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1. 发明申请

US20100184795A1 ASPARTATE OF 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, METHOD FOR PREPARING THE SAME, AND ANTIMICROBIAL PHARMACEUTICAL COMPOSITION COMPRISING THE SAME 有权
标题翻译： 1-环丙基-6-氟-7-（8-甲氧基亚氨基-2,6-二氮杂 - 螺[3.4]十六烷基-6-YL）-4-氧代-1,4-二氢 - [1,8]萘啶 -3-羧酸，其制备方法和包含其的抗微生物药物组合物
公开(公告)号：US20100184795A1
公开(公告)日：2010-07-22
申请号：US12595606
申请日：2008-04-14
申请人： Jei Man Ryu , Dong Rack Choi , Jin Yang , Sue Hye Yoon , Seung Hwan Kim , Sae Kwang Ku
发明人： Jei Man Ryu , Dong Rack Choi , Jin Yang , Sue Hye Yoon , Seung Hwan Kim , Sae Kwang Ku
IPC分类号： A61K31/4375 , C07D471/04
CPC分类号： C07D519/00
摘要： Disclosed are aspartic acid salts of 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, methods for preparing the same, and antimicrobial pharmaceutical compositions comprising the same.
摘要翻译：公开了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]萘啶-3-羧酸，及其制备方法，以及包含其的抗微生物药物组合物。

2. 发明授权

US08324238B2 Aspartate of 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, method for preparing the same, and antimicrobial pharmaceutical composition comprising the same 有权
标题翻译： 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]萘啶的天冬氨酸 -3-羧酸，其制备方法，以及包含其的抗微生物药物组合物
公开(公告)号：US08324238B2
公开(公告)日：2012-12-04
申请号：US12595606
申请日：2008-04-14
申请人： Jei Man Ryu , Dong Rack Choi , Jin Yang , Sue Hye Yoon , Seung Hwan Kim , Sae Kwang Ku
发明人： Jei Man Ryu , Dong Rack Choi , Jin Yang , Sue Hye Yoon , Seung Hwan Kim , Sae Kwang Ku
IPC分类号： A01N43/42 , A61K31/44 , C07D471/02
CPC分类号： C07D519/00
摘要： Disclosed are aspartic acid salts of 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, methods for preparing the same, and antimicrobial pharmaceutical compositions comprising the same.
摘要翻译：公开了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]萘啶-3-羧酸，及其制备方法，以及包含其的抗微生物药物组合物。

3. 发明申请

US20120130075A1 R-7-(3-AMINOMETHYL-4-METHOXYIMINO-3-METHYL-PYRROLIDIN-1-YL)-1-CYCLOPROPYL-6-FLUORO-4-OXO-1,4-DIHYDRO-[1,8]NAPHTHYRIDINE-3-CARBOXYLIC ACID AND L-ASPARTIC ACID SALT, PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME FOR ANTIMICROBIAL 有权
标题翻译： R-7-（3-氨基甲酰基-4-甲氧基亚氨基-3-甲基 - 吡咯烷-1-基）-1-环丙基-6-氟-4-氧代-1,4-二氢 - [1,8]萘啶-3 - 羧酸和L-阿拉伯酸盐，其制备方法和包含其抗药性的药物组合物
公开(公告)号：US20120130075A1
公开(公告)日：2012-05-24
申请号：US13387080
申请日：2010-07-27
申请人： Dong Rack Choi , Jin Yang , Sue Hye Yoon , Sung Jae Pyun , Seung Hwan Kim , Seung-Kyoo Seong , Jei Man Ryu
发明人： Dong Rack Choi , Jin Yang , Sue Hye Yoon , Sung Jae Pyun , Seung Hwan Kim , Seung-Kyoo Seong , Jei Man Ryu
IPC分类号： C07D471/04
CPC分类号： C07D215/56 , A61K9/0019 , A61K9/145 , A61K9/2059 , A61K9/4858 , A61K31/4375 , C07C229/24 , C07D471/04 , C07D487/04 , C07D498/06
摘要： Disclosed herein are R-7-(3-aminomethyl-4-methoxyimino-3-methyl-pyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-[1,8]naphthyridine-3-carboxylic acid and L-aspartic acid salt, process for the preparation thereof and pharmaceutical composition comprising the same for antimicrobial. Because the R-7-(3-aminomethyl-4-methoxyimino-3-methyl-pyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-[1,8]naphthyridine-3-carboxylic acid and L-aspartic acid salt is more soluble and less toxic and has less side effects as an antimicrobial agent than hydrochloride and the other salts (D-aspartate and phosphate) conventionally used, the salt may be useful for oral and injectable administration.
摘要翻译：本文公开了R-7-（3-氨基甲基-4-甲氧基亚氨基-3-甲基 - 吡咯烷-1-基）-1-环丙基-6-氟-4-氧代-1,4-二氢 - [1,8] 萘啶-3-羧酸和L-天冬氨酸盐，其制备方法和包含其的抗微生物剂的药物组合物。因为R-7-（3-氨基甲基-4-甲氧基亚氨基-3-甲基 - 吡咯烷-1-基）-1-环丙基-6-氟-4-氧代-1,4-二氢 - [1,8]萘啶 -3-羧酸和L-天冬氨酸盐比常规使用的盐酸盐和其他盐（D-天冬氨酸盐和磷酸盐）更易溶解，毒性更小，作为抗微生物剂的副作用较小，该盐可用于口服和注射给药。

