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公开(公告)号：US20230192890A1
公开(公告)日：2023-06-22
申请号：US17933229
申请日：2022-09-19
Applicant: PUBLIC UNIVERSITY CORPORATION YOKOHAMA CITY UNIVERSITY , PUBLIC UNIVERSITY CORPORATION NAGOYA CITY UNIVERSITY , PHARMA FOODS INTERNATIONAL CO., LTD.
Inventor： Mamoru SATO , Michiyuki YAMADA , Satoshi KANAZAWA , Masayoshi TOYOURA , Yuji SHOYA , Kenji SAITO , Chihiro YAMAZAKI
IPC: C07K16/40 , C12N9/99 , C12N15/09 , A61K39/395 , C12N15/63
CPC classification number: C07K16/40 , C12N9/99 , C12N15/09 , A61K39/395 , A61K39/3955 , C12N15/63 , C12Y305/03015 , C07K2317/33 , C07K2317/622 , A61K2039/505
Abstract: Provided are anti-PAD4 antibodies having excellent properties and an excellent method for treatment of RA. Used are anti-PAD4 antibodies that specifically bind to an epitope containing positions 345, 347, and 348 of PAD4. These anti-PAD4 antibodies may inhibit the citrullination activity of PAD4. In addition, these anti-PAD4 antibodies may have a KD (M) of 9.0×10−9 or less. Optionally, the anti-PAD4 antibody and a TNFα inhibitor are used in combination.
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公开(公告)号：US20180360832A1
公开(公告)日：2018-12-20
申请号：US15993299
申请日：2018-05-30
Applicant: ICOS CORPORATION
Inventor： Chanchal SADHU , Ken DICK , Jennifer TREIBERG , C. Gregory SOWELL , Edward A. KESICKI , Amy OLIVER
IPC: A61K31/506 , C07D473/32 , C07D473/24 , C07D473/38 , C07D473/40 , C07D473/34 , C12N9/12 , C12N9/99 , C07D473/16 , C07D473/00 , C07D473/30 , C07D403/12 , C07D487/04
CPC classification number: A61K31/506 , C07D403/12 , C07D473/00 , C07D473/16 , C07D473/24 , C07D473/30 , C07D473/32 , C07D473/34 , C07D473/38 , C07D473/40 , C07D487/04 , C12N9/1205 , C12N9/99 , C12Y207/01137
Abstract: Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3Kδ plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3Kδ, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3Kδ activity, including compounds that selectively inhibit PI3Kδ activity. Methods of using PI3Kδ inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3Kδ inhibitory compounds to inhibit PI3Kδ-mediated processes in vitro and in vivo.
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公开(公告)号：US10010550B2
公开(公告)日：2018-07-03
申请号：US15589910
申请日：2017-05-08
Applicant: ICOS CORPORATION
Inventor： Chanchal Sadhu , Ken Dick , Jennifer Treiberg , C. Gregory Sowell , Edward A. Kesicki , Amy Oliver
IPC: A61K31/513 , A61K31/506 , C07D473/32 , C12N9/12 , C07D487/04 , C07D473/40 , C12N9/99 , C07D473/34 , C07D473/30 , C07D473/24 , C07D473/16 , C07D473/00 , C07D403/12 , C07D473/38
CPC classification number: A61K31/506 , C07D403/12 , C07D473/00 , C07D473/16 , C07D473/24 , C07D473/30 , C07D473/32 , C07D473/34 , C07D473/38 , C07D473/40 , C07D487/04 , C12N9/1205 , C12N9/99 , C12Y207/01137
Abstract: Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3Kδ plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3Kδ, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3Kδ activity, including compounds that selectively inhibit PI3Kδ activity. Methods of using PI3Kδ inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3Kδ inhibitory compounds to inhibit PI3Kδ-mediated processes in vitro and in vivo.
