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    • 1. 发明授权
    • Piperidine derivative
    • 哌啶衍生物
    • US07834182B2
    • 2010-11-16
    • US12381099
    • 2009-03-06
    • Norikazu OhtakeRyo YoshimotoShigeru TokitaAkio KanataniSayaka Mizutani
    • Norikazu OhtakeRyo YoshimotoShigeru TokitaAkio KanataniSayaka Mizutani
    • C07D401/14C07D403/14A61K31/4545A61K31/496A61K31/454A61K31/4523A61K31/506A61P3/04A61P3/10C07D401/12C07D401/02C07D401/06
    • C07D211/58A61K31/454
    • Provided are a histamine-H3 receptor antagonist; and a preventive and/or a remedy for metabolic system diseases such as obesity, diabetes, hormone secretion disorder, hyperlipemia, gout, fatty liver, circulatory system diseases, for example, stenocardia, acute/congestive cardiac insufficiency, cardiac infarction, coronary arteriosclerosis, hypertension, nephropathy, sleep disorder and various diseases accompanied by sleep disorder such as idiopathic hypersomnia, repetitive hypersomnia, true hypersomnia, narcolepsy, sleep periodic acromotion disorder, sleep apnea syndrome, circadian rhythm disorder, chronic fatigue syndrome, REM sleep disorder, senile insomnia, night worker sleep insanitation, idiopathic insomnia, repetitive insomnia, true insomnia, electrolyte metabolism disorder; and central and peripheral nervous system diseases such as bulimia, emotional disorder, melancholia, anxiety, epilepsy, delirium, dementia, shinzophrenia, attention deficit/hyperactivity disorder, memory disorder, Alzheimer's disease, Parkinson's disease, sleep disorder, recognition disorder, motion disorder, paresthesia, dysosmia, epilepsy, morphine resistance, narcotic dependency, alcoholic dependency. The histamine-H3 receptor antagonist comprises a piperidine derivative compound of formula (I) [wherein X1 and X2 independently represent a nitrogen atom or CH; Y represents a specific group; X3 represents Os—(CH2)m; R1 and R2 independently resent a hydrogen atom, a halogen atom, a linear or branched lower alkyl group, a lower alkoxy group, or an acetyl group substituted with 2 or 3 fluorine atoms; s is 0 or 1; and m is an integer to make (m+s) 0 or from 1 to 4], or its pharmaceutically-acceptable salt.
    • 提供组胺H3受体拮抗剂; 代谢系统疾病如肥胖症,糖尿病,激素分泌障碍,高脂血症,痛风,脂肪肝,循环系统疾病,例如心动过速,急性/充血性心功能不全,心肌梗塞,冠状动脉硬化等的预防和/或补救措施, 高血压,肾病,睡眠障碍和伴有睡眠障碍的各种疾病,例如特发性睡眠过多,重度睡眠过多,睡眠周期性运动障碍,睡眠呼吸暂停综合征,昼夜节律紊乱,慢性疲劳综合征,REM睡眠障碍,老年性失眠, 夜间工人睡眠躁狂,特发性失眠,重复性失眠,真实失眠,电解质代谢紊乱; 注意力缺陷/多动症,记忆障碍,阿尔茨海默氏病,帕金森病,睡眠障碍,识别障碍,运动障碍,中枢神经系统疾病和中枢神经系统疾病如贪食症,情绪障碍,忧郁症,焦虑症,癫痫,del妄, 感觉异常,dysosmia,癫痫,吗啡抵抗,麻醉依赖,酒精依赖。 组胺H3受体拮抗剂包括式(I)的哌啶衍生物化合物[其中X1和X2独立地表示氮原子或CH; Y表示特定组; X3表示Os-(CH2)m; R1和R2分别独立地表示氢原子,卤素原子,直链或支链低级烷基,低级烷氧基或被2或3个氟原子取代的乙酰基; s为0或1; 和m是使(m + s)0或1至4]的整数]或其药学上可接受的盐。
    • 2. 发明授权
    • Piperidine derivative
    • 哌啶衍生物
    • US07547693B2
    • 2009-06-16
    • US10574087
    • 2004-09-21
    • Norikazu OhtakeRyo YoshimotoShigeru TokitaAkio KanataniSayaka Mizutani
    • Norikazu OhtakeRyo YoshimotoShigeru TokitaAkio KanataniSayaka Mizutani
    • C07D401/14C07D401/12C07D401/02C07D401/06A61K31/4545A61K31/496A61K31/454A61K31/4523C07D403/14A61K31/506A61P3/04A61P3/10
    • C07D211/58A61K31/454
    • Provided are a histamine-H3 receptor antagonist; and a preventive and/or a remedy for metabolic system diseases such as obesity, diabetes, hormone secretion disorder, hyperlipemia, gout, fatty liver, circulatory system diseases, for example, stenocardia, acute/congestive cardiac insufficiency, cardiac infarction, coronary arteriosclerosis, hypertension, nephropathy, sleep disorder and various diseases accompanied by sleep disorder such as idiopathic hypersomnnia, repetitive hypersomnnia, true hypersomnnia, narcolepsy, sleep periodic acromotion disorder, sleep apnea syndrome, circadian rhythm