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公开(公告)号：US10851162B2
公开(公告)日：2020-12-01
申请号：US16460632
申请日：2019-07-02
发明人： Tomoaki Komai , Takako Kimura , Daichi Baba , Yoshikuni Onodera , Kento Tanaka , Takashi Kagari , Anri Aki , Nobumi Nagaoka
摘要： It is intended to provide a therapeutic and/or prophylactic agent for transplant rejections, immunological diseases, allergic diseases, inflammatory diseases, thrombosis, cancers, etc., targeting human Orai1. The present invention provides, for example, a pharmaceutical composition comprising an antibody that specifically recognizes human Orai1 and has the activity of inhibiting human T cell activation.
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公开(公告)号：US10851111B2
公开(公告)日：2020-12-01
申请号：US16031165
申请日：2018-07-10
发明人： Motoshi Yamauchi , Keiji Nakayama
IPC分类号： C07D487/10 , B01J31/02 , B01J31/04 , B01J31/22 , C07B53/00 , C07D491/20 , B01J31/24 , B01J31/18 , B01J31/14
摘要： The present disclosure provides a method for efficiently producing and providing compounds having a spirooxindole skeleton, for example compounds having a spirooxindole skeleton and having antitumor activity that inhibit the interaction between Mdm2 protein and p53 protein, or intermediates thereof, using an asymmetric catalyst. Compounds having optically active tricyclic dispiroindole skeletons are obtained through catalytic asymmetric 1,3-dipolar cycloaddition reaction using ketimine as a reaction substrate and using a chiral ligand and a Lewis acid.
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公开(公告)号：US20200347030A1
公开(公告)日：2020-11-05
申请号：US16646130
申请日：2018-09-13
发明人： Toru Taniguchi , Osamu Iwamoto , Keiji Saito , Katsuyoshi Nakajima , Yasuyuki Ogawa , Nobuya Kurikawa , Seiko Nagata , Kaori Ito , Eriko Kioi
IPC分类号： C07D401/14 , C07D403/14 , C07D471/04 , C07D405/14 , C07D413/14 , C07D498/10
摘要： An object of the present invention is to provide a compound having an anti-inflammatory activity or a pharmacologically acceptable salt thereof.The solution of the present invention is a compound of general formula (1) or a pharmacologically acceptable salt thereof. wherein the symbols in the formula are defined below: A: e.g., Benzene, E: e.g., —CH2—, G: e.g., a 5-membered aromatic heterocyclic ring, X: e.g., cyclohexane, J: e.g., a 5-membered aromatic heterocyclic ring, Y: e.g., a phenyl group, R1, R2, R3: e.g., a halogen atom, R4: e.g., a C1-C6 alkyl group, R5: e.g., a hydrogen atom, R6a, R6b, R6c, R6d: e.g., a hydrogen atom, R7: e.g., a hydrogen atom, R8: e.g., a hydrogen atom, n1, n2, n3: e.g., 1.
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公开(公告)号：US10765738B2
公开(公告)日：2020-09-08
申请号：US15575255
申请日：2016-05-18
IPC分类号： A61K39/395 , A61K31/07 , A61K31/122 , A61K31/355 , A61K31/785 , C07K16/28 , A61K39/00 , A61K31/59 , A61K31/787 , A61K45/06 , A61K38/17 , A61P21/00 , A61P9/00 , A61P3/04 , A61P3/10 , A61P13/12 , A61P35/00 , A61K31/395
摘要： The present invention relates to the amelioration of toxic effects that are caused by therapies aimed at FGFR4-inhibition. In particular, the invention relates to the combination of FGFR4 inhibitors and agents capable of reducing bile acid levels and to the use thereof in the treatment of diseases.
