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1. 发明授权

US07439232B2 Heteroaryl 5-thio-β-D-glucopyranoside derivatives and therapeutic agents for diabetes containing the same 失效
标题翻译：杂芳基5-硫代-β-D-吡喃葡萄糖苷衍生物和含有它们的糖尿病治疗剂
公开(公告)号：US07439232B2
公开(公告)日：2008-10-21
申请号：US10551115
申请日：2004-02-06
申请人： Hiroyuki Kakinuma , Masakazu Sato , Hideaki Amada , Hajime Asanuma , Yuko Tsuchiya
发明人： Hiroyuki Kakinuma , Masakazu Sato , Hideaki Amada , Hajime Asanuma , Yuko Tsuchiya
IPC分类号： A01N43/04 , A61K31/70 , C07H15/00 , C07H17/00 , C07G3/00 , C07G11/00
CPC分类号： C07D409/12 , C07D409/14 , C07H17/02
摘要： There is provided a heteroaryl 5-thio-β-D-glucopyranoside compound of the following formula, which has an inhibitory effect on SGLT2 activity, or a pharmaceutically acceptable salt thereof or a hydrate thereof. There is also provided a pharmaceutical preparation, particularly a prophylactic or therapeutic agent for diabetes, diabetes-related diseases or diabetic complications, which comprises such a compound as an active ingredient.
摘要翻译：提供了对SGLT2活性具有抑制作用的下式的杂芳基5-硫代-β-D-吡喃葡萄糖苷化合物或其药学上可接受的盐或其水合物。还提供了药物制剂，特别是糖尿病，糖尿病相关疾病或糖尿病并发症的预防或治疗剂，其包含这种化合物作为活性成分。

2. 发明申请

US20060194809A1 Heteroaryl 5-thio-beta-d-gucopyranoside derivatives and therapeutic agents for diabetes containing the same 失效
标题翻译：杂芳基5-硫代-β-D-吡喃葡萄糖苷衍生物和含有它们的糖尿病治疗剂
公开(公告)号：US20060194809A1
公开(公告)日：2006-08-31
申请号：US10551115
申请日：2004-02-06
申请人： Hiroyuki Kakinuma , Masakazu Sato , Hideaki Amada , Hajime Asanuma , Yuko Tsuchiya
发明人： Hiroyuki Kakinuma , Masakazu Sato , Hideaki Amada , Hajime Asanuma , Yuko Tsuchiya
IPC分类号： A61K31/501 , A61K31/416 , C07D409/02
CPC分类号： C07D409/12 , C07D409/14 , C07H17/02
摘要： There is provided a heteroaryl 5-thio-β-D-glucopyranoside compound of the following formula, which has an inhibitory effect on SGLT2 activity, or a pharmaceutically acceptable salt thereof or a hydrate thereof. There is also provided a pharmaceutical preparation, particularly a prophylactic or therapeutic agent for diabetes, diabetes-related diseases or diabetic complications, which comprises such a compound as an active ingredient.
摘要翻译：提供了对SGLT2活性具有抑制作用的下式的杂芳基5-硫代-β-D-吡喃葡萄糖苷化合物或其药学上可接受的盐或其水合物。还提供了药物制剂，特别是糖尿病，糖尿病相关疾病或糖尿病并发症的预防或治疗剂，其包含这种化合物作为活性成分。

3. 发明申请

US20050209309A1 Aryl 5-thio-beta-d-glucopyranoside derivatives and remedies for diabetes containing the same 失效
标题翻译：芳基5-硫代-β-D-吡喃葡萄糖苷衍生物及含有其的糖尿病治疗药物
公开(公告)号：US20050209309A1
公开(公告)日：2005-09-22
申请号：US10518788
申请日：2003-08-08
申请人： Masakazu Sato , Hiroyuki Kakinuma , Hajime Asanuma
发明人： Masakazu Sato , Hiroyuki Kakinuma , Hajime Asanuma
IPC分类号： A61K31/7034 , A61P3/10 , A61P13/12 , A61P43/00 , C07H15/20 , C07H15/203 , C07D335/02 , A61K31/382 , C07D49/02
CPC分类号： C07H15/203 , C07H15/20
摘要： There is provided a 5-thio-β-D-glucopyranoside compound of the following formula, which has an inhibitory effect on SGLT2 activity, or a pharmaceutically acceptable salt thereof or a hydrate thereof. There is also provided a pharmaceutical preparation, particularly a prophylactic or therapeutic agent for diabetes, diabetes-related diseases or diabetic complications, which comprises such a compound as an active ingredient.
摘要翻译：提供了对SGLT2活性具有抑制作用的下式的5-硫代-β-D-吡喃葡萄糖苷化合物或其药学上可接受的盐或其水合物。还提供了药物制剂，特别是糖尿病，糖尿病相关疾病或糖尿病并发症的预防或治疗剂，其包含这种化合物作为活性成分。

