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1. 发明公开

KR1020030076446A (2Ｓ)-Ｎ-[5-[아미노(이미노)메틸]-2-티에닐]메틸-1-[(2Ｒ)-2-[(카복시메틸)아미노]-3,3-디페닐프로파노일]-2-피롤리딘카르복사미드 말레산 염 및 그의 제조방법 无效
标题翻译：（2S）-N- [5- [氨基（亚氨基）甲基] -2-苯基]甲基-1 - [（2R）-2 - [（羧甲基）氨基] -3,3-二苯基丙酰基] -2-吡咯烷酮甲酰胺酸盐和制剂
公开(公告)号：KR1020030076446A
公开(公告)日：2003-09-26
申请号：KR1020030017853
申请日：2003-03-21
申请人： 주식회사 엘지생명과학
发明人： 김애리 , 박재현 , 윤석균 , 박철원 , 조관형
IPC分类号： C07D409/12
CPC分类号： C07K5/06078 , C07K2299/00
摘要： PURPOSE: (2S) - N - £5 - £amino (imino) methyl| - 2 - thienyl| methyl - 1 - £(2R) - 2 - £(carboxymethyl) amino| - 3,3 - diphenylpropanoyl| - 2 - pyrolidinecarboxamide maleic acid salts and a preparation method thereof are provided, which compounds has improved properties such as improved stability and undeliquescence at 93% of relative humidity, so that it can be useful as a thrombin inhibitor. CONSTITUTION: (2S) - N - £5 - £amino (imino) methyl| - 2 - thienyl| methyl - 1 - £(2R) - 2 - £(carboxymethyl) amino| - 3,3 - diphenylpropanoyl| - 2 - pyrolidinecarboxamide maleic acid salts represented by formula 1 are provided. A method for preparing (2S) - N - £5 - £amino (imino) methyl| - 2 - thienyl| methyl - 1 - £(2R) - 2 - £(carboxymethyl) amino| - 3,3 - diphenylpropanoyl| - 2 - pyrolidinecarboxamide maleic acid salts of formula 1 comprises reacting a free compound of formula 1 with maleic acid in the presence of alcohol solvent, wherein alcohol solvent is selected from methanol, ethanol, propanol, butanol, isopropanol and octanol. Crystalline forms of (2S) - N - £5 - £amino (imino) methyl| - 2 - thienyl| methyl - 1 - £(2R) - 2 - £(carboxymethyl) amino| - 3,3 - diphenylpropanoyl| - 2 - pyrolidinecarboxamide maleic acid salts of formula 1 is prepared by recrystallizing the amorphous compound of formula 1.
摘要翻译：目的：（2S） - N - 5 - £氨基（亚氨基）甲基 2-噻吩基甲基-1 - （2R）-2 - （羧甲基）氨基| -3,3-二苯基丙酰基 -2-吡咯烷甲酰胺马来酸盐及其制备方法，该化合物具有改善的性能，例如93％相对湿度下的稳定性和未起泡性改善，因此可用作凝血酶抑制剂。构成：（2S） - N - 5 - £氨基（亚氨基）甲基 2-噻吩基甲基-1 - （2R）-2 - （羧甲基）氨基| -3,3-二苯基丙酰基 -2-吡啶烷甲酰胺马来酸盐由式1表示。制备（2S）-N - 5-£氨基（亚氨基）甲基的方法 2-噻吩基甲基-1 - （2R）-2 - （羧甲基）氨基| -3,3-二苯基丙酰基式2的吡咯烷甲酰胺马来酸盐包括在醇溶剂存在下使游离的式1化合物与马来酸反应，其中醇溶剂选自甲醇，乙醇，丙醇，丁醇，异丙醇和辛醇。（2S）-N - 5-£氨基（亚氨基）甲基的结晶形式 2-噻吩基甲基-1 - （2R）-2 - （羧甲基）氨基| -3,3-二苯基丙酰基式2的吡咯烷甲酰胺马来酸盐通过将式1的无定形化合物重结晶来制备。

