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71.发明公开신규 피라졸로[4,3-ｂ]피리딘 유도체 또는 이의 약학적으로허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 약학적 조성물 失效新型吡咯并[4,3-B]吡啶衍生物或其药学上可接受的盐，其制备方法和含有其作为活性成分的药物组合物
公开(公告)号：KR1020100057433A
公开(公告)日：2010-05-31
申请号：KR1020080116472
申请日：2008-11-21
Applicant: 한국화학연구원
IPC: C07D471/04 , C07D487/04
Abstract: PURPOSE: A pharmaceutical composition for preventing or treating melanoma containing a novel pyrazolo[4,3-b]pyridine derivative is provided to ensure suppression activity to tyrosine kinase. CONSTITUTION: A pyrazolo[4,3-b]pyridine derivative is denoted by chemical formula 1. A method for manufacturing the pyrazolo[4,3-b]pyridine derivative comprises: a step of reacting Boc-protected hydrazine to a compound of chemical formula 2 to obtain a compound of chemical formula 3; a step of adding acid to the compound of chemical formula 3 to obtain a compound of chemical formula 4; and a step of reacting benzylhalide or arylmethylene halide under the presence of inorganic base to obtain a compound of chemical formula 5.
Abstract translation: 目的：提供一种用于预防或治疗含有新型吡唑并[4,3-b]吡啶衍生物的黑色素瘤的药物组合物，以确保对酪氨酸激酶的抑制活性。 构成：吡唑并[4,3-b]吡啶衍生物由化学式1表示。吡唑并[4,3-b]吡啶衍生物的制造方法包括：使Boc-保护的肼与化学式 式2得到化学式3的化合物; 向化学式3的化合物中加入酸以获得化学式4的化合物的步骤; 和在无机碱存在下使苄基卤或芳基亚甲基卤反应得到化学式5的化合物的步骤。
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公开(公告)号：KR1020070119581A
公开(公告)日：2007-12-20
申请号：KR1020070060197
申请日：2007-06-20
Applicant: 한국화학연구원
IPC: C07D207/36
Abstract: A novel aromatic diamine is provided to be used for developing a novel liquid crystal alignment layer having excellent voltage holding ratio and a pretilt angle of 0.1-2° due to low surface polarization parameter. A method for preparing 1-(3,5-diaminophenyl)-pyrrolidine-2,5-dione represented by the formula(1) comprises the steps of: (a) protecting an amine of 3,5-dinitrophenylamine with a carbazole; (b) reducing the nitro with an amine; (c) protecting the amine with t-butoxycarbonyl; (d) deprotecting the carbazole; (e) reacting the de-protected amine with a succinic anhydride to form a succinic imide; and (f) deprotecting the t-butoxycarbonyl.
Abstract translation: 提供了一种新颖的芳族二胺，用于开发由于低表面极化参数而具有优异的电压保持率和0.1-2°的预倾角的新型液晶取向层。 由式（1）表示的制备1-（3,5-二氨基苯基） - 吡咯烷-2,5-二酮的方法包括以下步骤：（a）用咔唑保护3,5-二硝基苯胺胺; （b）用胺还原硝基; （c）用叔丁氧基羰基保护胺; （d）使咔唑脱保护; （e）使去保护的胺与琥珀酸酐反应以形成琥珀酰亚胺; 和（f）使叔丁氧基羰基脱保护。
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公开(公告)号：KR100744826B1
公开(公告)日：2007-08-01
申请号：KR1020060031041
申请日：2006-04-05
Applicant: 한국화학연구원
IPC: C07D401/04
Abstract: Quinolinone derivatives substituted with an imidazole group are provided to inhibit tyrosine kinase activity, so that they are useful for treatment of diseases caused by abnormal tyrosine kinase activity including tumor, psoriasis, rheumatism and diabetic retinopathy. The quinolinone derivatives substituted with the imidazole group and represented by the formula(1) and their pharmaceutically acceptable salts thereof are provided, wherein R^1 is hydrogen atom, halogen atom or C1-6 alkoxy group; R^2 and R^3 are each independently hydrogen atom, C1-6 alkyl group, amide group, pyridine group, phenyl group or phenyl group substituted by halogen atom, nitro group, -C(=O)-NR4R5, or -NR4R5; R^4 and R^5 are the same or different, and each independently hydrogen atom, C1-6 alkyl group or -C(=O)R6, or form a 5- or 6-membered ring together with a hetero atom selected from O and NR7; R6 is C1-6 alkyl group, amine group or aniline group; and R7 is hydrogen atom or C1-6 alkyl group.
