公开(公告)号：US07115575B2

公开(公告)日：2006-10-03

申请号：US11191024

申请日：2005-07-28

申请人： Hideki Fujikura ,  Toshihiro Nishimura ,  Kenji Katsuno ,  Masahiro Hiratochi ,  Akira Iyobe ,  Minoru Fujioka ,  Masayuki Isaji

发明人： Hideki Fujikura ,  Toshihiro Nishimura ,  Kenji Katsuno ,  Masahiro Hiratochi ,  Akira Iyobe ,  Minoru Fujioka ,  Masayuki Isaji

IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/415 ,  C07H17/00 ,  C07D231/20

CPC分类号： C07D231/20 ,  C07H17/02 ,  Y10S514/866 ,  Y10S514/909

摘要： The present invention relates to glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R1 represents a hydrogen atom or a lower alkyl group; one of Q1 and T1 represents a group represented by the general formula: while the other represents a lower alkyl group or a halo(lower alkyl) group; and R2 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a halo(lower alkyl) group or a halogen atom, or pharmaceutically acceptable salts thereof, which have an inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of diabetes, diabetic complications or obesity, and to pharmaceutical compositions comprising the same and intermediates thereof.

公开(公告)号：US07056892B2

公开(公告)日：2006-06-06

申请号：US11189832

申请日：2005-07-27

申请人： Hideki Fujikura ,  Toshihiro Nishimura ,  Kenji Katsuno ,  Masahiro Hiratochi ,  Akira Iyobe ,  Minoru Fujioka ,  Masayuki Isaji

发明人： Hideki Fujikura ,  Toshihiro Nishimura ,  Kenji Katsuno ,  Masahiro Hiratochi ,  Akira Iyobe ,  Minoru Fujioka ,  Masayuki Isaji

IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/415 ,  C07H17/00

CPC分类号： C07D231/20 ,  C07H17/02 ,  Y10S514/866 ,  Y10S514/909

摘要： The present invention relates to glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R1 represents a hydrogen atom or a lower alkyl group; one of Q1 and T1 represents a group represented by the general formula: while the other represents a lower alkyl group or a halo(lower alkyl) group; and R2 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a halo(lower alkyl) group or a halogen atom, or pharmaceutically acceptable salts thereof, which have an inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of diabetes, diabetic complications or obesity, and to pharmaceutical compositions comprising the same and intermediates thereof.

摘要翻译： 本发明涉及由以下通式表示的吡喃葡萄糖氧吡唑衍生物：其中R 1表示氢原子或低级烷基; Q 1和T 1之一表示由通式表示的基团：而另一个表示低级烷基或卤代（低级烷基）基团; 和R 2表示氢原子，低级烷基，低级烷氧基，低级烷硫基，卤代（低级烷基）基或卤素原子或其药学上可接受的盐，它们具有 在人SGLT2中的抑制活性，并且可用作预防或治疗糖尿病，糖尿病并发症或肥胖症的药剂，以及包含其的药物组合物及其中间体。

公开(公告)号：US20050261205A1

公开(公告)日：2005-11-24

申请号：US11189832

申请日：2005-07-27

申请人： Hideki Fujikura ,  Toshihiro Nishimura ,  Kenji Katsuno ,  Masahiro Hiratochi ,  Akira Iyobe ,  Minoru Fujioka ,  Masayuki Isaji

发明人： Hideki Fujikura ,  Toshihiro Nishimura ,  Kenji Katsuno ,  Masahiro Hiratochi ,  Akira Iyobe ,  Minoru Fujioka ,  Masayuki Isaji

IPC分类号： A61K31/7056 ,  A61P3/04 ,  A61P3/10 ,  C07D231/20 ,  C07H17/02

CPC分类号： C07D231/20 ,  C07H17/02 ,  Y10S514/866 ,  Y10S514/909

摘要： The present invention relates to glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R1 represents a hydrogen atom or a lower alkyl group; one of Q1 and T1 represents a group represented by the general formula: while the other represents a lower alkyl group or a halo(lower alkyl) group; and R2 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a halo(lower alkyl) group or a halogen atom, or pharmaceutically acceptable salts thereof, which have an inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of diabetes, diabetic complications or obesity, and to pharmaceutical compositions comprising the same and intermediates thereof.

