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    Carbamoyl-substituted spiro derivative
    1.
    发明授权
    Carbamoyl-substituted spiro derivative 有权
    氨基甲酰取代的螺衍生物

    公开(公告)号：US07960402B2

    公开(公告)日：2011-06-14

    申请号：US11662102

    申请日：2005-09-06

    Applicant: Makoto Jitsuoka ,  Norikazu Ohtake ,  Nagaaki Sato ,  Shigeru Tokita ,  Daisuke Tsukahara

    Inventor： Makoto Jitsuoka ,  Norikazu Ohtake ,  Nagaaki Sato ,  Shigeru Tokita ,  Daisuke Tsukahara

    IPC: A61K31/44 ,  A61K31/34 ,  A61K31/335 ,  C07D401/00 ,  C07D307/00

    CPC classification number: C07D307/94 ,  C07D209/96 ,  C07D401/12 ,  C07D405/08 ,  C07D405/12 ,  C07D405/14 ,  C07D471/10 ,  C07D487/04 ,  C07D491/10 ,  C07D493/10

    Abstract: A compound represented by, e.g. the formula (I): [wherein X, Y, Z, and W each independently represent optionally substituted methine; A, B, and D each independently represent —C(O)—, etc.; Q represents a methine or a nitrogen; and R represents the formula (II-1), optionally substituted with lower alkyl, etc.; (wherein R6 represents a lower alkyl, etc; and R7 and R8 each independently represents a lower alkyl, etc.)] or a pharmaceutically acceptable salt of the compound. The compounds and salt have antagonistic activity against a histamine H3 receptor or inverse agonistic activity against a histamine H3 receptor. They are useful in the prevention or treatment of metabolic diseases, circulatory diseases, or neurotic diseases.

    Abstract translation: 化合物。 式（I）：[其中X，Y，Z和W各自独立地表示任选取代的次甲基; A，B和D各自独立地表示-C（O） - 等; Q表示次甲基或氮; 并且R代表式（II-1），任选被低级烷基取代等; （其中R6表示低级烷基等; R7和R8各自独立地表示低级烷基等）]或化合物的药学上可接受的盐。 化合物和盐对组胺H3受体具有拮抗作用或对组胺H3受体具有反向激动作用。 它们可用于预防或治疗代谢疾病，循环系统疾病或神经病。

    Substituted Pyridone Derivative
    2.
    发明申请
    Substituted Pyridone Derivative 失效
    取代的吡啶酮衍生物

    公开(公告)号：US20080269287A1

    公开(公告)日：2008-10-30

    申请号：US11792110

    申请日：2005-11-30

    Applicant: Norikazu Ohtake ,  Takuya Suga ,  Shigeru Tokita

    Inventor： Norikazu Ohtake ,  Takuya Suga ,  Shigeru Tokita

    IPC: A61K31/4545 ,  C07D211/08 ,  A61P3/06 ,  A61P25/16 ,  A61P25/28 ,  A61P25/08 ,  A61P25/30 ,  A61P25/18

    CPC classification number: C07D401/12

    Abstract: Compounds of a formula (I) [wherein, A represents formula (III-1) R3 is a hydrogen, lower alkyl et al; m is 0 or 1; R1 is a hydrogen atom, halogen atom et al, R2 is a hydrogen et al; p is 0 to 4; X is a carbon atom or nitrogen atom; and X1 to X4 is a lower alkyl et al], or pharmaceutical acceptable salts thereof. These have a potency antagonistic to binding to histamine H3 receptor, or have a potency inhibiting the constant activity of histamine H3 receptor, and are useful in the therapy of obesity, diabetes et al.

