및 치료용 약학적 조성물
    • 取代多取代苯并噻唑或其药学上可接受的盐的新型吡啶衍生物,其制备方法和药物组合物,用于预防和治疗含有作为活性成分的异常细胞生长疾病
    • KR1020120100845A
    • 2012-09-12
    • KR1020120070944
    • 2012-06-29
    • 한국화학연구원
    • 김형래이정옥류재욱하재두조성윤정희정한선영이종국
    • C07D413/14A61K31/423A61K31/4427A61P35/00
    • PURPOSE: A pharmaceutical composition containing pyridine derivative subsituted with multiple substituted benzoxazole is provided to prevent and treat abnormal cell growth diseases. CONSTITUTION: A pyridine derivative substituted with multiple substituted benzoxazole is denoted by chemical formula 1. A method for preparing the derivative or pharmaceutically acceptable salt thereof comprises: a step of substituting a compound of chemical formula 2 to prepare a compound of chemical formula 4; a step of cyclizing the compound of chemical formula 4 to prepare a compound of chemical formula 5; a step of substituting the compound of chemical formula 5 to prepare a compound of chemical formula 6; a step of Suzuki coupling reaction of the compound of chemical formula 6 with a compound of chemical formula 7 to prepare a compound of chemical formula 8; a step of hydrogenation of the compound of chemical formula 8 to prepare a compound of chemical formula 9; a step of addition reaction of the compound of chemical formula 9 with a compound of chemical formula 10 to prepare a compound of chemical formula 11; and a step of deprotecting the compound of chemical formula 11.
    • 目的:提供含有由多取代苯并恶唑取代的吡啶衍生物的药物组合物,以预防和治疗异常的细胞生长疾病。 构成:用多取代的苯并恶唑取代的吡啶衍生物由化学式1表示。制备衍生物或其药学上可接受的盐的方法包括:用化学式2的化合物代替化学式4化合物的步骤; 使化学式4的化合物环化以制备化学式5的化合物的步骤; 用化学式5的化合物代替化学式6化合物的步骤; 化学式6的化合物与化学式7化合物的Suzuki偶联反应步骤,制备化学式8的化合物; 化学式8的化合物的氢化步骤,以制备化学式9的化合物; 化学式9的化合物与化学式10的化合物的加成反应步骤,制备化学式11的化合物; 以及使化学式11的化合物脱保护的工序。
    • 56. 发明公开
    • 테트라히드로이미다조피리딘기가 치환된 퀴놀리논 화합물
    • 喹诺酮类化合物取代四氢咪唑并吡啶类
    • KR1020110006171A
    • 2011-01-20
    • KR1020090063679
    • 2009-07-13
    • 한국화학연구원
    • 하재두한선영조성윤이종국이정옥김형래최상운
    • C07D403/04C07D403/02C07D487/04C07D487/02
    • PURPOSE: A tetrahydroimidazopyridine group-substituted novel quinolinone compound is provided to suppress vascular endothelial growth factor receptor(VEGFR) and flit 3(Flt3) and to treat abnormal cell growth diseases. CONSTITUTION: A tetrahydroimidazopyridine group-substituted quinolinone compound is denoted by chemical formula 1. The compound of chemical formula 1 is obtained by binding (4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine-2-yl)-acetic acid ethyl est compound of chemical formula 3 with 2-aminobenzaldehyde compound of chemical formula 2 under the presence of tertiary amine base. A pharmaceutical composition for treating tumor, psoriasis, rheumatism, diabetic retinosis contains the compound of chemical formula 1. The pharmaceutical composition is used in the form of oral administration or injection. The pharmaceutical composition is also used in the form of tablet, capsule, or powder. A therapeutic agent for psoriasis contains the compound of chemical formula 1.