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公开(公告)号：US20200171163A1
公开(公告)日：2020-06-04
申请号：US16613203
申请日：2018-05-14
发明人： Atsuko SAITO , Tsuyoshi HIRATA , Kensuke NAKAMURA
IPC分类号： A61K47/68 , C07K16/28 , A61P35/00 , A61K31/4745
摘要： It is an object of the present invention to provide an antibody binding to CDH6 and having internalization activity, an antibody-drug conjugate of the antibody and a drug having antitumor activity, a pharmaceutical product comprising the antibody-drug conjugate and having therapeutic effects on a tumor, a method for treating a tumor using the antibody, the antibody-drug conjugate or the pharmaceutical product, and the like. The present invention provides an anti-CDH6 antibody having internalization activity, an antibody-drug conjugate of the antibody and a drug having antitumor activity, a pharmaceutical product comprising the antibody or the antibody-drug conjugate, and a method for treating a tumor.
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36.发明申请公开(公告)号：US20200061031A1
公开(公告)日：2020-02-27
申请号：US16485777
申请日：2018-02-27
IPC分类号： A61K31/436 , A61K31/506 , A61K31/517 , A61K31/535 , C07K16/32
摘要： [Problem] To provide a therapeutic agent and a therapeutic method for EGFR-TKI-resistant non-small cell lung cancer.[Solution] Provided are: a therapeutic agent that contains an anti-HER3 antibody-drug conjugate as an active ingredient, or a therapeutic method characterized by administering an anti-HER3 antibody-drug conjugate.
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公开(公告)号：US20200039974A1
公开(公告)日：2020-02-06
申请号：US16337896
申请日：2017-09-28
发明人： Hiroaki Inagaki , Yoshihiro Shibata , Hidenori Namiki , Hideaki Kageji , Kiyoshi Nakayama , Yasuyuki Kaneta
IPC分类号： C07D413/14 , C07D401/14
摘要： The present invention relates to a compound having RET kinase inhibiting action or a pharmaceutically acceptable salt thereof, useful in the treatment of diseases such as cancer. In particular a compound represented by the following general formula (I) as defined herein: (I) or a pharmaceutically acceptable salt thereof.
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公开(公告)号：US20190309028A1
公开(公告)日：2019-10-10
申请号：US16465930
申请日：2017-12-01
发明人： Hanako ITO , Yasunori ONO , Kensuke NAKAMURA
摘要： The present invention provides a novel endo-β-N-acetylglucosaminidase that is isolated from a fungus belonging to the genus Rhizomucor and is active under high-temperature conditions; various mutant enzymes thereof; genes encoding the enzymes; a recombinant plasmid; a transformant transformed with the plasmid; and the like.
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公开(公告)号：US10383878B2
公开(公告)日：2019-08-20
申请号：US15285156
申请日：2016-10-04
发明人： Thore Hettmann , Reimar Abraham , Sabine Blum , Suguru Ueno
IPC分类号： A61K39/395 , A61K31/5377 , C07K16/28 , C07K16/32 , A61K47/68 , C07K16/30 , A61K39/00
摘要： To provide an antitumor drug having excellent therapeutic effect, which is excellent in terms of antitumor effect and safety. Provided is an antibody-drug conjugate in which an antitumor compound represented by the following formula is conjugated to an anti-HER3 antibody via a linker having a structure represented by the formula: -L1-L2-LP-NH—(CH2)n1-La-(CH2)n2-C(═O)— or -L1-L2-LP- (the anti-HER3 antibody is connected to the terminal of L1, the antitumor compound is connected to the carbonyl group of —(CH2)n2-C(═O)— moiety or the C terminal of LP, with the nitrogen atom of the amino group at position 1 as a connecting position).
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公开(公告)号：US10358498B2
公开(公告)日：2019-07-23
申请号：US15503095
申请日：2015-08-11
发明人： Reimar Abraham , Keisuke Fukuchi , Tanja Lange , Johannes Bange , Ichiro Watanabe , Shinko Hayashi , Toshiaki Ohtsuka
摘要： The present invention relates to novel antibodies against the FGF receptor 4 (FGFR4) and to the medical use thereof, in particular for the diagnosis prevention or treatment of diseases associated with FGFR expression, over expression or hyperactivity.
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