公开(公告)号：US09364438B2

公开(公告)日：2016-06-14

申请号：US14430956

申请日：2013-09-25

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Naoyuki Murata ,  Shigeo Yanai

IPC: A61K9/14 ,  A61K31/18 ,  A61K31/24 ,  A61K9/16

CPC classification number: A61K9/1688 ,  A61K9/14 ,  A61K31/18 ,  A61K31/24

Abstract: A method of producing crystal of a poorly water-soluble pharmaceutical compound, including mixing a solution of a poorly water-soluble pharmaceutical compound in a good solvent and nanobubble water or an aqueous nanobubble solution to precipitate crystal of the poorly water-soluble pharmaceutical compound. The crystal of a poorly water-soluble pharmaceutical compound obtained by the method is microparticulate and has more uniform particle size distribution, and is superior in the absorbability and sustainability.

Abstract translation: 一种生产水溶性差的药物化合物的方法，包括将难溶于水的药物化合物的溶液与纳米气泡水溶液或纳米气泡水溶液混合，使难溶于水的药物化合物的晶体析出。 通过该方法得到的水溶性差的药物的结晶为微粒状，粒径分布更均匀，吸收性和可持续性优异。

公开(公告)号：US09320714B2

公开(公告)日：2016-04-26

申请号：US13082890

申请日：2011-04-08

Applicant: Masahiko Koike ,  Hiroyoshi Koyama

Inventor： Masahiko Koike ,  Hiroyoshi Koyama

IPC: A61K9/28 ,  A61K9/20

CPC classification number: A61K9/2072

Abstract: The present invention can retain the volume of a tablet large without increasing the thickness of the tablet or the like dimension and prevents a plurality of tablets from sticking to each other even if they are subjected to a film-coating or the like treatment, so as to improve the yield. The tablet is a tablet (1) longer in one direction when seen in plan. The tablet (1) has side edges (6) each of which extends in a longitudinal direction and is formed in the shape of a curve projecting outwardly in plan view. The curve has a radius of curvature (R1) set to at least 1.5 times a length (L) of the tablet. This makes a projected area of the tablet (1) in plan view at least 97% with respect to a projected area of a standard elliptical tablet having opposite end portions each of which is formed by a semi-circle having a diameter of a width (W) of the tablet.

Abstract translation: 本发明可以在不增加片剂厚度等的情况下保持片剂的体积，并且即使进行薄膜包衣或类似的处理也能防止多个片剂彼此粘附，因此 提高产量。 平板电脑是平板电脑（1）在计划中看到的时间长一个方向。 片剂（1）具有侧边缘（6），每个边缘沿纵向方向延伸并且形成为在平面图中向外突出的曲线形状。 曲线的曲率半径（R1）设定为片剂长度（L）的至少1.5倍。 这使得平面图（1）中的平板（1）的投影面积相对于具有相对端部的标准椭圆形片的投影面积至少为97％，每个端部均由直径为宽度的半圆形成 W）。

公开(公告)号：US09266831B2

公开(公告)日：2016-02-23

申请号：US14303238

申请日：2014-06-12

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Tomomi Ikemoto ,  Toshiaki Nagata ,  Naohiro Fukuda

IPC: C07D207/34 ,  C07D207/337 ,  C07D207/333 ,  C07D207/36 ,  C07D401/12 ,  C07C225/14 ,  C07D207/30 ,  C07D207/48

CPC classification number: C07D207/337 ,  C07D207/30 ,  C07D207/333 ,  C07D207/34 ,  C07D207/36 ,  C07D207/48 ,  C07D401/12

Abstract: The present invention provides a production method of a sulfonylpyrrole compound useful as a pharmaceutical product, a production method of an intermediate used for the method, and a novel intermediate. The present invention relates to a method of producing sulfonylpyrrole compound (VIII), which includes reducing compound (III) and hydrolyzing the reduced product to give compound (IV), subjecting compound (IV) to a sulfonylation reaction to give compound (VI), and subjecting compound (VI) to an amination reaction.

