-
公开(公告)号:US10183949B2
公开(公告)日:2019-01-22
申请号:US15441385
申请日:2017-02-24
Applicant: The University of Tokyo , TOHOKU UNIVERSITY , Shionogi & Co., Ltd.
Inventor: Tetsuo Nagano , Takayoshi Okabe , Hirotatsu Kojima , Mitsuyasu Kawaguchi , Osamu Nureki , Ryuichiro Ishitani , Hiroshi Nishimasu , Junken Aoki , Nobuyuki Tanaka , Yasuhiko Kanda , Yoshiyuki Kioi , Yusuke Tateno , Shiro Kida , Junji Yamane
IPC: C07D491/107 , C07D239/47 , C07D239/36 , C07D405/12 , C07D401/12 , C07D403/06 , C07D413/06 , C07D471/08 , C07D409/12 , C07D417/12 , C07D413/12 , C07D403/12 , C07D401/04 , C07D403/04 , C07D471/10
Abstract: A compound according to any one of formula (Ia) to (Ic), or its pharmaceutically acceptable salt: wherein R1, R2, R3, R4a, R4c, R5 are as defined in the description.
-
公开(公告)号:US20240024266A1
公开(公告)日:2024-01-25
申请号:US18036998
申请日:2021-11-16
Applicant: Hiroshima University , Tokyo University of Pharmacy & Life Sciences , The University of Tokyo
Inventor: Tomoichiro Asano , Takemasa Sakaguchi , Takeshi Yamamotoya , Yusuke Nakatsu , Hisanaka Ito , Takayoshi Okabe , Jeffrey Encinas
IPC: A61K31/196 , A61P31/14 , A61K31/47 , A61K31/403 , A61K31/357 , A61K31/198 , A61K31/216 , A61K31/538 , A61K31/235 , A61K31/341 , A61K31/405 , A61K31/4439 , A61K31/4709 , A61K31/498 , A61K31/4045 , A61K31/27 , A61K31/194 , A61K31/192 , A61K31/683 , A61K31/4035 , A61K31/197 , A61K31/36 , A61K31/4406 , A61K31/245 , A61K31/472 , A61K31/444
CPC classification number: A61K31/196 , A61P31/14 , A61K31/47 , A61K31/403 , A61K31/357 , A61K31/198 , A61K31/216 , A61K31/538 , A61K31/235 , A61K31/341 , A61K31/405 , A61K31/4439 , A61K31/4709 , A61K31/498 , A61K31/4045 , A61K31/27 , A61K31/194 , A61K31/192 , A61K31/683 , A61K31/4035 , A61K31/197 , A61K31/36 , A61K31/4406 , A61K31/245 , A61K31/472 , A61K31/444
Abstract: [Problem] To develop novel therapeutic agents for viral diseases such as coronavirus infections.
[Solution] The present invention provides a therapeutic or prophylactic agent for viral diseases containing a compound with inhibitory activity against the function of Pin1 or a pharmaceutically acceptable salt thereof as an active ingredient.-
公开(公告)号:US20230133581A1
公开(公告)日:2023-05-04
申请号:US17905953
申请日:2021-03-09
Applicant: Hiroshima University , Tokyo University of Pharmacy & Life Sciences , The University of Tokyo
Inventor: Tomoichiro Asano , Yusuke Nakatsu , Hisanaka Ito , Takayoshi Okabe
IPC: C07D209/86 , C07D401/12 , C07D403/12 , C07D405/12 , C07C237/48 , C07D215/48 , C07D319/16 , A61P1/16 , A61P29/00 , A61P31/14 , A61P3/04 , C07D319/20 , C07C275/42
Abstract: [Problem] To develop a group of novel compounds with an inhibitory activity against the function of Pin1 so as to use them as candidate compounds for medicaments.
[Solution] The present invention provides: a compound represented by the following Formula (I) or a salt thereof, as well as a Pin1 inhibitor, a pharmaceutical composition, a therapeutic or prophylactic agent for inflammatory diseases, a therapeutic or prophylactic agent for fatty liver diseases, a therapeutic or prophylactic agent for obesity, and a therapeutic or prophylactic agent for COVID-19 that utilize the aforementioned compounds or the salts thereof:-
公开(公告)号:US20190382330A1
公开(公告)日:2019-12-19
申请号:US16464034
申请日:2017-11-29
Applicant: Hiroshima University , Tokyo University of Pharmacy & Life Sciences , The University of Tokyo
Inventor: Tomoichiro Asano , Yusuke Nakatsu , Hisanaka Ito , Takayoshi Okabe
IPC: C07C65/30 , A61P35/00 , A61P1/16 , A61P1/04 , A61K9/00 , C07C65/40 , C07C62/36 , C07D307/68 , C07C59/74 , C07D265/38 , C07D209/86 , C07D209/08 , C07C229/56 , C07C229/16
Abstract: An object of the present invention is to develop a therapeutic agent for an inflammatory disease such as an inflammatory bowel disease or NASH, which therapeutic agent shows less side effects and high effectiveness. The present invention provides a compound represented by Formula (I) or a salt thereof; and a Pin1 inhibitor, a pharmaceutical composition, a therapeutic agent or a prophylactic agent for an inflammatory disease, and a therapeutic agent or a prophylactic agent for colon cancer, containing the compound.