disorder, chronic fatigue syndrome, REM sleep disorder, senile insomnia, night worker sleep insanitation, idiopathic insomnia, repetitive insomnia, true insomnia, electrolyte metabolism disorder, and central and peripheral nervous system diseases such as bulimia, emotional disorder, melancholia, anxiety, epilepsy, delirium, dementia, shinzophrenia, attention deficit/hyperactivity disorder, memory disorder, Alzheimer's disease, Parkinson's disease, sleep disorder, recognition disorder, motion disorder, paresthesia, dysosmia, epilepsy, morphine resistance, narcotic dependency, alcoholic dependency. The histamine-H3 receptor antagonist comprises a piperidine derivative compound of formula (I) [wherein X1 and X2 independently represent a nitrogen atom or CH; Y represents a specific group; X3 represents Os—(CH2)m; R1 and R2 independently represent a hydrogen atom, a halogen atom, a linear or branched lower alkyl group, a lower alkoxy group, or an acetyl group substituted with 2 or 3 fluorine atoms; s is 0 or 1; and m is an integer to make (m+s) 0 or from 1 to 4], or its pharmaceutically-acceptable salt.
    • 提供组胺H3受体拮抗剂; 代谢系统疾病如肥胖症,糖尿病,激素分泌障碍,高脂血症,痛风,脂肪肝,循环系统疾病,例如心动过速,急性/充血性心功能不全,心肌梗塞,冠状动脉硬化等的预防和/或补救措施, 高血压,肾病,睡眠障碍和伴有睡眠障碍的各种疾病,例如特发性超嗜酸症,重复性嗜睡症,真实嗜睡症,发作性睡眠,睡眠周期性运动障碍,睡眠呼吸暂停综合征,昼夜节律紊乱,慢性疲劳综合征,REM睡眠障碍,老年性失眠, 夜间工作人员睡眠躁狂,特发性失眠,重复性失眠,真实失眠,电解质代谢障碍,以及中枢和周围神经系统疾病如贪食症,情绪障碍,忧郁症,焦虑症,癫痫,del妄,痴呆,注射缺陷/多动症, 记忆障碍,阿尔茨海默病,帕金森病 ,睡眠障碍,识别障碍,运动障碍,感觉异常,dysosmia,癫痫,吗啡抵抗,麻醉依赖,酒精依赖。 组胺H3受体拮抗剂包括式(I)的哌啶衍生物化合物[其中X1和X2独立地表示氮原子或CH; Y表示特定组; X3表示Os-(CH2)m; R1和R2独立地表示氢原子,卤素原子,直链或支链低级烷基,低级烷氧基或被2或3个氟原子取代的乙酰基; s为0或1; 和m是使(m + s)0或1至4]的整数]或其药学上可接受的盐。
    • 3. 发明申请
    • Novel piperidine derivative
    • 新型哌啶衍生物
    • US20090203710A1
    • 2009-08-13
    • US12381099
    • 2009-03-06
    • Norikazu OhtakeRyo YoshimotoShigeru TokitaAkio KanataniSayaka Mizutani
    • Norikazu OhtakeRyo YoshimotoShigeru TokitaAkio KanataniSayaka Mizutani
    • A61K31/4545C07D401/14C07D409/14A61K31/496A61K31/506A61K31/4725A61K31/4709
    • C07D211/58A61K31/454
    • Provided are a histamine-H3 receptor antagonist; and a preventive and/or a remedy for metabolic system diseases such as obesity, diabetes, hormone secretion disorder, hyperlipemia, gout, fatty liver, circulatory system diseases, for example, stenocardia, acute/congestive cardiac insufficiency, cardiac infarction, coronary arteriosclerosis, hypertension, nephropathy, sleep disorder and various diseases accompanied by sleep disorder such as idiopathic hypersomnia repetitive hypersomnia, true hypersomnia, narcolepsy, sleep periodic acromotion disorder, sleep apnea syndrome, circadian rhythm disorder, chronic fatigue syndrome, REM sleep disorder, senile insomnia, night worker sleep insanitation, idiopathic insomnia, repetitive insomnia, true insomnia, electrolyte metabolism disorder; and central and peripheral nervous system diseases such as bulimia, emotional disorder, melancholia, anxiety, epilepsy, delirium, dementia, shinzophrenia, attention deficit/hyperactivity disorder, memory disorder, Alzheimer's disease, Parkinson's disease, sleep disorder, recognition disorder, motion disorder, paresthesia, dysosmia, epilepsy, morphine resistance, narcotic dependency, alcoholic dependency. The histamine-H3 receptor antagonist comprises a piperidine derivative compound of formula (I) [wherein X1 and X2 independently represent a nitrogen atom or CH; Y represents a specific group; X3 represents Os—(CH2)m; R1 and R2 independently resent a hydrogen atom, a halogen atom, a linear or branched lower alkyl group, a lower alkoxy group, or an acetyl group substituted with 2 or 3 fluorine atoms; s is 0 or 1; and m is an integer to make (m+s) 0 or from 1 to 4], or its pharmaceutically-acceptable salt.
