公开(公告)号：US20170296521A1

公开(公告)日：2017-10-19

申请号：US15508012

申请日：2015-09-01

申请人： Daiichi Sankyo Company, Limited

发明人： Yoshiyuki Morishima ,  Yuko Honda ,  Chikako Kamisato

IPC分类号： A61K31/444 ,  A61K31/616 ,  A61K31/519 ,  A61K45/06 ,  A61K31/4365

CPC分类号： A61K31/444 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/4465 ,  A61K31/4709 ,  A61K31/519 ,  A61K31/60 ,  A61K31/616 ,  A61K45/00 ,  A61K45/06 ,  A61K2300/00

摘要： It is intended to provide a novel pharmaceutical composition that can suppress thromboembolism after stent placement. The present invention provides a pharmaceutical composition for the suppression of thromboembolism after stent placement, comprising edoxaban or a pharmaceutically acceptable salt thereof, or a hydrate of the compound or the salt.

公开(公告)号：US09751887B2

公开(公告)日：2017-09-05

申请号：US14926973

申请日：2015-10-29

申请人： Daiichi Sankyo Company, Limited

发明人： Yasuyuki Takeda ,  Kenji Yoshikawa ,  Yoshiko Kagoshima ,  Yuko Yamamoto ,  Ryoichi Tanaka ,  Yuichi Tominaga ,  Masaki Kiga ,  Yoshito Hamada

IPC分类号： C07D487/04

CPC分类号： C07D487/04

摘要： The present invention is intended to provide a compound or a pharmacologically acceptable salt thereof which is useful in the treatment of a tumor through its ROS1 kinase enzyme activity inhibitory effect and NTRK kinase enzyme inhibitory effect. The present invention provides a compound having an imidazo[1,2-b]pyridazine structure represented by the general formula (I) or a pharmacologically acceptable salt thereof, and a pharmaceutical composition comprising the compound. In the formula, R1, G, T, Y1, Y2, Y3, and Y4 are as defined herein.

公开(公告)号：US20170240562A1

公开(公告)日：2017-08-24

申请号：US15314887

申请日：2016-07-07

申请人： Daiichi Sankyo Company, Limited ,  Sanford Burnham Prebys Medical Discovery Institute

发明人： Shojiro Miyazaki ,  Yuko Yamamoto ,  Keisuke Suzuki ,  Masaharu Inui ,  Masanori Izumi ,  Kaori Soma ,  Anthony Pinkerton ,  Taeko Shinozaki

IPC分类号： C07D498/04

CPC分类号： C07D498/10 ,  A61K9/20 ,  A61K9/48 ,  A61K31/553 ,  C07D498/04

摘要： The present invention relates to a compound or a pharmacologically acceptable salt thereof having excellent tissue non-specific alkaline phosphatase inhibitory activity. The present invention provides a compound represented by the formula (I): wherein R1 represents a hydrogen atom, an optionally substituted C1-6 alkyl group, or the like, R2 and R3 are the same or different and each represent a hydrogen atom, an optionally substituted C1-6 alkyl group, or the like, R4 and R5 are the same or different and each represent a hydrogen atom, an optionally substituted C1-6 alkyl group, or the like, R6 represents a hydrogen atom or the like, each R7 may be the same or different and may each represent an optionally substituted C1-6 alkoxy group or the like, X represents —CH═, —C(—R7)═, or —N═, and m represents 1 to 4, or a pharmacologically acceptable salt thereof.

公开(公告)号：US20170233341A1

公开(公告)日：2017-08-17

申请号：US15582064

申请日：2017-04-28

申请人： Daiichi Sankyo Company, Limited

发明人： Masashi Watanabe ,  Takahiro Okachi ,  Michiaki Kawahara ,  Hiroshi Nagasawa ,  Noritada Sato ,  Takashi Takita ,  Gen Hasegawa

IPC分类号： C07D207/34

CPC分类号： C07D207/34 ,  A61K9/0095 ,  A61K9/2018 ,  A61K9/4858 ,  C07B2200/13 ,  C07D471/08

摘要： The present invention provides a production intermediate of an atropisomer of a pyrrole derivative having excellent mineralocorticoid receptor antagonistic activity, a method for producing the same, and a crystal thereof. A method for producing an atropisomer of a pyrrole derivative including a step of resolving a compound represented by the following general formula (I) [wherein R1 represents a methyl group or a trifluoromethyl group, R2 represents a hydrogen atom or a C1-C3 alkoxy group, and n represents an integer selected from 1 to 3] into its atropisomers, characterized by using an optically active amine having a cinchonine skeletal formula, and a crystal of (S)-1-(2-hydroxyethyl)-4-methyl-N-[4-(methylsulfonyl)phenyl]-5-[2-(trifluoromethyl)phenyl]-1H-pyrrole-3-carboxamide.