-
公开(公告)号:US11504379B2
公开(公告)日:2022-11-22
申请号:US16636746
申请日:2018-08-06
Applicant: Hiroshima University , Tokyo University of Pharmacy & Life Sciences , The University of Tokyo
Inventor: Tomoichiro Asano , Yusuke Nakatsu , Hisanaka Ito , Takayoshi Okabe
IPC: C07C275/36 , C07C275/28 , C07C275/38 , C07C233/46 , C07C233/63 , C07C233/51 , C07C233/87 , C07C271/22 , C07C235/40 , C07D209/88 , C07D209/82 , C07D215/02 , C07D295/195 , C07D233/24 , C07D265/38 , A61P3/04 , A61P29/00 , A61P35/00 , A61K45/06 , A61K31/216 , A61K31/473 , A61K31/198 , A61K31/538 , A61K31/404
Abstract: The purpose of the invention is to develop, as drug-candidate compounds, a group of novel compounds having the activity of inhibiting functions of Pin1. The invention provides: a compound represented by formula (I) or a salt thereof; and a Pin1 inhibitor, a pharmaceutical composition, a therapeutic or prophylactic agent for inflammatory diseases, a therapeutic or prophylactic agent for cancer, and a therapeutic or prophylactic agent for adiposity that use said compound/salt.
-
公开(公告)号:US11203565B2
公开(公告)日:2021-12-21
申请号:US16464034
申请日:2017-11-29
Applicant: Hiroshima University , Tokyo University of Pharmacy & Life Sciences , The University of Tokyo
Inventor: Tomoichiro Asano , Yusuke Nakatsu , Hisanaka Ito , Takayoshi Okabe
IPC: C07C65/30 , A61P35/00 , A61P1/16 , A61P1/04 , A61K9/00 , C07C65/40 , C07C62/36 , C07D307/68 , C07D209/86 , C07D209/08 , C07C229/56 , C07C229/16 , C07C59/74 , C07D265/38
Abstract: An object of the present invention is to develop a therapeutic agent for an inflammatory disease such as an inflammatory bowel disease or NASH, which therapeutic agent shows less side effects and high effectiveness. The present invention provides a compound represented by Formula (I) or a salt thereof; and a Pin1 inhibitor, a pharmaceutical composition, a therapeutic agent or a prophylactic agent for an inflammatory disease, and a therapeutic agent or a prophylactic agent for colon cancer, containing the compound.
-
公开(公告)号:US10689394B2
公开(公告)日:2020-06-23
申请号:US16306696
申请日:2017-06-14
Applicant: The University of Tokyo
Inventor: Hidenori Ichijo , Kengo Homma , Naomi Tsuburaya , Tetsuo Nagano , Takayoshi Okabe , Hirotatsu Kojima , Manabu Shimonishi , Takao Fujisawa , Norio Shiibata , Tsunehiko Higuchi , Seiichi Nakamura , Hidehiko Nakagawa , Shin-Ichi Ikeda
IPC: C07D495/04 , C07D401/04 , A61P21/02 , A61K31/4365 , A61P21/00
Abstract: A compound represented by the following formula (1) is provided: wherein X represents a sulfur atom or —CH═CH—; A1 to A4 each independently represent a carbon atom or a nitrogen atom, and at least one of A1 to A4 is a nitrogen atom; R1 represents any one of a 1,2,3,4-tetrahydroquinolyl group (or a 3,4-dihydro-1(2H)-quinolyl group), a 3,4-dihydro-4,4-dimethyl-1(2H)-quinolyl group, a 2,3,4,5-tetrahydro-1H-1-benzazepinyl group, or a substituent represented by the following formula (2): wherein R4 represents a 2,3,4-trifluorophenyl group, a 4-iodophenyl group, a 2,3-difluorophenyl group, a 3,5-difluorophenyl group, a 5-fluoro-2-methylphenyl group, a 3-pentafluorosulfanylphenyl group, a 2,6-dimethylphenyl group, a 4-benzyloxyphenyl group, a 3,5-bis(trifluoromethyl)biphenyl group, a 4-tert-butylphenyl group, a 3-methoxyphenyl group, an unsubstituted or substituted pyridyl group, or an unsubstituted or substituted naphthyl group; R5 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group optionally containing an oxygen atom and/or a double bond, or an unsubstituted or substituted aromatic lower alkyl group; R2 represents a hydrogen atom, a lower alkyl group, a lower acyl group, or an unsubstituted or substituted aromatic lower alkyl group; and R3 represents a hydrogen atom, or R2 and R3 may bind to each other to form a ring.
