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公开(公告)号:US08642626B2
公开(公告)日:2014-02-04
申请号:US13812437
申请日:2011-07-29
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
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
IPC分类号: A61K31/4439 , A61K31/415 , C07D231/12 , C07D231/20 , C07D231/38 , C07D403/06 , C07D401/06
CPC分类号: C07D231/12 , C07D231/14 , C07D231/20 , C07D231/38 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D403/04 , C07D403/06 , C07D413/04
摘要: Provided is a novel compound represented by formula [I] or a pharmaceutically acceptable salt thereof having antagonistic activity against group II metabolism-type glutamic acid (m-Glu) receptors. The compound or pharmaceutically acceptable salt thereof is useful as a prophylactic or therapeutic agent for diseases such as new mood disorders (depressive and bipolar disorders), anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, post-traumatic stress disorder, specific phobias, and acute stress disorder), schizophrenia, Alzheimer's disease, cognitive dysfunction, dementia, drug dependence, convulsions, tremors, pain, sleep disorders, and the like.
摘要翻译: 本发明提供由式[I]表示的新化合物或其对II类代谢型谷氨酸(m-Glu)受体具有拮抗作用的药学上可接受的盐。 化合物或其药学上可接受的盐可用作疾病的预防或治疗剂,例如新的情绪障碍(抑郁和双相性精神障碍),焦虑症(广泛性焦虑症,惊恐障碍,强迫症,社会焦虑症, 创伤性应激障碍,特异性恐惧症和急性应激障碍),精神分裂症,阿尔茨海默病,认知功能障碍,痴呆,药物依赖,惊厥,震颤,疼痛,睡眠障碍等。
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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。
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公开(公告)号:US20130123500A1
公开(公告)日:2013-05-16
申请号:US13812437
申请日:2011-07-29
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
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
IPC分类号: C07D231/12 , C07D231/20 , C07D231/38 , C07D403/06 , C07D401/06
CPC分类号: C07D231/12 , C07D231/14 , C07D231/20 , C07D231/38 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D403/04 , C07D403/06 , C07D413/04
摘要: Provided is a novel compound represented by formula [I] or a pharmaceutically acceptable salt thereof having antagonistic activity against group II metabolism-type glutamic acid (m-Glu) receptors. The compound or pharmaceutically acceptable salt thereof is useful as a prophylactic or therapeutic agent for diseases such as new mood disorders (depressive and bipolar disorders), anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, post-traumatic stress disorder, specific phobias, and acute stress disorder), schizophrenia, Alzheimer's disease, cognitive dysfunction, dementia, drug dependence, convulsions, tremors, pain, sleep disorders, and the like.
摘要翻译: 本发明提供由式[I]表示的新化合物或其对II类代谢型谷氨酸(m-Glu)受体具有拮抗作用的药学上可接受的盐。 化合物或其药学上可接受的盐可用作疾病的预防或治疗剂,例如新的情绪障碍(抑郁和双相性精神障碍),焦虑症(广泛性焦虑症,惊恐障碍,强迫症,社会焦虑症, 创伤性应激障碍,特异性恐惧症和急性应激障碍),精神分裂症,阿尔茨海默病,认知功能障碍,痴呆,药物依赖,惊厥,震颤,疼痛,睡眠障碍等。
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公开(公告)号:US20110065667A1
公开(公告)日:2011-03-17
申请号:US12951964
申请日:2010-11-22
