公开(公告)号：US20150307451A1

公开(公告)日：2015-10-29

申请号：US14693342

申请日：2015-04-22

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Masami YAMADA ,  Shinkichi SUZUKI ,  Takahiro SUGIMOTO ,  Minoru NAKAMURA ,  Hiroki SAKAMOTO ,  Makoto KAMATA

IPC: C07D209/46 ,  C07D401/14 ,  C07D403/04 ,  C07D401/10 ,  C07D403/10 ,  C07D405/14

CPC classification number: C07D405/14 ,  A61K31/045 ,  A61K31/13 ,  A61K31/325 ,  A61K31/4035 ,  A61K31/4155 ,  A61K31/4406 ,  A61K31/4439 ,  A61K31/445 ,  A61K31/55 ,  C07D209/46 ,  C07D401/06 ,  C07D401/10 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D405/04 ,  C07D471/04

Abstract: The present invention provides a compound having a cholinergic muscarinic M1 receptor positive allosteric modulator activity and useful as an agent for the prophylaxis or treatment of Alzheimer's disease, schizophrenia, pain, sleep disorder, Parkinson's disease dementia, dementia with Lewy bodies, and the like.The present invention relates to a compound represented by the formula (I) or a salt thereof. wherein each symbol is as described in the specification, or a salt thereof.

Abstract translation: 本发明提供具有胆碱能毒蕈碱M1受体阳性变构调节剂活性的化合物，可用作预防或治疗阿尔茨海默病，精神分裂症，疼痛，睡眠障碍，帕金森病痴呆，路易体痴呆等。 本发明涉及由式（I）表示的化合物或其盐。 其中每个符号如说明书中所述或其盐。

公开(公告)号：US20230348435A1

公开(公告)日：2023-11-02

申请号：US17999505

申请日：2021-05-20

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Tomoaki HASUI ,  Satoshi MIKAMI ,  Toru YAMASHITA ,  Shinji NAKAMURA ,  Shinji MORIMOTO ,  Toshihiro IMAEDA ,  Kazuaki TAKAMI ,  Masaki DAINI ,  Hiroyuki KAKEI ,  Minoru NAKAMURA ,  Fumie YAMAGUCHI ,  Chunxiang WANG ,  Sachie TAKASHIMA ,  Shogo HASHIZUME

IPC: C07D403/06 ,  A61K45/06 ,  C07D413/14 ,  C07D403/14 ,  C07D401/14 ,  C07D405/14

CPC classification number: C07D403/06 ,  A61K45/06 ,  C07D413/14 ,  C07D403/14 ,  C07D401/14 ,  C07D405/14

Abstract: The present invention refers to compounds of formula (I). The present invention also relates to compounds of formula (I) for use as G Protein coupled Receptor 139 (GPR139) antagonists in methods of medical treatment of e.g. depression, Alzheimer's disease schizophrenia, drug addiction, sleep disorders, pain, and attention deficit hyperactivity disorder. Exemplary compounds are e.g. 1-(OH-pyrazol-4-yl)methyl)-3-(phenyl)-1,3-dihydro-2H-imidazol-2-one derivatives and related compounds. The present description discloses the synthesis and characterisation of exemplary compounds, pharmacological data thereof, as well as exemplary tablet formulations comprising the compounds of the invention (e.g. page 100 to page 143; examples 1 to 167; test examples 1 and 2; tables 1 to 4).

公开(公告)号：US20220089525A1

公开(公告)日：2022-03-24

申请号：US17310164

申请日：2020-01-23

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Yuya OGURO ,  Makoto KAMATA ,  Satoshi MIKAMI ,  Shinji MORIMOTO ,  Sachie TAKASHIMA ,  Masaki DAINI ,  Osamu KUBO ,  Fumiaki KIKUCHI ,  Akinori TOITA ,  Florian PUENNER ,  Takahito KASAHARA ,  Masataka MURAKAMI ,  Shuhei IKEDA ,  Fumie YAMAGUCHI ,  Minoru NAKAMURA ,  Takafumi YUKAWA

IPC: C07C255/60 ,  C07D213/82 ,  C07D401/12 ,  C07D409/12 ,  A61P25/06 ,  A61P25/24 ,  A61P25/28 ,  A61P29/00

Abstract: A heterocyclic compound that can have an antagonistic action on an NMDA receptor containing the NR2B subunit, and is expected to be useful as a prophylactic or therapeutic agent for depression, bipolar disorder, migraine, pain, peripheral symptoms of dementia and the like is provided. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof.

