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1.
公开(公告)号:US20070004643A1
公开(公告)日:2007-01-04
申请号:US10582015
申请日:2004-12-08
CPC分类号: C07D213/30 , C07C271/22 , C07C2601/02 , C07C2601/04 , C07C2602/08 , C07D295/215 , C07D307/20 , C07D309/12
摘要: The present invention provides a compound represented by the formula (I): (wherein R1 is a lower alkyl substituted by a lower alkoxy or a heterocyclic group, or a heterocyclic group; R2 is a lower alkyl optionally substituted by a phenyl; and R3 is a lower alkyl optionally substituted by a halogen, a lower alkoxy or a phenyl, or a fused polycyclic hydrocarbon group), which is well absorbed orally, exhibits durability of good blood level and has potent calpain inhibitory activity.
摘要翻译: 本发明提供由式(I)表示的化合物:其中R 1是被低级烷氧基或杂环基或杂环基取代的低级烷基; R 2, / SUP>是任选被苯基取代的低级烷基; R 3是任选被卤素,低级烷氧基或苯基或稠合多环烃基取代的低级烷基,其是 良好的口腔吸收,具有良好的血液水平的耐久性,并具有强大的钙蛋白酶抑制活性。
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2.
公开(公告)号:US07491705B2
公开(公告)日:2009-02-17
申请号:US10582015
申请日:2004-12-08
IPC分类号: A61K38/05
CPC分类号: C07D213/30 , C07C271/22 , C07C2601/02 , C07C2601/04 , C07C2602/08 , C07D295/215 , C07D307/20 , C07D309/12
摘要: The present invention provides a compound represented by the formula (I): (wherein R1 is a lower alkyl substituted by a lower alkoxy or a heterocyclic group, or a heterocyclic group; R2 is a lower alkyl optionally substituted by a phenyl; and R3 is a lower alkyl optionally substituted by a halogen, a lower alkoxy or a phenyl, or a fused polycyclic hydrocarbon group), which is well absorbed orally, exhibits durability of good blood level and has potent calpain inhibitory activity.
摘要翻译: 本发明提供由式(I)表示的化合物:其中R1是被低级烷氧基或杂环基取代的低级烷基或杂环基; R2是任意被苯基取代的低级烷基,R3是 被卤素,低级烷氧基或苯基或稠合多环烃基任选取代的低级烷基),其口服良好吸收,具有良好的血液水平的耐久性,并具有有效的钙蛋白酶抑制活性。
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公开(公告)号:US09035059B2
公开(公告)日:2015-05-19
申请号:US14004950
申请日:2012-03-14
申请人: Tsuyoshi Busujima , Takahiro Oi , Hiroaki Tanaka , Yoshihisa Shirasaki , Kanako Iwakiri , Nagaaki Sato , Shigeru Tokita
发明人: Tsuyoshi Busujima , Takahiro Oi , Hiroaki Tanaka , Yoshihisa Shirasaki , Kanako Iwakiri , Nagaaki Sato , Shigeru Tokita
IPC分类号: C07D401/14 , C07D209/44 , C07D217/04 , C07D223/16 , C07D405/12 , C07D409/06 , C07D413/06 , C07D417/10 , A61K31/4035 , A61K31/454 , A61K31/472 , A61K31/497 , C07D217/18 , C07D217/06 , C07D217/22 , C07D401/06 , C07D401/10 , C07D401/12 , C07D403/12 , C07D405/06 , C07D413/12 , C07D417/06 , A61K9/16 , A61K9/20 , A61K9/48 , C07D217/20 , C07D217/26 , C07D405/14 , C07D409/14 , C07D417/12 , C07D417/14 , C07D495/04 , C07D217/10 , C07D401/08
CPC分类号: C07D217/18 , A61K9/1623 , A61K9/2018 , A61K9/4858 , C07D209/44 , C07D217/04 , C07D217/06 , C07D217/10 , C07D217/20 , C07D217/22 , C07D217/26 , C07D223/16 , C07D401/06 , C07D401/08 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/14 , C07D413/06 , C07D413/12 , C07D417/06 , C07D417/10 , C07D417/12 , C07D417/14 , C07D495/04
摘要: There are provided compounds represented by the following general formula (I) or pharmaceutically acceptable salts of thereof, which have a superior monoacylglycerol acyltransferase 2 inhibitory action: wherein Ring A represents a partially saturated heteroaryl group, an aryl group or a heteroaryl group, RB represents a C4-18 alkyl group, a C3-8 cycloalkyl group, a partially saturated aryl group, an aryl group, or the following formula (II): wherein V represents the formula —CR11R12—, —CO—, —CO—O—, or —CO—NH—, W represents a single bond or a C1-3 alkylene group, and Ring B represents a C3-8 cycloalkyl group, a C3-8 cycloalkenyl group, a partially saturated heteroaryl group, a saturated heterocyclyl group, an aryl group, or a heteroaryl group, Y represents a nitrogen atom or the formula N+(RF), RF represents a C1-4 alkyl group, and m and n, which may be the same or different, each represent an integer of 0 or 1.
