公开(公告)号：EP1932832A1

公开(公告)日：2008-06-18

申请号：EP06811388.5

申请日：2006-10-06

申请人： Astellas Pharma Inc.

发明人： SATO, Junji ,  HATTORI, Kazuyuki ,  KUBOTA, Hirokazu ,  MUNAKATA, Ryosuke ,  ASANO, Toru ,  MAEDA, Junko ,  KAWAKAMI, Masakatsu ,  KAMIKAWA, Akio

IPC分类号： C07D213/79 ,  A61K31/381 ,  A61K31/4025 ,  A61K31/404 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/42 ,  A61K31/425 ,  A61K31/426 ,  A61K31/427 ,  A61K31/4418 ,  A61K31/443 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4535

CPC分类号： C07D213/79 ,  C07D231/14 ,  C07D261/18 ,  C07D275/03 ,  C07D277/56 ,  C07D333/38 ,  C07D333/60 ,  C07D333/76 ,  C07D401/10 ,  C07D405/10 ,  C07D409/10 ,  C07D413/10 ,  C07D417/10

摘要： It is intended to provide an agent for treating or preventing hyperuricemia, gout, inflammatory bowel disease, diabetic nephropathy, diabetic retinopathy and so on which has a non-nucleic acid structure and exerts an excellent xanthine oxidase inhibiting action and a hypouricemic effect. It has been confirmed that a novel triarylcarboxylic acid derivative, which is characterized by having a carboxyl-substituted heteroaryl group and an aromatic ring group such as a phenyl group attached in para-position on a benzene ring and further carrying a cyano group on the same benzene ring, has a potent xanthine oxidase inhibiting action and a hypouricemic effect. Thus, it is found out that this compound is appropriately usable as an agent for treating or preventing hyperuricemia, gout, inflammatory bowel disease, diabetic nephropathy, diabetic retinopathy and so on.

摘要翻译： 旨在提供用于治疗或预防高尿酸血症，痛风，炎性肠病，糖尿病性肾病，糖尿病性视网膜病等的具有非核酸结构并且发挥优异的黄嘌呤氧化酶抑制作用和低血糖作用的药剂。 已经证实了一种新的三芳基羧酸衍生物，其特征在于在苯环的对位具有羧基取代的杂芳基和诸如苯基的芳环基团，并且在其上还携带有氰基 苯环，具有强效的黄嘌呤氧化酶抑制作用和低氧效应。 由此可知，该化合物适合用作治疗或预防高尿酸血症，痛风，炎症性肠病，糖尿病性肾病，糖尿病性视网膜病等的药剂。

公开(公告)号：EP2094662A1

公开(公告)日：2009-09-02

申请号：EP07859872.9

申请日：2007-12-13

申请人： Astellas Pharma Inc.

发明人： TERASAKA, Tadashi ,  ZENKOH, Tatsuya ,  HAYASHIDA, Hisashi ,  MATSUDA, Hiroshi ,  SATO, Junji ,  IMAMURA, Yoshimasa ,  NAGATA, Hiroshi ,  SEKI, Norio ,  TENDA, Yoshiyuki ,  TASAKI, Mamoru ,  TAKEDA, Masahiro ,  TABUCHI, Seiichiro ,  YASUDA, Minoru ,  TSUBAKI, Kazunori

IPC分类号： C07D213/64 ,  C07D401/06 ,  C07D209/08 ,  C07D209/42 ,  C07D401/12 ,  C07C233/20 ,  C07C233/60 ,  C07C233/73 ,  C07C233/18 ,  C07D213/81 ,  C07D413/04 ,  C07D237/14 ,  C07D213/82 ,  C07D213/56 ,  A61K31/4412 ,  A61P37/08

CPC分类号： C07D213/64 ,  C07C233/18 ,  C07C233/20 ,  C07C233/60 ,  C07C233/73 ,  C07C271/50 ,  C07C2601/08 ,  C07D209/08 ,  C07D209/14 ,  C07D209/24 ,  C07D209/42 ,  C07D211/76 ,  C07D213/56 ,  C07D213/80 ,  C07D213/81 ,  C07D213/82 ,  C07D235/08 ,  C07D237/04 ,  C07D237/14 ,  C07D263/22 ,  C07D263/38 ,  C07D277/34 ,  C07D333/38 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D405/04 ,  C07D409/10 ,  C07D413/04 ,  C07D413/14

摘要： The present invention relates to a novel compound or a salt thereof, which is useful as a CRTH2 antagonist, especially as a medicament for disorder that participates eosinophil, for example, allergic disorder such as asthma, allergic rhinitis, allergic dermatitis, conjunctival inflammation, hives, eosinophilic bronchitis, food allergy, inflammation of the nasal sinuses, multiple sclerosis, angiitis, or chronic obstructive pulmonary disease (COPD) and the like.

