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：

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：

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。

公开(公告)号：US20080318923A1

公开(公告)日：2008-12-25

申请号：US11883236

申请日：2006-01-30

申请人： Yoshinori Sekiguchi ,  Takeshi Kuwada ,  Masato Hayashi ,  Dai Nozawa ,  Yuri Amada ,  Tsuyoshi Shibata ,  Shuji Yamamoto ,  Hiroshi Ohta ,  Taketoshi Okubo ,  Takeshi Koami

发明人： Yoshinori Sekiguchi ,  Takeshi Kuwada ,  Masato Hayashi ,  Dai Nozawa ,  Yuri Amada ,  Tsuyoshi Shibata ,  Shuji Yamamoto ,  Hiroshi Ohta ,  Taketoshi Okubo ,  Takeshi Koami

IPC分类号： A61K31/397 ,  C07D209/04 ,  C07D401/02 ,  C07D213/02 ,  C07D217/00 ,  C07D413/02 ,  C07D403/14 ,  C07D241/02 ,  C07D471/02 ,  A61P25/00 ,  C07C317/14 ,  A61K31/437 ,  A61K31/501 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/4725 ,  A61K31/4545 ,  A61K31/454 ,  A61K31/404

CPC分类号： C07D401/12 ,  C07C309/87 ,  C07D209/38 ,  C07D209/40 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D413/04 ,  C07D417/12

摘要： It is intended to provide a drug which is efficacious against pathological conditions relating to arginine-vasopressin V1b receptor. More particularly speaking, it is intended to provide a drug which has a therapeutic or preventive effect on depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorders, hypertension, digestive diseases, drug addiction, epilepsy, brain infarction, brain ischemia, brain edema, head injury, inflammation, immune diseases, alopecia and so on. As the results of intensive studies, a novel 1,3-dihydro-2H-indol-2-one compound and a pyrrolidin-2-one compound fused with a heteroaromatic ring, which are highly selective antagonists of arginine-vasopressin V1b receptor, have high metabolic stabilities and show favorable brain penetration and high plasma concentrations, are found, thereby achieving the above objective.

摘要翻译： 旨在提供对精氨酸 - 加压素V1b受体有关的病理状况有效的药物。 更具体地说，它旨在提供一种对抑郁，焦虑，阿尔茨海默病，帕金森病，亨廷顿氏舞蹈病，进食障碍，高血压，消化系统疾病，药物成瘾，癫痫，脑梗死，脑缺血具有治疗或预防作用的药物 ，脑水肿，头部损伤，炎症，免疫疾病，脱发等。 作为深入研究的结果，作为精氨酸 - 加压素V1b受体的高度选择性拮抗剂的与杂芳环稠合的新的1,3-二氢-2H-吲哚-2-酮化合物和吡咯烷-2-酮化合物具有 发现高代谢稳定性并显示有利的脑渗透和高血浆浓度，从而达到上述目的。

公开(公告)号：US08030499B2

公开(公告)日：2011-10-04

申请号：US11883236

申请日：2006-01-30

申请人： Yoshinori Sekiguchi ,  Takeshi Kuwada ,  Masato Hayashi ,  Dai Nozawa ,  Yuri Amada ,  Tsuyoshi Shibata ,  Shuji Yamamoto ,  Hiroshi Ohta ,  Taketoshi Okubo ,  Takeshi Koami

发明人： Yoshinori Sekiguchi ,  Takeshi Kuwada ,  Masato Hayashi ,  Dai Nozawa ,  Yuri Amada ,  Tsuyoshi Shibata ,  Shuji Yamamoto ,  Hiroshi Ohta ,  Taketoshi Okubo ,  Takeshi Koami

IPC分类号： C07D209/04 ,  A61K31/404

CPC分类号： C07D401/12 ,  C07C309/87 ,  C07D209/38 ,  C07D209/40 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D413/04 ,  C07D417/12

摘要： It is intended to provide a drug which is efficacious against pathological conditions relating to arginine-vasopressin V1b receptor. More particularly speaking, it is intended to provide a drug which has a therapeutic or preventive effect on depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorders, hypertension, digestive diseases, drug addiction, epilepsy, brain infarction, brain ischemia, brain edema, head injury, inflammation, immune diseases, alopecia and so on. As the results of intensive studies, a novel 1,3-dihydro-2H-indol-2-one compound and a pyrrolidin-2-one compound fused with a heteroaromatic ring, which are highly selective antagonists of arginine-vasopressin V1b receptor, have high metabolic stabilities and show favorable brain penetration and high plasma concentrations, are found, thereby achieving the above objective.

