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1. 发明授权

US06552197B2 Condensed-hexacyclic compounds and a process therefor 失效
标题翻译：缩合六环化合物及其制备方法
公开(公告)号：US06552197B2
公开(公告)日：2003-04-22
申请号：US09876945
申请日：2001-06-11
申请人： Shinji Kamihara , Kazuaki Kanai , Shigeru Noguchi , Hirofumi Terasawa , Hiroaki Kitaoka
发明人： Shinji Kamihara , Kazuaki Kanai , Shigeru Noguchi , Hirofumi Terasawa , Hiroaki Kitaoka
IPC分类号： C07D47100
CPC分类号： C07D491/22 , Y02P20/55
摘要： Disclosed are a process for the preparation of a compound represented by the formula (1), which comprises treating a compound represented by the formula (2) with methanesulfonic acid and then subjecting the thus-treated compound to recrystallization; and Compound (1) so obtained. This Compound (1) is free of hygroscopicity, excellent in filterability and solubility and easy in handling. Furthermore, according to the preparation process of the present invention, an unnecessary isomer can be converted into the target one and separation of the target isomer can be conducted easily.
摘要翻译：公开了一种制备式（1）表示的化合物的方法，其包括用甲磺酸处理由式（2）表示的化合物，然后使经过处理的化合物进行重结晶; 和化合物（1）。该化合物（1）不具有吸湿性，过滤性和溶解性优异，易于处理。此外，根据本发明的制备方法，可以将不必要的异构体转化成目标物，并且可以容易地进行目标异构体的分离。

2. 发明授权

US06504029B1 Condensed-hexacyclic compounds and a process therefor 失效
公开(公告)号：US06504029B1
公开(公告)日：2003-01-07
申请号：US08501933
申请日：1995-07-13
申请人： Shinji Kamihara , Kazuaki Kanai , Shigeru Noguchi , Hirofumi Terasawa , Hiroaki Kitaoka
发明人： Shinji Kamihara , Kazuaki Kanai , Shigeru Noguchi , Hirofumi Terasawa , Hiroaki Kitaoka
IPC分类号： C07D47116
CPC分类号： C07D491/22 , Y02P20/55
摘要： Disclosed are a process for the preparation of a compound represented by the formula (1), which comprises treating a compound represented by the formula (2) with methanesulfonic acid and then subjecting the thus-treated compound to recrystallization; and Compound (1) so obtained. This Compound (1) is free of hygroscopicity, excellent in filterability and solubility and easy in handling. Furthermore, according to the preparation process of the present invention, an unnecessary isomer can be converted into the target one and separation of the target isomer can be conducted easily.

3. 发明授权

US5948913A Hydrate for drug use 失效
标题翻译：水合物用于药物使用
公开(公告)号：US5948913A
公开(公告)日：1999-09-07
申请号：US836583
申请日：1997-05-14
申请人： Kenjiro Yamamoto , Akihiko Miyadera , Hiroaki Kitaoka
发明人： Kenjiro Yamamoto , Akihiko Miyadera , Hiroaki Kitaoka
IPC分类号： C07D403/14 , A61K31/497 , A61P25/08 , C07D403/06 , A61K31/495
CPC分类号： C07D403/06
摘要： Crystals of 3-�2-�4-(3-chloro-2-methylphenyl)-1-piperazinyl!ethyl!-5,6-dimethoxy-1-(4-imidazolylmethyl)-1H-indazole dihydrochloride which is a hydrate for pharmaceutical use having excellent characteristics as a pharmaceutical material that has high storage stability and which substantially has specified X-ray diffraction characteristics, more particularly, the dihydrochloride is 3.5-hydrate.
摘要翻译： PCT No.PCT / JP95 / 02317 Sec。 371日期1997年5月14日 102（e）日期1997年5月14日PCT提交1995年11月14日PCT公布。公开号WO96 / 15124 日期1996年5月23日3- [2- [4-（3-氯-2-甲基苯基）-1-哌嗪基]乙基] -5,6-二甲氧基-1-（4-咪唑基甲基）-1H-吲唑二盐酸盐的晶体是具有优异特性的药物用水合物，其具有高储存稳定性且基本上具有规定的X射线衍射特性，特别是二盐酸盐为3.5水合物。

4. 发明授权

US06169108A Anhydrous crystals 失效
标题翻译：无水晶体
公开(公告)号：US06169108A
公开(公告)日：2001-01-02
申请号：US08913615
申请日：1997-11-07
申请人： Yukio Sato , Hiroaki Kitaoka , Tatsuya Terada , Makoto Ono
发明人： Yukio Sato , Hiroaki Kitaoka , Tatsuya Terada , Makoto Ono
IPC分类号： A61K3140
CPC分类号： C07D207/27
摘要： An anhydrous crystal of a compound represented by the formula: R2—CH2CONH—R1 wherein R1 represents a substituted or non-substituted pyridyl group or substituted or non-substituted phenyl group and R2 represents a substituted or non-substituted 2-oxo-1-pyrrolidinyl group, characterized in that said crystal is substantially free from hygroscopicity. For example, by drying a hydrous crystal of said compound at a temperature of 80° C. or above under reduced pressure, an anhydrous crystal is provided that exhibits a weight increase of 1% or less when stored under the relative humidity of 83% at the temperature of 25° C. for 30 days. By using the anhydrous crystal for the manufacture of a medicament comprising the compound as an active ingredient, a product with a constant content of the active ingredient can be obtained.
摘要翻译：由下式表示的化合物的无水晶体：R2-CH2CONH-R1其中R1表示取代或未取代的吡啶基或取代或未取代的苯基，R2表示取代或未取代的2-氧代-1- 吡咯烷基，其特征在于所述晶体基本上没有吸湿性。例如，通过在减压下在80℃以上的温度下干燥所述化合物的含水结晶，提供无水结晶，当在83％的相对湿度下储存时，其重量增加1％以下温度为25°C，持续30天。通过使用无水晶体制造包含该化合物作为活性成分的药物，可以获得具有恒定含量的活性成分的产物。

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