公开(公告)号：EP2840083B1

公开(公告)日：2017-09-13

申请号：EP13777902.1

申请日：2013-04-17

申请人： Astellas Pharma Inc.

发明人： NAKAJIMA, Yutaka ,  IMADA, Sunao ,  TAKASUNA, Yuji ,  AOYAMA, Naohiro ,  NIGAWARA, Takahiro ,  SHIRAKAMI, Shohei ,  SHIRAI, Fumiyuki ,  SATO, Junji ,  NAKANISHI, Keita ,  KUBO, Kaori

IPC分类号： C07D487/04 ,  C07D473/00 ,  A61K31/519 ,  A61K31/5377 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00

CPC分类号： A61K31/519 ,  A61K31/52 ,  A61K31/5377 ,  C07D473/00 ,  C07D487/04

公开(公告)号：EP2840083A1

公开(公告)日：2015-02-25

申请号：EP13777902.1

申请日：2013-04-17

申请人： Astellas Pharma Inc.

发明人： NAKAJIMA, Yutaka ,  IMADA, Sunao ,  TAKASUNA, Yuji ,  AOYAMA, Naohiro ,  NIGAWARA, Takahiro ,  SHIRAKAMI, Shohei ,  SHIRAI, Fumiyuki ,  SATO, Junji ,  NAKANISHI, Keita ,  KUBO, Kaori

IPC分类号： C07D487/04 ,  C07D473/00 ,  A61K31/519 ,  A61K31/5377 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00

CPC分类号： A61K31/519 ,  A61K31/52 ,  A61K31/5377 ,  C07D473/00 ,  C07D487/04

摘要： [Problem] On the basis of a cathepsin S inhibitory effect, an excellent agent for treating or preventing autoimmune disease, allergic disease, graft rejection of an organ, bone marrow or tissue, systemic lupus erythematosus, or the like is provided.
[Means for Solution] It was found that a nitrogen-containing bicyclic heterocyclic compound has the excellent cathepsin S inhibitory effect, thereby completing the invention. The compound of the present invention has the cathepsin S inhibitory effect, and can be used as an agent for preventing and/or treating autoimmune disease, allergic disease, graft rejection of an organ, bone marrow or tissue, systemic lupus erythematosus, or the like.

摘要翻译： [问题]基于组织蛋白酶S抑制效果，提供了用于治疗或预防自身免疫性疾病，过敏性疾病，器官，骨髓或组织的移植物排斥，系统性红斑狼疮等的优异的药剂。 [解决方案]发现含氮双环杂环化合物具有优异的组织蛋白酶S抑制作用，从而完成了本发明。 本发明的化合物具有组织蛋白酶S抑制作用，可用作预防和/或治疗自身免疫性疾病，过敏性疾病，器官移植排斥反应，骨髓或组织，系统性红斑狼疮等的药剂 。

公开(公告)号：EP2094662B1

公开(公告)日：2012-04-11

申请号：EP07859872.9

申请日：2007-12-13

申请人： Astellas Pharma Inc.

发明人： TERASAKA, Tadashi ,  ZENKOH, Tatsuya ,  HAYASHIDA, Hisashi ,  MATSUDA, Hiroshi ,  SATO, Junji ,  IMAMURA, Yoshimasa ,  NAGATA, Hiroshi ,  SEKI, Norio ,  TENDA, Yoshiyuki ,  TASAKI, Mamoru ,  TAKEDA, Masahiro ,  TABUCHI, Seiichiro ,  YASUDA, Minoru ,  TSUBAKI, Kazunori

IPC分类号： C07D213/64 ,  C07D401/06 ,  C07D209/08 ,  C07D209/42 ,  C07D401/12 ,  C07C233/20 ,  C07C233/60 ,  C07C233/73 ,  C07C233/18 ,  C07D213/81 ,  C07D413/04 ,  C07D237/14 ,  C07D213/82 ,  C07D213/56 ,  A61K31/4412 ,  A61P37/08

