트리아졸 화합물 및 이를 포함하는 결핵 치료용 약학 조성물
    3.
    发明公开
    트리아졸 화합물 및 이를 포함하는 결핵 치료용 약학 조성물 有权
    三唑化合物和药物组合物,用于治疗包括其的管状囊肿

    公开(公告)号:KR1020110046186A

    公开(公告)日:2011-05-04

    申请号:KR1020090103063

    申请日:2009-10-28

    Abstract: PURPOSE: A pharmaceutical composition containing triazole compounds for treating tuberculosis is provided to be used as an anti-tuberculosis therapeutic agent. CONSTITUTION: A triazole compound is denoted by chemical formula 1 or 2. In chemical formula 1 or 2, R1 is aryl or heteroaryl; R2 is hydroxy, keto, amino, azido, C1-16 alkyl amino, and C1-6 acyl amino group. A pharmaceutical composition for treating tuberculosis contains a triazole compound of chemical formula 1a or pharmaceutically acceptable salt thereof as an active ingredient.

    Abstract translation: 目的:提供含有用于治疗结核病的三唑化合物的药物组合物作为抗结核治疗剂。 组成:三唑化合物由化学式1或2表示。在化学式1或2中,R 1为芳基或杂芳基; R2是羟基,酮基,氨基,叠氮基,C1-16烷基氨基和C1-6酰基氨基。 用于治疗结核病的药物组合物含有化学式1a的三唑化合物或其药学上可接受的盐作为活性成分。

    β-아미노산 또는 아미노알콜 유도체의 합성 중간체로유용한 β-아지도 카보닐 화합물의 제조방법
    4.
    发明授权
    β-아미노산 또는 아미노알콜 유도체의 합성 중간체로유용한 β-아지도 카보닐 화합물의 제조방법 失效
    β-아미노산또는아미노알콜유도체의합성중체로β-β-β-β-β-β-β-β-β-β-β-β-β-β-β-β-β-

    公开(公告)号:KR100726673B1

    公开(公告)日:2007-06-11

    申请号:KR1020060033097

    申请日:2006-04-12

    Abstract: A method for preparing a beta-azido carbonyl compound is provided to obtain an intermediate useful for preparing beta-amino acids or aminoalcohols used in various medicines, particularly in beta-lactam antibiotics, HIV-protease inhibitor, etc., by a simple process with high efficiency. The method for preparing a beta-azido carbonyl compound represented by a formula 1 comprises a step of reacting an alpha, beta-unsaturated compound represented by a formula 2 with sodium azide in an organic solvent in the presence of hydrochloric acid and an organic catalyst. In the formulae 1 and 2, R1 is H or a C1-C6 alkyl; and R2 is H, a C1-C10 alkyl or hydroxy methyl substituted with benzyloxy, methyoxy or benzoyloxy, allyl group, or ester group.

    Abstract translation: 提供了用于制备β-叠氮基羰基化合物的方法以通过简单的方法获得用于制备用于各种药物,特别是β-内酰胺抗生素,HIV-蛋白酶抑制剂等中的β-氨基酸或氨基醇的中间体 高效率。 由式1表示的β-叠氮基羰基化合物的制备方法包括在盐酸和有机催化剂存在下,使式2表示的α,β-不饱和化合物与叠氮化钠在有机溶剂中反应的步骤。 在式1和2中,R1是H或C1-C6烷基; R2是H,被苄氧基,甲氧基或苯甲酰氧基,烯丙基或酯基取代的C1-C10烷基或羟甲基。

    2-아미노피리딘 유도체의 제조방법
    5.
    发明授权
    2-아미노피리딘 유도체의 제조방법 失效
    生产2-氨基吡啶衍生物的方法

    公开(公告)号:KR100574350B1

    公开(公告)日:2006-04-27

    申请号:KR1020040068822

    申请日:2004-08-31

    CPC classification number: C07D213/73 C07D213/77

    Abstract: 본 발명은 2-아미노피리딘 유도체를 제조하는 방법에 관한 것으로, 본 발명에 따라 3-치환-2,5,6-트리플루오르피리딘을 히드라진 일수화물과 반응시켜 히드라지노기를 도입시킨 후, 바로 수소로 환원반응 시키거나, 또는 히드라지노기를 탈리시킴으로써 불소 치환기 하나를 제거하고 다시 히드라진 일수화물과 반응시켜 히드라지노기를 도입시켜 수소로 환원반응 시키는 단계를 포함하는 2-아미노-3-플루오르피리딘 유도체를 제조하는 방법은, 저가의 원료물질들을 사용하여 산업적 적용이 용이한 공정을 통해 2-아미노피리딘 유도체를 고순도로 제조할 수 있으므로, CCR(cellular chemokine receptor: 세포화학수용체)5 모듈레이터(modulator)의 제조 뿐만 아니라 감염증 치료제(anti-infective agents)의 제조 등에 유용하게 활용될 수 있다.

