제초활성을 갖는 5-벤질옥시메틸-1,2-이속사졸린 유도체 및 이를 유효성분으로 포함하는 제초제 조성물
    63.
    发明授权
    제초활성을 갖는 5-벤질옥시메틸-1,2-이속사졸린 유도체 및 이를 유효성분으로 포함하는 제초제 조성물 有权
    具有除草活性的新型5-苄氧基甲基-1,2-异恶唑啉衍生物和包含其的除草组合物

    公开(公告)号:KR101124231B1

    公开(公告)日:2012-04-12

    申请号:KR1020090044042

    申请日:2009-05-20

    Abstract: 본 발명은 제초활성을 갖는 이속사졸린 유도체 및 이를 유효성분으로 포함하는 제초제 조성물에 관한 것으로, 상세하게는 하기 화학식 1로 표시되는 5-벤질옥시메틸-1,2-이속사졸린 유도체 및 이를 유효성분으로 포함하는 제초제 조성물에 관한 것이다.
    [화학식 1]

    [상기 화학식 1에서, A는 또는 이고;
    R
    1 , X
    1 , X
    2 , X
    3 , Y
    1 , Y
    2 및 Y
    3 는 각각 발명의 상세한 설명에서 정의한 바와 같다.]
    본 발명의 5-벤질옥시메틸-1,2-이속사졸린 유도체는 각종 잡초에 대한 제초활성이 우수할 뿐만 아니라, 낮은 농도에서 높은 제초활성을 보이므로, 안전성이 높은 제초제로 사용될 수 있다.
    5-벤질옥시메틸-1,2-이속사졸린 유도체, 제초제

    제초활성을 갖는 5-벤질옥시메틸-1,2-이속사졸린 유도체 및 이를 유효성분으로 포함하는 제초제 조성물
    64.
    发明公开
    제초활성을 갖는 5-벤질옥시메틸-1,2-이속사졸린 유도체 및 이를 유효성분으로 포함하는 제초제 조성물 有权
    新颖的5-苄氧基甲基-1,2-异辛唑衍生物,其具有除味活性和包含其的除草剂组合物

    公开(公告)号:KR1020100125042A

    公开(公告)日:2010-11-30

    申请号:KR1020090044042

    申请日:2009-05-20

    Abstract: PURPOSE: An isoxasoline derivative and herbicidal composition containing the same are provided to enhance high safety and herbicidal activity at low concentration. CONSTITUTION: A 5-benxyloxymethyl-1,2-isoxazoline derivative is denoted by chemical formula 1, 2 or 3. The composition further contains insecticidal agent, fungicidal agent, nematocidal agent, fertilizer or other herbicidal agent. A herbicidal composition contains 5-benzyloxymethyl-1,2-isoxasoline derivative as an active ingredient.

    Abstract translation: 目的:提供含有它们的异恶唑啉衍生物和除草组合物,以提高低浓度下的高安全性和除草活性。 构成:5-苯氧基甲基-1,2-异恶唑啉衍生物由化学式1,2或3表示。该组合物还含有杀虫剂,杀真菌剂,杀线虫剂,肥料或其它除草剂。 除草组合物含有5-苄氧基甲基-1,2-异唑啉衍生物作为活性成分。

    신규한 1-[1-(3,4-디알콕시벤질)-1H-피롤 화합물, 이의제조방법 및 이를 포함하는 천식 및 만성폐쇄성 폐질환을포함한 염증관련 질환, 관절염, 아토피 피부염, 암 및뇌질환의 치료 및 예방을 위한 약제학적 조성물
    66.
    发明公开
    신규한 1-[1-(3,4-디알콕시벤질)-1H-피롤 화합물, 이의제조방법 및 이를 포함하는 천식 및 만성폐쇄성 폐질환을포함한 염증관련 질환, 관절염, 아토피 피부염, 암 및뇌질환의 치료 및 예방을 위한 약제학적 조성물 失效
    1- [1-(3,4-二甲氧基苄基)-1H-吡咯烷酮化合物,其制备方法和药物组合物,用于治疗或预防哮喘,慢性阻塞性肺动脉疾病,ARTHRITIS,原发性恶性肿瘤,包括其的肿瘤和变应性脑疾病

    公开(公告)号:KR1020090058752A

    公开(公告)日:2009-06-10

    申请号:KR1020070125491

    申请日:2007-12-05

    Abstract: A 1-[1-(3,4-dialkoxybenzyl)-1H-pyrrole compound is provided to obtain excellent inhibition activity to PDE-4 enzyme and high enzyme selectivity. A 1-[1-(3,4-dialkoxybenzyl)-1H-pyrrole compound is denoted by the chemical formula 1. In the chemical formula 1, R1 and R2 are different or same. The R1 and R2 are individually hydrogen, saturated or unsaturated alkyl(C1-C7) of straight chain and branch chain, saturated or unsaturated alkyl(C1-C7) of straight chain and branch chain containing oxygen, nitrogen or sulfur, cycloalkyl of C3-C7, and cycloalkyl of C3-C7 containing oxygen, nitrogen, or sulfur. R1 and R2 is connected with (C1 - C3) alkylene or (C1 - C3) alkylene containing halogen.

