公开(公告)号：WO2016002968A1

公开(公告)日：2016-01-07

申请号：PCT/JP2015/069370

申请日：2015-06-30

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： YAMAMOTO, Satoshi ,  SHIRAI, Junya ,  ODA, Tsuneo ,  KONO, Mitsunori ,  OCHIDA, Atsuko ,  IMADA, Takashi ,  TOKUHARA, Hidekazu ,  TOMATA, Yoshihide ,  ISHII, Naoki ,  TAWADA, Michiko ,  FUKASE, Yoshiyuki ,  YUKAWA, Tomoya ,  FUKUMOTO, Shoji

IPC: C07D217/14 ,  A61K31/4375 ,  A61K31/472 ,  A61K31/4741 ,  C07D471/04 ,  C07D491/14 ,  A61P11/06 ,  A61P17/06 ,  A61P19/02 ,  A61P43/00

CPC classification number: C07D217/26 ,  A61K31/4375 ,  A61K31/472 ,  A61K31/4741 ,  C07D217/14 ,  C07D471/04 ,  C07D491/048 ,  C07D491/056 ,  C07D491/14 ,  C07F7/0812

Abstract: Provided are heterocyclic compounds having a RORγt inhibitory action represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.

Abstract translation: 提供具有由式（I）表示的RORγt抑制作用的杂环化合物：其中每个符号如说明书中所定义，或其盐。

公开(公告)号：WO2015134171A1

公开(公告)日：2015-09-11

申请号：PCT/US2015/015651

申请日：2015-02-12

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED ,  KEUNG, Walter ,  KWOK, Lily ,  SABAT, Mark ,  SCORAH, Nicholas ,  WANG, Haixia ,  WOODHEAD, Steven, John ,  GANGLOFF, Anthony, R.

Inventor： KEUNG, Walter ,  KWOK, Lily ,  SABAT, Mark ,  SCORAH, Nicholas ,  WANG, Haixia ,  WOODHEAD, Steven, John ,  GANGLOFF, Anthony, R.

IPC: C07D471/04 ,  C07D487/04 ,  A61K31/437 ,  A61K31/4985 ,  A61P29/00 ,  A61P37/00

CPC classification number: C07D487/04 ,  C07D471/04

Abstract: The present invention provides compounds of formula 1: which are useful as inhibitors of TBK-1, pharmaceutical compositions thereof, methods for treatment of conditions associated with TBK1, processes for making the compounds and intermediates thereof.

Abstract translation: 本发明提供式1化合物：其可用作TBK-1的抑制剂，其药物组合物，用于治疗与TBK1相关的病症的方法，用于制备化合物的方法及其中间体。

公开(公告)号：WO2015122187A1

公开(公告)日：2015-08-20

申请号：PCT/JP2015/000639

申请日：2015-02-12

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： SASAKI, Minoru ,  KAKEGAWA, Keiko ,  KIKUCHI, Fumiaki ,  IKEDA, Zenichi ,  NISHIKAWA, Yoichi

IPC: C07D307/81 ,  A61K31/343 ,  A61P3/00

CPC classification number: C07D307/81

Abstract: A fused heterocyclic compound having an enteropeptidase inhibitory action and use of the compound as a medicament for treatment or prophylaxis of obesity, diabetes mellitus, etc., are provided. Specifically, a compound represented by the following formula (I): wherein each symbol is as defined herein, or a salt thereof and use of the compound as a medicament for treatment or prophylaxis of obesity, diabetes mellitus, etc., are provided.

