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    • 3. 发明公开
    • 간 섬유화 억제작용을 나타내는 벤조[3,4-d]1,3-디옥솔란 유도체
    • 含有BENZO(3,4-D)1,3-DIOXOLAN衍生物的IVER纤维蛋白酶抑制组合物
    • KR1020010039263A
    • 2001-05-15
    • KR1019990047570
    • 1999-10-29
    • 제이더블유중외제약 주식회사
    • 문성환황태섭이수진정재욱이희윤김병규하종렬김대훈
    • C07D317/02
    • PURPOSE: A liver fibrosis inhibiting composition containing benzo(3,4-d) 1,3-dioxolan derivatives is provided for the inhibition and treatment of liver fibrosis in damaged liver. CONSTITUTION: The liver fibrosis inhibiting composition contains benzo(3,4-d) 1,3-dioxolan derivatives represented by formula (1), in which D is ethylthio, acethylthio, hydroxyethylthio, or any one compound selected from the compound of the formula (a-1) to (a-8), wherein R1, R1', R3 and R3' are independently hydrogen, hydroxy, lower alkyl, lower alkoxy, or carboxy, or R1 and R1' or R3 and R3' are individually oxo, lower alkyliden, lower alkoxyimino or hydroxyimino; R2 is hydrogen, lower alkyl substituted or unsubstituted with halogen, aryl, ar- lower alkyl, 5 to 6 ring heteroaryl containing hetero selected from nitrogen, oxygen and sulfur; R4, R6, R7 and R8 are individually hydrogen, lower alkoxy, hydroxycarbonyl, lower alkoxycarbonyl, lower ethylcarbamoyl, lower alkenylcarbamoyl, lower alkylidencarbamoyl or tri(lower alkyl)sillyl, or lower alkyl or aryl substituted or unsubstituted with halogen, hydroxy or lower alkoxy, 5 to 6 ring heteroaryl substituted or unsubstituted with hydroxy and carboxy and having at least one nitrogen; and R5 is hydrogen, halogen, nitro, cyano, hydroxy, lower alkoxy, amino, lower alkanoylamino, carboxy or lower alkoxycarbonyl.
    • 目的:提供含有苯并(3,4-d)1,3-二氧戊环衍生物的肝纤维化抑制组合物,用于抑制和治疗受损肝脏的肝纤维化。 构成:肝纤维化抑制组合物含有式(1)所示的苯并(3,4-d)1,3-二氧戊环衍生物,其中D为乙硫基,乙硫基,羟乙硫基,或选自式 (a-1)至(a-8),其中R1,R1',R3和R3'独立地是氢,羟基,低级烷基,低级烷氧基或羧基,或R1和R1'或R3和R3' ,低级亚烷基,低级烷氧基亚氨基或羟基亚氨基; R 2是氢,被卤素,芳基,芳基 - 低级烷基取代或未取代的低级烷基,含有选自氮,氧和硫的杂原子的5至6个环杂芳基; R4,R6,R7和R8分别是氢,低级烷氧基,羟基羰基,低级烷氧基羰基,低级乙基氨基甲酰基,低级链烯基氨基甲酰基,低级亚烷基氨基甲酰基或三(低级烷基)甲硅烷基,或被卤素,羟基或低级烷氧基取代或未取代的低级烷基或芳基 5至6个被羟基和羧基取代或未取代的且具有至少一个氮的环杂芳基; R 5为氢,卤素,硝基,氰基,羟基,低级烷氧基,氨基,低级烷酰氨基,羧基或低级烷氧基羰基。
    • 8. 发明公开
    • (E)-엔올티오에테르 유도체의 입체 선택적 제조방법
    • (E) - 醚衍生物
    • KR1019960007606A
    • 1996-03-22
    • KR1019940019644
    • 1994-08-10
    • 제이더블유중외제약 주식회사
    • 심영기황태섭이미정권희안송태흥
    • C07F7/08
    • 본 발명에 따르면, L-트레오닌의 유리 2차 히드록시기를 트리알킬실릴기로 보호한 다음, 보호된 L-트레오닌 유도체(Ⅰ)를 닌히드린으로 감성화(degradation)시켜 (2R)-2-(트리알킬실릴옥시)프로판알(Ⅱ)을 합성하고, 디알킬포스포네이트, 디아릴포스핀옥사이드 및 트리아릴포스포늄 등의 유기 인 화합물을 강염기로 처리하여 수득되는 안정화 포스포네이트 일리드, 포스핀옥사이드 일리드 또는 포스포늄 일리드와 상기 수득된 알데히드(Ⅱ)를 반응시키는 오너-워즈워드-애몬스(HWE) 반응에 의해 (E)-(3R)-3-t-부틸디메틸실릴옥시-1-페닐티오-1-부텐, (E)-(3R)-3-t-부틸디메틸실릴옥시-1-(p-메톡시페닐티오)-1-부텐, (E)-(3R)-3-t-부틸디메틸실릴옥시-1-(p-클로로페닐티오)-1-부텐 및 (E)-(3R)-3-t-부틸디메틸실릴옥시-1-1-(p-메틸페닐티오)-1-부텐등의 (E)-엔올티오에테르 유도체(Ⅳ)를 입체 선택적으로 제조하는 방법이 제공된다.
      본 발명은 종래의 제조 방법들에 비하여, 값싼 α-아미노산인 L-트레오닌을 출발물질로하여 짧은 제조공정을 거쳐 목적 화합물(Ⅳ)를 수득함으로써 제조원가를 낮출 수 있고 기존의 제조 방법에 비해 (E )-엔올티오에테르 유도체들을 높은 입체선택성으로 제조할 수 있다는 장점을 갖는다.
    • 9. 发明公开
    • 테트라플루오로벤질 아닐린 유도체 및 이의 약학적으로허용가능한 염 화합물의 제조방법
    • 取代的四氢呋喃并嘧啶化合物的制备方法及其药物批准的盐
    • KR1020060121768A
    • 2006-11-29
    • KR1020060047284
    • 2006-05-25
    • 제이더블유중외제약 주식회사
    • 황태섭김현규
    • C07C213/02
    • C07C227/04C07C229/64C07C251/24
    • Provided is a method for preparing substituted tetrafluorobenzylaniline derivatives and pharmaceutically acceptable salts thereof, which inhibits the formation of dimer impurities and provides tetrafluorobenzylaniline derivatives having storage stability and reduced toxicity. The method for preparing a substituted tetrafluorobenzylaniline compound represented by the following formula I and pharmaceutically acceptable salts thereof comprises the steps of: subjecting tetrafluorobenzyl alcohol to an oxidation reaction to prepare tetrafluorobenzaldehyde; subjecting the prepared tetrafluorobenzaldehyde and 5-amino-salicylic acid to dehydration condensation to prepare a tetrafluorobenziridine-5-aminosalicylic acid compound represented by the following formula II; and subjecting the tetrafluorobenziridine-5-aminosalicylic acid compound to hydrogenation.
    • 提供了制备取代的四氟苄苯胺衍生物及其药学上可接受的盐的方法,其抑制二聚体杂质的形成,并提供具有储存稳定性和降低的毒性的四氟苄基苯胺衍生物。 由下式I表示的取代的四氟苄基苯胺化合物及其药学上可接受的盐的制备方法包括以下步骤:使四氟苄醇进行氧化反应以制备四氟苯甲醛; 将所制备的四氟苯甲醛和5-氨基水杨酸进行脱水缩合,制备由下式II表示的四氟苯并吡啶-5-氨基水杨酸化合物; 并使四氟苯并吡啶-5-氨基水杨酸化合物氢化。