公开(公告)号：EP2695881A1

公开(公告)日：2014-02-12

申请号：EP12758359.9

申请日：2012-03-13

申请人： Astellas Pharma Inc.

发明人： YOSHIHARA, Kousei ,  SUZUKI, Daisuke ,  YAMAKI, Susumu ,  YAMADA, Hiroyoshi ,  MIHARA, Hisashi ,  SEKI, Norio

IPC分类号： C07D205/04 ,  A61K31/426 ,  A61K31/4402 ,  A61K31/4545 ,  A61K31/495 ,  A61K31/496 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/551 ,  A61P1/02 ,  A61P1/04 ,  A61P1/16 ,  A61P3/04 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  A61P11/00

CPC分类号： 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

摘要： [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.

摘要翻译： 本发明提供可用作药物组合物的有效成分的化合物，特别是用于预防和/或治疗VAP-1相关疾病的药物组合物。 [解决方法]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显示优异的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。 另外，本发明涉及含有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。

公开(公告)号：EP1923387B1

公开(公告)日：2011-10-19

申请号：EP06782418.5

申请日：2006-08-07

申请人： Astellas Pharma Inc.

发明人： YAMADA, Hiroyoshi ,  ITAHANA, Hirotsune ,  MORITOMO, Ayako ,  MATSUZAWA, Takaho ,  NOZAWA, Eisuke ,  AKUZAWA, Shinobu ,  HARADA, Koichiro

IPC分类号： C07D209/88 ,  A61K31/381 ,  A61K31/385 ,  A61K31/403 ,  A61K31/407 ,  A61K31/435 ,  A61K31/437 ,  A61K31/438 ,  A61K31/454 ,  A61K31/5377 ,  A61K31/538 ,  A61P1/00 ,  A61P25/06 ,  A61P43/00 ,  C07D221/16 ,  C07D265/38 ,  C07D333/78 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04

CPC分类号： C07D209/88 ,  C07D221/16 ,  C07D265/38 ,  C07D333/78 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D405/06 ,  C07D413/04 ,  C07D413/06 ,  C07D471/04 ,  C07D491/10 ,  C07D495/10

摘要： It is intended to provide a compound which can be used for preventing and/or treating a disease associated with 5HT2B receptor and 5HT7 receptor, particularly for treating irritable bowel syndrome (IBS) and/or preventing migraine. It was found that an acylguanidine derivative characterized by having a tricyclic structure or a pharmaceutically acceptable salt thereof has a strong antagonism to 5HT2B receptor and 5HT7 receptor. In addition, the compound of the invention having the antagonism to both receptors showed a better pharmacological action compared to the case where an antagonist selective to one of the receptors was solely used. From the above results, the compound of the invention is useful for preventing and/or treating a disease associated with 5HT2B receptor and 5HT7 receptor, particularly for treating irritable bowel syndrome (IBS) and/or preventing migraine.

摘要翻译： 旨在提供可用于预防和/或治疗与5HT2B受体和5HT7受体有关的疾病，特别是用于治疗过敏性肠综合征（IBS）和/或预防偏头痛的化合物。 发现特征在于具有三环结构的酰基胍衍生物或其药学上可接受的盐对5HT2B受体和5HT7受体具有强烈的拮抗作用。 另外，与单独使用对一种受体有选择性的拮抗剂的情况相比，对两种受体具有拮抗作用的本发明化合物显示出更好的药理作用。 根据上述结果，本发明化合物可用于预防和/或治疗与5HT2B受体和5HT7受体有关的疾病，特别是用于治疗肠易激综合征（IBS）和/或预防偏头痛。

公开(公告)号：EP1923387A1

公开(公告)日：2008-05-21

申请号：EP06782418.5

申请日：2006-08-07

申请人： Astellas Pharma Inc.

发明人： YAMADA, Hiroyoshi ,  ITAHANA, Hirotsune ,  MORITOMO, Ayako ,  MATSUZAWA, Takaho ,  NOZAWA, Eisuke ,  AKUZAWA, Shinobu ,  HARADA, Koichiro

IPC分类号： C07D209/88 ,  A61K31/381 ,  A61K31/385 ,  A61K31/403 ,  A61K31/407 ,  A61K31/435 ,  A61K31/437 ,  A61K31/438 ,  A61K31/454 ,  A61K31/5377 ,  A61K31/538 ,  A61P1/00 ,  A61P25/06 ,  A61P43/00 ,  C07D221/16 ,  C07D265/38 ,  C07D333/78 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04

