公开(公告)号：US09751878B2

公开(公告)日：2017-09-05

申请号：US15139531

申请日：2016-04-27

Applicant: Takeda Pharmaceutical Company Limited

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

IPC: C07D471/04

CPC classification number: C07D471/04

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 for the prophylaxis or treatment of diabetes mellitus are provided.

公开(公告)号：US09732086B2

公开(公告)日：2017-08-15

申请号：US14443598

申请日：2013-11-18

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Takahiro Sugimoto ,  Minoru Nakamura ,  Hiroki Sakamoto ,  Shinkichi Suzuki ,  Masami Yamada ,  Makoto Kamata ,  Takuto Kojima ,  Ikuo Fujimori ,  Kenichiro Shimokawa

IPC: C07D221/02 ,  A61K31/44 ,  C07D487/04 ,  C07D401/14 ,  C07D405/14 ,  C07D401/06 ,  C07D403/10 ,  C07D403/14 ,  C07D405/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D453/02 ,  C07D471/04 ,  C07D471/14 ,  C07D209/46 ,  C07D519/00

Abstract: Provided is a compound having a cholinergic muscarinic M1 receptor positive allosteric modulator activity, and useful as a prophylactic or therapeutic drug for Alzheimer's disease, schizophrenia, pain, sleep disorder and the like. The present invention relates to a compound represented by the formula wherein ring A is a 4- to 7-membered ring optionally having substituent(s); L is —O—, —S—, —SO— or —SO2—; R1 is a C1-6 alkyl group optionally having substituent(s) (provided that when L is —O—, R1 is not a C1-6 alkyl group optionally substituted by halogen atom(s)), or a cyclic group optionally having substituent(s); X1 is —CRa═ or —N═; X2 is —CRb═ or —N═; X3 is —CRc= or —N═; Ra, Rb and Rc are each a C1-6 alkyl group, C2-6 alkenyl group, C1-6 alkoxy group, C3-6 cycloalkyl group, C3-6 cycloalkoxy group or C6-14 aryl group, each of which optionally having substituent(s), H or halogen, or a salt thereof.

公开(公告)号：US09718814B2

公开(公告)日：2017-08-01

申请号：US15203522

申请日：2016-07-06

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Shigemitsu Matsumoto ,  Yasushi Hattori ,  Masashi Toyofuku ,  Shinji Morimoto ,  Takuto Kojima ,  Tomohiro Kaku ,  Mitsuhiro Ito

IPC: C07D417/12 ,  C07D417/14 ,  C07D213/82 ,  C07D333/38 ,  C07D285/135 ,  C07D409/14 ,  C07D231/12 ,  C07D413/14 ,  C07D277/56 ,  C07D409/12 ,  C07D307/79 ,  C07D407/12 ,  C07D231/14 ,  C07D333/40 ,  C07D285/08 ,  C07D413/12 ,  C07D307/81

CPC classification number: C07D417/14 ,  C07D213/82 ,  C07D231/12 ,  C07D231/14 ,  C07D277/56 ,  C07D285/08 ,  C07D285/135 ,  C07D307/79 ,  C07D307/81 ,  C07D333/38 ,  C07D333/40 ,  C07D407/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

Abstract: The present invention provides a compound having a lysine-specific demethylase-1 inhibitory action, and useful as a medicament such as a prophylactic or therapeutic agent for schizophrenia, developmental disorders, particularly diseases having intellectual disability (e.g., autistic spectrum disorders, Rett syndrome, Down's syndrome, Kabuki syndrome, fragile X syndrome, Kleefstra syndrome, neurofibromatosis type 1, Noonan syndrome, tuberous sclerosis), neurodegenerative diseases (e.g., Alzheimer's disease, Parkinson's disease, spinocerebellar degeneration (e.g., dentatorubural pallidoluysian atrophy) and Huntington's disease), epilepsy (e.g., Dravet syndrome) or drug dependence, and the like. A compound represented by the formula wherein each symbol is as defined in the present specification, or a salt thereof.

公开(公告)号：US09670229B2

公开(公告)日：2017-06-06

申请号：US15150013

申请日：2016-05-09

Applicant: Takeda Pharmaceutical Company Limited

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

IPC: C07D519/00 ,  C07D498/08 ,  C07D471/04 ,  C07D451/12 ,  C07D221/22 ,  A61K31/19 ,  A61K31/5386 ,  C07C53/40 ,  C07D453/02 ,  C07D471/08 ,  C07C53/18

CPC classification number: C07D498/08 ,  A61K31/19 ,  A61K31/5386 ,  C07C53/18 ,  C07C53/40 ,  C07D221/22 ,  C07D451/12 ,  C07D453/02 ,  C07D471/04 ,  C07D471/08 ,  C07D519/00

Abstract: The present invention provides 5-HT3 receptor antagonists of Formula (I): which are useful for the treatment of diseases treatable by inhibition of 5-HT3 receptor such as emesis, pain, drug addiction, neurodegenerative and psychiatric disorders, and GI disorders. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

公开(公告)号：US09655900B2

公开(公告)日：2017-05-23

申请号：US15176893

申请日：2016-06-08

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Misaki Homma ,  Toru Miyazaki ,  Yuya Oguro ,  Osamu Kurasawa

IPC: A61K31/519 ,  C07D495/04 ,  C07D498/20 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/55

CPC classification number: A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/55 ,  C07D495/04 ,  C07D498/20

Abstract: Provided is a compound useful for the prophylaxis or treatment of cancer.The present invention relates to a compound represented by formula (I): wherein each symbol in the formula is as defined in the specification, or a salt thereof or a prodrug thereof, which is useful for the prophylaxis or treatment of cancer.