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公开(公告)号：US10005732B2
公开(公告)日：2018-06-26
申请号：US14930409
申请日：2015-11-02
Inventor： Donald W. Landry , Yuli Xie , Yidong Liu , Gangli Gong , Shi-Xian Deng , Kirsten Alison Rinderspacher
IPC: C07D211/96 , C07D211/62 , C07D401/12 , C07D409/12 , C12N9/99 , C07F9/59
CPC classification number: C07D211/96 , C07D211/62 , C07D401/12 , C07D409/12 , C07F9/59 , C12N9/99
Abstract: The present invention relates to compounds that exhibit vasodilatory and anti-inflammatory effects by inhibiting the activity of soluble epoxide hydrolase (sEH). The present invention is also directed to methods of identifying such compounds, and use of such compounds for the treatment of diseases related to dysfunction of vasodilation, inflammation, and/or endothelial cells. In particular non-limiting embodiments, components of the invention may be used to treat hypertension.
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公开(公告)号：US09957315B2
公开(公告)日：2018-05-01
申请号：US15138682
申请日：2016-04-26
Applicant: Grifols, S.A.
Inventor： David Ownby , Thomas P. Zimmerman , Jennifer A. Hunt , Charles Miller , Senthil Ranganathan , Tonny Dessources
IPC: C12N7/00 , C12N7/01 , C12N7/02 , C12N9/99 , C12Q1/37 , A23J1/00 , C07K1/00 , C07K14/00 , C07K16/00 , C07K17/00 , C07K14/81 , C07K14/47 , C07K1/36 , C12N15/86
CPC classification number: C07K14/8125 , C07K1/36 , C07K14/4703 , C12N7/00 , C12N9/99 , C12N15/86 , C12Q1/37
Abstract: Described herein are methods for purifying recombinant, cell culture derived alpha1-protease inhibitor and removing a colored species that co-purifies with the recA1PI protein. Also described are methods for reducing the iron in cell culture derived alpha1-protease inhibitor.
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6.发明申请
公开(公告)号：US20170283378A1
公开(公告)日：2017-10-05
申请号：US15512237
申请日：2015-09-18
Applicant: Consejo Superior de Investigaciones Cientificas (CSIC) , Centro de Investigacion Biomedica en Red (CIBER)
IPC: C07D209/42 , C12N9/99 , C07D401/04 , A61K31/405 , C07D413/02 , C07D405/04
CPC classification number: C07D209/42 , A61K31/404 , A61K31/405 , A61P3/06 , A61P25/08 , A61P25/28 , A61P35/00 , C07D401/04 , C07D405/04 , C07D413/02 , C12N9/99
Abstract: The invention relates to substituted heterocyclic indole derivatives of Formula (I), which act as activators of the AMP-activated protein kinase (AMPK) and to the use of them for the treatment and prevention of diseases or disorders regulated by AMPK. As a result, these compounds can be used for the treatment of inflammatory, autoimmune, cardiovascular, neurological diseases and cancer.
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公开(公告)号：US09765055B2
公开(公告)日：2017-09-19
申请号：US14589690
申请日：2015-01-05
Applicant: Northwestern University
Inventor： Richard B. Silverman , Fengtian Xue
IPC: C07D401/06 , C07D405/14 , C12N9/99
CPC classification number: C07D401/06 , C07D405/14 , C12N9/99
Abstract: Compounds and related compositions and methods as can be used to selectively inhibit neuronal nitric oxide synthase and as can be employed in the treatment of various neurodegenerative diseases.
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公开(公告)号：US20170197983A1
公开(公告)日：2017-07-13
申请号：US15467548
申请日：2017-03-23
Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
Inventor： Tatsuki KOIKE , Yuichi KAJITA , Masato YOSHIKAWA , Shuhei IKEDA , Eiji KIMURA , Tomoaki HASUI , Toshiya NISHI , Hiromi FUKUDA
IPC: C07D498/08 , C07D413/14 , C07D417/14 , C07D471/08 , C07D471/10 , C07D405/14 , C07D213/74 , C07D239/42 , C07D401/04 , C07D401/14 , C07D487/18
CPC classification number: C07D498/08 , A61K9/2018 , A61K9/4858 , C07D213/12 , C07D213/72 , C07D213/74 , C07D239/42 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D451/02 , C07D451/04 , C07D471/08 , C07D471/10 , C07D487/08 , C07D487/10 , C07D487/18 , C07D491/08 , C07D491/18 , C12N9/99
Abstract: An object of the present invention is to provide a compound having a superior CH24H inhibitory action, which is useful as an agent for the prophylaxis or treatment of epilepsy, neurodegenerative disease and the like. The present invention relates to a compound represented by the formula: wherein each symbol is as defined in the specification, or a salt thereof.
