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公开(公告)号：US07169761B2
公开(公告)日：2007-01-30
申请号：US10491618
申请日：2003-08-04
申请人： Hiroshi Tomiyama , Atsushi Noda , Kayoko Kitta , Yoshinori Kobayashi , Masakazu Imamura , Takeshi Murakami , Kazuhiro Ikegai , Takayuki Suzuki , Eiji Kurosaki
发明人： Hiroshi Tomiyama , Atsushi Noda , Kayoko Kitta , Yoshinori Kobayashi , Masakazu Imamura , Takeshi Murakami , Kazuhiro Ikegai , Takayuki Suzuki , Eiji Kurosaki
CPC分类号： C07D309/12 , C07D309/10
摘要： The present invention provides an azulene derivative and a salt thereof, wherein an azulene ring is bonded to a benzene ring directly or via a lower alkylene which may be substituted with a halogen atom and the benzene ring is directly bonded to the glucose residue, and it is usable as a Na+-glucose cotransporter inhibitor, especially for a therapeutic and/or preventive agent for diabetes such as insulin-dependent diabetes (type 1 diabetes) and insulin-independent diabetes (type 2 diabetes), as well as diabetes-related diseases such as insulin-resistant diseases and obesity.
摘要翻译： 本发明提供了薁衍生物及其盐，其中薁环直接或通过可被卤素原子取代的低级亚烷基与苯环键接，苯环与葡萄糖残基直接键合， 可用作Na + + - 葡萄糖共转运蛋白抑制剂，特别是用于糖尿病治疗和/或预防剂如胰岛素依赖性糖尿病（1型糖尿病）和胰岛素不依赖性糖尿病（2型糖尿病） ，以及糖尿病相关疾病如胰岛素抵抗疾病和肥胖症。
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公开(公告)号：US20050124555A1
公开(公告)日：2005-06-09
申请号：US10491618
申请日：2003-08-04
申请人： Hiroshi Tomiyama , Atsushi Noda , Kayoko Kitta , Yoshinori Kobayashi , Masakazu Imamura , Takeshi Murakami , Kazuhiro Ikegai , Takayuki Suzuki , Eiji Kurosaki
发明人： Hiroshi Tomiyama , Atsushi Noda , Kayoko Kitta , Yoshinori Kobayashi , Masakazu Imamura , Takeshi Murakami , Kazuhiro Ikegai , Takayuki Suzuki , Eiji Kurosaki
IPC分类号： A61P3/04 , A61P3/10 , A61P43/00 , C07D309/10 , C07D309/12 , C07H15/24 , A61K31/704
CPC分类号： C07D309/12 , C07D309/10
摘要： The present invention provides an azulene derivative and a salt thereof, wherein an azulene ring is bonded to a benzene ring directly or via a lower alkylene which may be substituted with a halogen atom and the benzene ring is directly bonded to the glucose residue, and it is usable as a Na+-glucose cotransporter inhibitor, especially for a therapeutic and/or preventive agent for diabetes such as insulin-dependent diabetes (type 1 diabetes) and insulin-independent diabetes (type 2 diabetes), as well as diabetes-related diseases such as insulin-resistant diseases and obesity.
