公开(公告)号：KR101006254B1

公开(公告)日：2011-01-06

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: 본 발명은 N-히드록시-4-{5-[4-(5-이소프로필-2-메틸-1,3-티아졸-4-일)페녹시]펜톡시}벤즈아미딘 2 에탄술폰산염, 이의 제조방법, 상기 화합물을 포함하는 골다공증, 골절 또는 알러지성 염증질환의 예방 및 치료용 약학 조성물 및 상기 화합물을 포함하는 골다공증, 골절 또는 알러지성 염증질환의 예방 및 치료용 경구 제제에 관한 것이다.
N-히드록시-4-{5-[4-(5-이소프로필-2-메틸-1,3-티아졸-4-일)페녹시]펜톡시}벤즈아미딘 2 에탄술폰산염, 골다공증, 골절, 알러지성 염증질환

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。