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101.发明公开신규 다중치환 벤즈옥사졸로 치환된 피리딘 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 이상세포 성장 질환의 예방 및 치료용 약학적 조성물 无效取代多取代苯并噻唑或其药学上可接受的盐的新型吡啶衍生物，其制备方法和药物组合物，用于预防和治疗含有作为活性成分的异常细胞生长疾病
公开(公告)号：KR1020110033395A
公开(公告)日：2011-03-31
申请号：KR1020090090879
申请日：2009-09-25
Applicant: 한국화학연구원
IPC: C07D403/14 , C07D401/14 , A61K31/44 , A61P35/00
Abstract: PURPOSE: A novel multiple substituted-benzoxazole-substituted pyridine derivative is provided to suppress c-Met, Ron, KDR, Lck, Flt1, Flt3, Tie2, TrkA, TrkB, b-Raf, and Aurora-A and to prevent and treating abnormal cell growth diseases. CONSTITUTION: A multiple substituted-benzoxazole-substituted pyridine derivative is denoted by chemical formula 1. A method for preparing the pyridine derivative or pharmaceutically acceptable salt thereof comprises: a step of substituting a compound of chemical formula 2 to prepare a compound of chemical formula 4; a step of cyclizing the compound of chemical formula 4 to obtain a compound of chemical formula 5; a step of substituting amine compound with the compound of chemical formula 5 to obtain a compound of chemical formula 6; a step of performing Suzuki coupling reaction of the compound of chemical formula 6 with a compound of chemical formula 7 to prepare a compound of chemical formula 8; a step of hydrogenating the compound of chemical formula 8 to obtain a compound of chemical formula 9; a step of adding the compound of chemical formula 9 with a compound of chemical formula 10 to obtain a compound of chemical formula 11; and a step of deprotecting the compound of chemical formula 11 to obtain a compound of chemical formula 1a.
Abstract translation: 目的：提供一种新的多取代苯并恶唑取代的吡啶衍生物，以抑制c-Met，Ron，KDR，Lck，Flt1，Flt3，Tie2，TrkA，TrkB，b-Raf和Aurora-A，并预防和治疗异常 细胞生长疾病。 构成：化学式1表示多取代苯并恶唑取代的吡啶衍生物。制备吡啶衍生物或其药学上可接受的盐的方法包括：用化学式2的化合物代替化学式4的化合物 ; 环化化学式4的化合物以获得化学式5的化合物的步骤; 用化学式5的化合物代替胺化合物以获得化学式6化合物的步骤; 化学式6的化合物与化学式7的化合物进行Suzuki偶联反应以制备化学式8的化合物的步骤; 氢化化学式8的化合物以获得化学式9的化合物的步骤; 将化学式9的化合物与化学式10化合物相加的步骤，得到化学式11的化合物; 和使化学式11的化合物脱保护以获得化学式1a的化合物的步骤。
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102.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
Applicant: 한국화학연구원
IPC: C07D413/04 , C07D413/02
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。
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公开(公告)号：KR1020050031716A
公开(公告)日：2005-04-06
申请号：KR1020030067964
申请日：2003-09-30
Applicant: 한국화학연구원
IPC: A61K31/4152 , A61P35/00
CPC classification number: A61K31/4152 , A61K9/0053
Abstract: An anticancer composition comprising 3-methyl-(O-substituted oximino)-pyrazolin-5-one derivatives is provided, which derivatives inhibit activity of CDC25B enzyme which participates in cell differentiation and is overexpressed in cancer cells. The anticancer composition comprises 3-methyl-(O-substituted oximino)-pyrazolin-5-one derivatives represented by formula (1), and pharmaceutically acceptable salts thereof, wherein R1 is C1-C4 alkyl or substituted phenyl with a substituent that is one or more selected from hydrogen, halogen atom, C1-C4 alkyl, C1-C4 alkoxy, C2-C4 acyl and nitro; and R2 is C1-C4 alkyl, C2-C4 alkenyl, C2-C4 alkynyl, C2-C4 acyl, methanesulfonyl, toluenesulfonyl, C1-C4 alkoxycarbonylmethyl, carboxymethyl or inorganic metal or organic amine salts of carboxymethyl.
