새로운 오르토-나프토피라노퀴논 유도체 및 이를 포함하는항균 및 항진균제
    2.
    发明公开
    새로운 오르토-나프토피라노퀴논 유도체 및 이를 포함하는항균 및 항진균제 失效
    新型邻苯二甲酰亚胺衍生物和抗真菌剂及其使用的抗真菌剂

    公开(公告)号:KR1020020092160A

    公开(公告)日:2002-12-11

    申请号:KR1020020002032

    申请日:2002-01-14

    Abstract: PURPOSE: Provided are novel ortho-naphthopyranoquinone derivatives which are excellent in antimicrobial and antifungal activities with less toxicity, and a pharmaceutical composition including an antimicrobial agent and an antifungal agent, using the same. CONSTITUTION: The novel ortho-naphthopyranoquinone derivative is represented by the formula(1), wherein A is as represented in the description; B is O or C; R1 is hydrogen, a C1-C4 alkyl group, an acetyl group, -C(=O)R5, or -C(=O)OR6, wherein R5 and R6 are a C1-C4 alkyl group; R2 is hydrogen, a C1-C6 linear or branched alkyl group; C1-C4 alkoxy group, -C(=O)OR7, wherein R7 is a C1-C4 alkyl group or -CN; R3 and R4 are the same or different each other, and individually represent hydrogen, halogen atom, a halogen atom substituted or unsubstituted C1-C6 linear or branched alkyl group, -C(=O)R8; -CH2C(=O)R9, wherein R8 and R9 are hydrogen or a C1-C4 alkyl group; and R3 and R4 bind together to form 5 or 6 membered hetero cycle, wherein the hetero cycle is selected from N, S or O.

    Abstract translation: 目的:提供具有较低毒性的抗微生物和抗真菌活性优异的新型邻萘并芴醌衍生物,以及包含抗微生物剂和抗真菌剂的药物组合物。 构成:新型邻 - 萘并ran醌衍生物由式(1)表示,其中A如说明书所示; B是O或C; R1是氢,C1-C4烷基,乙酰基,-C(= O)R5或-C(= O)OR6,其中R5和R6是C1-C4烷基; R2是氢,C1-C6直链或支链烷基; C 1 -C 4烷氧基,-C(= O)OR 7,其中R 7是C 1 -C 4烷基或-CN; R 3和R 4彼此相同或不同,并分别表示氢,卤素原子,卤素原子取代或未取代的C 1 -C 6直链或支链烷基,-C(= O)R 8; -CH 2 C(= O)R 9,其中R 8和R 9是氢或C 1 -C 4烷基; 并且R3和R4结合在一起形成5或6元杂环,其中杂环选自N,S或O.

    2-에톡시프로피온산 유도체 또는 이의 약학적으로허용가능한 염, 이의 제조방법 및 이를 유효성분으로함유하는 당뇨병 예방 및 치료제
    8.
    发明公开
    2-에톡시프로피온산 유도체 또는 이의 약학적으로허용가능한 염, 이의 제조방법 및 이를 유효성분으로함유하는 당뇨병 예방 및 치료제 失效
    2-乙氧基酸衍生物或其药学上可接受的盐,其制备方法及其含有作为活性成分的糖尿病的预防和治疗剂

    公开(公告)号:KR1020080033795A

    公开(公告)日:2008-04-17

    申请号:KR1020060099978

    申请日:2006-10-13

    Abstract: A 2-ethoxypropionic acid derivative or pharmaceutically acceptable salt thereof is provided to be useful for preventing and treating diabetes more effectively by dually acting on a peroxisome proliferator-activated receptor alpha or gamma. A method of reaction formula (1) for preparing 2-ethoxypropionic acid derivatives includes the steps of: (i) coupling a compound of the formula 8 with a compound of the formula 9a in an organic solvent in the presence of a base to prepare a compound of the formula 10; (ii) reducing the compound of the formula 10 to prepare a compound of the formula 11; and (ii) subjecting the compound of the formula 11 and isocyanate(R3-NH-CH=O) or isothiocyanate(R3-NH-CH=S) to a coupling reaction and a hydrolysis reaction in the presence of a base, followed by thereto adding an acid to prepare a compound of the formula 1 through acidification.

    Abstract translation: 提供2-乙氧基丙酸衍生物或其药学上可接受的盐可用于通过双重作用于过氧化物酶体增殖物激活受体α或γ而更有效地预防和治疗糖尿病。 用于制备2-乙氧基丙酸衍生物的反应式(1)的方法包括以下步骤:(i)在有机溶剂中,在碱的存在下将式8的化合物与式9a的化合物偶合以制备 式10的化合物; (ii)还原式10的化合物以制备式11的化合物; 和(ii)在碱的存在下使式11化合物和异氰酸酯(R3-NH-CH = O)或异硫氰酸酯(R3-NH-CH = S)进行偶联反应和水解反应,然后 加入酸以通过酸化制备式1的化合物。

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