    Abstract translation: 本发明介绍了作为2-氨基涉及一种用于制备吡啶衍生物的方法中,用一水合肼反应,3-取代-2,5,6-在根据本发明的肼基,直接氢三氟吡啶 通过消去基团进行还原反应,或肼通过引入肼制备2-氨基-3-氟吡啶衍生物,包括减少与氢的步骤中再次除去一个氟取代基和一水合肼,并将反应, 方法,使用低成本的原料,可以通过易于处理的工业应用来制造高纯度的2-氨基吡啶衍生物,CCR(蜂窝趋化因子受体:化学细胞受体)以及5-调制器(调制器)的制备 并且可以有用地用于生产抗感染剂。

    임의적으로 베타-위치가 치환된 알파-아릴알킬기의 제거를통해 3급 아미드 화합물로부터 2급 아미드 화합물을제조하는 방법
    6.
    发明授权
    임의적으로 베타-위치가 치환된 알파-아릴알킬기의 제거를통해 3급 아미드 화합물로부터 2급 아미드 화합물을제조하는 방법 失效
    임의적으로베타 - 위치가치환된알파 - 아릴알킬기의제거를를해3아미드화합물로부터2급아미드화합물을제조하는방법

    公开(公告)号:KR100395779B1

    公开(公告)日:2003-08-21

    申请号:KR1020010028837

    申请日:2001-05-25

    Abstract: PURPOSE: Provided is a preparation method of secondary amide in high purity and yield from tertiary amide by elimination of β-substituted α-arylalkyl group in reaction with protonic acid in organic solvent. The α-arylethylamine or α-aryl-β-substituted ethylamine is used as a nitrogen source in synthesis of biologically active compounds. CONSTITUTION: The synthesis of the secondary amide is characterized by making a tertiary amide represented by the formula(2) react with protonic acid in organic solvent to manufacture a secondary amine represented by the formula(1) by stirring at 10-150 deg.C for 2-24 hours. In the formulae, R1 is C1-5 alkyl, C3-7cycloalkyl, heterocyclic or C6-15 aryl group substituted with one or more groups selected from low alkyl with C1-4, hydroxy, animo, halogen, alkoxy, monoalkylamino, dialkylamino and carboxyl group; R2 is C1-5 alkyl group substituted with more than one group selected from amino, hydroxy, mono alkylamino, alkoxy and halogen; Ar is phenyl or α- or β-naphthyl group substituted by one or more groups selected from halogen, methoxy, carbamoyl, sulfamoyl, nitro group; R3 is C6-15 alkyl, phenyl or heterocyclic group substituted by one or more groups selected from C1-4 low alkyl, hydroxy, amino, halogen, alkoxy, mon alkylamino, dialkyl amino, carboxyl, carbamoyl, sulfamoyl, nitro or cyano group; and R1 and R3 are connected to form a 5 or 6 membered ring. The protonic acid is selected from hydrochloric acid, acetic acid, trifluoroacetic acid and methanesulfonic acid.

    Abstract translation: 目的:提供一种高纯度仲酰胺的制备方法,该方法通过在有机溶剂中与质子酸反应,消除β-取代的α-芳基烷基,由叔酰胺得到。 α-芳基乙胺或α-芳基-β-取代的乙胺用作合成生物活性化合物的氮源。 构成:仲酰胺的合成的特征在于,使式(2)所示的叔酰胺与质子酸在有机溶剂中反应,在10〜150℃下搅拌制造式(1)所示的仲胺 持续2-24小时。 在通式中,R 1是被一个或多个选自低级烷基和C 1-4羟基,氨基,卤素,烷氧基,单烷基氨基,二烷基氨基和羧基的基团取代的C 1-5烷基,C 3-7环烷基,杂环基或C 6-15芳基 组; R2是被选自氨基,羟基,一烷基氨基,烷氧基和卤素的多于一个基团取代的C1-5烷基; Ar是被一个或多个选自卤素,甲氧基,氨基甲酰基,氨磺酰基,硝基的基团取代的苯基或α-或β-萘基; R 3为C 6-15烷基,苯基或被一个或多个选自C 1-4低级烷基,羟基,氨基,卤素,烷氧基,单烷基氨基,二烷基氨基,羧基,氨基甲酰基,氨磺酰基,硝基或氰基的基团取代的杂环基; 并且R1和R3连接形成5或6元环。 质子酸选自盐酸,乙酸,三氟乙酸和甲磺酸。