4. 发明授权

US08664240B2 R-7-(3-aminomethyl-4-methoxyimino-3-methyl-pyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-[1,8]naphthyridine-3-carboxylic acid and L-aspartic acid salt, process for the preparation thereof and pharmaceutical composition comprising the same for antimicrobial 有权
标题翻译： R-7-（3-氨基甲基-4-甲氧基亚氨基-3-甲基 - 吡咯烷-1-基）-1-环丙基-6-氟-4-氧代-1,4-二氢 - [1,8]二氮杂萘-3-酮 - 羧酸和L-天冬氨酸盐，其制备方法和包含其的抗微生物剂的药物组合物
公开(公告)号：US08664240B2
公开(公告)日：2014-03-04
申请号：US13387080
申请日：2010-07-27
申请人： Dong Rack Choi , Jin Yang , Sue Hye Yoon , Sung Jae Pyun , Seung Hwan Kim , Seung-Kyoo Seong , Jei Man Ryu
发明人： Dong Rack Choi , Jin Yang , Sue Hye Yoon , Sung Jae Pyun , Seung Hwan Kim , Seung-Kyoo Seong , Jei Man Ryu
IPC分类号： A01N43/42 , A61K31/44 , C07D471/04
CPC分类号： C07D215/56 , A61K9/0019 , A61K9/145 , A61K9/2059 , A61K9/4858 , A61K31/4375 , C07C229/24 , C07D471/04 , C07D487/04 , C07D498/06
摘要： Disclosed herein are R-7-(3-aminomethyl-4-methoxyimino-3-methyl-pyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-[1,8]naphthyridine-3-carboxylic acid and L-aspartic acid salt, process for the preparation thereof and pharmaceutical composition comprising the same for antimicrobial. Because the R-7-(3-aminomethyl-4-methoxyimino-3-methyl-pyrrolidin-1-yl) -1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-[1,8]naphthyridine-3-carboxylic acid and L-aspartic acid salt is more soluble and less toxic and has less side effects as an antimicrobial agent than hydrochloride and the other salts (D-aspartate and phosphate) conventionally used, the salt may be useful for oral and injectable administration.
摘要翻译：本文公开了R-7-（3-氨基甲基-4-甲氧基亚氨基-3-甲基 - 吡咯烷-1-基）-1-环丙基-6-氟-4-氧代-1,4-二氢 - [1,8] 萘啶-3-羧酸和L-天冬氨酸盐，其制备方法和包含其的抗微生物剂的药物组合物。因为R-7-（3-氨基甲基-4-甲氧基亚氨基-3-甲基 - 吡咯烷-1-基）-1-环丙基-6-氟-4-氧代-1,4-二氢 - [1,8]萘啶 -3-羧酸和L-天冬氨酸盐比常规使用的盐酸盐和其他盐（D-天冬氨酸盐和磷酸盐）更易溶解，毒性更小，作为抗微生物剂的副作用较小，该盐可用于口服和注射给药。

