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公开(公告)号：EP2275430B1
公开(公告)日：2012-05-16
申请号：EP09733364.5
申请日：2009-04-13
发明人： TAKEUCHI, Hideki , TSURU, Eiji
IPC分类号： C07H17/02 , A61K31/7056 , A61P3/10
CPC分类号： C07H17/02
摘要： Disclosed is a novel form of 3-(3-{4-[3-(β-D-glucopyranosyl-oxy)-5-isopropyl-1H-pyrazole-4-ylmethyl]-3-methylphenoxy}propylamino)-2,2-dimethyl-propionamide with improved storage stability. 3-(3-{4-[3-(β-D-glucopyranosyloxy)-5-isopropyl-1H-pyrazole-4-ylmethyl]-3-methyl-phenoxy}propylamino)-2,2-dimethylpropionamide hemifumarate dihydrate is useful as a pharmaceutical starting material because it has extremely outstanding storage stability. Moreover it shows extremely favourable crystallinity; and it is suited to industrial production because it can be purified by simple methods.
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公开(公告)号：EP2228378A1
公开(公告)日：2010-09-15
申请号：EP08867231.6
申请日：2008-12-24
发明人： TAKEUCHI, Hideki , TSURU, Eiji
IPC分类号： C07H17/02 , A61K31/7056 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/08 , A61P3/10 , A61P7/10 , A61P9/04 , A61P9/10 , A61P9/12 , A61P19/06 , A61P43/00
CPC分类号： C07H17/02
摘要： The present invention provides a novel form of 3-(3-{4-[3-(β-D-gluco-pyranosyloxy)-5-isopropyl-1H-pyrazol-4-ylmethyl]-3-methylphenoxy}propylamino)-2,2-dimethylpropionamide with improved storage stability. Since bis[3-(3-{4-[3-( - D-glucopyranosyloxy)-5-isopropyl-1H-pyrazol-4-ylmethyl]-3-methylphenoxy}pr opylamino)-2,2-dimethylpropionamide] monosebacate has extremely excellent storage stability, it is useful as a drug substance. Furthermore, it shows an extremely good crystalline property and can be purified by a convenient method, and therefore is suitable for the industrial preparation.
摘要翻译： 本发明提供3-（3- {4- [3-（β-D-吡喃葡萄糖基氧基）-5-异丙基-1H-吡唑-4-基甲基] -3-甲基苯氧基}丙基氨基）-2 ，具有改善的储存稳定性的2-二甲基丙酰胺。 由于双[3-（3- {4- [3 - （ - D-吡喃葡萄糖基氧基）-5-异丙基-1H-吡唑-4-基甲基] -3-甲基苯氧基}丙氨基）-2,2-二甲基丙酰胺] 极其优异的保存稳定性，作为药物有用。 此外，它表现出非常好的结晶性，并且可以通过简便的方法进行纯化，因此适用于工业制备。
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公开(公告)号：EP4091670A1
公开(公告)日：2022-11-23
申请号：EP21767151.0
申请日：2021-03-10
IPC分类号： A61P1/04 , C07D471/04 , A61K31/4188
摘要： As a drug substance, a crystal having good physical properties is preferable. However, the crystal form that is most excellent as a drug substance may vary with the compound. In general, it is difficult to predict a crystal form of a drug substance having good physical properties, and it is required to variously examine each compound. Therefore, an object of the present invention is to provide a crystal having good physical properties as a drug substance for a novel compound or a salt thereof.
The present invention relates to a crystal of the compound represented by the following formula (I) or a salt thereof useful for the treatment of an inflammatory bowel disease.-
公开(公告)号：EP2535342B1
公开(公告)日：2014-08-06
申请号：EP11742250.1
申请日：2011-02-09
发明人： JO, Kazumichi , TAKEUCHI, Hideki
IPC分类号： C07D495/04 , A61K31/519 , A61P5/04 , A61P15/08 , A61P15/16 , A61P15/18 , A61P35/00
CPC分类号： A61K31/519 , A61K9/0053 , A61K31/14 , C07B2200/13 , C07D495/04
摘要： An objective of the present invention is to improve the solubility of 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid. The present invention provides 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyl-oxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxy lic acid choline salt has excellent solubility and storage stability.
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公开(公告)号：EP2535342A1
公开(公告)日：2012-12-19
申请号：EP11742250.1
申请日：2011-02-09
发明人： JO, Kazumichi , TAKEUCHI, Hideki
IPC分类号： C07D495/04 , A61K31/519 , A61P5/04 , A61P15/08 , A61P15/16 , A61P15/18 , A61P35/00
CPC分类号： A61K31/519 , A61K9/0053 , A61K31/14 , C07B2200/13 , C07D495/04
摘要： An objective of the present invention is to improve the solubility of 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid.
