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公开(公告)号：US20190231777A1
公开(公告)日：2019-08-01
申请号：US16376518
申请日：2019-04-05
发明人： Jun TAKEUCHI , Satoshi ITADANI , Kazuya HASHIMURA , Masahiro IKURA , Masato HIGASHINO , Tetsuya YASUHIRO , Takeshi NAGAURA
IPC分类号： A61K31/506 , C07D409/14 , A61P29/00 , C07D405/14 , C07D487/04 , C07D471/04 , C07D239/47 , C07D401/12 , C07D213/75 , C07D401/14 , A61K31/663 , A61K31/519 , A61K31/444 , A61K31/136 , A61K45/06 , A61K31/5377
摘要： The present invention provides a drug containing a compound having Trk-inhibiting activity as an active ingredient in prophylaxis and/or therapy for Trk-related diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease. A compound represented by the general formula (I), wherein all symbols represent the same meanings as described in the specification, a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof is useful as a drug component having Trk-inhibiting activity in prophylaxis and/or therapy of diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease.
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公开(公告)号：US20170240527A1
公开(公告)日：2017-08-24
申请号：US15504514
申请日：2015-08-17
发明人： Jun TAKEUCHI , Satoshi ITADANI , Masahiro IKURA , Masato HIGASHINO , Hideomi KIJIMA , Shizuka ONO , Tetsuya YASUHIRO , Takeshi NAGAURA
IPC分类号： C07D401/12 , A61K45/06 , C07C309/04 , A61K31/506 , C07C309/30 , C07C309/29
CPC分类号： C07D401/12 , A61K31/506 , A61K45/00 , A61K45/06 , C07B2200/13 , C07C309/04 , C07C309/29 , C07C309/30 , C07D401/14
摘要： In order to provide a prophylactic and/or therapeutic agent for Trk-related diseases, the present invention provides a compound which has a selective Trk-inhibiting activity and persistently inhibits NGF vascular hyper permeability and does not have a drug interaction and in addition thereto, is excellent in solubility and absorbability against free bases. The compound of the present invention has a selective Trk-inhibiting activity and persistently inhibits NGF vascular hyper permeability and does not have a drug interaction and is excellent in solubility and absorbability against free bases, and is therefore useful as a prophylactic and/or therapeutic agent for Trk-related diseases.
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公开(公告)号：US20160000783A1
公开(公告)日：2016-01-07
申请号：US14768727
申请日：2014-02-18
发明人： Jun TAKEUCHI , Satoshi ITADANI , Kazuya HASHIMURA , Masahiro IKURA , Masato HIGASHINO , Tetsuya YASUHIRO , Takeshi NAGAURA
IPC分类号： A61K31/506 , A61K45/06 , C07D401/12 , A61K31/444 , A61K31/519 , C07D409/14 , A61K31/5377 , C07D405/14 , C07D239/47 , C07D487/04 , C07D401/14 , C07D213/75
CPC分类号： A61K31/506 , A61K31/136 , A61K31/444 , A61K31/519 , A61K31/5377 , A61K31/663 , A61K45/06 , C07D213/75 , C07D239/47 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D471/04 , C07D487/04 , Y02A50/414
摘要： The present invention provides a drug containing a compound having Trk-inhibiting activity as an active ingredient in prophylaxis and/or therapy for Trk-related diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease. A compound represented by the general formula (I), wherein all symbols represent the same meanings as described in the specification, a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof is useful as a drug component having Trk-inhibiting activity in prophylaxis and/or therapy of diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease.
摘要翻译： 本发明提供了含有Trk-抑制活性的化合物作为预防和/或治疗Trk相关疾病如疼痛，瘙痒，下尿路功能障碍，哮喘，过敏性鼻炎，炎性肠病或查加斯的有效成分的药物 疾病。 由通式（I）表示的化合物，其中所有符号表示与说明书中所述相同的含义，其盐，其N-氧化物，其溶剂化物或其前药可用作具有Trk- 抑制预防和/或治疗诸如疼痛，瘙痒，下尿路功能障碍，哮喘，过敏性鼻炎，炎性肠病或恰加斯病等疾病的活性。
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公开(公告)号：US20180289718A1
公开(公告)日：2018-10-11
申请号：US16005488
申请日：2018-06-11
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.
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公开(公告)号：US20170340634A1
公开(公告)日：2017-11-30
申请号：US15679568
申请日：2017-08-17
发明人： Jun TAKEUCHI , Satoshi ITADANI , Kazuya HASHIMURA , Masahiro IKURA , Masato HIGASHINO , Tetsuya YASUHIRO , Takeshi NAGAURA
IPC分类号： A61K31/506 , C07D471/04 , C07D409/14 , C07D405/14 , C07D401/14 , C07D401/12 , A61K31/136 , C07D213/75 , A61K45/06 , A61K31/663 , A61K31/5377 , A61K31/519 , A61K31/444 , C07D239/47 , C07D487/04
CPC分类号： A61K31/506 , A61K31/136 , A61K31/444 , A61K31/519 , A61K31/5377 , A61K31/663 , A61K45/06 , C07D213/75 , C07D239/47 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D471/04 , C07D487/04 , Y02A50/414
摘要： The present invention provides a drug containing a compound having Trk-inhibiting activity as an active ingredient in prophylaxis and/or therapy for Trk-related diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease. A compound represented by the general formula (I), wherein all symbols represent the same meanings as described in the specification, a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof is useful as a drug component having Trk-inhibiting activity in prophylaxis and/or therapy of diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease.
