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1. 发明申请

WO2006057507A1 AN ORAL PREPARATION HAVING IMPROVED BIOAVAILABILITY 审中-公开
标题翻译：具有改善生物利用度的口头准备
公开(公告)号：WO2006057507A1
公开(公告)日：2006-06-01
申请号：PCT/KR2005/003950
申请日：2005-11-22
申请人： DONG WHA PHARM.IND.CO., LTD , RYU, Jei Man , CHO, Soon Ki , JUNG, Se Hyun , SEONG, Seung Kyoo , CHO, Eun Hee , AHN, Seok Hoon , KIM, Yun Jung
发明人： RYU, Jei Man , CHO, Soon Ki , JUNG, Se Hyun , SEONG, Seung Kyoo , CHO, Eun Hee , AHN, Seok Hoon , KIM, Yun Jung
IPC分类号： A61K47/30 , A61P19/10
CPC分类号： C07D277/24 , A61K9/143 , A61K31/426
摘要： The present invention relates to an oral preparation of N-hydroxy-4- {5- [4- (5-isopropyl-2 -methyl- 1, 3-thiazol-4-yl)p henoxy] pentoxyl -benzamidine having improved bioavailability . More particularly, the present invention relates to an oral preparation comprising: N-hydroxy-4- {5- [4- (5-isopropyl-2-methyl-l, 3-thiazol-4- yl) phenoxy] pentoxy} -benzamidine or pharmaceutically acceptable salt thereof; and one or more carbonates selected from the group consisting of alkalimetal carbonate, alkalimetal bicarbonate and alkaline earth metal carbonate, and/or one or more disintegrants selected from the group consisting of sodium starch glycolate, carmellose calcium and croscarmellose sodium. The oral preparation according to the present invention inhibits gelation of N-hydroxy-4- {5- [4- (5-isopropyl-2-methyl-l, 3-thiazol-4-yl) p henoxy] pentoxy} -benzamidine or pharmaceutically acceptable salt thereof in the early stage of release, which increases dissolution rate and remarkably raises bioavailability.
摘要翻译：本发明涉及具有改善的生物利用度的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 - 苄脒的口服制剂。更具体地说，本发明涉及包含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} - 苄脒的口服制剂或其药学上可接受的盐; 和一种或多种选自碳酸亚烷基碳酸盐，碱金属碳酸氢盐和碱土金属碳酸盐的碳酸盐，和/或选自淀粉羟乙酸钠，羧甲纤维素钙和交联羧甲基纤维素钠的一种或多种崩解剂。根据本发明的口服制剂抑制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} - 苄脒或其药学上可接受的盐在释放的早期阶段，其增加溶解速率并显着提高生物利用度。

2. 发明申请

WO2006014087A1 NOVEL BENZAMIDINE DERIVATIVES, PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME 审中-公开
标题翻译：新颖的苯甲酸衍生物，其制备方法和包含其的药物组合物
公开(公告)号：WO2006014087A1
公开(公告)日：2006-02-09
申请号：PCT/KR2005/002545
申请日：2005-08-04
申请人： DONG WHA PHARMACEUTICAL. IND. CO., LTD. , LEE, Jin Soo , AHN, Seok Hoon , JIN, Young Goo , JIN, Sang Mi , PARK, Whui-Jung , KU, Sae Kwang , HWANG, Yun Ha , KIM, Pan Soo , YI, Sun Shin , RYU, Jei Man
发明人： LEE, Jin Soo , AHN, Seok Hoon , JIN, Young Goo , JIN, Sang Mi , PARK, Whui-Jung , KU, Sae Kwang , HWANG, Yun Ha , KIM, Pan Soo , YI, Sun Shin , RYU, Jei Man
IPC分类号： C07D277/22
CPC分类号： C07D417/06 , C07D277/24 , C07D277/28 , C07D277/40 , C07D277/42 , C07D277/46 , C07D277/48 , C07D277/52 , C07D417/04 , C07D417/12
摘要： The present invention relates to novel benzamidine derivatives, process for the preparation thereof and pharmaceutical composition comprising the same. The novel benzamidine derivatives of the present invention are useful for the prevention and treatment of osteoporosis, bone fractures and allergic inflammatory diseases .
摘要翻译：本发明涉及新的苄脒衍生物，其制备方法和包含其的药物组合物。本发明的新型苄脒衍生物可用于预防和治疗骨质疏松症，骨折和过敏性炎性疾病。

3. 发明申请

WO2006004368A1 AN IMPROVED PROCESS FOR PREPARING N-HYDROXY-4-{5- [4- (5-ISOPROPYL-2-METHYL-l, 3-THIAZOL-4-YL) -PHENOXY] -PENTOXY }-BENZAMIDINE 审中-公开
标题翻译：制备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} - 苯甲胺的改进方法
公开(公告)号：WO2006004368A1
公开(公告)日：2006-01-12
申请号：PCT/KR2005/002137
申请日：2005-07-05
申请人： DONG WHA PHARMACEUTICAL. IND. CO., LTD. , LEE, Jin Soo , AHN, Seok Hoon , JIN, Young Goo , PARK, Jae Hoon , SHIN, Dong Hyuk , CHO, Eun Hee , CHANG, Hwan Bong , JUNG, Young Ho
发明人： LEE, Jin Soo , AHN, Seok Hoon , JIN, Young Goo , PARK, Jae Hoon , SHIN, Dong Hyuk , CHO, Eun Hee , CHANG, Hwan Bong , JUNG, Young Ho
IPC分类号： C07D277/22
CPC分类号： C07D277/24
摘要： This invention relates to an improved method of preparing N-hydroxy-4-{5- [4- (5-isopropyl-2-methyl-l, 3-thiazol-4-yl) phenoxy] pentoxy }benzamidine .
摘要翻译：本发明涉及制备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}苄脒的改进方法。

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