公开(公告)号：US09657050B2

公开(公告)日：2017-05-23

申请号：US14858404

申请日：2015-09-18

申请人： DAIICHI SANKYO COMPANY, LIMITED ,  Masafumi Matsuo ,  Yasuhiro Takeshima ,  Orphan Disease Treatment Institute Co., Ltd.

发明人： Masafumi Matsuo ,  Yasuhiro Takeshima ,  Makoto Koizumi

IPC分类号： C07H21/02 ,  C07H21/04 ,  C12N15/113 ,  A61K38/00 ,  A61K48/00

CPC分类号： C07H21/04 ,  A61K38/00 ,  A61K48/00 ,  C12N15/113 ,  C12N2310/11 ,  C12N2310/3231 ,  C12N2320/33

摘要： Oligonucleotides having a nucleotide sequence complementary to nucleotide numbers such as 2571-2607, 2578-2592, 2571-2592, 2573-2592, 2578-2596, 2578-2601 or 2575-2592 of the dystrophin cDNA (Gene Bank accession No. NM_004006.1) and therapeutic agents for muscular dystrophy comprising such oligonucleotides.

公开(公告)号：US20170080049A1

公开(公告)日：2017-03-23

申请号：US15122011

申请日：2015-02-26

申请人： DAIICHI SANKYO COMPANY, LIMITED

发明人： Naomi MOROZUMI

IPC分类号： A61K38/16 ,  A61K31/573

CPC分类号： A61K38/16 ,  A61K9/0019 ,  A61K31/573 ,  A61K38/08 ,  A61K38/10 ,  A61K45/06 ,  A61K47/60 ,  A61K2300/00

摘要： Provided is a medicine for reducing and/or ameliorating growth failure induced by the administration of a steroid during a growth period, the medicine containing at least one type of natriuretic peptide receptor B (NPR-B) agonist as an active ingredient.

公开(公告)号：US20170050983A1

公开(公告)日：2017-02-23

申请号：US15118903

申请日：2015-02-13

申请人： DAIICHI SANKYO COMPANY, LIMITED

发明人： Tsuyoshi UEDA

IPC分类号： C07D513/04

CPC分类号： C07D513/04 ,  A61K31/444

摘要： An object of the present invention is to provide a novel method for producing a compound, a salt thereof, or a hydrate of the compound or the salt, which is an FXa inhibitor. The object can be attained by a production method in which a production method via a compound represented by formula (1-1), etc., from a compound represented by the following formula (1-x), etc., is used for a method for producing a compound represented by the following formula (X), etc. [wherein X represents a halogen atom or the like, and R1 represents an optionally substituted phenyl group].

摘要翻译： 本发明的目的是提供一种制备作为FXa抑制剂的化合物或其盐的化合物或其水合物的新方法。 该目的可以通过以下制备方法来实现：其中通过由下式（1-x）等表示的化合物等通过式（1-1）等表示的化合物的制备方法用于 用于制备由下式（X）表示的化合物的方法等[其中X表示卤素原子等，R 1表示任选取代的苯基]。

公开(公告)号：US20170035906A1

公开(公告)日：2017-02-09

申请号：US15302803

申请日：2015-04-06

申请人： DAIICHI SANKYO COMPANY, LIMITED

发明人： Hiroyuki NAITO ,  Takeshi MASUDA ,  Takashi NAKADA ,  Masao YOSHIDA ,  Shinji ASHIDA ,  Hideki MIYAZAKI ,  Yuji KASUYA ,  Koji MORITA ,  Yusuke OGITANI ,  Yuki ABE

IPC分类号： A61K47/48 ,  A61K31/4745 ,  C07K7/06 ,  C07K16/32 ,  C07K16/30

CPC分类号： A61K47/48646 ,  A61K31/4745 ,  A61K39/395 ,  A61K47/6803 ,  A61K47/6871 ,  C07K7/06 ,  C07K16/30 ,  C07K16/3015 ,  C07K16/3023 ,  C07K16/303 ,  C07K16/3038 ,  C07K16/3046 ,  C07K16/3061 ,  C07K16/3069 ,  C07K16/32