申请人: Toshio NAKAMURA , Makoto Tatsuzuki , Dai Nozawa , Tomoko Tamita , Seiji Masuda , Hiroshi Ohta , Shuhei Kashiwa , Aya Fujino , Shigeyuki Chaki , Toshiharu Shimazaki
发明人: Toshio NAKAMURA , Makoto Tatsuzuki , Dai Nozawa , Tomoko Tamita , Seiji Masuda , Hiroshi Ohta , Shuhei Kashiwa , Aya Fujino , Shigeyuki Chaki , Toshiharu Shimazaki
IPC分类号: A61K31/695 , C07D231/10 , C07D413/12 , C07D281/06 , C07F7/10 , A61K31/415 , A61K31/5377 , A61K31/553 , A61P25/28 , A61P25/18 , A61P3/10 , A61P25/24 , A61P25/08 , A61P25/00
CPC分类号: C07D231/14 , C07D231/40 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D403/14 , C07D413/04 , C07D413/14
摘要: The present invention provides a prophylactic or therapeutic agent for dementia, Alzheimer's disease, attention-deficit hyperactivity disorder, schizophrenia, eating disorders, obesity, diabetes, hyperlipidemia, sleep disorders, narcolepsy, sleep apnea syndrome, circadian rhythm disorder, depression, allergic rhinitis or other diseases.A phenylpyrazole derivative represented by formula (1) or a pharmaceutically acceptable salt thereof: {wherein R1 and R2, which may be the same or different, each represent C1-C6 alkyl or C3-C8 cycloalkyl, or R1 and R2 are attached to each other together with their adjacent nitrogen atom to form a 4- to 7-membered saturated heterocyclic ring (wherein said saturated heterocyclic ring may be substituted with halogen or C1-C6 alkyl), n represents an integer of 0 to 2, T represents a hydrogen atom, halogen or C1-C6 alkyl, and R represents formula (I): or the like}.
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公开(公告)号:US08183387B2
公开(公告)日:2012-05-22
申请号:US12951964
申请日:2010-11-22
申请人: Toshio Nakamura , Makoto Tatsuzuki , Dai Nozawa , Tomoko Tamita , Seiji Masuda , Hiroshi Ohta , Shuhei Kashiwa , Aya Fujino , Shigeyuki Chaki , Toshiharu Shimazaki
发明人: Toshio Nakamura , Makoto Tatsuzuki , Dai Nozawa , Tomoko Tamita , Seiji Masuda , Hiroshi Ohta , Shuhei Kashiwa , Aya Fujino , Shigeyuki Chaki , Toshiharu Shimazaki
IPC分类号: C07D231/10
CPC分类号: C07D231/14 , C07D231/40 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D403/14 , C07D413/04 , C07D413/14
摘要: The present invention provides a prophylactic or therapeutic agent for dementia, Alzheimer's disease, attention-deficit hyperactivity disorder, schizophrenia, eating disorders, obesity, diabetes, hyperlipidemia, sleep disorders, narcolepsy, sleep apnea syndrome, circadian rhythm disorder, depression, allergic rhinitis or other diseases.A phenylpyrazole derivative represented by formula (1) or a pharmaceutically acceptable salt thereof: {wherein R1 and R2, which may be the same or different, each represent C1-C6 alkyl or C3-C8 cycloalkyl, or R1 and R2 are attached to each other together with their adjacent nitrogen atom to form a 4- to 7-membered saturated heterocyclic ring (wherein said saturated heterocyclic ring may be substituted with halogen or C1-C6 alkyl), n represents an integer of 0 to 2, T represents a hydrogen atom, halogen or C1-C6 alkyl, and R represents formula (I): or the like}.
