中科微点-全球专利检索

  1. Login
  2. Sign Up

Search Results

95 records (took 0.033 seconds)

    베타아미노기를 갖는 1,2,5-트리아제판 유도체, 이의약학적으로 허용 가능한 염 및 이의 제조 방법
    22.
    发明公开
    베타아미노기를 갖는 1,2,5-트리아제판 유도체, 이의약학적으로 허용 가능한 염 및 이의 제조 방법 有权
    具有β型-AMINO ACYL组的1,2,5-三唑衍生物及其药物可接受的盐及其制备方法

    公开(公告)号：KR1020080007764A

    公开(公告)日：2008-01-23

    申请号：KR1020060066812

    申请日：2006-07-18

    Applicant: 한국화학연구원 ,  영진약품 주식회사

    Inventor： 김성수 ,  천혜경 ,  이상달 ,  안진희 ,  김기영 ,  강남숙 ,  강승규 ,  정원훈 ,  김성규 ,  김선영 ,  권재홍 ,  손상권 ,  신민기

    IPC: C07D255/02 ,  A61P3/00

    Abstract: A 1,2,5-triazepane derivative showing excellent DPP-IV inhibitory activity is provided to be effectively used for preventing or treating diseases mediated by DPP-IV such as insulin-dependent, insulin non-dependent diabetes, arthritis, obesity, osteoporosis, and damaged glucose resistance. A 1,2,5-triazepane derivative having a beta-amino group is represented by the formula(1), wherein R1 is a group represented by the structural formula(1-1) or (1-2); R2 is H, C1-6 alkyl, or a group represented by the structural formula(1-3); R3 is H, C1-6 alkyl, C3-6 cycloalkyl, CH2CO2R^b, COCO2R^b, pyrazine, and a group represented by the structural formula(1-4), (1-5) or (1-6); R^a is independently H, C1-6 alkyl, C3-6 cycloalkyl, C1-6 alkoxy, OCF3, halogen, CN, CF3, COOR^b or NR^bR^c; each R^b and R^c is independently H, C1-6 alkyl or C3-6 cycloalkyl; R^d is C1-6 alkyl, trifluoromethyl, and a group represented by the structural formula(1-1), (1-7), (1-8), or (1-9); R^e is C1-6 alkyl, C3-6 cycloalkyl, and a group represented by the structural formula(1) or (2); R^f is H, halogen, NR^bR^c, tetrazole, proline, and a group represented by the structural formula(1-10), (1-11), (1-12), or (1-13); A is CH, N, O or S; B is H, C1-6 alkyl, C3-6 cycloalkyl, benzyl or CO2R^d; X is O or S; and n is 0 or 1. A method for preparing the 1,2,5-triazepane derivative comprises the steps of: (a) subjecting an amino acid represented by the formula(2) and 1,2,5-triazepane to a condensation reaction to prepare a compound represented by the formula(4); (b) reacting the compound of the formula(4) with an electrophilic compound substituted with R2 to prepare a compound represented by the formula(5); and (c) deprotecting the compound of the formula(5). A pharmaceutical composition for preventing or treating diseases mediated by DPP-IV comprises an effective amount of the 1,2,5-triazepane derivative or a pharmaceutically acceptable salt and a pharmaceutically acceptable carrier.

    Abstract translation: 提供了显示优异的DPP-IV抑制活性的1,2,5-三氮丙平衍生物，其有效用于预防或治疗由DPP-IV介导的疾病，例如胰岛素依赖性，胰岛素非依赖型糖尿病，关节炎，肥胖症，骨质疏松症， 并损害葡萄糖耐量。 具有β-氨基的1,2,5-三氮杂环庚烷衍生物由式（1）表示，其中R1是由结构式（1-1）或（1-2）表示的基团。 R2是H，C1-6烷基或由结构式（1-3）表示的基团; R 3是H，C 1-6烷基，C 3-6环烷基，CH 2 CO 2 R b，COCO 2 R b，吡嗪和由结构式（1-4），（1-5）或（1-6）表示的基团。 R a a独立地为H，C 1-6烷基，C 3-6环烷基，C 1-6烷氧基，OCF 3，卤素，CN，CF 3，COOR b或NR b R c; 每个R b和R c独立地是H，C 1-6烷基或C 3-6环烷基; R 1-6是C1-6烷基，三氟甲基和由结构式（1-1），（1-7），（1-8）或（1-9）表示的基团。 R 1-6是C 1-6烷基，C 3-6环烷基和由结构式（1）或（2）表示的基团。 （1-10），（1-11），（1-12）或（1-13）表示的基团，其中R为氢，卤素，NR 4 b R c，四唑，脯氨酸和由结构式 ; A是CH，N，O或S; B是H，C 1-6烷基，C 3-6环烷基，苄基或CO 2 R d; X是O或S; 并且n为0或1.制备1,2,5-三氮杂环庚烷衍生物的方法包括以下步骤：（a）使由式（2）表示的氨基酸和1,2,5-三氮杂环庚烷进行缩合 反应制备式（4）表示的化合物; （b）使式（4）的化合物与被R 2取代的亲电子化合物反应，制备由式（5）表示的化合物。 和（c）使式（5）的化合物脱保护。 用于预防或治疗由DPP-IV介导的疾病的药物组合物包含有效量的1,2,5-三氮丙烯衍生物或其药学上可接受的盐和药学上可接受的载体。

    1,2-나프토퀴논유도체 및 약학적으로 허용되는 이들의염과 그 제조방법
    25.
    发明公开
    1,2-나프토퀴논유도체 및 약학적으로 허용되는 이들의염과 그 제조방법 失效
    1,2-萘醌衍生物及其药学上可接受的盐及其制备方法