摘要翻译: 提供具有优异的单酰基甘油酰基转移酶2抑制作用的由以下通式(I)表示的化合物或其药学上可接受的盐:其中环A表示部分饱和的杂芳基,芳基或杂芳基,RB表示 C4-18烷基,C3-8环烷基,部分饱和芳基,芳基或下式(Ⅱ)表示:其中V表示式-CR11R12-,-CO-,-CO-O- 或-CO-NH-,W表示单键或C1-3亚烷基,环B表示C3-8环烷基,C3-8环烯基,部分饱和杂芳基,饱和杂环基, 芳基或杂芳基,Y表示氮原子或式N +(RF),RF表示C1-4烷基,m和n可相同或不同,分别表示0以上的整数 或1。
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公开(公告)号:US20120010414A1
公开(公告)日:2012-01-12
申请号:US13257258
申请日:2010-03-19
申请人: Akito Yasuhara , Shuji Yamamoto , Hiroshi Ohta , Yoshihisa Shirasaki , Kazunari Sakagami , Masato Hayashi , Tsuyoshi Shibata , Youichi Shimazaki , Yuko Araki , Kumi Abe , Xiang-Min Sun
发明人: Akito Yasuhara , Shuji Yamamoto , Hiroshi Ohta , Yoshihisa Shirasaki , Kazunari Sakagami , Masato Hayashi , Tsuyoshi Shibata , Youichi Shimazaki , Yuko Araki , Kumi Abe , Xiang-Min Sun
IPC分类号: C07D471/04 , C07D405/12 , C07D409/12 , C07D405/14
CPC分类号: C07D471/04 , C07D405/12 , C07D405/14 , C07D409/12
摘要: The present invention aims to provide novel compounds of formula [I] or pharmaceutically acceptable salts thereof that are based on a glycine uptake inhibiting action and which are useful in the prevention or treatment of such diseases as schizophrenia, Alzheimer's disease, cognitive dysfunction, dementia, anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsory disorder, social anxiety disorder, posttraumatic stress disorder, specific phobia, acute stress disorder, etc.), depression, drug addiction, spasm, tremor, and sleep disorder:
摘要翻译: 本发明旨在提供基于甘氨酸摄取抑制作用的新颖的式[I]化合物或其药学上可接受的盐,其可用于预防或治疗精神分裂症,阿尔茨海默病,认知功能障碍,痴呆, 焦虑症(广泛性焦虑障碍,恐慌症,强迫症,社会焦虑症,创伤后应激障碍,特定恐惧症,急性应激障碍等),抑郁症,药物成瘾,痉挛,震颤和睡眠障碍:
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公开(公告)号:US20140005382A1
公开(公告)日:2014-01-02
申请号:US14004950
申请日:2012-03-14
申请人: Tsuyoshi Busujima , Takahiro Oi , Hiroaki Tanaka , Yoshihisa Shirasaki , Kanako Iwakiri , Nagaaki Sato , Shigeru Tokita
发明人: Tsuyoshi Busujima , Takahiro Oi , Hiroaki Tanaka , Yoshihisa Shirasaki , Kanako Iwakiri , Nagaaki Sato , Shigeru Tokita
IPC分类号: C07D217/18 , C07D401/06 , C07D417/06 , C07D405/14 , C07D405/06 , C07D401/10 , C07D401/12 , C07D417/10 , C07D405/12 , C07D417/14 , C07D409/06 , C07D413/06 , C07D409/14 , C07D495/04 , C07D413/12 , C07D417/12 , C07D217/26 , C07D403/12 , C07D217/20 , C07D209/44
CPC分类号: C07D217/18 , A61K9/1623 , A61K9/2018 , A61K9/4858 , C07D209/44 , C07D217/04 , C07D217/06 , C07D217/10 , C07D217/20 , C07D217/22 , C07D217/26 , C07D223/16 , C07D401/06 , C07D401/08 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/14 , C07D413/06 , C07D413/12 , C07D417/06 , C07D417/10 , C07D417/12 , C07D417/14 , C07D495/04
