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    3-아미도-1,2-벤조이소옥사졸 유도체, 그 염, 제조방법 및 용도
    12.
    发明公开
    3-아미도-1,2-벤조이소옥사졸 유도체, 그 염, 제조방법 및 용도 失效
    3-氨基-1,2-苯并唑衍生物及其盐，其制备方法及其用途

    公开(公告)号：KR1020030038868A

    公开(公告)日：2003-05-17

    申请号：KR1020010069013

    申请日：2001-11-06

    Applicant: 동화약품주식회사

    Inventor： 이진수 ,  안석훈 ,  진영구 ,  진상미 ,  구세광 ,  유제만 ,  정용호 ,  김은주 ,  조순기

    IPC: C07D261/20

    CPC classification number: C07D261/20

    Abstract: PURPOSE: Provided is a 3-amido-1,2-benzoisoxazole derivative or a pharmaceutically acceptable addition salt thereof which has improved bioavailability by increasing the aqueous solubility, shows excellent antagonistic effect on an LTB-4 receptor and prevents and/or treats osteoporosis. CONSTITUTION: The 3-amido-1,2-benzoisoxazole derivative of the formula(1) is prepared by introducing an amino acid residue into the amine group of 3-amido-1,2-benzoisoxazole. In the formula(1), R1 is hydrogen, a hydroxyl group, a linear or branched chain alkyl group with C1-C6, a benzyl group or a 2-methylthioethyl group; R2 is hydrogen or -COC(NH2)R3, and R3 is hydrogen, a hydroxyl group, a linear or branched chain alkyl group with C1-C6, a benzyl group, or a 2-methylthioethyl group.

    Abstract translation: 目的：提供通过增加水溶性而具有改善的生物利用度的3-酰氨基-1,2-苯并异恶唑衍生物或其药学上可接受的加成盐，对LTB-4受体显示出优异的拮抗作用并预防和/或治疗骨质疏松症。 构成：通过将氨基酸残基引入3-氨基-1,2-苯并异恶唑的胺基中，制备式（1）的3-酰氨基-1,2-苯并异恶唑衍生物。 在式（1）中，R 1是氢，羟基，具有C 1 -C 6，苄基或2-甲硫基乙基的直链或支链烷基; R2是氢或-COC（NH2）R3，R3是氢，羟基，具有C1-C6，苄基或2-甲硫基乙基的直链或支链烷基。

    신규한 벤즈아미딘 유도체, 이의 제조방법 및 이를포함하는 골다공증의 예방 또는 치료용 약학 조성물
    14.
    发明公开
    신규한 벤즈아미딘 유도체, 이의 제조방법 및 이를포함하는 골다공증의 예방 또는 치료용 약학 조성물 失效
    新型苯甲酸衍生物，其制备方法和用于预防或治疗包含其的药物组合物的药物组合物

    公开(公告)号：KR1020090012190A

    公开(公告)日：2009-02-02

    申请号：KR1020080073710

    申请日：2008-07-28

    Applicant: 동화약품주식회사

    Inventor： 유제만 ,  이진수 ,  진영구 ,  박재훈 ,  김보경 ,  원대연 ,  황연하 ,  김기윤 ,  구세광

    IPC: C07D417/06 ,  C07D417/04 ,  C07D277/42

    CPC classification number: C07D277/22 ,  C07D277/28 ,  C07D277/40 ,  C07D417/06

    Abstract: A benzamidine derivative is provided to be used for a pharmaceutical composition for preventing and treating osteoporosis and to suppress effectively differentiation of osteoclast at very low concentration. A benzamidine derivative is indicated as a chemical formula 1. In the chemical formula 1: R1 is methyl, ethyl, isopropyl, phenyl, pyridinyl, cyclohexyl, morpholinyl, group substituted or not substituted into C1~C6 alkyl, NR6R7 or CH2NR6R7; R2 is NR8R9, piperidine, pyrrolidine, imidazole or triazole; R3 and R4 are hydrogen, methyl, ethyl, halogen, hydroxy or methoxy group; R5 is hydroxy group; and R6 and R7 are hydrogen, methyl, ethyl, profile, hydroxyethyl, methoxyethyl, 2-morpholinoethyl, benzyl, pyridine-3-1-methyl, pyridine-4-1-methyl, 3-pyridinyl carbonyl or ethanesulfonyl.

    Abstract translation: 提供了一种苄脒衍生物，用于预防和治疗骨质疏松症的药物组合物，并以非常低的浓度有效地抑制破骨细胞的分化。 化学式1中，R1为甲基，乙基，异丙基，苯基，吡啶基，环己基，吗啉基，取代或未被C1〜C6烷基，NR6R7或CH2NR6R7取代的基团。 R2是NR8R9，哌啶，吡咯烷，咪唑或三唑; R3和R4是氢，甲基，乙基，卤素，羟基或甲氧基; R5是羟基; R 6和R 7是氢，甲基，乙基，异构体，羟乙基，甲氧基乙基，2-吗啉代乙基，苄基，吡啶-3-甲基，吡啶-4-甲基，3-吡啶基羰基或乙磺酰基。