Abstract translation: 本发明提供了可用作药物的磺酰基吡咯化合物的制备方法，用于该方法的中间体的制备方法和新的中间体。 本发明涉及一种制备磺酰基吡咯化合物（Ⅷ）的方法，其包括还原化合物（III）并水解还原产物得到化合物（Ⅳ），使化合物（Ⅳ）进行磺酰化反应得到化合物（Ⅵ）， 并使化合物（VI）进行胺化反应。

公开(公告)号：US09265730B2

公开(公告)日：2016-02-23

申请号：US14194050

申请日：2014-02-28

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Muneo Nonomura ,  Hiroki Ito ,  Hideo Hashimoto ,  Tadashi Urai

IPC: A61K9/16 ,  A61K9/24 ,  A61K9/48 ,  A61K31/4439 ,  A61K47/02

CPC classification number: A61K9/1676 ,  A61K9/209 ,  A61K9/4808 ,  A61K31/4439 ,  A61K47/02

Abstract: It is intended to provide a process for producing unstable amorphous benzimidazole compounds having a proton pump inhibitor function, and stable solid preparations for medicinal use containing these compounds which are produced by blending such an amorphous benzimidazole compound with a nontoxic base such as a basic inorganic salt, forming an intermediate coating layer on the layer containing the active ingredient and further forming an enteric coating layer or a release-controlling coating layer.

公开(公告)号：US20160039811A1

公开(公告)日：2016-02-11

申请号：US14779347

申请日：2014-03-27

Applicant: TAKEDA PHARMACETICAL COMPANY LIMITED

Inventor： Masato YOSHIDA ,  Hiroyuki NAGAMIYA ,  Yusuke OHBA ,  Masaki SETO ,  Takatoshi YOGO ,  Satoshi SASAKI ,  Norihito TOKUNAGA ,  Kazuyoshi ASO

IPC: C07D471/04 ,  C07D519/00

CPC classification number: C07D471/04 ,  C07D519/00

Abstract: Provided is a compound or a salt thereof, which has an excellent JAK inhibitory action, and is useful as a prophylactic or therapeutic agent for autoimmune diseases (rheumatoid arthritis, psoriasis, inflammatory bowel disease, Sjogren's syndrome, Behcet's syndrome, multiple sclerosis, systemic lupus erythematosus, etc.), cancer (leukemia, uterine leiomyosarcoma, prostate cancer, multiple myeloma, cachexia, myelofibrosis, etc.) and the like. The present invention relates to a compound represented by the formula (I) wherein each symbol is as defined in the present specification, or a salt thereof.

Abstract translation: 提供具有优异的JAK抑制作用的化合物或其盐，并且可用作自身免疫性疾病（类风湿性关节炎，牛皮癣，炎性肠病，干燥综合征，白塞氏综合征，多发性硬化症，系统性狼疮）的预防或治疗剂 红斑狼疮等），癌症（白血病，子宫平滑肌肉瘤，前列腺癌，多发性骨髓瘤，恶病质，骨髓纤维化等）等。 本发明涉及由式（I）表示的化合物，其中每个符号如本说明书中所定义，或其盐。

公开(公告)号：US09241945B2

公开(公告)日：2016-01-26

申请号：US14361554

申请日：2012-11-29

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Tetsuya Kawano ,  Yasushi Mima ,  Yumiko Ishii

IPC: A61K9/16 ,  A61K9/28 ,  A61K9/32 ,  A01N43/00 ,  A61K31/616 ,  A61K9/24 ,  A61K31/4439 ,  A61K45/06 ,  A61K9/20 ,  A61K9/50

Abstract: Provided is a dry coated tablet showing high stability of the active ingredient (proton pump inhibitor, acetylsalicylic acid), which stably and rapidly expresses the pharmacological effect of the active ingredient after administration. A dry coated tablet having an inner core and an outer layer, wherein the inner core is an enteric-coated tablet containing acetylsalicylic acid, and the outer layer contains enteric micro granules containing a proton pump inhibitor.

