公开(公告)号：US10053468B2

公开(公告)日：2018-08-21

申请号：US14902309

申请日：2014-07-02

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Satoshi Yamamoto ,  Junya Shirai ,  Hiroyuki Watanabe ,  Shoji Fukumoto ,  Tsuneo Oda ,  Hidekazu Tokuhara ,  Yoshihide Tomata ,  Naoki Ishii ,  Michiko Tawada ,  Mitsunori Kono ,  Atsuko Ochida ,  Takashi Imada ,  Yoshiyuki Fukase ,  Tomoya Yukawa

IPC: C07D491/056 ,  C07D217/26 ,  C07D401/06 ,  C07D405/06 ,  C07D409/06 ,  C07D413/06 ,  C07D417/06 ,  C07D471/04 ,  C07D491/048 ,  C07D401/12 ,  C07D413/12 ,  C07D491/04 ,  C07D413/14 ,  C07D401/04 ,  C07D405/12 ,  C07F7/08

CPC classification number: C07D491/056 ,  C07D217/26 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/06 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/06 ,  C07D471/04 ,  C07D491/04 ,  C07D491/048 ,  C07F7/0812

Abstract: The present invention relates to compound (I) or a salt thereof which has a RORγt inhibitory action. wherein each symbol is as defined in the specification.

公开(公告)号：US09963443B2

公开(公告)日：2018-05-08

申请号：US15316937

申请日：2015-06-08

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Tatsuki Koike ,  Shuhei Ikeda

IPC: A61K31/506 ,  C07D401/14 ,  A61K51/04 ,  C07D401/04 ,  C07D405/14 ,  C07D417/14

CPC classification number: C07D401/14 ,  A61K51/0455 ,  A61K51/0459 ,  C07B59/002 ,  C07B2200/05 ,  C07D401/04 ,  C07D405/14 ,  C07D417/14

Abstract: The present invention provides radiolabeled compounds useful as radiotracers for quantitative imaging of CH24H in mammals. The compound of the present invention is represented by the formula (I): wherein each symbol is as defined in the specification.

公开(公告)号：US20180118708A1

公开(公告)日：2018-05-03

申请号：US15572231

申请日：2016-05-06

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Toshitake KOBAYASHI ,  Morihisa SAITOH ,  Yasufumi WADA ,  Hiroshi NARA ,  Nobuyuki NEGORO ,  Masashi YAMASAKI ,  Takahiro TANAKA ,  Naomi KITAMOTO

IPC: C07D317/72 ,  A61P37/00 ,  A61P29/00 ,  A61P25/02 ,  A61P1/16 ,  A61P9/10

CPC classification number: C07D317/72 ,  A61K31/357 ,  A61P1/16 ,  A61P9/10 ,  A61P25/02 ,  A61P29/00 ,  A61P37/00

Abstract: The present invention provides compounds having a Toll-like receptor 4 (TLR4) signaling inhibitory action useful as preventive and therapeutic drugs of autoimmune disease and/or inflammatory disease or diseases such as chemotherapy-induced peripheral neuropathy (CIPN), chemotherapy-induced neuropathic pain (CINP), liver injury, ischemia-reperfusion injury (IRI) and the like.The present invention relates to a compound represented by formula (I) and a salt thereof: (wherein, each symbol is explained in greater detail in the specification).

公开(公告)号：US09931340B2

公开(公告)日：2018-04-03

申请号：US15014336

申请日：2016-02-03

Applicant: TAKEDA PHARMACUETICAL COMPANY LTD.

Inventor： William Farnaby ,  Charlotte Fieldhouse ,  Katherine Hazel ,  Catrina Kerr ,  Natasha Kinsella ,  David Livermore ,  Kevin Merchant ,  David Miller

IPC: A61K31/50 ,  A61K31/501 ,  C07D237/16 ,  C07D401/06

CPC classification number: A61K31/50 ,  A61K31/501 ,  A61K45/06 ,  C07D237/16 ,  C07D237/18 ,  C07D237/22 ,  C07D401/06 ,  C07D401/10 ,  C07D405/06 ,  C07D407/10 ,  C07F7/0812

Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy:

公开(公告)号：US20180072694A1

公开(公告)日：2018-03-15

申请号：US15561613

申请日：2016-03-25

Applicant: Takeda Pharmaceutical Company Limited

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

IPC: C07D307/79 ,  C07D413/04 ,  C07F9/655

CPC classification number: C07D307/79 ,  A61K31/343 ,  A61K31/422 ,  A61K31/665 ,  A61P3/04 ,  A61P3/10 ,  C07D413/04 ,  C07F9/38 ,  C07F9/65517

Abstract: The present invention relates to a condensed heterocyclic compound that has an enteropeptidase inhibitory effect, and use of the compound as a medicament for the treatment or prevention of obesity, diabetes mellitus, or the like. Specifically, the present invention relates to a compound represented by the formula (I) or a salt thereof, and use of the compound as a medicament for the treatment or prevention of obesity, diabetes mellitus, or the like [in the formula, each symbol is as defined in the specification].