摘要翻译： 本发明提供了薁衍生物及其盐，其中薁环直接或通过可被卤素原子取代的低级亚烷基与苯环键接，苯环与葡萄糖残基直接键合， 可用作Na + + - 葡萄糖共转运蛋白抑制剂，特别是用于糖尿病治疗和/或预防剂如胰岛素依赖性糖尿病（1型糖尿病）和胰岛素不依赖性糖尿病（2型糖尿病） ，以及糖尿病相关疾病如胰岛素抵抗疾病和肥胖症。
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公开(公告)号：US07977466B2
公开(公告)日：2011-07-12
申请号：US12173614
申请日：2008-07-15
申请人： Masakazu Imamura , Takeshi Murakami , Ryota Shiraki , Kazuhiro Ikegai , Takashi Sugane , Fumiyoshi Iwasaki , Eiji Kurosaki , Hiroshi Tomiyama , Atsushi Noda , Kayoko Kitta , Yoshinori Kobayashi
发明人： Masakazu Imamura , Takeshi Murakami , Ryota Shiraki , Kazuhiro Ikegai , Takashi Sugane , Fumiyoshi Iwasaki , Eiji Kurosaki , Hiroshi Tomiyama , Atsushi Noda , Kayoko Kitta , Yoshinori Kobayashi
IPC分类号： A61K31/7034 , C07H7/04
CPC分类号： C07D495/04 , A61K31/351 , A61K31/381 , A61K31/4035 , A61K31/404 , A61K31/41 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/4433 , A61K31/497 , A61K31/5377 , C07D405/10 , C07D407/10 , C07D409/10 , C07D413/10 , C07D417/10
摘要： The present invention provides C-glycoside derivatives and salts thereof, wherein B ring is bonded to A ring via —X— and A ring is directly bonded to the glucose residue, and it is usable as a Na+-glucose cotransporter inhibitor, especially for a therapeutic and/or preventive agent for diabetes such as insulin-dependent diabetes (type 1 diabetes) and insulin-independent diabetes (type 2 diabetes), as well as diabetes related diseases such as an insulin-resistant diseases and obesity.
摘要翻译： 本发明提供C-糖苷衍生物及其盐，其中B环通过-X-与A环结合，A环与葡萄糖残基直接结合，可用作Na + - 葡萄糖共转运蛋白抑制剂，尤其用于 胰岛素依赖性糖尿病（1型糖尿病）和胰岛素依赖性糖尿病（2型糖尿病）等糖尿病治疗剂和/或预防剂，以及糖尿病相关疾病如胰岛素抵抗疾病和肥胖症。
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公开(公告)号：US07772407B2
公开(公告)日：2010-08-10
申请号：US11710434
申请日：2007-02-26
申请人： Masakazu Imamura , Takeshi Murakami , Ryota Shiraki , Kazuhiro Ikegai , Takashi Sugane , Fumiyoshi Iwasaki , Eiji Kurosaki , Hiroshi Tomiyama , Atsushi Noda , Kayoko Kitta , Yoshinori Kobayashi
发明人： Masakazu Imamura , Takeshi Murakami , Ryota Shiraki , Kazuhiro Ikegai , Takashi Sugane , Fumiyoshi Iwasaki , Eiji Kurosaki , Hiroshi Tomiyama , Atsushi Noda , Kayoko Kitta , Yoshinori Kobayashi
IPC分类号： A61K31/7034 , A61K31/381 , C07H7/04 , C07D333/34 , C07D495/00
CPC分类号： C07D495/04 , A61K31/351 , A61K31/381 , A61K31/4035 , A61K31/404 , A61K31/41 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/4433 , A61K31/497 , A61K31/5377 , C07D405/10 , C07D407/10 , C07D409/10 , C07D413/10 , C07D417/10
摘要： The present invention provides C-glycoside derivatives and salts thereof, wherein B ring is bonded to A ring via —X— and A ring is directly bonded to the glucose residue, and it is usable as a Na+-glucose cotransporter inhibitor, especially for a therapeutic and/or preventive agent for diabetes such as insulin-dependent diabetes (type 1 diabetes) and insulin-independent diabetes (type 2 diabetes), as well as diabetes related diseases such as an insulin-resistant diseases and obesity.