    Abstract translation: 提供1- [1-(3,4-二烷氧基苄基)-1H-吡咯化合物以获得对PDE-4酶的优异抑制活性和高酶选择性。 化学式1表示1- [1-(3,4-二烷氧基苄基)-1H-吡咯化合物。在化学式1中,R 1和R 2不同或相同。 R1和R2分别是氢,饱和或不饱和的直链和支链烷基(C1-C7),含有氧,氮或硫的直链和支链的饱和或不饱和烷基(C1-C7),C3- C7和含有氧,氮或硫的C3-C7的环烷基。 R1和R2与(C1-C3)亚烷基或(C1-C3)亚烷基的卤素连接。

    1-[1-(3,4-디알콕시아릴)-피리딜메틸]-1H-피라졸 화합물의제조방법
    69.
    发明授权
    1-[1-(3,4-디알콕시아릴)-피리딜메틸]-1H-피라졸 화합물의제조방법 失效
    制备1- [1-(3,4-二氮代烷基) - 吡咯烷基] -1H-吡唑化合物的方法

    公开(公告)号:KR100838702B1

    公开(公告)日:2008-06-16

    申请号:KR1020070013408

    申请日:2007-02-08

    Abstract: A method for preparing a 1-[1-(3,4-dialkoxyaryl)-pyridylmethyl]-1H-pyrazole compound is provided to produce a desired product with high purity economically and industrially compared with a method for separating the desired product using a chiral column. A method for preparing a 1-[1-(3,4-dialkoxyaryl)-pyridylmethyl]-1H-pyrazole compound represented by a formula(1) comprises the steps of: (a) subjecting an aryl aldehyde compound represented by a formula(2) and 2-methyl-2-propanesulfinamide to condensation in the presence of titanium ethoxide(Ti(OEt)4) to prepare a compound represented by a formula(4); (b) reacting the compound of the formula(4) with a compound represented by a formula(5) to prepare a compound represented by a formula(6); (c) removing a sulfinyl group of the compound of the formula(6) under acidic condition to prepare an amine compound represented by a formula(7); (d) reacting the compound of the formula(7) with a compound represented by a formula(8) to prepare a cis-type compound represented by a formula(9); and (e) after N-aminating the cis-type compound of the formula(9) by dropping amino 4-nitrobenzoate represented by a formula(10) therein in the existence of a strong base, cyclizing the N-aminated compound to prepare the compound of the formula(1). In the formulae, A is CH; R1 is linear or branched saturated or unsaturated C1-7 alkyl which may be substituted or unsubstituted by halogen; R2 is C3-7 cycloalkyl or (C3-10)cycloalkyl(C1-7)alkyl; and R3 is phenyl which may be substituted by at least one substituent selected from the group consisting of C1-7 alkyl, C3-7 cycloalkyl, (C3-10)cycloalkyl(C1-7)alkyl, C1-7 alkoxy, (C1-7)alkoxy(C1-7)alkyl, (C1-7)alkylsiloxy(C1-7)alkyl, C1-5 alkoxycarbonyl, benzyloxy, halogen, nitro, cyano, C1-7 alkylsiloxy, carboxyl and formyl.

