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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

US20100216787A1 THIAZOLE DERIVATIVE 审中-公开
标题翻译：噻唑衍生物
公开(公告)号：US20100216787A1
公开(公告)日：2010-08-26
申请号：US12644594
申请日：2009-12-22
申请人： Masakazu Sato , Yuko Matsunaga , Hajime Asanuma , Hideaki Amada , Takeshi Koami , Tetsuo Takayama , Tetsuya Yabuuchi , Fumiyasu Shiozawa , Hironori Katakai , Hiroki Umemiya , Akiko Ikeda
发明人： Masakazu Sato , Yuko Matsunaga , Hajime Asanuma , Hideaki Amada , Takeshi Koami , Tetsuo Takayama , Tetsuya Yabuuchi , Fumiyasu Shiozawa , Hironori Katakai , Hiroki Umemiya , Akiko Ikeda
IPC分类号： A61K31/426 , C07D417/14 , A61K31/427 , A61K31/4439 , C07D417/04 , A61K31/428 , A61K31/5377 , A61K31/454 , C07D277/24 , C07D277/22 , A61P1/16 , A61P17/00 , A61P13/12
CPC分类号： A61K8/49 , A61Q7/00 , C07D417/04 , C07D417/06 , C07D417/14
摘要： A thiazolylimidazole derivative represented by the formula or a pharmaceutically acceptable salt thereof, and an ALK5 inhibitor, an therapeutic agent for alopecia or a hair growth agent having the above as an active ingredient, wherein: X1 and X2 are different from each other and represent a sulfur atom or a carbon atom; R1 represents a phenyl group; a substituted phenyl group; a phenyl group condensed with a hetero aromatic ring; a pyridyl group; or a pyridyl group condensed with a hetero aromatic ring; R2 represents a hydrogen atom, a halogen atom, an alkyl group having 1 to 6 carbon atoms, an alkyl group having 1 to 6 carbon atoms substituted with 1 to 5 halogen atoms, an alkoxy group having 1 to 6 carbon atoms, an alkanoyl group having 1 to 5 carbon atoms, or a hydroxyalkyl group having 1 to 6 carbon atoms, A represents a group which is represented by the formula. The present invention provides an inhibitory substance against ALK5 which is a TGF-β type I receptor and provides a hair growth stimulant or a hair growth agent based on its novel activities.
摘要翻译：由下式表示的噻唑咪唑衍生物或其药学上可接受的盐，以及ALK5抑制剂，秃发治疗剂或具有上述作为活性成分的毛发生长剂，其中：X1和X2彼此不同，表示硫原子或碳原子; R1表示苯基; 取代的苯基; 与杂芳环稠合的苯基; 吡啶基; 或与杂芳环稠合的吡啶基; R2表示氢原子，卤素原子，碳原子数1〜6的烷基，碳原子数1〜5的碳原子数1〜5的烷基，碳原子数1〜6的烷氧基，烷氧基具有1至5个碳原子，或具有1至6个碳原子的羟烷基，A表示由下式表示的基团。本发明提供一种抗ALK5抑制物质，其为TGF- I型受体，并且基于其新的活性提供毛发生长兴奋剂或毛发生长剂。