公开(公告)号：US20170137880A1

公开(公告)日：2017-05-18

申请号：US15123072

申请日：2015-03-04

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Jarlath Ffrench-Mullen ,  Eric Lai

IPC: C12Q1/68 ,  A61K31/495

CPC classification number: C12Q1/6883 ,  A61K31/495 ,  C12Q2600/106 ,  C12Q2600/112 ,  C12Q2600/156 ,  C12Q2600/16

Abstract: The present invention provides methods for treating depression such as major depressive disorder (MDD) in an individual. The invention further provides methods for determining if an individual suffering from depression is likely to respond favorably or experience an enhanced treatment effect in response to treatment with vortioxetine. The present invention also provides methods for treating cognitive impairment in an individual, optionally wherein the individual also suffers from depression and/or MDD. The invention further provides methods for determining if an individual suffering from cognitive impairment is likely to respond favorably or experience an enhanced treatment effect in response to treatment with vortioxetine. The methods comprise determining the presence of polymorphisms in the collagen, type XXVI, alpha 1 (COL26A1) gene and/or the calcium channel, voltage-dependent, L type, alpha 1C subunit (CACNA1C) gene and/or the CUB and Sushi Multiple Domains 1 (CSMD1) gene and/or the Zinc Finger Protein 494 (ZSCAN4) gene and/or the Zinc Finger Protein 551 (ZNF551) gene and/or the dymeclin (DYM) gene and/or the LINC00348 gene and/or the FOXL2NB gene and/or intergenic regions in the individual.

公开(公告)号：US09650343B2

公开(公告)日：2017-05-16

申请号：US15055156

申请日：2016-02-26

Applicant: Takeda Pharmaceutical Company Limited

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

IPC: C07D471/04 ,  C07D215/00 ,  C07D217/26 ,  C07F7/08 ,  C07D491/048 ,  C07D491/056 ,  A61K31/4375 ,  A61K31/472 ,  A61K31/4741 ,  C07D217/14 ,  C07D491/14

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

Abstract: The present invention provides a heterocyclic compound having a RORγt inhibitory action.The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification. or a salt thereof.

公开(公告)号：US20170114042A1

公开(公告)日：2017-04-27

申请号：US15316937

申请日：2015-06-08

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Tatsuki KOIKE ,  Shuhei IKEDA

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

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：US20170079915A1

公开(公告)日：2017-03-23

申请号：US15126334

申请日：2015-03-17

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Yukihiro NOMURA ,  Yuki TSUSHIMA ,  Yutaka EBISAWA

IPC: A61K9/14 ,  B29B9/10 ,  B01J2/22 ,  A61K31/501

CPC classification number: A61K9/146 ,  A61K9/145 ,  A61K31/4422 ,  A61K31/501 ,  B01J2/22 ,  B29B9/10 ,  B29K2001/08 ,  B29K2105/0035

Abstract: A solid dispersion for achieving improved solubility and absorbability of a pharmaceutically active ingredient, which contains (1) an amorphous pharmaceutically active ingredient, (2) one or more substances selected from among methyl cellulose and organic acids and (3) an enteric base material. In cases where methyl cellulose is contained therein, the solid dispersion does not contain any water-soluble polymer other than methyl cellulose.

公开(公告)号：US20170065553A1

公开(公告)日：2017-03-09

申请号：US15355357

申请日：2016-11-18

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Yutaka Tanoue ,  Tetsuya Matsuura ,  Yutaka Yamagata ,  Naoki Nagahara

IPC: A61K31/343 ,  A61K9/20 ,  A61K9/00

CPC classification number: A61K31/343 ,  A61K9/0056 ,  A61K9/006 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2027 ,  A61K9/2031 ,  A61K9/205 ,  A61K9/2054 ,  A61K9/2059 ,  A61K9/2063 ,  A61K9/2081 ,  A61K9/2095 ,  C07D307/81

Abstract: The present invention provides a preparation with improved disintegration property, a preparation showing improved bioavailability of a medicament, production methods thereof and the like. A rapidly disintegrating preparation comprising granules comprising a medicament coated with a coating layer containing sugar or sugar alcohol; and a disintegrant. A production method of a rapidly disintegrating preparation including a step of producing granules comprising a medicament, a step of forming a coating layer containing sugar or sugar alcohol on the obtained granules and a step of mixing the coated granules with a disintegrant and molding the mixture.

Abstract translation: 本发明提供了具有改善的崩解性的制剂，显示药物的生物利用度提高的制剂，其制备方法等。 一种快速崩解制剂，其包含颗粒，其包含涂覆有含有糖或糖醇的涂层的药物; 和崩解剂。 一种快速崩解制剂的制备方法，包括生产颗粒的步骤，其包括药物，在所得颗粒上形成含有糖或糖醇的包衣层的步骤，以及将包衣颗粒与崩解剂混合并模制该混合物的步骤。