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1. 发明申请

US20100069460A1 1-PHENYL 1-THIO-D-GLUCITOL DERIVATIVE 审中-公开
标题翻译： 1-苯基-1-硫代-D-葡萄糖苷衍生物
公开(公告)号：US20100069460A1
公开(公告)日：2010-03-18
申请号：US12516758
申请日：2007-12-14
申请人： Hiroyuki Kakinuma , Takahiro Oi , Yuko Hashimoto , Hitomi Takahashi , Yohei Kobashi , Yuki Iwata , Kenichi Kawabe , Masato Takahashi
发明人： Hiroyuki Kakinuma , Takahiro Oi , Yuko Hashimoto , Hitomi Takahashi , Yohei Kobashi , Yuki Iwata , Kenichi Kawabe , Masato Takahashi
IPC分类号： A61K31/382 , C07D335/02 , A61P3/10
CPC分类号： C07D335/02
摘要： A 1-phenyl 1-thio-D-glucitol compound represented by formula (I) or the like: or a pharmaceutically acceptable salt thereof or a hydrate thereof, or a pharmaceutical preparation comprising the same as an active ingredient is useful as a novel type of prophylactic or therapeutic agent for diabetes, diabetes-related diseases or diabetic complications, which inhibits both SGLT1 and SGLT2 activities to achieve not only suppression of glucose absorption from the digestive tract but also excretion of urinary sugars.
摘要翻译：由式（I）等表示的1-苯基-1-硫代-D-葡萄糖醇化合物或其药学上可接受的盐或其水合物，或其作为活性成分的药物制剂可用作新型用于糖尿病，糖尿病相关疾病或糖尿病并发症的预防或治疗剂，其抑制SGLT1和SGLT2活性，不仅抑制来自消化道的葡萄糖吸收，而且实现尿糖的排泄。

2. 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，

3. 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，

4. 发明授权

US08115017B2 C-phenyl 1-thioglucitol compound 失效
标题翻译： C-苯基1-硫代葡萄糖醇化合物
公开(公告)号：US08115017B2
公开(公告)日：2012-02-14
申请号：US12305157
申请日：2007-06-28
申请人： Hiroyuki Kakinuma , Takahiro Oi , Yohei Kobashi , Yuko Hashimoto , Hitomi Takahashi
发明人： Hiroyuki Kakinuma , Takahiro Oi , Yohei Kobashi , Yuko Hashimoto , Hitomi Takahashi
IPC分类号： C70D335/02
CPC分类号： C07D335/02 , C07H7/04
摘要： C-phenyl 1-thioglucitol compounds of the following formula (I) or pharmaceutically acceptable salts thereof or hydrates thereof: [wherein X represents a hydrogen atom or a C1-6 alkyl group, Y represents a C1-6 alkylene group or —O—(CH2)n- (wherein n represents an integer of 1 to 5), and Z represents —CONHRA or —NHCONHRB (provided that when Z represents —NHCONHRB, n is not 1), wherein RA represents a C1-6 alkyl group substituted with 1 to 3 substituents selected from the group consisting of a hydroxyl group and —CONH2, and RB represents a hydrogen atom or a C1-6 alkyl group substituted with 1 to 3 substituents selected from the group consisting of a hydroxyl group and —CONH2] are useful as prophylactic or therapeutic agents for diabetes, because of their suppressive effect on sugar (e.g., glucose) absorption through inhibition of SGLT1 activity, or alternatively, because of their suppressive effect on sugar (e.g., glucose) absorption and excretory effect on urinary sugars through inhibition of both SGLT1 and SGLT2 activities.
摘要翻译：下式（I）的C-苯基-1-硫代葡萄糖醇化合物或其药学上可接受的盐或其水合物：[其中X表示氢原子或C1-6烷基，Y表示C1-6亚烷基或-O- （CH 2）n - （其中n表示1〜5的整数），Z表示-CONHRA或-NHCONHRB（条件是当Z表示-NHCONHRB时，n不为1），其中RA表示C1-6烷基取代具有1〜3个选自羟基和-CONH 2的取代基，RB表示氢原子或被1〜3个选自羟基和-CONH 2的取代基取代的C 1-6烷基] 可用作糖尿病的预防或治疗剂，因为它们通过抑制SGLT1活性而对糖（例如葡萄糖）的吸收具有抑制作用，或者由于其对糖（例如葡萄糖）对尿液的吸收和排泄作用的抑制作用糖通过抑制SGLT1和SGLT2两种活性。

