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1. 发明授权

US07208524B2 5-amidino-2-hydroxybenzenesulfonamide derivatives, pharmaceutical compositions containing the same and intermediates for their preparation 失效
标题翻译： 5-脒基-2-羟基苯磺酰胺衍生物，含有它们的药物组合物及其制备中间体
公开(公告)号：US07208524B2
公开(公告)日：2007-04-24
申请号：US10398383
申请日：2001-10-02
申请人： Kosuke Okazaki , Masahiko Uchida , Harunobu Mukaiyama , Hiroaki Kobayashi , Yuichiro Kai , Hideki Takeuchi , Kenji Yokoyama , Yoshihiro Terao , Yuji Hoyano , Hiroaki Shiohara , Norihiko Kikuchi
发明人： Kosuke Okazaki , Masahiko Uchida , Harunobu Mukaiyama , Hiroaki Kobayashi , Yuichiro Kai , Hideki Takeuchi , Kenji Yokoyama , Yoshihiro Terao , Yuji Hoyano , Hiroaki Shiohara , Norihiko Kikuchi
IPC分类号： A61K31/195 , A61K31/18 , C07C59/52 , C07C307/06
CPC分类号： A61K31/18 , A61K31/40 , A61K31/421 , A61K31/445 , A61K31/5377 , A61K31/55 , A61K31/553 , C07C311/29 , C07C311/37 , C07C317/32 , C07C2601/14
摘要： The present invention relates to a 5-amidino-2-hydroxybenzenesulfonamide derivative represented by the general formula: wherein R1 is a hydrogen atom or an optionally substituted lower alkyl group; R2 is a di(lower alkyl)amino group, a lower alkyl group, a cycloalkyl group, an optionally substituted aryl group, an optionally substituted heterocycloalkyl group, or an optionally substituted aromatic heterocyclic group; T is an oxygen atom, a sulfur atom, a sulfonyl group etc.; Q is a hydrogen atom or an optionally substituted lower alkyl group; and Z is a hydrogen atom, a hydroxy group etc., or a pharmaceutically acceptable salt thereof, which exert a potent and selective activated blood coagulation factor X inhibitory activity and is useful as an agent for the prevention or treatment of a disease occurred associating an activated blood coagulation factor X, a pharmaceutical composition comprising the same, a pharmaceutical use thereof and an intermediate thereof.
摘要翻译：本发明涉及由以下通式表示的5-脒基-2-羟基苯磺酰胺衍生物：其中R 1是氢原子或任选取代的低级烷基; R 2是二（低级烷基）氨基，低级烷基，环烷基，任选取代的芳基，任选取代的杂环烷基或任选取代的芳族杂环基; T是氧原子，硫原子，磺酰基等; Q是氢原子或任意取代的低级烷基; Z是氢原子，羟基等，或其药学上可接受的盐，其具有有效和选择性的活化凝血因子X抑制活性，并且可用作预防或治疗疾病的药剂，活化凝血因子X，包含其的药物组合物，其药物用途及其中间体。

2. 发明申请

US20060116361A1 5-Amidino-2-hydroxybenzenesulfonamide derivatives, pharmaceutical compositions containing the same and intermediates for their preparation 失效
公开(公告)号：US20060116361A1
公开(公告)日：2006-06-01
申请号：US10398383
申请日：2001-10-02
申请人： Kosuke Okazaki , Masahiko Uchida , Harunobu Mukaiyama , Hiroaki Kobayashi , Yuichiro Kai , Hideki Takeuchi , Kenji Yokoyama , Yoshihiro Terao , Yuji Hoyano , Hiroaki Shiohara , Norihiko Kikuchi
发明人： Kosuke Okazaki , Masahiko Uchida , Harunobu Mukaiyama , Hiroaki Kobayashi , Yuichiro Kai , Hideki Takeuchi , Kenji Yokoyama , Yoshihiro Terao , Yuji Hoyano , Hiroaki Shiohara , Norihiko Kikuchi
IPC分类号： A61K31/44 , A61K31/40 , A61K31/195
CPC分类号： A61K31/18 , A61K31/40 , A61K31/421 , A61K31/445 , A61K31/5377 , A61K31/55 , A61K31/553 , C07C311/29 , C07C311/37 , C07C317/32 , C07C2601/14
摘要： The present invention relates to a 5-amidino-2-hydroxybenzenesulfonamide derivative represented by the general formula: wherein R1 is a hydrogen atom or an optionally substituted lower alkyl group; R2 is a di(lower alkyl)amino group, a lower alkyl group, a cycloalkyl group, an optionally substituted aryl group, an optionally substituted heterocycloalkyl group, or an optionally substituted aromatic heterocyclic group; T is an oxygen atom, a sulfur atom, a sulfonyl group etc.; Q is a hydrogen atom or an optionally substituted lower alkyl group; and Z is a hydrogen atom, a hydroxy group etc., or a pharmaceutically acceptable salt thereof, which exert a potent and selective activated blood coagulation factor X inhibitory activity and is useful as an agent for the prevention or treatment of a disease occurred associating an activated blood coagulation factor X, a pharmaceutical composition comprising the same, a pharmaceutical use thereof and an intermediate thereof.

