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公开(公告)号：US20220370491A1
公开(公告)日：2022-11-24
申请号：US17760908
申请日：2020-09-16
申请人： National University Corporation Tokyo Medical and Dental University , Takeda Pharmaceutical Company Limited
发明人： 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分类号： A61K31/713 , A61K47/54 , A61P25/00 , A61K9/00
摘要： 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.
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公开(公告)号：US20210024929A1
公开(公告)日：2021-01-28
申请号：US16980191
申请日：2019-03-13
申请人： National University Corporation Tokyo Medical and Dental University , Takeda Pharmaceutical Company Limited
发明人： Takanori Yokota , Tetsuya Nagata , Hideki Furukawa , Yasuo Nakagawa , Takatoshi Yogo , Ryosuke Tokunoh , Shigekazu Sasaki , Kosuke Hidaka , Tomohiro Seki , Kenichi Miyata , Akio Uchida
IPC分类号： C12N15/113 , A61P25/00
摘要： 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：US20230295628A1
公开(公告)日：2023-09-21
申请号：US18163506
申请日：2023-02-02
申请人： National University Corporation Tokyo Medical and Dental University , Takeda Pharmaceutical Company Limited
发明人： Takanori Yokota , Tetsuya Nagata , Hideki Furukawa , Yasuo Nakagawa , Takatoshi Yogo , Ryosuke Tokunoh , Shigekazu Sasaki , Kosuke Hidaka , Tomohiro Seki , Kenichi Miyata , Akio Uchida
IPC分类号： C12N15/113 , A61P25/00
CPC分类号： C12N15/113 , A61P25/00 , C12N2310/11 , C12N2310/341
摘要： 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.
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公开(公告)号：US11597928B2
公开(公告)日：2023-03-07
申请号：US16980191
申请日：2019-03-13
申请人： National University Corporation Tokyo Medical and Dental University , Takeda Pharmaceutical Company Limited
发明人： Takanori Yokota , Tetsuya Nagata , Hideki Furukawa , Yasuo Nakagawa , Takatoshi Yogo , Ryosuke Tokunoh , Shigekazu Sasaki , Kosuke Hidaka , Tomohiro Seki , Kenichi Miyata , Akio Uchida
IPC分类号： C07H21/04 , C12N15/113 , A61P25/00
摘要： 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：US20240117346A1
公开(公告)日：2024-04-11
申请号：US17767663
申请日：2020-10-09
申请人： National University Corporation Tokyo Medical and Dental University , Takeda Pharmaceutical Company Limited
发明人： Takanori Yokota , Tetsuya Nagata , Hiroki Yamada , Hideki Furukawa , Takatoshi Yogo , Kenichi Miyata , Akio Uchida , Naoki Tomita
IPC分类号： C12N15/113
CPC分类号： C12N15/113 , C12N2310/11 , C12N2310/315 , C12N2310/321 , C12N2310/3231 , C12N2310/341 , C12N2310/3515 , C12N2310/53 , C12N2320/51
摘要： In an embodiment, an object of the present invention is to provide a double-stranded nucleic acid complex having a novel structure.
In an embodiment, the present invention relates to a nucleic acid complex comprising a first nucleic acid strand and a second nucleic acid strand, wherein said first nucleic acid strand: (1) is capable of hybridizing to at least a part of a target transcriptional product; (2) has an antisense effect on the target transcriptional product; and (3) is a gapmer comprising a central region, and a 5′ wing region and a 3′ wing region, said second nucleic acid strand comprises at least one sugar-unmodified central region (first exposed region) consisting of one sugar-unmodified ribonucleoside or two or three contiguous sugar-unmodified ribonucleosides linked by an internucleoside bond, which is or are complementary to a part of said first nucleic acid strand, and said first nucleic acid strand is annealed to said second nucleic acid strand.-
公开(公告)号：US10968231B2
公开(公告)日：2021-04-06
申请号：US16497141
申请日：2018-03-29
发明人： Seiji Miwatashi , Yasufumi Miyamoto , Koji Watanabe , Yayoi Nakayama , Yuko Hitomi , Jumpei Aida , Nobuyuki Takakura , Hideki Furukawa , Naoyoshi Noguchi , Yasuhiro Hirata , Shizuo Kasai , Toshitake Kobayashi , Tsuyoshi Maekawa , Satoshi Sasaki , Shigemitsu Matsumoto
IPC分类号： C07D491/052 , C07D211/22 , C07D401/12 , C07D401/14
摘要： Provided is a novel aromatic ring compound which may have a GPR40 agonist activity and a GLP-1 secretagogue action. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof may have a GPR40 agonist activity and a GLP-1 secretagogue action, may be useful for the prophylaxis or treatment of cancer, obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia and the like, and may afford superior efficacy.
