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公开(公告)号：US20150203480A1
公开(公告)日：2015-07-23
申请号：US14671397
申请日：2015-03-27
Applicant: Astellas Pharma Inc.
Inventor： Kousei Yoshihara , Daisuke Suzuki , Susumu Yamaki , Hiroyoshi Yamada , Hisashi Mihara , Norio Seki
IPC: C07D413/12 , C07D213/74 , C07D295/192 , C07D403/12 , C07D239/34 , C07D239/42 , C07D401/04
CPC classification number: C07D413/12 , A61K31/4412 , C07D205/04 , C07D211/60 , C07D211/78 , C07D213/38 , C07D213/64 , C07D213/74 , C07D217/06 , C07D217/22 , C07D237/20 , C07D239/26 , C07D239/34 , C07D239/42 , C07D239/48 , C07D241/20 , C07D267/10 , C07D277/42 , C07D277/46 , C07D277/56 , C07D295/06 , C07D295/08 , C07D295/18 , C07D295/192 , C07D295/20 , C07D309/08 , C07D309/14 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/04 , C07D413/14
Abstract: [Problem]The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases.[Means for Solution]The present inventors have conducted intensive studies on a compound having a VAP-1 inhibitory activity, and as a result, they have found that the compound or a salt thereof of the present invention exhibits an excellent VAP-1 inhibitory activity and is useful for preventing and/or treating VAP-1-related diseases, in particular, diabetic nephropathy or diabetic macular edema, thereby completing the present invention. In addition, the present invention relates to a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases, which comprises the compound or a salt thereof of the present invention, and an excipient.
Abstract translation: [问题]本发明提供了作为药物组合物的活性成分，特别是用于预防和/或治疗VAP-1相关疾病的药物组合物有用的化合物。 [解决方案]本发明人对具有VAP-1抑制活性的化合物进行了深入研究，结果发现本发明的化合物或其盐表现出优异的VAP-1抑制活性 并且可用于预防和/或治疗VAP-1相关疾病，特别是糖尿病性肾病或糖尿病性黄斑水肿，从而完成本发明。 此外，本发明涉及包含本发明的化合物或其盐和赋形剂的药物组合物，特别是用于预防和/或治疗VAP-1相关疾病的药物组合物。
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公开(公告)号：US10301286B2
公开(公告)日：2019-05-28
申请号：US15749375
申请日：2016-08-02
Applicant: Astellas Pharma Inc.
Inventor： Takashi Sugane , Takuya Makino , Daisuke Yamashita , Yasuhiro Yonetoku , Daisuke Tanabe , Hisashi Mihara , Norio Asai , Kazuhiko Osoda , Takafumi Shimizu , Hiroyuki Moritomo , Keizo Sugasawa , Kyoichi Maeno , Naomi Hosogai
IPC: C07D403/06 , C07D401/14 , C07D405/14 , A61K31/496 , A61K31/501 , C07D403/14 , C07D409/14 , C07D417/14 , A61P13/02 , A61P13/10
Abstract: To provide a compound which can be used as an MC4 receptor agonist.The present inventors have investigated MC4 receptor agonists, and have found that a piperazine derivative has an action related to the agonists, thereby completing the present invention. That is, the piperazine derivative of the present invention has an MC4 receptor agonistic action, and can be used as an agent for preventing or treating bladder and/or urinary tract diseases, in particular, underactive bladder, hypotonic bladder, acontractile bladder, detrusor underactivity, neurogenic bladder, urethral relaxation failure, detrusor-external urethral sphincter dyssynergia, and voiding dysfunctions in benign prostatic hyperplasia.
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Patent Agency Ranking
公开(公告)号：US09051283B2
公开(公告)日：2015-06-09
申请号：US14099131
申请日：2013-12-06
Applicant: Astellas Pharma Inc.
