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    페닐-이속사졸 유도체 및 그의 제조방법
    5.
    发明公开
    페닐-이속사졸 유도체 및 그의 제조방법 有权
    苯丙酸衍生物及其制备方法

    公开(公告)号：KR1020120118665A

    公开(公告)日：2012-10-29

    申请号：KR1020110036172

    申请日：2011-04-19

    Applicant: 일양약품주식회사

    Inventor： 김동연 ,  조대진 ,  이공열 ,  김홍엽 ,  우석훈 ,  이해언 ,  김성무 ,  안충암 ,  윤승빈

    IPC: C07D413/06 ,  A61K31/496 ,  A61P31/16

    CPC classification number: A61K31/496 ,  A61K31/42 ,  A61K31/454 ,  A61K45/06 ,  C07D261/08 ,  C07D261/18 ,  C07D413/06

    Abstract: PURPOSE: A phenyl-isoxazole derivative and a method of manufacture thereof are provided to have influenza virus suppressing activity and to prevent the reproduction of the virus. CONSTITUTION: A phenyl-isoxazole derivative is represented by chemical formula 1. A manufacturing method of a compound of the chemical formula 1 comprises the following steps: manufacturing a compound of chemical formula 5 by reacting a compound of chemical formula 4 with hydroxylammoniumchloride under the presence of base; manufacturing a compound of chemical formula 7 which is isoxazol compound by using cyclization after manufacturing a compound of chemical formula 6 by using chloro reaction; and manufacturing a compound of chemical formula 9a or 9b by reacting with the compound of the chemical formula 2 or 3 after manufacturing a compound of chemical formula 8 by separating R10. The manufacturing method is processed under the presence of a tolerant solvent and/or acid or base.

    Abstract translation: 目的：提供苯基异恶唑衍生物及其制备方法以具有流感病毒抑制活性并防止病毒繁殖。 构成：苯基 - 异恶唑衍生物由化学式1表示。化学式1的化合物的制备方法包括以下步骤：通过使化学式4的化合物与羟基氯化铵在存在下反应来制备化学式5的化合物 的基数 通过使用氯代反应制造化学式6的化合物后，通过使用环化制造化合物7的化合物的化合物，其为异恶唑化合物; 在制造化学式8的化合物之后，通过分离R10，与化学式2或3的化合物反应制备化学式9a或9b的化合物。 该制造方法在耐受溶剂和/或酸或碱的存在下进行处理。

    Ν-페닐-2-피리미딘 이소티오시아네이트 유도체 및 그의 제조방법
    6.
    发明公开
    Ν-페닐-2-피리미딘 이소티오시아네이트 유도체 및 그의 제조방법 无效
    α-苯基-2-吡啶基异硫氰酸酯衍生物及其制备方法

    公开(公告)号：KR1020120052095A

    公开(公告)日：2012-05-23

    申请号：KR1020100113560

    申请日：2010-11-15

    Applicant: 일양약품주식회사

    Inventor： 김동연 ,  조대진 ,  이공열 ,  김홍엽 ,  우석훈 ,  이해언 ,  김성무 ,  안충암

    IPC: C07D239/42 ,  A61K31/505 ,  A61P31/12

    CPC classification number: Y02P20/55 ,  C07D239/42 ,  C07D401/04 ,  C07D403/04 ,  C07D417/04

    Abstract: PURPOSE: An N-phenyl-2-pyrimidine isothiocyanate derivative compound is provided to suppress influenza virus and to prevent and treat viral infection. CONSTITUTION: An N-phenyl-2-pyrimidine isothiocyanate derivative compound is denoted by chemical formula 1. A method for preparing the compound of chemical formula 1 comprises: a step of reacting a compound of chemical formula 4a or 4b with a compound of chemical formula 5 to prepare a compound of chemical formula 6a or 6b; and a step of removing PG.

