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31.发明公开
公开(公告)号：EP2881115A1
公开(公告)日：2015-06-10
申请号：EP13825231.7
申请日：2013-07-30
发明人： OKADA, Hiroki , KONEMURA, Takashi
IPC分类号： A61K31/426 , A61K31/4439 , A61K31/444 , A61K45/00 , A61P1/04 , A61P43/00
CPC分类号： A61K31/426 , A61K31/4439 , A61K31/444 , A61K45/06 , A61K2300/00
摘要： The present invention provides an agent for preventing or relapse-preventing, treating or ameliorating gastroesophageal reflux disease, in which existing treatment is not effective.
4-[({6-[Isobutyl(1,3-thiazol-2-ylsulfonyl)amino]-2,3-dihydro-1H-inden-5-yl}oxy)methyl]-3-methyl benzoic acid, a salt thereof or a prodrug thereof is effective in the prevention or relapse prevention, treatment or amelioration of gastroesophageal reflux disease.摘要翻译： 本发明提供预防或复发预防，治疗或改善胃食管反流病的药剂，其中现有治疗无效。 4 - [（{6- [异丁基（1,3-噻唑-2-基磺酰基）氨基] -2,3-二氢-1H-茚-5-基}氧基）甲基] -3-甲基苯甲酸盐 或其前药在预防或复发预防，治疗或改善胃食管反流病中是有效的。
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公开(公告)号：EP2468765B1
公开(公告)日：2015-04-22
申请号：EP12153114.9
申请日：2007-03-02
IPC分类号： A61K9/19 , A61K38/00 , A61K47/26 , C07K14/705 , A61K9/00
CPC分类号： C07K14/70503 , A61K9/0019 , A61K9/19 , A61K38/00 , A61K47/26 , C07K14/70532 , Y02A50/465 , Y02A50/481
摘要： As a substance which pharmacologically regulates the function of a cell surface functional molecule, a substance which has specificity and an activity or efficacy equal or superior to an antibody and does not require an advanced production technique and facility for application thereof to a pharmaceutical product has been demanded. The invention relates to a multimer of an extracellular domain of a cell surface functional molecule, particularly a tetramer of an extracellular domain of PD-1 or PD-L1. Further, the invention relates to an application of such a tetramer as a preventive and/or therapeutic agent for cancer, cancer metastasis, immunodeficiency, an infectious disease or the like and an application of PD-1 or PD-L1 as a testing or diagnostic agent or a research agent for such a disease.
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公开(公告)号：EP2794597A1
公开(公告)日：2014-10-29
申请号：EP12813423.6
申请日：2012-12-20
发明人： COURTNEY, Steve , YARNOLD, Chris , FLANAGAN, Stuart , BRACE, Gareth , BARKER. John , ICHIHARA, Osamu , GADOULEAU, Elise , RICHARDSON, Anthony , KONDO, Takashi , IMAGAWA, Akira , NAKATANI, Shingo , SUZUKI, Ryo , KOUYAMA, Sho
IPC分类号： C07D401/14 , C07D471/04 , C07D487/04 , A61K31/437 , A61K31/519 , A61P9/00
CPC分类号： C07D487/04 , C07D401/14 , C07D403/14 , C07D471/04
摘要： The present invention provides compounds of the general formula (I), their salts and N- oxides, and solvates and prodrugs thereof (wherein the characters are as defined in the description). The compounds of the general formula (I) are inhibitors of Factor XIa, so that they are useful in the prevention of and/or therapy for thromboembolic diseases.
摘要翻译： 本发明提供通式（I）的化合物，其盐和N-氧化物及其溶剂合物和前药（其中字符如说明书中所定义）。 通式（I）的化合物是因子XIa的抑制剂，因此它们可用于预防和/或治疗血栓栓塞性疾病。
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公开(公告)号：EP2786996A1
公开(公告)日：2014-10-08
申请号：EP12852725.6
申请日：2012-11-28
IPC分类号： C07D473/34 , A61K31/522 , A61P7/02 , A61P17/00 , A61P29/00 , A61P35/00 , A61P35/02 , A61P37/02 , A61P37/08 , A61P43/00
CPC分类号： C07D473/34 , A61K31/522 , C07B2200/13 , C07D473/00
摘要： The purinone derivative 6-amino-9-[(3R)-1-(2-butynoyl)-3-pyrrolidinyl]-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one hydrochloride has Btk-selective inhibitory activity and, in addition to having excellent metabolic stability, it is a compound that exhibits a high level of solubility and absorption with respect to the free base and can be crystallized, hence it can serve as a therapeutic agent for diseases involving B cells and mast cells.