3. 发明授权

US07589126B2 5-amidino-2-hydroxybenzenesulfonamide derivatives, pharmaceutical compositions containing the same and intermediates for their preparation 失效
标题翻译： 5-脒基-2-羟基苯磺酰胺衍生物，含有它们的药物组合物及其制备中间体
公开(公告)号：US07589126B2
公开(公告)日：2009-09-15
申请号：US11553573
申请日：2006-10-27
申请人： Kosuke Okazaki , Masahiko Uchida , Harunobu Mukaiyama , Hiroaki Kobayashi , Yuichiro Kai , Hideki Takeuchi , Kenji Yokoyama , Yoshihiro Terao , Yuji Hoyano , Hiroaki Shiohara , Norihiko Kikuchi
发明人： Kosuke Okazaki , Masahiko Uchida , Harunobu Mukaiyama , Hiroaki Kobayashi , Yuichiro Kai , Hideki Takeuchi , Kenji Yokoyama , Yoshihiro Terao , Yuji Hoyano , Hiroaki Shiohara , Norihiko Kikuchi
IPC分类号： A61K31/195 , A61K31/18
CPC分类号： A61K31/18 , A61K31/40 , A61K31/421 , A61K31/445 , A61K31/5377 , A61K31/55 , A61K31/553 , C07C311/29 , C07C311/37 , C07C317/32 , C07C2601/14
摘要： The present invention relates to a 5-amidino-2-hydroxybenzenesulfonamide derivative represented by the general formula: wherein R1 is a hydrogen atom or an optionally substituted lower alkyl group; R2 is a di(lower alkyl)amino group, a lower alkyl group, a cycloalkyl group, an optionally substituted aryl group, an optionally substituted heterocycloalkyl group, or an optionally substituted aromatic heterocyclic group; T is an oxygen atom, a sulfur atom, a sulfonyl group etc.; Q is a hydrogen atom or an optionally substituted lower alkyl group; and Z is a hydrogen atom, a hydroxy group etc., or a pharmaceutically acceptable salt thereof, which exert a potent and selective activated blood coagulation factor X inhibitory activity and is useful as an agent for the prevention or treatment of a disease occurred associating an activated blood coagulation factor X, a pharmaceutical composition comprising the same, a pharmaceutical use thereof and an intermediate thereof.
摘要翻译：本发明涉及由下列通式表示的5-脒基-2-羟基苯磺酰胺衍生物：其中R 1是氢原子或任意取代的低级烷基; R2是二（低级烷基）氨基，低级烷基，环烷基，任选取代的芳基，任选取代的杂环烷基或任选取代的芳族杂环基; T是氧原子，硫原子，磺酰基等; Q是氢原子或任意取代的低级烷基; Z是氢原子，羟基等，或其药学上可接受的盐，其具有有效和选择性的活化凝血因子X抑制活性，并且可用作预防或治疗疾病，活化凝血因子X，包含其的药物组合物，其药物用途及其中间体。

