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公开(公告)号：US10442797B2
公开(公告)日：2019-10-15
申请号：US15036981
申请日：2015-07-06
发明人： Noriyasu Haginoya , Takashi Suzuki , Miho Hayakawa , Masahiro Ota , Tomoharu Tsukada , Katsuhiro Kobayashi , Yosuke Ando , Takeshi Jimbo , Koichi Nakamura
IPC分类号： C07D405/14 , C07D409/14 , A61K31/444 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/5377 , C07B59/00 , C07C309/04 , C07C309/35
摘要： The present disclosure provides novel compounds or salts thereof, or crystals of the compounds or the salts, which inhibit Axl and are useful in the treatment of a disease caused by hyperfunction of Axl, the treatment of a disease associated with hyperfunction of Axl, and/or the treatment of a disease involving hyperfunction of Axl.The present disclosure provides pyridone derivatives having a tetrahydropyranylmethyl group represented by the following formula (I) having various substituents, or salts thereof, or crystals of the compounds or the salts, wherein R1, R2, R3, R4, R5, W, X, Y, and Z are each as defined in the specification:
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62.发明申请公开(公告)号：US20190240210A1
公开(公告)日：2019-08-08
申请号：US16342639
申请日：2017-10-16
发明人： Takahiko SEKI
IPC分类号： A61K31/4439 , A61P35/00 , A61K31/7052
CPC分类号： A61K31/4439 , A61K31/7052 , A61K31/706 , A61K45/00 , A61P35/00 , A61P35/02 , A61P43/00
摘要： It is intended to provide a medicament and a method for treating cancer, comprising a compound having MDM2 inhibiting activity and a DNA methyltransferase inhibitor in combination. The present invention provides a medicament comprising (3′R,4′S,5′R)—N-[(3R,6S)-6-carbamoyltetrahydro-2H-pyran-3-yl]-6″-chloro-4′-(2-chloro-3-fluoropyridin-4-yl)-4,4-dimethyl-2″-oxo-1″,2″-dihydrodispiro[cyclohexane-1,2′-pyrrolidine-3′,3″-indole]-5′-carboxamide or a pharmaceutically acceptable salt thereof and a DNA methyltransferase inhibitor in combination, and a treatment method using the compound or a salt thereof and a DNA methyltransferase inhibitor in combination.
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63.发明申请公开(公告)号：US20190112606A1
公开(公告)日：2019-04-18
申请号：US16227902
申请日：2018-12-20
申请人： NATIONAL INSTITUTES OF BIOMEDICAL INNOVATION, HEALTH AND NUTRITION , DAIICHI SANKYO COMPANY, LIMITED
发明人： Ken ISHII , Kouji KOBIYAMA , Taiki AOSHI , Fumihiko TAKESHITA , Yuji KASUYA , Takako NIWA , Makoto KOIZUMI
IPC分类号： C12N15/117 , A61K31/7125 , C12N7/00 , A61K39/145 , A61K39/155 , A61K39/39 , A61K31/713 , C07H21/04 , A61K39/12 , C08B37/00
摘要： The present invention provides an oligodeoxynucleotide containing humanized K type CpG oligodeoxynucleotide and poly deoxyadenylate, wherein the poly deoxyadenylate is placed on the 3′-side of the humanized K type CpG oligodeoxynucleotide. In addition, the present invention provides a complex containing the aforementioned oligodeoxynucleotide and β-1,3-glucan.
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公开(公告)号：US10253060B2
公开(公告)日：2019-04-09
申请号：US15704856
申请日：2017-09-14
发明人： Satoshi Komoriya , Yasuhiro Nakagami , Emiko Hatano , Takashi Ohnuki , Kayoko Masuda , Mayumi Iizuka , Yasunori Ono
IPC分类号： C12N1/14 , C07J63/00 , C07J71/00 , C12P15/00 , C12P17/02 , C12P33/00 , C12P33/02 , C12P33/06 , C12P33/20 , C12R1/645 , C12R1/785
摘要： It is intended to provide a novel terpenoid derivative that exhibits anti-inflammatory action and a cytoprotective action by activating the Keap1/Nrf2/ARE signaling pathway. The present invention provides terpenoid derivative A represented by the following formula (I):
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公开(公告)号：US10189804B2
公开(公告)日：2019-01-29
申请号：US15568691
申请日：2016-04-22
发明人： Masayuki Murakami , Yuichi Aki , Daisuke Fukatsu , Kenichi Kimura , Makoto Michida , Koji Hamaoka
IPC分类号： C07D295/155 , C07D227/04 , C07C227/04 , C07C227/42 , C07C229/48 , C07C229/52 , C07D295/14 , C07C205/57 , C07C227/06 , C07C227/10 , C07C227/36 , A61K31/4453 , C07B61/00 , C07C227/08
摘要： It is an object of the present invention to provide an excellent method for producing an excellent therapeutic agent.The solution of the present invention is as shown in the following scheme: wherein R1 represents a C1-C6 alkyl group, R2 represents a C1-C6 alkyl group, and R3 represents a C1-C6 alkyl group.
