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：US20210024929A1

公开(公告)日：2021-01-28

申请号：US16980191

申请日：2019-03-13

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

Inventor： Takanori Yokota ,  Tetsuya Nagata ,  Hideki Furukawa ,  Yasuo Nakagawa ,  Takatoshi Yogo ,  Ryosuke Tokunoh ,  Shigekazu Sasaki ,  Kosuke Hidaka ,  Tomohiro Seki ,  Kenichi Miyata ,  Akio Uchida

IPC: C12N15/113 ,  A61P25/00

Abstract: Developed and provided is: a nucleic acid agent that is efficiently delivered to the central nervous system, to which drug delivery is inhibited by the blood brain barrier mechanism, and that provides an antisense effect to a target transcription product at the delivery site; and a composition containing such a nucleic acid agent.
Provided is a double-stranded nucleic acid complex consisting of a first nucleic acid strand and a second nucleic acid strand that are annealed to each other; wherein the first nucleic acid strand hybridizes with part of a target transcription product and has an antisense effect on the target transcription product; and wherein the second nucleic acid strand includes a base sequence complementary to the first nucleic acid strand and is conjugated to a phosphatidylethanolamine or an analog thereof.

公开(公告)号：US10214498B2

公开(公告)日：2019-02-26

申请号：US15517227

申请日：2015-10-22

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Yoshihiro Banno ,  Masahiro Kamaura ,  Kazuaki Takami ,  Koichiro Fukuda ,  Shigekazu Sasaki

IPC: A61P27/02 ,  C07K14/47 ,  C12N15/09 ,  A61K31/415 ,  A61K31/505 ,  C07D213/65 ,  C07D213/70 ,  C07D231/12 ,  C07D231/22 ,  C07D239/34 ,  A61K31/4418 ,  A61K31/421 ,  C07D263/38 ,  C07D263/46

Abstract: Provided is a heterocyclic compound having a superior RBP4-lowering action and useful as a medicament for the prophylaxis or treatment of a disease or symptom mediated by an increase in RBP4 or retinol supplied by RBP4. A compound represented by the formula (I): wherein each symbol is as defined in the Description, or a salt thereof has a superior RBP4-lowering action, and is useful as a medicament for the prophylaxis or treatment of a disease or symptom mediated by an increase in RBP4 or retinol supplied by RBP4.

公开(公告)号：US20150045351A1

公开(公告)日：2015-02-12

申请号：US14381347

申请日：2013-03-06

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Tomokazu Kusumoto ,  Shigekazu Sasaki ,  Hironobu Maezaki

IPC: C07D495/06 ,  C07D491/06 ,  C07D487/06

CPC classification number: C07D495/06 ,  C07D487/06 ,  C07D491/06

Abstract: The present invention provides a compound having a superior serotonin 5-HT2C receptor activating action.The present invention relates to a compound represented by the formula (1) wherein ring A is an aromatic carbocycle optionally having substituent(s) or an aromatic heterocycle optionally having substituent(s), X is —N(R1)—, —O— or the like, when ring A is an aromatic carbocycle optionally having substituent(s), then R1 is a hydrogen atom, an alkyl group optionally having substituent(s), or the like, and when ring A is an aromatic heterocycle optionally having substituent(s), then R1 is a hydrogen atom, an alkyl group optionally having substituent(s), a cycloalkyl group optionally having substituent(s), or the like, is a single bond or a double bond, and n is an integer of 0, 1 or 2, or a salt thereof.

Abstract translation: 本发明提供具有优良的5-羟色胺5-HT 2C受体激活作用的化合物。 本发明涉及由式（1）表示的化合物，其中环A是任选具有取代基的芳族碳环或任选具有取代基的芳族杂环，X是-N（R 1） - ，-O- 当环A是任选具有取代基的芳族碳环，则R1是氢原子，任选具有取代基的烷基等，当环A是任选具有取代基的芳族杂环时， 那么R 1是氢原子，任选具有取代基的烷基，任选具有取代基的环烷基等是单键或双键，n是整数 0,1或2，或其盐。

公开(公告)号：US09944596B2

公开(公告)日：2018-04-17

申请号：US15518782

申请日：2015-10-22

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Yoshihiro Banno ,  Masahiro Kamaura ,  Takahiko Taniguchi ,  Kazuaki Takami ,  Koichiro Fukuda ,  Shigekazu Sasaki

IPC: C07D207/08 ,  A61K31/401

CPC classification number: C07D207/08 ,  A61K31/40 ,  A61K31/401 ,  C12N15/09

Abstract: Provided is a heterocyclic compound having a superior RBP4-lowering action and useful as a medicament for the prophylaxis or treatment of a disease or symptom mediated by an increase in RBP4 or retinol supplied by RBP4. A compound represented by the formula (I): wherein each symbol is as defined in the Description, or a salt thereof has a superior RBP4-lowering action, and is useful as a medicament for the prophylaxis or treatment of a disease or symptom mediated by an increase in RBP4 or retinol supplied by RBP4.

公开(公告)号：US09469637B2

公开(公告)日：2016-10-18

申请号：US14397066

申请日：2013-04-24

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Satoshi Mikami ,  Shinji Nakamura ,  Tomoko Ashizawa ,  Shigekazu Sasaki ,  Takahiko Taniguchi ,  Izumi Nomura ,  Masanori Kawasaki

IPC: C07D241/36 ,  C07D471/04 ,  C07D519/00

CPC classification number: C07D471/04 ,  A61K9/20 ,  A61K31/498 ,  A61K31/555 ,  C07D519/00 ,  C07F7/1804

Abstract: The present invention provides a compound having a PDE2A selective inhibitory action, which is useful as an agent for the prophylaxis or treatment of schizophrenia, Alzheimer's disease and the like.The present invention is a compound represented by the formula (1): wherein each symbol is as described in the specification, or a salt thereof.