Abstract translation: 提供具有肠肽酶抑制作用的稠合杂环化合物和该化合物作为治疗或预防肥胖症，糖尿病等的药物的用途。 具体地，提供由下式（I）表示的化合物：其中每个符号如本文所定义，或其盐，并且使用该化合物作为治疗或预防肥胖症，糖尿病等的药物。

公开(公告)号：WO2014202999A1

公开(公告)日：2014-12-24

申请号：PCT/GB2014/051900

申请日：2014-06-20

Applicant: TAKEDA CAMBRIDGE LIMITED ,  TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： TEALL, Martin

IPC: C07D401/12 ,  A61K31/454 ,  A61P25/00

CPC classification number: C07D401/12 ,  A61K31/454

Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof in which m, n, W, X, Y, Z, R 1 , R 2 , R 3 , R 4 and R 5 are as defined in the specification, 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m，n，W，X​​，Y，Z，R 1，R 2，R 3，R 4和R 5如本说明书中所定义，含有它们的组合物及其 用于治疗。

公开(公告)号：WO2014039831A1

公开(公告)日：2014-03-13

申请号：PCT/US2013/058527

申请日：2013-09-06

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED ,  CHERUVALLATH, Zacharia ,  KOMANDLA, Mallareddy ,  LAWSON, John David ,  MCBRIDE, Christopher ,  TANG, Mingnam

Inventor： CHERUVALLATH, Zacharia ,  KOMANDLA, Mallareddy ,  LAWSON, John David ,  MCBRIDE, Christopher ,  TANG, Mingnam

IPC: C07D487/14 ,  A61K31/4162 ,  A61P3/04

CPC classification number: C07D487/04 ,  A61K31/4162 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/506 ,  C07D487/14 ,  C07D519/00

Abstract: Disclosed are compounds of Formula (1), and pharmaceutically acceptable salts thereof, wherein L, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , and R 7 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating obesity and related diseases, disorders, and conditions associated with MetAP2.

Abstract translation: 公开了式（1）的化合物及其药学上可接受的盐，其中L，R 1，R 2，R 3，R 4，R 5，R 6和R 7在说明书中定义。 本公开还涉及用于制备式1化合物的材料和方法，含有它们的药物组合物及其用于治疗与MetAP2相关的肥胖症和相关疾病，病症和病症的用途。

公开(公告)号：WO2013183784A1

公开(公告)日：2013-12-12

申请号：PCT/JP2013/065905

申请日：2013-06-04

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： TAKAHARA, Maiko ,  YAMANE, Ikurou ,  MISAKI, Masafumi

IPC: A61K9/16 ,  A61K9/20 ,  A61K9/28 ,  A61K31/513

CPC classification number: A61K31/506 ,  A61K9/1652 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/2077 ,  A61K9/2813 ,  A61K9/284 ,  A61K9/2866 ,  A61K31/513

Abstract: The present invention provides a solid preparation excellent in disintegration property and preservation stability. The present invention relates to a solid preparation containing (1) 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-4-fluorobenzonitrile (compound (A)) or a salt thereof, (2) a saccharide, and (3) sodium stearyl fumarate. In addition, the present invention relates to a solid preparation containing (1) compound (A) or a salt thereof, (2) a saccharide, and (3) stearic acid or talc in a naked tablet part.

Abstract translation: 本发明提供了崩解性和保存稳定性优异的固体制剂。 本发明涉及含有（1）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] -4-氟苄腈（化合物（A））或其盐，（2）糖类和（3）硬脂酰富马酸钠。 另外，本发明涉及含有（1）化合物（A）或其盐，（2）糖类和（3）裸片剂中的硬脂酸或滑石的固体制剂。

公开(公告)号：WO2013122260A1

公开(公告)日：2013-08-22

申请号：PCT/JP2013/054246

申请日：2013-02-14

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： DEHARU, Yuko

IPC: A61K9/20 ,  A61K9/28 ,  A61K31/5377

CPC classification number: C07D413/14 ,  A61K9/2054 ,  A61K9/2866 ,  A61K31/5377

Abstract: Provided is a tablet showing improved hygroscopicity, which contains, as a pharmaceutically active ingredient, a compound showing deliquescence at a relative humidity of not less than 80% at 25 degrees C. A tablet containing a compound showing deliquescence at a relative humidity of not less than 80% at 25 degrees C and an additive showing an equilibrium moisture absorption rate at relative humidity 75% at 25 degrees C of not less than 7 wt% relative to its dry weight.