    1-시클로프로필-6-플루오로-7-(8-메톡시이미노-2,6-디아자-스피로[3.4]옥트-6-일)-4-옥소-1,4-디히드로-[1,8]나프티리딘-3-카르복실산 아스파르트산 염, 이의 제조방법 및 이를포함하는 항균용 약학 조성물
    15.
    发明公开
    1-시클로프로필-6-플루오로-7-(8-메톡시이미노-2,6-디아자-스피로[3.4]옥트-6-일)-4-옥소-1,4-디히드로-[1,8]나프티리딘-3-카르복실산 아스파르트산 염, 이의 제조방법 및 이를포함하는 항균용 약학 조성물 有权
    1-环丙基-6-氟-7-（8-甲氧基-2,6-二氮杂 - 螺[3.4]辛-6-基）-4-氧代-1,4-二氢 - [1,8]萘啶-3- - 羧酸类阿糖酸盐，其制备方法和包含其抗药性的药物组合物

    公开(公告)号：KR1020080092893A

    公开(公告)日：2008-10-16

    申请号：KR1020080034411

    申请日：2008-04-14

    Applicant: 동화약품주식회사

    Inventor： 유제만 ,  최동락 ,  양진 ,  윤수혜 ,  김승환 ,  구세광

    IPC: C07D471/04 ,  A61K31/4375

    CPC classification number: C07D519/00

    Abstract: A 1-cyclopropyl-6-fluoro-7-(8-methoxyimino-2,6-diaza-spiro[3.4]oct-6-yl)-4-oxo-1,4-dihydro-[1,8]naphthyridine-3-carboxylic acid aspartic acid salt is provided to improve physicochemical properties including solubility and stability as compared to phosphate or hydrochloride thereof, and minimize toxicity, so that the compound is useful as antimicrobial agent in food and medicines. A 1-cyclopropyl-6-fluoro-7-(8-methoxyimino-2,6-diaza-spiro[3.4]oct-6-yl)-4-oxo-1,4-dihydro-[1,8]naphthyridine-3-carboxylic acid aspartic acid salt represented by the formula(1) is prepared by reacting 1-cyclopropyl-6-fluoro-7-(8-methoxyimino-2,6-diaza-spiro[3.4]oct-6-yl)-4-oxo-1,4-dihydro-[1,8]naphthyridine-3-carboxylic acid with aspartic acid in inert organic solvent selected from ethyl acetate, methanol, ethanol, isopropanol, acetone, acetonitrile, hexane, isopropyl ether and water. An antimicrobial pharmaceutical composition comprises 1-cyclopropyl-6-fluoro-7-(8-methoxyimino-2,6-diaza-spiro[3.4]oct-6-yl)-4-oxo-1,4-dihydro-[1,8]naphthyridine-3-carboxylic acid aspartic acid salt, and is formulated as injection. The aspartic acid salt is D-aspartic acid salt, L-aspartic acid salt or racemic mixture thereof.

    Abstract translation: 1-环丙基-6-氟-7-（8-甲氧基亚氨基-2,6-二氮杂 - 螺[3.4]辛-6-基）-4-氧代-1,4-二氢 - [1,8] 提供3-羧酸天冬氨酸盐以提高与其磷酸盐或盐酸盐相比的溶解度和稳定性的物理化学性质，并且使毒性最小化，使得该化合物可用作食品和药物中的抗微生物剂。 1-环丙基-6-氟-7-（8-甲氧基亚氨基-2,6-二氮杂 - 螺[3.4]辛-6-基）-4-氧代-1,4-二氢 - [1,8] 由式（1）表示的3-羧酸天冬氨酸盐通过1-环丙基-6-氟-7-（8-甲氧基亚氨基-2,6-二氮杂 - 螺[3.4]辛-6-基） - 4-氧代-1,4-二氢 - [1,8]二氮杂萘-3-羧酸与天冬氨酸在惰性有机溶剂中的溶液，选自乙酸乙酯，甲醇，乙醇，异丙醇，丙酮，乙腈，己烷，异丙醚和水。 抗微生物药物组合物包含1-环丙基-6-氟-7-（8-甲氧基亚氨基-2,6-二氮杂 - 螺[3.4]辛-6-基）-4-氧代-1,4-二氢 - [1,3' 8]萘啶-3-羧酸天冬氨酸盐，并配制成注射剂。 天冬氨酸盐是D-天冬氨酸盐，L-天冬氨酸盐或其外消旋混合物。

    골절 치료용 약제학적 조성물
    17.
    发明公开
    골절 치료용 약제학적 조성물 失效
    用于治疗骨折的药物组合物

    公开(公告)号：KR1020060049858A

    公开(公告)日：2006-05-19

    申请号：KR1020050060425

    申请日：2005-07-05

    Applicant: 동화약품주식회사

    Inventor： 이진수 ,  구세광 ,  이정우 ,  양희복 ,  유제만

    IPC: A61K31/426 ,  A61K31/155

    CPC classification number: A61K31/426

    Abstract: 본 발명은 골절 치료용 조성물에 관한 것으로, 상세하게는 N-히드록시-4-{5-[4-(5-이소프로필-2-메틸-1,3-티아졸-4-일)페녹시]펜톡시}-벤즈아미딘, 4-{5-[4-(5-이소프로필-2-메틸-1,3-티아졸-4-일)페녹시]펜톡시}-벤즈아미딘 또는 이의 약제학적으로 허용 가능한 염을 포함하는 골절 치료용 조성물에 관한 것이다.
    본 발명의 조성물은 가골의 체적을 유의성 있게 감소시키고, 가골의 골밀도 및 골강도를 유의성 있게 증가시키며, 가골 조직내 결합조직 및 연골조직의 함량을 유의성 있게 감소시키고, 골조직 함량을 유의성 있게 증가시킴으로, 골절시 형성된 가골의 소실 및 가골의 골화를 촉진시킨다. 따라서, 본 발명의 조성물은 골절에 대한 치유 촉진제로 유용하게 사용할 수 있다.
    골절, 벤즈아미딘

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