    임의적으로 베타-위치가 치환된 알파-아릴알킬기의 제거를통해 3급 아미드 화합물로부터 2급 아미드 화합물을제조하는 방법

    公开(公告)号:KR1020020089873A

    公开(公告)日:2002-11-30

    申请号:KR1020010028837

    申请日:2001-05-25

    Abstract: PURPOSE: Provided is a preparation method of secondary amide in high purity and yield from tertiary amide by elimination of β-substituted α-arylalkyl group in reaction with protonic acid in organic solvent. The α-arylethylamine or α-aryl-β-substituted ethylamine is used as a nitrogen source in synthesis of biologically active compounds. CONSTITUTION: The synthesis of the secondary amide is characterized by making a tertiary amide represented by the formula(2) react with protonic acid in organic solvent to manufacture a secondary amine represented by the formula(1) by stirring at 10-150 deg.C for 2-24 hours. In the formulae, R1 is C1-5 alkyl, C3-7cycloalkyl, heterocyclic or C6-15 aryl group substituted with one or more groups selected from low alkyl with C1-4, hydroxy, animo, halogen, alkoxy, monoalkylamino, dialkylamino and carboxyl group; R2 is C1-5 alkyl group substituted with more than one group selected from amino, hydroxy, mono alkylamino, alkoxy and halogen; Ar is phenyl or α- or β-naphthyl group substituted by one or more groups selected from halogen, methoxy, carbamoyl, sulfamoyl, nitro group; R3 is C6-15 alkyl, phenyl or heterocyclic group substituted by one or more groups selected from C1-4 low alkyl, hydroxy, amino, halogen, alkoxy, mon alkylamino, dialkyl amino, carboxyl, carbamoyl, sulfamoyl, nitro or cyano group; and R1 and R3 are connected to form a 5 or 6 membered ring. The protonic acid is selected from hydrochloric acid, acetic acid, trifluoroacetic acid and methanesulfonic acid.

    Abstract translation: 目的:提供高纯度的仲酰胺的制备方法,通过在有机溶剂中与质子酸反应除去β-取代的α-芳烷基,由叔酰胺得到。 在生物活性化合物的合成中使用α-芳基乙胺或α-芳基-β-取代的乙胺作为氮源。 构成:仲酰胺的合成的特征在于使式(2)表示的叔酰胺与有机溶剂中的质子酸反应,通过在10-150℃下搅拌制造式(1)表示的仲胺 2-24小时。 在式中,R 1是被一个或多个选自具有C 1-4,羟基,脒,卤素,烷氧基,单烷基氨基,二烷基氨基和羧基的低级烷基取代的C 1-5烷基,C 3-7环烷基,杂环基或C 6-15芳基 组; R2是被多于一个选自氨基,羟基,单烷基氨基,烷氧基和卤素的基团取代的C1-5烷基; Ar是被一个或多个选自卤素,甲氧基,氨基甲酰基,氨磺酰基,硝基的基团取代的苯基或α-或β-萘基; R3是被一个或多个选自C1-4低级烷基,羟基,氨基,卤素,烷氧基,一个烷基氨基,二烷基氨基,羧基,氨基甲酰基,氨磺酰基,硝基或氰基的基团取代的C 6-15烷基,苯基或杂环基。 R1和R3连接形成5或6元环。 质子酸选自盐酸,乙酸,三氟乙酸和甲磺酸。

    1,3,5-위치가 치환된 2,4,6-트리요오드벤젠 유도체의 제조방법
    8.
    发明公开
    1,3,5-위치가 치환된 2,4,6-트리요오드벤젠 유도체의 제조방법 失效
    制备1,3,5-取代的2,4,6-三氢苯并噻吩衍生物的方法