    Abstract translation: 目的：提供N-苯基-2-嘧啶异硫氰酸酯衍生物化合物以抑制流感病毒并预防和治疗病毒感染。 构成：化学式1表示N-苯基-2-嘧啶异硫氰酸酯衍生物化合物。化学式1化合物的制备方法包括：使化学式4a或4b的化合物与化学式 以制备化学式6a或6b的化合物; 以及去除PG的步骤。

    염산레르카니디핀의 새로운 제조방법
    7.
    发明公开
    염산레르카니디핀의 새로운 제조방법 无效
    制备氯卡吡啶盐酸盐的方法

    公开(公告)号：KR1020070119276A

    公开(公告)日：2007-12-20

    申请号：KR1020060053681

    申请日：2006-06-15

    Applicant: 일양약품주식회사

    Inventor： 조대진 ,  김홍엽 ,  이공열

    IPC: A61K31/4406 ,  A61P9/12

    CPC classification number: A61K31/4422 ,  A61K2121/00

    Abstract: A method for preparing lercanidipine hydrochloride is provided to shorten the process by using a coupling agent of a,a-dichloromethylmethylether, mass-produce the lercanidipine hydrochloride due to a shortened process, decrease of the toxic gas generation and a simple purifying step and easily remove a by-product of methyl formate through concentration under reduced pressure. A method for preparing lercanidipine hydrochloride represented by the formula(1) comprises a step of reacting 2,6-dimethyl-5-methoxycarbonyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3-carboxylic acid represented by the formula(2) with 2,N-dimethyl-N-(3,3-diphenylpropyl)-1-amino-2-propanol represented by the formula(3) in the presence of a coupling reagent of a,a-dichloromethylmethylether represented by the formula(5) and solvent such as ethylacetate, dichloromethane, methanol, N,N-dimethylformamide and 1,4-dioxane at a reaction temperature of 10-60 deg.C.

    Abstract translation: 提供盐酸氯卡地平的方法，通过使用α-二氯甲基甲基醚的偶联剂缩短工艺，由于缩短了工艺，大量生产盐酸氯卡尼地平，有毒气体产生减少和简单的纯化步骤，容易除去 甲酸甲酯的副产物通过减压浓缩。 由式（1）表示的盐酸乐卡地平盐酸盐的制备方法包括使由式（1）表示的2,6-二甲基-5-甲氧基羰基-4-（3-硝基苯基）-1,4-二氢吡啶-3-羧酸 （2）与由式（3）表示的2，N-二甲基-N-（3,3-二苯基丙基）-1-氨基-2-丙醇在α-二氯甲基甲基醚的偶联试剂存在下，由 式（5）和溶剂如乙酸乙酯，二氯甲烷，甲醇，N，N-二甲基甲酰胺和1,4-二恶烷，反应温度为10-60℃。

    이토프라이드·염산염 중간체인4-[2-(디메틸아미노)에톡시]벤질아민의 새로운 제조방법
    8.
    发明授权
    이토프라이드·염산염 중간체인4-[2-(디메틸아미노)에톡시]벤질아민의 새로운 제조방법 失效
    制备Itopride·HCl中间体4- [2-二甲基氨基乙氧基]苄胺的方法

    公开(公告)号：KR100595117B1

    公开(公告)日：2006-06-30

    申请号：KR1020040058972

    申请日：2004-07-28

    Applicant: 일양약품주식회사

    Inventor： 김동연 ,  김재근 ,  조대진 ,  이공열 ,  김홍엽 ,  우석훈

    IPC: C07C213/06

    CPC classification number: C07C213/06 ,  C07C213/00 ,  C07C217/58

    Abstract: 본 발명은 소화관 운동 부활제로 유용한 하기 화학식1인 이토프라이드·염산염의 중간체에 대한 새로운 제조방법에 관한 것으로,
    더욱 상세하게는, 본 발명에 따른 화학식2와 화학식3의 화합물을 시발물질로 사용하여 에스테르화 반응을 통하여 단일공정의 이토프라이드·염산염 중간체인 화학식1의 4-[2-(디메틸아미노)에톡시]벤질아민 제조방법을 제공함으로써, 제조공정시 간단한 정제과정과 선택적인 반응을 통하여 높은 수율과 생산단가를 낮출 수 있으며, 유독가스가 발생하지 않아 환경오염 및 인체에 해를 주지 않고, 특히, 50kg/㎠의 초고압 수소반응 및 금속촉매를 이용한 환원반응의 공정을 시행하지 않아 제조시 매우 안전하고 특별한 제조장치가 필요없는 것을 특징으로 하는 이토프라이드·염산염 중간체에 대한 제조방법에 관한 것이다.
    이토프라이드·염산염, 부정수소증상, 소화기계, 소화관 운동

