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：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：US07601734B2

公开(公告)日：2009-10-13

申请号：US11578169

申请日：2005-04-08

申请人： Toshihito Kumagai ,  Toshio Nakamura ,  Yuri Amada ,  Yoshinori Sekiguchi

发明人： Toshihito Kumagai ,  Toshio Nakamura ,  Yuri Amada ,  Yoshinori Sekiguchi

IPC分类号： A61K31/44 ,  A61P25/18 ,  A61P25/24

CPC分类号： C07D491/048 ,  C07D471/04 ,  C07D495/04

摘要： An object of the present invention is to provide a cyclic amine compound which has a potent inhibitory effect on the binding of α2C-adrenoceptor and is useful in preventing and treating disorders attributable to α2C-adrenoceptor.The above-described object is solved by the following cyclic amine compound, etc., wherein X is O, S, SO, SO2 or NR2, etc.; R1 is a hydrogen atom, a cyano group, a carboxyl group, a C2-C13 alkoxycarbonyl group, a carbamoyl group, etc.; Ar1 and Ar2 are the same or different and each represent an aryl or heteroaryl group which may be substituted by 1 to 3 substituents and so on; ring B is a benzene ring may be substituted by 1 to 3 substituents and so on; n is an integer from 1 to 10; and p and q are the same or different and each represent an integer of 1 or 2.

摘要翻译： 本发明的目的是提供对α2C-肾上腺素能受体的结合具有强效抑制作用的环胺化合物，可用于预防和治疗归因于α2C-肾上腺素受体的病症。 上述目的通过以下环胺化合物等来解决，其中X是O，S，SO，SO 2或NR 2等; R1是氢原子，氰基，羧基，C2-C13烷氧基羰基，氨基甲酰基等; Ar 1和Ar 2相同或不同，各自表示可被1〜3个取代基等取代的芳基或杂芳基; 环B为苯环可被1〜3个取代基取代等; n是1至10的整数; p和q相同或不同，各自表示1或2的整数。

公开(公告)号：US20070244145A1

公开(公告)日：2007-10-18

申请号：US11578169

申请日：2005-04-08

申请人： Toshihito Kumagai ,  Toshio Nakamura ,  Yuri Amada ,  Yoshinori Sekiguchi

发明人： Toshihito Kumagai ,  Toshio Nakamura ,  Yuri Amada ,  Yoshinori Sekiguchi

IPC分类号： A61K31/44 ,  A61P25/18 ,  A61P25/24

CPC分类号： C07D491/048 ,  C07D471/04 ,  C07D495/04

摘要： An object of the present invention is to provide a cyclic amine compound which has a potent inhibitory effect on the binding of α2C-adrenoceptor and is useful in preventing and treating disorders attributable to α2C-adrenoceptor. The above-described object is solved by the following cyclic amine compound, etc., wherein X is O, S, SO, SO2 or NR2, etc.; R1 is a hydrogen atom, a cyano group, a carboxyl group, a C2-C13 alkoxycarbonyl group, a carbamoyl group, etc.; Ar1 and Ar2 are the same or different and each represent an aryl or heteroaryl group which may be substituted by 1 to 3 substituents and so on; ring B is a benzene ring may be substituted by 1 to 3 substituents and so on; n is an integer from 1 to 10; and p and q are the same or different and each represent an integer of 1 or 2.

摘要翻译： 本发明的目的是提供对α2C-肾上腺素能受体的结合具有强效抑制作用的环胺化合物，可用于预防和治疗归因于α2C-肾上腺素受体的病症。 上述目的通过以下环胺化合物等来解决，其中X是O，S，SO，SO 2或NR 2等; R 1是氢原子，氰基，羧基，C 1 -C 13烷氧基羰基，氨基甲酰基等 。 Ar 1和Ar 2相同或不同，各自表示可被1至3个取代基等取代的芳基或杂芳基; 环B为苯环可被1〜3个取代基取代等; n是1至10的整数; p和q相同或不同，各自表示1或2的整数。

公开(公告)号：US06476056B2

公开(公告)日：2002-11-05

申请号：US09922807

申请日：2001-08-07

申请人： Atsuro Nakazato ,  Taketoshi Okubo ,  Toshio Nakamura ,  Shigeyuki Chaki ,  Kazuyuki Tomisawa ,  Masashi Nagamine ,  Kenji Yamamoto ,  Koichiro Harada ,  Masanori Yoshida