Abstract translation: 提供包含3-甲基 - （O-取代的肟基） - 吡唑啉-5-酮衍生物的抗癌组合物，该衍生物抑制参与细胞分化且在癌细胞中过表达的CDC25B酶的活性。 抗癌组合物包含由式（1）表示的3-甲基 - （O-取代的肟基） - 吡唑啉-5-酮衍生物及其药学上可接受的盐，其中R1是C1-C4烷基或具有取代基的取代苯基 或更多选自氢，卤素原子，C 1 -C 4烷基，C 1 -C 4烷氧基，C 2 -C 4酰基和硝基; R2为C1-C4烷基，C2-C4烯基，C2-C4炔基，C2-C4酰基，甲磺酰基，甲苯磺酰基，C1-C4烷氧基羰基甲基，羧甲基或羧甲基的无机金属或有机胺盐。
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104.发明授权제초활성을 갖는9-(5-이속사졸린메톡시페닐)이미노-8-치아-1,6-디아자비시클로[4.3.0]노난-7-온 유도체 失效제초활성을갖는9-（5-이속사졸린메톡시페닐）이미노-8-치아-1,6디아자비시클로[4.3.0]노난-7-온유도체
公开(公告)号：KR100454099B1
公开(公告)日：2004-10-26
申请号：KR1020020049819
申请日：2002-08-22
Applicant: 한국화학연구원
IPC: C07D495/04
Abstract: PURPOSE: Provided are derivatives of 9-(5-isoxazolinemethoxyphenyl)imino-8-thia-1.6-diazabicylco£4.3.0|nonane-7-one, represented by the formula(1) and herbicides containing them as active ingredients and having excellent herbicidal activity and selectivity when applied to a rice paddy. CONSTITUTION: Derivatives are represented by the formula(1), wherein R is C1-C6 alkyl, phenyl or substituted phenyl, wherein substituents are 1-3 of halogen atom, C1-C3 alkyl, C1-C3 alkoxy, C1-C3 haloalkyl, cyano, nitro, carboxyl and esters of carboxy acid.
Abstract translation: 用途：提供由式（1）表示的9-（5-异恶唑啉甲氧基苯基）亚氨基-8-硫杂-1,6-二氮杂双环[4.3.0]壬烷-7-酮的衍生物和含有它们作为活性成分的除草剂， 除草活性和选择性，当应用到稻田。 构成：衍生物由式（1）表示，其中R为C 1 -C 6烷基，苯基或取代的苯基，其中取代基为卤素原子，C 1 -C 3烷基，C 1 -C 3烷氧基，C 1 -C 3卤代烷基， 氰基，硝基，羧基和羧酸的酯。
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公开(公告)号：KR1020020019751A
公开(公告)日：2002-03-13
申请号：KR1020000052918
申请日：2000-09-07
Applicant: 한국화학연구원
IPC: A01N43/80
CPC classification number: A01N43/80 , C07D413/04
Abstract: PURPOSE: Provided are 5-benzyloxymethyl-1,2-isoxazoline derivatives having an excellent herbicidal activity, its manufacturing method and herbicides containing the derivative as an active ingredient. CONSTITUTION: 5-benzyloxymethyl-1,2-isoxazoline derivative is represented by the formula(I), in which each X1, X2 and X3 represents hydrogen, methyl group, ethyl group, halogen group, methoxy group or nitro group (provided that it is an exception that X1, X2 and X3 are decimals all together); and Y1, Y2 and Y3 are respectively hydrogen or fluorine.