公开(公告)号：US20210332053A1

公开(公告)日：2021-10-28

申请号：US17201878

申请日：2021-03-15

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Yuya OGURO ,  Shigemitsu MATSUMOTO ,  Takeshi WAKABAYASHI ,  Norihito TOKUNAGA ,  Taku KAMEI ,  Mitsuhiro ITO ,  Satoshi MIKAMI ,  Masaki SETO ,  Shinji MORIMOTO ,  Shinji NAKAMURA ,  Sachie TAKASHIMA ,  Masataka MURAKAMI ,  Masaki DAINI ,  Makoto KAMATA ,  Minoru NAKAMURA ,  Yasufumi WADA ,  Hiroyuki KAKEI ,  Kazuaki TAKAMI ,  Taisuke TAWARAISHI ,  Jumpei AIDA ,  Kouichi IWANAGA ,  Satoshi YAMAMOTO

IPC: C07D487/04 ,  A61K9/20 ,  A61K9/48 ,  C07D471/04 ,  A61P25/00

Abstract: The present invention provides a heterocyclic compound having an antagonistic action on an NMDA receptor containing the NR2B subunit, and expected to be useful as an agent for the prophylaxis or treatment of major depression, bipolar disorder, migraine, pain, behavioral and psychological symptoms of dementia and the like.
The present invention relates to a compound represented by the formula (I): wherein each symbol is as described in the description, or a salt thereof.

公开(公告)号：US20210087186A1

公开(公告)日：2021-03-25

申请号：US16961476

申请日：2019-01-30

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Yuta TANAKA ,  Tomohiro OHASHI ,  Zenichi IKEDA ,  Yuta TANAKA ,  Florian PÜNNER ,  Takeshi YAMAMOTO ,  Keiko KAKEGAWA ,  Fumiaki KIKUCHI ,  Nao MORISHITA ,  Takahito KASAHARA ,  Masaki SETO ,  Minoru NAKAMURA ,  Kazuaki TAKAMI ,  Masataka MURAKAMI ,  Masaki DAINI ,  Satoshi MIKAMI ,  Minoru SASAKI

IPC: C07D471/04 ,  C07D495/04 ,  C07D487/04 ,  C07D491/048 ,  C07D519/00

Abstract: The present invention provides a compound having a glucosylceramide lowering action (e.g., promoting glucosylceramide metabolism, inhibition of glucosylceramide synthesis, promoting glucosylceramide catabolism, etc.), which is expected to be useful as an agent for the prophylaxis or treatment of lysosome diseases (e.g., Gaucher's disease), neurodegenerative diseases (e.g., Parkinson's disease, Lewy body dementia, multiple-system atrophy) and the like.
The present invention relates to a compound represented by the formula (I) wherein each symbol is as described in the specification, or a salt thereof.

公开(公告)号：US20180162850A1

公开(公告)日：2018-06-14

申请号：US15735418

申请日：2016-06-23

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Takahiro SUGIMOTO ,  Shinkichi SUZUKI ,  Hiroki SAKAMOTO ,  Masami YAMADA ,  Minoru NAKAMURA ,  Makoto KAMATA ,  Kenichiro SHIMOKAWA ,  Masaki OGINO ,  Eiji KIMURA ,  Masataka MURAKAMI ,  Jinichi YONEMORI ,  Takuto KOJIMA

IPC: C07D413/14 ,  C07D413/10 ,  C07D265/22 ,  C07D417/10 ,  C07F7/08 ,  C07D491/107 ,  A61P25/28

CPC classification number: C07D265/22 ,  A61P25/28 ,  C07B2200/07 ,  C07D413/04 ,  C07D413/06 ,  C07D413/10 ,  C07D413/14 ,  C07D417/06 ,  C07D417/10 ,  C07D471/04 ,  C07D491/107 ,  C07F7/02 ,  C07F7/0814

Abstract: The present invention provides a compound having a cholinergic muscarinic M1 receptor positive allosteric modulator activity, which may be useful as a prophylactic or therapeutic drug for Alzheimer's disease, schizophrenia, pain, sleep disorder, Parkinson's disease dementia, dementia with Lewy bodies and the like. The present invention relates to a compound represented by the formula (I) or a salt thereof: wherein each symbol is as defined in the attached DESCRIPTION.

公开(公告)号：US20180000780A1

公开(公告)日：2018-01-04

申请号：US15685800

申请日：2017-08-24

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Masami YAMADA ,  Shinkichi SUZUKI ,  Takahiro SUGIMOTO ,  Minoru NAKAMURA ,  Hiroki SAKAMOTO ,  Makoto KAMATA

IPC: A61K31/4035 ,  A61K31/045 ,  A61K31/4406 ,  C07D471/04

CPC classification number: C07D405/14 ,  A61K31/045 ,  A61K31/13 ,  A61K31/325 ,  A61K31/4035 ,  A61K31/4155 ,  A61K31/4406 ,  A61K31/4439 ,  A61K31/445 ,  A61K31/55 ,  C07D209/46 ,  C07D401/06 ,  C07D401/10 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D405/04 ,  C07D471/04

Abstract: The present invention provides a compound having a cholinergic muscarinic M1 receptor positive allosteric modulator activity and useful as an agent for the prophylaxis or treatment of Alzheimer's disease, schizophrenia, pain, sleep disorder, Parkinson's disease dementia, dementia with Lewy bodies, and the like.The present invention relates to a compound represented by the formula (I) or a salt thereof. wherein each symbol is as described in the specification, or a salt thereof.