4. 发明授权

US07217832B2 5-amidino-2-hydroxybenzenesulfonamide derivatives, pharmaceutical compositions containing the same and intermediates for their preparation 失效
公开(公告)号：US07217832B2
公开(公告)日：2007-05-15
申请号：US11359430
申请日：2006-02-23
申请人： Kosuke Okazaki , Masahiko Uchida , Harunobu Mukaiyama , Hiroaki Kobayashi , Yuichiro Kai , Hideki Takeuchi , Kenji Yokoyama , Yoshihiro Terao , Yuji Hoyano , Hiroaki Shiohara , Norihiko Kikuchi
发明人： Kosuke Okazaki , Masahiko Uchida , Harunobu Mukaiyama , Hiroaki Kobayashi , Yuichiro Kai , Hideki Takeuchi , Kenji Yokoyama , Yoshihiro Terao , Yuji Hoyano , Hiroaki Shiohara , Norihiko Kikuchi
IPC分类号： C07D265/30 , C07D271/113 , C07D277/30 , C07C255/53 , C07C255/63
CPC分类号： A61K31/18 , A61K31/40 , A61K31/421 , A61K31/445 , A61K31/5377 , A61K31/55 , A61K31/553 , C07C311/29 , C07C311/37 , C07C317/32 , C07C2601/14
摘要： The present invention relates to a 5-amidino-2-hydroxybenzenesulfonamide derivative represented by the general formula: wherein R1 is a hydrogen atom or an optionally substituted lower alkyl group; R2 is a di(lower alkyl)amino group, a lower alkyl group, a cycloalkyl group, an optionally substituted aryl group, an optionally substituted heterocycloalkyl group, or an optionally substituted aromatic heterocyclic group; T is an oxygen atom, a sulfur atom, a sulfonyl group etc.; Q is a hydrogen atom or an optionally substituted lower alkyl group; and Z is a hydrogen atom, a hydroxy group etc., or a pharmaceutically acceptable salt thereof, which exert a potent and selective activated blood coagulation factor X inhibitory activity and is useful as an agent for the prevention or treatment of a disease occurred associating an activated blood coagulation factor X, a pharmaceutical composition comprising the same, a pharmaceutical use thereof and an intermediate thereof.

5. 发明申请

US20070105829A1 5-AMIDINO-2-HYDROXYBENZENESULFONAMIDE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME AND INTERMEDIATES FOR THEIR PREPARATION 失效
标题翻译： 5-氨基-2-羟基苯甲酰胺衍生物，含有它们的药物组合物及其制备中间体
公开(公告)号：US20070105829A1
公开(公告)日：2007-05-10
申请号：US11553573
申请日：2006-10-27
申请人： Kosuke OKAZAKI , Masahiko Uchida , Harunobu Mukaiyama , Hiroaki Kobayashi , Yuichiro Kai , Hideki Takeuchi , Kenji Yokoyama , Yoshihiro Terao , Yuji Hoyano , Hiroaki Shiohara , Norihiko Kikuchi
发明人： Kosuke OKAZAKI , Masahiko Uchida , Harunobu Mukaiyama , Hiroaki Kobayashi , Yuichiro Kai , Hideki Takeuchi , Kenji Yokoyama , Yoshihiro Terao , Yuji Hoyano , Hiroaki Shiohara , Norihiko Kikuchi
IPC分类号： A61K31/553 , A61K31/55 , A61K31/5377 , A61K31/445 , A61K31/421 , A61K31/40 , A61K31/18
CPC分类号： A61K31/18 , A61K31/40 , A61K31/421 , A61K31/445 , A61K31/5377 , A61K31/55 , A61K31/553 , C07C311/29 , C07C311/37 , C07C317/32 , C07C2601/14
摘要： The present invention relates to a 5-amidino-2-hydroxybenzenesulfonamide derivative represented by the general formula: wherein R1 is a hydrogen atom or an optionally substituted lower alkyl group; R2 is a di(lower alkyl)amino group, a lower alkyl group, a cycloalkyl group, an optionally substituted aryl group, an optionally substituted heterocycloalkyl group, or an optionally substituted aromatic heterocyclic group; T is an oxygen atom, a sulfur atom, a sulfonyl group etc.; Q is a hydrogen atom or an optionally substituted lower alkyl group; and Z is a hydrogen atom, a hydroxy group etc., or a pharmaceutically acceptable salt thereof, which exert a potent and selective activated blood coagulation factor X inhibitory activity and is useful as an agent for the prevention or treatment of a disease occurred associating an activated blood coagulation factor X, a pharmaceutical composition comprising the same, a pharmaceutical use thereof and an intermediate thereof.
摘要翻译：本发明涉及由以下通式表示的5-脒基-2-羟基苯磺酰胺衍生物：其中R 1是氢原子或任选取代的低级烷基; R 2是二（低级烷基）氨基，低级烷基，环烷基，任选取代的芳基，任选取代的杂环烷基或任选取代的芳族杂环基; T是氧原子，硫原子，磺酰基等; Q是氢原子或任意取代的低级烷基; Z是氢原子，羟基等，或其药学上可接受的盐，其具有有效和选择性的活化凝血因子X抑制活性，并且可用作预防或治疗疾病的药剂，活化凝血因子X，包含其的药物组合物，其药物用途及其中间体。

