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71.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
Applicant: 한국화학연구원
IPC: A61K31/4152 , A61P29/00
CPC classification number: A61K31/433 , A61K31/4439 , A61K31/496 , A61K31/5377 , Y10S514/825 , Y10S514/886
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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公开(公告)号：KR1020080016249A
公开(公告)日：2008-02-21
申请号：KR1020060078095
申请日：2006-08-18
Applicant: 한국화학연구원
IPC: C07D277/42 , C07D277/36 , C07D277/34 , A61P29/00
Abstract: A novel thiazole derivative is provided to inhibit effectively the enzymatic activity of 5-lipoxygenase(5-LO) acting when an arachidonic acid is converted into a leukotriene metabolite, thereby being used as a prophylactic and therapeutic agent of various inflammatory diseases and cancers. A thiazole derivative is represented by the formula(1), wherein each R1 and R2 is independently H, OR7, NO2, halogen or C1-4 linear, branched, or cyclic alkyl; each R3, R4, R5 and R6 is independently H, CF3, OR7, CO2R7, NR7R8, NO2, NHCOR7, C(=O)R7, SR7, halogen, C1-4 linear, branched or cyclic alkyl(in which each R7 and R8 is independently H, unsubstituted or F-substituted C1-6 linear, branched, or cyclic alkyl, or aryl); X is NH, O, S or SO2; Y is C or N. A method for preparing a thiazole derivative represented by the formula(1a) comprises a step of reacting an acetophenone derivative represented by the formula(2) with an aniline derivative represented by the formula(2) and a thiocyanate salt, wherein the R1 to R6, and Y are same as defined above. A pharmaceutical composition for preventing or treating asthma, chronic obstructive lung disease, arthritis, psoriasis, atopic dermatitis, allergy, enteritis, and cancer comprises the thiazole derivative, or a pharmaceutically acceptable salt thereof, a hydrate, solvate or isomer thereof as an effective ingredient.
Abstract translation: 提供了一种新的噻唑衍生物，用于有效地抑制花生四烯酸转化为白三烯代谢物时作用的5-脂氧合酶（5-LO）的酶活性，从而用作各种炎性疾病和癌症的预防和治疗剂。 噻唑衍生物由式（1）表示，其中每个R 1和R 2独立地为H，OR 7，NO 2，卤素或C 1-4直链，支链或环状烷基; 每个R 3，R 4，R 5和R 6独立地是H，CF 3，OR 7，CO 2 R 7，NR 7 R 8，NO 2，NHCOR 7，C（= O）R 7，SR 7，卤素，C 1-4直链，支链或环状烷基（其中每个R 7和 R8独立地是H，未取代的或F-取代的C 1-6直链，支链或环状烷基或芳基）; X是NH，O，S或SO 2; Y为C或N.由式（1a）表示的噻唑衍生物的制备方法包括使式（2）表示的苯乙酮衍生物与式（2）表示的苯胺衍生物和硫氰酸盐 ，其中R1至R6和Y与上述定义相同。 用于预防或治疗哮喘，慢性阻塞性肺病，关节炎，牛皮癣，特应性皮炎，过敏，肠炎和癌症的药物组合物包含噻唑衍生物或其药学上可接受的盐，其水合物，溶剂化物或异构体作为有效成分 。
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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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74.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 Ranking76.发明授权
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77.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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