摘要翻译： 本发明提供C-糖苷衍生物及其盐，其中B环通过-X-与A环结合，A环与葡萄糖残基直接结合，可用作Na + - 葡萄糖共转运蛋白抑制剂，尤其用于 胰岛素依赖性糖尿病（1型糖尿病）和胰岛素依赖性糖尿病（2型糖尿病）等糖尿病治疗剂和/或预防剂，以及糖尿病相关疾病如胰岛素抵抗疾病和肥胖症。
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公开(公告)号：US07202350B2
公开(公告)日：2007-04-10
申请号：US10541615
申请日：2004-03-12
申请人： Masakazu Imamura , Takeshi Murakami , Ryota Shiraki , Kazuhiro Ikegai , Takashi Sugane , Fumiyoshi Iwasaki , Eiji Kurosaki , Hiroshi Tomiyama , Atsushi Noda , Kayoko Kitta , Yoshinori Kobayashi
发明人： Masakazu Imamura , Takeshi Murakami , Ryota Shiraki , Kazuhiro Ikegai , Takashi Sugane , Fumiyoshi Iwasaki , Eiji Kurosaki , Hiroshi Tomiyama , Atsushi Noda , Kayoko Kitta , Yoshinori Kobayashi
CPC分类号： C07D495/04 , A61K31/351 , A61K31/381 , A61K31/4035 , A61K31/404 , A61K31/41 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/4433 , A61K31/497 , A61K31/5377 , C07D405/10 , C07D407/10 , C07D409/10 , C07D413/10 , C07D417/10
摘要： The present invention provides C-glycoside derivatives and salts thereof, wherein B ring is bonded to A ring via —X— and A ring is directly bonded to the glucose residue, and it is usable as a Na+-glucose cotransporter inhibitor, especially for a therapeutic and/or preventive agent for diabetes such as insulin-dependent diabetes (type 1 diabetes) and insulin-independent diabetes (type 2 diabetes), as well as diabetes related diseases such as an insulin-resistant diseases and obesity.
摘要翻译： 本发明提供C-糖苷衍生物及其盐，其中B环通过-X-与A环键合，并且A环直接键合到葡萄糖残基，并且其可用作Na + 葡萄糖共转运蛋白抑制剂，特别是用于糖尿病的治疗和/或预防剂，例如胰岛素依赖性糖尿病（1型糖尿病）和不依赖胰岛素的糖尿病（2型糖尿病），以及糖尿病相关疾病如胰岛素抵抗 疾病和肥胖。
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公开(公告)号：US20070161787A1
公开(公告)日：2007-07-12
申请号：US11710434
申请日：2007-02-26
申请人： Masakazu Imamura , Takeshi Murakami , Ryota Shiraki , Kazuhiro Ikegai , Takashi Sugane , Fumiyoshi Iwasaki , Eiji Kurosaki , Hiroshi Tomiyama , Atsushi Noda , Kayoko Kitta , Yoshinori Kobayashi
发明人： Masakazu Imamura , Takeshi Murakami , Ryota Shiraki , Kazuhiro Ikegai , Takashi Sugane , Fumiyoshi Iwasaki , Eiji Kurosaki , Hiroshi Tomiyama , Atsushi Noda , Kayoko Kitta , Yoshinori Kobayashi
IPC分类号： A61K31/7052 , C07H17/00
CPC分类号： C07D495/04 , A61K31/351 , A61K31/381 , A61K31/4035 , A61K31/404 , A61K31/41 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/4433 , A61K31/497 , A61K31/5377 , C07D405/10 , C07D407/10 , C07D409/10 , C07D413/10 , C07D417/10
摘要： The present invention provides C-glycoside derivatives and salts thereof, wherein B ring is bonded to A ring via —X— and A ring is directly bonded to the glucose residue, and it is usable as a Na+-glucose cotransporter inhibitor, especially for a therapeutic and/or preventive agent for diabetes such as insulin-dependent diabetes (type 1 diabetes) and insulin-independent diabetes (type 2 diabetes), as well as diabetes related diseases such as an insulin-resistant diseases and obesity.
