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公开(公告)号：EP4157225A1
公开(公告)日：2023-04-05
申请号：EP21729034.5
申请日：2021-05-26
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公开(公告)号：EP4019496A1
公开(公告)日：2022-06-29
申请号：EP20854718.2
申请日：2020-08-19
发明人： OTANI, Shuhei , FUJITO, Takayuki , IMURA, Naoko , KIJIMA, Hideomi , PARENT, Stephan D. , BEVILL, Melanie Janelle , JOHNSON, Courtney S. , HOUSTON, Travis Lee
IPC分类号： C07D205/04
摘要： An object of the present invention is to provide a compound with an improved balance of S1P 5 receptor agonist activity with respect to S1P 1 receptor, and a form suitable for drug substances of pharmaceuticals. Provided is Compound I having high S1P 5 receptor-selective agonist activity on the S1P 1 receptor. In addition, the crystal forms of Compound I, the salts of Compound I, and the crystal forms of salts thereof disclosed in the present invention are provided as drug substances of pharmaceuticals.
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公开(公告)号：EP3999183A1
公开(公告)日：2022-05-25
申请号：EP20841280.9
申请日：2020-07-16
发明人： KAKUUCHI, Akito , UMEMURA, Shuhei , SVENSSON, Mats , RUVINSKY, Anatoly , INOYAMA, Daigo , KRILOV, Goran , TAKAHASHI, Hidenori , KONZE, Kyle , VERRAS, Andreas , CRUMPLER, Simon , VALLADE, Maelle , MACLEOD, Calum , SANDERSON, James N. , BULL, Richard J. , GAINES, Simon
IPC分类号： A61P25/28 , A61P35/00 , A61P43/00 , C07D261/08 , C07D471/04 , C07D487/04 , C07D487/10 , C07D498/10 , C07D231/06 , A61K31/415 , A61K31/4178 , A61K31/422 , A61K31/424 , A61K31/5025 , A61K31/519 , A61K31/53
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4.发明公开
公开(公告)号：EP3976327A1
公开(公告)日：2022-04-06
申请号：EP20727311.1
申请日：2020-05-26
发明人： BEE, Markus , GALLINGER, Helena , SAIFERT, Alexander , WEBER-STEBLIWEZ, Andreas , SCHLÖGEL, Georg , NISHIURA, Akio , SASAKI, Akinori , GOTO, Masaoki
IPC分类号： B26D7/18
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公开(公告)号：EP3854783A1
公开(公告)日：2021-07-28
申请号：EP19862582.4
申请日：2019-09-19
IPC分类号： C07D207/16 , A61K31/40 , A61P7/02 , A61P9/10 , A61P43/00
摘要： 4-({(4S)-1-(4-Carbamimidoylbenzoyl)-4-[4-(methylsulfonyl)piperazin-1-yl]-L-prolyl}amino) benzoic acid di(4-toluenesulfonate) or dibenzenesulfonate or their crystal forms can be useful pharmaceutical ingredients because of their low hygroscopicity and excellent storage stability.
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公开(公告)号：EP3854781A1
公开(公告)日：2021-07-28
申请号：EP19862361.3
申请日：2019-09-19
IPC分类号： C07C235/56 , A61K31/196 , A61K31/216 , A61K31/351 , A61P25/00 , A61P25/18 , A61P25/20 , A61P43/00 , C07C327/48 , C07D309/06
摘要： An object of the present invention is to provide a DP receptor antagonist. A compound represented by general formula (I):
(wherein all symbols are as shown in the specification) and a pharmaceutically acceptable salt thereof have DP receptor antagonistic activity and are also highly safe, and thus are useful as active ingredients of pharmaceuticals for DP receptor-mediated diseases. In addition, the compound represented by the general formula (I) and the pharmaceutically acceptable salt thereof also have good transferability to the central nervous system, and thus are particularly useful as a preventive and/or therapeutic agent for diseases associated with DP receptors present in the central nervous system among DP receptor-mediated diseases, that is, sleep-wake disorders.-
公开(公告)号：EP3804758A1
公开(公告)日：2021-04-14
申请号：EP19812634.4
申请日：2019-05-30
发明人： NISHIKAWA, Hiroyoshi , TOGASHI, Yosuke , OHYAMA, Yukiya , YOSHIDA, Takao , TAKEDA, Kazuhiko , KODA, Kenichi , HONDA, Atsushi , OYAGI, Atsushi , KAKINUMA, Toru , MURATA, Masayuki
摘要： The present invention addresses the problem of providing: a method for identifying a malignant tumor patient in whom an immune checkpoint inhibitor can be expected to be more effective; and an agent for suppressing the advance, suppressing the recurrence, and/or treating a malignant tumor characterized by prescription based on the method. The present invention provides: the determination of a malignant tumor patient in whom an immune checkpoint inhibitor can be expected to be more effective, said determination being made by analyzing evaluation items comprising a combination of PD-1 expression intensity and proportion of PD-1 expressing cells, etc., in Treg cells and CD8 + T cells in tumor tissue or blood; and an agent for suppressing the advance, suppressing the recurrence, and/or treating a malignant tumor characterized by prescription based on the determination.