    • 提供组胺H3受体拮抗剂; 代谢系统疾病如肥胖症,糖尿病,激素分泌障碍,高脂血症,痛风,脂肪肝,循环系统疾病,例如心动过速,急性/充血性心功能不全,心肌梗塞,冠状动脉硬化等的预防和/或补救措施, 高血压,肾病,睡眠障碍和伴有睡眠障碍的各种疾病,如特发性睡眠过度睡眠反复睡眠超声,真正的睡眠过度睡眠,发作性睡眠,睡眠周期性运动障碍,睡眠呼吸暂停综合征,昼夜节律紊乱,慢性疲劳综合征,REM睡眠障碍,老年失眠,夜间 工人睡眠躁狂,特发性失眠,重复性失眠,真正失眠,电解质代谢障碍; 注意力缺陷/多动症,记忆障碍,阿尔茨海默氏病,帕金森病,睡眠障碍,识别障碍,运动障碍,中枢神经系统疾病和中枢神经系统疾病如贪食症,情绪障碍,忧郁症,焦虑症,癫痫,del妄, 感觉异常,dysosmia,癫痫,吗啡抵抗,麻醉依赖,酒精依赖。 组胺H3受体拮抗剂包括式(I)的哌啶衍生物化合物[其中X1和X2独立地表示氮原子或CH; Y表示特定组; X3表示Os-(CH2)m; R1和R2分别独立地表示氢原子,卤素原子,直链或支链低级烷基,低级烷氧基或被2或3个氟原子取代的乙酰基; s为0或1; 和m是使(m + s)0或1至4]的整数]或其药学上可接受的盐。
    • 6. 发明授权
    • Pyridone derivative
    • 吡啶酮衍生物
    • US07732456B2
    • 2010-06-08
    • US10591373
    • 2005-03-04
    • Norikazu OtakeYuji HagaAkira NayaSayaka MizutaniAkio Kanatani
    • Norikazu OtakeYuji HagaAkira NayaSayaka MizutaniAkio Kanatani
    • A61K31/444C07D401/02
    • C07D213/69C07D237/16C07D239/52C07D401/12C07D401/14C07D403/12C07D409/14C07D451/02C07D471/04
    • The invention provides pyridone derivatives represented by a general formula (I) [in the formula, R1 and R2 may be same or different and stands for H, etc., or R1 and R2 may form an aliphatic nitrogen-containing heterocyclic group together with the N to which they bind; X1-X3 may be same or different and stand for methine or N, provided not all of them simultaneously stand for nitrogen; X4-X7 may be same or different and stand for methine or N, provided that three or more of them do not simultaneously stand for N; Y1 and Y3 may be same or different and stand for single bond, —O—, —NR—, —S—, etc; Y2 stands for lower lkylene, etc.; R stands for H, etc., L stands for methylene; Z1 and Z2 may be same or different and stand for single bond or lower alkylene; or R1, L and Z2 may form an aliphatic nitrogen-containing heterocyclic group with the N to which R1 binds; and Ar stands for aromatic carbocyclic group, etc.].
    • 本发明提供由通式(I)表示的吡啶酮衍生物[在该式中,R 1和R 2可以相同或不同,代表H等,或者R 1和R 2可以与脂族含氮杂环基一起形成 他们绑定的N X1-X3可以相同或不同,代替次甲基或N,但不是全部同时代表氮; X4-X7可以相同或不同,代表次甲基或N,条件是它们中的三个或更多不同时代表N; Y1和Y3可以相同或不同,代表单键,-O-,-NR-,-S-等; Y2代表低级亚烷基等; R代表H等,L代表亚甲基; Z 1和Z 2可以相同或不同,代表单键或低级亚烷基; 或R1,L和Z2可以与R1结合的N形成脂族含氮杂环基; 和Ar代表芳族碳环基团等]。