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1. 发明授权

US08822503B2 2-pyridone compounds 有权
标题翻译： 2-吡啶酮化合物
公开(公告)号：US08822503B2
公开(公告)日：2014-09-02
申请号：US13081201
申请日：2011-04-06
申请人： Takanori Kawaguchi , Kengo Watatani , Keiko Fusegi , Masahiro Bohno , Hajime Asanuma , Shoichi Kuroda , Yudai Imai , Tomomichi Chonan , Nagaaki Sato , Shigeru Tokita , Shigetada Sasako , Takumi Okada , Keishi Hayashi , Shin Itoh , Noriko Saito , Rui Jibiki , Seishi Ishiyama , Hirofumi Ota
发明人： Takanori Kawaguchi , Kengo Watatani , Keiko Fusegi , Masahiro Bohno , Hajime Asanuma , Shoichi Kuroda , Yudai Imai , Tomomichi Chonan , Nagaaki Sato , Shigeru Tokita , Shigetada Sasako , Takumi Okada , Keishi Hayashi , Shin Itoh , Noriko Saito , Rui Jibiki , Seishi Ishiyama , Hirofumi Ota
IPC分类号： A61K31/4439 , C07D401/06
CPC分类号： C07D401/10 , C07D213/64 , C07D401/12 , C07D401/14 , C07D405/10 , C07D413/06 , C07D417/06 , C07D417/14
摘要： A 2-pyridone compound represented by the formula [1]: {wherein in the formula [1], the ring represented by A represents a benzene ring or a pyridine ring, X represents any of the structures represented by the formulas [3] shown below: V represents a single bond or a lower alkylene group, and W represents a single bond, an ether bond or a lower alkylene group (wherein the lower alkylene group may contain an ether bond)}, a tautomer or stereoisomer of the compound, a pharmaceutically acceptable salt thereof, or a solvate thereof is a compound that has an excellent GK activating effect and is useful as a pharmaceutical.
摘要翻译：由式[1]表示的2-吡啶酮化合物：其中，在式[1]中，由A表示的环表示苯环或吡啶环，X表示由式[3]表示的任何结构 V表示单键或低级亚烷基，W表示单键，醚键或低级亚烷基（其中低级亚烷基可以含有醚键）}，化合物的互变异构体或立体异构体，其药学上可接受的盐或其溶剂合物是具有优异的GK活化作用并可用作药物的化合物。

