公开(公告)号：US20150119412A1

公开(公告)日：2015-04-30

申请号：US14525593

申请日：2014-10-28

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Shizuo Kasai ,  Takashi Nakahata ,  Asato Kina ,  Hideki Hirose ,  Takeshi Yamasaki ,  Tohru Yamashita ,  Yoichi Nishikawa

IPC: C07D401/12 ,  C07D239/22 ,  C07D211/86

CPC classification number: C07D401/12 ,  C07D211/86 ,  C07D239/22 ,  C07D401/04 ,  C07D401/14

Abstract: A compound having an SSTR5 antagonist action and use of the compound as a medicament are provided. Specifically, a compound represented by the following formula: wherein each symbol is as defined herein, or a salt thereof, a medicament comprising the compound or a salt thereof, and use of the compound or a salt thereof as an agent the prophylaxis or treatment of diabetes mellitus are provided.

Abstract translation: 提供具有SSTR5拮抗作用的化合物和该化合物作为药物的用途。 具体地，由下式表示的化合物或其盐，其中每个符号如本文所定义，或其盐，包含该化合物或其盐的药物，以及该化合物或其盐的用途作为预防或治疗 提供糖尿病。

公开(公告)号：US20150111922A1

公开(公告)日：2015-04-23

申请号：US14402751

申请日：2013-05-29

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Colm Carroll ,  Anne Goldby ,  Martin Teall

IPC: C07D401/14 ,  C07D401/12

CPC classification number: C07D401/12 ,  A61K31/454 ,  A61K31/4545 ,  A61K45/06 ,  C07D211/96 ,  C07D401/14

Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof: (I) in which m, n, W, X, Y, Z, R1, R2, R3 and R4 are as defined in the specification, for use in the treatment or prevention of a diseases o conition mediated by a prokineticin, such as psychiatric and neurological conditions.

Abstract translation: 本发明提供式（I）化合物及其药学上可接受的盐：（I）其中m，n，w，X，Y，Z，R 1，R 2，R 3和R 4如本说明书中所定义， 治疗或预防由促运动素介导的疾病，如精神病学和神经病学疾病。

公开(公告)号：US09011926B2

公开(公告)日：2015-04-21

申请号：US14488823

申请日：2014-09-17

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Naoki Nagahara ,  Naoki Asakawa ,  Muneo Nonomura

IPC: A61K9/16 ,  B05D7/00 ,  A61K31/4439

CPC classification number: A61K9/1682 ,  A61J3/005 ,  A61K9/167 ,  A61K9/1676 ,  A61K9/1694 ,  A61K9/5078 ,  A61K31/4439 ,  B01J2/003

Abstract: In a production process of granules containing a biologically active substance, variation in the elution profile of the biologically active substance is reduced by heating the temperature of granules to about 50° C. or higher and maintaining the temperature for about 1 minute or longer. By setting the spray speed to about 90 mg/min or more per 1 g of cores when a spray agent for a primary agent containing the biologically active substance is sprayed while spraying a binding liquid to the cores and setting the total feeding weight per unit area for a centrifugal fluidized bed coating granulation machine to about 1.5 g/cm2 or more, the variation in the elution profile of the biologically active substance from the granules is reduced.

Abstract translation: 在含有生物活性物质的颗粒的生产方法中，通过将颗粒的温度加热至约50℃或更高并保持约1分钟或更长时间来降低生物活性物质的洗脱曲线的变化。 当喷雾含有生物活性物质的主剂的喷雾剂，同时喷涂粘合液体至核心并设定每单位面积的总进料重量时，通过将喷雾速度设定为每1g核心约90mg / min或更高 对于离心流化床包衣造粒机至约1.5g / cm 2或更高，来自颗粒的生物活性物质的洗脱曲线的变化减小。

公开(公告)号：US08980322B2

公开(公告)日：2015-03-17

申请号：US10549150

申请日：2004-03-16

Applicant: Naoki Nagahara ,  Keiko Miyamoto ,  Yohko Akiyama

Inventor： Naoki Nagahara ,  Keiko Miyamoto ,  Yohko Akiyama

IPC: A61K9/14 ,  A61K9/20 ,  A61K9/48 ,  A61K9/24

CPC classification number: A61K9/209

Abstract: The present invention provides a controlled release composition showing release of an active ingredient (proton pump inhibitor) controlled in two or more steps at different release rates, which contains 1) a release-controlled part A capable of controlling release of the active ingredient to occur at a predetermined rate, 2) a release-controlled part B capable of controlling release of the active ingredient to occur at a predetermined rate lower than the release rate of the release-controlled part A, and where necessary, 3) a release-controlled part C capable of controlling release of the active ingredient to occur at a predetermined rate faster than the release rate of the release-controlled part B, wherein the release of the active ingredient from the release-controlled part B precedes the release of the active ingredient from the release-controlled part A (when release-controlled part C is contained, the release of the active ingredient from the release-controlled part C precedes the release of the active ingredient from the release-controlled part B).