摘要: There are provided compounds represented by the following general formula (I) or pharmaceutically acceptable salts of thereof, which have a superior monoacylglycerol acyltransferase 2 inhibitory action: wherein Ring A represents a partially saturated heteroaryl group, an aryl group or a heteroaryl group, RB represents a C4-18 alkyl group, a C3-8 cycloalkyl group, a partially saturated aryl group, an aryl group, or the following formula (II): wherein V represents the formula —CR11R12—, —CO—, —CO—O—, or —CO—NH—, W represents a single bond or a C1-3 alkylene group, and Ring B represents a C3-8 cycloalkyl group, a C3-8 cycloalkenyl group, a partially saturated heteroaryl group, a saturated heterocyclyl group, an aryl group, or a heteroaryl group, Y represents a nitrogen atom or the formula N+(RF), RF represents a C1-4 alkyl group, and m and n, which may be the same or different, each represent an integer of 0 or 1.
摘要翻译: 提供具有优异的单酰基甘油酰基转移酶2抑制作用的由以下通式(I)表示的化合物或其药学上可接受的盐:其中环A表示部分饱和的杂芳基,芳基或杂芳基,RB表示 C4-18烷基,C3-8环烷基,部分饱和芳基,芳基或下式(Ⅱ)表示:其中V表示式-CR11R12-,-CO-,-CO-O- 或-CO-NH-,W表示单键或C1-3亚烷基,环B表示C3-8环烷基,C3-8环烯基,部分饱和杂芳基,饱和杂环基, 芳基或杂芳基,Y表示氮原子或式N +(RF),RF表示C1-4烷基,m和n可相同或不同,分别表示0以上的整数 或1。
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公开(公告)号:US20120116095A1
公开(公告)日:2012-05-10
申请号:US13383513
申请日:2010-07-15
申请人: Akito Yasuhara , Kazunari Sakagami , Hiroshi Ohta , Masato Hayashi , Yoshihisa Shirasaki , Shuji Yamamoto , Youichi Shimazaki , Yuko Araki , Kumi Abe , Xiang-Min Sun
发明人: Akito Yasuhara , Kazunari Sakagami , Hiroshi Ohta , Masato Hayashi , Yoshihisa Shirasaki , Shuji Yamamoto , Youichi Shimazaki , Yuko Araki , Kumi Abe , Xiang-Min Sun
IPC分类号: C07D249/12 , C07D233/14
CPC分类号: C07D249/10
摘要: The present invention aims to provide novel compounds represented by formula [I] or pharmaceutically acceptable salts thereof: which are useful for prevention or treatment of diseases such as schizophrenia, Alzheimer's disease, cognitive impairment, dementia, anxiety disorders (e.g., generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, post-traumatic stress disorder, specific phobias, acute stress disorder), depression, drug dependence, convulsion, tremor, pain, or sleep disorders, based on their inhibitory effect against glycine uptake.
摘要翻译: 本发明旨在提供由式[I]表示的新化合物或其药学上可接受的盐:其可用于预防或治疗诸如精神分裂症,阿尔茨海默病,认知障碍,痴呆,焦虑症(例如广泛性焦虑症, 基于它们对甘氨酸摄取的抑制效果,恐慌症,强迫症,社交焦虑症,创伤后应激障碍,特异性恐惧症,急性应激障碍),抑郁症,药物依赖性,惊厥,震颤,疼痛或睡眠障碍。
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公开(公告)号:US09181229B2
公开(公告)日:2015-11-10
申请号:US14004997
申请日:2012-03-15
申请人: Naoya Ono , Shoichi Kuroda , Yoshihisa Shirasaki , Tetsuo Takayama , Yoshinori Sekiguchi , Fumihito Ushiyama , Yusuke Oka
发明人: Naoya Ono , Shoichi Kuroda , Yoshihisa Shirasaki , Tetsuo Takayama , Yoshinori Sekiguchi , Fumihito Ushiyama , Yusuke Oka
IPC分类号: C07D413/04 , C07D403/04 , C07D417/04 , C07D413/14
CPC分类号: C07D413/04 , C07D403/04 , C07D413/14 , C07D417/04
摘要: Provided are novel compounds that bind to FKBP12 or pharmaceutically acceptable salts thereof, as well as new therapeutics useful in the prevention or treatment of alopecia which comprise those compounds or pharmaceutically acceptable salts thereof. Specifically, compounds represented by formula (1) [where R1 represents either the following formula (2) or (3)] or pharmaceutically acceptable salts thereof are provided.