摘要翻译： 旨在提供对精氨酸 - 加压素V1b受体有关的病理状况有效的药物。 更具体地说，它旨在提供一种对抑郁，焦虑，阿尔茨海默病，帕金森病，亨廷顿氏舞蹈病，进食障碍，高血压，消化系统疾病，药物成瘾，癫痫，脑梗死，脑缺血具有治疗或预防作用的药物 ，脑水肿，头部损伤，炎症，免疫疾病，脱发等。 作为深入研究的结果，作为精氨酸 - 加压素V1b受体的高度选择性拮抗剂的与杂芳环稠合的新的1,3-二氢-2H-吲哚-2-酮化合物和吡咯烷-2-酮化合物具有 发现高代谢稳定性并显示有利的脑渗透和高血浆浓度，从而实现上述目的。

公开(公告)号：US20100081825A1

公开(公告)日：2010-04-01

申请号：US12444275

申请日：2007-10-05

申请人： Yoshinori Sekiguchi ,  Kosuke Kanuma ,  Kazunari Sakagami ,  Masato Hayashi ,  Shuhei Kashiwa ,  Katsunori Omodera

发明人： Yoshinori Sekiguchi ,  Kosuke Kanuma ,  Kazunari Sakagami ,  Masato Hayashi ,  Shuhei Kashiwa ,  Katsunori Omodera

IPC分类号： C07D211/58 ,  C07D401/10

CPC分类号： C07D405/12 ,  C07D211/58 ,  C07D401/10 ,  C07D401/12 ,  C07D405/10 ,  C07D409/12

摘要： Disclosed is a pharmaceutical composition comprising a compound represented by the formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient, which has an antagonistic activity on a melanin-concentrating hormone receptor. The pharmaceutical composition is useful, due to its antagonistic activity on a MCH receptor, for the prevention or treatment of a disease such as depression, anxiety disorders (e.g., generalized anxiety disorder, post traumatic stress disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder), attention deficit disorder, mania, manic-depressive disorder, schizophrenia, mood disorders, stress, sleep disorder, attacks, memory impairment, cognitive impairment, dementia, amnesia, delirium, obesity, eating disorder, appetite disorder, hyperphagia, bulimia, cibophobia, diabetes, a cardiovascular diseases, hypertension, dyslipidemia, cardiac infarction, movement disorder (e.g., Parkinson's disease, epilepsy, convulsion, tremor), drug abuse and drug addiction.

摘要翻译： 公开了一种药物组合物，其包含式（I）表示的化合物或其药学上可接受的盐作为活性成分，其对黑色素浓缩激素受体具有拮抗作用。 由于其对MCH受体的拮抗活性，药物组合物可用于预防或治疗诸如抑郁症，焦虑症（例如广泛性焦虑症，创伤后应激障碍，恐慌症，强迫症， 社会焦虑障碍），注意力缺陷障碍，躁狂症，躁狂抑郁障碍，精神分裂症，情绪障碍，压力，睡眠障碍，发作，记忆障碍，认知障碍，痴呆，遗忘症，del妄，肥胖，进食障碍，食欲障碍， 糖尿病，心血管疾病，高血压，血脂异常，心肌梗死，运动障碍（如帕金森病，癫痫，惊厥，震颤），药物滥用和药物成瘾。

公开(公告)号：US20080090863A1

公开(公告)日：2008-04-17

申请号：US11664392

申请日：2005-09-27

申请人： Yoshinori Sekiguchi ,  Kosuke Kanuma ,  Katsunori Omodera ,  Kumi Sato ,  Masato Hayashi ,  Shuji Yamamoto

发明人： Yoshinori Sekiguchi ,  Kosuke Kanuma ,  Katsunori Omodera ,  Kumi Sato ,  Masato Hayashi ,  Shuji Yamamoto

IPC分类号： A61K31/44 ,  A61K31/4439 ,  A61K31/47 ,  A61P25/00 ,  A61P3/04 ,  A61P9/00 ,  C07D213/75 ,  C07D215/00 ,  C07D401/08 ,  C07D413/08

CPC分类号： C07D213/74 ,  C07D213/75 ,  C07D215/38 ,  C07D221/04 ,  C07D401/04

摘要： The present invention encompasses novel substituted pyridine compounds of Formula (I): which act as MCH receptor antagonists. These compositions and pharmaceutical compositions thereof are useful in the prophylaxis or treatment of improving memory function, sleeping and arousal, anxiety, depression, mood disorders, seizure, obesity, diabetes, appetite and eating disorders, cardiovascular disease, hypertension, dyslipidemia, myocardial infarction, binge eating disorders including bulimia, anorexia, mental disorders including manic depression, schizophrenia, delirium, dementia, stress, cognitive disorders, attention deficit disorder, substance abuse disorders and dyskinesias including Parkinson's disease, epilepsy, and addiction.