6. 发明申请

US20060205812A1 5-Amidino-2-hydroxybenzenesulfonamide derivatives, pharmaceutical compositions containing the same and intermediates for their preparation 失效
标题翻译： 5-脒基-2-羟基苯磺酰胺衍生物，含有它们的药物组合物及其制备中间体
公开(公告)号：US20060205812A1
公开(公告)日：2006-09-14
申请号：US11359430
申请日：2006-02-23
申请人： Kosuke Okazaki , Masahiko Uchida , Harunobu Mukaiyama , Hiroaki Kobayashi , Yuichiro Kai , Hideki Takeuchi , Kenji Yokoyama , Yoshihiro Terao , Yuji Hoyano , Hiroaki Shiohara , Norihiko Kikuchi
发明人： Kosuke Okazaki , Masahiko Uchida , Harunobu Mukaiyama , Hiroaki Kobayashi , Yuichiro Kai , Hideki Takeuchi , Kenji Yokoyama , Yoshihiro Terao , Yuji Hoyano , Hiroaki Shiohara , Norihiko Kikuchi
IPC分类号： A61K31/24 , A61K31/195 , C07C311/47
CPC分类号： A61K31/18 , A61K31/40 , A61K31/421 , A61K31/445 , A61K31/5377 , A61K31/55 , A61K31/553 , C07C311/29 , C07C311/37 , C07C317/32 , C07C2601/14
摘要： The present invention relates to a 5-amidino-2-hydroxybenzenesulfonamide derivative represented by the general formula: wherein R1 is a hydrogen atom or an optionally substituted lower alkyl group; R2 is a di(lower alkyl)amino group, a lower alkyl group, a cycloalkyl group, an optionally substituted aryl group, an optionally substituted heterocycloalkyl group, or an optionally substituted aromatic heterocyclic group; T is an oxygen atom, a sulfur atom, a sulfonyl group etc.; Q is a hydrogen atom or an optionally substituted lower alkyl group; and Z is a hydrogen atom, a hydroxy group etc., or a pharmaceutically acceptable salt thereof, which exert a potent and selective activated blood coagulation factor X inhibitory activity and is useful as an agent for the prevention or treatment of a disease occurred associating an activated blood coagulation factor X, a pharmaceutical composition comprising the same, a pharmaceutical use thereof and an intermediate thereof.
摘要翻译：本发明涉及由以下通式表示的5-脒基-2-羟基苯磺酰胺衍生物：其中R 1是氢原子或任选取代的低级烷基; R 2是二（低级烷基）氨基，低级烷基，环烷基，任选取代的芳基，任选取代的杂环烷基或任选取代的芳族杂环基; T是氧原子，硫原子，磺酰基等; Q是氢原子或任意取代的低级烷基; Z是氢原子，羟基等，或其药学上可接受的盐，其具有有效和选择性的活化凝血因子X抑制活性，并且可用作预防或治疗疾病，活化凝血因子X，包含其的药物组合物，其药物用途及其中间体。