    Abstract translation: 提供了一种制备1- [1-(3,4-二烷氧基芳基) - 吡啶基甲基] -1H-吡唑化合物的方法,与使用手性的分离所需产物的方法相比,在经济和工业上产生具有高纯度的所需产物 柱。 制备由式(1)表示的1- [1-(3,4-二烷氧基芳基) - 吡啶基甲基] -1H-吡唑化合物的方法包括以下步骤:(a)使由式 2)和2-甲基-2-丙磺酰胺在乙醇钛(Ti(OEt)4)存在下缩合以制备由式(4)表示的化合物; (b)使式(4)的化合物与式(5)表示的化合物反应,制备由式(6)表示的化合物; (c)在酸性条件下除去式(6)化合物的亚磺酰基以制备由式(7)表示的胺化合物; (d)使式(7)的化合物与式(8)表示的化合物反应,制备由式(9)表示的顺式化合物; 和(e)通过在存在强碱的情况下滴加由式(10)表示的式(10)表示的氨基-4-硝基苯甲酸将式(9)的顺式式化合物N-胺化后,使N-胺化化合物环化以制备 式(1)的化合物。 在式中,A为CH; R1是可被卤素取代或未取代的直链或支链饱和或不饱和C 1-7烷基; R2是C3-7环烷基或(C3-10)环烷基(C1-7)烷基; 并且R 3是可以被至少一个选自C 1-7烷基,C 3-7环烷基,(C 3-10)环烷基(C 1-7)烷基,C 1-7烷氧基, 7)烷氧基(C 1-7)烷基,(C 1-7)烷基甲硅烷氧基(C 1-7)烷基,C 1-5烷氧基羰基,苄氧基,卤素,硝基,氰基,C 1-7烷基甲硅烷氧基,羧基和甲酰基。

    1,2,4-티아다이아졸리딘-3,5-다이온 화합물을 포함하는염증관련 질환의 치료 및 예방을 위한 약제학적 조성물
    70.
    发明授权
    1,2,4-티아다이아졸리딘-3,5-다이온 화합물을 포함하는염증관련 질환의 치료 및 예방을 위한 약제학적 조성물 失效
    用于治疗或预防包含1,2,4-噻二唑-3,5-二酮化合物的药物的药物组合物

    公开(公告)号:KR100837785B1

    公开(公告)日:2008-06-13

    申请号:KR1020070005148

    申请日:2007-01-17

    Abstract: A novel 1,2,4-thiadiazolidine-3,5-dione compound is provided to show excellent activity and enzyme selectivity on Lck SH2, thereby being usefully used for treating and preventing inflammation related diseases such as rheumatoid arthritis with high selectivity without side effects. A pharmaceutical composition for treating and preventing a disease induced by inflammation comprises a 1,2,4-thiadiazolidine-3,5-dione compound represented by a formula(1) or a pharmaceutically acceptable salt thereof as an effective ingredient. In the formula(1), A is linear or branched saturated or unsaturated C1-7 alkyl, indenyl, (C1-7)alkoxycarbonyl(C1-7)alkyl, phenyl, benzyl or C2H5(C=O)HR2R3(wherein A may be substituted by halogen, carboxyl, C1-7 alkoxycarbonyl, C1-7 alkoxy, nitro or hydroxy when A is alkyl, phenyl or benzyl); R1 is H, linear or branched saturated or unsaturated C1-7 alkyl, (C1-7)alkoxycarbonyl(C1-7)alkyl, phenyl, phenyl(C1-5)alkyl or phenylcarbonylmethyl; and each R2 and R2 is independently H, linear or branched saturated or unsaturated C1-7 alkyl or phenyl, or R2 and R3 may form a ring together with C1-5 alkylene. A pharmaceutical composition for treating and preventing rheumatoid arthritis comprises the 1,2,4-thiadiazolidine-3,5-dione compound of the formula(1) or a pharmaceutically acceptable salt thereof as an effective ingredient.

    Abstract translation: 提供了一种新的1,2,4-噻二唑烷-3,5-二酮化合物,以显示对Lck SH2的极好的活性和酶选择性,从而有效地用于治疗和预防炎症相关疾病如类风湿性关节炎,具有高选择性,无副作用 。 用于治疗和预防炎性疾病的药物组合物包含由式(1)表示的1,2,4-噻二唑烷-3,5-二酮化合物或其药学上可接受的盐作为有效成分。 在式(1)中,A是直链或支链饱和或不饱和的C1-7烷基,茚基,(C1-7)烷氧基羰基(C1-7)烷基,苯基,苄基或C2H5(C = O)HR2R3(其中A可以 苯基或苄基)被卤素,羧基,C 1-7烷氧基羰基,C 1-7烷氧基,硝基或羟基取代。 R1是H,直链或支链饱和或不饱和的C1-7烷基,(C1-7)烷氧基羰基(C1-7)烷基,苯基,苯基(C1-5)烷基或苯基羰基甲基; 并且每个R 2和R 2独立地为H,直链或支链饱和或不饱和的C 1-7烷基或苯基,或者R 2和R 3可与C 1-5亚烷基一起形成环。 用于治疗和预防类风湿性关节炎的药物组合物包含式(1)的1,2,4-噻二唑烷-3,5-二酮化合物或其药学上可接受的盐作为有效成分。

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