2. 发明公开

KR1020030076445A (2Ｓ)-Ｎ-[5-[아미노(이미노)메틸]-2-티에닐]메틸-1-[(2Ｒ)-2-[(카복시메틸)아미노]-3,3-디페닐프로파노일]-2-피롤리딘카르복사미드ㆍｎＨ2Ｏ의 새로운 결정형 无效
标题翻译：（2S）-N- [5- [氨基（亚氨基）甲基] -2-苯基]甲基-1 - [（2R）-2 - [（羧甲基）氨基] -3,3-二苯基丙酰基] -2的晶体形式 - 吡咯烷酮酰胺NH 2 O
公开(公告)号：KR1020030076445A
公开(公告)日：2003-09-26
申请号：KR1020030017851
申请日：2003-03-21
申请人： 주식회사 엘지생명과학
发明人： 김애리 , 박재현 , 윤석균 , 김봉찬 , 김성지 , 조관형
IPC分类号： C07D409/12
CPC分类号： C07D409/12 , C07K5/06078 , C07K2299/00
摘要： PURPOSE: Crystalline forms of (2S) - N - £5 - £amino (imino) methyl| - 2 - thienyl| methyl - 1 - £(2R) - 2 - £(carboxymethyl) amino| - 3,3 - diphenylpropanoyl| - 2 - pyrolidinecarboxamide·nH2O are provided, which compounds have improved physicochemical activity than amorphous forms. CONSTITUTION: Crystalline forms of (2S) - N - £5 - £amino (imino) methyl| - 2 - thienyl| methyl - 1 - £(2R) - 2 - £(carboxymethyl) amino| - 3,3 - diphenylpropanoyl| - 2 - pyrolidinecarboxamide·nH2O represented by formula 1 are provided, wherein n is number of crystal within a molecule, and 0, 1, 3, 4, 6 or 7.5; X-ray diffraction angle is 13.6, 14.7, 23.2 and 27.5 degree and the water content is 2 to 9% when n is 1; X-ray diffraction angle is 7.0, 12.2 and 19.2 degree and the water content is 9 to 15% when n is 4; and X-ray diffraction angle is 7.3, 9.1, 18.0 and 28.8 degree and the water content is 16 to 26% when n is 7.5.
摘要翻译：目的：（2S）-N - 5-£氨基（亚氨基）甲基的结晶形式 2-噻吩基甲基-1 - （2R）-2 - （羧甲基）氨基| -3,3-二苯基丙酰基 -2-吡咯烷甲酰胺·nH 2 O，这些化合物比无定形形式具有改善的物理化学活性。构成：（2S）-N - 5-£氨基（亚氨基）甲基的结晶形式 2-噻吩基甲基-1 - （2R）-2 - （羧甲基）氨基| -3,3-二苯基丙酰基提供了由式1表示的2-吡啶烷甲酰胺·nH 2 O，其中n是分子内的结晶数，0,1,3,4,6或7.5; 当n为1时，X射线衍射角为13.6,14.7,23.2和27.5度，水含量为2〜9％当n为4时，X射线衍射角为7.0,12.2,19.2度，含水率为9〜15％当n为7.5时，X射线衍射角为7.3°，9.1°，18.0°和28.8°，水含量为16％〜26％。

3. 发明公开

KR1020010063274A 〔1-｛〔1-（1,3-벤조디옥솔-5-일메틸-1Ｈ-이미다졸-5-일〕메틸｝-4-(1-나프틸)-1Ｈ-피롤-3-일〕（4-메틸-1-피페라지닐）메타논의 약학적 조성물 无效
标题翻译： 1- {1-（1,3-苯并二唑-5-基甲基）-1H-咪唑-5-基甲基} -4-（1-萘基）-1H-吡咯-3-基（4-甲基 - 哌嗪基）甲酮
公开(公告)号：KR1020010063274A
公开(公告)日：2001-07-09
申请号：KR1019990060305
申请日：1999-12-22
申请人： 주식회사 엘지생명과학
发明人： 김애리 , 이진화 , 박재현 , 이선화 , 이승학
IPC分类号： A61K31/41 , A61K31/335 , A61K31/50
CPC分类号： A61K31/357 , A61K9/08 , A61K9/2013 , A61K31/4164 , A61K31/498
摘要： PURPOSE: Pharmaceutical compositions of £1-{1-(1,3-benzodioxol-5-ylmethyl-1h-imidazole-5-yl)methyl}-4- (1-naphthyl)-1h-pyrrole-3-yl|(4-methyl-1-piperazinyl) methanone containing pharmaceutically allowable acidulants, dissolving agents for oral administration, or especially buffering agent for an injection is prepared to increase in vivo bioavailability and pharmacokinetic property thereof. CONSTITUTION: The compound represented by the chemical formula 1 is characterized by incorporating pharmaceutically allowable acidulants, dissolving agents, and buffering agents where the amount of acidulants selected from tartaric acid, citric acid and alginic acid is preferably in the equivalent ratio ranging from 0.2 to 1 based on the compound and the amount of dissolving agents selected from sodium lauryl sulfate, Poloxamer¬R (polyethylene polypropylene glycol), Tween¬R 20, 40, 60 (polyoxyethylene 20, 40, 60 sorbitan monostearate) is preferably in the parts by weight ranging from 1 to 500wt.% based on the compound and also the amount of buffering agent selected from glycine-hydrochloric acid solution, acetic acid-acetic acid salts solution, citric acid-citric acid salts solution, phosphoric acid-phosphoric acid salts solution is preferably in the concentration ranging 10 to 50mg/ml based on the compound. Further, the composition also contains diluent, flavor, lubricant, suspension agent, binder, disintegrating agent, stabilizer, tonicity adjustment agent and preservative agent.
摘要翻译：目的：1- {1-（1,3-苯并间二氧杂环戊烯-5-基甲基-1H-咪唑-5-基）甲基} -4-（1-萘基）-1H-吡咯-3-基}（ 4-甲基-1-哌嗪基）甲酮，其制备用于口服给药的溶解剂或特别是用于注射的缓冲剂，以提高其体内生物利用度和药代动力学性质。构成：由化学式1表示的化合物的特征在于加入药学上可允许的酸化剂，溶解剂和缓冲剂，其中选自酒石酸，柠檬酸和海藻酸的酸化剂的量优选为0.2至1当量比基于化合物和选自月桂基硫酸钠，泊洛沙姆-R（聚乙烯聚丙二醇），Tween-20,40,60（聚氧乙烯20,40,60脱水山梨糖醇单硬脂酸酯）的溶解剂的量优选为重量份基于化合物1〜500重量％，选自甘氨酸 - 盐酸溶液，乙酸 - 乙酸盐溶液，柠檬酸 - 柠檬酸盐溶液，磷酸 - 磷酸盐溶液的缓冲剂的量为优选浓度为10至50mg / ml，基于该化合物。此外，该组合物还含有稀释剂，香料，润滑剂，悬浮剂，粘合剂，崩解剂，稳定剂，张力调节剂和防腐剂。

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