摘要翻译: 提供与FKBP12或其药学上可接受的盐结合的新化合物,以及可用于预防或治疗脱发的新治疗剂,其包含那些化合物或其药学上可接受的盐。 具体地,提供由式(1)表示的化合物[其中R 1表示下式(2)或(3)]或其药学上可接受的盐。
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公开(公告)号:US08623898B2
公开(公告)日:2014-01-07
申请号:US13257258
申请日:2010-03-19
申请人: Akito Yasuhara , Shuji Yamamoto , Hiroshi Ohta , Yoshihisa Shirasaki , Kazunari Sakagami , Masato Hayashi , Tsuyoshi Shibata , Youichi Shimazaki , Yuko Araki , Kumi Abe , Xiang-Min Sun
发明人: Akito Yasuhara , Shuji Yamamoto , Hiroshi Ohta , Yoshihisa Shirasaki , Kazunari Sakagami , Masato Hayashi , Tsuyoshi Shibata , Youichi Shimazaki , Yuko Araki , Kumi Abe , Xiang-Min Sun
IPC分类号: C07D471/04 , C07D405/12 , C07D409/12 , C07D405/14 , A01N43/64 , A01N43/50 , A61K31/41
CPC分类号: C07D471/04 , C07D405/12 , C07D405/14 , C07D409/12
摘要: The present invention aims to provide novel compounds of formula [I] or pharmaceutically acceptable salts thereof that are based on a glycine uptake inhibiting action and which are useful in the prevention or treatment of such diseases as schizophrenia, Alzheimer's disease, cognitive dysfunction, dementia, anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsory disorder, social anxiety disorder, posttraumatic stress disorder, specific phobia, acute stress disorder, etc.), depression, drug addiction, spasm, tremor, and sleep disorder:
摘要翻译: 本发明旨在提供基于甘氨酸摄取抑制作用的新颖的式[I]化合物或其药学上可接受的盐,其可用于预防或治疗精神分裂症,阿尔茨海默病,认知功能障碍,痴呆, 焦虑症(广泛性焦虑障碍,恐慌症,强迫症,社会焦虑症,创伤后应激障碍,特定恐惧症,急性应激障碍等),抑郁症,药物成瘾,痉挛,震颤和睡眠障碍:
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公开(公告)号:US20130345419A1
公开(公告)日:2013-12-26
申请号:US14004997
申请日:2012-03-15
申请人: Naoya Ono , Shoichi Kuroda , Yoshihisa Shirasaki , Tetsuo Takayama , Yoshinori Sekiguchi , Fumihito Ushiyama , Yusuke Oka
发明人: Naoya Ono , Shoichi Kuroda , Yoshihisa Shirasaki , Tetsuo Takayama , Yoshinori Sekiguchi , Fumihito Ushiyama , Yusuke Oka
IPC分类号: C07D413/04 , C07D403/04 , C07D417/04 , C07D413/14
CPC分类号: C07D413/04 , C07D403/04 , C07D413/14 , C07D417/04
摘要: Provided are novel compounds that bind to FKBP12 or pharmaceutically acceptable salts thereof, as well as new therapeutics useful in the prevention or treatment of alopecia which comprise those compounds or pharmaceutically acceptable salts thereof. Specifically, compounds represented by formula (1) [where R1 represents either the following formula (2) or (3)] or pharmaceutically acceptable salts thereof are provided.
摘要翻译: 提供与FKBP12或其药学上可接受的盐结合的新化合物,以及可用于预防或治疗脱发的新治疗剂,其包含那些化合物或其药学上可接受的盐。 具体地,提供由式(1)表示的化合物[其中R 1表示下式(2)或(3)]或其药学上可接受的盐。
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