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. 发明授权

US06720424B1 Aminobenzoic acid derivatives 失效
标题翻译：氨基苯甲酸衍生物
公开(公告)号：US06720424B1
公开(公告)日：2004-04-13
申请号：US10019525
申请日：2002-01-02
申请人： Hisaya Wada , Hajime Asanuma , Tetsuo Takayama , Masakazu Sato , Takehiro Yamagishi , Masabumi Shibuya
发明人： Hisaya Wada , Hajime Asanuma , Tetsuo Takayama , Masakazu Sato , Takehiro Yamagishi , Masabumi Shibuya
IPC分类号： C07D21172
CPC分类号： C07D213/80 , C07C235/24 , C07C235/38 , C07C317/50 , C07C323/63 , C07C2601/02
摘要： Aminobenzoic acid derivatives represented by Formula (1) as follows: (wherein, R1 represents a hydrogen atom, a C1-6alkyl group, or the like; R2 represents a hydrogen atom, a C1-6alkyl group, or the like; R3 represents a C8-25alkyl group, or the like; R4 represents a hydrogen atom or a group represented by OR9 or CO2R10 (wherein R9 and R10 represent a hydrogen atom or a C1-6 alkyl group); A represents a group represented by S(O)qR15 (wherein q is 0, 1, or 2, R15 represents a C1-6alkyl group, a phenyl C1-3alkyl group, or a group represented by (CH2)mOR16 (wherein m is 2 or 3, and R16 represents a hydrogen atom or a methoxymethyl group), or the like; X represents O, a single bond, CH═CH, or a group represented by NR27 (wherein R27 represents a hydrogen atom or a t-butoxycarbonyl group); Y represents O, CONH, NHCO, or a group represented by NR28 (wherein R28 represents a hydrogen atom or a t-butoxycarbonyl group); and n is an integer of 0 to 15) or pharmaceutically acceptable salts of the same are employed as VEGF receptor antagonists, and in particular as therapeutic agents for the diseases in which VEGF is involved.
摘要翻译：式（1）表示的氨基苯甲酸衍生物如下：（其中，R 1表示氢原子，C 1-6烷基等; R 2表示氢原子，C 1-6烷基或 R 3表示氢原子或由OR 9或CO 2 R 10表示的基团（其中R 9和R 10分别表示碳原子数3〜10的烷基， >表示氢原子或C 1-6烷基）; A表示由S（O）q R 15表示的基团（其中q为0,1或2，R 15为C 1-6烷基，苯基C 1-3烷基或由（CH 2）mOR 16表示的基团（其中m为2或3，R 16表示氢原子或甲氧基甲基）等; X表示O，单键，CH = CH或由NR 27表示的基团（其中R 27表示氢原子或叔丁氧基羰基）; Y表示O，CONH，NHCO或由NR a表示的基团， 28>（其中R 28表示氢原子或叔丁氧基羰基），n为0〜15的整数）或药物其可接受的盐用作VEGF受体拮抗剂，特别是作为涉及VEGF的疾病的治疗剂。

4. 发明申请

US20110288293A1 ISOQUINOLINE DERIVATIVE 失效
标题翻译：异喹啉衍生物
公开(公告)号：US20110288293A1
公开(公告)日：2011-11-24
申请号：US13142230
申请日：2009-12-25
申请人： Tetsuo Takayama , Hajime Asanuma , Daisuke Wakasugi , Rie Nishikawa , Yoshinori Sekiguchi , Madoka Kawamura , Naoya Ono , Tetsuya Yabuuchi , Takahiro Oi , Yusuke Oka , Shoichi Kuroda , Fumito Uneuchi , Takeshi Koami
发明人： Tetsuo Takayama , Hajime Asanuma , Daisuke Wakasugi , Rie Nishikawa , Yoshinori Sekiguchi , Madoka Kawamura , Naoya Ono , Tetsuya Yabuuchi , Takahiro Oi , Yusuke Oka , Shoichi Kuroda , Fumito Uneuchi , Takeshi Koami
IPC分类号： C07D413/12 , C07D401/12 , C07D405/12 , C07D217/24 , C07D409/12 , C07D471/04 , C07D401/06 , C07D217/16 , C07D417/12
CPC分类号： C07D217/16 , C07D217/18 , C07D217/20 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D471/04
摘要： A compound represented by formula (I) or a pharmaceutically acceptable salt thereof has an effect of inhibiting CRTH2 and, therefore, is useful as a preventive or a remedy for allergic diseases such as asthma, atopic dermatitis and allergic rhinitis.
摘要翻译：由式（I）表示的化合物或其药学上可接受的盐具有抑制CRTH2的作用，因此可用作哮喘，特应性皮炎和过敏性鼻炎等过敏性疾病的预防或治疗。

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. 发明申请

US20050209309A1 Aryl 5-thio-beta-d-glucopyranoside derivatives and remedies for diabetes containing the same 失效
标题翻译：芳基5-硫代-β-D-吡喃葡萄糖苷衍生物及含有其的糖尿病治疗药物
公开(公告)号：US20050209309A1
公开(公告)日：2005-09-22
申请号：US10518788
申请日：2003-08-08
申请人： Masakazu Sato , Hiroyuki Kakinuma , Hajime Asanuma
发明人： Masakazu Sato , Hiroyuki Kakinuma , Hajime Asanuma
IPC分类号： A61K31/7034 , A61P3/10 , A61P13/12 , A61P43/00 , C07H15/20 , C07H15/203 , C07D335/02 , A61K31/382 , C07D49/02
CPC分类号： C07H15/203 , C07H15/20
摘要： There is provided a 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。