    Abstract translation: 式（I）化合物[其中，A表示式（III-1）R 3是氢，低级烷基等; m为0或1; R1是氢原子，卤原子等，R2是氢等; p为0〜4; X是碳原子或氮原子; X1〜X4为低级烷基等]或其药学上可接受的盐。 它们对结合组胺H3受体具有拮抗作用，或具有抑制组胺H3受体的恒定活性的效力，并且可用于治疗肥胖症，糖尿病等。

    OXOTETRAHYDROFURAN-2-YL-BENZIMIDAZOLE DERIVATIVE
    4.
    发明申请
    OXOTETRAHYDROFURAN-2-YL-BENZIMIDAZOLE DERIVATIVE 有权
    氧自由基2-YL-苯并咪唑衍生物

    公开(公告)号：US20110144162A1

    公开(公告)日：2011-06-16

    申请号：US13059307

    申请日：2009-08-03

    Applicant: Tomoharu Iino ,  Masanori Asai ,  Akio Ohno ,  Seiichi Inamura ,  Makoto Ishikawa ,  Norikazu Ohtake

    Inventor： Tomoharu Iino ,  Masanori Asai ,  Akio Ohno ,  Seiichi Inamura ,  Makoto Ishikawa ,  Norikazu Ohtake

    IPC: A61K31/444 ,  C07D401/14 ,  A61K31/4439 ,  A61P3/10

    CPC classification number: C07D405/14 ,  A61K31/4439 ,  A61K31/444 ,  A61K38/28 ,  A61K38/31 ,  A61K45/06 ,  A61K2300/00

    Abstract: The present invention relates to compounds, which are useful for treatment and/or prevention of diabetes mellitus, diabetes mellitus complications or obesity, since the compounds have glucokinase-activating effects, and are presented in Formula (I): wherein R1 represents a carbamoyl group; R2 represents a lower alkyl group; both of X1 and X2 represent CH, or any one of X1 and X2 represents a nitrogen atom and the other represents CH; a group of represents a group selected from the group consisting of a pyridinyl, a pyrazinyl, a pyrazolyl, a thiadiazolyl, a triazolyl, an isoxazolyl and a thiazolyl group; and k is zero or 1, or relates to pharmaceutically acceptable salts thereof.

    Abstract translation: 本发明涉及可用于治疗和/或预防糖尿病，糖尿病并发症或肥胖症的化合物，因为该化合物具有葡糖激酶活化作用，并且呈现在式（I）中：其中R1表示氨基甲酰基 ; R2表示低级烷基; X1和X2都表示CH，或X1和X2中的任一个表示氮原子，另一个表示CH; 一组表示选自吡啶基，吡嗪基，吡唑基，噻二唑基，三唑基，异恶唑基和噻唑基的基团。 且k为0或1，或与其药学上可接受的盐有关。

    Novel piperidine derivative
    7.
    发明申请
    Novel piperidine derivative 失效
    新型哌啶衍生物

    公开(公告)号：US20090203710A1

    公开(公告)日：2009-08-13

    申请号：US12381099

    申请日：2009-03-06

    Applicant: Norikazu Ohtake ,  Ryo Yoshimoto ,  Shigeru Tokita ,  Akio Kanatani ,  Sayaka Mizutani

    Inventor： Norikazu Ohtake ,  Ryo Yoshimoto ,  Shigeru Tokita ,  Akio Kanatani ,  Sayaka Mizutani

    IPC: A61K31/4545 ,  C07D401/14 ,  C07D409/14 ,  A61K31/496 ,  A61K31/506 ,  A61K31/4725 ,  A61K31/4709

    CPC classification number: C07D211/58 ,  A61K31/454

    Abstract: 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.

    Abstract translation: 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。

    Carbamoyl-Substituted Spiro Derivative
    8.
    发明申请
    Carbamoyl-Substituted Spiro Derivative 有权
    氨基甲酰取代的螺衍生物

    公开(公告)号：US20080171753A1

    公开(公告)日：2008-07-17

    申请号：US11662102

    申请日：2005-09-06

    Applicant: Makoto Jitsuoka ,  Norikazu Ohtake ,  Nagaaki Sato ,  Shigeru Tokita ,  Daisuke Tsukahara

    Inventor： Makoto Jitsuoka ,  Norikazu Ohtake ,  Nagaaki Sato ,  Shigeru Tokita ,  Daisuke Tsukahara

    IPC: A61K31/497

    CPC classification number: C07D307/94 ,  C07D209/96 ,  C07D401/12 ,  C07D405/08 ,  C07D405/12 ,  C07D405/14 ,  C07D471/10 ,  C07D487/04 ,  C07D491/10 ,  C07D493/10

    Abstract: A compound represented by, e.g. the formula (I): [wherein X, Y, Z, and W each independently represent optionally substituted methine; A, B, and D each independently represent —C(O)—, etc.; Q represents a methine or a nitrogen; and R represents the formula (II-1), optionally substituted with lower alkyl, etc.; (wherein R6 represents a lower alkyl, etc; and R7 and R8 each independently represents a lower alkyl, etc.)] or a pharmaceutically acceptable salt of the compound. The compounds and salt have antagonistic activity against a histamine H3 receptor or inverse agonistic activity against a histamine H3 receptor. They are useful in the prevention or treatment of metabolic diseases, circulatory diseases, or neurotic diseases.