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公开(公告)号：US20170049772A1
公开(公告)日：2017-02-23
申请号：US15281702
申请日：2016-09-30
Applicant: ICOS CORPORATION
Inventor： Chanchal SADHU , Ken DICK , Jennifer TREIBERG , C. Gregory SOWELL , Edward A. KESICKI , Amy OLIVER
IPC: A61K31/506 , C12N9/99 , C12N9/12
CPC classification number: A61K31/506 , C07D403/12 , C07D473/00 , C07D473/16 , C07D473/24 , C07D473/30 , C07D473/32 , C07D473/34 , C07D473/38 , C07D473/40 , C07D487/04 , C12N9/1205 , C12N9/99 , C12Y207/01137
Abstract: Methods of inhibiting phosphotidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating disease, such as disorders of immunity and inflammation, in which PI3Kδ plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3Kδ, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3Kδ activity, including compounds that selectively inhibit PI3Kδ activity. Methods of using PI3Kδ inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3Kδ inhibitory compounds to inhibit PI3Kδ-mediated processes in vitro and in vivo.
Abstract translation: 公开了抑制磷脂酰肌醇3-激酶δ同种型（PI3Kδ）活性的方法，以及治疗PI3Kδ在白细胞功能中起作用的疾病如免疫和炎症病症的方法。 优选地，所述方法使用选择性抑制PI3Kδ的活性剂，而不显着抑制其它PI3K同种型的活性。 提供抑制PI3Kδ活性的化合物，包括选择性抑制PI3Kδ活性的化合物。 还提供了使用PI3Kδ抑制化合物抑制癌细胞生长或增殖的方法。 因此，本发明提供了在体外和体内使用PI3Kδ抑制化合物抑制PI3Kδ介导的过程的方法。
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公开(公告)号：US20170007583A1
公开(公告)日：2017-01-12
申请号：US15116296
申请日：2015-02-04
Applicant: LYTIX BIOPHARMA AS
Inventor： John S. SVENDSEN , Wenche STENSEN , Frederick A. LEESON
IPC: A61K31/428 , C12N9/99 , A61K31/4439
CPC classification number: A61K31/428 , A61K31/4439 , C12N9/99
Abstract: The present invention provides a compound of formula (I) wherein: Y represents a C or N atom which may be substituted or form a cyclic group with R′″ but may not be a quaternary C atom; R′ is —OR1, —CONH2, —CF3, F, —OH, —NO2, —CN or —OCOR1 in which R1, is C1-3 alkyl and each may be in the beta or gamma position; R″ is C1-3 alkyl or H; and R′″ is H or a group consisting of 1-12 non-hydrogen atoms and may be linear, branched and/or incorporate one or more cyclic groups, cyclic groups may be aromatic and/or heterocyclic and 2 or more cyclic groups may be linked or fused and each may be substituted; or a salt, hydrate or solvate of a compound of formula (I) for use in the treatment or prevention of a neurodegenerative disorder by inhibiting formation of neurofibrillary (tau) tangles and/or by inhibiting Dyrk 1A. The invention further relates to non-therapeutic uses of these compounds.
Abstract translation: 本发明提供了式（I）化合物，其中：Y表示可以被取代或与R''形成环状基团但不可以是季C原子的C或N原子; R'是-OR 1，-CONH 2 ，-CF 3，F，-OH，-NO 2，-CN或-OCOR 1，其中R 1，是C 1-3烷基，各自可以是β或γ位; R“是C 1-3烷基或H; 并且R'“是H或由1-12个非氢原子组成的基团，并且可以是直链，支链和/或并入一个或多个环状基团，环状基团可以是芳族和/或杂环的，并且2个或更多个环状基团可以 连接或稠合并且各自可以被取代;或式（I）化合物的盐，水合物或溶剂化物，其用于通过抑制神经原纤维（tau）缠结的形成和/或通过抑制来治疗或预防神经变性疾病 Dyrk 1A。本发明还涉及这些化合物的非治疗用途。