7. 发明授权

US07230031B2 Thyroid hormone receptor ligand, medicinal compositions containing the same and use thereof 失效
标题翻译：甲状腺激素受体配体，含有其的药物组合物及其用途
公开(公告)号：US07230031B2
公开(公告)日：2007-06-12
申请号：US10502737
申请日：2003-01-28
申请人： Hiroaki Shiohara , Tetsuya Nakamura , Norihiko Kikuchi , Tomonaga Ozawa , Makio Kitazawa
发明人： Hiroaki Shiohara , Tetsuya Nakamura , Norihiko Kikuchi , Tomonaga Ozawa , Makio Kitazawa
IPC分类号： A61K31/19 , C07C303/00
CPC分类号： C07D213/75 , A61K31/19 , A61K31/22 , A61K31/223 , A61K31/225 , A61K31/27 , A61K31/341 , A61K31/351 , A61K31/40 , A61K31/426 , A61K31/44 , A61K31/4406 , A61K31/50 , A61K31/5375 , A61K31/54 , C07C59/72 , C07C233/25 , C07C233/56 , C07C235/66 , C07C309/65 , C07C311/29 , C07C317/22 , C07C323/41 , C07C323/67 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07D209/08 , C07D213/76 , C07D237/14 , C07D249/12 , C07D253/075 , C07D257/04 , C07D257/06 , C07D271/07 , C07D277/34 , C07D295/13 , C07D295/192 , C07D295/26 , C07D307/12 , C07D309/06 , C07D403/12 , C07D413/12 , C07D417/12
摘要： The present invention provides a compound represented by general formula (I): or pharmaceutically acceptable salts thereof, wherein W is O, S(O)m, CH2 and the like; R1 is halogen, lower alkyl, halo-lower alkyl, CN and the like; R3 is hydrogen and the like; R4 is hydrogen, halogen, alkyl, halo-lower alkyl, substituted alkyl, aryl, aralkyl, alkoxy, substituted alkoxy, alkanoyl, aroyl, —CONR7(R8), —S(O)mR9, —SO2NR7(R8) and the like; R5 is hydrogen, halogen, alkyl, substituted alkyl and the like; A is —N(R6)CO—A1—COR10 and the like; pharmaceutical compositions containing them and their uses, which have a high affinity to human thyroid hormone receptors, in particular human thyroid hormone receptor β.
摘要翻译：本发明提供由通式（I）表示的化合物或其药学上可接受的盐，其中W为O，S（O）m，CH 2等 ; R 1是卤素，低级烷基，卤代低级烷基，CN等; R 3是氢等; R 4是氢，卤素，烷基，卤代低级烷基，取代的烷基，芳基，芳烷基，烷氧基，取代的烷氧基，烷酰基，芳酰基，-CONR 7 S（O）m R 9，-SO 2 NR 7，S（O）（R 8 S 8）等; R 5是氢，卤素，烷基，取代的烷基等; A是-N（R 6）CO-A 1 -COR 10等; 含有它们的药物组合物及其用途，其对人甲状腺激素受体，特别是甲状腺激素受体β具有高亲和力。