    • 目的:提供四氢咪唑并吡啶基取代的新型喹啉酮化合物,以抑制血管内皮生长因子受体(VEGFR)和flit 3(Flt3),并治疗异常细胞生长疾病。 组成:化学式1表示四氢咪唑并吡啶基取代的喹啉酮化合物。化学式1化合物是通过将(4,5,6,7-四氢-1H-咪唑并[4,5-c]吡啶-2 - 基) - 乙酸乙酯,化学式3化合物与化学式2的2-氨基苯甲醛化合物在叔胺碱存在下反应。 用于治疗肿瘤,牛皮癣,风湿病,糖尿病性视网膜病变的药物组合物含有化学式1的化合物。药物组合物以口服给药或注射的形式使用。 药物组合物也以片剂,胶囊剂或粉剂的形式使用。 牛皮癣治疗剂含有化学式1的化合物。
    • 59. 发明公开
    • 이미다졸을 포함하는 이차아민으로 치환된 벤조피란유도체 및 그의 제조방법
    • 由含有咪唑的二级胺取代的苯并噻吩衍生物及其制备方法
    • KR1020040014023A
    • 2004-02-14
    • KR1020020047189
    • 2002-08-09
    • 한국화학연구원
    • 이규양이선경유성은서지희김낙정황선경김은숙이병호서호원이정옥최상운
    • C07D405/12
    • C07D405/12
    • PURPOSE: Benzopyran derivatives substituted by secondary amine containing imidazole and a method for preparing the same are provided. The compounds are useful for treatment of cancer, diabetic retinopathy and external brain wound. CONSTITUTION: Benzopyran derivatives substituted by secondary amine containing imidazole represented by the formula(1), partial stereo isomers thereof and pharmaceutically acceptable salts thereof are provided, wherein R1 is H, CN, NO2 or NH2; R2 is CH3, CHORaRa or CHOOZ; Ra is C1-C4 linear or branched chain alkyl; Z is C2-C6 linear or branched chain alkyl; R3 and R4 are independently H, Cl, Br, F, C1-C3 linear or branched chain alkyl, ORb, CF3, OCF3, NO2 or CO2Rb; Rb is H or C1-C3 alkyl; and * is chiral carbon. A method for preparing the compound of the formula(I) comprises reacting epoxide compounds of the formula(II) with imidazole containing secondary amine compounds of the formula(III) in the presence of metal salt and a solvent, wherein the metal salt is selected from Mg(ClO4)2, COCl2, LiClO4, NaClO4, CaCl2, ZnCl2, LiBF4 and Zn(Tf)2; and the solvent is selected from acetonitrile, tetrahydrofuran and dimethylformamide.
    • 目的:提供由含仲胺的咪唑取代的苯并吡喃衍生物及其制备方法。 该化合物可用于治疗癌症,糖尿病性视网膜病变和外部脑部伤口。 构成:提供由式(1)表示的含仲胺的咪唑取代的苯并吡喃衍生物,其部分立体异构体及其药学上可接受的盐,其中R1为H,CN,NO2或NH2; R2是CH3,CHORaRa或CHOOZ; Ra是C1-C4直链或支链烷基; Z是C 2 -C 6直链或支链烷基; R 3和R 4独立地为H,Cl,Br,F,C 1 -C 3直链或支链烷基,ORb,CF 3,OCF 3,NO 2或CO 2 R b; Rb是H或C 1 -C 3烷基; 和*是手性碳。 制备式(I)化合物的方法包括在金属盐和溶剂的存在下使式(II)的环氧化合物与含有式(III)的仲胺化合物的咪唑反应,其中选择金属盐 从Mg(ClO4)2,COCl2,LiClO4,NaClO4,CaCl2,ZnCl2,LiBF4和Zn(Tf)2; 溶剂选自乙腈,四氢呋喃和二甲基甲酰胺。
    • 60. 发明公开
    • 믹소첼린-에이를 유효성분으로 하는 항산화 및 항암용약학 조성물
    • 含有MYXOCHELIN-A作为有效成分的抗氧化剂和抗癌药物组合物
    • KR1020030005787A
    • 2003-01-23
    • KR1020010041239
    • 2001-07-10
    • 한국화학연구원
    • 안종웅이호현노재성이계형이정옥최상운권중호
    • A61K31/165
    • PURPOSE: A pharmaceutical composition containing myxochelin-A which exhibits excellent anticancer activity against human cancer cells, together with excellent antioxidant activity as a main component is provided which can be effectively used as an effective antioxidant and anticancer agent. CONSTITUTION: The pharmaceutical composition contains myxochelin-A of formula 1 obtained by being separated from myxobacteria or being chemically synthesized or semisynthesized. The myxochelin-A is purely separated by the steps of: separating a biomass and absorption resin by culturing Angiococcus disciformis strains as myxobacteria in the presence of absorption resin and centrifuging a culture solution; adding an organic solvent, preferably a mixed solvent of acetone and methanol; extracting and filtering to remove the biomass and absorption resin; preparing an active fraction by concentrating the filtrate under reduced pressure and extracting a crude extract in an organic solvent; and successively performing silica gel liquid chromatography and recycling preparative HPLC.
    • 目的:提供能够有效地用作有效的抗氧化剂和抗癌剂的含有对人类癌细胞具有优异抗癌活性的粘液素-A的药物组合物,以及优异的抗氧化活性为主要成分。 构成:药物组合物含有通过与粘液细菌分离或化学合成或半合成获得的式1的粘液素-A。 通过以下步骤纯化粘液素-A:通过在吸收树脂存在下培养球状球形细菌菌株作为粘液细菌分离生物质和吸收树脂并离心培养液; 加入有机溶剂,优选丙酮和甲醇的混合溶剂; 提取和过滤除去生物质和吸收树脂; 通过减压浓缩滤液并在有机溶剂中萃取粗提取物制备活性级分; 并依次进行硅胶液相色谱和再循环制备型HPLC。