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21.发明授权
公开(公告)号：EP2898902B1
公开(公告)日：2019-03-20
申请号：EP13838722.0
申请日：2013-09-13
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公开(公告)号：EP3026045B1
公开(公告)日：2018-10-03
申请号：EP14828976.2
申请日：2014-07-23
IPC分类号： C07D215/54 , C07D401/12 , C07D401/14 , A61K31/4709 , A61K31/5377 , A61P9/00 , A61P13/12 , A61P25/02 , A61P35/00 , A61P35/02 , A61P35/04 , A61P37/02 , A61P43/00
CPC分类号： C07D401/14 , C07D215/54 , C07D401/12
摘要： A compound represented by general formula (I): has a strong Axl inhibitory activity by introducing a distinctive bicyclic structure in which a saturated carbon ring is fused to a pyridone ring, and can be a therapeutic agent for Axl-related diseases, for example, cancer such as acute myeloid leukemia, melanoma, breast cancer, pancreatic cancer, and glioma, kidney diseases, immune system diseases, and circulatory system diseases.
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公开(公告)号：EP3112362B1
公开(公告)日：2018-09-26
申请号：EP15756097.0
申请日：2015-02-26
发明人： OGAWA, Seiji , WATANABE, Toshihide , SUGIMOTO, Isamu , TANI, Kousuke , MORIYUKI, Kazumi , GOTO, Yoshikazu , YAMANE, Shinsaku
IPC分类号： C07D407/04 , A61K31/352 , A61K31/427 , A61K31/4709 , A61P1/00 , A61P1/04 , A61P1/16 , A61P7/00 , A61P11/00 , A61P13/12 , A61P15/00 , A61P17/14 , A61P19/04 , A61P19/08 , A61P25/00 , A61P27/02
CPC分类号： C07D417/04 , A61K45/06 , C07D407/04 , C07D417/12
摘要： To provide an excellent selective EP2 agonist in a safe manner. A compound represented by general formula (I): (wherein all symbols are as defined in the specification), a salt or N-oxide of the compound, or a solvate or prodrug of the compound or the salt or N-oxide has a selective EP2 agonist activity and is highly safe, and is therefore useful as a drug, especially as a therapeutic agent for EP2 receptor-related diseases including immune diseases, allergic diseases, neuronal death, dysmenorrhea, premature birth, miscarriage, baldness, ocular diseases, erectile dysfunction, arthritis, lung injury, pulmonary fibrosis, pulmonary emphysema, bronchitis, chronic obstructive pulmonary disease, bone diseases, cartilage injury and others.
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公开(公告)号：EP3150577B1
公开(公告)日：2018-08-29
申请号：EP16002350.3
申请日：2012-09-27
发明人： Naganawa, Atsushi , Kusumi, Kensuke , Otsuki, Kazuhiro , Sekiguchi, Tetsuya , Kakuuchi, Akito , Shinozaki, Koji , Yamamoto, Hiroshi , Nonaka, Shigeyuki
IPC分类号： C07D205/04 , A61K31/397 , A61K31/40 , A61K31/445 , A61K31/4523 , A61K31/453 , A61K31/454 , A61K31/4545 , A61K31/5377 , A61P9/00 , A61P9/06 , A61P9/10 , A61P9/12 , A61P9/14 , A61P11/00 , A61P25/00 , A61P43/00 , C07D207/10 , C07D207/12 , C07D211/48
CPC分类号： A61K31/445 , A61K31/397 , A61K31/40 , A61K31/4523 , A61K31/453 , A61K31/454 , A61K31/4545 , C07D205/04 , C07D207/12 , C07D207/16 , C07D211/48 , C07D211/52 , C07D401/12 , C07D405/12
摘要： The compound represented by the formula (I-1): wherein all the symbols have the same meanings as described in the specification, has two cyclic groups, particularly phenoxy groups at specific substitution positions and thus has high human S1P 2 antagonistic activity. The compound may therefore be used as a therapeutic agent for S1P 2 -mediated diseases such as diseases resulting from vascular constriction, fibrosis and respiratory diseases.
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公开(公告)号：EP2980072B1
公开(公告)日：2018-04-25
申请号：EP14775353.7
申请日：2014-03-25
发明人： KUSUMI, Kensuke , NAGANAWA, Atsushi , OTSUKI, Kazuhiro , SEKIGUCHI, Tetsuya , SHINOZAKI, Koji , YAMAMOTO, Hiroshi , YAMAMOTO, Yasuko
IPC分类号： C07D207/12 , A61K31/40 , A61K31/451 , A61P1/16 , A61P3/06 , A61P3/10 , A61P9/00 , A61P9/04 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/00 , A61P13/12 , A61P17/02 , A61P19/02 , A61P25/00 , A61P25/04 , A61P27/02 , A61P27/06
CPC分类号： C07D211/52 , C07D207/12 , C07D211/44 , C07D211/48
摘要： An object of the present invention is to provide a compound having strong human S1P 2 antagonistic activity in order to develop a useful medicament for therapy of a S1P 2 -mediated disease such as a disease resulting from vascular constriction, fibrosis and respiratory disease. The compound represented by the general formula (I): wherein all the symbols have the same meanings as described in the specification, has a halogen atom or a haloalkyl group and a phenoxy group at certain substitution sites, and thus has strong human S1P 2 antagonistic activity. Therefore, the compound can be a therapeutic agent for a S1P 2 -mediated disease, such as a disease resulting from vascular constriction, fibrosis and respiratory disease.