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66.发明申请公开(公告)号：US20190010450A1
公开(公告)日：2019-01-10
申请号：US15748136
申请日：2016-07-29
摘要： The present invention relates to an isolated mesenchymal stem cell-like human multipotent stem cell population characterized by being EphA7 positive, medical materials containing the cell population, and a method for producing the cell population comprising separating EphA7-positive cells from adherent cells derived from a tissue comprising capillary vessels.
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公开(公告)号：US20190008981A1
公开(公告)日：2019-01-10
申请号：US16142354
申请日：2018-09-26
发明人： Takeshi Masuda , Hiroyuki Naito , Takashi Nakada , Masao Yoshida , Shinji Ashida , Hideki Miyazaki , Yuji Kasuya , Koji Morita , Yuki Abe , Yusuke Ogitani
IPC分类号： A61K47/68 , C07K16/28 , C07K16/30 , A61K31/4745 , A61K31/48
摘要： As an antitumor drug which is excellent in terms of antitumor effect and safety, there is provided an antibody-drug conjugate in which an antitumor compound represented by the following formula is conjugated to an antibody via a linker having a structure represented by the following formula: -L1-L2-LP-NH—(CH2)n1-La-Lb-Lc- wherein the antibody is connected to the terminal of L1, and the antitumor compound is connected to the terminal of Lc with the nitrogen atom of the amino group at position 1 as a connecting position.
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公开(公告)号：US10174035B2
公开(公告)日：2019-01-08
申请号：US15560466
申请日：2016-03-29
发明人： Kirandeep Kaur Samby , Yogesh Baban Surase , Sagar Ramdas Amale , Suresh Kumar Gorla , Priyanka Patel , Ashwani Kumar Verma
IPC分类号： C07D471/04 , C07D473/34 , C07D519/00
摘要： The present invention relates to a pyrazole derivative of formula (I), a pharmaceutically acceptable salt thereof, a prodrug thereof, a hydrate thereof, stereoisomer thereof or a deuterium form thereof, wherein, n, Y, Ra, R1, R2, R3, R4, R5 and R6 are as defined hereinafter in the specification, a pharmaceutical composition comprising a compound of formula (I) as an active ingredient, methods of production, and methods of use thereof. Particularly, the present invention provides a compound of formula (I) as inhibitors of phosphatidylinositol-3-kinase (PI3K), which can be used for treating or preventing inflammatory, autoimmune, orphan and hyperproliferative disease and disorder.
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公开(公告)号：US10172806B2
公开(公告)日：2019-01-08
申请号：US15622714
申请日：2017-06-14
发明人： Shuichi Yada , Ryoichi Hayakawa , Atsutoshi Ito , Hideki Yano
IPC分类号： A61K31/485 , A61K31/135 , A61K31/194 , A61K9/08 , A61K9/20 , A61K9/00 , A61K9/50 , A61K9/14 , A61K47/14 , A61K47/32 , A61K47/34 , A61K47/36 , A61K47/38
摘要： An object of the present invention is to provide a pharmaceutical composition having abuse deterrent properties and thereby prevent the abuse of a pharmacologically active component by an abuser (abuse through snorting, abuse through injection, or abuse through snorting or injection of a temporarily extracted drug). The present invention provides a pharmaceutical composition having abuse deterrent properties that possesses both a physical barrier and a chemical barrier to being abused by an abuser, a method for producing the same and a method for using the same.
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公开(公告)号：US20190000847A1
公开(公告)日：2019-01-03
申请号：US16060643
申请日：2016-12-15
发明人： Ken ISHII
IPC分类号： A61K31/506
摘要： The present invention provides a therapeutic agent for a wound comprising a compound represented by the formula (I) wherein R1 represents a hydroxy C1-C6 alkyl group, a C2-C7 alkanoyl group, a C2-C7 alkanoyl C1-C6 alkyl group, a (C1-C6 alkoxy)carbonyl group, a (C1-C6 alkoxy)carbonyl C1-C6 alkyl group, a carboxy group, or a carboxy C1-C6 alkyl group, or a pharmacologically acceptable salt thereof as an active ingredient.
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