8. 发明申请

US20090239860A1 NOVEL BENZOFURAN DERIVATIVE, MEDICINAL COMPOSITION CONTAINING THE SAME, AND USES OF THESE 审中-公开
标题翻译：新的苯唑嘌呤衍生物，含有它们的药物组合物及其用途
公开(公告)号：US20090239860A1
公开(公告)日：2009-09-24
申请号：US10597443
申请日：2005-01-21
申请人： Tetsuya Nakamura , Hiroaki Shiohara , Yoshihiro Terao , Satoko Nakayama , Keiji Miyazawa , Hideki Ohnota
发明人： Tetsuya Nakamura , Hiroaki Shiohara , Yoshihiro Terao , Satoko Nakayama , Keiji Miyazawa , Hideki Ohnota
IPC分类号： A61K31/5377 , C07D413/00 , A61P35/00
CPC分类号： C07D405/12
摘要： The present invention provides compounds represented by general formula (I): or pharmaceutical acceptable salts thereof, wherein R1 is hydrogen or lower alkyl; R2 is lower alkyl, halo-lower alkyl, cycloalkyl, heterocycloalkyl, aryl, aralkyl, arylalkenyl, aryloxy-lower alkyl, heteroaryl, heteroaryl-lower alkyl, etc; R3, R4, R5 and R6 are each hydrogen, halogen, cyano, lower alkyl, halo-lower alkyl, lower alkoxy, hydroxy, aryl, etc; provided that at least one of R3, R4, R5 and R6 is other than hydrogen. Compound (I) of the present invention shows a potent adenosine A2A receptor antagonistic activity, and are useful for treating or preventing a disease mediated by adenosine A2A receptors such as motor function disorders, depression, anxiety disorders, cognitive function disorders, cerebral ischemia disorders, restless legs syndrome and the like.
摘要翻译：本发明提供由通式（I）表示的化合物或其药学上可接受的盐，其中R 1是氢或低级烷基; R2是低级烷基，卤代低级烷基，环烷基，杂环烷基，芳基，芳烷基，芳基烯基，芳氧基 - 低级烷基，杂芳基，杂芳基 - 低级烷基等; R3，R4，R5和R6各自为氢，卤素，氰基，低级烷基，卤代低级烷基，低级烷氧基，羟基，芳基等; 条件是R3，R4，R5和R6中的至少一个不是氢。本发明的化合物（I）显示有效的腺苷A 2A受体拮抗活性，可用于治疗或预防由腺苷A2A受体介导的疾病，例如运动功能障碍，抑郁症，焦虑症，认知功能障碍，脑缺血障碍，不安腿综合征等。

9. 发明申请

US20050085541A1 Novel thyroid hormone receptor ligand, medicinal compositions containing the same and use thereof 失效
标题翻译：新型甲状腺激素受体配体，含有该甲状腺激素受体配体的药物组合物及其应用
公开(公告)号：US20050085541A1
公开(公告)日：2005-04-21
申请号：US10502737
申请日：2003-01-28
申请人： Hiroaki Shiohara , Tetsuya Nakamura , Norihiko Kikuchi , Tomonaga Ozawa , Makio Kitazawa
发明人： Hiroaki Shiohara , Tetsuya Nakamura , Norihiko Kikuchi , Tomonaga Ozawa , Makio Kitazawa
IPC分类号： A61K31/19 , A61K31/22 , A61K31/223 , A61K31/225 , A61K31/27 , A61K31/341 , A61K31/351 , A61K31/40 , A61K31/426 , A61K31/44 , A61K31/4406 , A61K31/50 , A61K31/5375 , A61K31/54 , A61P1/16 , A61P3/04 , A61P3/10 , A61P5/14 , A61P5/16 , A61P9/04 , A61P9/06 , A61P9/10 , A61P9/12 , A61P17/00 , A61P17/06 , A61P19/10 , A61P25/24 , A61P27/06 , A61P35/00 , A61P37/08 , A61P43/00 , C07C59/72 , C07C233/25 , C07C233/56 , C07C235/66 , C07C309/65 , C07C311/29 , C07C317/22 , C07C323/41 , C07C323/67 , C07D209/08 , C07D213/75 , C07D213/76 , C07D237/14 , C07D249/12 , C07D253/075 , C07D257/04 , C07D257/06 , C07D271/06 , C07D271/07 , C07D277/24 , C07D277/34 , C07D295/13 , C07D295/192 , C07D295/26 , C07D307/12 , C07D309/06 , C07D403/12 , C07D413/12 , C07D417/12 , A61K31/24 , A61K31/12 , A61K31/165 , A61K31/18
CPC分类号： C07D213/75 , A61K31/19 , A61K31/22 , A61K31/223 , A61K31/225 , A61K31/27 , A61K31/341 , A61K31/351 , A61K31/40 , A61K31/426 , A61K31/44 , A61K31/4406 , A61K31/50 , A61K31/5375 , A61K31/54 , C07C59/72 , C07C233/25 , C07C233/56 , C07C235/66 , C07C309/65 , C07C311/29 , C07C317/22 , C07C323/41 , C07C323/67 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07D209/08 , C07D213/76 , C07D237/14 , C07D249/12 , C07D253/075 , C07D257/04 , C07D257/06 , C07D271/07 , C07D277/34 , C07D295/13 , C07D295/192 , C07D295/26 , C07D307/12 , C07D309/06 , C07D403/12 , C07D413/12 , C07D417/12
摘要： The present invention provides a compound represented by general formula (I): or pharmaceutically acceptable salts thereof, wherein W is O, S(O)m, CH2 and the like; R1 is halogen, lower alkyl, halo-lower alkyl, CN and the like; R3 is hydrogen and the like; R4 is hydrogen, halogen, alkyl, halo-lower alkyl, substituted alkyl, aryl, aralkyl, alkoxy, substituted alkoxy, alkanoyl, aroyl, —CONR7(R8), —S(O)mR9, —SO2NR7(R8) and the like; R5 is hydrogen, halogen, alkyl, substituted alkyl and the like; A is —N(R6)CO-A1-COR10 and the like; pharmaceutical compositions containing them and their uses, which have a high affinity to human thyroid hormone receptors, in particular human thyroid hormone receptor β.
摘要翻译：本发明提供由通式（I）表示的化合物或其药学上可接受的盐，其中W为O，S（O）m，CH 2等 ; R 1是卤素，低级烷基，卤代低级烷基，CN等; R 3是氢等; R 4是氢，卤素，烷基，卤代低级烷基，取代的烷基，芳基，芳烷基，烷氧基，取代的烷氧基，烷酰基，芳酰基，-CONR 7 S（O）m R 9，-SO 2 NR 7，S（O）（R 8 S 8）等; R 5是氢，卤素，烷基，取代的烷基等; A是-N（R 6）CO-A 1 -COR 10等; 含有它们的药物组合物及其用途，其对人甲状腺激素受体，特别是甲状腺激素受体β具有高亲和力。

