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1. 发明申请

US20130144050A1 CRYSTAL FORM OF 4-ISOPROPYLPHENYL GLUCITOL COMPOUND AND PROCESS FOR PRODUCTION THEREOF 有权
标题翻译： 4-异丙基苯酚化合物的晶体形式及其生产方法
公开(公告)号：US20130144050A1
公开(公告)日：2013-06-06
申请号：US13816647
申请日：2011-08-19
申请人： Yoshihiro Kimura , Koreaki Imura , Naoto Osaki , Ayumi Matsushima
发明人： Yoshihiro Kimura , Koreaki Imura , Naoto Osaki , Ayumi Matsushima
IPC分类号： A61K31/7028 , C07H15/203 , C07H1/00
CPC分类号： C07H15/203 , C07D309/10 , C07H1/00
摘要： A highly stable crystal of (1S)-1,5-anhydro-1-[5-(4-{(1E)-4-[(1-{[2-(dimethylamino)ethyl]amino}-2-methyl-1-oxopropan-2-yl)amino]-3,3-dimethyl-4-oxobut-1-en-1-yl}benzyl)-2-methoxy-4-(propan-2-yl)phenyl]-D-glucitol, and a process for producing the crystal are provided. Specifically, an ethanolate having the following physical properties, and a plurality of other crystal forms transformed from the ethanolate are provided: (a) Having peaks at 2θ=5.9 degrees, 17.1 degrees, 17.6 degrees and 21.5 degrees in X-ray powder diffraction (Cu—Kα); (b) Showing characteristic absorption bands at 3538 cm−1, 3357 cm−1, 2964 cm−1, 1673 cm−1, 1634 cm−1 and 1505 cm−1 in an infrared absorption spectrum; and (c) Having a melting point in a vicinity of 111° C.
摘要翻译：（1S）-1,5-脱水-1- [5-（4 - {（1E）-4 - [（1 - {[2-（二甲基氨基）乙基]氨基} -2-甲基 - -1-氧代丙-2-基）氨基] -3,3-二甲基-4-氧代丁-1-烯-1-基}苄基）-2-甲氧基-4-（丙-2-基）苯基] 葡萄糖醇，以及晶体的制造方法。具体地，提供具有以下物理性质的乙醇化物和从乙醇化物转化的多种其它晶体形式：（a）在X射线粉末衍射（2θ= 5.9度，17.1度，17.6度和21.5度）处具有峰值 Cu-Kalpha）; （b）在红外吸收光谱中显示在3538cm-1,3337cm-1,2964cm-1,1673cm -1，1634cm -1和1505cm -1处的特征吸收带; 和（c）熔点在111℃附近

2. 发明授权

US07238719B2 Process for producing 1,2,3-Triazole compounds 失效
标题翻译：制备1,2,3-三唑化合物的方法
公开(公告)号：US07238719B2
公开(公告)日：2007-07-03
申请号：US10502392
申请日：2003-02-03
申请人： Shohei Yasuda , Koreaki Imura , Yumiko Okada , Shinichiro Tsujiyama
发明人： Shohei Yasuda , Koreaki Imura , Yumiko Okada , Shinichiro Tsujiyama
IPC分类号： A61K31/41 , C07D249/04
CPC分类号： C07D249/04 , Y02P20/55
摘要： Disclosed is a process for efficiently producing a compound represented by formula (I): wherein R1 represents aryl, amino, alkyl, or alkoxy; R2 represents a protective group of the carboxylic acid; and R3 represents an alkali metal, a hydrogen atom, alkyl, aryl, alkylsulfonyl, arylsulfonyl, or trialkylsilyl. This process is characterized by reacting a compound of formula (II) with a compound of formula (III) in the presence of a transition metal compound.
摘要翻译：公开了一种有效制备由式（I）表示的化合物的方法：其中R 1表示芳基，氨基，烷基或烷氧基; R 2表示羧酸的保护基; R 3表示碱金属，氢原子，烷基，芳基，烷基磺酰基，芳基磺酰基或三烷基甲硅烷基。该方法的特征在于使式（II）化合物与式（III）化合物在过渡金属化合物存在下反应。