Inventor： Kousei Yoshihara , Daisuke Suzuki , Susumu Yamaki , Hiroyoshi Yamada , Hisashi Mihara , Norio Seki
IPC: C07D401/12 , A61K31/4412 , C07D267/10 , C07D205/04 , C07D211/60 , C07D211/78 , C07D213/38 , C07D213/64 , C07D213/74 , C07D217/06 , C07D217/22 , C07D237/20 , C07D239/26 , C07D239/42 , C07D241/20 , C07D277/42 , C07D277/46 , C07D277/56 , C07D295/06 , C07D295/08 , C07D295/18 , C07D295/20 , C07D309/08 , C07D309/14 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/14 , C07D239/48
CPC classification number: C07D413/12 , A61K31/4412 , C07D205/04 , C07D211/60 , C07D211/78 , C07D213/38 , C07D213/64 , C07D213/74 , C07D217/06 , C07D217/22 , C07D237/20 , C07D239/26 , C07D239/34 , C07D239/42 , C07D239/48 , C07D241/20 , C07D267/10 , C07D277/42 , C07D277/46 , C07D277/56 , C07D295/06 , C07D295/08 , C07D295/18 , C07D295/192 , C07D295/20 , C07D309/08 , C07D309/14 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/04 , C07D413/14
Abstract: [Problem]The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases.[Means for Solution]The present inventors have conducted intensive studies on a compound having a VAP-1 inhibitory activity, and as a result, they have found that the compound or a salt thereof of the present invention exhibits an excellent VAP-1 inhibitory activity and is useful for preventing and/or treating VAP-1-related diseases, in particular, diabetic nephropathy or diabetic macular edema, thereby completing the present invention. In addition, the present invention relates to a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases, which comprises the compound or a salt thereof of the present invention, and an excipient.
Abstract translation: [问题]本发明提供了作为药物组合物的活性成分，特别是用于预防和/或治疗VAP-1相关疾病的药物组合物有用的化合物。 [解决方案]本发明人对具有VAP-1抑制活性的化合物进行了深入研究，结果发现本发明的化合物或其盐表现出优异的VAP-1抑制活性 并且可用于预防和/或治疗VAP-1相关疾病，特别是糖尿病性肾病或糖尿病性黄斑水肿，从而完成本发明。 此外，本发明涉及包含本发明的化合物或其盐和赋形剂的药物组合物，特别是用于预防和/或治疗VAP-1相关疾病的药物组合物。
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公开(公告)号：US09844549B2
公开(公告)日：2017-12-19
申请号：US15506561
申请日：2015-08-25
Applicant: ASTELLAS PHARMA INC.
Inventor： Taisuke Takahashi , Hiroaki Tanaka , Michinori Akaiwa , Kenji Negoro , Hisashi Mihara , Hideyoshi Fuji , Hajime Takamatsu
IPC: C07D417/14 , A61K31/506 , A61K31/496 , A61K31/4439 , C07D417/12
CPC classification number: A61K31/496 , A61K31/4439 , A61K31/506 , C07D417/12 , C07D417/14
Abstract: A compound which is useful as an active ingredient for a pharmaceutical composition for treating urine storage dysfunction, voiding dysfunction, lower urinary tract dysfunction, and the like. The present inventors have found that a 2-aminothiazole derivative has an excellent muscarinic M3 receptor-positive allosteric modulator activity and is expected as an agent for preventing or treating bladder/urinary tract diseases associated with bladder contractions via a muscarinic M3 receptor, thereby completing the present invention. 2-aminothiazole derivative or a salt thereof of the present invention is expected as an agent for preventing or treating bladder/urinary tract diseases associated with bladder contractions via a muscarinic M3 receptor, for example voiding dysfunction such as underactive bladder.
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公开(公告)号：US09556160B2
公开(公告)日：2017-01-31
申请号：US14671397
申请日：2015-03-27
Applicant: Astellas Pharma Inc.
Inventor： Kousei Yoshihara , Daisuke Suzuki , Susumu Yamaki , Hiroyoshi Yamada , Hisashi Mihara , Norio Seki
IPC: C07D413/04 , C07D401/12 , A61K31/5377 , A61K31/4412 , C07D413/12 , C07D205/04 , C07D211/60 , C07D211/78 , C07D213/38 , C07D213/64 , C07D213/74 , C07D217/06 , C07D217/22 , C07D237/20 , C07D239/26 , C07D239/42 , C07D241/20 , C07D277/42 , C07D277/46 , C07D277/56 , C07D295/06 , C07D295/08 , C07D295/18 , C07D295/20 , C07D309/08 , C07D309/14 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/14 , C07D239/48 , C07D267/10 , C07D239/34 , C07D295/192
CPC classification number: C07D413/12 , A61K31/4412 , C07D205/04 , C07D211/60 , C07D211/78 , C07D213/38 , C07D213/64 , C07D213/74 , C07D217/06 , C07D217/22 , C07D237/20 , C07D239/26 , C07D239/34 , C07D239/42 , C07D239/48 , C07D241/20 , C07D267/10 , C07D277/42 , C07D277/46 , C07D277/56 , C07D295/06 , C07D295/08 , C07D295/18 , C07D295/192 , C07D295/20 , C07D309/08 , C07D309/14 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/04 , C07D413/14
Abstract: [Problem]The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases.[Means for Solution]The present inventors have conducted intensive studies on a compound having a VAP-1 inhibitory activity, and as a result, they have found that the compound or a salt thereof of the present invention exhibits an excellent VAP-1 inhibitory activity and is useful for preventing and/or treating VAP-1-related diseases, in particular, diabetic nephropathy or diabetic macular edema, thereby completing the present invention. In addition, the present invention relates to a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases, which comprises the compound or a salt thereof of the present invention, and an excipient.
