公开(公告)号：US20080280928A1

公开(公告)日：2008-11-13

申请号：US11630042

申请日：2005-06-24

申请人： Atsuro Nakazato ,  Taketoshi Okubo ,  Dai Nozawa ,  Tomoko Tamita ,  Ludo E.J. Kennis

发明人： Atsuro Nakazato ,  Taketoshi Okubo ,  Dai Nozawa ,  Tomoko Tamita ,  Ludo E.J. Kennis

IPC分类号： A61K31/437 ,  C07D471/04 ,  A61K31/519 ,  A61P25/00 ,  C07D487/04

CPC分类号： C07D471/04 ,  C07D487/04

摘要： [PROBLEM TO BE SOLVED] An object of the present invention is to provide an antagonist against CRF receptors and/or an agonist for δ receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be involved, such as depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastrointestinal diseases, drug dependence, cerebral infarction, cerebral ischemia, cerebral edema, cephalic external wound, inflammation, immunity-related diseases, alopecia, irritable bowel syndrome, sleep disorders, epilepsy, dermatitides, schizophrenia, pain, etc. [SOLUTION] A pyrrolopyrimidine or pyrrolopyridine derivative substituted with a cyclic amino group represented by the following a [I] has a high affinity for CRF receptors and/or δ receptors, and is effective against diseases in which CRF is considered to be involved.

摘要翻译： [待解决的问题]本发明的目的是提供一种拮抗CRF受体拮抗剂和/或δ受体激动剂，其作为治疗或预防药物是有效的，其涉及CRF被认为是涉及的疾病，例如 抑郁症，焦虑症，阿尔茨海默氏病，帕金森病，亨廷顿氏舞蹈病，进食障碍，高血压，胃肠道疾病，药物依赖，脑梗塞，脑缺血，脑水肿，头部外伤，炎症，免疫相关疾病，脱发，肠易激综合征， 睡眠障碍，癫痫，皮肤病，精神分裂症，疼痛等。解决方案由以下[I]表示的环状氨基取代的吡咯并嘧啶或吡咯并吡啶衍生物对CRF受体和/或δ受体具有高亲和力，并且是 对抗CRF被认为参与的疾病有效。

公开(公告)号：US07365078B2

公开(公告)日：2008-04-29

申请号：US10584952

申请日：2005-01-06

申请人： Atsuro Nakazato ,  Taketoshi Okubo ,  Dai Nozawa ,  Tomoko Tamita ,  Ludo E. J. Kennis

发明人： Atsuro Nakazato ,  Taketoshi Okubo ,  Dai Nozawa ,  Tomoko Tamita ,  Ludo E. J. Kennis

IPC分类号： A01N43/54 ,  A61K31/505 ,  C07D239/00 ,  C07D471/00 ,  C07D487/00 ,  C07D491/00

CPC分类号： C07D487/16

摘要： An object of the present invention is to provide an antagonist against CRF receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be involved, such as depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastral diseases, drug dependence, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, cephalic external wound, inflammation, immunity-related diseases, alpecia, irritable bowel syndrome, sleep disorders, dermatitides, schizophrenia, pain, etc. A triaza-cyclopenta[cd]indene derivative represented by the following formula [I]: has a high affinity for CRF receptors and is effective against diseases in which CRF is considered to be involved

摘要翻译： 本发明的目的是提供一种抗CRF受体的拮抗剂，其作为治疗或预防药物是有效的，其涉及CRF被认为涉及的疾病，例如抑郁症，焦虑症，阿尔茨海默氏病，帕金森病，亨廷顿氏舞蹈病，进食 疾病，高血压，胃疾病，药物依赖，癫痫，脑梗塞，脑缺血，脑水肿，头部外伤，炎症，免疫相关疾病，特异性，肠易激综合征，睡眠障碍，皮肤病，精神分裂症，疼痛等。 由下式[I]表示的三氮杂 - 环戊二烯并[cd]茚衍生物：对CRF受体具有高亲和力，并且对于CRF被认为涉及的疾病有效

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：US20070293670A1

公开(公告)日：2007-12-20

申请号：US11630041

申请日：2005-06-24

申请人： Atsuro Nakazato ,  Taketoshi Okubo ,  Dai Nozawa ,  Ludo Kennis ,  Marcel De Bruyn