发明人： Atsuro Nakazato ,  Taketoshi Okubo ,  Toshio Nakamura ,  Shigeyuki Chaki ,  Kazuyuki Tomisawa ,  Masashi Nagamine ,  Kenji Yamamoto ,  Koichiro Harada ,  Masanori Yoshida

IPC分类号： A61K3144

CPC分类号： C07D213/40 ,  C07C233/25 ,  C07C233/33 ,  C07C233/54 ,  C07C235/38 ,  C07C235/78 ,  C07C237/30 ,  C07C247/10 ,  C07C275/32 ,  C07C311/27 ,  C07C311/29 ,  C07C311/46 ,  C07C323/20 ,  C07C323/41 ,  C07C323/60 ,  C07D213/643 ,  C07D213/65 ,  C07D213/68

摘要： An aryloxyaniline derivative represented by the formula: wherein Ar1 and Ar2 are the same or different, and are each a substituted or unsubstituted phenyl group, a substituted or unsubstituted pyridyl group or a naphthyl group, provided that Ar1 and Ar2 are not both phenyl or both naphthyl and are not phenyl and naphthyl, R1 is a hydrogen atom, a substituted or unsubstituted alkyl group having 1 to 10 carbon atoms, an alkoxy group having 1 to 10 carbon atoms, a substituted or unsubstituted phenyl group or a group of the formula: —NR2(R3) (wherein R2 and R3 are the same or different, and are each a hydrogen atom or an alkyl group having 1 to 10 carbon atoms, X1 is a hydrogen atom, an alkyl group having 1 to 5 carbon atoms, an alkoxy group having 1 to 5 carbon atoms, a phenoxy group, a halogen atom, a trifluoromethyl group, a carbamoyl group or an aminosulfonyl group, Y1 is a branched or unbranched alkylene group having 1 to 6 carbon atoms or a single bond; and pharmaceutically acceptable salts thereof.

摘要翻译： 由下式表示的芳氧基苯胺衍生物：其中Ar1和Ar2相同或不同，并且各自为取代或未取代的苯基，取代或未取代的吡啶基或萘基，条件是Ar 1和Ar 2不同时为苯基或两者 萘基，不是苯基和萘基，R1是氢原子，取代或未取代的碳原子数1〜10的烷基，碳原子数1〜10的烷氧基，取代或未取代的苯基或下式的基团： -NR2（R3）（其中R2和R3相同或不同，并且各自为氢原子或具有1-10个碳原子的烷基，X 1为氢原子，具有1至5个碳原子的烷基， 具有1至5个碳原子的烷氧基，苯氧基，卤素原子，三氟甲基，氨基甲酰基或氨基磺酰基，Y1是具有1至6个碳原子或单键的支链或非支链亚烷基; 可以接受 的盐。

公开(公告)号：US06333358B1

公开(公告)日：2001-12-25

申请号：US09485006

申请日：2000-02-01

申请人： Atsuro Nakazato ,  Taketoshi Okubo ,  Toshio Nakamura ,  Shigeyuki Chaki ,  Kazuyuki Tomisawa ,  Masashi Nagamine ,  Kenji Yamamoto ,  Koichiro Harada ,  Masanori Yoshida

发明人： Atsuro Nakazato ,  Taketoshi Okubo ,  Toshio Nakamura ,  Shigeyuki Chaki ,  Kazuyuki Tomisawa ,  Masashi Nagamine ,  Kenji Yamamoto ,  Koichiro Harada ,  Masanori Yoshida

IPC分类号： A61K31135

CPC分类号： C07D213/40 ,  C07C233/25 ,  C07C233/33 ,  C07C233/54 ,  C07C235/38 ,  C07C235/78 ,  C07C237/30 ,  C07C247/10 ,  C07C275/32 ,  C07C311/27 ,  C07C311/29 ,  C07C311/46 ,  C07C323/20 ,  C07C323/41 ,  C07C323/60 ,  C07D213/643 ,  C07D213/65 ,  C07D213/68

摘要： An aryloxyaniline derivative represented by the formula: wherein Ar1 and Ar2 are each a substituted or unsubstituted phenyl group, pyridyl group or naphthyl group, R1 is a hydrogen atom, an alkyl group, etc., X1 is a hydrogen atom, an alkyl group, etc., y1 is a branched or unbranched alkylene group having 1 to 6 carbon atoms or a single bond; or a pharmaceutically acceptable salt thereof can provide medicines having a high affinity for MDR, and therefore, exhibiting a therapeutic or preventive effect on anxiety, related diseases thereto, depression, etc.

