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，

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，

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。

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。

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。

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 。

公开(公告)号：US20120172598A1

公开(公告)日：2012-07-05

申请号：US13496625

申请日：2010-09-17

申请人： Hideaki Amada ,  Daisuke Matsuda ,  Ayako Bohno

发明人： Hideaki Amada ,  Daisuke Matsuda ,  Ayako Bohno

IPC分类号： C07D471/04

CPC分类号： C07D471/04 ,  A61K31/4745

摘要： The present invention provides compounds having superior TAFIa inhibitory activity. They are dihydroimidazoquinoline compounds represented by the following formula (I) or pharmaceutically acceptable salts thereof: wherein R is a hydrogen atom or a C1-10 alkyl group; R1 is a hydrogen atom, a C1-10 alkyl group, a C3-8 cycloalkyl group or a substituent having the structure represented by the following formula Ia or Ib: where R3 is a C1-6 alkyl group; R4 is a C1-6 alkyl group, a C3-8 cycloalkyl group, or a benzyl group; and R2 is a hydrogen atom or a substituent having the structure represented by the following formula Ic or Id:

摘要翻译： 本发明提供具有优异TAFIa抑制活性的化合物。 它们是由下式（I）表示的二氢咪唑并喹啉化合物或其药学上可接受的盐：其中R是氢原子或C1-10烷基; R1是氢原子，C1-10烷基，C3-8环烷基或具有由下式Ia或Ib表示的结构的取代基：其中R3是C1-6烷基; R4是C1-6烷基，C3-8环烷基或苄基; 并且R 2是氢原子或具有由下式Ic或Id表示的结构的取代基：

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。

公开(公告)号：US20130137865A1

公开(公告)日：2013-05-30

申请号：US13814869

申请日：2011-08-11

申请人： Toshio Nakamura ,  Kazunari Sakagami ,  Kazuhide Konishi ,  Kanako Yamamoto ,  Seiji Masuda ,  Yohei Matsuda ,  Kumiko Okada ,  Tsuyoshi Shibata ,  Hiroshi Ohta ,  Akito Yasuhara ,  Hiroshi Kawamoto ,  Hideaki Amada ,  Hiroki Urabe ,  Rie Nishikawa ,  Shuhei Kashiwa ASHIWA

发明人： Toshio Nakamura ,  Kazunari Sakagami ,  Kazuhide Konishi ,  Kanako Yamamoto ,  Seiji Masuda ,  Yohei Matsuda ,  Kumiko Okada ,  Tsuyoshi Shibata ,  Hiroshi Ohta ,  Akito Yasuhara ,  Hiroshi Kawamoto ,  Hideaki Amada ,  Hiroki Urabe ,  Rie Nishikawa ,  Shuhei Kashiwa ASHIWA

IPC分类号： C07D413/14 ,  C07D413/04 ,  C07D403/04 ,  C07D231/38

CPC分类号： C07D413/14 ,  C07D231/38 ,  C07D403/04 ,  C07D403/14 ,  C07D413/04

摘要： A compound represented by formula [I] and a pharmaceutically accepted salt of said compound are a novel compound and a pharmaceutically accepted salt thereof which exert antagonistic activity against group II metabotropic glutamate (mGlu) receptors, and are effective as a novel preventive or therapeutic agent for disorders such as mood disorders (depressive disorder, bipolar disorder, etc.), anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, posttraumatic stress disorder, a specific phobic disorder, acute stress disorder, etc.), schizophrenia, Alzheimer's disease, cognitive impairment, dementia, drug dependence, convulsions, shivering, pain, sleep disorders, and the like.

摘要翻译： 由式[I]表示的化合物和所述化合物的药学上可接受的盐是对II族代谢型谷氨酸（mGlu）受体具有拮抗作用的新化合物及其药学上可接受的盐，并且作为新的预防或治疗剂是有效的 用于诸如情绪障碍（抑郁障碍，双相情感障碍等），焦虑障碍（广泛性焦虑症，恐慌症，强迫症，社会焦虑症，创伤后应激障碍，特异性恐怖症，急性应激障碍等） ，精神分裂症，阿尔茨海默病，认知障碍，痴呆，药物依赖，抽搐，发抖，疼痛，睡眠障碍等。

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。