5. 发明申请

US20080200526A1 Composition for the Prevention and Treatment of Allergic Inflammatory Disease 审中-公开
标题翻译：用于预防和治疗过敏性炎症的组合物
公开(公告)号：US20080200526A1
公开(公告)日：2008-08-21
申请号：US11631762
申请日：2005-07-05
申请人： Jin Soo Lee , Sae Kwang Ku , Sang Ho Lee , Jei Man Ryu
发明人： Jin Soo Lee , Sae Kwang Ku , Sang Ho Lee , Jei Man Ryu
IPC分类号： A61K31/426 , A61P29/00
CPC分类号： A61K31/426
摘要： Disclosed herein is a composition for the treatment and prevention of allergic inflammatory diseases comprising N-hydroxy-4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxy]pentoxy}-benzamidine, 4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxy]pentoxy}-benzamidine or pharmaceutically acceptable salts. The composition exhibits excellent medicinal effects on allergic inflammatory diseases, with a great reduction in typical chronic inflammation symptoms, such as an increase of eosinophil level in bronchoalveolar lavage fluid, total leukocyte level and eosinophil level in blood, the hypertrophy or hyperplasia of bronchial epithelium due to an increase in the number of mucus cells, a reduction in alveolar surface area resulting from the hyptertrophy of alveolar walls, and the infiltration of inflammatory cells.
摘要翻译：本文公开了用于治疗和预防过敏性炎性疾病的组合物，其包含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} - 苯甲脒，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。该组合物对过敏性炎性疾病表现出优异的药用效果，典型的慢性炎症症状大大减少，如支气管肺泡灌洗液中嗜酸性粒细胞水平的增加，血液中的总白细胞水平和嗜酸性粒细胞水平，支气管上皮的肥大或增生增加粘液细胞的数量，由肺泡壁的低渗引起的肺泡表面积的减少和炎性细胞的浸润。

6. 发明申请

US20090054642A1 NOVEL BENZAMIDINE DERIVATIVE, PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING SAME 失效
标题翻译：新型苯扎明衍生物，其制备方法和包含其的药物组合物
公开(公告)号：US20090054642A1
公开(公告)日：2009-02-26
申请号：US12162701
申请日：2007-01-31
申请人： Jei Man Ryu , Jin Soo Lee , Young Goo Jin , Ki Young Lee , Jae Hoon Park , Yun Ha Hwang , Sae Kwang Ku
发明人： Jei Man Ryu , Jin Soo Lee , Young Goo Jin , Ki Young Lee , Jae Hoon Park , Yun Ha Hwang , Sae Kwang Ku
IPC分类号： C07D417/02 , C07D277/20 , C07D413/02 , C07D413/14
CPC分类号： C07D417/04 , C07D277/28 , C07D417/12
摘要： The present invention relates to a novel benzamidine derivative, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The benzamidine derivative of the present invention effectively inhibits osteoclast differentiation at an extremely low concentration, and greatly increases the trabecular bone volume, and thus it can be advantageously used for the prevention and treatment of osteoporosis.
摘要翻译：本发明涉及一种新的苄脒衍生物，其制备方法和包含其的药物组合物。本发明的苄脒衍生物以极低的浓度有效抑制破骨细胞分化，大大增加小梁骨体积，因此可有利地用于预防和治疗骨质疏松症。

7. 发明授权

US08178688B2 Benzamidine derivatives, process for the preparation thereof and pharmaceutical composition comprising the same 有权
标题翻译：苄脒衍生物，其制备方法和包含其的药物组合物
公开(公告)号：US08178688B2
公开(公告)日：2012-05-15
申请号：US11659556
申请日：2005-08-04
申请人： Jin Soo Lee , Seok Hoon Ahn , Young Goo Jin , Sang Mi Jin , Whui-Jung Park , Sae Kwang Ku , Yun Ha Hwang , Pan Soo Kim , Sun Shin Yi , Jei Man Ryu
发明人： Jin Soo Lee , Seok Hoon Ahn , Young Goo Jin , Sang Mi Jin , Whui-Jung Park , Sae Kwang Ku , Yun Ha Hwang , Pan Soo Kim , Sun Shin Yi , Jei Man Ryu
IPC分类号： C07D277/20 , C07D277/30 , C07D417/02 , C07D417/04 , C07D417/06 , C07D417/08
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。

