公开(公告)号：US07557111B2

公开(公告)日：2009-07-07

申请号：US10584951

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： C07D495/04 ,  A61K31/519

CPC分类号： C07D495/04

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, epilepsy, dermatitides, schizophrenia, etc.A thienopyrimidine or thienopyridine derivative substituted with a cyclic amino group 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，癫痫，皮肤病，精神分裂症等。 由下式[I]表示的环状氨基取代的噻吩并嘧啶或噻吩并吡啶衍生物对CRF受体具有高亲和力，对于认为涉及CRF的疾病有效。

公开(公告)号：US20090111835A1

公开(公告)日：2009-04-30

申请号：US12338698

申请日：2008-12-18

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： A61K31/519 ,  C07D495/04 ,  A61K31/4365

CPC分类号： C07D495/04

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 thienopyrimidine or thienopyridine derivative substituted with a cyclic amino group 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]表示的环状氨基取代的噻吩并嘧啶或噻吩并吡啶衍生物对CRF受体具有高亲和力，对于认为涉及CRF的疾病有效。

公开(公告)号：US20070060602A1

公开(公告)日：2007-03-15

申请号：US10584952

申请日：2005-01-06

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

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

IPC分类号： A61K31/519 ,  C07D487/14

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：US20110130364A1

公开(公告)日：2011-06-02

申请号：US12951556

申请日：2010-11-22

申请人： Atsuro NAKAZATO ,  Taketoshi Okubo ,  Dai Nozawa ,  Mikako Yamaguchi ,  Tomoko Tamita ,  Ludo E.J. Kennis ,  Marcel F.L. De Bruyn ,  Jean-Pierre A.M. Bongartz ,  Frans M.A. Van Den Keybus ,  Yves E.M. Van Roosbroeck ,  Marcel G.M. Luyckx ,  Robert J.M. Hendrickx

发明人： Atsuro NAKAZATO ,  Taketoshi Okubo ,  Dai Nozawa ,  Mikako Yamaguchi ,  Tomoko Tamita ,  Ludo E.J. Kennis ,  Marcel F.L. De Bruyn ,  Jean-Pierre A.M. Bongartz ,  Frans M.A. Van Den Keybus ,  Yves E.M. Van Roosbroeck ,  Marcel G.M. Luyckx ,  Robert J.M. Hendrickx

IPC分类号： A61K31/675 ,  C07D487/04 ,  A61K31/519 ,  C07D471/04 ,  A61K31/437 ,  C07F9/6561 ,  A61K31/55 ,  A61K31/397 ,  A61K31/553 ,  A61P25/00 ,  A61P1/00 ,  A61P9/12 ,  A61P9/00 ,  A61P29/00 ,  A61P17/00

CPC分类号： C07D471/04 ,  C07D487/04 ,  C07F9/6561

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, gastric diseases, drug dependence, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, cephalic external wound, inflammation, immunity-related diseases, alopecia, irritable bowel syndrome, sleep disorders, epilepsy, dermatitides, schizophrenia, etc. This problem can be solved with a pyrrolopyrimidine or pyrrolopyridine derivative substituted with a cyclic amino group represented by formula [I] below which 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，脱发，肠易激综合征，睡眠障碍，癫痫，皮肤病，精神分裂症等。 可以用由以下式[I]表示的环氨基取代的吡咯并嘧啶或吡咯并吡啶衍生物来解决问题，其具有对CRF受体的高亲和力，并且对于CRF被认为涉及的疾病是有效的。

公开(公告)号：US20110124862A1

公开(公告)日：2011-05-26

申请号：US13018928

申请日：2011-02-01

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： C07D487/04 ,  C07D471/04

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 formula [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/或对δ受体的激动剂，其作为用于涉及CRF的疾病的治疗或预防剂是有效的，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。[溶液]由下式[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受体具有高亲和性， 对抗CRF被认为参与的疾病有效。

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：US20090291940A1

公开(公告)日：2009-11-26

申请号：US12296082

申请日：2007-03-30

申请人： Taketoshi Okubo ,  Toshihito Kumagai ,  Takaaki Ishii ,  Toshio Nakamura ,  Kumi Abe ,  Yuri Amada ,  Tomoko Ishizaka ,  Xiang-Min Sun ,  Yoshinori Sekiguchi ,  Shigetada Sasako ,  Takanori Shimizu ,  Takayuki Nagatsuka

发明人： Taketoshi Okubo ,  Toshihito Kumagai ,  Takaaki Ishii ,  Toshio Nakamura ,  Kumi Abe ,  Yuri Amada ,  Tomoko Ishizaka ,  Xiang-Min Sun ,  Yoshinori Sekiguchi ,  Shigetada Sasako ,  Takanori Shimizu ,  Takayuki Nagatsuka

IPC分类号： A61K31/553 ,  A61K31/541 ,  A61K31/5377 ,  A61K31/497 ,  A61K31/517 ,  A61K31/4709 ,  C07D417/14 ,  C07D413/14 ,  C07D403/14 ,  C07D401/14

CPC分类号： C07D401/12

摘要： Disclosed is an aminopyrrolidine compound represented by the formula [I] or a pharmaceutically acceptable salt thereof. The compound or the salt is useful as a prophylactic/therapeutic agent for mode disorder such as depression, anxiety disorder, anorexia, cachexia, pain and drug dependence, whose action relies on the MC4 receptor antagonistic effect.

摘要翻译： 公开了由式[I]表示的氨基吡咯烷化合物或其药学上可接受的盐。 化合物或盐可用作模式障碍如抑郁症，焦虑障碍，厌食症，恶病质，疼痛和药物依赖性的预防/治疗剂，其作用依赖于MC4受体拮抗作用。

公开(公告)号：US08044068B2

公开(公告)日：2011-10-25

申请号：US12296082

申请日：2007-03-30

申请人： Taketoshi Okubo ,  Toshihito Kumagai ,  Takaaki Ishii ,  Toshio Nakamura ,  Kumi Abe ,  Yuri Amada ,  Tomoko Ishizaka ,  Xiang-Min Sun ,  Yoshinori Sekiguchi ,  Shigetada Sasako ,  Takanori Shimizu ,  Takayuki Nagatsuka

发明人： Taketoshi Okubo ,  Toshihito Kumagai ,  Takaaki Ishii ,  Toshio Nakamura ,  Kumi Abe ,  Yuri Amada ,  Tomoko Ishizaka ,  Xiang-Min Sun ,  Yoshinori Sekiguchi ,  Shigetada Sasako ,  Takanori Shimizu ,  Takayuki Nagatsuka

IPC分类号： A61K31/47 ,  C07D453/04

CPC分类号： C07D401/12

摘要： Disclosed is an aminopyrrolidine compound represented by the formula [I] or a pharmaceutically acceptable salt thereof. The compound or the salt is useful as a prophylactic/therapeutic agent for mode disorder such as depression, anxiety disorder, anorexia, cachexia, pain and drug dependence, whose action relies on the MC4 receptor antagonistic effect.

摘要翻译： 公开了由式[I]表示的氨基吡咯烷化合物或其药学上可接受的盐。 化合物或盐可用作模式障碍如抑郁症，焦虑障碍，厌食症，恶病质，疼痛和药物依赖性的预防/治疗剂，其作用依赖于MC4受体拮抗作用。

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。