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公开(公告)号：US20090069252A1
公开(公告)日：2009-03-12
申请号：US12173614
申请日：2008-07-15
申请人： Masakazu Imamura , Takeshi Murakami , Ryota Shiraki , Kazuhiro Ikegai , Takashi Sugane , Fumiyoshi Iwasaki , Eiji Kurosaki , Hiroshi Tomiyama , Atsushi Noda , Kayoko Kitta , Yoshinori Kobayashi
发明人： Masakazu Imamura , Takeshi Murakami , Ryota Shiraki , Kazuhiro Ikegai , Takashi Sugane , Fumiyoshi Iwasaki , Eiji Kurosaki , Hiroshi Tomiyama , Atsushi Noda , Kayoko Kitta , Yoshinori Kobayashi
IPC分类号： A61K31/7042 , C07H7/06
CPC分类号： C07D495/04 , A61K31/351 , A61K31/381 , A61K31/4035 , A61K31/404 , A61K31/41 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/4433 , A61K31/497 , A61K31/5377 , C07D405/10 , C07D407/10 , C07D409/10 , C07D413/10 , C07D417/10
摘要： The present invention provides C-glycoside derivatives and salts thereof, wherein B ring is bonded to A ring via —X— and A ring is directly bonded to the glucose residue, and it is usable as a Na+-glucose cotransporter inhibitor, especially for a therapeutic and/or preventive agent for diabetes such as insulin-dependent diabetes (type 1 diabetes) and insulin-independent diabetes (type 2 diabetes), as well as diabetes related diseases such as an insulin-resistant diseases and obesity.
摘要翻译： 本发明提供C-糖苷衍生物及其盐，其中B环通过-X-与A环结合，A环与葡萄糖残基直接结合，可用作Na + - 葡萄糖共转运蛋白抑制剂，尤其用于 胰岛素依赖性糖尿病（1型糖尿病）和胰岛素依赖性糖尿病（2型糖尿病）等糖尿病治疗剂和/或预防剂，以及糖尿病相关疾病如胰岛素抵抗疾病和肥胖症。
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公开(公告)号：US20060122126A1
公开(公告)日：2006-06-08
申请号：US10541615
申请日：2004-03-12
申请人： Masakazu Imamura , Takeshi Murakami , Ryota Shiraki , Kazuhiro Ikegai , Takashi Sugane , Fumiyoshi Iwasaki , Eiji Kurosaki , Hiroshi Tomiyama , Atsushi Noda , Kayoko Kitta , Yoshinori Kobayashi
发明人： Masakazu Imamura , Takeshi Murakami , Ryota Shiraki , Kazuhiro Ikegai , Takashi Sugane , Fumiyoshi Iwasaki , Eiji Kurosaki , Hiroshi Tomiyama , Atsushi Noda , Kayoko Kitta , Yoshinori Kobayashi
IPC分类号： C07H23/00 , A61K31/7052
CPC分类号： C07D495/04 , A61K31/351 , A61K31/381 , A61K31/4035 , A61K31/404 , A61K31/41 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/4433 , A61K31/497 , A61K31/5377 , C07D405/10 , C07D407/10 , C07D409/10 , C07D413/10 , C07D417/10
摘要： The present invention provides C-glycoside derivatives and salts thereof, wherein B ring is bonded to A ring via —X— and A ring is directly bonded to the glucose residue, and it is usable as a Na+-glucose cotransporter inhibitor, especially for a therapeutic and/or preventive agent for diabetes such as insulin-dependent diabetes (type 1 diabetes) and insulin-independent diabetes (type 2 diabetes), as well as diabetes related diseases such as an insulin-resistant diseases and obesity.