摘要： As an antitumor drug which is excellent in terms of antitumor effect and safety and has an excellent therapeutic effect, there is provided an antibody-drug conjugate in which an antitumor compound represented by the following formula is conjugated to an anti-HER2 antibody via a linker having a structure represented by the formula: L1-L2-LP-NH—(CH2)n1-La-Lb-Lc or -L1-L2-LP- wherein the anti-HER2 antibody is connected to the terminal L1, and the antitumor compound is connected to the terminal Lc or LP with the nitrogen atom of the amino group at position 1 as the connecting position.

摘要翻译： 作为抗肿瘤效果和安全性优异并且具有优异治疗效果的抗肿瘤药物，提供了抗体 - 药物偶联物，其中由下式表示的抗肿瘤化合物通过接头与抗HER2抗体缀合 具有下列结构：L 1 -L 2 -LP -NH-（CH 2）n 1 -L a -L b -L ​​c或-L 1 -L 2 -LP - 其中抗HER2抗体为 连接到末端L 1，并且将抗肿瘤化合物连接到位置1处的氨基的氮原子的末端L c或LP连接作为连接位置。

公开(公告)号：US09562096B2

公开(公告)日：2017-02-07

申请号：US14966292

申请日：2015-12-11

申请人： DAIICHI SANKYO COMPANY, LIMITED

发明人： Yoshitaka Isumi ,  Toshiyuki Sato ,  Jun Hasegawa ,  Tatsuya Inoue

IPC分类号： C07K16/00 ,  A61K39/395 ,  C07K16/28 ,  A61K39/00

CPC分类号： C07K16/28 ,  A61K39/3955 ,  A61K2039/505 ,  C07K16/2803 ,  C07K2317/24 ,  C07K2317/33 ,  C07K2317/565 ,  C07K2317/70 ,  C07K2317/75 ,  C07K2317/76 ,  C07K2317/92

摘要： Problem to be SolvedThe present invention relates to an antibody having an anti-angiogenesis activity. More specifically, the present invention relates to an antibody against ROBO4 and a pharmaceutical composition containing the antibody. An object of the present invention is to provide an anti-ROBO4 antibody having an anti-angiogenesis effect, a pharmaceutical composition or the like comprising the antibody, a method for suppressing angiogenesis using the antibody, etc. Another object of the present invention is to provide a method for producing the antibody. The antibody of the present invention activates the downstream signal of ROBO4 and has a suppressive activity against cell migration induced by VEGF or bFGF. The antibody of the present invention also exhibits an anti-angiogenesis effect in in-vivo models.

摘要翻译： 本发明涉及具有抗血管生成活性的抗体。 更具体地，本发明涉及抗ROBO4的抗体和含有抗体的药物组合物。 本发明的目的是提供具有抗血管生成作用的抗ROBO4抗体，包含抗体的药物组合物等，抑制使用该抗体的血管生成的方法等。本发明的另一个目的是 提供生产抗体的方法。 本发明的抗体激活ROBO4的下游信号，并且具有抗VEGF或bFGF诱导的细胞迁移的抑制活性。 本发明的抗体在体内模型中也表现出抗血管生成作用。

公开(公告)号：US09555077B2

公开(公告)日：2017-01-31

申请号：US14002570

申请日：2011-09-02

申请人： Noboru Murakami ,  Keiko Nakahara ,  Kenji Kangawa

发明人： Noboru Murakami ,  Keiko Nakahara ,  Kenji Kangawa

IPC分类号： A61K38/18 ,  A61K38/22

CPC分类号： A61K38/22

摘要： An object of the present invention is to provide a hypothermic agent for an animal, a therapeutic agent for hyperthermia in an animal, etc. The present invention provides a hypothermic agent for an animal, a therapeutic agent for hyperthermia in an animal, etc., the agents etc. comprising desacyl ghrelin or its derivative, or a pharmaceutically acceptable salt thereof as an active ingredient.

摘要翻译： 本发明的目的在于提供动物的低温药，动物体内的热疗用治疗剂等。本发明提供动物用低温药，动物体内的高热治疗剂等， 所述药剂等包含脱酰基生长素释放肽或其衍生物或其药学上可接受的盐作为活性成分。