中科微点-全球专利检索

  1. Login
  2. Sign Up

Search Results

102 records (took 0.021 seconds)

    이미다졸린 고리가 치환된 카바페넴 유도체
    31.
    发明公开
    이미다졸린 고리가 치환된 카바페넴 유도체 失效
    用咪唑啉环取代的卡宾芬衍生物

    公开(公告)号：KR1020010077072A

    公开(公告)日：2001-08-17

    申请号：KR1020000004630

    申请日：2000-01-31

    Applicant: 한국과학기술연구원

    Inventor： 조정혁 ,  오창현 ,  이기수 ,  이창식 ,  이인규 ,  이숙자

    IPC: C07D477/20

    Abstract: PURPOSE: Provided are novel 1-β-methylcarbapenem derivatives substituted by pyrrolidine containing imidazoline ring which are strong antibiotics against resistant bacteria. CONSTITUTION: The compound is represented by chemical formula 1, where R is C1-6 low alkyl, aryl and benzyl group which are substituted by one or more groups from hydrogen, hydroxy, amine, sulfonyl and aminosulfonyl group. The process of preparing the compound consists of: converting diazoazetidione compound, chemical formula 2, to two ring keto ester under rhodium acetate catalyst and reacting at 0-5deg.C with diphenylchlorophosphate under base such as diisopropylethylamine; reacting the resultant with thiol derivative of chemical formula 3, and eliminating allyl group from the product by reacting with tributyltinhydride under tetrakisphosphine palladium(0) catalyst at room temp. for 2 hours. After reactions, distilled water is added to extract the water layer and it is freeze dried to get the final compound.

    Abstract translation: 目的：提供由吡咯烷咪唑啉环取代的新颖的1-β-甲基碳青霉烯衍生物，它们是抗性细菌的强抗生素。 构成：该化合物由化学式1表示，其中R为被氢，羟基，胺，磺酰基和氨基磺酰基中的一个或多个基团取代的C 1-6低级烷基，芳基和苄基。 制备化合物的方法包括：在乙酸铑催化剂下将二唑并二酮化合物，化学式2转化为两个环酮酯，并在0-5℃与二氯丙酸二苯酯在二异丙基乙胺的碱下反应; 使所得物与化学式3的硫醇衍生物反应，并在室温下在四膦合钯（0）催化剂下与三丁基氢化锡反应从产物中除去烯丙基。 2小时。 反应后，加入蒸馏水提取水层，冷冻干燥，得到最终的化合物。

    벤즈아미드 화합물 및 그 제조방법
    32.
    发明公开
    벤즈아미드 화합물 및 그 제조방법 失效
    苯并咪唑化合物及其制备方法

    公开(公告)号：KR1020010073626A

    公开(公告)日：2001-08-01

    申请号：KR1020000002390

    申请日：2000-01-19

    Applicant: 한국과학기술연구원

    Inventor： 조정혁 ,  오창현 ,  오창석 ,  변종수 ,  이숙자

    IPC: C07D307/00

    Abstract: PURPOSE: The benzamide compounds and a producing method thereof are provided, thereby the benzamide compounds can label technesium which is a radioisotope and F-18 with no having disadvantages of prior arts. CONSTITUTION: The benzamide compounds are represented by formula (1), in which R is methanesulfonyl, paratoluenesulfonyl or trifluoromethanesulfonyl. The compound of formula (1a) is produced by dissolving the compound of formula (7) in sulfonyl chloride, neutralizing the solution with sodium sulfate, and removing the solvent to produce the compound of formula (8); dissolving the compound of formula (8) in toluene, dropping thionyl chloride to the solution, removing the solvent by distilling under reduced pressure, dissolving it in organic solvent, and reacting the solution with the compound of formula (6) to produce the compound of formula (9); dissolving the compound of formula (9) in organic solvent and reacting the solution with boron tribromide to produce the compound of formula (10); and dissolving the compound of formula (10) in organic solvent and reacting the solution with methanesulfonyl chloride.