摘要翻译: 本发明提供了用于痴呆,阿尔茨海默病,注意缺陷多动障碍,精神分裂症,进食障碍,肥胖症,糖尿病,高脂血症,睡眠障碍,发作性睡眠障碍,睡眠呼吸暂停综合征,昼夜节律紊乱,抑郁,过敏性鼻炎或 其他疾病 由式(1)表示的苯基吡唑衍生物或其药学上可接受的盐:其中可以相同或不同的R 1和R 2各自表示C 1 -C 6烷基或C 3 -C 8环烷基,或者R 1和R 2各自连接 与其相邻的氮原子一起形成4-至7-元饱和杂环(其中所述饱和杂环可被卤素或C 1 -C 6烷基取代),n表示0至2的整数,T表示氢 原子,卤素或C 1 -C 6烷基,R表示式(I):等)。
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公开(公告)号:US20100267687A1
公开(公告)日:2010-10-21
申请号:US12741754
申请日:2008-11-13
申请人: Toshio Nakamura , Makoto Tatsuzuki , Dai Nozawa , Tomoko Tamita , Seiji Masuda , Hiroshi Ohta , Shuhei Kashiwa , Aya Fujino , Shigeyuki Chaki , Toshiharu Shimazaki
发明人: Toshio Nakamura , Makoto Tatsuzuki , Dai Nozawa , Tomoko Tamita , Seiji Masuda , Hiroshi Ohta , Shuhei Kashiwa , Aya Fujino , Shigeyuki Chaki , Toshiharu Shimazaki
IPC分类号: A61K31/4155 , C07D403/12 , A61P25/28 , A61P25/18 , A61P25/08 , A61P3/04 , A61P3/10 , A61P3/06 , C07D413/14 , A61K31/5377 , C07D231/14 , C07D401/14 , A61K31/4439 , A61K31/422 , A61K31/454 , A61K31/553 , C07D403/14 , A61K31/496
CPC分类号: C07D231/14 , C07D231/40 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D403/14 , C07D413/04 , C07D413/14
摘要: The present invention provides a prophylactic or therapeutic agent for dementia, Alzheimer's disease, attention-deficit hyperactivity disorder, schizophrenia, eating disorders, obesity, diabetes, hyperlipidemia, sleep disorders, narcolepsy, sleep apnea syndrome, circadian rhythm disorder, depression, allergic rhinitis or other diseases.A phenylpyrazole derivative represented by formula (1) or a pharmaceutically acceptable salt thereof: {wherein R1 and R2, which may be the same or different, each represent C1-C6 alkyl or C3-C8 cycloalkyl, or R1 and R2 are attached to each other together with their adjacent nitrogen atom to form a 4- to 7-membered saturated heterocyclic ring (wherein said saturated heterocyclic ring may be substituted with halogen or C1-C6 alkyl), n represents an integer of 0 to 2, T represents a hydrogen atom, halogen or C1-C6 alkyl, and R represents formula (I): or the like}.
摘要翻译: 本发明提供了用于痴呆,阿尔茨海默病,注意缺陷多动障碍,精神分裂症,进食障碍,肥胖症,糖尿病,高脂血症,睡眠障碍,发作性睡眠障碍,睡眠呼吸暂停综合征,昼夜节律紊乱,抑郁,过敏性鼻炎或 其他疾病 由式(1)表示的苯基吡唑衍生物或其药学上可接受的盐:其中可以相同或不同的R 1和R 2各自表示C 1 -C 6烷基或C 3 -C 8环烷基,或者R 1和R 2各自连接 与其相邻的氮原子一起形成4-至7-元饱和杂环(其中所述饱和杂环可被卤素或C 1 -C 6烷基取代),n表示0至2的整数,T表示氢 原子,卤素或C 1 -C 6烷基,R表示式(I):等)。
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公开(公告)号:US08193176B2
公开(公告)日:2012-06-05
申请号:US12951978
申请日:2010-11-22
申请人: Toshio Nakamura , Makoto Tatsuzuki , Dai Nozawa , Tomoko Tamita , Seiji Masuda , Hiroshi Ohta , Shuhei Kashiwa , Aya Fujino , Shigeyuki Chaki , Toshiharu Shimazaki
发明人: Toshio Nakamura , Makoto Tatsuzuki , Dai Nozawa , Tomoko Tamita , Seiji Masuda , Hiroshi Ohta , Shuhei Kashiwa , Aya Fujino , Shigeyuki Chaki , Toshiharu Shimazaki
IPC分类号: A61K31/5377 , A61K31/4155 , A61K31/397 , A61K31/553 , A61K31/496
CPC分类号: C07D231/14 , C07D231/40 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D403/14 , C07D413/04 , C07D413/14
摘要: The present invention provides a prophylactic or therapeutic agent for dementia, Alzheimer's disease, attention-deficit hyperactivity disorder, schizophrenia, eating disorders, obesity, diabetes, hyperlipidemia, sleep disorders, narcolepsy, sleep apnea syndrome, circadian rhythm disorder, depression, allergic rhinitis or other diseases.A phenylpyrazole derivative represented by formula (1) or a pharmaceutically acceptable salt thereof: {wherein R1 and R2, which may be the same or different, each represent C1-C6 alkyl or C3-C8 cycloalkyl, or R1 and R2 are attached to each other together with their adjacent nitrogen atom to form a 4- to 7-membered saturated heterocyclic ring (wherein said saturated heterocyclic ring may be substituted with halogen or C1-C6 alkyl), n represents an integer of 0 to 2, T represents a hydrogen atom, halogen or C1-C6 alkyl, and R represents formula (I): or the like}.