摘要翻译： 本发明包括式（I）的新型取代的吡啶化合物：其作为MCH受体拮抗剂。 这些组合物及其药物组合物可用于预防或治疗改善记忆功能，睡眠和觉醒，焦虑，抑郁，情绪障碍，癫痫发作，肥胖，糖尿病，食欲和进食障碍，心血管疾病，高血压，血脂异常，心肌梗死， 包括贪食症，厌食症，包括躁狂抑郁症，精神分裂症，del妄，痴呆，压力，认知障碍，注意力缺陷障碍，药物滥用障碍和包括帕金森氏病，癫痫和成瘾在内的运动障碍的暴饮暴食症。

公开(公告)号：US09139609B2

公开(公告)日：2015-09-22

申请号：US14000556

申请日：2012-02-20

申请人： Tomohiro Sugimoto ,  Naoki Sasamoto ,  Jun Kurosaka ,  Masato Hayashi ,  Kanako Yamamoto ,  Masato Kashimura ,  Yasunobu Ushiki ,  Haruhisa Ogita ,  Tomoaki Miura ,  Kenichi Kanemoto ,  Kou Kumura ,  Satoshi Yoshida ,  Keiji Tamura ,  Eiki Shitara

发明人： Tomohiro Sugimoto ,  Naoki Sasamoto ,  Jun Kurosaka ,  Masato Hayashi ,  Kanako Yamamoto ,  Masato Kashimura ,  Yasunobu Ushiki ,  Haruhisa Ogita ,  Tomoaki Miura ,  Kenichi Kanemoto ,  Kou Kumura ,  Satoshi Yoshida ,  Keiji Tamura ,  Eiki Shitara

IPC分类号： A61K31/70 ,  C07H17/08

CPC分类号： C07H17/08

摘要： A macrolide compound represented by the formula (I) effective against erythromycin resistant bacteria (for example, resistant pneumococci, streptococci and mycoplasmas).

摘要翻译： 由式（I）表示的大环内酯化合物对抗红霉素抗性细菌（例如抗性肺炎球菌，链球菌和支原体）有效。

公开(公告)号：US08141426B2

公开(公告)日：2012-03-27

申请号：US12315742

申请日：2008-12-05

申请人： Naoki Ikeuchi ,  Hisashi Fujiwara ,  Masami Yakabe ,  Masato Hayashi

发明人： Naoki Ikeuchi ,  Hisashi Fujiwara ,  Masami Yakabe ,  Masato Hayashi

IPC分类号： G01P15/125 ,  G01P9/04 ,  G01C19/56

CPC分类号： G01P15/125 ,  G01C19/5719 ,  G01P2015/0814

摘要： A displacement measurement apparatus for a microstructure according to the present invention measures a displacement of the microstructure having a fixed portion electrode including a first electrode and a second electrode and a movable portion electrode located oppositely to the fixed portion electrode. A bias generating circuit applies a bias signal to between the first electrode and the movable portion electrode so that influence of a noise signal on a detection signal picked up from between the second electrode and the movable portion electrode may be reduced. A C/V converting circuit converts a capacitance change that is picked up from between the second electrode and the movable portion electrode into a voltage. A detecting circuit detects a displacement of the movable portion electrode based on the voltage.

摘要翻译： 根据本发明的用于微结构的位移测量装置测量具有包括第一电极和第二电极的固定部分电极和位于与固定部分电极相对的可动部电极的微结构的位移。 偏置产生电路将偏置信号施加到第一电极和可动部分电极之间，从而可以减少噪声信号对从第二电极和可动部分电极之间拾取的检测信号的影响。 C / V转换电路将从第二电极和可动部分电极之间拾取的电容变化转换为电压。 检测电路基于电压检测可动部分电极的位移。

公开(公告)号：US07895984B2

公开(公告)日：2011-03-01

申请号：US12174423

申请日：2008-07-16

申请人： Takahiro Taira ,  Shojiro Fukuda ,  Masato Hayashi

发明人： Takahiro Taira ,  Shojiro Fukuda ,  Masato Hayashi

IPC分类号： F02M35/10

CPC分类号： F02M35/112 ,  F02M35/02 ,  F02M35/10222 ,  F02M35/10229 ,  F02M35/10321 ,  F02M35/1036

摘要： An intake passage is formed by connecting upper and lower cases 10, 20 of an intake manifold. The lower case 10 has a recessed portion 50 on an inner surface 17a. The recessed portion 50 has a deep surface 53 to which a negative pressure outlet port 42 opens, and an opening 51 is provided in an upper portion of the recessed portion 50. The upper case 20 has a projecting portion 60 extending further downwards towards the negative pressure outlet port 42 than mating surfaces 10a, 20a and projects into the recessed portion 50 through an opening 52. The projecting portion 60 is positioned above the negative pressure outlet port 42 and between the negative pressure outlet port 42 and the inner surface 17a. A lower end portion 63 of the projecting portion 60 is formed into an arc-like shape of which central portion 65 projects downwards.

摘要翻译： 通过连接进气歧管的上壳体10和下壳体20形成进气通道。 下壳体10在内表面17a上具有凹部50。 凹部50具有负压出口42打开的深表面53，并且在凹部50的上部设置有开口51.上壳体20具有向下延伸朝向负的突出部分60 压力出口42比配合面10a，20a突出并通过开口52突出到凹部50.凸出部分60位于负压出口42的上方，负压出口42和内表面17a之间。 突出部分60的下端部分63形成为中心部分65向下突出的弧形形状。