摘要翻译： 由下式表示的芳氧基苯胺衍生物：其中Ar1和Ar2各自为取代或未取代的苯基，吡啶基或萘基，R1为氢原子，烷基等，X1为氢原子，烷基， y1是具有1〜6个碳原子或单键的支链或非支链亚烷基; 或其药学上可接受的盐可以提供对MDR具有高亲和力的药物，因此对焦虑，其相关疾病，抑郁等具有治疗或预防作用。

公开(公告)号：US20100113776A1

公开(公告)日：2010-05-06

申请号：US12519083

申请日：2007-12-14

申请人： Toshio Nakamura ,  Dai Nozawa ,  Makoto Tatsuzuki ,  Hiroahi Ohta ,  Takeshi Kuwada ,  Tomoko Ishizaka ,  Tomoko Tamita ,  Seiji Masuda

发明人： Toshio Nakamura ,  Dai Nozawa ,  Makoto Tatsuzuki ,  Hiroahi Ohta ,  Takeshi Kuwada ,  Tomoko Ishizaka ,  Tomoko Tamita ,  Seiji Masuda

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

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

摘要： A novel pyrazole derivative of the following formula having a histamine H3 receptor antagonistic effect: or a pharmaceutically acceptable salt thereof or a pharmaceutical preparation comprising the same as an active ingredient is effective for prevention or treatment of dementia, Alzheimer's disease, attention-deficit hyperactivity disorder, schizophrenia, eating disorders, obesity, diabetes, hyperlipidemia, sleep disorders, narcolepsy, sleep apnea syndrome, circadian rhythm disorder, depression, allergic rhinitis or other diseases.

摘要翻译： 具有组胺H3受体拮抗作用的下式的新型吡唑衍生物或其药学上可接受的盐或包含其作为活性成分的药物制剂可有效预防或治疗痴呆，阿尔茨海默病，注意力缺陷多动障碍 精神分裂症，进食障碍，肥胖症，糖尿病，高脂血症，睡眠障碍，发作性睡眠障碍，睡眠呼吸暂停综合征，昼夜节律紊乱，抑郁症，过敏性鼻炎或其他疾病。

公开(公告)号：US08642626B2

公开(公告)日：2014-02-04

申请号：US13812437

申请日：2011-07-29

申请人： Toshio Nakamura ,  Kazunari Sakagami ,  Kazuhide Konishi ,  Kanako Yamamoto ,  Seiji Masuda ,  Yohei Matsuda ,  Kumiko Okada ,  Tsuyoshi Shibata ,  Hiroshi Ohta ,  Akito Yasuhara ,  Hiroshi Kawamoto

发明人： Toshio Nakamura ,  Kazunari Sakagami ,  Kazuhide Konishi ,  Kanako Yamamoto ,  Seiji Masuda ,  Yohei Matsuda ,  Kumiko Okada ,  Tsuyoshi Shibata ,  Hiroshi Ohta ,  Akito Yasuhara ,  Hiroshi Kawamoto

IPC分类号： A61K31/4439 ,  A61K31/415 ,  C07D231/12 ,  C07D231/20 ,  C07D231/38 ,  C07D403/06 ,  C07D401/06

CPC分类号： C07D231/12 ,  C07D231/14 ,  C07D231/20 ,  C07D231/38 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D413/04

摘要： Provided is a novel compound represented by formula [I] or a pharmaceutically acceptable salt thereof having antagonistic activity against group II metabolism-type glutamic acid (m-Glu) receptors. The compound or pharmaceutically acceptable salt thereof is useful as a prophylactic or therapeutic agent for diseases such as new mood disorders (depressive and bipolar disorders), anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, post-traumatic stress disorder, specific phobias, and acute stress disorder), schizophrenia, Alzheimer's disease, cognitive dysfunction, dementia, drug dependence, convulsions, tremors, pain, sleep disorders, and the like.

摘要翻译： 本发明提供由式[I]表示的新化合物或其对II类代谢型谷氨酸（m-Glu）受体具有拮抗作用的药学上可接受的盐。 化合物或其药学上可接受的盐可用作疾病的预防或治疗剂，例如新的情绪障碍（抑郁和双相性精神障碍），焦虑症（广泛性焦虑症，惊恐障碍，强迫症，社会焦虑症， 创伤性应激障碍，特异性恐惧症和急性应激障碍），精神分裂症，阿尔茨海默病，认知功能障碍，痴呆，药物依赖，惊厥，震颤，疼痛，睡眠障碍等。

