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    • 2. 发明授权
    • 두 고리형 테트라하이드로퓨란 화합물과 이의 제조방법
    • 두고리형테트라하이드로퓨란화합물과이의제조방두
    • KR100645371B1
    • 2006-11-14
    • KR1020050061697
    • 2005-07-08
    • 한국과학기술연구원
    • 조용서배애님차주환고훈영신철
    • C07D493/04
    • Novel bicyclic tetrahydrofuran derivatives, and a process for preparing the same compounds are provided to improve efficiency of preparation, so that they are useful as intermediates for synthesis of natural products. The bicyclic tetrahydrofuran derivatives represented by the formula(1) are provided, wherein n is 1 or 2; R is phenyl group or substituted phenyl group by C1-C6 alkyl group, C1-C6 alkoxy group, hydroxy group or C1-C6 hydroxyalkyl group; and R1 is C1-C6 alkyl group. The bicyclic tetrahydrofuran derivatives represented by the formula(1) are prepared by intramolecular cyclizing tetrahydrofuran-allenol derivatives in the presence of alcohol compounds, transition metal catalyst and carbon monoxide(CO), wherein the transition metal catalyst is palladium chloride or copper chloride; and the reaction temperature is 0 to 25 deg.C.
    • 新型双环四氢呋喃衍生物及其制备方法可提高制备效率,因此它们可用作合成天然产物的中间体。 提供由式(1)表示的双环四氢呋喃衍生物,其中n是1或2; R 1为C 1 -C 6烷基,C 1 -C 6烷氧基,羟基或C 1 -C 6羟烷基的苯基或取代的苯基; 并且R 1是C 1 -C 6烷基。 由式(1)表示的双环四氢呋喃衍生物是在醇化合物,过渡金属催化剂和一氧化碳(CO)存在下通过分子内环化四氢呋喃 - 烯醇衍生物制备的,其中过渡金属催化剂为氯化钯或氯化铜; 反应温度为0〜25℃。
    • 4. 发明授权
    • 신규한 옥심계 아자 두 고리 화합물 및 그 제조방법
    • 신규한옥심계아자두고리화합물및그제조방법
    • KR100465277B1
    • 2005-01-13
    • KR1020020004200
    • 2002-01-24
    • 한국과학기술연구원
    • 고훈영최경일조용서배애님차주환공재양정대영
    • C07D453/02C07D471/08C07D261/06
    • PURPOSE: Azabicyclic compounds having an oxime moiety and a preparation method thereof are provided, which can be useful for treatment of cerebral nervous diseases caused by choline neurotransmission disorders including Alzheimer's disease. CONSTITUTION: An azabicyclic compounds having an oxime moiety represented by the formula(I) and pharmaceutically acceptable salts thereof are provided, wherein n is 1 or 2; m is 0 or 1; and R is at least one substituent selected from the group consisting of hydrogen, F, Cl, methoxy, OH, NH2, NO2, 3, 4-dimethoxy, 2, 4-dimethoxy, cyano, C1-C6 alkyl, 1, 2 or 3 fluorine atom substituted C1-C6 alkyl, 4-methoxybenzyloxy, t-butoxycarbonyl, C2-C6 alkenyl, 1, 2 or 3 fluorine atom substituted C2-C6 alkynyl, C3-C7 cycloalkyl and aromatic atom group, in which the aromatic atom group is selected from phenyl, 2- or 3-thienyl, 2- or 3-puridyl, 2- or 3-pyrrolyl; and the substituent of the aromatic atom group is selected from the group consisting of Cl, Br, F, trifluoromethyl, NH2, NO2 and C1-C4 straight or branched chain alkyl.
