Patents by Inventor Fumiyuki Shirai
Fumiyuki Shirai has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
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Publication number: 20230127046Abstract: A compound represented by the general formula (I) given below or a pharmacologically acceptable salt thereof has been found to have a strong G9a inhibitory effect. The compound (I) or the pharmacologically acceptable salt thereof inhibits G9a and thereby has high usefulness for the treatment, prevention or suppression of various pathological conditions (proliferative disease such as cancer, ?-globin abnormality, fibrosis, pain, neurodegenerative disease, Prader-Willi syndrome, malaria, viral infection, myopathy, autism, etc.).Type: ApplicationFiled: November 26, 2020Publication date: April 27, 2023Applicants: RIKEN, TOKYO UNIVERSITY OF PHARMACY AND LIFE SCIENCES, MICROBIAL CHEMISTRY RESEARCH FOUNDATIONInventors: Tatsunobu SUMIYA, Yosuke NISHIGAYA, Ryosuke NAMIE, Noriaki HASHIMOTO, Akihiro ITO, Fumiyuki SHIRAI, Ko KIKUZATO, Minoru YOSHIDA
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Patent number: 11566017Abstract: Provided is a cell proliferation inhibitor comprising a compound of the formula (1) or a pharmacologically acceptable salt thereof: wherein J1 and J2 each represent CH or N, with the proviso that J1 and J2 are not simultaneously CH; r represents 0 to 4; each R101 is the same or different when r is 2 or more, and R101 represents a C1-6 alkyl group optionally substituted with a halogen atom or the like; s represents 0 to 5; each R102 is the same or different when s is 2 or more, and R102 represents a halogen atom or the like; R103 represents a hydrogen atom, a C1-6 alkyl group, a C3-6 cycloalkyl group, or a C3-6 cycloalkyl C1-6 alkyl group; and R101 and R103 are optionally linked together to form a five- to seven-membered ring hetero ring when R101 is present at the 8-position.Type: GrantFiled: December 26, 2018Date of Patent: January 31, 2023Assignees: RIKEN, JAPANESE FOUNDATION FOR CANCER RESEARCH, KABUSHIKI KAISHA YAKULT HONSHAInventors: Minoru Yoshida, Hiroyuki Seimiya, Yoko Yashiroda, Kenichi Washizuka, Fumiyuki Shirai, Nobuko Yoshimoto, Junichi Kazami
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Publication number: 20230017537Abstract: The present invention aims to provide a novel compound having a high mPTP-opening inhibitory activity and/or a useful therapeutic effect on various diseases. An aspect of the present invention relates to a mitochondrial permeability transition pore (mPTP)-opening inhibitor, a medicament or a pharmaceutical composition comprising a compound represented by formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are the same as defined in the specification and the claims, a stereoisomer thereof, a prodrug thereof, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, as an active ingredient. Another aspect of the present invention relates to a compound represented by formula (Ia), wherein R1a, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are the same as defined in the specification and the claims, a stereoisomer thereof, a prodrug thereof, or a salt thereof, or a solvate thereof.Type: ApplicationFiled: June 17, 2020Publication date: January 19, 2023Applicant: RIKENInventors: Tadafumi KATO, Mie SAKASHITA, Hirochika KAWAKAMI, Ko KIKUZATO, Fumiyuki SHIRAI
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Patent number: 11414429Abstract: Provided are 2-(piperidin-1-yl)pyrimidin-4(3H)-ones or pharmaceutically acceptable salts thereof, each characterized by having a 1,8-diazaspiro[4.5]deca-3-ene, 1-oxa-8-azaspiro[4.5]deca-3-ene, 2,8-diazaspiro[4.5]deca-3-ene, 2-oxa-8-azaspiro[4.5]deca-3-ene, 2,9-diazaspiro[5.5]undeca-3-ene, 1-oxa-9-azaspiro[5.5]undeca-3-ene, 1,9-diazaspiro[5.5]undeca-4-ene, or 3,9-diazaspiro[5.Type: GrantFiled: June 30, 2017Date of Patent: August 16, 2022Assignees: RIKEN, JAPANESE FOUNDATION FOR CANCER RESEARCH, KABUSHIKI KAISHA YAKULT HONSHAInventors: Minoru Yoshida, Hiroyuki Seimiya, Masayuki Okue, Yoko Yashiroda, Fumiyuki Shirai, Takeshi Tsumura, Yuko Kano, Kenichi Washizuka, Nobuko Yoshimoto, Yasuko Kouda, Takehiro Fukami, Tsubasa Chikada, Takashi Watanabe
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Publication number: 20210061789Abstract: Provided is a cell proliferation inhibitor comprising a compound of the formula (1) or a pharmacologically acceptable salt thereof: wherein J1 and J2 each represent CH or N, with the proviso that J1 and J2 are not simultaneously CH; r represents 0 to 4; each R101 is the same or different when r is 2 or more, and R101 represents a C1-6 alkyl group optionally substituted with a halogen atom or the like; s represents 0 to 5; each R102 is the same or different when s is 2 or more, and R102 represents a halogen atom or the like; R103 represents a hydrogen atom, a C1-6 alkyl group, a C3-6 cycloalkyl group, or a C3-6 cycloalkyl C1-6 alkyl group; and R101 and R103 are optionally linked together to form a five- to seven-membered ring hetero ring when R101 is present at the 8-position.Type: ApplicationFiled: December 26, 2018Publication date: March 4, 2021Applicants: RIKEN, JAPANESE FOUNDATION FOR CANCER RESEARCH, KABUSHIKI KAISHA YAKULT HONSHAInventors: Minoru YOSHIDA, Hiroyuki SEIMIYA, Yoko YASHIRODA, Kenichi WASHIZUKA, Fumiyuki SHIRAI, Nobuko YOSHIMOTO, Junichi KAZAMI
