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：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：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：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：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：US08796272B2

公开(公告)日：2014-08-05

申请号：US14000261

申请日：2012-02-21

申请人： Minoru Moriya ,  Hiroshi Ohta ,  Shuji Yamamoto ,  Kumi Abe ,  Yuko Araki ,  Xiang-Min Sun ,  Daisuke Wakasugi

发明人： Minoru Moriya ,  Hiroshi Ohta ,  Shuji Yamamoto ,  Kumi Abe ,  Yuko Araki ,  Xiang-Min Sun ,  Daisuke Wakasugi

IPC分类号： A61K31/50 ,  A61K31/501

CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14

摘要： The present invention relates to novel compounds of formula [I] or pharmaceutically acceptable salts thereof: The compounds of the present invention are useful in the 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, spasm, tremor, pain, Parkinson's disease, attention deficit hyperactivity disorder, bipolar disorder, eating disorder, or sleep disorders, which is based on the glycine uptake-inhibiting action.

摘要翻译： 本发明涉及式[I]的新化合物或其药学上可接受的盐：本发明的化合物可用于预防或治疗诸如精神分裂症，阿尔茨海默氏病，认知障碍，痴呆，焦虑症（例如， 广泛性焦虑症，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，痉挛，震颤，疼痛，帕金森病，注意缺陷多动障碍，双相 紊乱，进食障碍或睡眠障碍，其基于甘氨酸摄取抑制作用。

公开(公告)号：US20130331571A1

公开(公告)日：2013-12-12

申请号：US14000261

申请日：2012-02-21

申请人： Minoru Moriya ,  Hiroshi Ohta ,  Shuji Yamamoto ,  Kumi Abe ,  Yuko Araki ,  Xiang-Min Sun ,  Daisuke Wakasugi

发明人： Minoru Moriya ,  Hiroshi Ohta ,  Shuji Yamamoto ,  Kumi Abe ,  Yuko Araki ,  Xiang-Min Sun ,  Daisuke Wakasugi

IPC分类号： C07D401/04 ,  C07D417/14 ,  C07D413/14 ,  C07D401/14

CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14

摘要： The present invention relates to novel compounds of formula [I] or pharmaceutically acceptable salts thereof: The compounds of the present invention are useful in the 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, spasm, tremor, pain, Parkinson's disease, attention deficit hyperactivity disorder, bipolar disorder, eating disorder, or sleep disorders, which is based on the glycine uptake-inhibiting action.

摘要翻译： 本发明涉及式[I]的新化合物或其药学上可接受的盐：本发明的化合物可用于预防或治疗诸如精神分裂症，阿尔茨海默氏病，认知障碍，痴呆，焦虑症（例如， 广泛性焦虑症，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，痉挛，震颤，疼痛，帕金森病，注意缺陷多动障碍，双相 紊乱，进食障碍或睡眠障碍，其基于甘氨酸摄取抑制作用。

公开(公告)号：US08729271B2

公开(公告)日：2014-05-20

申请号：US13823574

申请日：2011-09-16

申请人： Minoru Moriya ,  Akito Yasuhara ,  Kazunari Sakagami ,  Hiroshi Ohta ,  Kumi Abe ,  Shuji Yamamoto ,  Yuko Araki ,  Hiroki Urabe ,  Xiang-Min Sun

发明人： Minoru Moriya ,  Akito Yasuhara ,  Kazunari Sakagami ,  Hiroshi Ohta ,  Kumi Abe ,  Shuji Yamamoto ,  Yuko Araki ,  Hiroki Urabe ,  Xiang-Min Sun

IPC分类号： A01N43/40 ,  A61K31/44 ,  A01N43/64 ,  A61K31/41 ,  C07D213/00 ,  C07D401/00 ,  C07D419/00

CPC分类号： C07D405/14 ,  C07D233/90 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

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-compulsive disorder, social anxiety disorder, posttraumatic stress disorder, specific phobia, acute stress disorder, etc.), depression, drug addiction, spasm, tremor, pain, 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， 焦虑障碍（广泛性焦虑症，惊恐障碍，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，疼痛和睡眠障碍：

公开(公告)号：US20130184460A1

公开(公告)日：2013-07-18

申请号：US13823574

申请日：2011-09-16

申请人： Minoru Moriya ,  Akito Yasuhara ,  Kazunari Sakagami ,  Hiroshi Ohta ,  Kumi Abe ,  Shuji Yamamoto ,  Yuko Araki ,  Hiroki Urabe ,  Xiang-Min Sun

发明人： Minoru Moriya ,  Akito Yasuhara ,  Kazunari Sakagami ,  Hiroshi Ohta ,  Kumi Abe ,  Shuji Yamamoto ,  Yuko Araki ,  Hiroki Urabe ,  Xiang-Min Sun

IPC分类号： C07D405/14 ,  C07D403/12 ,  C07D401/12

CPC分类号： C07D405/14 ,  C07D233/90 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

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-compulsive disorder, social anxiety disorder, posttraumatic stress disorder, specific phobia, acute stress disorder, etc.), depression, drug addiction, spasm, tremor, pain, 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， 焦虑障碍（广泛性焦虑症，惊恐障碍，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，疼痛和睡眠障碍：