    • 目的:提供具有肟部分的氮杂双环化合物及其制备方法,其可用于治疗由包括阿尔茨海默病在内的胆碱神经传递障碍引起的脑神经疾病。 构成:提供了具有由式(I)表示的肟部分的氮杂双环化合物及其药学上可接受的盐,其中n是1或2; m是0或1; 和R是至少一个选自氢,F,Cl,甲氧基,OH,NH 2,NO 2,3,4-二甲氧基,2,4-二甲氧基,氰基,C 1 -C 6烷基,1,2或3个 3个氟原子取代的C 1 -C 6烷基,4-甲氧基苄氧基,叔丁氧基羰基,C 2 -C 6烯基,1,2或3个氟原子取代的C 2 -C 6炔基,C 3 -C 7环烷基和芳族原子基团, 选自苯基,2-或3-噻吩基,2-或3-嘌呤基,2-或3-吡咯基; 并且芳族原子基团的取代基选自Cl,Br,F,三氟甲基,NH 2,NO 2和C 1 -C 4直链或支链烷基。
    • 5. 发明授权
    • 신규한 알케닐 아자 두 고리 화합물 및 그 제조방법
    • 신규한알케닐아자두고리화합물및그제조방법
    • KR100441404B1
    • 2004-07-23
    • KR1020020004199
    • 2002-01-24
    • 한국과학기술연구원
    • 고훈영최경일조용서배애님차주환공재양정대영
    • C07D453/02C07D471/08C07D261/06
    • PURPOSE: An alkenyl azabicyclic compound and a preparation method thereof are provided, which can be useful for treatment of cerebral nervous diseases caused by choline neurotransmission disorders. CONSTITUTION: An alkenyl azabicyclic compound represented by the formula(I) and pharmaceutically acceptable salts thereof are provided, wherein n is 1 or 2; and R is selected from the group consisting of hydrogen, F, Cl, methoxy, OH, NH2, NO2, 3,4-dimethoxy, 2,4-dimethoxy, cyano, C1-C6 alkyl, 1, 2 or 3 fluorine substituted C1-C6 alkyl, 4-methoxybenzyloxy, t-butoxycarbonyl, C2-C6 alkenyl, 1, 2 or 3 fluorine substituted C2-C6 alkynyl and C3-C7 cyloalkyl. A method for preparing the alkenyl azabicyclic compound of the formula(I) comprises a compound of the formula(II) with a compound of the formula(III) or formula(IV), wherein R1, R2 and R3 are independently C1-C6 alkyl, aryl or arylalkyl.
    • 目的:提供烯基氮杂双环化合物及其制备方法,其可用于治疗由胆碱神经传递紊乱引起的脑神经疾病。 构成:提供由式(I)表示的烯基氮杂双环化合物及其药学上可接受的盐,其中n是1或2; 并且R选自氢,F,Cl,甲氧基,OH,NH 2,NO 2,3,4-二甲氧基,2,4-二甲氧基,氰基,C 1 -C 6烷基,1,2或3个氟取代的C 1 -C 6烷基,4-甲氧基苄氧基,叔丁氧基羰基,C 2 -C 6烯基,1,2或3个氟取代的C 2 -C 6炔基和C 3 -C 7环烷基。 用于制备式(I)的烯基氮杂双环化合物的方法包括式(II)的化合物与式(III)或式(IV)的化合物,其中R 1,R 2和R 3独立地为C 1 -C 6烷基 ,芳基或芳基烷基。
    • 6. 发明公开
    • 새로운 메틸리덴 피페리딘일 옥사졸리딘온 유도체 및이들의 제조방법
    • 甲基哌啶基氧杂环丁酮衍生物及其制备方法
    • KR1020040037686A
    • 2004-05-07
    • KR1020020066268
    • 2002-10-29
    • 한국과학기술연구원
    • 고훈영조용서배애님차주환김혜연이재석김학수김상희
    • C07D413/10
    • C07D413/10C07D413/14C07D417/14
    • PURPOSE: Methylidene piperidinyl oxazolidinone derivatives and a preparation method thereof are provided, which compounds have improved antimicrobial activity, so that they can be useful for treatment of infection of pathogenic bacteria having resistance to conventional antibiotics. CONSTITUTION: Methylidene piperidinyl oxazolidinone derivatives represented by the formula(1) or pharmaceutically acceptable salts thereof are provided, wherein X is oxygen or sulfur atom; R1 and R2 are independently hydrogen, cyano, alkyl, halogen, acetoxy, ethoxycarbonyl, hydroxy, hydroxyamino, methoxyimino, aminoethyl, or one or more hetero atom selected from oxygen, nitrogen and sulfur; and n is 1 or 2. The method for preparing the methylidene piperidinyl oxazolidinone derivatives of the formula(1) comprises reacting a compound of the formula(2) with a compound of the formula(3) in the presence of catalyst with or without organic solvent.