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公开(公告)号：US20160331757A1
公开(公告)日：2016-11-17
申请号：US15112647
申请日：2015-01-30
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。
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公开(公告)号：US20180256573A1
公开(公告)日：2018-09-13
申请号：US15975130
申请日：2018-05-09
发明人： Jun TAKEUCHI , Satoshi ITADANI , Kazuya HASHIMURA , Masahiro IKURA , Masato HIGASHINO , Tetsuya YASUHIRO , Takeshi NAGAURA
IPC分类号： A61K31/506 , A61K31/5377 , A61K45/06 , C07D409/14 , C07D487/04 , C07D471/04 , C07D239/47 , C07D401/12 , C07D213/75 , C07D401/14 , A61K31/663 , A61K31/519 , A61K31/444 , A61K31/136 , C07D405/14
CPC分类号： A61K31/506 , A61K31/136 , A61K31/444 , A61K31/519 , A61K31/5377 , A61K31/663 , A61K45/06 , C07D213/75 , C07D239/47 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D471/04 , C07D487/04 , Y02A50/414
摘要： The present invention provides a drug containing a compound having Trk-inhibiting activity as an active ingredient in prophylaxis and/or therapy for Trk-related diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease. A compound represented by the general formula (I), wherein all symbols represent the same meanings as described in the specification, a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof is useful as a drug component having Trk-inhibiting activity in prophylaxis and/or therapy of diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease.
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公开(公告)号：US20170027939A1
公开(公告)日：2017-02-02
申请号：US15291700
申请日：2016-10-12
发明人： Jun TAKEUCHI , Satoshi ITADANI , Kazuya HASHIMURA , Masahiro IKURA , Masato HIGASHINO , Tetsuya YASUHIRO , Takeshi NAGAURA
IPC分类号： A61K31/506
CPC分类号： A61K31/506 , A61K31/136 , A61K31/444 , A61K31/519 , A61K31/5377 , A61K31/663 , A61K45/06 , C07D213/75 , C07D239/47 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D471/04 , C07D487/04 , Y02A50/414
摘要： The present invention provides a drug containing a compound having Trk-inhibiting activity as an active ingredient in prophylaxis and/or therapy for Trk-related diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease. A compound represented by the general formula (I), wherein all symbols represent the same meanings as described in the specification, a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof is useful as a drug component having Trk-inhibiting activity in prophylaxis and/or therapy of diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease.
摘要翻译： 本发明提供了含有Trk-抑制活性的化合物作为预防和/或治疗Trk相关疾病如疼痛，瘙痒，下尿路功能障碍，哮喘，过敏性鼻炎，炎性肠病或查加斯的有效成分的药物 疾病。 由通式（I）表示的化合物：其中所有符号表示与说明书中所述相同的含义，其盐，其N-氧化物，其溶剂化物或其前药可用作具有Trk- 抑制预防和/或治疗诸如疼痛，瘙痒，下尿路功能障碍，哮喘，过敏性鼻炎，炎性肠病或恰加斯病等疾病的活性。
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公开(公告)号：US20160280684A1
公开(公告)日：2016-09-29
申请号：US15173161
申请日：2016-06-03
发明人： Jun TAKEUCHI , Satoshi ITADANI , Kazuya HASHIMURA , Masahiro IKURA , Masato HIGASHINO , Tetsuya YASUHIRO , Takeshi NAGAURA
IPC分类号： C07D401/14
CPC分类号： A61K31/506 , A61K31/136 , A61K31/444 , A61K31/519 , A61K31/5377 , A61K31/663 , A61K45/06 , C07D213/75 , C07D239/47 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D471/04 , C07D487/04 , Y02A50/414
摘要： The present invention provides a drug containing a compound having Trk-inhibiting activity as an active ingredient in prophylaxis and/or therapy for Trk-related diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease. A compound represented by the general formula (I), wherein all symbols represent the same meanings as described in the specification, a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof is useful as a drug component having Trk-inhibiting activity in prophylaxis and/or therapy of diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease.
摘要翻译： 本发明提供了含有Trk-抑制活性的化合物作为预防和/或治疗Trk相关疾病如疼痛，瘙痒，下尿路功能障碍，哮喘，过敏性鼻炎，炎性肠病或查加斯的有效成分的药物 疾病。 由通式（I）表示的化合物：其中所有符号表示与说明书中所述相同的含义，其盐，其N-氧化物，其溶剂化物或其前药可用作具有Trk- 抑制预防和/或治疗诸如疼痛，瘙痒，下尿路功能障碍，哮喘，过敏性鼻炎，炎性肠病或恰加斯病等疾病的活性。
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