7. 发明授权

US5571820A Heterocyclic compound 失效
标题翻译：杂环化合物
公开(公告)号：US5571820A
公开(公告)日：1996-11-05
申请号：US428119
申请日：1995-04-28
申请人： Yutaka Ohuchi , Masaji Suzuki , Hajime Asanuma , Sadakazu Yokomori , Katsuo Hatayama , Yoshihiko Isobe , Chika Ito , Makoto Muramatsu
发明人： Yutaka Ohuchi , Masaji Suzuki , Hajime Asanuma , Sadakazu Yokomori , Katsuo Hatayama , Yoshihiko Isobe , Chika Ito , Makoto Muramatsu
IPC分类号： C07D451/04 , A61K31/46
CPC分类号： C07D451/04
摘要： Endo-N-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl)-1 -isopropyl-2(1H)-quinolone-3-carboxamide shown by formula (I): ##STR1## or an acid addition salt thereof exhibits a potent action for stimulating a serotonin 4 receptor and is effective for the treatment of diseases and for the improvement of conditions, caused by a reduced motility in the gastrointestinal tract.
摘要翻译： PCT No.PCT / JP93 / 01484第 371日期：1995年4月28日 102（e）日期1995年4月28日PCT提交1993年10月15日PCT公布。第WO94 / 12497号公报日期：2002年6月9日由式（I）表示的内-N-（8-甲基-8-氮杂双环[3.2.1]辛-3-基）-1-异丙基（1H） - 喹诺酮-3-甲酰胺：（I）或其酸加成盐显示出刺激5-羟色胺4受体的有效作用，并且对于治疗由胃肠道中的运动性降低引起的疾病和改善病症是有效的。

8. 发明授权

US08461329B2 Isoquinoline derivative 失效
标题翻译：异喹啉衍生物
公开(公告)号：US08461329B2
公开(公告)日：2013-06-11
申请号：US13142230
申请日：2009-12-25
申请人： Tetsuo Takayama , Hajime Asanuma , Daisuke Wakasugi , Rie Nishikawa , Yoshinori Sekiguchi , Madoka Kawamura , Naoya Ono , Tetsuya Yabuuchi , Takahiro Oi , Yusuke Oka , Shoichi Kuroda , Fumito Uneuchi , Takeshi Koami
发明人： Tetsuo Takayama , Hajime Asanuma , Daisuke Wakasugi , Rie Nishikawa , Yoshinori Sekiguchi , Madoka Kawamura , Naoya Ono , Tetsuya Yabuuchi , Takahiro Oi , Yusuke Oka , Shoichi Kuroda , Fumito Uneuchi , Takeshi Koami
IPC分类号： C07D413/12 , C07D401/12 , C07D405/12 , C07D217/24
CPC分类号： C07D217/16 , C07D217/18 , C07D217/20 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D471/04
摘要： A compound represented by formula (I) or a pharmaceutically acceptable salt thereof has an effect of inhibiting CRTH2 and, therefore, is useful as a preventive or a remedy for allergic diseases such as asthma, atopic dermatitis and allergic rhinitis.
摘要翻译：由式（I）表示的化合物或其药学上可接受的盐具有抑制CRTH2的作用，因此可用作哮喘，特应性皮炎和过敏性鼻炎等过敏性疾病的预防或治疗。

