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    신규한 벤즈아미딘 유도체, 이의 제조방법 및 이를포함하는 골다공증의 예방 또는 치료용 약학 조성물
    2.
    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。

    Ｎ-히드록시-4-｛5-〔4-（5-이소프로필-2-메틸-1,3-티아졸-4-일）페녹시〕펜톡시｝벤즈아미딘 2 에탄술폰산염, 이의제조방법 및 이를 포함하는 약학 조성물
    3.
    发明公开
    Ｎ-히드록시-4-｛5-〔4-（5-이소프로필-2-메틸-1,3-티아졸-4-일）페녹시〕펜톡시｝벤즈아미딘 2 에탄술폰산염, 이의제조방법 및 이를 포함하는 약학 조성물 失效
    N-羟基-4- {5- [4-（5-异丙基-2-甲基-1,3-噻唑-4-基）苯氧基]戊氧基}苯甲胺二乙酸盐，其制备方法和包含药物组合物 一样

    公开(公告)号：KR1020080094634A

    公开(公告)日：2008-10-23

    申请号：KR1020080036880

    申请日：2008-04-21

    Applicant: 동화약품주식회사

    Inventor： 이진수 ,  조순기 ,  성승규 ,  진영구 ,  박재훈 ,  김보경 ,  차자현 ,  조은희 ,  유제만

    IPC: C07D277/24 ,  A61K31/426 ,  A61P19/10

    CPC classification number: C07D277/24

    Abstract: An N- hydroxy-4- benzamidine 2 ethansulfonic acid salt is provided to show excellent solubility, stability, and bioavailability, as well as a higher initial release rate than 2 methansulfonic acid salt thereof. An N-hydroxy-4-benzamidine 2 ethansulfonic acid salt is represented by a formula(1) and is prepared by reacting N- hydroxy-4-benzamidine and ethanesulfonic acid in an inert solvent. A pharmaceutical composition for preventing and treating osteoporosis, bone fractures, allergic or inflammatory diseases comprises the N- hydroxy-4-benzamidine 2 ethansulfonic acid salt and a pharmaceutically acceptable carrier. An oral formulation for preventing and treating osteoporosis, bone fractures, and allergic inflammatory diseases, comprises the N- hydroxy-4-benzamidine 2 ethansulfonic acid salt along with (a) at least one carbonate selected from the group consisting of alkali metal carbonate, alkali metal bicarbonate and alkaline earth metal carbonate; (b) at least one disintegrant selected from the group consisting of sodium carboxymethyl starch, sodium carmellose, calcium carmellose and sodium croscarmellose; or a combination of (a) and (b).

    Abstract translation: 提供N-羟基-4-苄脒2乙磺酸盐以显示出优异的溶解性，稳定性和生物利用度，以及比其二甲基磺酸盐更高的初始释放速率。 N-羟基-4-苯甲脒2乙磺酸盐由式（1）表示，并通过N-羟基-4-苯甲脒和乙磺酸在惰性溶剂中反应制备。 用于预防和治疗骨质疏松症，骨折，过敏或炎性疾病的药物组合物包括N-羟基-4-苄脒2乙磺酸盐和药学上可接受的载体。 用于预防和治疗骨质疏松症，骨折和过敏性炎性疾病的口服制剂包括N-羟基-4-苯甲脒2乙磺酸盐以及（a）至少一种选自碱金属碳酸盐，碱金属的碳酸盐 金属碳酸氢盐和碱土金属碳酸盐; （b）至少一种选自羧甲基淀粉钠，羧甲纤维素钠，羧甲纤维素钙和交联羧甲纤维素钠的崩解剂; 或（a）和（b）的组合。

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