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1. 发明专利

IL180985D0 N-HYDROXY-4-{5-[4-(5-ISOPROPYL-2-METHYL-1,3-THIAZOL-4-YL)PHENOXY]PENTOXY}BENZAMIDINE 2 METHANESULFONIC ACID SALT 未知
公开(公告)号：IL180985D0
公开(公告)日：2007-07-04
申请号：IL18098507
申请日：2007-01-25
申请人： DONG WHA PHARM IND CO LTD , JIN SOO LEE , JEI MAN RYU , SEOK HOON AHN , YOUNG GOO JIN , DONG HYUK SHIN , EUN HEE CHO , SEUNG KYOO SEONG , SOON KI CHO , CHAN SEOK JEON , KI YOUNG LEE , SE HYUN JUNG
IPC分类号： C07D20100101
摘要： Disclosed is an N-Hydroxy-4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxy]pentoxy} benzamidine 2 methansulfonic acid salt, which has excellent bioavailability. Also disclosed are a method of preparing the compound and a pharmaceutical composition comprising the compound.

2. 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。

3. 发明申请

US20060286032A1 A radiosotope-chitosan complex for treatment of prostate cancer 审中-公开
标题翻译：一种用于治疗前列腺癌的放射性脱氧壳聚糖复合物
公开(公告)号：US20060286032A1
公开(公告)日：2006-12-21
申请号：US10570295
申请日：2004-09-08
申请人： Jei-Man Ryu , Dong-Hyuk Shin , Seung-Kyoo Seong , Hee-Bog Yang , Eun-Jung Bae , Young-Jun Song , Kyung-Bae Park , Byung-Chul Shin
发明人： Jei-Man Ryu , Dong-Hyuk Shin , Seung-Kyoo Seong , Hee-Bog Yang , Eun-Jung Bae , Young-Jun Song , Kyung-Bae Park , Byung-Chul Shin
IPC分类号： A61K51/00 , C08B37/08
CPC分类号： A61K51/06 , A61K51/1282
摘要： Disclosed is a composition for treating prostate cancer. The composition for treating prostate cancer comprises as an effective ingredient a radioisotope-chitosan complex that includes a therapeutic radioisotope emitting beta radiation and chitosan. Also, the present invention discloses a kit for preparing the composition. When directly administered to a prostate cancer tissue, the radioisotope- chitosan complex is deposited in the applied target site while not leaking from the applied target site, and strongly inhibits the growth of prostate cancer cells while minimizing the side effects of conventional therapies, including urinary incontinence, urethral stricture and rectal bleeding. In addition, the radioisotope-chitosan complex may be used as an effective therapeutic agent for hormone-independent prostate cancer that is resistant to hormone therapy.
摘要翻译：公开了用于治疗前列腺癌的组合物。用于治疗前列腺癌的组合物包括放射性同位素 - 壳聚糖复合物作为有效成分，其包括发射β辐射和壳聚糖的治疗性放射性同位素。此外，本发明公开了一种用于制备组合物的试剂盒。当直接施用于前列腺癌组织时，放射性同位素 - 壳聚糖复合物沉积在施用的靶位点，而不会从施用的靶位点泄漏，并强烈地抑制前列腺癌细胞的生长，同时最小化常规治疗的副作用，包括尿尿失禁，尿道狭窄和直肠出血。此外，放射性同位素 - 壳聚糖复合物可用作对激素治疗具有抗性的激素非依赖性前列腺癌的有效治疗剂。