公开(公告)号：US20170081332A1

公开(公告)日：2017-03-23

申请号：US15311025

申请日：2015-05-15

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Takahiro SUGIMOTO ,  Kenichiro SHIMOKAWA ,  Takuto KOJIMA ,  Hiroki SAKAMOTO ,  Ikuo FUJIMORI ,  Minoru NAKAMURA ,  Masami YAMADA ,  Masataka MURAKAMI ,  Makoto KAMATA ,  Shinkichi SUZUKI

IPC: C07D487/04 ,  C07D471/04

CPC classification number: C07D487/04 ,  A61K31/437 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/501 ,  A61K31/519 ,  C07D471/04

Abstract: The present invention provides a compound having a cholinergic muscarinic M1 receptor positive allosteric modulator activity, which may be useful as medicaments such as a prophylactic or therapeutic drug for Alzheimer's disease, schizophrenia, pain, sleep disorder, Parkinson's disease dementia, dementia with Lewy bodies and the like, and the like. The present invention relates to a compound represented by the formula (I) wherein ring A is an optionally substituted 5- or 6-membered ring; R is a C1-6 alkyl group substituted by 1 to 5 halogen atoms; and X is —CH═ or —N═, or a salt thereof.

公开(公告)号：US20240309016A1

公开(公告)日：2024-09-19

申请号：US18606857

申请日：2024-03-15

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Mitsunori KONO ,  Yusuke SASAKI ,  Yuya OGURO ,  Zenichi IKEDA ,  Osamu KUBO ,  Masaki SETO ,  Toru YAMASHITA ,  Makoto KAMATA ,  Kenjiro SATO ,  Matthew Thomas REYNOLDS ,  Kazuaki TAKAMI ,  Asato KINA ,  Takafumi YUKAWA ,  Minoru NAKAMURA ,  Taku KAMEI ,  Hiroyuki KAKEI ,  Fumie YAMAGUCHI ,  Tomohiro OHASHI ,  Keiko KAKEGAWA ,  Takuto KOJIMA ,  Florian PÜNNER ,  Masataka MURAKAMI ,  Takahiko TANIGUCHI ,  Tatsuki KOIKE ,  Yuichi KAJITA ,  Yuhei MIYANOHANA ,  Kohei TAKEUCHI ,  Yoshiteru ITO ,  Norihito TOKUNAGA ,  Yasushi HATTORI ,  Eiji KIMURA ,  Martin Alexander PAWLICZEK ,  Marilena PIRA ,  Shuhei IKEDA ,  Noriyuki TEZUKA ,  Yoshikazu WATANABE ,  Kevin CURRAN ,  Nicolle DOERING ,  Maria HOPKINS ,  Ben JOHNSON ,  Andre KIRYANOV ,  Jon LAM ,  Sean MURPHY ,  Natasha O'ROURKE ,  Holly REICHARD ,  Paul TANIS ,  Yunlong ZHANG

IPC: C07D498/14 ,  A61K31/407 ,  A61K31/437 ,  A61P25/26 ,  C07D498/04

CPC classification number: C07D498/14 ,  A61K31/407 ,  A61K31/437 ,  A61P25/26 ,  C07D498/04

Abstract: The present invention provides a heterocyclic compound having an orexin type 2 receptor agonist activity.
A compound represented by the formula (I):




wherein each symbol is as described in the specification, or a salt thereof has an orexin type 2 receptor agonist activity, and is useful as an agent for the prophylaxis or treatment of narcolepsy.

公开(公告)号：US20240109874A1

公开(公告)日：2024-04-04

申请号：US18504741

申请日：2023-11-08

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Masami YAMADA ,  Shinkichi SUZUKI ,  Takahiro SUGIMOTO ,  Minoru NAKAMURA ,  Hiroki SAKAMOTO ,  Makoto KAMATA

IPC: C07D405/14 ,  A61K31/045 ,  A61K31/13 ,  A61K31/325 ,  A61K31/4035 ,  A61K31/4155 ,  A61K31/4406 ,  A61K31/4439 ,  A61K31/445 ,  A61K31/55 ,  C07D209/46 ,  C07D401/06 ,  C07D401/10 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D405/04

CPC classification number: C07D405/14 ,  A61K31/045 ,  A61K31/13 ,  A61K31/325 ,  A61K31/4035 ,  A61K31/4155 ,  A61K31/4406 ,  A61K31/4439 ,  A61K31/445 ,  A61K31/55 ,  C07D209/46 ,  C07D401/06 ,  C07D401/10 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D405/04 ,  C07D471/04

Abstract: The present invention provides a compound having a cholinergic muscarinic M1 receptor positive allosteric modulator activity and useful as an agent for the prophylaxis or treatment of Alzheimer's disease, schizophrenia, pain, sleep disorder, Parkinson's disease dementia, dementia with Lewy bodies, and the like.
The present invention relates to a compound represented by the formula (I) or a salt thereof.




wherein each symbol is as described in the specification, or a salt thereof.