8. 发明申请

US20100249402A1 NOVEL BENZAMIDINE DERIVATIVES, PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING OSTEPOROSIS COMPRISING THE SAME 审中-公开
标题翻译：新型苯扎明衍生物，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：US20100249402A1
公开(公告)日：2010-09-30
申请号：US12670814
申请日：2008-07-28
申请人： Jei Man Ryu , Jin Soo Lee , Young Goo Jin , Jae Hoon Park , Bo Kyung Kim , Dae Yeon Won , Yun-Ha Hwang , Ki Yoon Kim , Sae Kwang Ku
发明人： Jei Man Ryu , Jin Soo Lee , Young Goo Jin , Jae Hoon Park , Bo Kyung Kim , Dae Yeon Won , Yun-Ha Hwang , Ki Yoon Kim , Sae Kwang Ku
IPC分类号： C07D417/02 , C07D413/02
CPC分类号： C07D277/22 , C07D277/28 , C07D277/40 , C07D417/06
摘要： The present invention relates to novel benzamidine derivatives, a process for the preparation thereof and a pharmaceutical composition for preventing or treating osteoporosis comprising the same. The benzamidine derivatives of the present invention effectively inhibit osteoclast differentiation at an extremely low concentration, and thus can be advantageously used for the prevention and treatment of osteoporosis.
摘要翻译：本发明涉及新的苄脒衍生物，其制备方法和用于预防或治疗包含其的骨质疏松症的药物组合物。本发明的苄脒衍生物以极低的浓度有效抑制破骨细胞分化，因此可有利地用于预防和治疗骨质疏松症。

9. 发明授权

US07943646B2 Benzamidine derivative, process for the preparation thereof and pharmaceutical composition comprising same 失效
标题翻译：苄脒衍生物，其制备方法和包含其的药物组合物
公开(公告)号：US07943646B2
公开(公告)日：2011-05-17
申请号：US12162701
申请日：2007-01-31
申请人： Jei Man Ryu , Jin Soo Lee , Young Goo Jin , Ki Young Lee , Jae Hoon Park , Yun Ha Hwang , Sae Kwang Ku
发明人： Jei Man Ryu , Jin Soo Lee , Young Goo Jin , Ki Young Lee , Jae Hoon Park , Yun Ha Hwang , Sae Kwang Ku
IPC分类号： C07D277/22 , A61K31/426 , A61K31/155 , A61P19/10
CPC分类号： C07D417/04 , C07D277/28 , C07D417/12
摘要： The present invention relates to a novel benzamidine derivative, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The benzamidine derivative of the present invention effectively inhibits osteoclast differentiation at an extremely low concentration, and greatly increases the trabecular bone volume, and thus it can be advantageously used for the prevention and treatment of osteoporosis.
摘要翻译：本发明涉及一种新的苄脒衍生物，其制备方法和包含其的药物组合物。本发明的苯甲脒衍生物以极低的浓度有效抑制破骨细胞分化，大大增加小梁骨体积，因此可有利地用于预防和治疗骨质疏松症。

10. 发明申请

US20100240890A1 Novel benzamidine derivatives, process for the preparation thereof and pharmaceutical composition comprising the same 有权
标题翻译：新型苯甲脒衍生物，其制备方法和包含其的药物组合物
公开(公告)号：US20100240890A1
公开(公告)日：2010-09-23
申请号：US11659556
申请日：2005-08-04
申请人： Jin Soo Lee , Seok Hoon Ahn , Young Goo Jin , Sang Mi Jin , Whui-Jung Park , Sae Kwang Ku , Yu Ha Hwang , Pan Soo Kim , Sun Shin Yi , Jei Man Ryu
发明人： Jin Soo Lee , Seok Hoon Ahn , Young Goo Jin , Sang Mi Jin , Whui-Jung Park , Sae Kwang Ku , Yu Ha Hwang , Pan Soo Kim , Sun Shin Yi , Jei Man Ryu
IPC分类号： C07D277/30 , C07D417/04 , C07D277/40 , C07D277/48 , C07D417/12
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。

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