Abstract translation: 提供用咪唑基团取代的喹啉酮衍生物抑制酪氨酸激酶活性，因此它们可用于治疗由酪氨酸激酶活性异常引起的疾病，包括肿瘤，牛皮癣，风湿病和糖尿病性视网膜病。 提供了咪唑基取代的并且由式（1）表示的喹啉酮衍生物及其药学上可接受的盐，其中R 1是氢原子，卤素原子或C 1-6烷氧基; 硝基，-C（= O）-NR 4 R 5或-NR 4 R 5取代的苯基或苯基 ; R 4和R 5相同或不同，并且各自独立地为氢原子，C 1-6烷基或-C（= O）R 6，或与选自以下的杂原子一起形成5或6元环： O和NR7; R6是C1-6烷基，胺基或苯胺基; 并且R 7是氢原子或C 1-6烷基。
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公开(公告)号：KR100714370B1
公开(公告)日：2007-05-02
申请号：KR1020050101516
申请日：2005-10-26
Applicant: 한국화학연구원
IPC: C07D487/04
Abstract: 본 발명은 항종양 활성을 갖는 [1,2,4]-트리아졸로[4,3-c]퀴나졸린 유도체에 관한 것으로, 더욱 상세하게는 티로신 키나제에 대한 억제활성이 우수하여 비정상적인 키나제의 활성으로 야기되는 질환 예를 들면 암, 특히 결장직장암, 유방암, 폐암, 전립선암, 췌장암, 방광암, 신장암, 백혈병, 림프종과 같은 고증식성 질환 치료에 유효한 신규 구조의 [1,2,4]-트리아졸로[4,3-c]퀴나졸린 유도체 및 이의 약학적으로 허용 가능한 염과, 이 화합물의 의약적 용도에 관한 것이다.
티로신 키나제, [1,2,4]-트리아졸로[4,3-c]퀴나졸린, 항종양Abstract translation: 技术领域本发明涉及具有抗肿瘤活性的[1,2,4]三唑并[4,3-c]喹唑啉衍生物，更具体地涉及对酪氨酸激酶的抑制活性， 引起疾病，例如癌症，特别是结肠直肠癌，乳腺癌，肺癌，前列腺癌，胰腺癌，膀胱癌，肾癌，白血病，[1,1'-新颖结构是有效的历史研究增殖性疾病如淋巴瘤是三唑 [4,3-c]喹唑啉衍生物及其药学上可接受的盐，以及该化合物的药物用途。
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75.发明授权극성 말단기를 함유한 알킬측쇄 방향족기를 갖는 폴리아믹산 수지, 이를 함유한 수직배향형 조성물 및 이를 이용한 액정 배향막과 액정 셀 失效含极性基团封端的含有烷基侧链的聚酰胺酸，含有取向的组合物和液晶取向膜以及使用它们的电池
公开(公告)号：KR100623273B1
公开(公告)日：2006-09-19
申请号：KR1020040101942
申请日：2004-12-06
Applicant: 한국화학연구원
IPC: C07C217/84 , C07C217/90 , C07C211/52
Abstract: 본 발명은 극성 말단기를 함유한 알킬측쇄를 갖는 방향족 디아민과, 이를 함유한 수직배향형 조성물 및 이를 이용한 액정 배향막과 액정 셀에 관한 것으로서, 더욱 상세하게는 극성 말단기를 함유한 알킬측쇄를 갖는 신규의 방향족 디아민과, 그리고 상기 신규의 방향족 디아민을 도입하여 제조된 폴리아믹산 수지와, 폴리아믹산 유도체가 적정비로 함유된 수직배향형 조성물과, 그리고 상기 조성물을 사용하여 극성 기재에 대한 우수한 표면도포성, 내열성, 표면경도, 투명성 및 액정 주입특성이 우수성을 갖는 액정 배향막과 89° 이상의 선경사각을 갖는 액정 셀에 관한 것이다.