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公开(公告)号:US20110065668A1
公开(公告)日:2011-03-17
申请号:US12951978
申请日:2010-11-22
申请人: Toshio NAKAMURA , Makoto Tatsuzuki , Dai Nozawa , Tomoko Tamita , Seiji Masuda , Hiroshi Ohta , Shuhei Kashiwa , Aya Fujino , Shigeyuki Chaki , Toshiharu Shimazaki
发明人: Toshio NAKAMURA , Makoto Tatsuzuki , Dai Nozawa , Tomoko Tamita , Seiji Masuda , Hiroshi Ohta , Shuhei Kashiwa , Aya Fujino , Shigeyuki Chaki , Toshiharu Shimazaki
IPC分类号: A61K31/695 , A61K31/415 , A61K31/5377 , A61K31/553 , A61P25/28 , A61P25/18 , A61P3/10 , A61P25/24 , A61P25/08 , A61P25/00
CPC分类号: C07D231/14 , C07D231/40 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D403/14 , C07D413/04 , C07D413/14
摘要: The present invention provides a prophylactic or therapeutic agent for dementia, Alzheimer's disease, attention-deficit hyperactivity disorder, schizophrenia, eating disorders, obesity, diabetes, hyperlipidemia, sleep disorders, narcolepsy, sleep apnea syndrome, circadian rhythm disorder, depression, allergic rhinitis or other diseases.A phenylpyrazole derivative represented by formula (1) or a pharmaceutically acceptable salt thereof: {wherein R1 and R2, which may be the same or different, each represent C1-C6 alkyl or C3-C8 cycloalkyl, or R1 and R2 are attached to each other together with their adjacent nitrogen atom to form a 4- to 7-membered saturated heterocyclic ring (wherein said saturated heterocyclic ring may be substituted with halogen or C1-C6 alkyl), n represents an integer of 0 to 2, T represents a hydrogen atom, halogen or C1-C6 alkyl, and R represents formula (I): or the like}.
