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1. 发明申请

US20130137865A1 HETEROARYL-PYRAZOLE DERIVATIVE 审中-公开
标题翻译：异丙基吡唑衍生物
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。

2. 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。

3. 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。

4. 发明申请

US20110213143A1 COMPOUND HAVING TAFIA INHIBITORY ACTIVITY 审中-公开
标题翻译：具有TAFIA抑制活性的化合物
公开(公告)号：US20110213143A1
公开(公告)日：2011-09-01
申请号：US13126685
申请日：2009-10-28
申请人： Hideaki Amada , Daisuke Matsuda , Masahiro Bohno , Shiuji Saito , Ayako Bohno
发明人： Hideaki Amada , Daisuke Matsuda , Masahiro Bohno , Shiuji Saito , Ayako Bohno
IPC分类号： C07D487/04 , C07D471/04 , C07D498/04 , C07D471/14
CPC分类号： C07D471/04 , C07D487/04
摘要： Provided are compounds having superior TAFIa inhibitory activity. Specifically, there are provided compounds represented by the following formula (I) or pharmaceutically acceptable salts thereof: wherein A is a benzene ring or a pyridine ring; X is the formula —(CH2)—, the formula —(CH2)2—, an oxygen atom, a nitrogen atom or a single bond; Y is the formula —(CH2)3—NH—R3, the formula —(CH2)4—NH—R3 or a 2-aminopyridyl group; R3 is a hydrogen atom, a C1-6 alkyl group, or the formula —CO2R4; R4 is a C1-6 alkyl group, the formula —CHR5OC(O)R6, or a substituent having the structure represented by the following formula Ia; R5 is a C1-6 alkyl group; R6 is a C1-6 alkyl group, a C3-8 cycloalkyl group, or a phenyl group; R7 is a C1-6 alkyl group or a phenyl group; R1 is a hydrogen atom, a halogen atom, a C1-4 alkyl group substituted by 1-3 halogen atoms, a C1-10 alkyl group, a C1-8 alkoxy group, a C3-8 cycloalkyl group, a C3-8 cycloalkoxy group, a C4-14 cycloalkylalkyl group, or a phenyl group; R2 is CO2R8, or a tetrazolyl group; R8 is a hydrogen atom, a C1-10 alkyl group, or a substituent having the structure represented by the following formula Ib or Ic; m and n are each an integer of zero or one.
摘要翻译：提供具有优异TAFIa抑制活性的化合物。具体地，提供由下式（I）表示的化合物或其药学上可接受的盐：其中A是苯环或吡啶环; X是式 - （CH 2） - ，式 - （CH 2）2 - ，氧原子，氮原子或单键; Y是式 - （CH2）3-NH-R3，式 - （CH2）4-NH-R3或2-氨基吡啶基; R 3是氢原子，C 1-6烷基或式-CO 2 R 4; R4是C1-6烷基，式-CHR5OC（O）R6或具有由下式Ia表示的结构的取代基; R5是C1-6烷基; R6是C1-6烷基，C3-8环烷基或苯基; R7是C1-6烷基或苯基; R1是氢原子，卤素原子，被1-3个卤素原子取代的C1-4烷基，C1-10烷基，C1-8烷氧基，C3-8环烷基，C3-8环烷氧基基团，C4-14环烷基烷基或苯基; R2是CO2R8或四唑基; R8是氢原子，C1-10烷基或具有由下式Ib或Ic表示的结构的取代基; m和n分别为0或1的整数。

5. 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。

6. 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，

7. 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。

8. 发明授权

US07214714B2 20-hydroxyeicosatetraenoic acid production inhibitors 有权
标题翻译： 20-羟基二十碳四烯酸生产抑制剂
公开(公告)号：US07214714B2
公开(公告)日：2007-05-08
申请号：US10475869
申请日：2002-04-26
申请人： Masakazu Sato , Noriyuki Miyata , Takaaki Ishii , Yuko Matsunaga , Hideaki Amada
发明人： Masakazu Sato , Noriyuki Miyata , Takaaki Ishii , Yuko Matsunaga , Hideaki Amada
IPC分类号： A61K31/136 , A61K31/402 , C07C259/14 , C07D207/20 , C07D211/00 , C07D213/00 , C07D215/00 , C07D241/00 , C07D295/00 , C07D491/00
CPC分类号： C07D213/75 , A61K31/136 , A61K31/402 , A61K31/4418 , A61K31/451 , A61K31/4525 , A61K31/47 , A61K31/495 , A61K31/496 , A61K31/5375 , A61K31/54 , A61K31/55 , C07C259/14 , C07D207/20 , C07D211/22 , C07D211/46 , C07D211/60 , C07D211/62 , C07D211/70 , C07D213/74 , C07D217/04 , C07D295/13 , C07D295/135 , C07D295/15 , C07D401/04 , C07D491/10
摘要： A hydroxyformamidine compound represented by the following formula or a pharmaceutically acceptable salt thereof [wherein R1 represents a substituted morpholino group, a substituted piperidino group, a piperazin-1-yl group, a substituted piperazin-1-yl group, a thiomorpholin-1-yl group, a perhydroazepin-1-yl group, a perhydroazocin-1-yl group, a tetrahydropyridin-1-yl group, a pyrrolin-1-yl group, etc.; X represents a nitrogen atom or a group represented by CR5; and R2 to R5 are the same or different and each represents a hydrogen atom, a C1-4 alkyl group, a C1-4 alkoxy group, a trifluoromethyl group or a halogen atom.] There is provided a drug which inhibits an enzyme producing 20-HETE participating in a contracting or dilating action for microvessels and an inducing action for cell proliferation in main organs such as kidney and cerebrovascular vessels.
摘要翻译：由下式表示的羟基脒化合物或其药学上可接受的盐[其中R 1表示取代的吗啉代基，取代的哌啶子基，哌嗪-1-基，取代的哌嗪-1-基，吡咯啉-1-基，四氢吡啶-1-基，吡咯啉-1-基，四氢吡啶-1-基，四氢吡啶-1-基，四氢吡啶-1-基，吡咯啉-1-基等。 X表示氮原子或由CR 5表示的基团; R 5和R 5相同或不同，各自表示氢原子，C 1-4烷基，C 1-4烷基， SUB 1-4个烷氧基，三氟甲基或卤素原子。]提供了抑制参与微血管的收缩或扩张作用的20-HETE的酶和细胞增殖诱导作用的药物在主要器官如肾脏和脑血管血管。

9. 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。

10. 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。

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