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    2,4-디브로모-5-플루오르벤조산 및 그 제조방법
    41.
    发明授权
    2,4-디브로모-5-플루오르벤조산 및 그 제조방법 失效
    2,4-二溴-5-氟苯甲酸及其制备方法

    公开(公告)号：KR1019900007370B1

    公开(公告)日：1990-10-08

    申请号：KR1019870012142

    申请日：1987-10-30

    Applicant: 한국화학연구원 ,  씨제이 주식회사

    Inventor： 최중권 ,  홍성엽 ,  이영수 ,  구본암

    IPC: C07C61/15 ,  C07C63/70

    Abstract: A process for preparing 2,4-dibromo-5-fluorobenzoic acid of formula (I) comprises (A) obtaining 2,4-dibromo-5-fluorotoluene (II) 3- fluorotoluene (B) reacting (II) with Br2 in the presence of UV to form 3-fluoro-alpha, alpha, 4,5-tetrabromotoluene (IV) (C) hydrolyzing (IV) and reacting with Jones reagent to obtain (I). (I) is an intermediate in the synthesis of a potent antibacterial compound.

    Abstract translation: 制备式（I）的2,4-二溴-5-氟苯甲酸的方法包括（A）得到2,4-二溴-5-氟甲苯（II）3-氟甲苯（B），使（Ⅱ）与 UV的存在形成3-氟-α，α4,5-四溴甲苯（Ⅳ）（C）水解（Ⅳ）并与琼斯试剂反应得到（Ⅰ）。 （I）是合成有效抗菌化合物的中间体。

    이미다졸기가 치환된 퀴놀리논 유도체
    45.
    发明授权
    이미다졸기가 치환된 퀴놀리논 유도체 失效
    이미다졸기가치환된퀴놀리논유도체

    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

    Inventor： 하재두 ,  조성윤 ,  공재양 ,  최중권

    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。

    항종양 활성을 갖는〔1,2,4〕―트리아졸로〔4,3―ｃ〕퀴나졸린 유도체
    46.
    发明授权
    항종양 활성을 갖는〔1,2,4〕―트리아졸로〔4,3―ｃ〕퀴나졸린 유도체 失效
    具有抗肿瘤活性的[1,2,4]三唑并[4,3-c]喹唑啉衍生物

    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

    Inventor： 하재두 ,  조성윤 ,  조희영 ,  공재양 ,  최중권

    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, 항종양

    Abstract 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。

    퀴나졸린 유도체
    47.
    发明公开
    퀴나졸린 유도체 失效
    喹诺酮衍生物

    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

    Inventor： 하재두 ,  김군도 ,  공재양 ,  최중권

    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.

    1,2-나프토퀴논유도체 및 약학적으로 허용되는 이들의염과 그 제조방법
    48.
    发明授权
    1,2-나프토퀴논유도체 및 약학적으로 허용되는 이들의염과 그 제조방법 失效
    1,2-나프토퀴논유도체및약학적적로허용되는이들의염과과과그제조방1,2

    公开(公告)号：KR100455458B1

    公开(公告)日：2004-11-08

    申请号：KR1020010064474

    申请日：2001-10-18

    Applicant: 한국화학연구원 ,  (주)바이오니아

    Inventor： 최중권 ,  김성수 ,  하재두 ,  강승규 ,  양승돈 ,  조성윤 ,  안진희 ,  천혜경

    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.

    피리딘을 포함한 β-아미노알코올 유도체
    49.
    发明公开
    피리딘을 포함한 β-아미노알코올 유도체 失效
    含有吡啶的氨基醇衍生物

    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

    Inventor： 최중권 ,  김성수 ,  하재두 ,  강승규 ,  천혜경 ,  양승돈 ,  한상섭 ,  염을균

    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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