公开(公告)号：US20170217888A1

公开(公告)日：2017-08-03

申请号：US15515243

申请日：2015-10-23

申请人： Ono Pharmaceutical Co., Ltd

发明人： Kentaro YASHIRO ,  Daisuke WAKAMATSU ,  Tetsuji SAITO

IPC分类号： C07D213/61

CPC分类号： C07D213/61 ,  A61K31/17 ,  A61K31/341 ,  A61K31/351 ,  A61K31/381 ,  A61K31/4045 ,  A61K31/417 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/426 ,  A61K31/435 ,  A61K31/4545 ,  A61K31/4965 ,  A61K31/505 ,  C07C233/26 ,  C07C233/29 ,  C07C275/32 ,  C07C275/40 ,  C07D209/30 ,  C07D213/40 ,  C07D213/74 ,  C07D233/64 ,  C07D239/26 ,  C07D241/12 ,  C07D271/06 ,  C07D277/28 ,  C07D307/52 ,  C07D309/04 ,  C07D333/20 ,  C07D333/28 ,  C07D413/06

摘要： The present invention relates to a compound represented by the general formula (I) (wherein the definition of each group has the same meaning as described in the specification). The compound is useful as preventive and/or therapeutic agent for KCNQ2-5 channel-related diseases.

公开(公告)号：US20180289718A1

公开(公告)日：2018-10-11

申请号：US16005488

申请日：2018-06-11

申请人： ONO PHARMACEUTICAL CO., LTD.

发明人： Tetsuji SAITO ,  Masato HIGASHINO ,  Soichi KAWAHARADA ,  Arwel LEWIS ,  Mark Stuart CHAMBERS ,  Alastair RAE ,  Kim Louise HIRST ,  Charles David HARTLEY

IPC分类号： A61K31/5383 ,  C07D487/04 ,  A61K31/4439 ,  C07D519/00 ,  C07D498/04 ,  C07D473/32 ,  C07D471/04 ,  C07D413/12 ,  C07D401/12 ,  C07D413/14 ,  C07D401/14 ,  C07D403/12 ,  A61K31/437 ,  A61K31/4985 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/538 ,  A61K31/517 ,  A61K31/4709 ,  A61K45/06

摘要： The present invention provides compounds represented by formula (I), pharmaceutically acceptable salts thereof, N-oxides thereof, solvates thereof or prodrugs thereof (wherein the characters are as defined in the description). The compounds represented by formula (I) have affinity and selectivity for the gamma-aminobutyric acid A receptor subunit alpha 5 (GABAA α5) and act as GABAA α5 negative allosteric modulators (GABAA α5 NAM), so that they are useful in the prevention and/or treatment of diseases which are related to the GABAA α5 such as Alzheimer's disease.

公开(公告)号：US20160331757A1

公开(公告)日：2016-11-17

申请号：US15112647

申请日：2015-01-30

申请人： ONO PHARMACEUTICAL CO., LTD.

发明人： Tetsuji SAITO ,  Masato HIGASHINO ,  Soichi KAWAHARADA ,  Arwel LEWIS ,  Mark Stuart CHAMBERS ,  Alastair RAE ,  Kim Louise HIRST ,  Charles David HARTLEY

IPC分类号： A61K31/5383 ,  A61K31/538 ,  C07D471/04 ,  A61K31/517 ,  C07D487/04 ,  A61K31/4985 ,  C07D473/32 ,  C07D498/04 ,  C07D413/12 ,  C07D413/14 ,  C07D401/14 ,  A61K31/4439 ,  A61K31/423 ,  A61K31/4184 ,  C07D403/12 ,  C07D401/12 ,  A61K31/4709 ,  A61K31/437 ,  C07D519/00 ,  A61K45/06

CPC分类号： A61K31/5383 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/4985 ,  A61K31/517 ,  A61K31/538 ,  A61K45/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/12 ,  C07D413/14 ,  C07D471/04 ,  C07D473/32 ,  C07D487/04 ,  C07D498/04 ,  C07D519/00

摘要： The present invention provides compounds represented by formula (I), pharmaceutically acceptable salts thereof, N-oxides thereof, solvates thereof or prodrugs thereof (wherein the characters are as defined in the description). The compounds represented by formula (I) have affinity and selectivity for the gamma-aminobutyric acid A receptor subunit alpha 5 (GABAA α5) and act as GABAA α5 negative allosteric modulators (GABAA α5 NAM), so that they are useful in the prevention and/or treatment of diseases which are related to the GABAA α5 such as Alzheimer's disease.

摘要翻译： 本发明提供由式（I）表示的化合物，其药学上可接受的盐，其N-氧化物，其溶剂合物或其前药（其中字符如说明书中所定义）。 由式（I）表示的化合物对γ-氨基丁酸A受体亚基α5（GABAAα5）具有亲和性和选择性，并且作为GABAAα5负变构调节剂（GABAAα5NAM），因此它们可用于预防和 /或治疗与GABAAα5相关的疾病如阿尔茨海默病。

公开(公告)号：US20180346422A1

公开(公告)日：2018-12-06

申请号：US16059270

申请日：2018-08-09

申请人： Ono Pharmaceutical Co., Ltd.