3. 发明授权

US08822674B2 Crystal form of 4-isopropylphenyl glucitol compound and process for production thereof 有权
标题翻译： 4-异丙基苯基硬糖醇化合物的结晶形式及其生产方法
公开(公告)号：US08822674B2
公开(公告)日：2014-09-02
申请号：US13816647
申请日：2011-08-19
申请人： Yoshihiro Kimura , Koreaki Imura , Naoto Osaki , Ayumi Matsushima
发明人： Yoshihiro Kimura , Koreaki Imura , Naoto Osaki , Ayumi Matsushima
IPC分类号： C07H7/04
CPC分类号： C07H15/203 , C07D309/10 , C07H1/00
摘要： A highly stable crystal of (1S)-1,5-anhydro-1-[5-(4-{(1E)-4-[(1-{[2-(dimethylamino)ethyl]amino}-2-methyl-1-oxopropan-2-yl)amino]-3,3-dimethyl-4-oxobut-1-en-1-yl}benzyl)-2-methoxy-4-(propan-2-yl)phenyl]-D-glucitol, and a process for producing the crystal are provided. Specifically, an ethanolate having the following physical properties, and a plurality of other crystal forms transformed from the ethanolate are provided: (a) Having peaks at 2θ=5.9 degrees, 17.1 degrees, 17.6 degrees and 21.5 degrees in X-ray powder diffraction (Cu—Kα); (b) Showing characteristic absorption bands at 3538 cm−1, 3357 cm−1, 2964 cm−1, 1673 cm−1, 1634 cm−1 and 1505 cm−1 in an infrared absorption spectrum; and (c) Having a melting point in a vicinity of 111° C.
摘要翻译：（1S）-1,5-脱水-1- [5-（4 - {（1E）-4 - [（1 - {[2-（二甲基氨基）乙基]氨基} -2-甲基 - -1-氧代丙-2-基）氨基] -3,3-二甲基-4-氧代丁-1-烯-1-基}苄基）-2-甲氧基-4-（丙-2-基）苯基] 葡萄糖醇，以及晶体的制造方法。具体地说，提供具有以下物理性质的乙醇化物和从乙醇化物转化的多种其它晶体形式：（a）在X射线粉末衍射中在2θ= 5.9度，17.1度，17.6度和21.5度处具有峰值（Cu-Kα）; （b）在红外吸收光谱中显示在3538cm-1,3337cm-1,2964cm-1,1673cm -1，1634cm -1和1505cm -1处的特征吸收带; 和（c）熔点在111℃附近

4. 发明申请

US20050080270A1 Process for producing 1 2 3 triazole compound 失效
标题翻译： 1 2 3三唑化合物的制备方法
公开(公告)号：US20050080270A1
公开(公告)日：2005-04-14
申请号：US10502392
申请日：2003-02-03
申请人： Shohei Yasuda , Koreaki Imura , Yumiko Okada , Shinichiro Tsujiyama
发明人： Shohei Yasuda , Koreaki Imura , Yumiko Okada , Shinichiro Tsujiyama
IPC分类号： C07D249/04
CPC分类号： C07D249/04 , Y02P20/55
摘要： Disclosed is a process for efficiently producing a compound represented by formula (I): wherein R1 represents aryl, amino, alkyl, or alkoxy; R2 represents a protective group of the carboxylic acid; and R3 represents an alkali metal, a hydrogen atom, alkyl, aryl, alkylsulfonyl, arylsulfonyl, or trialkylsilyl. This process is characterized by reacting a compound of formula (II) with a compound of formula (III) in the presence of a transition metal compound.
摘要翻译：公开了一种有效制备由式（I）表示的化合物的方法：其中R 1表示芳基，氨基，烷基或烷氧基; R 2表示羧酸的保护基; R 3表示碱金属，氢原子，烷基，芳基，烷基磺酰基，芳基磺酰基或三烷基甲硅烷基。该方法的特征在于使式（II）化合物与式（III）化合物在过渡金属化合物存在下反应。

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