    Abstract translation: 化合物。 式（I）：[其中X，Y，Z和W各自独立地表示任选取代的次甲基; A，B和D各自独立地表示-C（O） - 等; Q表示次甲基或氮; 并且R代表式（II-1），任选被低级烷基取代等; （其中R 6表示低级烷基等; R 7和R 8各自独立地表示低级烷基等）]或 化合物的药学上可接受的盐。 化合物和盐对组胺H3受体具有拮抗作用或对组胺H3受体具有反向激动作用。 它们可用于预防或治疗代谢疾病，循环系统疾病或神经病。

    Oxotetrahydrofuran-2-yl-benzimidazole derivative
    9.
    发明授权
    Oxotetrahydrofuran-2-yl-benzimidazole derivative 有权
    氧四氢呋喃-2-基 - 苯并咪唑衍生物

    公开(公告)号：US08609699B2

    公开(公告)日：2013-12-17

    申请号：US13059307

    申请日：2009-08-03

    Applicant: Tomoharu Iino ,  Masanori Asai ,  Akio Ohno ,  Seiichi Inamura ,  Makoto Ishikawa ,  Norikazu Ohtake

    Inventor： Tomoharu Iino ,  Masanori Asai ,  Akio Ohno ,  Seiichi Inamura ,  Makoto Ishikawa ,  Norikazu Ohtake

    IPC: A61K31/4439 ,  C07D401/14

    CPC classification number: C07D405/14 ,  A61K31/4439 ,  A61K31/444 ,  A61K38/28 ,  A61K38/31 ,  A61K45/06 ,  A61K2300/00

    Abstract: The present invention relates to compounds, which are useful for treatment and/or prevention of diabetes mellitus, diabetes mellitus complications or obesity, since the compounds have glucokinase-activating effects, and are presented in Formula (I): wherein R1 represents a carbamoyl group; R2 represents a lower alkyl group; both of X1 and X2 represent CH, or any one of X1 and X2 represents a nitrogen atom and the other represents CH; a group of represents a group selected from the group consisting of a pyridinyl, a pyrazinyl, a pyrazolyl, a thiadiazolyl, a triazolyl, an isoxazolyl and a thiazolyl group; and k is zero or 1, or relates to pharmaceutically acceptable salts thereof.

    Abstract translation: 本发明涉及可用于治疗和/或预防糖尿病，糖尿病并发症或肥胖症的化合物，因为该化合物具有葡糖激酶活化作用，并且呈现在式（I）中：其中R1表示氨基甲酰基 ; R2表示低级烷基; X1和X2都表示CH，或X1和X2中的任一个表示氮原子，另一个表示CH; 一组表示选自吡啶基，吡嗪基，吡唑基，噻二唑基，三唑基，异恶唑基和噻唑基的基团。 且k为0或1，或与其药学上可接受的盐有关。

    Piperidine derivative
    10.
    发明授权
    Piperidine derivative 失效
    哌啶衍生物

    公开(公告)号：US07834182B2

    公开(公告)日：2010-11-16

    申请号：US12381099

    申请日：2009-03-06

    Applicant: Norikazu Ohtake ,  Ryo Yoshimoto ,  Shigeru Tokita ,  Akio Kanatani ,  Sayaka Mizutani

    Inventor： Norikazu Ohtake ,  Ryo Yoshimoto ,  Shigeru Tokita ,  Akio Kanatani ,  Sayaka Mizutani

    IPC: C07D401/14 ,  C07D403/14 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/454 ,  A61K31/4523 ,  A61K31/506 ,  A61P3/04 ,  A61P3/10 ,  C07D401/12 ,  C07D401/02 ,  C07D401/06

    CPC classification number: C07D211/58 ,  A61K31/454

    Abstract: 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.

    Abstract translation: 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。

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