    Abstract translation: 目的：提供苯甲酰胺化合物及其制备方法，由此苯甲酰胺化合物可以标记作为放射性同位素的技术和不具有现有技术缺点的F-18。 构成：苯甲酰胺化合物由式（1）表示，其中R是甲磺酰基，对甲苯磺酰基或三氟甲磺酰基。 式（1a）化合物通过将式（7）化合物溶解在磺酰氯中，用硫酸钠中和溶液并除去溶剂以制备式（8）化合物来制备。 将式（8）化合物溶于甲苯中，将亚硫酰氯滴加至溶液中，通过减压蒸馏除去溶剂，将其溶解在有机溶剂中，并使该溶液与式（6）化合物反应，生成 公式（9）; 将式（9）化合物溶解在有机溶剂中，并使该溶液与三溴化硼反应，生成式（10）化合物; 并将式（10）的化合物溶于有机溶剂中，并使该溶液与甲磺酰氯反应。

    입체선택성 이중고리를 가지는 티올 유도체, 그의 제조방법 및그를 치환기로 갖는 카바페넴 유도체
    34.
    发明公开
    입체선택성 이중고리를 가지는 티올 유도체, 그의 제조방법 및그를 치환기로 갖는 카바페넴 유도체 无效
    具有立体选择性双环的THIOL衍生物及其制备方法，以及含有该取代基的CARBOPHENEM衍生物

    公开(公告)号：KR1020000020034A

    公开(公告)日：2000-04-15

    申请号：KR1019980038444

    申请日：1998-09-17

    Applicant: 한국과학기술연구원

    Inventor： 조정혁 ,  오창현 ,  이기수

    IPC: C07D477/04 ,  C07D487/04

    Abstract: PURPOSE: 1-beta-methyl-2-thiol carageen derivatives having thiol derivatives in 2-position are prepared which has a stability for DHP-1 enzyme. CONSTITUTION: Trans-L-hydroxyproline and potassium cyanate are dehydrogenated to give cyclized 7-hydroxy-1,3-diazabicyclo(3.3.0)octan-2,4-dione, followed by alkylation with alkyl halide and calcium carbonate, and treated with methyl sulfonyl chloride in the presence of triethyl amine to give a compound(formula 3). Obtained compound(3) is treated with potassium thioacetate and hydrolyzed by 4N-NaOH to give thiol derivatives(formula 1; R is lower allyl containing hydrogen, methyl, ethyl, propyl, butyl, and alkyl group containing hydroxy group such as benzyl, ethyl alcohol etc. 1-beta-methyl-2-thiol carageen derivatives(formula 2) are prepared from the thiol derivatives.

    Abstract translation: 目的：制备具有2-位巯基衍生物的1-β-甲基-2-硫醇卡拉胶衍生物，其对DHP-1酶具有稳定性。 构成：将反式-L-羟基脯氨酸和氰酸钾脱氢，得到环化的7-羟基-1,3-二氮杂双环（3.3.0）辛-2,4-二酮，然后用烷基卤和碳酸钙烷基化，并用 甲基磺酰氯在三乙胺存在下反应，得到化合物（式3）。 得到的化合物（3）用硫代乙酸钾处理，用4N-NaOH水解，得到硫醇衍生物（式1; R为含有氢，甲基，乙基，丙基，丁基和含有羟基的烷基的低级烯丙基，例如苄基，乙基 醇等。由硫醇衍生物制备1-β-甲基-2-硫醇卡拉胶衍生物（式2）。

    새로운 결정형을 갖는 7-아미노-3-비닐-세팔로스포린산염 수화물 및 이의 제조방법
    39.
    发明授权
    새로운 결정형을 갖는 7-아미노-3-비닐-세팔로스포린산염 수화물 및 이의 제조방법 有权
    具有新晶形的7-氨基-3-乙烯基头孢菌素水合物及其制备方法

