公开(公告)号：US08399663B2

公开(公告)日：2013-03-19

申请号：US12753415

申请日：2010-04-02

申请人： Junya Ohmori ,  Makoto Kasai ,  Takenori Kimura ,  Noritaka Hamada ,  Ryo Mizoguchi ,  Satoshi Miyamoto ,  Noriyuki Kawano

发明人： Junya Ohmori ,  Makoto Kasai ,  Takenori Kimura ,  Noritaka Hamada ,  Ryo Mizoguchi ,  Satoshi Miyamoto ,  Noriyuki Kawano

IPC分类号： C07D403/12 ,  A61K31/53 ,  A61P25/28

CPC分类号： A61K31/53 ,  C07D403/12

摘要： Anytime obtained is uniform crystal of N-(4-fluorophenyl)-N′-phenyl-N″-(pyrimidin-2-ylmethyl)-1,3,5-triazine-2,4,6-triamine (compound A) and/or N,N′-bis (4-fluorophenyl)-N″-(pyrimidin-2-ylmethyl)-1,3,5-triazine-2,4,6-triamine (compound B) as a medicament or a starting material for the preparation of the medicament, and provided are a fumarate of the compound A and/or the compound B having excellent stability and a novel crystal thereof. A salt of the compound A and/or the compound B with fumaric acid enables uniform crystal to be anytime obtained, and thus, it is a compound that is very useful as a medicament or a starting material for the preparation of the medicament having excellent stability.

摘要翻译： 得到的N-（4-氟苯基）-N'-苯基-N“ - （嘧啶-2-基甲基）-1,3,5-三嗪-2,4,6-三胺（化合物A）和 /或N，N'-二（4-氟苯基）-N“ - （嘧啶-2-基甲基）-1,3,5-三嗪-2,4,6-三胺（化合物B）作为药物或起始物 用于制备药物的材料，并且提供具有优异的稳定性和新颖结晶的化合物A和/或化合物B的富马酸盐。 化合物A和/或化合物B与富马酸的盐能够随时获得均匀的结晶，因此，作为制备具有优异稳定性的药物的药物或原料非常有用的化合物 。

公开(公告)号：US20090203741A1

公开(公告)日：2009-08-13

申请号：US12307843

申请日：2007-07-13

申请人： Noritaka Hamada ,  Ryo Mizoguchi ,  Kuniyuki Sano ,  Takaaki Sakaida ,  Yuji Awamura ,  Yu Iwakawa ,  Takahiko Tobe ,  Takashi Sugane

发明人： Noritaka Hamada ,  Ryo Mizoguchi ,  Kuniyuki Sano ,  Takaaki Sakaida ,  Yuji Awamura ,  Yu Iwakawa ,  Takahiko Tobe ,  Takashi Sugane

IPC分类号： A61K31/437 ,  C07D401/14 ,  A61P25/18

CPC分类号： C07D413/14

摘要： Object Provided are β-form crystal, γ-form crystal, and α-form crystal of a benzoxadiazole derivative, wherein a uniform crystal having sufficient qualities can be obtained with high reproducibility, and they can be anytime supplied as crystals of drug substance for use in producing pharmaceuticals, are particularly suitable for mass synthesis in industrial production, hardly exhibit hygroscopicity and have particularly excellent photo-resistance.Means for Resolution A solving means includes β-form crystal of 4-[3-isopropyl-5-(6-phenyl-3-pyridyl)-4H-1,2,4-triazol-4-yl]-2,1,3-benzoxadiazole, which shows an endothermic peak at 145 to 150° C. according to a differential scanning calorimeter analysis (DSC analysis) and shows X-ray powder diffraction peaks at 9.8, 11.1, 12.8, 13.3, 17.1, 20.2, 21.2 and 22.3 in 2θ(°), and the like.

