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1. 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。

2. 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。

3. 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。

4. 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。

5. 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。

6. 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。

7. 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。

8. 发明授权

US07078400B2 20-HETE synthase inhibitor 失效
标题翻译： 20-HETE合酶抑制剂
公开(公告)号：US07078400B2
公开(公告)日：2006-07-18
申请号：US10609547
申请日：2003-07-01
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： A61P7/02
CPC分类号： A61K31/155 , A61K31/166 , A61K31/18 , A61K31/245 , A61K31/275 , A61K31/341 , A61K31/343 , A61K31/351 , A61K31/352 , A61K31/357 , A61K31/36 , A61K31/381 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/404 , A61K31/415 , A61K31/416 , A61K31/4192 , A61K31/42 , A61K31/4245 , A61K31/426 , A61K31/428 , A61K31/429 , A61K31/433 , A61K31/44 , A61K31/4402 , A61K31/445 , A61K31/4453 , A61K31/45 , A61K31/472 , A61K31/502 , A61K31/505 , A61K31/522 , A61K31/5375 , C07C311/21 , C07C311/46 , C07C317/40 , C07C323/12 , C07C323/19 , C07C323/41 , C07C323/52 , C07C323/65 , C07C335/26 , C07C2601/08 , C07C2601/14
摘要： The present invention relates to an inhibitor for production of 20-hydroxyeicosatetraenoic acid, comprising, as an effective ingredient, specific hydroxyformamidine derivatives or pharmaceutically-acceptable salts thereof. The inhibitors according to the present invention are useful as therapeutic agents for kidney diseases, cerebrovascular diseases, or circulatory diseases.In addition, the present invention also provides novel hydroxyformamidine derivatives or pharmaceutically-acceptable salts thereof.
摘要翻译：本发明涉及一种用于制备20-羟基二十碳烯四烯酸的抑制剂，其包含作为有效成分的特定羟基甲脒衍生物或其药学上可接受的盐。根据本发明的抑制剂可用作肾脏疾病，脑血管疾病或循环系统疾病的治疗剂。此外，本发明还提供新的羟基甲脒衍生物或其药学上可接受的盐。

9. 发明授权

US06864254B1 Inhibitor for 20-hete-yielding enzyme 失效
标题翻译：抑制剂为20-hte生产酶
公开(公告)号：US06864254B1
公开(公告)日：2005-03-08
申请号：US09869103
申请日：2000-11-01
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： A61K31/155 , A61K31/166 , A61K31/18 , A61K31/245 , A61K31/275 , A61K31/341 , A61K31/343 , A61K31/351 , A61K31/352 , A61K31/357 , A61K31/36 , A61K31/381 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/404 , A61K31/415 , A61K31/416 , A61K31/4192 , A61K31/42 , A61K31/4245 , A61K31/426 , A61K31/428 , A61K31/429 , A61K31/433 , A61K31/44 , A61K31/4402 , A61K31/445 , A61K31/4453 , A61K31/45 , A61K31/472 , A61K31/502 , A61K31/505 , A61K31/522 , A61K31/5375 , C07C311/21 , C07C311/46 , C07C317/40 , C07C323/12 , C07C323/19 , C07C323/41 , C07C323/52 , C07C323/65 , C07C335/26 , A81K31/155
CPC分类号： A61K31/155 , A61K31/166 , A61K31/18 , A61K31/245 , A61K31/275 , A61K31/341 , A61K31/343 , A61K31/351 , A61K31/352 , A61K31/357 , A61K31/36 , A61K31/381 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/404 , A61K31/415 , A61K31/416 , A61K31/4192 , A61K31/42 , A61K31/4245 , A61K31/426 , A61K31/428 , A61K31/429 , A61K31/433 , A61K31/44 , A61K31/4402 , A61K31/445 , A61K31/4453 , A61K31/45 , A61K31/472 , A61K31/502 , A61K31/505 , A61K31/522 , A61K31/5375 , C07C311/21 , C07C311/46 , C07C317/40 , C07C323/12 , C07C323/19 , C07C323/41 , C07C323/52 , C07C323/65 , C07C335/26 , C07C2601/08 , C07C2601/14
摘要： An inhibitor for 20-hydroxyeicosatetraenoic acid production which comprises as the active ingredient a specific hydroxyformamidine derivative or a pharmacologically acceptable salt thereof. It is useful especially as a remedy for kidney diseases, cerebrovascular diseases, or circulatory diseases. The novel hydroxyformamidine derivative or pharmacologically acceptable salt thereof is also provided.
摘要翻译：一种20-羟基二十碳烯四烯酸生产抑制剂，其包含作为活性成分的特定羟基甲脒衍生物或其药理学上可接受的盐。特别是作为肾脏疾病，脑血管疾病或循环系统疾病的补救措施是有用的。还提供了新的羟基甲脒衍生物或其药理学上可接受的盐。

10. 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。

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