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：US09487511B2

公开(公告)日：2016-11-08

申请号：US14682695

申请日：2015-04-09

Applicant: Takeda Pharmaceutical Company Limited

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

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

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.

Abstract translation: 本发明提供具有赖氨酸特异性脱甲基酶-1抑制作用的化合物，可用作精神分裂症，发育障碍，特别是具有智力障碍的疾病（例如自闭症谱系，Rett综合征， 唐氏综合征，歌舞伎综合征，脆性X综合征，克莱斯特综合征，1型神经纤维瘤病，Noonan综合征，结节性硬化症），神经变性疾病（如阿尔茨海默氏病，帕金森病，脊髓小脑变性（例如，牙周性苍白球萎缩症）和亨廷顿疾病）），癫痫 （例如，Dravet综合征）或药物依赖性等。 由下式表示的化合物，其中每个符号如本说明书中所定义，或其盐。

公开(公告)号：US20230037538A1

公开(公告)日：2023-02-09

申请号：US17847456

申请日：2022-06-23

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Dennis Solas ,  Anatoliy Kitaygorodskyy ,  Kumar Paulvannan ,  Vishwanath R. Lingappa ,  Masato Yoshikawa ,  Masahiro Ito ,  Yuta Tanaka ,  Keiko Kakegawa ,  Tomohiro Ohashi ,  Takuto Kojima ,  Akinori Toita ,  Osamu Kubo ,  Fumiaki Kikuchi ,  Florian Pünner ,  Junsi Wang

IPC: C07D217/20 ,  C07D405/06 ,  C07D471/04 ,  C07D401/10 ,  C07D405/10 ,  C07D413/10 ,  C07D405/12 ,  C07D401/12 ,  A61P25/28

Abstract: The present invention relates to compounds expected to be useful in the prevention and/or treatment of diseases such as amyotrophic lateral sclerosis, frontotemporal dementia, chronic traumatic encephalopathy, Alzheimer's disease, frontotemporal lobar degeneration, multisystem proteinopathy and the like, a method for preventing or treating such diseases, and the like.

公开(公告)号：US20220370491A1

公开(公告)日：2022-11-24

申请号：US17760908

申请日：2020-09-16

Applicant: National University Corporation Tokyo Medical and Dental University ,  Takeda Pharmaceutical Company Limited

Inventor： Takanori Yokota ,  Testuya Nagata ,  Hideki Furukawa ,  Takatoshi Yogo ,  Yasuo Nakagawa ,  Shigekazu Sasaki ,  Ryosuke Tokunoh ,  Tomohiro Seki ,  Kosuke Hidaka ,  Fumiaki Kikuchi ,  Osamu Kubo ,  Takahito Kasahara ,  Takuto Kojima ,  Junsi Wang ,  Norihito Tokunaga

IPC: A61K31/713 ,  A61K47/54 ,  A61P25/00 ,  A61K9/00

Abstract: The object of the present invention is to provide a nucleic acid agent that is efficiently delivered to the nervous system, for example, the central nervous system to which drug delivery can be prevented by BBB, and produces an antisense effect on the target transcriptional product at the delivery site, and a composition comprising the same. In an embodiment, the present invention provides a double-stranded nucleic acid complex formed by annealing a first nucleic acid strand that hybridizes to a part of a target transcriptional product and has an antisense effect on the target transcriptional product, and a second nucleic acid strand that comprises a base sequence complementary to the first nucleic acid strand and is bound to a C22-35 alkyl group optionally substituted with a hydroxy group or an analog thereof.

公开(公告)号：US10899752B2

公开(公告)日：2021-01-26

申请号：US16394762

申请日：2019-04-25

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Takahiro Sugimoto ,  Shinkichi Suzuki ,  Hiroki Sakamoto ,  Masami Yamada ,  Minoru Nakamura ,  Makoto Kamata ,  Kenichiro Shimokawa ,  Masataka Murakami ,  Jinichi Yonemori ,  Takuto Kojima

IPC: C07D413/14 ,  C07D413/04 ,  C07D413/06 ,  C07D413/10 ,  C07D417/06 ,  C07D471/04 ,  C07D491/107 ,  C07D265/22 ,  C07F7/02 ,  A61P25/28 ,  C07D417/10 ,  C07F7/08

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：US10696651B2

公开(公告)日：2020-06-30

申请号：US16323863

申请日：2017-08-09

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Jun Fujimoto ,  Xin Liu ,  Osamu Kurasawa ,  Terufumi Takagi ,  Douglas Robert Cary ,  Hiroshi Banno ,  Yasutomi Asano ,  Takuto Kojima

IPC: C07D401/12 ,  C07D403/12 ,  C07D401/14 ,  C07D213/75 ,  C07D405/12 ,  C07D239/42 ,  C07D241/12 ,  C07D471/04 ,  C07D498/04 ,  C07D213/65 ,  A61P35/00 ,  C07D241/20 ,  C07D213/73 ,  A61K31/53 ,  A61K31/505 ,  A61K31/4406 ,  A61K31/444 ,  A61K31/4965 ,  C07D213/68 ,  C07D213/42 ,  A61K31/506 ,  A61K31/497 ,  A61K31/4375 ,  C07D239/20 ,  A61P43/00 ,  A61K31/5383 ,  A61K31/437 ,  A61K31/44 ,  C07D253/06 ,  C07D231/12 ,  C07D239/30 ,  C07D239/34 ,  C07D239/48 ,  C07D253/07 ,  C07D409/12 ,  C07D487/04