发明人： Kentaro Yashiro ,  Daisuke WAKAMATSU ,  Tetsuji SAITO

IPC分类号： C07D213/61 ,  C07D307/52 ,  A61K31/17 ,  C07D213/40 ,  C07D209/30 ,  C07D277/28 ,  C07D271/06 ,  C07C233/29 ,  C07C233/26 ,  C07D241/12 ,  C07D413/06 ,  C07D239/26 ,  C07D233/64 ,  C07D333/28 ,  C07D333/20 ,  C07C275/40 ,  C07C275/32 ,  C07D309/04 ,  C07D213/74 ,  A61K31/505 ,  A61K31/4965 ,  A61K31/4545 ,  A61K31/435 ,  A61K31/426 ,  A61K31/4245 ,  A61K31/422 ,  A61K31/417 ,  A61K31/4045 ,  A61K31/381 ,  A61K31/351 ,  A61K31/341

摘要： The present invention relates to a compound represented by the general formula (I) (wherein the definition of each group has the same meaning as described in the specification). The compound is useful as preventive and/or therapeutic agent for KCNQ2-5 channel-related diseases.

公开(公告)号：US20200157050A1

公开(公告)日：2020-05-21

申请号：US16752076

申请日：2020-01-24

申请人： Ono Pharmaceutical Co., Ltd.

发明人： Kentaro YASHIRO ,  Daisuke WAKAMATSU ,  Tetsuji SAITO

IPC分类号： C07D213/61 ,  A61K31/17 ,  A61K31/341 ,  A61K31/351 ,  A61K31/381 ,  A61K31/4045 ,  A61K31/417 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/426 ,  A61K31/435 ,  A61K31/4545 ,  A61K31/4965 ,  A61K31/505 ,  C07D213/74 ,  C07D309/04 ,  C07C275/32 ,  C07C275/40 ,  C07D333/20 ,  C07D333/28 ,  C07D233/64 ,  C07D239/26 ,  C07D413/06 ,  C07D241/12 ,  C07C233/26 ,  C07C233/29 ,  C07D271/06 ,  C07D277/28 ,  C07D209/30 ,  C07D213/40 ,  C07D307/52

摘要： The present invention relates to a compound represented by the general formula (I) (wherein the definition of each group has the same meaning as described in the specification). The compound is useful as preventive and/or therapeutic agent for KCNQ2-5 channel-related diseases.

公开(公告)号：US20190135755A1

公开(公告)日：2019-05-09

申请号：US16095370

申请日：2017-04-21

申请人： ONO PHARMACEUTICAL CO., LTD.

发明人： Kentaro YASHIRO ,  Hideomi KIJIMA ,  Daisuke WAKAMATSU ,  Tetsuji SAITO

IPC分类号： C07D213/61 ,  A61P13/10 ,  A61K9/20

摘要： Crystal polymorphism may exist in a crystalline compound. In the case where crystal polymorphism exists, depending on the crystal form, solubility, dissolution rate, stability against heat, light, humidity, etc. or the like is different. Accordingly, in the production of a pharmaceutical product, it is a very important task to select a crystal form of a drug substance most suitable for a disease indication and a dosage form. The present invention relates to novel crystal forms (A crystal, W crystal, and a hydrate crystal (H crystal)) of a compound I having a strong opening action with respect to KCNQ2-5 channels.

公开(公告)号：US20190127320A1

公开(公告)日：2019-05-02

申请号：US16095374

申请日：2017-04-21

申请人： ONO PHARMACEUTICAL CO., LTD.

发明人： Kentaro YASHIRO ,  Masashi KATO ,  Tetsuji SAITO ,  Takuya OKADA ,  Daisuke WAKAMATSU ,  Adam James DAVENPORT ,  Christopher Charles STIMSON

IPC分类号： C07C275/32 ,  C07C271/30 ,  A61P13/02

CPC分类号： C07C275/32 ,  A61K31/17 ,  A61K31/27 ,  A61K31/341 ,  A61K31/351 ,  A61K31/4045 ,  A61K31/42 ,  A61K31/426 ,  A61K31/44 ,  A61K31/4545 ,  A61K31/4965 ,  A61K31/505 ,  A61P13/02 ,  A61P13/10 ,  C07C271/30 ,  C07C2602/08 ,  C07D209/14 ,  C07D213/40 ,  C07D213/64 ,  C07D213/74 ,  C07D239/26 ,  C07D241/12 ,  C07D261/08 ,  C07D277/28 ,  C07D307/52 ,  C07D309/04

摘要： An object of the present invention is to provide a novel compound having a strong opening action with respect to KCNQ2-5 channels. A compound represented by the general formula (1) (wherein the definition of each group is as described in the specification) is provided. The compound represented by the general formula (1) has a strong opening action with respect to KCNQ2-5 channels, and therefore is useful as a prophylactic and/or therapeutic agent for a KCNQ2-5 channel-related disease (for example, dysuria, overactive bladder, or the like).