公开(公告)号：US09827255B2

公开(公告)日：2017-11-28

申请号：US14974033

申请日：2015-12-18

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Zacharia Cheruvallath ,  John David Lawson ,  Christopher McBride

IPC: A61K31/665 ,  A61K31/683 ,  C07F9/6558 ,  A61K31/66 ,  A61K45/06

CPC classification number: A61K31/665 ,  A61K31/155 ,  A61K31/192 ,  A61K31/216 ,  A61K31/336 ,  A61K31/397 ,  A61K31/4985 ,  A61K31/64 ,  A61K31/66 ,  A61K31/662 ,  A61K31/683 ,  A61K38/28 ,  A61K45/06 ,  A61P3/10 ,  C07F9/65586 ,  A61K2300/00

Abstract: Disclosed are compounds of Formula 1, stereoisomers thereof and pharmaceutically acceptable salts of the compounds and stereoisomers, wherein R1 and R2 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.

公开(公告)号：US20170319565A1

公开(公告)日：2017-11-09

申请号：US15600833

申请日：2017-05-22

Applicant: Takeda Pharmaceutical Company Limited ,  Zinfandel Pharmaceuticals, Inc.

Inventor： Allen D. Roses ,  Rajneesh Taneja

IPC: A61K31/4439 ,  C12Q1/68 ,  C07D417/12

CPC classification number: A61K31/4439 ,  C07D417/12 ,  C12Q1/6883 ,  C12Q2600/106 ,  C12Q2600/118 ,  C12Q2600/156 ,  C12Q2600/158 ,  C12Q2600/172 ,  Y10T436/143333

Abstract: Provided herein are drug products with low dose pioglitazone for use in the treatment (e.g., delay of onset) of cognitive impairment of the Alzheimer's type. Methods of manufacture thereof are also provided. Further provided are methods of treatment for Alzheimer's disease including administering a drug product with low dose pioglitazone. The methods may include determining whether the subject is at risk of developing Alzheimer's disease based upon the subject's age and TOMM40 523 genotype.

公开(公告)号：US09776962B2

公开(公告)日：2017-10-03

申请号：US14898633

申请日：2014-08-08

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Jumpei Aida ,  Yayoi Yoshitomi ,  Yuko Hitomi ,  Naoyoshi Noguchi ,  Yasuhiro Hirata ,  Hideki Furukawa ,  Akito Shibuya ,  Koji Watanabe ,  Yasufumi Miyamoto ,  Tomohiro Okawa ,  Nobuyuki Takakura ,  Seiji Miwatashi

IPC: C07D211/34 ,  C07D211/22 ,  C07D213/30 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/10 ,  C07D413/14

CPC classification number: C07D211/34 ,  C07D211/22 ,  C07D213/30 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/10 ,  C07D413/14

Abstract: Provided is a novel aromatic ring compound having a GPR40 agonist activity and a GLP-1 secretagogue action. A compound represented by the formula: wherein each symbol is as described in the DESCRIPTION, or a salt thereof has a GPR40 agonist activity and a GLP-1 secretagogue action, is useful for the prophylaxis or treatment of cancer, obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia and the like, and affords superior efficacy.

公开(公告)号：US09770452B2

公开(公告)日：2017-09-26

申请号：US15334198

申请日：2016-10-25

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Stephen Hitchcock ,  Holger Monenschein ,  Holly Reichard ,  Huikai Sun ,  Shota Kikuchi ,  Todd Macklin ,  Maria Hopkins

IPC: A61K31/53 ,  A61K31/5377 ,  C07D241/44 ,  C07D471/04 ,  C07D487/04 ,  C07D405/12 ,  A61K31/197 ,  A61K31/498 ,  A61K31/4985 ,  A61K31/5025 ,  A61K45/06

CPC classification number: A61K31/5377 ,  A61K31/197 ,  A61K31/498 ,  A61K31/4985 ,  A61K31/5025 ,  A61K45/06 ,  C07D241/44 ,  C07D405/12 ,  C07D471/04 ,  C07D487/04

Abstract: The present invention provides compounds of Formula (I): that are GPR6 modulators and are therefore useful for the treatment of diseases treatable by modulation of GPR6, in particular treating Parkinson disease, levodopa induced dyskinesias, Huntington's disease, other dyskinesias, akinesias, and motor disorders involving dysfunction of the striatum, schizophrenia and drug addiction. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

公开(公告)号：US09757377B2

公开(公告)日：2017-09-12

申请号：US15272755

申请日：2016-09-22

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Maiko Harada ,  Ikurou Yamane ,  Masafumi Misaki

IPC: A61K9/28 ,  A61K31/51 ,  A61K9/20 ,  A61K9/16 ,  A61K31/506 ,  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.