公开(公告)号：US09238667B2

公开(公告)日：2016-01-19

申请号：US14388383

申请日：2013-03-28

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Mitsuhisa Yamano ,  Masatoshi Yamada ,  Hirotsugu Usutani

IPC: C07F15/00 ,  B01J31/24 ,  C07B53/00 ,  C07D471/04 ,  C07F9/50 ,  C07C231/18 ,  C07C309/30 ,  C07C241/04 ,  C07C51/41

CPC classification number: C07F15/0073 ,  B01J31/24 ,  B01J31/2495 ,  B01J2231/645 ,  B01J2531/822 ,  C07B53/00 ,  C07B2200/07 ,  C07C51/412 ,  C07C231/18 ,  C07C241/04 ,  C07C309/30 ,  C07C2601/14 ,  C07C2601/16 ,  C07D471/04 ,  C07F9/5027 ,  C07C243/38 ,  C07C233/47 ,  C07C233/81 ,  C07C59/255

Abstract: [Problem] Provision of a superior rhodium catalyst and a production method of amine compound.[Solving Means] A rhodium complex coordinated with a compound represented by the formula

Abstract translation: [问题]提供优异的铑催化剂和胺化合物的制备方法。 [解决方案]与由式表示的化合物配位的铑络合物

公开(公告)号：US09200051B2

公开(公告)日：2015-12-01

申请号：US14287514

申请日：2014-05-27

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Taiji Asami ,  Ayumu Niida

IPC: C07K14/605

CPC classification number: C07K14/605 ,  A61K38/00

Abstract: The present invention provides a novel peptide compound having an activating action on GLP-1 receptors and GIP receptors and use of the peptide compound as a medicament. Specifically, a peptide containing a partial sequence represented by the formula (I) or a salt thereof and a medicament comprising the same are provided. P1-Tyr-Aib-Glu-Gly-Thr-αMePhe-Thr-Ser-Asp-Tyr-A11-A12-A13-Leu-Asp-A16-A17-Ala-Gln-A20-Glu-Phe-Val-Lys-Trp-Leu-Leu-Lys-A29 SEQ ID NO: 1 (I)wherein each symbol is as defined herein.

Abstract translation: 本发明提供了对GLP-1受体和GIP受体具有活化作用的新型肽化合物以及肽化合物作为药物的用途。 具体地，提供含有由式（I）表示的部分序列的肽或其盐和包含其的药物。 P1-Tyr-Aib-Glu-Gly-Thr-αMePhe-Thr-Ser-Asp-Tyr-A11-A12-A13-Leu-Asp-A16-A17-Ala-Gln-A20-Glu-Phe-Val-Lys- Trp-Leu-Leu-Lys-A29 SEQ ID NO：1（I）其中每个符号如本文所定义。

公开(公告)号：US09181249B2

公开(公告)日：2015-11-10

申请号：US14577480

申请日：2014-12-19

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Jason Brown ,  Steve Hitchcock ,  Maria Hopkins ,  Shota Kikuchi ,  Holger Monenschein ,  Holly Reichard ,  Kristin Schleicher ,  Huikai Sun ,  Todd Macklin

IPC: A61K31/4965 ,  C07D471/04

CPC classification number: C07D471/04

Abstract: The present invention provides compounds of formula I: which are useful as modulators of GPR6, pharmaceutical compositions thereof, methods for treatment of conditions associated with GPR6, processes for making the compounds and intermediates thereof.

Abstract translation: 本发明提供式I化合物：其可用作GPR6的调节剂，其药物组合物，用于治疗与GPR6相关的病症的方法，以及用于制备化合物及其中间体的方法。

公开(公告)号：US09181186B2

公开(公告)日：2015-11-10

申请号：US14377951

申请日：2013-02-12

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Seiji Miwatashi ,  Hideo Suzuki ,  Tomohiro Okawa ,  Yasufumi Miyamoto ,  Takeshi Yamasaki ,  Yuko Hitomi ,  Yasuhiro Hirata

IPC: C07D213/64 ,  C07D405/14 ,  C07D401/12 ,  C07D239/34 ,  C07D213/30 ,  C07D213/68 ,  C07D213/69 ,  C07D213/55 ,  C07D403/12

CPC classification number: C07D213/64 ,  C07D213/30 ,  C07D213/55 ,  C07D213/68 ,  C07D213/69 ,  C07D239/34 ,  C07D401/12 ,  C07D403/12 ,  C07D405/14

Abstract: Provided is an aromatic ring compound having a GPR40 agonist activity. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof has a GPR40 agonist activity, and is useful as an agent for the prophylaxis or treatment of diabetes and the like.

Abstract translation: 提供具有GPR40激动剂活性的芳环化合物。 由式（I）表示的化合物：其中每个符号如说明书所述，或其盐具有GPR40激动剂活性，并且可用作预防或治疗糖尿病等的药剂。