CPC分类号： C07D213/64 ,  C07C233/18 ,  C07C233/20 ,  C07C233/60 ,  C07C233/73 ,  C07C271/50 ,  C07C2601/08 ,  C07D209/08 ,  C07D209/14 ,  C07D209/24 ,  C07D209/42 ,  C07D211/76 ,  C07D213/56 ,  C07D213/80 ,  C07D213/81 ,  C07D213/82 ,  C07D235/08 ,  C07D237/04 ,  C07D237/14 ,  C07D263/22 ,  C07D263/38 ,  C07D277/34 ,  C07D333/38 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D405/04 ,  C07D409/10 ,  C07D413/04 ,  C07D413/14

摘要： The present invention relates to a novel compound or a salt thereof, which is useful as a CRTH2 antagonist, especially as a medicament for disorder that participates eosinophil, for example, allergic disorder such as asthma, allergic rhinitis, allergic dermatitis, conjunctival inflammation, hives, eosinophilic bronchitis, food allergy, inflammation of the nasal sinuses, multiple sclerosis, angiitis, or chronic obstructive pulmonary disease (COPD) and the like.

摘要翻译： 本发明涉及一种新的化合物或其盐，其可用作CRTH2拮抗剂，特别是用作参与嗜酸性粒细胞的病症的药物，例如过敏性疾病如哮喘，过敏性鼻炎，过敏性皮炎，结膜炎症，荨麻疹 ，嗜酸性支气管炎，食物过敏，鼻窦炎，多发性硬化，血管炎或慢性阻塞性肺病（COPD）等。

公开(公告)号：EP1992361B1

公开(公告)日：2012-05-02

申请号：EP07714807.0

申请日：2007-02-22

申请人： Astellas Pharma Inc.

发明人： KAWAKAMI, Masakatsu ,  KETO, Yoshihiro ,  IKEDA, Ken ,  FUKUDA, Mari ,  SATO, Junji

IPC分类号： A61K45/00 ,  A61K31/381 ,  A61K31/4025 ,  A61K31/4155 ,  A61K31/42 ,  A61K31/427 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/4535 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/55 ,  A61P1/00 ,  A61P1/04 ,  A61P43/00 ,  C07D213/79

CPC分类号： C07D401/12 ,  A61K31/00 ,  A61K31/381 ,  A61K31/4025 ,  A61K31/4155 ,  A61K31/42 ,  A61K31/427 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/4535 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/55 ,  A61K45/06 ,  C07D213/79 ,  C07D231/14 ,  C07D261/18 ,  C07D275/03 ,  C07D277/56 ,  C07D333/40 ,  C07D401/10 ,  C07D405/10 ,  C07D405/12 ,  C07D409/10 ,  C07D413/10 ,  C07D417/10 ,  C07D417/12

摘要： It is intended to provide a remedy or a preventive for digestive ulcer being efficacious for ulcer in the small intestine, etc., on which the existing gastric antisecretory agents such as proton pump inhibitors exert no effect, and superior in efficaciousness and safety to Allopurinol. A medicinal composition, which contains a non-purine xanthine oxidase inhibitor as the active ingredient, is useful as a remedy or a preventive for ulceration in the digestive tract caused by gastric acid, pepsin, stress, Helicobacter pylori, the attack by NSAID, etc. This medicinal composition is particularly useful as a nonconventional remedy for ulcer because of being efficacious against ulcer in the small intestine on which the existing remedies for gastric and duodenal ulcer inhibiting gastric acid secretion such as proton pump inhibitors exert no effect.

公开(公告)号：EP1932832B1

公开(公告)日：2010-12-01

申请号：EP06811388.5

申请日：2006-10-06

申请人： Astellas Pharma Inc.

发明人： SATO, Junji ,  HATTORI, Kazuyuki ,  KUBOTA, Hirokazu ,  MUNAKATA, Ryosuke ,  ASANO, Toru ,  MAEDA (WATANABE), Junko. ,  KAWAKAMI, Masakatsu ,  KAMIKAWA, Akio

IPC分类号： C07D213/79 ,  A61K31/381 ,  A61K31/4025 ,  A61K31/404 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/42 ,  A61K31/425 ,  A61K31/426 ,  A61K31/427 ,  A61K31/4418 ,  A61P19/06

CPC分类号： C07D213/79 ,  C07D231/14 ,  C07D261/18 ,  C07D275/03 ,  C07D277/56 ,  C07D333/38 ,  C07D333/60 ,  C07D333/76 ,  C07D401/10 ,  C07D405/10 ,  C07D409/10 ,  C07D413/10 ,  C07D417/10