4. 发明授权

US07414072B2 Aryl 5-thio-β-d-glucopyranoside derivatives and therapeutic agents for diabetes containing the same 失效
标题翻译：芳基5-硫代-β-D-吡喃葡萄糖苷衍生物和含有它们的糖尿病治疗剂
公开(公告)号：US07414072B2
公开(公告)日：2008-08-19
申请号：US10518788
申请日：2003-08-08
申请人： Masakazu Sato , Hiroyuki Kakinuma , Hajime Asanuma
发明人： Masakazu Sato , Hiroyuki Kakinuma , Hajime Asanuma
IPC分类号： A01N43/04 , A01N43/18 , C07D335/02
CPC分类号： C07H15/203 , C07H15/20
摘要： There is provided a 5-thio-β-D-glucopyranoside compound of the following formula, which has an inhibitory effect on SGLT2 activity, or a pharmaceutically acceptable salt thereof or a hydrate thereof. There is also provided a pharmaceutical preparation, particularly a prophylactic or therapeutic agent for diabetes, diabetes-related diseases or diabetic complications, which comprises such a compound as an active ingredient.
摘要翻译：提供了对SGLT2活性具有抑制作用的下式的5-硫代-β-D-吡喃葡萄糖苷化合物或其药学上可接受的盐或其水合物。还提供了药物制剂，特别是糖尿病，糖尿病相关疾病或糖尿病并发症的预防或治疗剂，其包含这种化合物作为活性成分。

5. 发明授权

US07250522B2 Method for selective preparation of aryl 5-thio-β-D-aldohexopyranosides 失效
标题翻译：芳基5-硫代-β-D-吡喃半乳糖苷的选择性制备方法
公开(公告)号：US07250522B2
公开(公告)日：2007-07-31
申请号：US10521809
申请日：2003-08-08
申请人： Masakazu Sato , Hiroyuki Kakinuma , Hajime Asanuma
发明人： Masakazu Sato , Hiroyuki Kakinuma , Hajime Asanuma
IPC分类号： C07D335/02
CPC分类号： C07H15/203 , C07H15/20
摘要： The present invention provides a method for preparing an aryl 5-thio-β-D-aldohexopyranoside derivative of Formula (III), which comprises reacting a 5-thio-D-aldohexopyranose derivative of Formula (I) with Ar-OH of Formula (II) in the presence of a phosphine represented by PR11R12R13 and an azo reagent represented by R21—N═N—R22 in accordance with the following scheme
摘要翻译：本发明提供了制备式（III）的5-硫代-β-D-吡喃葡萄糖苷衍生物的方法，该方法包括使式（I）的5-硫代-D-去二羟基吡喃糖衍生物与式（I）的Ar-OH反应， II）在由PR 11和12 R 12表示的膦和由R 21表示的偶氮试剂存在下， SUP> -NNR <22>根据以下方案

6. 发明授权

US07288566B2 N-hydroxyformamidine derivatives 失效
标题翻译： N-羟基甲脒衍生物
公开(公告)号：US07288566B2
公开(公告)日：2007-10-30
申请号：US10527716
申请日：2003-09-11
申请人： Masakazu Sato , Hiroyuki Kakinuma , Hideaki Amada
发明人： Masakazu Sato , Hiroyuki Kakinuma , Hideaki Amada
IPC分类号： C07C249/04 , C07D207/06 , A61K31/40 , A61K31/155
CPC分类号： C07C251/34 , C07C259/14 , C07D207/06 , C07D295/135 , C07D319/06
摘要： An N-hydroxyformamidine compound of the following formula or a pharmaceutically acceptable salt thereof: wherein R1, A and R are as defined herein. The compounds inhibit 20-HETE-producing enzymes, 20-HETE being involved in the effects of causing microvascular constriction or dilation in major organs (e.g., kidneys, cerebral blood vessels) or of inducing cell proliferation.
摘要翻译：下式的N-羟基甲脒化合物或其药学上可接受的盐：其中R 1，A和R如本文所定义。该化合物抑制20-HETE产生酶，20-HETE参与在主要器官（例如肾脏，脑血管）中引起微血管收缩或扩张或诱导细胞增殖的作用。