    公开(公告)号：KR101061256B1

    公开(公告)日：2011-08-31

    申请号：KR1020090031068

    申请日：2009-04-10

    Applicant: 한국과학기술연구원

    Inventor： 오창현 ,  유병용 ,  김정훈 ,  유승원 ,  구대호

    IPC: C07D501/22 ,  C07D501/20 ,  C07D501/06 ,  C07D501/32

    CPC classification number: Y02P20/55

    Abstract: 본 발명은 새로운 결정형을 갖는 7-아미노-3-비닐-세팔로스포린산염 수화물 및 이의 제조방법에 관한 것으로, 구체적으로 Cu 타겟 방사의 X선 회절 패턴에서, 2θ로 표시된 특성피크가 8.98±0.3, 18.06±0.3, 28.95±0.3, 32.32±0.3, 33.76±0.3 및 34.40±0.3에서 나타나는 새로운 결정형태를 갖는 7-아미노-3-비닐-세팔로스포린산염 수화물 및 이의 제조방법에 관한 것이다. 본 발명에 의하면, 아미노기 보호기의 탈보호화 단계에서 취급이 용이하고 안정한 신타 CLEC-PA(Cross-Linked Enzyme Crystal-Penicilline G Amidase/Acylase) 효소를 이용하여 고순도, 고효율의 새로운 결정성 7-AVCA 수화물을 공업적으로 합성할 수 있어, 상기 7-AVCA를 중간체로 사용하는 세팔로스포린계 항생제 개발시 유용하게 사용될 수 있다.
    7-AVCA, 7-아미노-3-비닐-세팔로스포린산, 결정성 수화물, 신타 CLEC-PA 효소, 세파디니르

    Abstract translation: 本发明是7-氨基-3-乙烯基具有新晶形 - 涉及头孢菌素盐水合物和其制造方法，特别是在Cu辐射靶的X射线衍射图案，由2θ8.98＆plusmn表示特征峰; 0.3 它们的头孢盐水合物和生产方法 - 7-氨基-3-乙烯基一种具有新晶体形式可出现在0.3 ;, 18.06＆plusmn; 0.3，28.95＆plusmn; 0.3，32.32＆plusmn; 0.3，33.76＆plusmn; 0.3和34.40＆plusmn 它涉及。 根据本发明，容易在氨基保护基团和稳定合酶CLEC-PA（交联酶晶体，青霉素酰化酶/酰化酶）高纯度，高效率的新晶体的脱保护步骤使用酶促7- AVCA水合物处理 可以在工业规模上合成，7-AVCA一个可以有效地头孢菌素用作中间体开发抗生素时使用。

    단백질 키나아제 저해활성을 갖는 신규의 1,6-치환된 인돌 화합물
    40.
    发明公开
    단백질 키나아제 저해활성을 갖는 신규의 1,6-치환된 인돌 화합물 有权
    新颖的1,6-二取代吲哚化合物作为蛋白激酶抑制剂

    公开(公告)号：KR1020110045688A

    公开(公告)日：2011-05-04

    申请号：KR1020090102359

    申请日：2009-10-27

    Applicant: 한국과학기술연구원

    Inventor： 심태보 ,  함영진 ,  유경호 ,  오창현 ,  하정미 ,  최환근 ,  김환 ,  전은진

    IPC: C07D403/04 ,  C07D209/04 ,  A61K31/40 ,  A61P35/00

    CPC classification number: C07D403/04 ,  A61K31/404 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04

    Abstract: PURPOSE: A 1,6-substituted indole compound with an activity of suppressing protein kinase is provided to prevent and treat tumor caused by protein kinase. CONSTITUTION: A 1,6-substituted indole compound is denoted by chemical formula 1. A pharmaceutical composition contains the 1,6-subsituted indole compound as an active ingredient. The pharmaceutical composition is used for preventing and treating tumor disease caused by mechanism of protein kinase of Raf, KDR, Fms, Tie2, SAPK2a, Ret, Abl, Abl(T315I), ALK, Aurora A, Bmx, Src, EphA1, FGFR, Flt3, Itk, JAK2, Met, PDGFR, Plk, Ret, Syk, or Trk.

    Abstract translation: 目的：提供具有抑制蛋白激酶活性的1,6-取代吲哚化合物，以预防和治疗由蛋白激酶引起的肿瘤。 构成：1,6-取代的吲哚化合物由化学式1表示。药物组合物含有1,6-取代的吲哚化合物作为活性成分。 该药物组合物用于预防和治疗由Raf，KDR，Fms，Tie2，SAPK2a，Ret，Abl，Abl（T315I），ALK，Aurora A，Bmx，Src，EphA1，FGFR等蛋白激酶的机制引起的肿瘤疾病， Flt3，Itk，JAK2，Met，PDGFR，Plk，Ret，Syk或Trk。

Patent Agency Ranking