Abstract translation: 本发明提供一种控释组合物，其显示以不同释放速率控制两步或多步的活性成分（质子泵抑制剂）的释放，其包含1）能够控制活性成分释放的释放控制部分A 以预定的速率，2）释放控制部分B，其能够以比释放控制部分A的释放速率低的预定速率控制活性成分的释放，并且如果需要，3）释放控制 C部分能够以比释放控制部分B的释放速度更快的预定速率控制活性成分的释放，其中活性成分从释放控制部分B的释放先于活性成分的释放 从释放控制部分A（当含有释放控制部分C时，活性成分从释放控制部分C的释放先于th 从释放控制部分B释放活性成分。

公开(公告)号：US20150057298A1

公开(公告)日：2015-02-26

申请号：US14463780

申请日：2014-08-20

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： William BUFFHAM ,  Hannah CANNING ,  Richard DAVENPORT ,  William FARNABY ,  Stephen MACK ,  Alka PARMAR ,  Susanne WRIGHT

IPC: C07D239/34 ,  C07D213/78 ,  C07C235/46

CPC classification number: C07D239/34 ,  A61K31/195 ,  A61K31/277 ,  A61K31/44 ,  A61K31/505 ,  C07C235/44 ,  C07C235/46 ,  C07C235/52 ,  C07C255/54 ,  C07C2601/02 ,  C07C2601/04 ,  C07D213/78 ,  C07D213/81

Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1, X, m, R2, Y, R3, Z, n, R4, A and B are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.

Abstract translation: 本发明提供式（I）化合物及其药学上可接受的盐，其中R 1，X，m，R 2，Y，R 3，Z，n，R 4，A和B如说明书中所定义， 含有它们的药物组合物及其在治疗中的用途。

公开(公告)号：US08957069B2

公开(公告)日：2015-02-17

申请号：US13255366

申请日：2010-03-09

Applicant: Tetsuya Tsukamoto ,  Takeshi Wakabayashi ,  Taiichi Ohra

Inventor： Tetsuya Tsukamoto ,  Takeshi Wakabayashi ,  Taiichi Ohra

IPC: A61K31/496 ,  A61K31/541 ,  A61K31/5377 ,  A61K31/519 ,  C07D307/79 ,  C07D307/80 ,  C07D307/81 ,  C07D405/06 ,  C07D405/14 ,  C07D487/04 ,  C07D413/12 ,  C07D491/113 ,  C07D417/06 ,  C07D413/06 ,  C07D493/10 ,  C07D405/04 ,  C07D405/12 ,  C07D407/04 ,  C07D407/12 ,  C07D417/12 ,  A61K31/551 ,  C07D413/04

CPC classification number: C07D307/79 ,  C07D307/80 ,  C07D307/81 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D407/04 ,  C07D407/12 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12 ,  C07D493/10

Abstract: The present invention provides a compound represented by the following formula (I): wherein: Ring A represents an optionally substituted piperazine ring, an optionally substituted morpholine ring, or an optionally substituted bromopiperazine ring; R1 and R2 are the same or different from each other, and represent a hydrogen atom or optionally substituted lower alkyl; R3 and R4 are the same or different from each other, and represent a hydrogen atom or halogenated or non-halogenated lower alkyl; R3 to R7 are the same or different from each other, and represent a hydrogen atom, hydroxy, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkoxy, optionally substituted cycloalkyl, optionally substituted aryl, an optionally substituted aromatic heterocyclic ring, optionally substituted amino, or acyl; and represents a single bond or double bond, wherein R2 and R3 do not exist when carbon atoms respectively adjacent to R2: and R3 form a double bond, and there is no case where all of R1 to R7 are hydrogen atoms, and R1 and R2; may form a ring together with an adjacent carbon atom; or a salt thereof.

Abstract translation: 本发明提供由下式（I）表示的化合物：其中：环A表示任选取代的哌嗪环，任选取代的吗啉环或任选取代的溴代哌嗪环; R1和R2彼此相同或不同，表示氢原子或任选取代的低级烷基; R3和R4彼此相同或不同，表示氢原子或卤代或非卤代低级烷基; R 3至R 7彼此相同或不同，并且表示氢原子，羟基，任选取代的低级烷基，任选取代的低级烯基，任选取代的低级烷氧基，任选取代的环烷基，任选取代的芳基，任选取代的芳族杂环， 任选取代的氨基或酰基; 并且表示单键或双键，其中当分别相邻于R2：和R3的碳原子形成双键时，R2和R3不存在，并且不存在所有R 1至R 7都是氢原子的情况，并且R 1和R 2 ; 可与邻近的碳原子一起形成环; 或其盐。

公开(公告)号：US08932853B2

公开(公告)日：2015-01-13

申请号：US13520090

申请日：2010-12-28

Applicant: Masaki Hosoya ,  Yuya Kunisada ,  Masanobu Shoji ,  Noriko Yamazoe

Inventor： Masaki Hosoya ,  Yuya Kunisada ,  Masanobu Shoji ,  Noriko Yamazoe

IPC: C12N5/00 ,  C12N5/071 ,  C12N5/02 ,  G01N33/50 ,  A61K35/39

CPC classification number: C12N5/0676 ,  A61K35/39 ,  C12N5/0678 ,  C12N2501/155 ,  C12N2501/16 ,  C12N2501/385 ,  C12N2501/727 ,  C12N2506/45 ,  G01N33/507