-
公开(公告)号:US20190177336A1
公开(公告)日:2019-06-13
申请号:US16306696
申请日:2017-06-14
Applicant: The University of Tokyo
Inventor: Hidenori Ichijo , Kengo Homma , Naomi Tsuburaya , Tetsuo Nagano , Takayoshi Okabe , Hirotatsu Kojima , Manabu Shimonishi , Takao Fujisawa , Norio Shiibata , Tsunehiko Higuchi , Seiichi Nakamura , Hidehiko Nakagawa , Shin-Ichi Ikeda
IPC: C07D495/04 , C07D401/04 , A61P21/00
Abstract: It is an object of the present invention to provide a compound inhibiting the binding between ALS-related mutant SOD1 and Derlin-1, a medicament comprising the compound, and a method for treating ALS by administering the medicament to a patient. More specifically, the aforementioned compound is represented by the following formula (1): wherein X represents a sulfur atom or —CH═CH—; A1 to A4 each independently represent a carbon atom or a nitrogen atom, and at least one of A1 to A4 is a nitrogen atom; R1 represents a 1,2,3,4-tetrahydroquinolyl group (or a 3,4-dihydro-1(2H)-quinolyl group), a 3,4-dihydro-4,4-dimethyl-1(2H)-quinolyl group, a 2,3,4,5-tetrahydro-1H-1-benzazepinyl group, or a substituent represented by the following formula (2): wherein R4 represents an unsubstituted or optionally substituted phenyl group, an unsubstituted or optionally substituted pyridyl group, or an unsubstituted or optionally substituted naphthyl group, and R5 represents any one of a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group (optionally containing an oxygen atom and/or a double bond), or an unsubstituted or optionally substituted aromatic lower alkyl group; R2 represents a hydrogen atom, a lower alkyl group, a lower acyl group, or an unsubstituted or optionally substituted aromatic lower alkyl group; and R3 represents a hydrogen atom, or R2 and R3 may bind to each other to form a ring.
-
公开(公告)号:US11071738B2
公开(公告)日:2021-07-27
申请号:US16636752
申请日:2018-08-06
Applicant: Hiroshima University , Tokyo University of Pharmacy & Life Sciences , The University of Tokyo
Inventor: Tomoichiro Asano , Yusuke Nakatsu , Hisanaka Ito , Takayoshi Okabe
IPC: A61K31/19 , A61K31/415 , A61K31/5377 , A61P1/16 , A61P3/04 , A61K31/341 , A61K31/403 , A61K31/4184 , A61K31/4439 , A61K45/06
Abstract: The purpose of the invention is to develop a novel therapeutic agent for fatty liver diseases such as NASH or NAFLD. The invention provides a therapeutic or prophylactic agent for fatty liver diseases that comprises, as an active ingredient, a compound represented by formula (I) or a pharmaceutically acceptable salt thereof. The invention also provides a therapeutic or prophylactic agent for adiposity that comprises, as an active ingredient, a compound represented by formula (I) or a pharmaceutically acceptable salt thereof.
-
公开(公告)号:US10189843B2
公开(公告)日:2019-01-29
申请号:US15120763
申请日:2015-02-26
Applicant: The University of Tokyo , TOHOKU UNIVERSITY , Shionogi & Co., Ltd.
Inventor: Tetsuo Nagano , Takayoshi Okabe , Hirotatsu Kojima , Mitsuyasu Kawaguchi , Osamu Nureki , Ryuichiro Ishitani , Hiroshi Nishimasu , Junken Aoki , Chiaki Fujikoshi , Manabu Katou , Masahide Odan , Nobuyuki Tanaka , Yusuke Tateno , Junji Yamane
IPC: C07D487/04 , C07D491/147 , C07D519/00 , C07D487/18
Abstract: The present invention provides a compound of formula (1), wherein R1, R2, R3, R4a, R4b, R5a and R5b are as defined in the description, which has an autotaxin inhibitory activity, a pharmaceutical composition comprising the compound as an active ingredient, and a method of prevention or treatment of a disease involving autotaxin, which is characterized by administering the compound.
-
-
-
-
-
-
-
-
-