4. 发明授权

US07678810B2 Thiazole derivative 失效
标题翻译：噻唑衍生物
公开(公告)号：US07678810B2
公开(公告)日：2010-03-16
申请号：US10591614
申请日：2005-03-04
申请人： Masakazu Sato , Yuko Matsunaga , Hajime Asanuma , Hideaki Amada , Takeshi Koami , Tetsuo Takayama , Tetsuya Yabuuchi , Fumiyasu Shiozawa , Hironori Katakai , Hiroki Umemiya , Akiko Ikeda
发明人： Masakazu Sato , Yuko Matsunaga , Hajime Asanuma , Hideaki Amada , Takeshi Koami , Tetsuo Takayama , Tetsuya Yabuuchi , Fumiyasu Shiozawa , Hironori Katakai , Hiroki Umemiya , Akiko Ikeda
IPC分类号： A61K31/4439 , C07D277/62 , C07D317/48
CPC分类号： A61K8/49 , A61Q7/00 , C07D417/04 , C07D417/06 , C07D417/14
摘要： A thiazolylimidazole derivative represented by the formula or a pharmaceutically acceptable salt thereof, and an ALK5 inhibitor, an therapeutic agent for alopecia or a hair growth agent having the above as an active ingredient, wherein: X1 and X2 are different from each other and represent a sulfur atom or a carbon atom; R1 represents a phenyl group; a substituted phenyl group; a phenyl group condensed with a hetero aromatic ring; a pyridyl group; or a pyridyl group condensed with a hetero aromatic ring; R2 represents a hydrogen atom, a halogen atom, an alkyl group having 1 to 6 carbon atoms, an alkyl group having 1 to 6 carbon atoms substituted with 1 to 5 halogen atoms, an alkoxy group having 1 to 6 carbon atoms, an alkanoyl group having 1 to 5 carbon atoms, or a hydroxyalkyl group having 1 to 6 carbon atoms, A represents a group which is represented by the formula. The present invention provides an inhibitory substance against ALK5 which is a TGF-β type I receptor and provides a hair growth stimulant or a hair growth agent based on its novel activities.
摘要翻译：由下式表示的噻唑咪唑衍生物或其药学上可接受的盐，以及ALK5抑制剂，秃发治疗剂或具有上述作为活性成分的毛发生长剂，其中：X1和X2彼此不同，表示硫原子或碳原子; R1表示苯基; 取代的苯基; 与杂芳环稠合的苯基; 吡啶基; 或与杂芳环稠合的吡啶基; R2表示氢原子，卤素原子，碳原子数1〜6的烷基，碳原子数1〜5的碳原子数1〜5的烷基，碳原子数1〜6的烷氧基，烷氧基具有1至5个碳原子，或具有1至6个碳原子的羟烷基，A表示由下式表示的基团。本发明提供一种抗ALK5抑制物质，其为TGF- I型受体，并且基于其新的活性提供毛发生长兴奋剂或毛发生长剂。

5. 发明申请

US20070154428A1 Thiazole derivative 失效
标题翻译：噻唑衍生物
公开(公告)号：US20070154428A1
公开(公告)日：2007-07-05
申请号：US10591614
申请日：2005-03-04
申请人： Masakazu Sato , Yuko Matsunaga , Hajime Asanuma , Hideaki Amada , Takeshi Koami , Tetsuo Takayama , Tetsuya Yabuuchi , Fumiyasu Shiozawa , Hironori Katakai , Hiroki Umemiya , Akiko Ikeda
发明人： Masakazu Sato , Yuko Matsunaga , Hajime Asanuma , Hideaki Amada , Takeshi Koami , Tetsuo Takayama , Tetsuya Yabuuchi , Fumiyasu Shiozawa , Hironori Katakai , Hiroki Umemiya , Akiko Ikeda
IPC分类号： A61K8/49 , A61K31/5377 , A61K31/496 , A61K31/4709 , A61K31/454 , A61K31/427 , C07D417/02
CPC分类号： A61K8/49 , A61Q7/00 , C07D417/04 , C07D417/06 , C07D417/14
摘要： A thiazolylimidazole derivative represented by the formula or a pharmaceutically acceptable salt thereof, and an ALK5 inhibitor, an therapeutic agent for alopecia or a hair growth agent having the above as an active ingredient, wherein: X1 and X2 are different from each other and represent a sulfur atom or a carbon atom; R1 represents a phenyl group; a substituted phenyl group; a phenyl group condensed with a hetero aromatic ring; a pyridyl group; or a pyridyl group condensed with a hetero aromatic ring; R2 represents a hydrogen atom, a halogen atom, an alkyl group having 1 to 6 carbon atoms, an alkyl group having 1 to 6 carbon atoms substituted with 1 to 5 halogen atoms, an alkoxy group having 1 to 6 carbon atoms, an alkanoyl group having 1 to 5 carbon atoms, or a hydroxyalkyl group having 1 to 6 carbon atoms, A represents a group which is represented by the formula. The present invention provides an inhibitory substance against ALK5 which is a TGF-β type I receptor and provides a hair growth stimulant or a hair growth agent based on its novel activities.
摘要翻译：由下式表示的噻唑咪唑衍生物或其药学上可接受的盐，以及ALK5抑制剂，秃发治疗剂或具有上述作为活性成分的毛发生长剂，其中：X 1和X 2 2个彼此不同，表示硫原子或碳原子; R 1表示苯基; 取代的苯基; 与杂芳环稠合的苯基; 吡啶基; 或与杂芳环稠合的吡啶基; R 2表示氢原子，卤素原子，具有1至6个碳原子的烷基，具有1至5个被1至5个卤素原子取代的碳原子的烷基，具有1个至6个碳原子，具有1至5个碳原子的烷酰基或具有1至6个碳原子的羟烷基，A表示由下式表示的基团。本发明提供了抗ALK5的抑制物质，其为TGF-β1型受体，并且基于其新的活性提供毛发生长刺激剂或毛发生长剂。

