公开(公告)号：US08637557B2

公开(公告)日：2014-01-28

申请号：US13502636

申请日：2010-10-04

申请人： Tetsuya Yabuuchi ,  Yusuke Oka ,  Shoichi Kuroda ,  Takahiro Oi ,  Yoshinori Sekiguchi

发明人： Tetsuya Yabuuchi ,  Yusuke Oka ,  Shoichi Kuroda ,  Takahiro Oi ,  Yoshinori Sekiguchi

IPC分类号： A61K31/427 ,  A61K31/4245 ,  C07D277/20 ,  C07D271/06

CPC分类号： C07D417/04 ,  C07D417/14

摘要： A compound represented by formula (1) or a pharmaceutically acceptable salt thereof, which has a PI3 kinase γ inhibitory effect and is useful as a prophylactic or therapeutic agent for articular rheumatism, Crohn's disease, irritable colitis, Sjoegren's syndrome, multiple sclerosis, systemic lupus erythematosus, asthma, atopic dermatitis, arteriosclerosis, organ transplant rejection, cancer, retinopathy, psoriasis, arthrosis deformans, age-related macular degeneration, type II diabetes, insulin resistance, obesity, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), hyperlipemia, etc.

摘要翻译： 由式（1）表示的化合物或其药学上可接受的盐，其具有PI3激酶γ抑制作用，并且可用作关节风湿病，克罗恩病，过敏性结肠炎，Sjoegren综合征，多发性硬化症，系统性狼疮的预防或治疗剂 红斑狼疮，哮喘，特应性皮炎，动脉硬化，器官移植排斥，癌症，视网膜病变，牛皮癣，变形性关节炎，年龄相关性黄斑变性，II型糖尿病，胰岛素抵抗，肥胖，非酒精性脂肪性肝病（NAFLD），非酒精性 脂肪性肝炎（NASH），高脂血症等

公开(公告)号：US08461329B2

公开(公告)日：2013-06-11

申请号：US13142230

申请日：2009-12-25

申请人： Tetsuo Takayama ,  Hajime Asanuma ,  Daisuke Wakasugi ,  Rie Nishikawa ,  Yoshinori Sekiguchi ,  Madoka Kawamura ,  Naoya Ono ,  Tetsuya Yabuuchi ,  Takahiro Oi ,  Yusuke Oka ,  Shoichi Kuroda ,  Fumito Uneuchi ,  Takeshi Koami

发明人： Tetsuo Takayama ,  Hajime Asanuma ,  Daisuke Wakasugi ,  Rie Nishikawa ,  Yoshinori Sekiguchi ,  Madoka Kawamura ,  Naoya Ono ,  Tetsuya Yabuuchi ,  Takahiro Oi ,  Yusuke Oka ,  Shoichi Kuroda ,  Fumito Uneuchi ,  Takeshi Koami

IPC分类号： C07D413/12 ,  C07D401/12 ,  C07D405/12 ,  C07D217/24

CPC分类号： C07D217/16 ,  C07D217/18 ,  C07D217/20 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D471/04

摘要： A compound represented by formula (I) or a pharmaceutically acceptable salt thereof has an effect of inhibiting CRTH2 and, therefore, is useful as a preventive or a remedy for allergic diseases such as asthma, atopic dermatitis and allergic rhinitis.

摘要翻译： 由式（I）表示的化合物或其药学上可接受的盐具有抑制CRTH2的作用，因此可用作哮喘，特应性皮炎和过敏性鼻炎等过敏性疾病的预防或治疗。

公开(公告)号：US20130096310A1

公开(公告)日：2013-04-18

申请号：US13805944

申请日：2011-06-22

申请人： Tetsuo Takayama ,  Madoka Kawamura ,  Daisuke Wakasugi ,  Rie Nishikawa ,  Yoshinori Sekiguchi

发明人： Tetsuo Takayama ,  Madoka Kawamura ,  Daisuke Wakasugi ,  Rie Nishikawa ,  Yoshinori Sekiguchi

IPC分类号： C07D217/18

CPC分类号： C07D217/18 ,  C07D217/20

摘要： A compound represented by formula (I) or a pharmaceutically acceptable salt thereof has an effect of inhibiting CRTH2 and, therefore, is useful as a pharmaceutical.

摘要翻译： 由式（I）表示的化合物或其药学上可接受的盐具有抑制CRTH2的作用，因此可用作药物。

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：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：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：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：US20060276449A1

公开(公告)日：2006-12-07

申请号：US10569833

申请日：2004-08-27

申请人： Toshihito Kumagai ,  Takeshi Kuwada ,  Tsuyoshi Shibata ,  Masato Hayashi ,  Yuri Fujisawa ,  Yoshinori Sekiguchi

发明人： Toshihito Kumagai ,  Takeshi Kuwada ,  Tsuyoshi Shibata ,  Masato Hayashi ,  Yuri Fujisawa ,  Yoshinori Sekiguchi

IPC分类号： A61K31/404 ,  C07D403/14 ,  C07D403/04

CPC分类号： C07D403/04

摘要： A 1,3-dihydro-2H-indol-2-one derivative expressed by Formula 1 (wherein R1 is a halogen atom, a C1 to C4 alkyl group, etc., and R2 is a hydrogen atom, a halogen atom, etc., or R2 is in the 6-position of the indol-2-one and R1 and R2 join together to form a C3 to C6 alkylene group, R3 is a halogen atom, a hydroxyl group, etc., and R4 is a hydrogen atom, a halogen atom, a C1 to C4 alkyl group, etc., or R4 is in the 3-position of the phenyl and R3 and R4 join together to form a methylenedioxy group, R5 is a hydrogen atom or a fluorine atom, R6 is an ethylamino group, a dimethylamino group, etc., R7 is a C1 to C4 alkoxy group, and R8 is a C1 to C4 alkoxy group), or a pharmaceutically acceptable salt of this derivative. This is a novel compound that has antagonistic activity against an aruginine-vasopressin V1b receptor.