10. 发明授权

US07217697B2 Glucopyranosyloxypyrazole derivative medicinal composition containing the same medicinal use thereof and intermediate therefor 失效
标题翻译：含有相同药用的吡喃葡萄糖氧吡唑衍生物药物组合物及其中间体
公开(公告)号：US07217697B2
公开(公告)日：2007-05-15
申请号：US10479083
申请日：2002-05-27
申请人： Hiroaki Shiohara , Hideki Fujikura , Nobuhiko Fushimi , Fumiaki Ito , Masayuki Isaji
发明人： Hiroaki Shiohara , Hideki Fujikura , Nobuhiko Fushimi , Fumiaki Ito , Masayuki Isaji
IPC分类号： A01N43/04 , A61K31/70 , C07H15/00 , C07H17/00
CPC分类号： C07D231/20 , C07H15/26 , C07H17/02
摘要： The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R1 is a hydrogen atom or a hydroxyalkyl group; one of Q and T is a group represented by the general formula; the other is an optionally substituted alkyl group or a cycloalkyl group; and R2 is a halogen atom, a hydroxy group, an optionally substituted alkyl group, an optionally substituted alkoxy group, an alkylthio group, a group of the general formula: -A-R3 wherein A is a single bond, an oxygen atom, a methylene group, an ethylene group, —OCH2— or —CH2O—; and R3 is a cycloalkyl group, a heterocycloalkyl group, an optionally substituted aryl group, an optionally substituted tiazolyl group or an optionally substituted pyridyl group, pharmaceutically acceptable salts thereof or prodrugs thereof, which exert an excellent inhibitory activity in human SGLT1, and therefore are useful as drugs for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, pharmaceutical compositions comprising the same, pharmaceutical uses thereof and production intermediates thereof.
摘要翻译：本发明提供由以下通式表示的吡喃葡萄糖氧吡唑衍生物：其中R 1是氢原子或羟烷基; Q和T之一是由通式表示的基团; 另一个是任选取代的烷基或环烷基; R 2是卤素原子，羟基，任意取代的烷基，任意取代的烷氧基，烷硫基，通式为-AR 3的基团，其中A是单键，氧原子，亚甲基，亚乙基，-OCH 2 - 或-CH 2 O-; 和R 3是环烷基，杂环烷基，任选取代的芳基，任选取代的噻唑基或任选取代的吡啶基，其药学上可接受的盐或其前药，其具有优异的抑制性因此可用作预防或治疗与糖尿病，糖尿病并发症或肥胖症等高血糖症相关的疾病的药物，其药物组合物，药物组合物及其生产中间体。

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