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公开(公告)号：US11471436B2
公开(公告)日：2022-10-18
申请号：US15532389
申请日：2015-12-03
发明人： Kensuke Kusumi , Haruto Kurata , Atsushi Naganawa , Yasuyo Kodera , Yuichi Inagaki , Hiroya Takizawa , Mark Allan Wolf , Joseph Raker
IPC分类号： A61K31/397 , A61P25/28 , C07D205/04 , C07D401/10 , C07D207/16 , C07D403/10 , A61K31/015 , A61K31/19 , C07C13/20 , C07C13/48
摘要： A compound represented by general formula (I) wherein all the symbols are as defined in the specification has a selective S1P5 receptor agonist activity due to having a linker from a phenyl group to a cyclic substituent in a dihydronaphthalene skeleton; i.e., due to having a short linker of one atom or less as L in general formula (I), and can therefore serve as an agent for treating S1P5-mediated disease, e. g., neurodegenerative disease such as schizophrenia.
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公开(公告)号：US20220204468A1
公开(公告)日：2022-06-30
申请号：US17695796
申请日：2022-03-15
IPC分类号： C07D309/06 , A61P25/20 , C07C233/81 , C07C235/64 , C07C327/48
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.
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公开(公告)号：US11261154B2
公开(公告)日：2022-03-01
申请号：US17264603
申请日：2019-07-30
发明人： Shoji Nojima , Kenji Sasaki , Tohru Kambe , Takashi Konemura , Yoshikazu Goto
IPC分类号： C07C311/21
摘要： A compound represented by general formula (I) (in the formula, all symbols are as described in the description) or a salt thereof has a potent nerve-protecting and/or -repairing activity, and therefore can be used as a therapeutic agent for neuropathy (e.g., chronic inflammatory demyelinating polyneuropathy, Guillain-Barre syndrome, periarteritis nodosa, allergic vasculitis, diabetic peripheral neuropathy, entrapment neuropathy, peripheral neuropathy associated with the administration of a chemotherapeutic drug, or peripheral neuropathy associated with Charcot-Marie-Tooth disease).
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公开(公告)号：US20220033371A1
公开(公告)日：2022-02-03
申请号：US17276284
申请日：2019-09-19
IPC分类号： C07D309/06 , C07C235/64 , C07C233/81 , C07C327/48 , A61P25/20
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.
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![NOVEL CRYSTAL OF (3S)-3-[2-(6-AMINO-2-FLUOROPYRIDIN-3-YL)-4-FLUORO-1H-IMIDAZOL-5-YL]-7-[5-CHLORO-2-(1H-TETRAZOL-1-YL)PHENYL]-2,3-DIHYDROINDOLIZIN-5(1H)-ONE](/abs-image/US/2021/12/23/US20210395250A1/abs.jpg.150x150.jpg)
公开(公告)号：US20210395250A1
公开(公告)日：2021-12-23
申请号：US17297649
申请日：2019-11-29
发明人： Takayuki FUJITO , Shizuka ONO , Shuhei OHTANI
IPC分类号： C07D471/04
摘要： A novel crystal form of (3S)-3-[2-(6-amino-2-fluoropyridin-3-yl)-4-fluoro-1H-imidazol-5-yl]-7-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]-2,3-dihydroindolizin-5(1H)-one, which is (3S)-3-[2-(6-amino-2-fluoropyridin-3-yl)-4-fluoro-1H-imidazol-5-yl]-7-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]-2,3-dihydroindolizin-5(1H)-one-3-hydroxybenzoic acid (1/1).
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公开(公告)号：US20210332009A1
公开(公告)日：2021-10-28
申请号：US17264603
申请日：2019-07-30
发明人： Shoji NOJIMA , Kenji SASAKI , Tohru KAMBE , Takashi KONEMURA , Yoshikazu GOTO
IPC分类号： C07C311/21
摘要： A compound represented by general formula (I) (in the formula, all symbols are as described in the description) or a salt thereof has a potent nerve-protecting and/or -repairing activity, and therefore can be used as a therapeutic agent for neuropathy (e.g., chronic inflammatory demyelinating polyneuropathy, Guillain-Barre syndrome, periarteritis nodosa, allergic vasculitis, diabetic peripheral neuropathy, entrapment neuropathy, peripheral neuropathy associated with the administration of a chemotherapeutic drug, or peripheral neuropathy associated with Charcot-Marie-Tooth disease).
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公开(公告)号：US11052091B2
公开(公告)日：2021-07-06
申请号：US16472192
申请日：2017-12-20
IPC分类号： C07D473/14 , A61K31/52 , A61P35/00 , A61K31/5377 , A61K31/538 , C07D473/16
摘要： The present invention relates to a Brk inhibitory compound represented by general formula (I) (wherein, all symbols represent the same meanings as the symbols set forth in the specification), a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug of any of these.
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公开(公告)号：US20210198361A1
公开(公告)日：2021-07-01
申请号：US17058794
申请日：2019-05-30
发明人： Hiroyoshi NISHIKAWA , Yosuke TOGASHI , Yukiya OHYAMA , Takao YOSHIDA , Kazuhiko TAKEDA , Kenichi KODA , Atsushi HONDA , Atsushi OYAGI , Toru KAKINUMA , Masayuki MURATA
摘要： The object of the present invention is to provide a method for identifying a patient with malignant tumor on which the effect of an immune checkpoint inhibitor can be more expected, and agents for suppressing the progression of, suppressing the recurrence of, and/or treating malignant tumor, characterized by prescriptions based on those.
The present invention can provide agents for suppressing the progression of, suppressing the recurrence of, and/or treating malignant tumor, characterized by prescriptions based on identifying a patient with a malignant tumor on which the effect of an immune checkpoint inhibitor can be more expected, by analyzing the evaluation items consisting of combinations such as the PD-1 expression intensity, the percentage of the number of PD-1 expressing cells and the like in Treg cells and CD8+ T cells in tumor tissue or blood.-
公开(公告)号：US20210169842A1
公开(公告)日：2021-06-10
申请号：US17149327
申请日：2021-01-14
发明人： Tohru KAMBE , Toru MARUYAMA , Shinsaku YAMANE , Satoshi NAKAYAMA , Kousuke TANI
IPC分类号： A61K31/335 , C07D313/06 , A61K31/4427 , C07D407/12 , A61K9/00 , C07D417/04 , C07D405/06 , A61K31/558 , C07D401/06
摘要： Since a compound represented by the general formula (I) (wherein definition of each group is as described in the specification), a salt thereof, a solvate thereof, or a prodrug thereof has strong and sustaining intraocular pressure lowering activity and, further, has no side effect on eyes such as ocular stimulating property (hyperemia, corneal clouding etc.), aqueous humor protein rise etc., it has high safety, and can be an excellent agent for preventing and/or treating glaucoma etc.
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公开(公告)号：US10738280B2
公开(公告)日：2020-08-11
申请号：US15558473
申请日：2016-03-17
发明人： Hideyuki Okano , Seiji Shiozawa , Fumihiko Kisa
摘要： To produce and/or maintain naïve 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 naïve 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.
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