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    • 5. 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。
    • 6. 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。
    • 7. 发明申请
    • Novel piperidine derivative
    • US20070105901A1
    • 2007-05-10
    • US10574087
    • 2004-09-21
    • Norikazu OhtakeRyo YoshimotoShigeru TokitaAkio KanataniSayaka Date
    • Norikazu OhtakeRyo YoshimotoShigeru TokitaAkio KanataniSayaka Date
    • A61K31/4545C07D401/14
    • 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 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.
    • 8. 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。
    • 9. 发明申请
    • Novel azole derivatives
    • 新型唑衍生物
    • US20060111380A1
    • 2006-05-25
    • US10536360
    • 2003-11-25
    • Norikazu OtakeYuji HagaMakoto JitsuokaAkio Kanatani
    • Norikazu OtakeYuji HagaMakoto JitsuokaAkio Kanatani
    • A61K31/4747C07D471/10
    • C07D491/10
    • The present invention relates to a compound of the formula (I): wherein Az is a group comprising a monocyclic azole or a bicyclic aromatic ring of the same or different fused azoles; T, U, V and W are independently methine or nitrogen, said methine being optionally substituted by a substituent, and at least two of T, U, V and W are said methine groups; and X is nitrogen or methine. The compounds of the present invention are useful as agents for the treatment of various kinds of diseases related to NPY, for example, cardiovascular disorders, nervous system disorders, genitative diseases, metabolic diseases, genital or reproductive disorders, gastrointestinal disorders, respiratory disorders, inflammatory diseases or glaucoma, and the like.
    • 本发明涉及式(I)化合物:其中Az是包含相同或不同稠合唑的单环唑或双环芳环的基团; T,U,V和W独立为次甲基或氮,所述次甲基任选被取代基取代,T,U,V和W中的至少两个为所述次甲基; X是氮或次甲基。 本发明的化合物可用作治疗与NPY相关的各种疾病的药剂,例如心血管疾病,神经系统疾病,基因疾病,代谢疾病,生殖器或生殖障碍,胃肠道疾病,呼吸系统疾病,炎症性疾病 疾病或青光眼等。
    • 10. 发明授权
    • Azole derivatives
    • 唑衍生物
    • US07589096B2
    • 2009-09-15
    • US12071808
    • 2008-02-26
    • Norikazu OtakeYuji HagaMakoto JitsuokaAkio Kanatani
    • Norikazu OtakeYuji HagaMakoto JitsuokaAkio Kanatani
    • A61K31/438A61K31/506A61K31/4545C07D233/96C07D401/14C07D401/02
    • C07D491/10
    • The present invention relates to a compound of the formula (I): wherein Az is a group comprising a monocyclic azole or a bicyclic aromatic ring of the same or different fused azoles; T, U, V and W are independently methine or nitrogen, wherein a methine may be optionally substituted by a substituent, and at least two of T, U, V and W are methine groups; and X is nitrogen or methine. The compounds of the present invention are useful as agents for the treatment of various kinds of diseases related to NPY, for example, cardiovascular disorders, nervous system disorders, genitative diseases, metabolic diseases, genital or reproductive disorders, gastro-intestinal disorders, respiratory disorders, inflammatory diseases or glaucoma, and the like.
    • 本发明涉及式(I)化合物:其中Az是包含相同或不同稠合唑的单环唑或双环芳环的基团; T,U,V和W独立地是次甲基或氮,其中次甲基可以任选地被取代基取代,并且T,U,V和W中的至少两个是次甲基; X是氮或次甲基。 本发明的化合物可用作治疗与NPY相关的各种疾病的药剂,例如心血管疾病,神经系统疾病,基因疾病,代谢疾病,生殖器或生殖障碍,胃肠道疾病,呼吸障碍 ,炎症性疾病或青光眼等。