5. 发明申请

US20100004465A1 C-PHENYL 1-THIOGLUCITOL COMPOUND 失效
标题翻译： C-PHENYL 1-THIOGLUCITOL化合物
公开(公告)号：US20100004465A1
公开(公告)日：2010-01-07
申请号：US12305157
申请日：2007-06-28
申请人： Hiroyuki Kakinuma , Takahiro Oi , Yohei Kobashi , Yuko Hashimoto , Hitomi Takahashi
发明人： Hiroyuki Kakinuma , Takahiro Oi , Yohei Kobashi , Yuko Hashimoto , Hitomi Takahashi
IPC分类号： C07D335/02
CPC分类号： C07D335/02 , C07H7/04
摘要： C-phenyl 1-thioglucitol compounds of the following formula (I) or pharmaceutically acceptable salts thereof or hydrates thereof: [wherein X represents a hydrogen atom or a C1-6 alkyl group, Y represents a C1-6 alkylene group or —O—(CH2)n- (wherein n represents an integer of 1 to 5), and Z represents —CONHRA or —NHCONHRB (provided that when Z represents —NHCONHRB, n is not 1), wherein RA represents a C1-6 alkyl group substituted with 1 to 3 substituents selected from the group consisting of a hydroxyl group and —CONH2, and RB represents a hydrogen atom or a C1-6 alkyl group substituted with 1 to 3 substituents selected from the group consisting of a hydroxyl group and —CONH2] are useful as prophylactic or therapeutic agents for diabetes, because of their suppressive effect on sugar (e.g., glucose) absorption through inhibition of SGLT1 activity, or alternatively, because of their suppressive effect on sugar (e.g., glucose) absorption and excretory effect on urinary sugars through inhibition of both SGLT1 and SGLT2 activities.
摘要翻译：下式（I）的C-苯基-1-硫代葡萄糖醇化合物或其药学上可接受的盐或其水合物：[其中X表示氢原子或C1-6烷基，Y表示C1-6亚烷基或-O- （CH 2）n - （其中n表示1〜5的整数），Z表示-CONHRA或-NHCONHRB（条件是当Z表示-NHCONHRB时，n不为1），其中RA表示C1-6烷基取代具有1〜3个选自羟基和-CONH 2的取代基，RB表示氢原子或被1〜3个选自羟基和-CONH 2的取代基取代的C 1-6烷基] 可用作糖尿病的预防或治疗剂，因为它们通过抑制SGLT1活性而对糖（例如葡萄糖）的吸收具有抑制作用，或者由于其对糖（例如葡萄糖）对尿液的吸收和排泄作用的抑制作用糖通过抑制 SGLT1和SGLT2两种活动。

6. 发明申请

US20080132563A1 1-Thio-D-Glucitol Derivatives 有权
标题翻译： 1-Thio-D-葡萄糖醇衍生物
公开(公告)号：US20080132563A1
公开(公告)日：2008-06-05
申请号：US11794498
申请日：2006-01-10
申请人： Hiroyuki Kakinuma , Yuko Hashimoto , Takahiro Oi , Hitomi Takahashi
发明人： Hiroyuki Kakinuma , Yuko Hashimoto , Takahiro Oi , Hitomi Takahashi
IPC分类号： C07D335/02 , A61K31/382 , A61P3/10
CPC分类号： C07D409/14 , A61K31/382 , A61K31/7004 , A61K45/06 , C07D335/02 , C07D409/04 , C07D409/10 , C07D417/10 , C07D495/04 , A61K2300/00
摘要： The present invention provides a 1-thio-D-glucitol compound of the following formula, which shows the action of inhibiting the activity of SGLT2, a pharmaceutically acceptable salt of the compound, or a hydrate of the compound or the salt; and a pharmaceutical comprising such a compound as an active ingredient, especially, a pharmaceutical for preventing or treating diabetes, diabetes-related disease, or diabetic complication. The invention also provides a method for producing the 1-thio-D-glucitol compound and its intermediate.
摘要翻译：本发明提供下式的1-硫代-D-葡萄糖醇化合物，其显示抑制SGLT2的活性，化合物的药学上可接受的盐或化合物或其盐的水合物的作用; 以及包含作为活性成分的化合物，特别是糖尿病预防或治疗药物，糖尿病相关疾病或糖尿病并发症的药物。本发明还提供了1-硫代-D-葡萄糖醇化合物及其中间体的制备方法。

7. 发明授权

US07910619B2 1-thio-D-glucitol derivatives 有权
公开(公告)号：US07910619B2
公开(公告)日：2011-03-22
申请号：US11794498
申请日：2006-01-10
申请人： Hiroyuki Kakinuma , Yuko Hashimoto , Takahiro Oi , Hitomi Takahashi
发明人： Hiroyuki Kakinuma , Yuko Hashimoto , Takahiro Oi , Hitomi Takahashi
IPC分类号： A61K31/382 , C07D335/02
CPC分类号： C07D409/14 , A61K31/382 , A61K31/7004 , A61K45/06 , C07D335/02 , C07D409/04 , C07D409/10 , C07D417/10 , C07D495/04 , A61K2300/00
摘要： The present invention provides a 1-thio-D-glucitol compound of the following formula, which shows the action of inhibiting the activity of SGLT2, a pharmaceutically acceptable salt of the compound, or a hydrate of the compound or the salt; and a pharmaceutical comprising such a compound as an active ingredient, especially, a pharmaceutical for preventing or treating diabetes, diabetes-related disease, or diabetic complication. The invention also provides a method for producing the 1-thio-D-glucitol compound and its intermediate.