    公开(公告)号:KR1020000019428A

    公开(公告)日:2000-04-06

    申请号:KR1019980037520

    申请日:1998-09-11

    Abstract: PURPOSE: A preparation method of 1,3,5-substituted 2,4,6-triiodobenzene derivatives by reacting 1,3,5-substituted benzene derivatives with iodine chloride(ICI) and a base is provided which gives a high-purity product in a high yield. CONSTITUTION: 2,4,6-Triiodobenzene derivatives(1) substituted in the 1,3,5-position are prepared by reacting 1,3,5-substituted benzene derivatives(2) with iodine chloride(ICI) and a base in a mixture solvent of methanol and dichloromethane(CH2Cl2) at 0-80°C for 0.5-60 hr. In formula, R1 is a hydroxy, amino or nitro group; R2, R3 are independently 1-5C alkyl, CO2R4 or COR5; R4 is H or C1-7 alkyl; R5 is 1-3C alkyl amino, -N(R6)CH2CH(OR7)CH2OR7, -N(R6)CH(CH2OR7)CH(OR7)CH(OR7)CH2OR7 or -N(R6)CH(CH2OR7)CHOR7(R6,R7 are independently H, 1-2C alkyl or 1-3C acyl). The mixture ratio of methanol to dichloromethane is 1: 1 - 10: 1. The product is useful as an important intermediate of a contrast medium of X-rays.

    Abstract translation: 目的:提供1,3,5-取代的2,4,6-三碘苯衍生物通过使1,3,5-取代的苯衍生物与碘化氯(ICI)和碱反应的制备方法,得到高纯度产物 以高收益。 构成:通过使1,3,5-取代的苯衍生物(2)与氯化碘(ICI)反应制得,在1,3,5-位上取代的2,4,6-三碘苯衍生物(1) 甲醇和二氯甲烷(CH 2 Cl 2)的混合溶剂在0-80℃下反应0.5-60小时。 在式中,R 1是羟基,氨基或硝基; R2,R3独立地为1-5C烷基,CO2R4或COR5; R4是H或C1-7烷基; R5是1-3C烷基氨基,-N(R6)CH2CH(OR7)CH2OR7,-N(R6)CH(CH2OR7)CH(OR7)CH(OR7)CH2OR7或-N(R6)CH(CH2OR7)CHOR7 ,R7独立地为H,1-2C烷基或1-3C酰基)。 甲醇与二氯甲烷的混合比为1:1〜10:1。该产品可用作X射线造影剂的重要中间体。

    퀴놀리진 카르복실산 유도체

    公开(公告)号:KR100241673B1

    公开(公告)日:2000-03-02

    申请号:KR1019970038037

    申请日:1997-08-09

    Abstract: 하기 화학식 1의 4-옥소-퀴놀리진-3-카르복실산 유도체, 그의 라세미 화합물, 거울상 이성질체 또는 입체 이성질체, 및 그의 제약학적으로 허용되는 염이 제공된다.

    식 중,
    R
    1 은 탄소 원자수 1 내지 4의 저급 알킬기, 할로겐으로 치환된 탄소 원자수 1 내지 4의 저급 알킬기 또는 탄소 원자수 1 내지 4의 저급 알콕시기이고,
    R
    2 는 고리형 아민이고,
    R
    3 , R
    4 , R
    5 , R
    6 , R
    7 , R
    8 , R
    9 , R
    10 , R
    11 , R
    12 , R
    13 및 R
    14 는 서로 동일하거나 또는 상이한 것으로서, 각각 H, 탄소 원자수 1 내지 4의 저급 알킬기, 또는 피리딜 또는 아릴로 치환된 탄소 원자수 1 내지 4의 저급 알킬기이다.

    신규한 퀴놀론카르복실산 유도체

    公开(公告)号:KR1019990052329A

    公开(公告)日:1999-07-05

    申请号:KR1019970071789

    申请日:1997-12-22

    Abstract: 본 발명은 하기 일반식(I)의 신규한 퀴놀론카르복실산 유도체 및 그의 약제학적으로 허용되는 염, 그의 제조방법 및 이를 활성 성분으로 함유하는 항균 조성물에 관한 것으로, 일반식(I)의 화합물은 항균력이 우수하고, 광범위한 항균 스펙트럼을 가지므로 항균제로 유용하다.

    (상기식에서, X, R
    1 , R
    2 , R
    3 , R
    4 , R
    5 및 R
    6 은명세서중에서 정의한 바와 같다).

Patent Agency Ranking