摘要翻译： 嘌呤酮衍生物6-氨基-9 - [（3R）-1-（2-丁炔酰基）-3-吡咯烷基] -7-（4-苯氧基苯基）-7,9-二氢-8H-嘌呤-8-酮盐酸盐 Btk选择性抑制活性，除了具有优异的代谢稳定性之外，还是对游离碱显示出高水平的溶解性和吸收性并且可以结晶的化合物，因此它可以用作涉及涉及疾病的治疗剂 B细胞和肥大细胞。
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35.发明授权Azetidinecarboxylic acid derivative and medicinal use thereof 有权Azetidincarboxylsäurederivat以及它们的医疗用途
公开(公告)号：EP2371811B1
公开(公告)日：2014-10-08
申请号：EP11168698.6
申请日：2005-12-12
IPC分类号： C07C229/14 , A61K31/12 , A61K31/166 , A61K31/197 , A61K31/215 , A61K31/397 , A61K31/4035 , A61K31/41 , A61K31/437 , A61K31/4409 , A61K31/4412
CPC分类号： C07F5/027 , A61K31/12 , A61K31/166 , A61K31/197 , A61K31/215 , A61K31/397 , A61K31/4035 , A61K31/41 , A61K31/437 , A61K31/4409 , A61K31/4412 , A61K31/4439 , A61K31/4725 , A61K31/55 , A61K31/69 , A61K45/06 , C07C229/14 , C07C2602/10 , C07D205/04 , C07D211/70 , C07D271/06 , C07D401/12 , C07D409/06 , C07D471/04 , A61K2300/00
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公开(公告)号：EP2508204B1
公开(公告)日：2014-09-24
申请号：EP12005031.5
申请日：2003-06-25
IPC分类号： A61K45/00 , A61K31/437 , A61K31/445 , A61P9/00 , A61P9/06 , A61P9/10 , A61P9/12 , A61P9/14 , A61P13/12 , A61P25/06 , A61P43/00 , C07D211/48 , C07D471/04
CPC分类号： C07D471/04 , A61K31/437 , A61K31/445 , C07D211/48
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37.发明公开
公开(公告)号：EP2740724A1
公开(公告)日：2014-06-11
申请号：EP12822308.8
申请日：2012-08-03
IPC分类号： C07C405/00 , A61K9/10 , A61K31/5575 , A61K47/10 , A61K47/26 , A61K47/34 , A61K47/36 , A61K47/40 , A61K47/44 , A61P19/08 , C07C69/732 , C07C69/92 , C07C235/16
CPC分类号： C07C59/56 , A61K9/0019 , A61K47/26 , A61K47/6951 , C07C235/06 , C07C235/16 , C07C405/00 , C07C2601/04 , C07C2601/08 , Y10T428/2982
摘要： The present invention provides a compound of which active form is represented by a formula (A). and which can be injected into a joint cavity which is an affected part of disorders and can be accumulated in the joint cavity to exert the pharmacological effect thereof in a sustained manner, for the purpose of ameliorating cartilage disorders without developing any side effect. A compound according to the present invention, which is represented by a formula (I):
(wherein all of symbols are as defined in the description), is a compound that can achieve the above-mentioned purpose. This compound does not exhibit any side effect on the cardiovascular system even when the compound is administered in an effective amount for exhibiting a cartilage regeneration activity, and is therefore extremely useful as a safe and effective preventive and/or therapeutic agent for cartilage disorders. Since a suspension produced using this compound can be injected without requiring the incision of the affected part, it can reduce the burden on patients, and is extremely useful as a medicinal agent.摘要翻译： 本发明提供活性形式由式（A）表示的化合物。 并且其可以注射到作为疾病的部分的关节腔中，并且可以以持续的方式累积在关节腔中以发挥其药理作用，以改善软骨疾病而不产生副作用。 由式（I）表示的本发明化合物（其中全部符号如说明书中所定义）是可以实现上述目的的化合物。 即使当化合物以有效的量施用以显示软骨再生活性时，该化合物也不会对心血管系统显示任何副作用，因此作为软骨疾病的安全有效的预防和/或治疗剂非常有用。 由于可以注射使用该化合物制成的悬浮液，而不需要切开患部，可以减轻患者的负担，作为药剂极为有用。
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公开(公告)号：EP1806147B1
公开(公告)日：2014-04-30
申请号：EP05795461.2
申请日：2005-10-20