摘要翻译: 本发明提供了用于痴呆,阿尔茨海默病,注意缺陷多动障碍,精神分裂症,进食障碍,肥胖症,糖尿病,高脂血症,睡眠障碍,发作性睡眠障碍,睡眠呼吸暂停综合征,昼夜节律紊乱,抑郁,过敏性鼻炎或 其他疾病 由式(1)表示的苯基吡唑衍生物或其药学上可接受的盐:其中可以相同或不同的R 1和R 2各自表示C 1 -C 6烷基或C 3 -C 8环烷基,或者R 1和R 2各自连接 与其相邻的氮原子一起形成4-至7-元饱和杂环(其中所述饱和杂环可被卤素或C 1 -C 6烷基取代),n表示0至2的整数,T表示氢 原子,卤素或C 1 -C 6烷基,R表示式(I):等)。
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公开(公告)号:US07888354B2
公开(公告)日:2011-02-15
申请号:US12741754
申请日:2008-11-13
申请人: Toshio Nakamura , Makoto Tatsuzuki , Dai Nozawa , Tomoko Tamita , Seiji Masuda , Hiroshi Ohta , Shuhei Kashiwa , Aya Fujino , Shigeyuki Chaki , Toshiharu Shimazaki
发明人: Toshio Nakamura , Makoto Tatsuzuki , Dai Nozawa , Tomoko Tamita , Seiji Masuda , Hiroshi Ohta , Shuhei Kashiwa , Aya Fujino , Shigeyuki Chaki , Toshiharu Shimazaki
IPC分类号: A61K31/5377 , A61K31/397 , A61K31/495 , A61K31/4155 , C07D413/14 , C07D403/14 , C07D205/02 , C07D231/10
CPC分类号: C07D231/14 , C07D231/40 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D403/14 , C07D413/04 , C07D413/14
摘要: The present invention provides a prophylactic or therapeutic agent for dementia, Alzheimer's disease, attention-deficit hyperactivity disorder, schizophrenia, eating disorders, obesity, diabetes, hyperlipidemia, sleep disorders, narcolepsy, sleep apnea syndrome, circadian rhythm disorder, depression, allergic rhinitis or other diseases.A phenylpyrazole derivative represented by formula (1) or a pharmaceutically acceptable salt thereof: {wherein R1 and R2, which may be the same or different, each represent C1-C6 alkyl or C3-C8 cycloalkyl, or R1 and R2 are attached to each other together with their adjacent nitrogen atom to form a 4- to 7-membered saturated heterocyclic ring (wherein said saturated heterocyclic ring may be substituted with halogen or C1-C6 alkyl), n represents an integer of 0 to 2, T represents a hydrogen atom, halogen or C1-C6 alkyl, and R represents formula (I): or the like}.
摘要翻译: 本发明提供了用于痴呆,阿尔茨海默病,注意缺陷多动障碍,精神分裂症,进食障碍,肥胖症,糖尿病,高脂血症,睡眠障碍,发作性睡眠障碍,睡眠呼吸暂停综合征,昼夜节律紊乱,抑郁,过敏性鼻炎或 其他疾病 由式(1)表示的苯基吡唑衍生物或其药学上可接受的盐:其中可以相同或不同的R 1和R 2各自表示C 1 -C 6烷基或C 3 -C 8环烷基,或者R 1和R 2各自连接 与其相邻的氮原子一起形成4-至7-元饱和杂环(其中所述饱和杂环可被卤素或C 1 -C 6烷基取代),n表示0至2的整数,T表示氢 原子,卤素或C 1 -C 6烷基,R表示式(I):等)。
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公开(公告)号:US08609847B2
公开(公告)日:2013-12-17
申请号:US13144591
申请日:2010-02-05
申请人: Toshio Nakamura , Seiji Masuda , Aya Futamura
发明人: Toshio Nakamura , Seiji Masuda , Aya Futamura
IPC分类号: C07D215/38
CPC分类号: C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , C07D471/04
摘要: The present invention provides a prophylactic or therapeutic agent for dementia, Alzheimer's disease, attention-deficit hyperactivity disorder, schizophrenia, eating disorders, obesity, diabetes, hyperlipidemia, sleep disorders, narcolepsy, sleep apnea syndrome, circadian rhythm disorder, depression, allergic rhinitis or other diseases.A dihydroquinolinone derivative represented by formula (1) or a pharmaceutically acceptable salt thereof: {wherein Q represents the following formula (A) or (B)}
摘要翻译: 本发明提供了用于痴呆,阿尔茨海默病,注意缺陷多动障碍,精神分裂症,进食障碍,肥胖,糖尿病,高脂血症,睡眠障碍,发作性睡眠障碍,睡眠呼吸暂停综合征,昼夜节律紊乱,抑郁,过敏性鼻炎或 其他疾病 由式(1)表示的二氢喹啉酮衍生物或其药学上可接受的盐:其中Q表示下式(A)或(B)}
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