7. 发明申请

US20060004078A1 N-hydroxyformamidine derivatives 失效
标题翻译： N-羟基甲脒衍生物
公开(公告)号：US20060004078A1
公开(公告)日：2006-01-05
申请号：US10527716
申请日：2003-09-11
申请人： Masakazu Sato , Hiroyuki Kakinuma , Hideaki Amada
发明人： Masakazu Sato , Hiroyuki Kakinuma , Hideaki Amada
IPC分类号： A61K31/40 , C07D207/04 , A61K31/155
CPC分类号： C07C251/34 , C07C259/14 , C07D207/06 , C07D295/135 , C07D319/06
摘要： An N-hydroxyformamidine derivative of the following formula or a pharmaceutically acceptable salt thereof: (wherein R1 represents a hydrogen atom, a C1-4 alkyl group, a C1-4 alkoxy group or a halogen atom, A represents a C1-10 alkylene group or a group of the following formula: (wherein m, n and p each represent an integer of 0 to 4), and R represents an N,N-di-C1-6 alkylamino group, a dioxanyl group, a C1-4 alkyl-substituted dioxanyl group, a C1-4 alkoxy-C1-4 alkoxy group or a group of the following formula: (wherein s and t each represent an integer of 1 to 4, B represents a methylene group, an oxygen atom, a sulfur atom, a nitrogen atom, a C1-4 alkyl-substituted nitrogen atom, a phenyl-substituted nitrogen atom or a benzyl-substituted nitrogen atom, R2 represents a hydrogen atom or a C1-4 alkyl group, and r represents an integer of 0 to 2)). The present invention aims to provide an agent for inhibiting 20-HETE-producing enzymes, 20-HETE being involved in the effects of causing microvascular constriction or dilation in major organs (e.g., kidneys, cerebral blood vessels) or of inducing cell proliferation, etc.
摘要翻译：下式的N-羟基甲脒衍生物或其药学上可接受的盐：（其中R 1表示氢原子，C 1-4烷基，C 1〜 C 1-4烷氧基或卤素原子，A表示C 1-10烷基或下式的基团：（其中m，n和p各自表示 0〜4的整数），R表示N，N-二-C 1-6烷基氨基，二烷基，C 1-4烷基取代的二烷基，C 1-4烷氧基-C 1-4烷氧基或下式的基团：（其中s和t各自表示1〜 4，B表示亚甲基，氧原子，硫原子，氮原子，C 1-4烷基取代的氮原子，苯基取代的氮原子或苄基取代的氮原子，R 2表示氢原子或C 1-4烷基，r表示0〜2的整数））。本发明的目的在于提供一种抑制20-HETE产生酶的药剂，20-HETE涉及在主要器官（例如，肾脏，脑血管）中引起微血管收缩或扩张或诱导细胞增殖等的作用。

8. 发明申请

US20100022460A1 C-PHENYL GLYCITOL COMPOUND 有权
标题翻译： C-PHENYL GLYCITOL化合物
公开(公告)号：US20100022460A1
公开(公告)日：2010-01-28
申请号：US12301463
申请日：2007-05-18
申请人： Hiroyuki Kakinuma , Yohei Kobashi , Yuko Hashimoto , Takahiro Oi , Hitomi Takahashi , Hideaki Amada , Yuki Iwata
发明人： Hiroyuki Kakinuma , Yohei Kobashi , Yuko Hashimoto , Takahiro Oi , Hitomi Takahashi , Hideaki Amada , Yuki Iwata
IPC分类号： A61K31/70 , C07H1/00
CPC分类号： C07D405/10 , C07D309/12
摘要： Provided is a novel C-phenyl glycitol compound that may serve as a prophylactic or therapeutic agent for diabetes by inhibiting both SGLT1 activity and SGLT2 activity, thereby exhibiting a glucose absorption suppression action and a urine glucose excretion action. A C-phenyl glycitol compound represented by Formula (I) below or a pharmaceutically acceptable salt thereof or a hydrate thereof wherein R1 and R2 are the same or different and represent a hydrogen atom, a hydroxyl group, a C1-6 alkyl group, a C1-6 alkoxy group or a halogen atom, R3 is a hydrogen atom, a C1-6 alkyl group, a C1-6 alkoxy group or a halogen atom, Y is a C1-6 alkylene group, —O—(CH2)n— (n is an integer of 1 to 4) or a C2-6 alkenylene group, provided that when Z is —NHC(═NH)NH2 or —NHCON(RB)RC, n is not 1, Z is —CONHRA, —NHC(═NH)NH2 or —NHCON(RB)RC,
摘要翻译：提供了可以通过抑制SGLT1活性和SGLT2活性而作为糖尿病的预防或治疗剂的新颖的C-苯基糖醇化合物，从而表现出葡萄糖吸收抑制作用和尿葡萄糖排泄作用。由下式（I）表示的C-苯基糖醇化合物或其药学上可接受的盐或其水合物，其中R 1和R 2相同或不同，表示氢原子，羟基，C 1-6烷基， C 1-6烷氧基或卤原子，R 3为氢原子，C 1-6烷基，C 1-6烷氧基或卤素原子，Y为C 1-6亚烷基，-O-（CH 2）n - （n为1〜4的整数）或C 2-6亚烯基，条件是当Z为-NHC（-NH）NH 2或-NHCON（RB）RC时，n不为1，Z为-CONHRA， - NHC（-NH）NH 2或-NHCON（RB）RC，