Abstract translation: 本发明人对具有VAP-1抑制活性的化合物进行了深入研究，结果发现本发明的化合物或其盐表现出优异的VAP-1抑制活性，可用于预防 和/或治疗VAP-1相关疾病，特别是糖尿病性肾病或糖尿病性黄斑水肿，从而完成本发明。 此外，本发明涉及包含本发明的化合物或其盐和赋形剂的药物组合物，特别是用于预防和/或治疗VAP-1相关疾病的药物组合物。
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公开(公告)号：US08716470B2
公开(公告)日：2014-05-06
申请号：US13755822
申请日：2013-01-31
Applicant: Astellas Pharma Inc.
Inventor： Kousei Yoshihara , Daisuke Suzuki , Susumu Yamaki , Hiroyoshi Yamada , Hisashi Mihara , Norio Seki
IPC: C07D417/04 , A61K31/5377
CPC classification number: C07D413/12 , A61K31/4412 , C07D205/04 , C07D211/60 , C07D211/78 , C07D213/38 , C07D213/64 , C07D213/74 , C07D217/06 , C07D217/22 , C07D237/20 , C07D239/26 , C07D239/34 , C07D239/42 , C07D239/48 , C07D241/20 , C07D267/10 , C07D277/42 , C07D277/46 , C07D277/56 , C07D295/06 , C07D295/08 , C07D295/18 , C07D295/192 , C07D295/20 , C07D309/08 , C07D309/14 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/04 , C07D413/14
Abstract: [Problem]The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases.[Means for Solution]The present inventors have conducted intensive studies on a compound having a VAP-1 inhibitory activity, and as a result, they have found that the compound or a salt thereof of the present invention exhibits an excellent VAP-1 inhibitory activity and is useful for preventing and/or treating VAP-1-related diseases, in particular, diabetic nephropathy or diabetic macular edema, thereby completing the present invention. In addition, the present invention relates to a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases, which comprises the compound or a salt thereof of the present invention, and an excipient.
Abstract translation: [问题]本发明提供了作为药物组合物的活性成分，特别是用于预防和/或治疗VAP-1相关疾病的药物组合物有用的化合物。 [解决方案]本发明人对具有VAP-1抑制活性的化合物进行了深入研究，结果发现本发明的化合物或其盐表现出优异的VAP-1抑制活性 并且可用于预防和/或治疗VAP-1相关疾病，特别是糖尿病性肾病或糖尿病性黄斑水肿，从而完成本发明。 此外，本发明涉及包含本发明的化合物或其盐和赋形剂的药物组合物，特别是用于预防和/或治疗VAP-1相关疾病的药物组合物。
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公开(公告)号：US20130143860A1
公开(公告)日：2013-06-06
申请号：US13755822
申请日：2013-01-31
Applicant: Astellas Pharma Inc.
Inventor： Kousei YOSHIHARA , Daisuke Suzuki , Susumu Yamaki , Hiroyoshi Yamada , Hisashi Mihara , Norio Seki
IPC: A61K31/5377 , C07D401/14 , C07D403/14 , A61K31/506 , C07D413/14
CPC classification number: C07D413/12 , A61K31/4412 , C07D205/04 , C07D211/60 , C07D211/78 , C07D213/38 , C07D213/64 , C07D213/74 , C07D217/06 , C07D217/22 , C07D237/20 , C07D239/26 , C07D239/34 , C07D239/42 , C07D239/48 , C07D241/20 , C07D267/10 , C07D277/42 , C07D277/46 , C07D277/56 , C07D295/06 , C07D295/08 , C07D295/18 , C07D295/192 , C07D295/20 , C07D309/08 , C07D309/14 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/04 , C07D413/14
Abstract: [Problem]The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases.[Means for Solution]The present inventors have conducted intensive studies on a compound having a VAP-1 inhibitory activity, and as a result, they have found that the compound or a salt thereof of the present invention exhibits an excellent VAP-1 inhibitory activity and is useful for preventing and/or treating VAP-1-related diseases, in particular, diabetic nephropathy or diabetic macular edema, thereby completing the present invention. In addition, the present invention relates to a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases, which comprises the compound or a salt thereof of the present invention, and an excipient.
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