公开(公告)号：US20050137143A1

公开(公告)日：2005-06-23

申请号：US10979154

申请日：2004-11-03

申请人： Hideki Fujikura ,  Toshihiro Nishimura ,  Kenji Katsuno ,  Masahiro Hiratochi ,  Akira Iyobe ,  Minoru Fujioka ,  Masayuki Isaji

发明人： Hideki Fujikura ,  Toshihiro Nishimura ,  Kenji Katsuno ,  Masahiro Hiratochi ,  Akira Iyobe ,  Minoru Fujioka ,  Masayuki Isaji

IPC分类号： A61K31/7056 ,  A61P3/04 ,  A61P3/10 ,  C07D231/20 ,  C07H17/02

CPC分类号： C07D231/20 ,  C07H17/02 ,  Y10S514/866 ,  Y10S514/909

摘要： The present invention relates to glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R1 represents a hydrogen atom or a lower alkyl group; one of Q1 and T1 represents a group represented by the general formula: while the other represents a lower alkyl group or a halo(lower alkyl) group; and R2 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a halo(lower alkyl) group or a halogen atom, or pharmaceutically acceptable salts thereof, which have an inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of diabetes, diabetic complications or obesity, and to pharmaceutical compositions comprising the same and intermediates thereof.

公开(公告)号：US06972283B2

公开(公告)日：2005-12-06

申请号：US10759138

申请日：2004-01-20

申请人： Hideki Fujikura ,  Toshihiro Nishimura ,  Kenji Katsuno ,  Masahiro Hiratochi ,  Akira Iyobe ,  Minoru Fujioka ,  Masayuki Isaji

发明人： Hideki Fujikura ,  Toshihiro Nishimura ,  Kenji Katsuno ,  Masahiro Hiratochi ,  Akira Iyobe ,  Minoru Fujioka ,  Masayuki Isaji

IPC分类号： A61K31/7056 ,  A61P3/04 ,  A61P3/10 ,  C07D231/20 ,  C07H17/02 ,  A61K31/70 ,  A61K31/415 ,  A61K31/7042 ,  C07H17/00

CPC分类号： C07D231/20 ,  C07H17/02 ,  Y10S514/866 ,  Y10S514/909

摘要： The present invention relates to glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R1 represents a hydrogen atom or a lower alkyl group; one of Q1 and T1 represents a group represented by the general formula: while the other represents a lower alkyl group or a halo(lower alkyl) group; and R2 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a halo(lower alkyl) group or a halogen atom, or pharmaceutically acceptable salts thereof, which have an inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of diabetes, diabetic complications or obesity, and to pharmaceutical compositions comprising the same and intermediates thereof.

摘要翻译： 本发明涉及由以下通式表示的吡喃葡萄糖氧吡唑衍生物：其中R 1表示氢原子或低级烷基; Q 1和T 1之一表示由通式表示的基团，而另一个表示低级烷基或卤代（低级烷基）基团; 和R 2表示氢原子，低级烷基，低级烷氧基，低级烷硫基，卤代（低级烷基）基或卤素原子或其药学上可接受的盐，它们具有 在人SGLT2中的抑制活性，并且可用作预防或治疗糖尿病，糖尿病并发症或肥胖症的药剂，以及包含其的药物组合物及其中间体。

公开(公告)号：US20050261206A1

公开(公告)日：2005-11-24

申请号：US11191024

申请日：2005-07-28

申请人： Hideki Fujikura ,  Toshihiro Nishimura ,  Kenji Katsuno ,  Masahiro Hiratochi ,  Akira Iyobe ,  Minoru Fujioka ,  Masayuki Isaji

发明人： Hideki Fujikura ,  Toshihiro Nishimura ,  Kenji Katsuno ,  Masahiro Hiratochi ,  Akira Iyobe ,  Minoru Fujioka ,  Masayuki Isaji

IPC分类号： A61K31/7056 ,  A61P3/04 ,  A61P3/10 ,  C07D231/20 ,  C07H17/02

CPC分类号： C07D231/20 ,  C07H17/02 ,  Y10S514/866 ,  Y10S514/909

摘要： The present invention relates to glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R1 represents a hydrogen atom or a lower alkyl group; one of Q1 and T1 represents a group represented by the general formula: while the other represents a lower alkyl group or a halo(lower alkyl) group; and R2 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a halo(lower alkyl) group or a halogen atom, or pharmaceutically acceptable salts thereof, which have an inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of diabetes, diabetic complications or obesity, and to pharmaceutical compositions comprising the same and intermediates thereof.