CPC分类号： C07D209/88 ,  C07D221/16 ,  C07D265/38 ,  C07D333/78 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D405/06 ,  C07D413/04 ,  C07D413/06 ,  C07D471/04 ,  C07D491/10 ,  C07D495/10

摘要： [Problem] To provide a compound which can be used in the prevention and/or treatment of diseases in which S-HT 2B receptor and 5-HT 7 receptor are concerned, particularly in the treatment of irritable bowel syndrome (IBS) and/or prevention of migraine. [Means for Resolution] It was found that an acylguanidine derivative having a tricyclic structure or a pharmaceutically acceptable salt thereof has a strong antagonism to 5-HT 2B receptor and 5-HT 7 receptor. In addition, the compound of the present invention having antagonism to both of the receptors showed superior pharmacological action in comparison with the case of the single use of an antagonist selective for either one of the receptors. Based on the above, the compound of the present invention is useful in preventing and/or treating diseases in which 5-HT 2B receptor and 5-HT 7 receptor are concerned, particularly in treating irritable bowel syndrome (IBS) and/or preventing migraine.

摘要翻译： [问题]提供可用于预防和/或治疗其中涉及S-HT2B受体和5-HT7受体的疾病的化合物，特别是用于治疗肠易激综合征（IBS）和/或预防 偏头痛。 [解决手段]发现具有三环结构的酰基胍衍生物或其药学上可接受的盐对5-HT 2B受体和5-HT 7受体具有强烈的拮抗作用。 此外，与单独使用对任何一种受体具有选择性的拮抗剂的情况相比，对两种受体都具有拮抗作用的本发明化合物显示出优良的药理学作用。 基于上述，本发明化合物可用于预防和/或治疗其中涉及5-HT2B受体和5-HT7受体的疾病，特别是在治疗肠易激综合征（IBS）和/或预防偏头痛方面。

公开(公告)号：EP3002278A1

公开(公告)日：2016-04-06

申请号：EP15191536.0

申请日：2012-03-13

申请人： Astellas Pharma Inc.

发明人： YOSHIHARA, Kousei ,  SUZUKI, Daisuke ,  YAMAKI, Susumu ,  YAMADA, Hiroyoshi ,  MIHARA, Hisashi ,  SEKI, Norio

IPC分类号： C07D205/04 ,  A61K31/426 ,  A61K31/4402 ,  A61K31/4545 ,  A61K31/495 ,  A61K31/496 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/551 ,  A61P1/02 ,  A61P1/04 ,  A61P1/16 ,  A61P3/04 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  A61P11/00

CPC分类号： 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

摘要： [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.

公开(公告)号：EP1852129A1

公开(公告)日：2007-11-07

申请号：EP06713158.1

申请日：2006-02-07

申请人： Astellas Pharma Inc.

发明人： AKUZAWA, Shinobu ,  ITO, Hiroyuki ,  WATANABE, Toshihiro ,  YAMADA, Hiroyoshi

IPC分类号： A61K45/00 ,  A61K31/166 ,  A61K31/343 ,  A61K31/351 ,  A61K31/352 ,  A61K31/385 ,  A61K31/41 ,  A61K31/4168 ,  A61K31/4196 ,  A61K31/421 ,  A61K31/426 ,  A61K45/06 ,  A61P1/04 ,  C07D233/88 ,  C07D249/14 ,  C07D257/06 ,  C07D263/28 ,  C07D277/18 ,  C07D277/20 ,  C07D277/38 ,  C07D277/46

CPC分类号： A61K31/438 ,  A61K31/085 ,  A61K31/16 ,  A61K31/166 ,  A61K31/215 ,  A61K31/343 ,  A61K31/351 ,  A61K31/352 ,  A61K31/385 ,  A61K31/403 ,  A61K31/41 ,  A61K31/4168 ,  A61K31/4196 ,  A61K31/421 ,  A61K31/426 ,  A61K45/06 ,  C07D209/54 ,  C07D221/20 ,  C07D233/88 ,  C07D249/14 ,  C07D257/06 ,  C07D263/28 ,  C07D277/18 ,  C07D303/06 ,  C07D305/14 ,  C07D307/94 ,  C07D319/14 ,  C07D327/02 ,  C07D333/50 ,  C07D335/04 ,  A61K2300/00

摘要： The invention relates to a medicament for IBS, which comprises a dual antagonist for 5-HT 2B and 5-HT 7 receptors having selective binding affinities for 5-HT 2B and 5-HT 7 receptors.
The pharmaceutical composition of the invention is useful as a drug which is excellent in the therapeutic effect on IBS and shows lessened side effects occurring in the existing remedies for IBS, because it showed good pharmacological actions in comparison with the case of independently using a 5-HT 2B receptor antagonist having selective binding affinity for 5-HT 2B receptor or a 5-HT 7 receptor antagonist having selective binding affinity for 5-HT 7 receptor.