    • 目的:提供亚甲基哌啶基恶唑烷酮衍生物及其制备方法,该化合物具有改善的抗微生物活性,因此它们可用于治疗对常规抗生素具有抗性的病原菌的感染。 构成:提供由式(1)表示的亚甲基哌啶恶唑烷酮衍生物或其药学上可接受的盐,其中X是氧或硫原子; R 1和R 2独立地是氢,氰基,烷基,卤素,乙酰氧基,乙氧基羰基,羟基,羟基氨基,甲氧基亚氨基,氨基乙基或一个或多个选自氧,氮和硫的杂原子; 并且n为1或2.制备式(1)的亚甲基哌啶基恶唑烷酮衍生物的方法包括使式(2)化合物与式(3)化合物在催化剂存在或不与有机物 溶剂。
    • 7. 发明公开
    • 신규한 옥심계 아자 두 고리 화합물 및 그 제조방법
    • 含氧化合物的亚甲基化合物及其制备方法
    • KR1020030063854A
    • 2003-07-31
    • KR1020020004200
    • 2002-01-24
    • 한국과학기술연구원
    • 고훈영최경일조용서배애님차주환공재양정대영
    • C07D453/02C07D471/08C07D261/06
    • PURPOSE: Azabicyclic compounds having an oxime moiety and a preparation method thereof are provided, which can be useful for treatment of cerebral nervous diseases caused by choline neurotransmission disorders including Alzheimer's disease. CONSTITUTION: An azabicyclic compounds having an oxime moiety represented by the formula(I) and pharmaceutically acceptable salts thereof are provided, wherein n is 1 or 2; m is 0 or 1; and R is at least one substituent selected from the group consisting of hydrogen, F, Cl, methoxy, OH, NH2, NO2, 3, 4-dimethoxy, 2, 4-dimethoxy, cyano, C1-C6 alkyl, 1, 2 or 3 fluorine atom substituted C1-C6 alkyl, 4-methoxybenzyloxy, t-butoxycarbonyl, C2-C6 alkenyl, 1, 2 or 3 fluorine atom substituted C2-C6 alkynyl, C3-C7 cycloalkyl and aromatic atom group, in which the aromatic atom group is selected from phenyl, 2- or 3-thienyl, 2- or 3-puridyl, 2- or 3-pyrrolyl; and the substituent of the aromatic atom group is selected from the group consisting of Cl, Br, F, trifluoromethyl, NH2, NO2 and C1-C4 straight or branched chain alkyl.
    • 目的:提供具有肟部分的氮杂双环化合物及其制备方法,其可用于治疗由胆碱神经传递障碍(包括阿尔茨海默氏病)引起的脑神经疾病。 构成:提供具有由式(I)表示的肟部分及其药学上可接受的盐的氮杂双环化合物,其中n为1或2; m为0或1; R为至少一个选自氢,F,Cl,甲氧基,OH,NH2,NO2,3,4-二甲氧基,2,4-二甲氧基,氰基,C1-C6烷基,1,2或 3个氟原子取代的C1-C6烷基,4-甲氧基苄氧基,叔丁氧基羰基,C2-C6烯基,1,2或3个氟原子取代的C2-C6炔基,C3-C7环烷基和芳族原子基团,其中芳族原子团 选自苯基,2-或3-噻吩基,2-或3-取代基,2-或3-吡咯基; 芳基原子的取代基选自Cl,Br,F,三氟甲基,NH 2,NO 2和C 1 -C 4直链或支链烷基。