摘要翻译： 本发明提供C-糖苷衍生物及其盐，其中B环通过-X-与A环键合，并且A环直接键合到葡萄糖残基，并且其可用作Na + 葡萄糖共转运蛋白抑制剂，特别是用于糖尿病的治疗和/或预防剂，例如胰岛素依赖性糖尿病（1型糖尿病）和不依赖胰岛素的糖尿病（2型糖尿病），以及糖尿病相关疾病如胰岛素抵抗 疾病和肥胖。
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9.发明申请公开(公告)号：US20070293690A1
公开(公告)日：2007-12-20
申请号：US11631634
申请日：2005-07-07
申请人： Hiroshi Tomiyama , Masayuki Yokota , Atsushi Noda , Yoshinori Kobayashi , Junko Ogasawara , Yasumasa Hayashi , Masatoshi Inakoshi , Hirofumi Nakamura , Tokuo Koide , Kenichiro Sakamoto , Yohei Yamashita , Akio Miyafuji , Takayuki Suzuki , Noriyuki Kawano , Junji Miyata , Masakazu Imamura , Takashi Sugane
发明人： Hiroshi Tomiyama , Masayuki Yokota , Atsushi Noda , Yoshinori Kobayashi , Junko Ogasawara , Yasumasa Hayashi , Masatoshi Inakoshi , Hirofumi Nakamura , Tokuo Koide , Kenichiro Sakamoto , Yohei Yamashita , Akio Miyafuji , Takayuki Suzuki , Noriyuki Kawano , Junji Miyata , Masakazu Imamura , Takashi Sugane
IPC分类号： C07D309/02
CPC分类号： C07C49/255 , C07C45/48 , C07C45/63 , C07C45/71 , C07C49/245 , C07H7/04 , C07H15/04
摘要： A process for producing an azulene derivative useful as a Na+-glucose cotransporter inhibitor, which is high in yield, is simple in operation, is low in cost, is suited for environmental protection, and is advantageous industrially, the process being characterized by reducing and deprotecting at least one compound selected from penta-acyl compounds and tetra-acyl compounds or salts thereof to obtain a C-glycoside compound; and a useful intermediate for synthesis of such an azulene derivative, obtained in the course of the above process.
摘要翻译： 制备用作产率高的Na + + - 葡萄糖共转运蛋白抑制剂的薁衍生物的方法操作简单，成本低，适用于环境保护，在工业上有利 该方法的特征在于将至少一种选自五酰基化合物和四酰基化合物或其盐的化合物还原和去保护以获得C-糖苷化合物; 以及在上述方法中获得的这种薁衍生物的合成的有用中间体。
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公开(公告)号：US20090182039A1
公开(公告)日：2009-07-16
申请号：US11988383
申请日：2006-07-06
申请人： Masakazu Imamura , Takayuki Suzuki , Takeshi Murakami , Keita Nakanishi , Hiroshi Uebayashi , Haruka Nakamura , Masamichi Yuda , Naoko Amenomiya , Yuuji Awamura , Hiroshi Tomiyama
发明人： Masakazu Imamura , Takayuki Suzuki , Takeshi Murakami , Keita Nakanishi , Hiroshi Uebayashi , Haruka Nakamura , Masamichi Yuda , Naoko Amenomiya , Yuuji Awamura , Hiroshi Tomiyama
IPC分类号： A61K31/351 , C07D315/00
CPC分类号： C07C215/90 , C07D309/10
摘要： A choline salt crystal of (1S)-1,5-anhydro-1-[5-(azulen-2-ylmethyl)-2-hydroxyphenyl]-D-glucitol which shows an endothermic peak at 194 to 198° C. as measured by differential scanning calorimetry (DSC analysis) and shows main peaks at about 2θ (°) 5.58, 14.72, 16.80, 17.82, 21.02, and 22.46 as measured by X-ray powder diffraction. Thus, a crystal of an azulene compound can be produced which is in a single crystal form, has a constant quality, can be produced with good reproducibility, can be provided stably as a crystal of an drug substance for use in the preparation of a pharmaceutical and is excellent in storage stability.
摘要翻译： （1S）-1,5-脱水-1- [5-（薁-2-基甲基）-2-羟基苯基] -D-葡萄糖醇的胆碱盐晶体，其在194至198℃下显示吸热峰 通过差示扫描量热法（DSC分析），并且通过X射线粉末衍射测量显示在约2θ（°）5.58,14.72,16.80,17.82,21.02和22.46处的主峰。 因此，可以制造az烯化合物的结晶，其为单晶形式，具有恒定的质量，可以以良好的再现性制备，可以稳定地提供用作制备药物的药物的晶体 储存稳定性优异。
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