摘要： It is intended to provide a remedy or a preventive for hyperuricemia, gout, inflammatory bowel disease, diabetic nephropathy, diabetic retinitis and so on which has a non-nucleic acid structure and exerts an excellent xanthine oxidase inhibitory effect and a uric acid level-lowering effect. It has been confirmed that a novel triarylcarboxlic acid derivative, which is characterized by having a carboxyl-substituted heteroaryl group and an aromatic ring group such as a phenyl group attached in para-position on a benzene ring and further carrying a cyano group on the same benzene ring, has a potent xanthine oxidase inhibitory effect and a uric acid level-lowering effect. Thus, it is found out that this compound is appropriately usable as a remedy or a preventive for hyperuricemia, gout, inflammatory bowel disease, diabetic nephropathy, diabetic retinitis and so on.

摘要翻译： 其目的在于提供具有非核酸结构并发挥出色的黄嘌呤氧化酶抑制作用和尿酸水平降低作用的高尿酸血症，痛风，炎性肠病，糖尿病性肾病，糖尿病性视网膜炎等的治疗或预防 影响。 已经证实了一种新的三芳基羧酸衍生物，其特征在于在苯环的对位具有羧基取代的杂芳基和诸如苯基的芳环基团，并且在其上还带有氰基 苯环，具有强效的黄嘌呤氧化酶抑制作用和尿酸水平降低作用。 因此，发现该化合物适合用作高尿酸血症，痛风，炎性肠病，糖尿病肾病，糖尿病性视网膜炎等的治疗或预防。

公开(公告)号：EP1992361A1

公开(公告)日：2008-11-19

申请号：EP07714807.0

申请日：2007-02-22

申请人： Astellas Pharma Inc.

发明人： KAWAKAMI, Masakatsu ,  KETO, Yoshihiro ,  IKEDA, Ken ,  FUKUDA, Mari ,  SATO, Junji

IPC分类号： A61K45/00 ,  A61K31/381 ,  A61K31/4025 ,  A61K31/4155 ,  A61K31/42 ,  A61K31/427 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/4535 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/55 ,  A61P1/00 ,  A61P1/04 ,  A61P43/00 ,  C07D213/79

CPC分类号： C07D401/12 ,  A61K31/00 ,  A61K31/381 ,  A61K31/4025 ,  A61K31/4155 ,  A61K31/42 ,  A61K31/427 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/4535 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/55 ,  A61K45/06 ,  C07D213/79 ,  C07D231/14 ,  C07D261/18 ,  C07D275/03 ,  C07D277/56 ,  C07D333/40 ,  C07D401/10 ,  C07D405/10 ,  C07D405/12 ,  C07D409/10 ,  C07D413/10 ,  C07D417/10 ,  C07D417/12

摘要： An object of the present invention is to provide an agent for treating or preventing digestive ulcer that is effective even to ulcer of small intestine and others, for which gastric acid secretion inhibitors such as proton pump inhibitors are ineffective, and is superior to allopurinol in the efficaciousness and the safety.
The pharmaceutical composition of the present invention comprising a non-purine xanthine oxidase inhibitor as the active ingredient is useful as an agent for treating or preventing ulcer that forms in digestive tracts by the attack of gastric acid, pepsin, stress, Helicobacter pylori bacteria, NSAID, etc. In particular, it is useful as an ulcer remedy heretofore unknown in the art as it is effective even for ulcer in small intestine for which gastric/duodenal ulcer remedies that inhibit gastric acid secretion such as proton pump inhibitors are ineffective.

摘要翻译： 本发明的目的是提供一种用于治疗或预防消化性溃疡的药剂，即使对于小肠等的溃疡也是有效的，其中胃酸分泌抑制剂如质子泵抑制剂无效，并且优于别嘌呤醇 有效性和安全性。 包含非嘌呤黄嘌呤氧化酶抑制剂作为活性成分的本发明的药物组合物可用作治疗或预防胃酸，胃蛋白酶，应激，幽门螺杆菌，NSAID的侵袭在消化道中形成的溃疡的药剂 特别地，作为本领域迄今未知的溃疡治疗是有用的，因为即使对于抑制胃酸分泌的胃/十二指肠溃疡治疗如质子泵抑制剂也是无效的小肠溃疡也是有效的。