극성 말단기, 측쇄, 방향족 디아민, 폴리아믹산 수지, 수직배향형, 액정 배향막, 액정 셀-
Patent Agency Ranking
公开(公告)号：KR1020050110439A
公开(公告)日：2005-11-23
申请号：KR1020040035452
申请日：2004-05-19
Applicant: 한국화학연구원
IPC: C07D491/056
Abstract: 본 발명은 티로신 키나제에 대한 억제활성이 우수하여 비정상적인 키나제의 활성으로 야기되는 질환 예를 들면 암, 건선, 류마티스 관절염, 당뇨병성 망막증 등의 치료에 유용한 신규 화합물로서 퀴나졸린의 C-6과 C-7번 위치가 1,4-디옥산기에 의해 연결된 3환 구조의 퀴나졸린 유도체와 이의 제조방법 그리고 이의 의약적 용도에 관한 것이다.
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公开(公告)号：KR100455458B1
公开(公告)日：2004-11-08
申请号：KR1020010064474
申请日：2001-10-18
IPC: C07F1/06
Abstract: PURPOSE: Provided are a preparation method of 1,2-naphthoquinone derivatives of formula(1) and their pharmaceutically acceptable salt which inhibit the activity of protein phosphatase. The compounds are widely used in treatment of type 1 and 2 diabetes, autoimmune diseases, acute and chronic infection and various cancers. CONSTITUTION: The method of preparation of 1,2-naphthoquinone derivatives represented by the formula(1) as defined in the specification and their pharmaceutically acceptable salt comprises the steps of: oxidizing a naphthol compound of formula(2) with selenium oxides and obtaining a compound of formula(3); and substituting B at 4 position of the compound(3) using mixtures selected from (Pb(OAc)2),CeCl3 7H2O and NaIO3 mixture and RMgX and CuCN mixture.
Abstract translation: 用途：提供了式（1）的1,2-萘醌衍生物及其药学上可接受的盐的制备方法，其抑制蛋白磷酸酶的活性。 该化合物广泛用于治疗1型和2型糖尿病，自身免疫性疾病，急性和慢性感染以及各种癌症。 构成：由说明书中定义的式（1）代表的1,2-萘醌衍生物及其药学上可接受的盐的制备方法包括以下步骤：用氧化硒氧化式（2）的萘酚化合物，得到 式（3）的化合物; 并且使用选自（Pb（OAc）2），CeCl 3·7H 2 O和NaIO 3混合物以及RMgX和CuCN混合物的混合物代替化合物（3）的4位的B.
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公开(公告)号：KR1020020020288A
公开(公告)日：2002-03-15
申请号：KR1020000053309
申请日：2000-09-08
Applicant: 한국화학연구원
IPC: C07D213/24
Abstract: PURPOSE: Provided are β-aminoalcohol derivative containing pyridine, its pharmaceutically acceptable salt and its manufacturing method. The β-aminoalcohol derivative has a hypotensive effect and reduces weight, and is thus used as a therapeutic gent in hyperglycemia related diseases or obesity. CONSTITUTION: β-aminoalcohol derivative containing pyridine is represented by the formula(I), wherein A is halogen atom or haloalkyl substituted or unsubstituted phenyl, thiophene, phenyloxymethyl, naphthyloxymethyl, or biphenyloxymethyl group; R is hydrogen or C1-4 alkyl group; Y is methylene or oxygen; and G is at least one substituent selected from the group consisting of hydrogen, halogen atom, C1-3 alkyl, alkoxy, amino, cyano, phenyl substituted urea, phenyl or C1-3 alkyl substituted carboxamide, carboxylester, alkoxy carbonyl methyloxy, alkoxycarbonylalkyl group, alkoxycarbonylacryl and tetrazol group. It is manufactured by condensation reaction with a compound of the formula(II) and a compound of the formula(III) and hydrogenation with organic metal catalyst.
Abstract translation: 目的：提供含有吡啶的β-氨基醇衍生物及其药学上可接受的盐及其制备方法。 β-氨基醇衍生物具有降血压作用并减轻体重，因此用作高血糖相关疾病或肥胖症的治疗方法。 构成：含有吡啶的β-氨基醇衍生物由式（I）表示，其中A为卤素原子或卤代烷基取代或未取代的苯基，噻吩，苯氧基甲基，萘氧基甲基或联苯氧基甲基; R是氢或C 1-4烷基; Y是亚甲基或氧; G为至少一个选自氢，卤素原子，C 1-3烷基，烷氧基，氨基，氰基，苯基取代的脲，苯基或C 1-3烷基取代的羧酰胺，羧酸酯，烷氧基羰基甲氧基，烷氧羰基烷基 ，烷氧基羰基丙烯酰基和四唑基。 通过与式（II）的化合物和式（III）的化合物进行缩合反应并用有机金属催化剂氢化制备。
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