摘要翻译： 由式1表示的1,3-二氢-2H-吲哚-2-酮衍生物（其中R 1是卤素原子，C 1至C 1烷基， 4个烷基等，R 2是氢原子，卤原子等，或R 2 2位在6位的 吲哚-2-酮和R 1和R 2连接在一起以形成C 6 -C 6亚烷基， 亚烷基，R 3是卤素原子，羟基等，R 4是氢原子，卤原子，C 1， / SUB→C 4烷基等，或R 4在苯基的3位和R 3和R 3 连接在一起形成亚甲二氧基，R 5是氢原子或氟原子，R 6是乙氨基，二甲基氨基 基团等，R 7是C 1-4烷氧基的C 1至C 8，并且R 8是 C 1至C 4烷氧基），或该衍生物的药学上可接受的盐。 这是一种新的化合物，具有对抗葡萄糖酸加压素V1b受体的拮抗作用。

公开(公告)号：US20130345419A1

公开(公告)日：2013-12-26

申请号：US14004997

申请日：2012-03-15

申请人： Naoya Ono ,  Shoichi Kuroda ,  Yoshihisa Shirasaki ,  Tetsuo Takayama ,  Yoshinori Sekiguchi ,  Fumihito Ushiyama ,  Yusuke Oka

发明人： Naoya Ono ,  Shoichi Kuroda ,  Yoshihisa Shirasaki ,  Tetsuo Takayama ,  Yoshinori Sekiguchi ,  Fumihito Ushiyama ,  Yusuke Oka

IPC分类号： C07D413/04 ,  C07D403/04 ,  C07D417/04 ,  C07D413/14

CPC分类号： C07D413/04 ,  C07D403/04 ,  C07D413/14 ,  C07D417/04

摘要： Provided are novel compounds that bind to FKBP12 or pharmaceutically acceptable salts thereof, as well as new therapeutics useful in the prevention or treatment of alopecia which comprise those compounds or pharmaceutically acceptable salts thereof. Specifically, compounds represented by formula (1) [where R1 represents either the following formula (2) or (3)] or pharmaceutically acceptable salts thereof are provided.

摘要翻译： 提供与FKBP12或其药学上可接受的盐结合的新化合物，以及可用于预防或治疗脱发的新治疗剂，其包含那些化合物或其药学上可接受的盐。 具体地，提供由式（1）表示的化合物[其中R 1表示下式（2）或（3）]或其药学上可接受的盐。

公开(公告)号：US07528124B2

公开(公告)日：2009-05-05

申请号：US10569833

申请日：2004-08-27

申请人： Toshihito Kumagai ,  Takeshi Kuwada ,  Tsuyoshi Shibata ,  Masato Hayashi ,  Yuri Fujisawa ,  Yoshinori Sekiguchi

发明人： Toshihito Kumagai ,  Takeshi Kuwada ,  Tsuyoshi Shibata ,  Masato Hayashi ,  Yuri Fujisawa ,  Yoshinori Sekiguchi

IPC分类号： A61K31/404 ,  C07D209/04 ,  C07D403/04

CPC分类号： C07D403/04

摘要： A 1,3-dihydro-2H-indol-2-one derivative expressed by Formula 1 (wherein R1 is a halogen atom, a C1 to C4 alkyl group, etc., and R2 is a hydrogen atom, a halogen atom, etc., or R2 is in the 6-position of the indol-2-one and R1 and R2 join together to form a C3 to C6 alkylene group, R3 is a halogen atom, a hydroxyl group, etc., and R4 is a hydrogen atom, a halogen atom, a C1 to C4 alkyl group, etc., or R4 is in the 3-position of the phenyl and R3 and R4 join together to form a methylenedioxy group, R5 is a hydrogen atom or a fluorine atom, R6 is an ethylamino group, a dimethylamino group, etc., R7 is a C1 to C4 alkoxy group, and R8 is a C1 to C4 alkoxy group), or a pharmaceutically acceptable salt of this derivative. This is a novel compound that has antagonistic activity against an aruginine-vasopressin V1b receptor.

摘要翻译： 由式1表示的1,3-二氢-2H-吲哚-2-酮衍生物（其中，R 1为卤素原子，C 1〜C 4烷基等，R 2为氢原子，卤素原子等） ，或R2为吲哚-2-酮的6-位，R 1和R 2连接在一起形成C 3〜C 6亚烷基，R 3为卤素原子，羟基等，R 4为氢原子 卤素原子，C 1〜C 4烷基等，或者R 4在苯基的3-位，R3和R4连接在一起形成亚甲二氧基，R5是氢原子或氟原子，R6是 乙基氨基，二甲基氨基等，R7为C1〜C4烷氧基，R8为C1〜C4烷氧基）或该衍生物的药学上可接受的盐。 这是一种新的化合物，具有对抗葡萄糖酸加压素V1b受体的拮抗作用。