4. 发明申请

US20090176846A1 N-hydroxy-4- {5- [4- (5-isopropyl-2-methyl-1, 3-thiazol-4-yl) phenoxy] pentoxy} benzamidine 2 methanesulfonic acid salt 审中-公开
标题翻译： 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2甲磺酸盐
公开(公告)号：US20090176846A1
公开(公告)日：2009-07-09
申请号：US10584984
申请日：2005-11-22
申请人： Jei Man Ryu , Jin Soo Lee , Dong Hyuk Shin , Seung Kyoo Seong , Soon Ki Cho , Chan Seok Jeon , Young Goo Jin , Ki Young Lee , Se Hyun Jung , Eun Hee Cho , Seok Hoon Ahn
发明人： Jei Man Ryu , Jin Soo Lee , Dong Hyuk Shin , Seung Kyoo Seong , Soon Ki Cho , Chan Seok Jeon , Young Goo Jin , Ki Young Lee , Se Hyun Jung , Eun Hee Cho , Seok Hoon Ahn
IPC分类号： A61K31/426 , C07D277/28
CPC分类号： C07D277/24 , A61K9/143 , A61K31/426
摘要： Disclosed is an N-Hydroxy-4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxy]pentoxy} benzamidine 2 methansulfonic acid salt, which has excellent bioavailability. Also disclosed are a method of preparing the compound and a pharmaceutical composition comprising the compound.
摘要翻译：公开了具有优异生物利用度的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2甲磺酸盐。还公开了制备该化合物的方法和包含该化合物的药物组合物。

5. 发明申请

US20080166297A1 Radionuclide-Chitosan Complex Having an Improved Stablilized Gelatin in Administering Them to the Body and Their Preparation Method 审中-公开
标题翻译：具有改善的稳定明胶的放射性核素 - 壳聚糖复合物在体内及其制备方法
公开(公告)号：US20080166297A1
公开(公告)日：2008-07-10
申请号：US11720572
申请日：2005-12-01
申请人： Jei-Man Ryu , Dong-Hyuk Shin , Seung-Kyoo Seong , Hee-Bog Yang , Young-Jun Song , Eun-Jung Bae , Kyung-Bae Park , Byung-Chul Shin
发明人： Jei-Man Ryu , Dong-Hyuk Shin , Seung-Kyoo Seong , Hee-Bog Yang , Young-Jun Song , Eun-Jung Bae , Kyung-Bae Park , Byung-Chul Shin
IPC分类号： A61K51/04 , C07F5/00
CPC分类号： A61K51/06 , A61K31/22 , A61K51/1213
摘要： The present invention relates to a radionuclide-chitosan complex solution and its preparation method, and more particularly to the radionuclide-chitosan complex solution having a viscosity of 300˜2,400 cps, comprising an aqueous chitosan solution or a freeze-dried chitosan labeled with a radionuclide. The radionuclide-chitosan complex solution according to the present invention has a stable gelation state at a target region when injected into the body while maintaining a labeling yield of radioisotope to chitosan above 99%. Side effects may be minimized and treatment efficiency may be increased when injected to a patient.
摘要翻译：本发明涉及放射性核素 - 壳聚糖复合溶液及其制备方法，更具体地涉及粘度为300〜2400cps的放射性核素 - 壳聚糖复合溶液，其包含壳聚糖水溶液或用放射性核素标记的冷冻干燥壳聚糖。本发明的放射性核素 - 壳聚糖复合溶液在注射到体内时在靶区域具有稳定的凝胶化状态，同时保持壳聚糖的放射性同位素的标记收率高于99％。副作用可能最小化，并且当注射到患者时可以增加治疗效率。