公开(公告)号：US20050119192A1

公开(公告)日：2005-06-02

申请号：US10507611

申请日：2003-03-04

申请人： Akira Iyobe ,  Hirotaka Teranishi ,  Kazuya Tatani ,  Shigeru Yonekubo ,  Masayuki Isaji

发明人： Akira Iyobe ,  Hirotaka Teranishi ,  Kazuya Tatani ,  Shigeru Yonekubo ,  Masayuki Isaji

IPC分类号： A61K31/7034 ,  A61P3/04 ,  A61P3/10 ,  C07H15/203 ,  A61K31/7028 ,  C07H11/04

CPC分类号： C07H15/203 ,  A61K31/7034

摘要： The present invention provides crystals of 2-(4-methoxybenzyl)phenyl 6-O-ethoxycarbonyl-β-D-glucopyranoside, pharmaceutical compositions containing the same and their uses, which exhibit excellent SGLT2 inhibitory activities, and are useful for treating or preventing diseases associated with hyperglycemia.

摘要翻译： 本发明提供2-（4-甲氧基苄基）苯基6-O-乙氧基羰基-β-D-吡喃葡萄糖苷的晶体，含有该结晶的药物组合物及其用途，其表现出优异的SGLT2抑制活性，可用于治疗或预防疾病 与高血糖相关。

公开(公告)号：US07371730B2

公开(公告)日：2008-05-13

申请号：US10507611

申请日：2003-03-04

申请人： Akira Iyobe ,  Hirotaka Teranishi ,  Kazuya Tatani ,  Shigeru Yonekubo ,  Masayuki Isaji

发明人： Akira Iyobe ,  Hirotaka Teranishi ,  Kazuya Tatani ,  Shigeru Yonekubo ,  Masayuki Isaji

IPC分类号： A01N43/04 ,  A61K31/70 ,  C07H15/00 ,  C07H15/24

CPC分类号： C07H15/203 ,  A61K31/7034

摘要： The present invention provides crystals of 2-(4-methoxybenzyl)phenyl 6-O-ethoxycarbonyl-β-D-glucopyranoside, pharmaceutical compositions containing the same and their uses, which exhibit excellent SGLT2 inhibitory activities, and are useful for treating or preventing diseases associated with hyperglycemia.

摘要翻译： 本发明提供2-（4-甲氧基苄基）苯基6-O-乙氧基羰基-β-D-吡喃葡萄糖苷的晶体，含有该结晶的药物组合物及其用途，其表现出优异的SGLT2抑制活性，可用于治疗或预防疾病 与高血糖相关。

公开(公告)号：US5294718A

公开(公告)日：1994-03-15

申请号：US101006

申请日：1993-08-03

申请人： Arao Ujiie ,  Hiromu Harada ,  Akira Iyobe ,  Masahiko Uchida ,  Koji Kamata

发明人： Arao Ujiie ,  Hiromu Harada ,  Akira Iyobe ,  Masahiko Uchida ,  Koji Kamata

IPC分类号： A61K31/47 ,  A61P7/02 ,  C07D401/04 ,  C07D401/10 ,  A61K31/445

CPC分类号： C07D401/04

摘要： Piperidino-3,4-dihydrocarbostyril compounds represented by the formula: ##STR1## wherein R.sup.1 represents a hydroxy group or an acyloxy group having 2 to 11 carbon atoms; one of R.sup.2 and R.sup.3 represents a nitro group, a cyano group, an alkoxycarbonyl group having 2 to 7 carbon atoms, an alkyl group having 1 to 4 carbon atoms, a haloalkyl group having 1 to 3 carbons atoms, or a halogen atom, and the other represents a hydrogen atom; and pharmaceutically acceptable salts thereof, exhibit platelet aggregation inhibiting activity and thus being useful as therapeutic agents for the prevention or treatment of cerebral ischemic disorders and arterial ischemic disorders.

摘要翻译： 由下式表示的哌啶子基-3,4-二氢喹诺酮化合物：其中R 1表示羟基或具有2至11个碳原子的酰氧基; R 2和R 3中的一个表示硝基，氰基，具有2至7个碳原子的烷氧基羰基，具有1至4个碳原子的烷基，具有1至3个碳原子的卤代烷基或卤素原子，以及 另一个表示氢原子; 其药学上可接受的盐具有血小板聚集抑制活性，因此可用作预防或治疗脑缺血障碍和动脉缺血障碍的治疗剂。