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公开(公告)号：US20150152052A1
公开(公告)日：2015-06-04
申请号：US14389004
申请日：2013-03-28
发明人： Minoru Sasaki , Hideki Furukawa , Kousuke Hidaka , Kyoko Toyofuku , Takatoshi Yogo , Toshiki Murata
IPC分类号： C07D211/60 , C07D405/14 , C07D413/12 , C07D498/04 , C07D401/12 , C07D401/06
CPC分类号： C07D211/60 , C07D401/06 , C07D401/12 , C07D405/14 , C07D413/12 , C07D498/04
摘要： Provided is an aromatic ring compound having a glucagon antagonistic action, which is useful for the prophylaxis or treatment of diabetes and the like. A compound represented by the formula (I): wherein each symbol is as defined in the DESCRIPTION, or a salt thereof has a superior glucagon antagonistic action, and is useful as a glucagon antagonist, a glucose production inhibitor or an agent for the prophylaxis or treatment of diabetes and the like.
摘要翻译： 提供具有胰高血糖素拮抗作用的芳香环化合物，其可用于预防或治疗糖尿病等。 由式（I）表示的化合物：其中各符号如说明书所定义，或其盐具有优良的胰高血糖素拮抗作用，可用作胰高血糖素拮抗剂，葡萄糖产生抑制剂或预防或 治疗糖尿病等。
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公开(公告)号：US11186565B2
公开(公告)日：2021-11-30
申请号：US16499432
申请日：2018-03-29
发明人： Seiji Miwatashi , Yasufumi Miyamoto , Koji Watanabe , Yayoi Nakayama , Yuko Hitomi , Jumpei Aida , Nobuyuki Takakura , Hideki Furukawa , Naoyoshi Noguchi , Yasuhiro Hirata , Kazuaki Takami , Norihito Tokunaga , Tomohiro Okawa , Akito Shibuya , Shizuo Kasai , Toshitake Kobayashi , Tsuyoshi Maekawa
IPC分类号： C07D401/12 , C07C59/72 , C07D211/22 , C07D213/64 , C07D401/10 , C07D401/14 , C07D413/10
摘要： Provided is a novel aromatic ring compound which may have a GPR40 agonist activity and a GLP-1 secretagogue action. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof may have a GPR40 agonist activity and a GLP-1 secretagogue action, may be useful for the prophylaxis or treatment of cancer, obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia and the like, and may afford superior efficacy.
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公开(公告)号：US09776962B2
公开(公告)日：2017-10-03
申请号：US14898633
申请日：2014-08-08
发明人： 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分类号： C07D211/34 , C07D211/22 , C07D213/30 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/10 , C07D413/14
CPC分类号： C07D211/34 , C07D211/22 , C07D213/30 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/10 , C07D413/14
摘要： 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.
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公开(公告)号：US09073864B2
公开(公告)日：2015-07-07
申请号：US14389004
申请日：2013-03-28
发明人： Minoru Sasaki , Hideki Furukawa , Kousuke Hidaka , Kyoko Toyofuku , Takatoshi Yogo , Toshiki Murata
IPC分类号： C07D211/06 , A61K31/445 , C07D211/60 , C07D401/12 , C07D401/06 , C07D413/12 , C07D498/04 , C07D405/14
CPC分类号： C07D211/60 , C07D401/06 , C07D401/12 , C07D405/14 , C07D413/12 , C07D498/04
摘要： Provided is an aromatic ring compound having a glucagon antagonistic action, which is useful for the prophylaxis or treatment of diabetes and the like. A compound represented by the formula (I): wherein each symbol is as defined in the DESCRIPTION, or a salt thereof has a superior glucagon antagonistic action, and is useful as a glucagon antagonist, a glucose production inhibitor or an agent for the prophylaxis or treatment of diabetes and the like.
摘要翻译： 提供具有胰高血糖素拮抗作用的芳香环化合物，其可用于预防或治疗糖尿病等。 由式（I）表示的化合物：其中各符号如说明书所定义，或其盐具有优良的胰高血糖素拮抗作用，可用作胰高血糖素拮抗剂，葡萄糖产生抑制剂或预防或 治疗糖尿病等。
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