    Ｎ-페닐-2-피리미딘-아민 유도체 및 그의 제조방법
    9.
    发明公开
    Ｎ-페닐-2-피리미딘-아민 유도체 및 그의 제조방법 有权
    具有抗癌活性的N-苯基-2-吡啶胺衍生物，其用于治疗癌症及其制备方法

    公开(公告)号：KR1020040095155A

    公开(公告)日：2004-11-12

    申请号：KR1020040017594

    申请日：2004-03-16

    Applicant: 일양약품주식회사

    Inventor： 김동연 ,  김재근 ,  조대진 ,  이공열 ,  김홍엽 ,  우석훈 ,  배우철 ,  이선애 ,  한병철 ,  김용석

    IPC: C07D401/14

    CPC classification number: C07D401/04 ,  C07D401/12

    Abstract: PURPOSE: N-phenyl-2-pyrimidine-amine derivatives and a process for the preparation thereof are provided, which compounds have improved anti-cancer activity, so that it can be useful for treatment of cancers such as lung cancer, stomach cancer, colon cancer, pancreas cancer, liver cancer, prostate cancer, breast cancer, leukemia, blood cancer, brain cancer, bladder cancer, rectal cancer and cervix cancer. CONSTITUTION: The N-phenyl-2-pyrimidine-amine derivatives represented by formula (1) and pharmaceutically acceptable salts thereof are provided, wherein R1 is 3-pyridyl or 4-pyridyl; R2 and R3 are independently hydrogen or lower alkyl; R6 or R7 are substituted with a radical of formula (2); X is oxygen or NH; n is 0 or 1; and R9 is C5 to C10 aliphatic group, optionally substituted monocyclic radical which contains 1 to 3 hetero atoms selected from nitrogen, oxygen and sulfur, and 5- to 7-membered cyclic ring, optionally benzene ring fused bi- or tri-cyclic radical, or lower alkyl substituted piperazinyl or homopiperazinyl, wherein R4, R5, R7 and R8 are simultaneously hydrogen or one or two of them are independently halogen, lower alkyl or lower alkoxy when the radical of formula (2) is substituted with R6, and one or two of R4, R5, R6 and R8 are independently halogen, lower alkyl or lower alkoxy when the radical of formula (2) is substituted with R7, provided that one or more of R4, R5, R7 and R8, or one or more of R4, R5, R6 and R8 is halogen when R6 or R7 are substituted with the radical of formula (2) of which R9 is 4-methylpiperazine and n is 0.

    Abstract translation: 目的：提供N-苯基-2-嘧啶胺衍生物及其制备方法，该化合物具有改善的抗癌活性，因此其可用于治疗癌症，例如肺癌，胃癌，结肠 癌症，胰腺癌，肝癌，前列腺癌，乳腺癌，白血病，血癌，脑癌，膀胱癌，直肠癌和子宫颈癌。 构成：提供由式（1）表示的N-苯基-2-嘧啶 - 胺衍生物及其药学上可接受的盐，其中R1是3-吡啶基或4-吡啶基; R2和R3独立地是氢或低级烷基; R6或R7被式（2）的基团取代; X是氧或NH; n为0或1; 并且R 9为C 5至C 10脂族基团，任选取代的单环基团，其含有1-3个选自氮，氧和硫的杂原子，以及5-至7-元环，任选苯环稠合的双 - 或三 - 环基， 或低级烷基取代的哌嗪基或高哌嗪基，其中当式（2）的基团被R6取代时，其中R4，R5，R7和R8同时为氢或一个或两个独立地为卤素，低级烷基或低级烷氧基， 当式（2）的基团被R 7取代时，R 4，R 5，R 6和R 8中的两个独立地为卤素，低级烷基或低级烷氧基，条件是R 4，R 5，R 7和R 8中的一个或多个， 当R6或R7被其中R9是4-甲基哌嗪并且n是0的式（2）的基团取代时，R4，R5，R6和R8是卤素。

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