摘要翻译： 本发明提供的是具有苯并二唑衍生物的β型晶体，γ型晶体和α型晶体，其中可以以高再现性获得具有足够质量的均匀晶体，并且它们可随时作为使用的药物晶体提供 在生产药物中，特别适用于工业生产中的大量合成，几乎不具有吸湿性并且具有特别优异的耐光性。 解决方法A解决方案包括4- [3-异丙基-5-（6-苯基-3-吡啶基）-4H-1,2,4-三唑-4-基] -2,1， 根据差示扫描量热分析（DSC分析），在145〜150℃显示出吸热峰，在9.8,11.1,12.8,13.3,17.1,20.2,21.2和/ 22.3 in 2theta（°）等。

公开(公告)号：US08278333B2

公开(公告)日：2012-10-02

申请号：US12307843

申请日：2007-07-13

申请人： Noritaka Hamada ,  Ryo Mizoguchi ,  Kuniyuki Sano ,  Takaaki Sakaida ,  Yuji Awamura ,  Yu Iwakawa ,  Takahiko Tobe ,  Takashi Sugane

发明人： Noritaka Hamada ,  Ryo Mizoguchi ,  Kuniyuki Sano ,  Takaaki Sakaida ,  Yuji Awamura ,  Yu Iwakawa ,  Takahiko Tobe ,  Takashi Sugane

IPC分类号： A61K31/4439 ,  C07D413/14

CPC分类号： C07D413/14

摘要： ObjectProvided are β-form crystal, γ-form crystal, and α-form crystal of a benzoxadiazole derivative, wherein a uniform crystal having sufficient qualities can be obtained with high reproducibility, and they can be anytime supplied as crystals of drug substance for use in producing pharmaceuticals, are particularly suitable for mass synthesis in industrial production, hardly exhibit hygroscopicity and have particularly excellent photo-resistance.Means for ResolutionA solving means includes β-form crystal of 4-[3-isopropyl-5-(6-phenyl-3-pyridyl)-4H-1,2,4-triazol-4-yl]-2,1,3-benzoxadiazole, which shows an endothermic peak at 145 to 150° C. according to a differential scanning calorimeter analysis (DSC analysis) and shows X-ray powder diffraction peaks at 9.8, 11.1, 12.8, 13.3, 17.1, 20.2, 21.2 and 22.3 in 2θ(°), and the like.

摘要翻译： 本发明提供一种苯并恶二唑衍生物的结晶，γ型结晶和α型结晶，其中可以以高再现性获得具有足够质量的均匀结晶，并且可随时作为药物物质的晶体供应 用于生产药物，特别适用于工业生产中的大量合成，几乎不具有吸湿性并且具有特别优异的耐光性。 解决方法A解决方法包括4- [3-异丙基-5-（6-苯基-3-吡啶基）-4H-1,2,4-三唑-4-基] -2,1' ，根据差示扫描量热分析（DSC分析），在145〜150℃显示出吸热峰，显示出9.8,11.1,12.8,13.3,17.1,20.2,21.2的X射线粉末衍射峰 和22.3英寸（2英寸）;（°）等。

公开(公告)号：US20060223831A1

公开(公告)日：2006-10-05

申请号：US10553151

申请日：2004-04-14

申请人： Isao Kinoyama ,  Kenichirou Sakamoto ,  Hiroki Okui ,  Noritaka Hamada ,  Akira Matsuhisa

发明人： Isao Kinoyama ,  Kenichirou Sakamoto ,  Hiroki Okui ,  Noritaka Hamada ,  Akira Matsuhisa

IPC分类号： A61K31/497 ,  C07D403/02

CPC分类号： C07D403/06

摘要： The 1-(2-methoxyethyl)-2-methyl-4,9-dioxo-3-(pyrazin-2-ylmethyl)-4,9-dihydro-1H-naphtho[2,3-d]imidazol-3-ium bromide of the invention and its crystals, particularly α- and β- form Crystals, have no hygroscopic property, have excellent stability and therefore are useful as production materials of medicines. Particularly, the β- form Crystal is most stable and markedly useful as a bulk for medicines.

摘要翻译： 将1-（2-甲氧基乙基）-2-甲基-4,9-二氧代-3-（吡嗪-2-基甲基）-4,9-二氢-1H-萘并[2,3-d]咪唑-3-酮 本发明的溴化物及其晶体，特别是α-和β-晶体，不具有吸湿性，具有优异的稳定性，因此可用作药物的生产材料。 特别地，晶体晶体是最稳定的并且显着地用作药物的主体。