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公开(公告)号：EP3789040A1
公开(公告)日：2021-03-10
申请号：EP19793796.4
申请日：2019-04-26
发明人： ARIZA, Yuko
IPC分类号： A61K45/00 , A61K31/4985 , A61K31/505 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/52 , A61K31/522 , A61P9/00 , A61P13/12 , A61P17/00 , A61P37/06 , A61P43/00
摘要： The problem of the present invention is to find an effective preventive and/or therapeutic agent for an autoimmune disease, in particular, pemphigus, pemphigoid, ANCA-related angiitis and to provide the same as a medicine. The compounds having a Btk inhibitory activity to be used in the present invention inhibits antibody production from B cells and, moreover, inhibits the formation of neutrophil extracellular traps (NETs). Thus, these compounds are useful for preventing and/or treating an autoimmune disease, in particular, pemphigus, pemphigoid, ANCA-related angiitis
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公开(公告)号：EP3763743A1
公开(公告)日：2021-01-13
申请号：EP19751922.6
申请日：2019-02-08
发明人： SHIBAYAMA, Shiro , SHIMBO, Takuya , TEZUKA, Tomoya , THROSBY, Mark , DE KRUIF, Cornelis Adriaan , VAN LOO, Pieter Fokko , KLOOSTER, Rinse
IPC分类号： C07K16/46
摘要： The present invention addresses the problem of providing a novel drug for the prevention of autoimmune diseases, the suppression of the progression of the symptoms of autoimmune diseases, the suppression of the recurrence of autoimmune diseases, or the treatment of autoimmune diseases. As a result of diligent investigation, the inventors of the present invention have focused on PD-1/CD3 bispecific antibodies as substances that can solve the abovementioned problem and have confirmed that said bispecific antibodies make it possible to achieve pharmaceuticals that reduce the occurrence of the adverse effects known as infusion-related reaction and cytokine release syndrome. In addition, the inventors have confirmed that said bispecific antibodies allow for interaction between PD-1 and its ligand PD-L1 and have discovered that said feature contributes to enhanced and sustained activity.
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公开(公告)号：EP3702357A1
公开(公告)日：2020-09-02
申请号：EP20170445.9
申请日：2015-12-09
发明人： TANAKA, Motoyuki , KONDO, Takashi , HIROOKA, Yasuo , NISHIYAMA, Taihei , HIRAMATSU, Atsushi , KODA, Tomoyuki , KOUYAMA, Sho
IPC分类号： C07D471/04 , A61K31/444 , A61P7/02 , A61P43/00
摘要： A compound represented by general formula (I) (wherein all symbols are as defined in the description) or a salt, solvate, N-oxide form or prodrug thereof is a potent FXIa inhibitor, has excellent oral absorption properties and kinetics in blood, can exert a potent anti-coagulation activity over a long period of time after being administered orally, and has a discrepancy between the anti-coagulation activity thereof and the CYP-inhibiting activity thereof. Therefore, the compound or the salt, solvate, N-oxide form or prodrug thereof can be used as an efficient prophylactic and/or therapeutic agent for vascular occlusive diseases.
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