9. 发明申请

US20110237791A1 2-PYRIDONE COMPOUNDS 有权
标题翻译： 2-吡啶酮化合物
公开(公告)号：US20110237791A1
公开(公告)日：2011-09-29
申请号：US13081201
申请日：2011-04-06
申请人： Takanori KAWAGUCHI , Kengo WATATANI , Keiko FUSEGI , Masahiro BOHNO , Hajime ASANUMA , Shoichi KURODA , Yudai IMAI , Tomomichi CHONAN , Nagaaki SATO , Shigeru TOKITA , Shigetada SASAKO , Takumi OKADA , Keishi HAYASHI , Shin ITOH , Noriko SAITO , Rui JIBIKI , Seishi ISHIYAMA , Hirofumi OTA
发明人： Takanori KAWAGUCHI , Kengo WATATANI , Keiko FUSEGI , Masahiro BOHNO , Hajime ASANUMA , Shoichi KURODA , Yudai IMAI , Tomomichi CHONAN , Nagaaki SATO , Shigeru TOKITA , Shigetada SASAKO , Takumi OKADA , Keishi HAYASHI , Shin ITOH , Noriko SAITO , Rui JIBIKI , Seishi ISHIYAMA , Hirofumi OTA
IPC分类号： C07D213/64 , C07D401/12 , C07D401/06 , C07D405/06 , C07D413/14
CPC分类号： C07D401/10 , C07D213/64 , C07D401/12 , C07D401/14 , C07D405/10 , C07D413/06 , C07D417/06 , C07D417/14
摘要： A 2-pyridone compound represented by the formula [1]: {wherein in the formula [1], the ring represented by A represents a benzene ring or a pyridine ring, X represents any of the structures represented by the formulas [3] shown below: V represents a single bond or a lower alkylene group, and W represents a single bond, an ether bond or a lower alkylene group (wherein the lower alkylene group may contain an ether bond)}, a tautomer or stereoisomer of the compound, a pharmaceutically acceptable salt thereof, or a solvate thereof is a compound that has an excellent GK activating effect and is useful as a pharmaceutical.
摘要翻译：由式[1]表示的2-吡啶酮化合物：其中，在式[1]中，由A表示的环表示苯环或吡啶环，X表示由式[3]表示的任何结构 V表示单键或低级亚烷基，W表示单键，醚键或低级亚烷基（其中低级亚烷基可以含有醚键）}，化合物的互变异构体或立体异构体，其药学上可接受的盐或其溶剂合物是具有优异的GK活化作用并可用作药物的化合物。

10. 发明申请

US20100298557A1 PYRAZOLOPYRIMIDINE COMPOUND 审中-公开
标题翻译：吡唑并嘧啶化合物
公开(公告)号：US20100298557A1
公开(公告)日：2010-11-25
申请号：US12521518
申请日：2007-12-28
申请人： Makoto Yagi , Hiroki Umemiya , Hajime Asanuma , Yusuke Oka , Rie Nishikawa , Keisi Hayashi , Takumi Okada , Takanori Shimizu , Shigetada Sasako
发明人： Makoto Yagi , Hiroki Umemiya , Hajime Asanuma , Yusuke Oka , Rie Nishikawa , Keisi Hayashi , Takumi Okada , Takanori Shimizu , Shigetada Sasako
IPC分类号： C07D487/04 , C07D491/113 , C07D498/04
CPC分类号： C07D487/04 , C07D519/00
摘要： Disclosed is a novel compound having Syk and/or Abl inhibitory activities, which is useful for prevention/treatment of allergic diseases, autoimmune diseases, arthritides and cancers. Specifically disclosed is a pyrazolopyrimidine compound represented by the formula [I] or [III] below, a tautomer thereof, a stereoisomer thereof, a pharmaceutically acceptable salt thereof, or a solvent of any of them.
摘要翻译：公开了具有Syk和/或Abl抑制活性的新化合物，其可用于预防/治疗过敏性疾病，自身免疫性疾病，关节炎和癌症。具体公开的是由下式[I]或[III]表示的吡唑并嘧啶化合物，其互变异构体，其立体异构体，其药学上可接受的盐或其任何溶剂。

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