公开(公告)号：US20130137865A1

公开(公告)日：2013-05-30

申请号：US13814869

申请日：2011-08-11

申请人： Toshio Nakamura ,  Kazunari Sakagami ,  Kazuhide Konishi ,  Kanako Yamamoto ,  Seiji Masuda ,  Yohei Matsuda ,  Kumiko Okada ,  Tsuyoshi Shibata ,  Hiroshi Ohta ,  Akito Yasuhara ,  Hiroshi Kawamoto ,  Hideaki Amada ,  Hiroki Urabe ,  Rie Nishikawa ,  Shuhei Kashiwa ASHIWA

发明人： Toshio Nakamura ,  Kazunari Sakagami ,  Kazuhide Konishi ,  Kanako Yamamoto ,  Seiji Masuda ,  Yohei Matsuda ,  Kumiko Okada ,  Tsuyoshi Shibata ,  Hiroshi Ohta ,  Akito Yasuhara ,  Hiroshi Kawamoto ,  Hideaki Amada ,  Hiroki Urabe ,  Rie Nishikawa ,  Shuhei Kashiwa ASHIWA

IPC分类号： C07D413/14 ,  C07D413/04 ,  C07D403/04 ,  C07D231/38

CPC分类号： C07D413/14 ,  C07D231/38 ,  C07D403/04 ,  C07D403/14 ,  C07D413/04

摘要： A compound represented by formula [I] and a pharmaceutically accepted salt of said compound are a novel compound and a pharmaceutically accepted salt thereof which exert antagonistic activity against group II metabotropic glutamate (mGlu) receptors, and are effective as a novel preventive or therapeutic agent for disorders such as mood disorders (depressive disorder, bipolar disorder, etc.), anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, posttraumatic stress disorder, a specific phobic disorder, acute stress disorder, etc.), schizophrenia, Alzheimer's disease, cognitive impairment, dementia, drug dependence, convulsions, shivering, pain, sleep disorders, and the like.

摘要翻译： 由式[I]表示的化合物和所述化合物的药学上可接受的盐是对II族代谢型谷氨酸（mGlu）受体具有拮抗作用的新化合物及其药学上可接受的盐，并且作为新的预防或治疗剂是有效的 用于诸如情绪障碍（抑郁障碍，双相情感障碍等），焦虑障碍（广泛性焦虑症，恐慌症，强迫症，社会焦虑症，创伤后应激障碍，特异性恐怖症，急性应激障碍等） ，精神分裂症，阿尔茨海默病，认知障碍，痴呆，药物依赖，抽搐，发抖，疼痛，睡眠障碍等。

公开(公告)号：US08376934B2

公开(公告)日：2013-02-19

申请号：US13092702

申请日：2011-04-22

申请人： Kazuhiko Takahashi ,  Toshio Nakamura

发明人： Kazuhiko Takahashi ,  Toshio Nakamura

IPC分类号： A61B1/00 ,  A61B1/04 ,  G06F3/033

CPC分类号： B25J9/06 ,  A61B1/00147 ,  A61B1/0052 ,  A61B1/0055 ,  A61B5/065 ,  A61B34/30 ,  A61B34/37 ,  A61B2034/2059 ,  A61B2034/306 ,  A61B2090/064

摘要： A multijoint manipulator apparatus includes a tubular-member, linear-motion-transmission-members, a drive-unit, a position-detector, a tension-detector, an operation-unit, and a movement-degree-calculation-unit. The linear-members are inserted in the tubular-member, one end and the other end of each of the linear-members being fixed to the vicinity of a joint of the tubular-member and the drive-unit, respectively. The drive-unit moves the linear-members. The position-detector and the tension-detector detect positions and tension of the linear-members, respectively. A desired position/posture of a point of interest is input to the operation-unit. The calculation-unit calculates a current position/posture of the point, a weighting factor serving to give priority to and move the linear-members the tension of which is relatively low among the linear-members, and movement degrees of the linear-members to move the point to the desired position/posture, and causes the drive-unit to pull the linear-members.

摘要翻译： 多关节机械手装置包括管状构件，直线运动传递构件，驱动单元，位置检测器，张力检测器，操作单元和移动程度计算单元。 线性构件插入管状构件中，每个线性构件的一端和另一端分别固定在管状构件和驱动单元的接头附近。 驱动单元移动线性元件。 位置检测器和张力检测器分别检测线性元件的位置和张力。 将感兴趣点的期望位置/姿势输入到操作单元。 计算单元计算点的当前位置/姿势，用于优先使线性构件中的线性构件的张力相对较低的直线构件的加权系数和线性构件的移动度向 将点移动到期望的位置/姿势，并且使驱动单元拉动线性构件。