9. 发明授权

US07973012B2 C-phenyl glycitol compound 有权
标题翻译： C-苯基甘氨醇化合物
公开(公告)号：US07973012B2
公开(公告)日：2011-07-05
申请号：US12301463
申请日：2007-05-18
申请人： Hiroyuki Kakinuma , Yohei Kobashi , Yuko Hashimoto , Takahiro Oi , Hitomi Takahashi , Hideaki Amada , Yuki Iwata
发明人： Hiroyuki Kakinuma , Yohei Kobashi , Yuko Hashimoto , Takahiro Oi , Hitomi Takahashi , Hideaki Amada , Yuki Iwata
IPC分类号： A01N43/04 , A61K31/70 , C07H1/00 , C07H5/04
CPC分类号： C07D405/10 , C07D309/12
摘要： Provided is a novel C-phenyl glycitol compound that may serve as a prophylactic or therapeutic agent for diabetes by inhibiting both SGLT1 activity and SGLT2 activity, thereby exhibiting a glucose absorption suppression action and a urine glucose excretion action. A C-phenyl glycitol compound represented by Formula (I) below or a pharmaceutically acceptable salt thereof or a hydrate thereof wherein R1 and R2 are the same or different and represent a hydrogen atom, a hydroxyl group, a C1-6 alkyl group, a C1-6 alkoxy group or a halogen atom, R3 is a hydrogen atom, a C1-6 alkyl group, a C1-6 alkoxy group or a halogen atom, Y is a C1-6 alkylene group, —O—(CH2)n- (n is an integer of 1 to 4) or a C2-6 alkenylene group, provided that when Z is —NHC(═NH)NH2 or —NHCON(RB)RC, n is not 1, Z is —CONHRA, —NHC(═NH)NH2 or —NHCON(RB)RC,
摘要翻译：提供了可以通过抑制SGLT1活性和SGLT2活性而作为糖尿病的预防或治疗剂的新颖的C-苯基糖醇化合物，从而表现出葡萄糖吸收抑制作用和尿葡萄糖排泄作用。由下式（I）表示的C-苯基糖醇化合物或其药学上可接受的盐或其水合物，其中R 1和R 2相同或不同，表示氢原子，羟基，C 1-6烷基， C 1-6烷氧基或卤原子，R 3为氢原子，C 1-6烷基，C 1-6烷氧基或卤素原子，Y为C 1-6亚烷基，-O-（CH 2）n - （n为1〜4的整数）或C 2-6亚烯基，条件是当Z为-NHC（= NH）NH 2或-NHCON（RB）RC时，n不为1，Z为-CONHRA， - NHC（= NH）NH 2或-NHCON（RB）RC，

10. 发明申请

US20050256317A1 Process for selective production of aryl 5-thio-beta-d- aldohexopyranosides 失效
标题翻译：选择性生产芳基5-硫代-β-D-二氢吡喃糖苷的方法
公开(公告)号：US20050256317A1
公开(公告)日：2005-11-17
申请号：US10521809
申请日：2003-08-08
申请人： Masakazu Sato , Hiroyuki Kakinuma
发明人： Masakazu Sato , Hiroyuki Kakinuma
IPC分类号： A61K31/7034 , A61P3/10 , A61P13/12 , A61P43/00 , C07H15/20 , C07H15/203 , C07D335/02
CPC分类号： C07H15/203 , C07H15/20
摘要： The present invention provides a method for preparing an aryl 5-thio-β-D-aldohexopyranoside derivative of Formula (III), which comprises reacting a 5-thio-D-aldohexopyranose derivative of Formula (I) with Ar—OH of Formula (II) in the presence of a phosphine represented by PR11R12R13 and an azo reagent represented by R21—N═N—R22 in accordance with the following scheme.
摘要翻译：本发明提供了制备式（III）的5-硫代-β-D-吡喃葡萄糖苷衍生物的方法，该方法包括使式（I）的5-硫代-D-去二羟基吡喃糖衍生物与式（I）的Ar-OH反应， II）在由PR 11和12 R 12表示的膦和由R 21表示的偶氮试剂存在下， SUP> -NNR <22>根据以下方案。

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