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1. 发明授权

US07169761B2 Azulene derivatives and salts thereof 失效
标题翻译：薁衍生物及其盐
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
IPC分类号： A01N43/04 , A61K31/70 , C07H1/00
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。

2. 发明申请

US20050124555A1 Azulene derivatives and salts thereof 失效
标题翻译：薁衍生物及其盐
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。

3. 发明申请

US20070161787A1 C-glycoside derivatives and salts thereof 有权
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.

4. 发明授权

US07977466B2 C-glycoside derivatives and salts thereof 有权
标题翻译： C-糖苷衍生物及其盐
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。

5. 发明授权

US07772407B2 C-glycoside derivatives and salts thereof 有权
标题翻译： C-糖苷衍生物及其盐
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。

6. 发明授权

US07202350B2 C-glycoside derivatives and salts thereof 有权
标题翻译： C-糖苷衍生物及其盐
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
IPC分类号： C07H1/00 , A61K31/70 , 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。

7. 发明申请

US20090069252A1 C-GLYCOSIDE DERIVATIVES AND SALTS THEREOF 有权
标题翻译： C-GLYCOSIDE衍生物及其销售
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。

8. 发明申请

US20060122126A1 C-glycoside derivatives and salts thereof 有权
标题翻译： C-糖苷衍生物及其盐
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。

9. 发明申请

US20050084840A1 Method for screening drug for improving insulin resistance 审中-公开
标题翻译：筛选药物以改善胰岛素抵抗的方法
公开(公告)号：US20050084840A1
公开(公告)日：2005-04-21
申请号：US10502279
申请日：2003-01-22
申请人： Hideki Endoh , Ryosuke Nakano , Eiji Kurosaki , Miyuki Kato , Hiroyuki Yokota , Kazunori Inabe
发明人： Hideki Endoh , Ryosuke Nakano , Eiji Kurosaki , Miyuki Kato , Hiroyuki Yokota , Kazunori Inabe
IPC分类号： A61P3/10 , C12N1/19 , C12N1/21 , C12N15/10 , C12N15/12 , C12Q1/68 , G01N33/566 , C12N1/18 , C12N15/74 , C12Q1/00
CPC分类号： G01N33/566 , C12N15/1055 , C12Q1/6897 , G01N2333/70567
摘要： Disclosing a method for screening a protein interactive with PPAR in a ligand-dependent manner, works as a useful tool for screening a drug ameliorating insulin resistance. By the method, ECHLP as a main action ligand-dependent PPAR binding molecule, FLJ13111 as a main action ligand-selective factor interactive with PPARγ and AOP2 as an adverse action ligand-dependent PPAR binding molecule were obtained. By using ECHLP interactive with PPAR, FLJ13111 interactive with PPAR and AOP2 interactive with PPAR, a screening system for a drug ameliorating insulin resistance is constructed and disclosed, the drug giving selectively the main action with no occurrence of the adverse action. Additionally, a method for producing a pharmaceutical composition for ameliorating insulin resistance is disclosed, which contains as the active component, a promoting agent of the main action through PPAR, an agonist specific to the main action through PPAR, an inhibitor of ECHLP interactive with PPAR to promote the main action through PPAR, a substance suppressing the adverse action through PPARγ, an inhibitor of AOP2 interactive with PPAR to suppress the adverse action through PPARγ, an activating agent of FLJ13111 interactive with PPAR to promote the main action through PPAR or an activator of FLJ13111 expression.
摘要翻译：披露以配体依赖的方式筛选与PPAR相互作用的蛋白质的方法，其作为筛选改善胰岛素抵抗的药物的有用工具。通过该方法，获得了作为主要作用配体依赖性PPAR结合分子的ECHLP，FLJ13111作为与PPARgamma和AOP2作为不利作用配体依赖性PPAR结合分子相互作用的主要作用配体选择性因子。通过使用ECHLP与PPAR交互，FLJ13111与PPAR和AOP2交互式与PPAR交互，构建并公开了改善胰岛素抵抗的药物筛选系统，该药物选择性地给予主要作用，不发生不良反应。另外，公开了一种制备用于改善胰岛素抵抗的药物组合物的方法，其包含通过PPAR作为主要作用的主要作用的促进剂，通过PPAR主要作用的激动剂，与PPAR相互作用的ECHLP抑制剂通过PPAR促进PPAR的主要作用，PPARgamma是与PPAR相互作用的AOP2抑制剂，通过PPARgamma的抑制剂来抑制不良反应，PPARgamma是与PPAR相互作用的FLJ13111激活剂，通过PPAR或激活剂促进主要作用的FLJ13111表达。

10. 发明申请

US20110003757A1 PHARMACEUTICAL COMPOSITIONS FOR TREATING FATTY LIVER DISEASE 审中-公开
标题翻译：用于治疗脂肪肝疾病的药物组合物
公开(公告)号：US20110003757A1
公开(公告)日：2011-01-06
申请号：US12865634
申请日：2009-01-29
申请人： Eiji Kurosaki , Toshiyuki Takasu , Noriaki Maeda , Shunji Yamazaki
发明人： Eiji Kurosaki , Toshiyuki Takasu , Noriaki Maeda , Shunji Yamazaki
IPC分类号： A61K31/7004 , A61K31/7042 , A61P1/16
CPC分类号： C07D309/10 , C07D409/10 , C07H7/04 , C07H15/203 , C07H15/26
摘要： The present invention provides a pharmaceutical composition useful as a therapeutic agent for fatty liver disease. A pharmaceutical composition, which comprises (1S)-1,5-anhydro-1-[5-(azulen-2-ylmethyl)-2-hydroxyphenyl]-D-glucitol or a pharmaceutically acceptable salt thereof, (1S)-1,5-anhydro-1-[3-(1-benzothiophen-2-ylmethyl)-4-fluorophenyl]-D-glucitol or a pharmaceutically acceptable salt thereof, or alternatively, (1S)-1,5-anhydro-1-[4-chloro-3-(4-ethoxybenzyl)phenyl]-D-glucitol or a pharmaceutically acceptable salt thereof, more specifically such a pharmaceutical composition for treating fatty liver disease, such as nonalcoholic fatty liver disease in one embodiment, or nonalcoholic simple fatty liver and/or nonalcoholic steatohepatitis in another embodiment.
摘要翻译：本发明提供可用作脂肪肝病治疗剂的药物组合物。一种药物组合物，其包含（1S）-1,5-脱水-1- [5-（薁-2-基甲基）-2-羟基苯基] -D-葡萄糖醇或其药学上可接受的盐，（1S）-1， 5-脱水-1- [3-（1-苯并噻吩-2-基甲基）-4-氟苯基] -D-葡萄糖醇或其药学上可接受的盐，或者，（1S）-1,5-脱水-1- [ 4-氯-3-（4-乙氧基苄基）苯基] -D-葡萄糖醇或其药学上可接受的盐，更具体地说，这种用于治疗脂肪肝疾病的药物组合物，例如在一个实施方案中的非酒精性脂肪肝疾病，或非酒精单纯脂肪肝和/或非酒精性脂肪性肝炎。

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