发明人： ODANI, Tomoyuki, ONO PHARMACEUTICAL CO., LTD. , TADA, Hideaki, ONO PHARMACEUTICAL CO., LTD. , YAMADA, Kimiho
IPC分类号： A61K45/00 , A61K31/7088 , A61K38/00 , A61K39/395 , A61K48/00 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/02 , A61P37/04 , A61P37/06 , A61P37/08
CPC分类号： C07K14/47 , A61K31/7088 , A61K38/1709 , A61K38/1774 , A61K39/3955 , A61K45/06 , A61K2039/505 , C07K16/18 , C07K16/28 , C07K2319/30 , G01N33/6854 , Y02A50/39 , Y02A50/394 , Y02A50/466
摘要： The present invention relates to use of an antagonist of BIR1 (B cell immunoglobulin receptor 1) related to the present invention, a method for screening the antagonist, in addition to subtype polypeptides of BIR1, the polynucleotide encoding them and antibodies for the polypeptides. BIR1 functions as an immunosuppressive receptor, and the antagonist of BIRI has immunopotentive activity, which is able to use for preventing and/or treating a cancer, an immunodeficiency disease or an infectious disease.
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公开(公告)号：EP1790639B1
公开(公告)日：2014-03-26
申请号：EP05776646.1
申请日：2005-08-26
发明人： KOKUBO, Masaya, Ono Pharmaceutical Co., Ltd. , TAKAOKA, Yoshikazu, Ono Pharmaceutical Co., Ltd , SHIBAYAMA, Shiro, Ono Pharmaceutical Co., Ltd.
IPC分类号： C07D233/16 , C07D233/64 , A61K31/4178 , A61K31/4196 , A61K31/4439 , A61K31/4725 , A61K45/00 , A61P11/00 , A61P19/02 , A61P29/00 , A61P31/18 , A61P35/00 , A61P35/04 , A61P37/06 , A61P43/00 , C07D233/84 , C07D233/90 , C07D401/14 , C07D403/12 , C07D403/14 , C07D471/10 , C07D487/10
CPC分类号： C07D471/10 , C07D233/16 , C07D233/84 , C07D233/90 , C07D401/14 , C07D403/12 , C07D403/14 , C07D487/10
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公开(公告)号：EP2703381A1
公开(公告)日：2014-03-05
申请号：EP12777023.8
申请日：2012-04-27
发明人： HAYASHI, Yujiro
IPC分类号： C07C205/18 , C07C201/12 , C07C205/44 , C07D307/42 , C07B53/00 , C07B61/00
CPC分类号： C07D307/45 , C07B53/00 , C07C67/30 , C07C69/732 , C07C69/738 , C07C201/12 , C07C205/05 , C07C2601/08 , C07C2601/14 , C07D307/42 , C07C205/18 , C07C205/44 , C07C205/41 , C07C205/55
摘要： The present invention provides a method that allows production of stereospecific and asymmetrical five-membered ring-containing compounds serving as synthetic intermediates for formation of five-membered rings of prostaglandins and the like, with high yield and excellent stereoselectivity in terms of diastereoselectivity and enantioselectivity in a short process without requiring troublesome procedures such as optical resolution. The method for producing a five-membered ring-containing compound includes a cyclization step of condensing and cyclizing an α, β-unsaturated nitro compound represented by the following chemical formula (I) with a 1,4-butanedione compound, in the presence of a catalyst formed by a compound having a pyrrolidine ring and an optically active α-carbon relative to the nitrogen on the ring, in a water-insoluble organic solvent and/or a non-oxygen atom-containing water-soluble organic solvent so as to produce the five-membered ring-containing compound represented by the following chemical formula (II).
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