摘要翻译： 本发明涉及用于IBS的药物，其包含对5-HT 2B和5-HT 7受体具有选择性结合亲和力的5-HT 2B和5-HT 7受体的双重拮抗剂。 本发明的药物组合物作为对IBS的治疗效果优异的药物是有用的，并且在IBS的现有疗法中显示减轻的副作用，因为与独立使用5- 具有对5-HT 2B受体的选择性结合亲和力的HT 2B受体拮抗剂或对5-HT 7受体具有选择性结合亲和力的5-HT 7受体拮抗剂。

公开(公告)号：EP3795590A1

公开(公告)日：2021-03-24

申请号：EP19804452.1

申请日：2019-05-17

申请人： Astellas Pharma Inc.

发明人： ASANO, Toru ,  SANO, Yorikata ,  MORINAKA, Akifumi ,  SHIRAI, Hiroki ,  HIRAYAMA, Kazunori ,  AKAIWA, Michinori ,  YAMADA, Hiroyoshi ,  SHIRAISHI, Nobuyuki

IPC分类号： C07K16/28 ,  A61K31/16 ,  A61K31/395 ,  A61K39/395 ,  A61K47/65 ,  A61K47/68 ,  A61K51/10 ,  A61P1/00 ,  A61P1/04 ,  A61P1/18 ,  A61P5/14 ,  A61P11/00 ,  A61P13/10 ,  A61P13/12 ,  A61P15/00 ,  A61P17/00 ,  A61P35/00 ,  C12N15/13 ,  A61K103/00

摘要： Provided are a conjugate comprising an anti-human MUC1 antibody Fab fragment and a peptide linker and/or a ligand, a composition for diagnosis and/or a pharmaceutical composition comprising the conjugate, a method for diagnosing and/or treating a cancer using the conjugate, and the like. In the conjugate used, the anti-human MUC1 antibody Fab fragment is bound to the ligand via the peptide linker or the like.

公开(公告)号：EP3002278B1

公开(公告)日：2017-04-19

申请号：EP15191536.0

申请日：2012-03-13

申请人： Astellas Pharma Inc.

发明人： YOSHIHARA, Kousei ,  SUZUKI, Daisuke ,  YAMAKI, Susumu ,  YAMADA, Hiroyoshi ,  MIHARA, Hisashi ,  SEKI, Norio

IPC分类号： C07D205/04 ,  A61K31/426 ,  A61K31/4402 ,  A61K31/4545 ,  A61K31/495 ,  A61K31/496 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/551 ,  A61P1/02 ,  A61P1/04 ,  A61P1/16 ,  A61P3/04 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  A61P11/00

CPC分类号： 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

公开(公告)号：EP1988075B1

公开(公告)日：2012-01-25

申请号：EP07714469.9

申请日：2007-02-19

申请人： Astellas Pharma Inc.

发明人： SEO, Ryushi ,  KAKU, Hidetaka ,  YAMADA, Hiroyoshi ,  KAGA, Daisuke ,  AKUZAWA, Shinobu

IPC分类号： C07D207/34 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/404 ,  A61K31/422 ,  A61K31/433 ,  A61K31/439 ,  A61K31/454 ,  A61K31/4725 ,  A61P1/00 ,  A61P43/00 ,  C07D401/04 ,  C07D401/10 ,  C07D403/04 ,  C07D407/04 ,  C07D409/04 ,  C07D409/12 ,  C07D413/04 ,  C07D417/04 ,  C07D453/02

CPC分类号： C07D207/34 ,  C07D401/04 ,  C07D401/10 ,  C07D403/04 ,  C07D407/04 ,  C07D409/04 ,  C07D409/12 ,  C07D413/04 ,  C07D417/04 ,  C07D453/02

摘要： [PROBLEMS] To provide a compound which can be used for the prevention and/or treatment of a disease associated with a 5-HT2B receptor or a 5-HT7 receptor, particularly for the treatment of irritable bowel syndrome (IBS). [MEANS FOR SOLVING PROBLEMS] It is found that a pyrrole derivative having a guanidinocarbonyl group or an amide group at position-3 as a substituent or a pharmaceutically acceptable salt thereof has a potent antagonistic effect on both of a 5-HT2B receptor and a 5-HT7 receptor. The compound shows a better pharmacological activity compared to an antagonist which is selective to either of these receptors. Therefore, the compound is useful for the prevention and/or treatment of a disease associated with a 5-HT2B receptor or a 5-HT7 receptor, particularly for the treatment of irritable bowel syndrome (IBS).