Abstract translation: 目的：提供具有优异除草活性的5-苄氧基甲基-1,2-异恶唑啉衍生物，其制造方法和含有该衍生物作为活性成分的除草剂。 构成：5-苄氧基甲基-1,2-异恶唑啉衍生物由式（I）表示，其中X1，X2和X3各自表示氢，甲基，乙基，卤素基，甲氧基或硝基（条件是它 是一个例外，X1，X2和X3都是小数） Y1，Y2和Y3分别为氢或氟。
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Patent Agency Ranking106.发明授权
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107.发明公开
公开(公告)号：KR1020000056677A
公开(公告)日：2000-09-15
申请号：KR1019990006209
申请日：1999-02-25
Applicant: 한국화학연구원
IPC: C07D235/00
CPC classification number: C07D413/12 , A01N43/80
Abstract: PURPOSE: 2-(5-Isoxazolinyl methyloxyphenyl)-4,5,6,7-tetrahydro-2H-indazole derivatives having herbicidal activity is provided which is useful as herbicides for control of paddy weeds. CONSTITUTION: A herbicidal compound of formula 1, their preparation method and their use as herbicides are described. In formula, X is Cl or hydroxy, R is C1-5 alkyl, substituted or unsubstituted phenyl, cyano, carboxylic acid group, carboxylic acid ester or substituted or unsubstituted hetero. As the compounds have excellent herbicidal activity against paddy weeds comprising ECHOR, SCPJU, MOOVA, CYPSE and SAGPY, and better selectivity, the compounds are typically useful as herbicides for control of paddy weeds in conditions with seeded rice and transferred rice.
Abstract translation: 目的：提供具有除草活性的2-（5-异唑啉基甲氧基苯基）-4,5,6,7-四氢-2H-吲唑衍生物，其可用作防治稻田杂草的除草剂。 构成：描述了式1的除草化合物，其制备方法及其作为除草剂的用途。 在式中，X为Cl或羟基，R为C 1-5烷基，取代或未取代的苯基，氰基，羧酸基，羧酸酯或取代或未取代的杂原子。 由于化合物对包括ECHOR，SCPJU，MOOVA，CYPSE和SAGPY的稻田杂草具有优异的除草活性，并且具有更好的选择性，所以化合物通常可用作用于在播种稻和转移稻的条件下控制稻田杂草的除草剂。
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公开(公告)号：KR100142922B1
公开(公告)日：1998-07-15
申请号：KR1019950007218
申请日：1995-03-31
Applicant: 한국화학연구원
IPC: C07D239/28 , C07D213/89 , C07D239/30 , C07D239/42 , C07D241/52
Abstract: 본 발명은 방향족 헤테로고리 아민 N-옥사이드의 제조방법에 관한 것으로서, 더욱 상세하게는 다음 구조식(II)로 표시되는 방향족 헤테로고리 아민을 불화수소(HF)수용액 촉매, 디메틸포름아미드와 메탄올 혼합용매하에서 m-클로로과벤조산 산화제로 반응시켜, 짧은시간에 높은 수율로 다음 구조식(I)로 표시되는 방향족 헤테로고리 아민 N-옥사이드를 제조하는 신규 제조방법에 관한것이다.
상기식에서,
X및Y는 각각 같거나 다른 것으로서 CH또는 N이며, R은 클로로, 카르복실산, 아미노, 옥소, C
1 ∼ C
4 의 알킬 또는 리보스(ribose)이며, n은 치환기 R의 갯수로서 1내지 3의 정수이다.-
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公开(公告)号：KR1019950004703B1
公开(公告)日：1995-05-04
申请号：KR1019920010223
申请日：1992-06-12
Applicant: 한국화학연구원
IPC: C07D249/12
Abstract: The new compound as 5-alkoxy-1-alkyl-3-aryl -1,2,4-triazole (I) and its derivatives is prepared by (1) reacting benzaldehyde and semicarbazide to get benzaldehyde 2-alkylsemicarbazone (II), (2) cycling (II) with bromide to get 1-alkyl-3-aryl -1,2,4-triazole-5-on (III), (3) reacting (III) with methyl 2-bromo propionate to get (I). (I) is useful for soybean to multiply the branches.
Abstract translation: （I）及其衍生物的新化合物是通过（1）使苯甲醛和氨基脲反应得到苯甲醛2-烷基缩氨基脲（II），（ 2）用溴化物循环（II）得到1-烷基-3-芳基-1,2,4-三唑-5-基（III），（3）使（III）与2-溴丙酸甲酯反应得到（I ）。 （I）可用于大豆繁殖分支。
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