发明人： Atsuro Nakazato ,  Taketoshi Okubo ,  Dai Nozawa ,  Ludo Kennis ,  Marcel De Bruyn

IPC分类号： C07D487/04

CPC分类号： C07D487/04 ,  C07D471/04

摘要： [PROBLEM TO BE SOLVED]An object of the present invention is to provide an antagonist against CRF receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be involved, such as depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastrointestinal diseases, drug dependence, cerebral infarction, cerebral ischemia, cerebral edema, cephalic external wound, inflammation, immunity-related diseases, alopecia, irritable bowel syndrome, sleep disorders, epilepsy, dermatitides, schizophrenia, pain, etc. [SOLUTION]A pyrrolopyrimidine or pyrrolopyridine derivative substituted with tetrahydropyridine represented by the following formula [I]: has a high affinity for CRF receptors and is effective against diseases in which CRF is considered to be involved.

摘要翻译： [待解决的问题]本发明的目的是提供一种抗CRF受体的拮抗剂，其作为治疗或预防药物是有效的，其涉及CRF被认为涉及的疾病，例如抑郁症，焦虑症，阿尔茨海默病，帕金森病 疾病，亨廷顿氏舞蹈病，饮食失调，高血压，胃肠道疾病，药物依赖，脑梗死，脑缺血，脑水肿，头部外伤，炎症，免疫相关疾病，脱发，肠易激综合征，睡眠障碍，癫痫，皮肤病，精神分裂症 ，疼痛等。[解决方案]由下式[I]表示的用四氢吡啶取代的吡咯并嘧啶或吡咯并吡啶衍生物对CRF受体具有高亲和力，并且对于被认为涉及CRF的疾病是有效的。

公开(公告)号：US20130281465A1

公开(公告)日：2013-10-24

申请号：US13994043

申请日：2011-12-16

申请人： Dai Nozawa ,  Ryo Suzuki ,  Aya Futamura ,  Rie Shimono ,  Masahito Abe ,  Hiroshi Ohta ,  Yuko Araki

发明人： Dai Nozawa ,  Ryo Suzuki ,  Aya Futamura ,  Rie Shimono ,  Masahito Abe ,  Hiroshi Ohta ,  Yuko Araki

IPC分类号： C07D403/12 ,  C07D405/14 ,  A61K31/4439 ,  A61K31/506 ,  A61K31/4192 ,  C07D401/14

CPC分类号： A61K31/4192 ,  A61K31/4439 ,  A61K31/506 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14

摘要： A compound represented by formula (IA) or a pharmaceutically acceptable salt thereof, which is useful for the treatment or prevention of diseases such sleep disorder, depression, anxiety disorder, panic disorder, schizophrenia, drug dependence, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, pain, gastrointestinal diseases, epilepsy, inflammation, immune-related diseases, endocrine-related diseases, and hypertension, and of which the action relies on an orexin (OX) receptor antagonistic activity.

摘要翻译： 由式（IA）表示的化合物或其药学上可接受的盐，其可用于治疗或预防睡眠障碍，抑郁症，焦虑障碍，恐慌症，精神分裂症，药物依赖，阿尔茨海默氏病，帕金森病，亨廷顿舞蹈病 ，饮食失调，疼痛，胃肠道疾病，癫痫，炎症，免疫相关疾病，内分泌相关疾病和高血压，其作用依赖于食欲素（OX）受体拮抗作用。

公开(公告)号：US20140228377A1

公开(公告)日：2014-08-14

申请号：US14131090

申请日：2012-07-04

申请人： Masahito Abe ,  Aya Futamura ,  Ryo Suzuki ,  Dai Nozawa ,  Hiroshi Ohta ,  Yuko Araki

发明人： Masahito Abe ,  Aya Futamura ,  Ryo Suzuki ,  Dai Nozawa ,  Hiroshi Ohta ,  Yuko Araki

IPC分类号： C07D498/04 ,  C07D413/14

CPC分类号： C07D498/04 ,  C07D413/14

摘要： A compound represented by formula (IA) or a pharmaceutically acceptable salt thereof, which acts relying on an orexin (OX) receptor antagonistic activity and is useful for the treatment or prevention of diseases such as sleep disorder, depression, anxiety disorder, panic disorder, schizophrenia, drug dependence, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, head ache, migraine, pain, gastrointestinal diseases, epilepsy, inflammations, immune-related diseases, endocrine-related diseases and hypertension.