Abstract: The present invention provides a method of more efficiently producing pancreas cells, particularly pancreatic hormone-producing cells, a method of stably producing pancreas cells in a large amount by more efficiently inducing differentiation of stem cells into pancreas cells, a medicament containing a pancreas cells and a screening method using the cells.A method of producing pancreatic hormone-producing cells, including subjecting stem cells to the following steps (1)-(4): (1) a step of cultivating stem cells in a medium containing an activator of activin receptor-like kinase-4,7 and a GSK3 inhibitor (2) a step of cultivating the cells obtained in the aforementioned step (1) in a medium containing an activator of activin receptor-like kinase-4,7 (3) a step of cultivating the cells obtained in the aforementioned step (2) in a medium containing any one or more kinds selected from the group consisting of (a) retinoic acid receptor agonists, (b) at least one kind selected from the group consisting of inhibitors of AMP-activated protein kinase and/or activin receptor-like kinase-2,3,6, and BMP antagonists, and (c) inhibitors of activin receptor-like kinase-4,5,7 (4) a step of cultivating the cells obtained in the aforementioned step (3).

Abstract translation: 本发明提供一种更有效地产生胰腺细胞，特别是胰腺激素产生细胞的方法，通过更有效地诱导干细胞分化成胰腺细胞，大量稳定产生胰腺细胞的方法，含有胰腺细胞的药物和 使用细胞的筛选方法。 一种产生胰腺激素的细胞的方法，包括对干细胞进行以下步骤（1） - （4）：（1）在含有激活素受体样激酶-4的活化剂的培养基中培养干细胞的步骤， 7和GSK3抑制剂（2）在含有激活素受体样激酶-4,7（3）的活化剂的培养基中培养上述步骤（1）中获得的细胞的步骤（3） 上述步骤（2）在含有选自（a）视黄酸受体激动剂，（b）至少一种选自AMP活化蛋白激酶抑制剂和/ 或激活素受体样激酶-2,3,6和BMP拮抗剂，和（c）激活素受体样激酶-4,5,7的抑制剂（4）培养上述步骤（3）中获得的细胞的步骤 ）。

公开(公告)号：US20140357552A1

公开(公告)日：2014-12-04

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. (I) 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 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。 （I）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，其中每个符号如本文所定义。

公开(公告)号：US20140256757A1

公开(公告)日：2014-09-11

申请号：US14280942

申请日：2014-05-19

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Ronald J. Christopher ,  Paul Covington

IPC: A61K31/513 ,  A61K31/4439 ,  A61K31/155

CPC classification number: A61K31/4439 ,  A61K31/131 ,  A61K31/155 ,  A61K31/44 ,  A61K31/513 ,  A61K45/06 ,  A61K2039/505 ,  C07C257/06 ,  C07C317/40 ,  C07C2602/08 ,  C07D209/26 ,  C07K16/2896 ,  C07K16/40 ,  C07K2317/76 ,  A61K2300/00

Abstract: Pharmaceutical compositions comprising 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-benzonitrile and pharmaceutically acceptable salts thereof in combination with metformin and in combination with pioglitazone.

Abstract translation: 包含2 - [[6 - [（3R）-3-氨基-1-哌啶基] -3,4-二氢-3-甲基-2,4-二氧代-1（2H） - 嘧啶基]甲基] - 苄腈 和其药学上可接受的盐与二甲双胍组合并与吡格列酮组合。

公开(公告)号：US20140256693A1

公开(公告)日：2014-09-11

申请号：US14173388

申请日：2014-02-05

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Masuo Yamaoka ,  Takahito Hara

IPC: C07D487/04 ,  A61K45/06 ,  A61K31/4188

CPC classification number: C07D487/04 ,  A61K31/4188 ,  A61K45/06

Abstract: The present invention mainly aims to provide a drug for the prophylaxis or treatment of androgen-independent prostate cancer, which is highly useful as a pharmaceutical agent. The present invention provides a drug for the prophylaxis or treatment of androgen-independent prostate cancer, containing a steroid C17,20 lyase inhibitor, particularly, a compound represented by the formula (I): wherein n is an integer of 1 to 3, and Ar is an aromatic ring optionally having substituent(s), or a salt thereof or a prodrug thereof.

Abstract translation: 本发明的目的在于提供一种用于预防或治疗雄激素依赖性前列腺癌的药物，其作为药剂是非常有用的。 本发明提供一种用于预防或治疗雄激素依赖性前列腺癌的药物，其含有类固醇C17,20裂解酶抑制剂，特别是由式（I）表示的化合物：其中n为1〜3的整数， Ar是任选具有取代基的芳香环，或其盐或其前药。