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公开(公告)号：EP3210969A4
公开(公告)日：2018-03-28
申请号：EP15852712
申请日：2015-10-23
IPC分类号： C07C275/32 , A61K31/17 , A61K31/341 , A61K31/351 , A61K31/381 , A61K31/4045
CPC分类号： C07D213/61 , A61K31/17 , A61K31/341 , A61K31/351 , A61K31/381 , A61K31/4045 , A61K31/417 , A61K31/422 , A61K31/4245 , A61K31/426 , A61K31/435 , A61K31/4545 , A61K31/4965 , A61K31/505 , C07C233/26 , C07C233/29 , C07C275/32 , C07C275/40 , C07D209/30 , C07D213/40 , C07D213/74 , C07D233/64 , C07D239/26 , C07D241/12 , C07D271/06 , C07D277/28 , C07D307/52 , C07D309/04 , C07D333/20 , C07D333/28 , C07D413/06
摘要： The present invention relates to a compound represented by the general formula (I) (wherein the definition of each group has the same meaning as described in the specification). The compound is useful as preventive and/or therapeutic agent for KCNQ2-5 channel-related diseases.
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27.发明公开
公开(公告)号：EP3290413A1
公开(公告)日：2018-03-07
申请号：EP17193874.9
申请日：2012-12-20
发明人： KONDO, Takashi , IMAGAWA, Akira , NAKATANI, Shingo , SUZUKI, Ryo , KOUYAMA, Sho , COURTNEY, Steve , YARNOLD, Chris , FLANAGAN, Stuart , BRACE, Gareth Neil , BARKER, John , ICHIHARA, Osamu , GADOULEAU, Elise , RICHARDSON, Anthony
IPC分类号： C07D401/14 , C07D471/04 , C07D487/04 , A61K31/437 , A61K31/519 , A61P9/00
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： 本发明提供了通式（I）的化合物，它们的盐和N-氧化物，以及它们的溶剂化物和前药（其中特征如说明书中所定义）。 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：EP3272858A1
公开(公告)日：2018-01-24
申请号：EP16765082.9
申请日：2016-03-17
发明人： OKANO, Hideyuki , SHIOZAWA, Seiji , KISA, Fumihiko
IPC分类号： C12N5/10 , C12N5/0735 , C12N15/09
CPC分类号： C12N5/0696 , C12N5/10 , C12N15/09 , C12N2501/01 , C12N2501/20 , C12N2501/60 , C12N2501/602 , C12N2501/603 , C12N2501/605 , C12N2501/606
摘要： To produce and/or maintain naive pluripotent stem cells capable of highly expressing genes important for maintaining an undifferentiated state, which could not be achieved by known methods for producing pluripotent stem cells. The present invention can produce naive pluripotent stem cells capable of maintaining an undifferentiated state by introducing and allowing transient expression of six genes (Oct3/4, Klf4, c-Myc, Sox2, Nanog, and Klf2) among the so-called initializing factors, and further performing culturing in a medium containing LIF, an MEK inhibitor, a GSK3 inhibitor, a cAMP production promoter, a TGF-β inhibitor and a PKC inhibitor. Thus, the problem of the present invention can be solved.
摘要翻译： 为了产生和/或维持能够高度表达对维持未分化状态重要的基因的幼稚多能干细胞，这是通过用于产生多能干细胞的已知方法不能实现的。 本发明可通过在所谓的初始化因子中导入并允许六种基因（Oct3 / 4，Klf4，c-Myc，Sox2，Nanog和Klf2）的瞬时表达来产生能够维持未分化状态的幼稚多能干细胞， 并进一步在含有LIF，MEK抑制剂，GSK3抑制剂，cAMP产生促进剂，TGF-β抑制剂和PKC抑制剂的培养基中进行培养。 因此，可以解决本发明的问题。
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公开(公告)号：EP2889309B1
公开(公告)日：2017-12-27
申请号：EP15151984.0
申请日：2007-03-02
IPC分类号： C07K14/705 , A61K9/19 , A61K47/26 , A61K9/00 , A61K38/00
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：EP2794597B1
公开(公告)日：2017-11-15
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
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