公开(公告)号：EP1988075A1

公开(公告)日：2008-11-05

申请号：EP07714469.9

申请日：2007-02-19

申请人： Astellas Pharma Inc.

发明人： SEO, Ryushi ,  KAKU, Hidetaka ,  YAMADA, Hiroyoshi ,  KAGA, Daisuke ,  AKUZAWA, Shinobu

IPC分类号： C07D207/34 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/404 ,  A61K31/422 ,  A61K31/433 ,  A61K31/439 ,  A61K31/454 ,  A61K31/4725 ,  A61P1/00 ,  A61P43/00 ,  C07D401/04 ,  C07D401/10 ,  C07D403/04 ,  C07D407/04 ,  C07D409/04 ,  C07D409/12 ,  C07D413/04 ,  C07D417/04 ,  C07D453/02

CPC分类号： C07D207/34 ,  C07D401/04 ,  C07D401/10 ,  C07D403/04 ,  C07D407/04 ,  C07D409/04 ,  C07D409/12 ,  C07D413/04 ,  C07D417/04 ,  C07D453/02

摘要： [Problem] To provide a compound which may be used for the prevention and/or treatment of diseases in which 5-HT 2B receptor and 5-HT 7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS).
[Means for Resolution] It was found that a pyrrole derivative characterized by the possession of a guanidinocarbonyl group or amido group as a substituent group at the 3-position, or a pharmaceutically acceptable salt thereof, has a strong antagonism for both of the 5-HT 2B receptor and 5-HT 7 receptor. In addition, the compound of the present invention having the antagonistic activity for both of the receptors showed a good pharmacological action in comparison with the case in which an antagonist selective for either one of the receptors was used alone. Based on the above, the compound of the present invention is useful for the prevention and/or treatment of diseases in which 5-HT 2B receptor and 5-HT 7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS).

摘要翻译： [问题]提供可用于预防和/或治疗涉及5-HT 2B受体和5-HT 7受体的疾病的化合物，特别是用于治疗肠易激综合征（IBS）。 [解决方法]发现特征在于3-位的胍基羰基或酰胺基作为取代基的吡咯衍生物或其药学上可接受的盐对5- HT 2B受体和5-HT 7受体。 此外，与对于任一种受体选择性拮抗剂单独使用的情况相比，具有对两种受体具有拮抗作用的本发明化合物显示出良好的药理作用。 基于上述，本发明的化合物可用于预防和/或治疗涉及5-HT 2B受体和5-HT 7受体的疾病，特别是用于治疗肠易激综合征（IBS）。

公开(公告)号：EP3904331A1

公开(公告)日：2021-11-03

申请号：EP19903140.2

申请日：2019-12-27

申请人： Astellas Pharma Inc. ,  RIKEN ,  NATIONAL INSTITUTES FOR QUANTUM AND RADIOLOGICAL SCIENCE AND TECHNOLOGY

发明人： MIZUTANI, Tsuyoshi ,  YAMADA, Hiroyoshi ,  TOYA, Hiroki ,  FUJIKAWA, Akihiko ,  YOSHIMURA, Seiji ,  KIKUCHI, Shigetoshi ,  MIYAJIMA, Daigo ,  TAKEUCHI, Toshiaki ,  AIDA, Takuzo ,  AOKI, Ichio

IPC分类号： C07C211/63 ,  C07C211/64 ,  C07C309/13 ,  C07D207/06 ,  C07D211/34 ,  C07D211/62 ,  C07D217/10 ,  B82Y15/00 ,  A61K49/06 ,  C07F9/38

摘要： Provided is a novel nanoparticle, a contrast agent for magnetic resonance imaging containing the same, and a zwitterionic ligand compound used in production of the nanoparticle. The contrast agent for MRI of the present invention can be suitably used as a contrast agent for MRI in a medical field. The nanoparticle and the zwitterionic ligand compound of the present invention are applicable to various pharmaceutical compositions and the like, including a contrast agent for MRI, and can be used widely in the fields of pharmaceuticals, biotechnology, and the like, including various diagnosis methods and examination reagents.