    公开(公告)号：KR1020030032592A

    公开(公告)日：2003-04-26

    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

    CPC classification number: C07C235/84 ,  A61K31/166

    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: 目的：提供抑制蛋白磷酸酶活性的式（1）的1,2-萘醌衍生物及其药学上可接受的盐的制备方法。 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，急性和慢性感染和各种癌症。 构成：由说明书中定义的式（1）表示的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）化合物; 并且使用选自（Pb（OAc）2），CeCl 3·7H 2 O和NaIO 3混合物的混合物和RMgX和CuCN混合物在化合物（3）的4位置取代B。

    피리딘을 포함한 β-아미노알코올 유도체
    26.
    发明授权
    피리딘을 포함한 β-아미노알코올 유도체 失效
    피리딘을포함한-아미노알코올유도체

    公开(公告)号：KR100380520B1

    公开(公告)日：2003-04-23

    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: 用途：提供含有吡啶的β-氨基醇衍生物，其药学上可接受的盐及其制造方法。 β-氨基醇衍生物具有降压作用并减轻体重，因此用作高血糖相关疾病或肥胖症的治疗剂。 构成：含吡啶的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为氢或C 1-4烷基; Y是亚甲基或氧; G是至少一个选自氢，卤原子，C1-3烷基，烷氧基，氨基，氰基，苯基取代的脲，苯基或C1-3烷基取代的羧酰胺，羧酸酯，烷氧基羰基甲氧基，烷氧基羰基烷基 ，烷氧基羰基丙烯酰基和四唑基。 它是通过与式（II）化合物和式（III）化合物缩合反应并用有机金属催化剂氢化而制得的。

    Ｎ1-2-티오펜-2-일에틸-Ｎ2-치환된 바이구아나이드 유도체,이의 제조방법 및 이를 유효성분으로 함유하는 약학 조성물
    30.
    发明公开
    Ｎ1-2-티오펜-2-일에틸-Ｎ2-치환된 바이구아나이드 유도체,이의 제조방법 및 이를 유효성분으로 함유하는 약학 조성물 失效
    N1-2-替戊-2-炔基-N 2取代的生物分子衍生物，其制备方法和包含其的药物组合物

    公开(公告)号：KR1020100041175A

    公开(公告)日：2010-04-22

    申请号：KR1020080100221

    申请日：2008-10-13

    Applicant: 한올바이오파마주식회사 ,  한국화학연구원

    Inventor： 김성욱 ,  전성수 ,  천혜경 ,  김광록 ,  이상달 ,  정원훈 ,  이종철

    IPC: C07D333/08 ,  C07D333/14 ,  C07D333/22

    CPC classification number: C07D333/20

    Abstract: PURPOSE: A pharmaceutical composition containing N1-2-thiopene-2-ylethyl-N2-substituted biguanide derivative is provided to ensure function of reducing blood sugar and lipid and to prevent and treat diabetes, metabolic syndrome, or p53-deficient cancer. CONSTITUTION: A N1-2-thiopene-2-ylethyl-N2-substituted biguanide derivative compound is denoted by chemical formula 1. In chemical formula 1, R is C1-C8 alkyl, aryl, C1-C8 alkoxyalkyl, C3-C7 cycloalkyl, C3-C7 cycloalkylC1-C3 alkyl, substituted phenyl or phenyl C1-C3 alkyl, substituted naphthyl or naphthyl C1-C3 alkyl. A method for preparing a compound of chemical formula 1 comprises: a step of reacting a compound of chemical formula 2 with NaBH4 to obtain a compound of chemical formula 3; a step of reacting the compound of chemical formula 3 with thionylchloride in organic solvent to obtain a compound of chemical formula 4; a step of reacting the compound of chemical formula 4 with sodium cyanide in DMSO to obtain a compound of chemical formula 5; a step of reacting the compound of chemical formula 5 with sodium borohydride and nickel chloride hydrate to obtain a compound of chemical formula 6; a step of reacting the compound of chemical formula 6 with R-isothiocyanate(RNACS) under the presence of base in organic solvent to obtain a compound of chemical formula 8; and a step of reacting the compound of chemical formula 8 in guanidine solution under the presence of mercury oxide.

    Abstract translation: 目的：提供含有N1-2-噻吩-2-基乙基-N2-取代双胍衍生物的药物组合物，以确保降低血糖和脂质的功能，并预防和治疗糖尿病，代谢综合征或p53缺陷型癌症。 构成：化学式1表示N1-2-噻吩-2-基乙基-N2-取代双胍衍生物化合物。在化学式1中，R为C1-C8烷基，芳基，C1-C8烷氧基烷基，C3-C7环烷基， C 3 -C 7环烷基C 1 -C 3烷基，取代的苯基或苯基C 1 -C 3烷基，取代的萘基或萘基C 1 -C 3烷基。 制备化学式1的化合物的方法包括：使化学式2的化合物与NaBH 4反应以获得化学式3的化合物的步骤; 使化学式3的化合物与亚硫酰氯在有机溶剂中反应得到化学式4的化合物的步骤; 使化学式4的化合物与氰化钠在DMSO中反应得到化学式5的化合物的步骤; 使化学式5的化合物与硼氢化钠和氯化镍水合物反应以获得化学式6的化合物的步骤; 使化学式6的化合物与R-异硫氰酸酯（RNACS）在碱的存在下在有机溶剂中反应得到化学式8的化合物的步骤; 以及在氧化汞存在下，将化学式8的化合物与胍溶液反应的步骤。

Patent Agency Ranking