6. 发明申请

US20080031811A1 Method For Preparing Radioactive Film 审中-公开
标题翻译：放射性膜制备方法
公开(公告)号：US20080031811A1
公开(公告)日：2008-02-07
申请号：US11575170
申请日：2005-09-12
申请人： Jei-Man Ryu , Yu-Eun Kim , Seung-Kyoo Seong , Dong-Hyuk Shin , Byung-Ho Cho , Young-Jun Song , Kyung-Bae Park , Byung-Chul Shin
发明人： Jei-Man Ryu , Yu-Eun Kim , Seung-Kyoo Seong , Dong-Hyuk Shin , Byung-Ho Cho , Young-Jun Song , Kyung-Bae Park , Byung-Chul Shin
IPC分类号： A61K51/12 , A61M36/14
CPC分类号： A61K51/1279 , C08J5/18 , C08J2375/04 , C08K3/16 , C08K3/28
摘要： The present invention relates to a method for preparing a radioactive film for local radioactive treatment. More particularly, the present invention relates to a method for preparing a radioactive film comprising the steps of; dissolving 0.1˜14.5 weight % of a stable nuclide and 13˜32.5 weight % of a film-forming base for the total amount of a solvent in the solvent; applying a stable nuclide solution on a release paper by a coater and drying; and irradiating a stable nuclide film with neutrons in a nuclear reactor. A method for preparing a radioactive film according to the present invention provides a radioactive film having a uniform distribution of radionuclides and an even thickness. Therefore, the therapeutic efficacy of the radioactive film for selective treatment of a lesion may be maximized by attaching the radioactive film on a patient's skin or a mucous membrane and by direct radioactive radiation.
摘要翻译：本发明涉及一种用于局部放射性处理的放射性膜的制备方法。更具体地，本发明涉及一种制备放射性膜的方法，包括以下步骤：将0.1〜14.5重量％的稳定核素和13〜32.5重量％的成膜基质溶解在溶剂中的溶剂的总量; 通过涂布机将稳定的核素溶液施加在剥离纸上并干燥; 并在核反应堆中用中子照射稳定的核素膜。根据本发明的制备放射性膜的方法提供了具有均匀分布的放射性核素的均匀厚度的放射性膜。因此，通过将放射性膜附着在患者的皮肤或粘膜上以及通过直接的放射性辐射，用于选择性治疗病变的放射性膜的治疗功效可以最大化。

7. 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。

8. 发明申请

US20100317853A1 NOVEL IMATINIB CAMSYLATE AND METHOD FOR PREPARING THEREOF 审中-公开
标题翻译：新型樟脑磺酸钠及其制备方法
公开(公告)号：US20100317853A1
公开(公告)日：2010-12-16
申请号：US12525962
申请日：2008-02-01
申请人： Yoon Seok Oh , Jae Kyung Lim , Dong Hyuk Shin , Seung Kyoo Seong , Sang Ho Lee , Hak Soo Lee , Eun Hee Cho , Jei Man Ryu
发明人： Yoon Seok Oh , Jae Kyung Lim , Dong Hyuk Shin , Seung Kyoo Seong , Sang Ho Lee , Hak Soo Lee , Eun Hee Cho , Jei Man Ryu
IPC分类号： C07D401/14
CPC分类号： C07D401/04
摘要： The present invention relates to a novel imatinib camsylate and a method for preparing the same. Imatinib camsylate according to the present invention has a faster absorption rate and higher absorption concentration in terms of pharmacokinetics, and further has excellent water solubility, as compared to commercially available imatinib mesylate.
摘要翻译：本发明涉及新颖的伊马替尼樟脑磺酸盐及其制备方法。与市售的甲磺酸伊马替尼相比，本发明的伊马替尼樟脑磺酸盐在药代动力学方面具有更快的吸收速率和更高的吸收浓度，并且还具有优异的水溶性。

9. 发明申请

US20070254930A1 Oral Preparation Having Improved Bioavailability 审中-公开
标题翻译：具有改善生物利用度的口服制剂
公开(公告)号：US20070254930A1
公开(公告)日：2007-11-01
申请号：US11577469
申请日：2005-11-22
申请人： Jei Ryu , Soon Cho , Se Jung , Seung-Kyoo Seong , Eun Cho , Seok Ahn , Yun-Jung Kim
发明人： Jei Ryu , Soon Cho , Se Jung , Seung-Kyoo Seong , Eun Cho , Seok Ahn , Yun-Jung Kim
IPC分类号： A61K31/426 , A61P19/10 , C07D277/28
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) phenoxy]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-1,3-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-1,3-thiazol-4-yl) phenoxy]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} - 苄脒或药学上的凝胶化在释放的早期阶段可接受的盐，其增加溶解速率并显着提高生物利用度。

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