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，

9. 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，

10. 发明授权

US06670382B2 Hydroxyformamidine derivatives and medicines containing the same 失效
标题翻译：羟基甲脒衍生物和含有其的药物
公开(公告)号：US06670382B2
公开(公告)日：2003-12-30
申请号：US10311003
申请日：2002-12-12
申请人： Masakazu Sato , Noriyuki Miyata , Takaaki Ishii , Yuko Kobayashi , Hideaki Amada
发明人： Masakazu Sato , Noriyuki Miyata , Takaaki Ishii , Yuko Kobayashi , Hideaki Amada
IPC分类号： C07D21353
CPC分类号： C07D213/74
摘要： Pharmaceutical agents for inhibiting the production of 20-HETE which participates in constriction or dilation of microvessels in major organs such as the kidneys and the cerebral blood vessels, or participates in causing cell proliferation are provided. The present invention relates to hydroxyamidine compounds represented by the formula: wherein R1 represents a group represented by the formula: R2—(CH2)m— (wherein R2 represents a C3-8 cycloalkyl group, a C2-6 alkoxycarbonyl group, a C2-10 alkenyl group, a C2-6 alkynyl group, a substituted or non-substituted aryl group, or the like, and m is an integer of 1 to 8), a group represented by the formula: R3—A— (wherein R3 represents a hydrogen atom, a C1-6 alkoxy group, a C3-8 cycloalkoxy group, or the like, and A represents a straight-chain C2-10 alkylene group which may be substituted with a C1-6 alkyl group or a trifluoromethyl group), or a C3-8 cycloalkyl group, and X represents an oxygen atom or a sulfur atom, or pharmaceutically acceptable salts thereof, and relates to medicines including the same as active ingredients.
摘要翻译：提供了用于抑制参与诸如肾脏和脑血管等主要器官的微血管收缩或扩张的20-HETE的生产的药剂，或参与引起细胞增殖。本发明涉及由下式表示的羟基脒化合物：其中R 1表示由下式表示的基团：R 2 - （CH 2）m - （其中R 2表示C 3-8环烷基， C 2-6烷氧基羰基，C 2-10烯基，C 2-6炔基，取代或未取代的芳基等，m为1〜8的整数），式 R 3 -A-（其中R 3表示氢原子，C 1-6烷氧基，C 3-8环烷氧基等，A表示直链C 2-10亚烷基，可以被C 1-6烷基或三氟甲基取代）或C 3-8环烷基，X表示氧原子或硫原子，或其药学上可接受的盐，并且涉及含有活性的药物配料。

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