8. 发明申请

US20110098469A1 1-THIO-D-GLUCITOL DERIVATIVES 有权
标题翻译： 1-THIO-D-葡萄糖苷衍生物
公开(公告)号：US20110098469A1
公开(公告)日：2011-04-28
申请号：US12982343
申请日：2010-12-30
申请人： Hiroyuki KAKINUMA , Yuko Hashimoto , Takahiro Ol , Hitomi Takahashi
发明人： Hiroyuki KAKINUMA , Yuko Hashimoto , Takahiro Ol , Hitomi Takahashi
IPC分类号： C07D335/02 , C07D409/12 , C07D409/10 , C07D409/04 , C07D417/10 , C07D495/04
CPC分类号： C07D409/14 , A61K31/382 , A61K31/7004 , A61K45/06 , C07D335/02 , C07D409/04 , C07D409/10 , C07D417/10 , C07D495/04 , A61K2300/00
摘要： The present invention provides a 1-thio-D-glucitol compound of the following formula, which shows the action of inhibiting the activity of SGLT2, a pharmaceutically acceptable salt of the compound, or a hydrate of the compound or the salt; and a pharmaceutical comprising such a compound as an active ingredient, especially, a pharmaceutical for preventing or treating diabetes, diabetes-related disease, or diabetic complication. The invention also provides a method for producing the 1-thio-D-glucitol compound and its intermediate.
摘要翻译：本发明提供下式的1-硫代-D-葡萄糖醇化合物，其显示抑制SGLT2的活性，化合物的药学上可接受的盐或化合物或其盐的水合物的作用; 以及包含作为活性成分的化合物，特别是糖尿病预防或治疗药物，糖尿病相关疾病或糖尿病并发症的药物。本发明还提供了1-硫代-D-葡萄糖醇化合物及其中间体的制备方法。

9. 发明授权

US08017792B2 1-thio-D-glucitol derivatives 有权
标题翻译： 1-硫代-D-葡萄糖醇衍生物
公开(公告)号：US08017792B2
公开(公告)日：2011-09-13
申请号：US12982343
申请日：2010-12-30
申请人： Hiroyuki Kakinuma , Yuko Hashimoto , Takahiro Ol , Hitomi Takahashi
发明人： Hiroyuki Kakinuma , Yuko Hashimoto , Takahiro Ol , Hitomi Takahashi
IPC分类号： C07D335/02
CPC分类号： C07D409/14 , A61K31/382 , A61K31/7004 , A61K45/06 , C07D335/02 , C07D409/04 , C07D409/10 , C07D417/10 , C07D495/04 , A61K2300/00
摘要： The present invention provides a 1-thio-D-glucitol compound of the following formula, which shows the action of inhibiting the activity of SGLT2, a pharmaceutically acceptable salt of the compound, or a hydrate of the compound or the salt; and a pharmaceutical comprising such a compound as an active ingredient, especially, a pharmaceutical for preventing or treating diabetes, diabetes-related disease, or diabetic complication. The invention also provides a method for producing the 1-thio-D-glucitol compound and its intermediate.
摘要翻译：本发明提供下式的1-硫代-D-葡萄糖醇化合物，其显示抑制SGLT2的活性，化合物的药学上可接受的盐或化合物或其盐的水合物的作用; 以及包含作为活性成分的化合物，特别是糖尿病预防或治疗药物，糖尿病相关疾病或糖尿病并发症的药物。本发明还提供了1-硫代-D-葡萄糖醇化合物及其中间体的制备方法。

10. 发明授权

US08872638B2 Controlling communication among multiple industrial control systems 有权
公开(公告)号：US08872638B2
公开(公告)日：2014-10-28
申请号：US13446172
申请日：2012-04-13
申请人： Kazuhito Akiyama , Michiharu Kudo , Hitomi Takahashi , Naohiko Uramoto
发明人： Kazuhito Akiyama , Michiharu Kudo , Hitomi Takahashi , Naohiko Uramoto
IPC分类号： H04B3/36 , H04L29/06
CPC分类号： H04L63/1408 , H04L67/12
摘要： A communication control method and system for controlling communication among multiple industrial control systems connected via a network. The communication control system includes: a communication relay apparatus for relaying communication between at least two of multiple industrial control systems; a monitoring section for monitoring the multiple industrial control systems; and a control section for switching, if the monitoring section detects an anomaly from at least one of the multiple industrial control systems, communication between an industrial control system detected with an anomaly and a second industrial control system so that the communication is performed via the communication relay apparatus.

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