The present invention provides 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyl-oxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxy lic acid choline salt has excellent solubility and storage stability.摘要翻译： 本发明的一个目标是提高的3- [2-氟-5-（2,3-二氟-6-甲氧基苄基氧基）-4-甲氧基苯基] -2,4-二氧代-1,2,3-溶解度， 4四氢噻吩[3,4-d]嘧啶-5-羧酸。 本发明提供了3- [2-氟-5-（2,3-二氟-6-甲氧基苄基氧基）-4-甲氧基苯基] -2,4-二氧代-1,2,3,4-四氢噻吩并[3， 4-d]嘧啶-5-羧基LIC酸胆碱盐具有优异的溶解性和储存稳定性。
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公开(公告)号：EP2275430A1
公开(公告)日：2011-01-19
申请号：EP09733364.5
申请日：2009-04-13
发明人： TAKEUCHI, Hideki , TSURU, Eiji
IPC分类号： C07H17/02 , A61K31/7056 , A61P3/10
CPC分类号： C07H17/02
摘要： The present invention provides a novel form of 3-(3-{4-[3-(β-D-glucopyranosyloxy)-5-isopropyl-1H-pyrazol-4-ylmethyl]-3-methylphenoxy}propylamino)-2,2-dimethylpropionamide with improved storage stability. Since 3-(3-{4-[3-(β-D-glucopyranosyloxy)-5-isopropyl-1H-pyrazol-4-ylmethyl]-3-methylphenoxy}-propylamino)-2,2-dimethylpropionamide hemifumarate dihydrate has extremely excellent storage stability, it is useful as a drug substance. Furthermore, it shows an extremely good crystalline property and can be purified by a convenient method, and therefore is suitable for the industrial preparation.
摘要翻译： 本发明提供3-（3- {4- [3-（β-D-吡喃葡萄糖基氧基）-5-异丙基-1H-吡唑-4-基甲基] -3-甲基苯氧基}丙基氨基）-2,2 - 二甲基丙酰胺具有改善的储存稳定性。 由于3-（3- {4- [3-（β-D-吡喃葡萄糖基氧基）-5-异丙基-1H-吡唑-4-基甲基] -3-甲基苯氧基}丙基氨基）-2,2-二甲基丙酰胺半富马酸盐二水合物 保存稳定性优异，作为药物有用。 此外，它表现出非常好的结晶性，并且可以通过简便的方法进行纯化，因此适用于工业制备。
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公开(公告)号：EP4177257A1
公开(公告)日：2023-05-10
申请号：EP21837478.3
申请日：2021-07-05
发明人： TAKEUCHI, Hideki , JO, Kazumichi
IPC分类号： C07D495/04 , A61K31/4365 , A61P5/10 , A61P25/00 , A61P25/16
摘要： [Problem] An object of the present invention is to provide a compound which has high storage stability and is suitable for use as a drug substance.
[Solution] The present invention relates to a succinate salt of 1-{[(4aR,6R,8aR)-2-amino-3-cyano-8-methyl-4,4a, 5,6,7,8,8a,9-octahydrothieno[3,2-g]quinolin-6-yl]carbonyl}-3-[2-(dimethylamino)ethyl]-1-propylurea, which is suitable as a drug substance having excellent storage stability and crystallinity and is useful for the treatment or prevention of Parkinson's disease, restless legs syndrome, hyperprolactinemia or the like.-
9.发明公开NOVEL CRYSTALS OF 5-HYDROXYCARBAMIMIDOYL-2-HYDROXYBENZENESULFONAMIDE DERIVATIVE 审中-公开NEUE KRISTALLE EINES 5-羟基卡马西平2-羟基苯并呋喃胺衍生物
公开(公告)号：EP1486485A1
公开(公告)日：2004-12-15
申请号：EP03744508.7
申请日：2003-03-04
发明人： MUKAIYAMA, Harunobu , KAI, Yuichiro , TAKEUCHI, Hideki , YOKOYAMA, Kenji , TERAO, Yoshihiro , AKAHANE, Satoshi
IPC分类号： C07C317/32 , A61K31/216 , A61P7/02
CPC分类号： C07C317/32
摘要： The present invention provides a novel crystalline form of n-butyl [4-[2-[2-hydroxy-5-(N-hydroxycarbamimidoyl) benzenesulfonylamino]ethyl]-2'-methanesulfonyl-3-yloxy] acetate hydrochloride, pharmaceutical compositions containing the same and their uses, which exhibits excellent inhibitory activities against activated blood coagulation factor X, and is useful for the treatment or prevention of a tromboembolic disease.
摘要翻译： 本发明提供了一种新的结晶形式的正丁基Ä4-Ä2-²2-羟基-5-（N-羟基甲脒基）苯磺酰基氨基乙基-2'-甲磺酰基-3-基氧乙酸盐酸盐，含有它们的药物组合物及其用途， 对活化凝血因子X表现出优异的抑制活性，可用于治疗或预防血栓栓塞性疾病。
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