Abstract: Provided is a heterocyclic compound that may have a GCN2 inhibitory action, and is expected to be useful for the prophylaxis or treatment of GCN2 associated diseases including cancer and the like. 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：US10676461B2

公开(公告)日：2020-06-09

申请号：US16342892

申请日：2017-10-17

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Katsunori Nagai ,  Takuto Kojima ,  Shinichi Imamura ,  Masao Hirakata

IPC: C07D401/14 ,  A61P3/00 ,  A61P35/00 ,  A61K9/00 ,  A61K31/05 ,  A61K31/09 ,  A61K31/57 ,  A61K31/58 ,  A61K31/6615 ,  A61P43/00 ,  A61K31/498 ,  A61K45/06

Abstract: The present invention relates to N-((3S,4R)-1-((8-chloroquinoxalin-6-yl)carbonyl)-3-(4-fluorophenyl)piperidin-4-yl)-1-methyl-5-(trifluoromethyl)-1H-pyrazole-3-carboxamide, which is a compound that can be useful for the treatment or prevention of SPT-related diseases including congenital diseases associated with the storage of sphingolipids, such as cancer and Niemann-Pick disease, or a salt thereof.

公开(公告)号：US10323027B2

公开(公告)日：2019-06-18

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 ,  Masataka Murakami ,  Jinichi Yonemori ,  Takuto Kojima

IPC: C07D413/14 ,  C07D413/04 ,  C07D413/06 ,  C07D413/10 ,  C07D417/06 ,  C07D471/04 ,  C07D265/22 ,  C07D491/107 ,  C07F7/02 ,  A61P25/28 ,  C07D417/10 ,  C07F7/08

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：US20150266881A1

公开(公告)日：2015-09-24

申请号：US14435085

申请日：2013-10-11

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Naoki Tomita ,  Daisuke Tomita ,  Yusuke Tominari ,  Shinichi Imamura ,  Shinji Morimoto ,  Takuto Kojima ,  Masashi Toyofuku ,  Yasushi Hattori ,  Tomohiro Kaku ,  Mitsuhiro Ito

IPC: C07D487/04 ,  C07D231/38 ,  C07C237/38 ,  C07C237/30 ,  C07D241/12 ,  C07D213/36 ,  C07D471/04 ,  C07D207/46 ,  C07D241/18 ,  C07D319/18 ,  C07D265/36 ,  C07D333/20 ,  C07D285/135 ,  C07D277/38 ,  C07D405/12 ,  C07D417/12 ,  C07D413/12 ,  C07D223/12 ,  C07D513/04 ,  C07C237/40

CPC classification number: C07D487/04 ,  A61K45/06 ,  C07C237/30 ,  C07C237/38 ,  C07C237/40 ,  C07C255/29 ,  C07C255/58 ,  C07C255/60 ,  C07C317/40 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07D207/12 ,  C07D207/46 ,  C07D211/58 ,  C07D213/36 ,  C07D213/40 ,  C07D223/12 ,  C07D231/38 ,  C07D231/40 ,  C07D241/12 ,  C07D241/18 ,  C07D261/14 ,  C07D265/36 ,  C07D277/38 ,  C07D285/135 ,  C07D295/135 ,  C07D309/14 ,  C07D319/18 ,  C07D333/20 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D513/04

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, Alzheimer's disease, Parkinson's disease or Huntington's disease, and the like. The present invention relates to a compound represented by the formula wherein A is a hydrocarbon group optionally having substituent(s), or a heterocyclic group optionally having substituent(s); B is a benzene ring optionally having further substituent(s); R1, R2 and R3 are each independently a hydrogen atom, a hydrocarbon group optionally having substituent(s), or a heterocyclic group optionally having substituent(s); A and R1 are optionally bonded to each other to form, together with the adjacent nitrogen atom, a cyclic group optionally having substituent(s); and R2 and R3 are optionally bonded to each other to form, together with the adjacent nitrogen atom, a cyclic group optionally having substituent(s), or a salt thereof.

Abstract translation: 本发明提供了具有赖氨酸特异性脱甲基酶1抑制作用的化合物，可用作精神分裂症，阿尔茨海默病，帕金森病或亨廷顿病等预防或治疗药物等药物。 本发明涉及由下式表示的化合物：其中A是任选具有取代基的烃基或任选具有取代基的杂环基; B是任选具有其它取代基的苯环; R 1，R 2和R 3各自独立地为氢原子，任选具有取代基的烃基或任选具有取代基的杂环基; A和R1任选地彼此键合，与相邻的氮原子一起形成任选具有取代基的环状基团; R 2和R 3可以相互键合，与相邻的氮原子一起形成任选具有取代基的环状基团或其盐。