摘要翻译： 由式（IA）表示的化合物或其药学上可接受的盐，其依赖于食欲肽（OX）受体拮抗活性，并且可用于治疗或预防诸如睡眠障碍，抑郁症，焦虑障碍，恐慌症， 精神分裂症，药物依赖，阿尔茨海默病，帕金森病，亨廷顿舞蹈病，饮食失调，头痛，偏头痛，疼痛，胃肠道疾病，癫痫，炎症，免疫相关疾病，内分泌相关疾病和高血压。

公开(公告)号：US20140081025A1

公开(公告)日：2014-03-20

申请号：US14115933

申请日：2012-05-08

申请人： Ryo Suzuki ,  Aya Futamura ,  Masahito Abe ,  Shuhei Kashiwa ,  Nobutaka Hattori ,  Dai Nozawa ,  Hiroshi Ohta ,  Yuko Araki

发明人： Ryo Suzuki ,  Aya Futamura ,  Masahito Abe ,  Shuhei Kashiwa ,  Nobutaka Hattori ,  Dai Nozawa ,  Hiroshi Ohta ,  Yuko Araki

IPC分类号： C07D413/14 ,  C07D413/12 ,  C07D401/14

CPC分类号： C07D413/14 ,  C07D401/14 ,  C07D403/12 ,  C07D413/12

摘要： The compound represented by formula (IA) or a pharmaceutically acceptable salt thereof is based on orexin (OX) receptor antagonist activity, is useful in the treatment and prevention of illnesses including sleep disorder, depression, anxiety disorder, panic disorder, schizophrenia, drug dependency, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorders, pain, gastrointestinal disease, epilepsy, inflammation, immunological disease, endocrinological related disease, and hypertension.

摘要翻译： 由式（IA）表示的化合物或其药学上可接受的盐是基于食欲肽（OX）受体拮抗剂活性，可用于治疗和预防包括睡眠障碍，抑郁症，焦虑障碍，恐慌症，精神分裂症，药物依赖性 ，阿尔茨海默病，帕金森病，亨廷顿舞蹈病，进食障碍，疼痛，胃肠道疾病，癫痫，炎症，免疫疾病，内分泌相关疾病和高血压。

公开(公告)号：US20060084657A1

公开(公告)日：2006-04-20

申请号：US10499011

申请日：2002-12-19

申请人： Atsuro Nakazato ,  Takaaki Ishii ,  Dai Nozawa

发明人： Atsuro Nakazato ,  Takaaki Ishii ,  Dai Nozawa

IPC分类号： A61K31/496 ,  A61K31/497 ,  A61K31/506 ,  A61K31/517 ,  C07D403/14

CPC分类号： C07D239/26 ,  A61K31/496 ,  A61K31/517 ,  C07D209/48 ,  C07D231/12 ,  C07D233/70 ,  C07D233/84 ,  C07D239/96 ,  C07D261/08 ,  C07D263/32 ,  C07D277/28 ,  C07D277/34 ,  C07D277/40 ,  C07D277/56 ,  C07D295/02 ,  C07D295/13 ,  C07D307/91 ,  C07D311/90 ,  C07D313/18

摘要： A piperazine derivative represented by the formula (1): wherein n is an integer of 1 to 8; R1 represents hydrogen or C1-10 alkyl; A represents CH or nitrogen; Ar1 represents phenyl or substituted phenyl; and Y represents a group represented by the formula Y1-Y2-Ar2 or Y3-Y4(Ar5)-Ar6 or a pharmaceutically acceptable salt of the derivative. The novel piperazine derivative has MC4 receptor antagonistic activity.

摘要翻译： 由式（1）表示的哌嗪衍生物：其中n为1至8的整数; R 1表示氢或C 1-10烷基; A表示CH或氮; Ar 1表示苯基或取代的苯基; Y表示由式Y 1 -Y 2 -OR 2或Y 3 -Y 3表示的基团。 （Ar 5） - Ar 6或其衍生物的药学上可接受的盐。 新型哌嗪衍生物具有MC4受体拮抗作用。