Abstract translation: 本发明提供一种显示改善的吸湿性的片剂，其含有作为药物活性成分的在25℃下相对湿度不小于80％显示潮解的化合物。含有相对湿度不低于潮解的化合物的片剂 在25℃下为80％以上，相对于其干重，相对湿度为75％，相对湿度75％，相对于其干重不小于7重量％。

公开(公告)号：WO2013058409A1

公开(公告)日：2013-04-25

申请号：PCT/JP2012/077662

申请日：2012-10-19

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： TANOUE, Yutaka ,  MURAKAWA, Yusuke ,  MIZUNO, Yumiko ,  ENOTO, Kaoru

IPC: A61K9/20 ,  A61K31/4439

CPC classification number: A61K31/4439 ,  A61K9/2018 ,  A61K9/2031 ,  A61K9/2054

Abstract: Provided is a sustained-release preparation containing pioglitazone or a salt thereof as an active ingredient and showing superior sustainability. A sustained-release preparation containing pioglitazone or a salt thereof, which shows a dissolution ratio of pioglitazone of average 25-58% at the 2-hour time point, and average 60-100% at the 4-hour time point, in a dissolution test according to the 50 rpm USP Paddle Method and using pH 2.0 KC1/HC1 buffer at 37°C as a test solution.

Abstract translation: 本发明提供含有吡格列酮或其盐作为活性成分并显示出优异的可持续性的缓释制剂。 一种含有吡格列酮或其盐的持续释放制剂，其在2小时时间点显示吡格列酮的平均25-58％的溶解比，在4小时时间点平均为60-100％ 根据50rpm USP桨法测试，并在37℃下使用pH 2.0 KCl / HCl缓冲液作为测试溶液。

公开(公告)号：WO2013027845A1

公开(公告)日：2013-02-28

申请号：PCT/JP2012/071523

申请日：2012-08-21

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED ,  TANIGUCHI, Takahiko ,  MIURA, Shotaro ,  HASUI, Tomoaki ,  HALLDIN, Christer ,  STEPANOV, Vladimir ,  TAKANO, Akihiro

Inventor： TANIGUCHI, Takahiko ,  MIURA, Shotaro ,  HASUI, Tomoaki ,  HALLDIN, Christer ,  STEPANOV, Vladimir ,  TAKANO, Akihiro

IPC: C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D498/08 ,  A61K31/501 ,  A61K51/04

CPC classification number: A61K51/0459 ,  A61K51/0463 ,  A61K51/0468 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D498/08

Abstract: The present invention provides radiolabeled compounds useful as radiotracers for quantitative imaging of PDE10A in mammals. The compound of the present invention is represented by the formula (I): wherein each symbols are as defined in the specification.

Abstract translation: 本发明提供了用作放射性示踪剂的放射性标记化合物，用于哺乳动物中PDE10A的定量成像。 本发明的化合物由式（I）表示：其中每个符号如说明书中所定义。

公开(公告)号：WO2012158884A1

公开(公告)日：2012-11-22

申请号：PCT/US2012/038292

申请日：2012-05-17

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED ,  ROSEN, Oliver ,  WEBB, Iain James

Inventor： ROSEN, Oliver ,  WEBB, Iain James

IPC: A61K31/40 ,  A61K31/4164

CPC classification number: A61K31/4188 ,  A61K31/00 ,  A61K45/06 ,  A61K2300/00

Abstract: The present invention provides pharmaceutical compositions and methods for treating cancer comprising administering a therapeutically effective amount of a 17-alpha hydroxylase/C17, 20-lyase inhibitor.

Abstract translation: 本发明提供用于治疗癌症的药物组合物和方法，包括施用治疗有效量的17-α羟化酶/ C17,20-裂解酶抑制剂。