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Publication number: 20210060016Abstract: To provide an anticancer agent for preventing and/or treating cancer, comprising a tankyrase inhibitor containing a tankyrase inhibitory compound and a microtubule inhibitor containing a microtubule inhibitory compound as active ingredients.Type: ApplicationFiled: December 26, 2018Publication date: March 4, 2021Applicants: JAPANESE FOUNDATION FOR CANCER RESEARCH, RIKEN, KABUSHIKI KAISHA YAKULT HONSHAInventors: Hiroyuki SEIMIYA, Minoru YOSHIDA, Yoko YASHIRODA, Yukiko MURAMATSU, Fumiyuki SHIRAI, Kenichi WASHIZUKA
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Publication number: 20200172554Abstract: Provided are 2-(piperidin-1-yl)pyrimidin-4(3H)-ones or pharmaceutically acceptable salts thereof, each characterized by having a 1,8-diazaspiro[4.5]deca-3-ene, 1-oxa-8-azaspiro[4.5]deca-3-ene, 2,8-diazaspiro[4.5]deca-3-ene, 2-oxa-8-azaspiro[4.5]deca-3-ene, 2,9-diazaspiro[5.5]undeca-3-ene, 1-oxa-9-azaspiro[5.5]undeca-3-ene, 1,9-diazaspiro[5.5]undeca-4-ene, or 3,9-diazaspiro[5.Type: ApplicationFiled: June 30, 2017Publication date: June 4, 2020Applicants: RIKEN, JAPANESE FOUNDATION FOR CANCER RESEARCHInventors: Minoru YOSHIDA, Hiroyuki SEIMIYA, Masayuki OKUE, Yoko YASHIRODA, Fumiyuki SHIRAI, Takeshi TSUMURA, Yuko KANO, Kenichi WASHIZUKA, Nobuko YOSHIMOTO, Yasuko KOUDA, Takehiro FUKAMI, Tsubasa CHIKADA, Takashi WATANABE
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Patent number: 9585889Abstract: On the basis of a cathepsin S inhibitory effect, an excellent agent for treating or preventing autoimmune disease, allergic disease, graft rejection of an organ, bone marrow or tissue, systemic lupus erythematosus, or the like is provided. It was found that a nitrogen-containing bicyclic heterocyclic compound has an excellent cathepsin S inhibitory effect, thereby completing the invention. The compound of the present invention has an cathepsin S inhibitory effect, and can be used as an agent for preventing and/or treating autoimmune disease, allergic disease, graft rejection of an organ, bone marrow or tissue, systemic lupus erythematosus, or the like.Type: GrantFiled: February 8, 2016Date of Patent: March 7, 2017Assignee: Astellas Pharma Inc.Inventors: Yutaka Nakajima, Sunao Imada, Yuji Takasuna, Naohiro Aoyama, Takahiro Nigawara, Shohei Shirakami, Fumiyuki Shirai, Junji Sato, Keita Nakanishi, Kaori Kubo
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Publication number: 20160228442Abstract: On the basis of a cathepsin S inhibitory effect, an excellent agent for treating or preventing autoimmune disease, allergic disease, graft rejection of an organ, bone marrow or tissue, systemic lupus erythematosus, or the like is provided. It was found that a nitrogen-containing bicyclic heterocyclic compound has an excellent cathepsin S inhibitory effect, thereby completing the invention. The compound of the present invention has an cathepsin S inhibitory effect, and can be used as an agent for preventing and/or treating autoimmune disease, allergic disease, graft rejection of an organ, bone marrow or tissue, systemic lupus erythematosus, or the like.Type: ApplicationFiled: February 8, 2016Publication date: August 11, 2016Applicant: ASTELLAS PHARMA INC.Inventors: Yutaka Nakajima, Sunao Imada, Yuji Takasuna, Naohiro Aoyama, Takahiro Nigawara, Shohei Shirakami, Fumiyuki Shirai, Junji Sato, Keita Nakanishi, Kaori Kubo
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Patent number: 9328118Abstract: [Problem] On the basis of a cathepsin S inhibitory effect, an excellent agent for treating or preventing autoimmune disease, allergic disease, graft rejection of an organ, bone marrow or tissue, systemic lupus erythematosus, or the like is provided. [Means for Solution] It was found that a nitrogen-containing bicyclic heterocyclic compound has the excellent cathepsin S inhibitory effect, thereby completing the invention. The compound of the present invention has the cathepsin S inhibitory effect, and can be used as an agent for preventing and/or treating autoimmune disease, allergic disease, graft rejection of an organ, bone marrow or tissue, systemic lupus erythematosus, or the like.Type: GrantFiled: April 17, 2013Date of Patent: May 3, 2016Assignee: Astellas Pharma Inc.Inventors: Yutaka Nakajima, Sunao Imada, Yuji Takasuna, Naohiro Aoyama, Takahiro Nigawara, Shohei Shirakami, Fumiyuki Shirai, Junji Sato, Keita Nakanishi, Kaori Kubo
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Publication number: 20150126488Abstract: [Problem] On the basis of a cathepsin S inhibitory effect, an excellent agent for treating or preventing autoimmune disease, allergic disease, graft rejection of an organ, bone marrow or tissue, systemic lupus erythematosus, or the like is provided. [Means for Solution] It was found that a nitrogen-containing bicyclic heterocyclic compound has the excellent cathepsin S inhibitory effect, thereby completing the invention. The compound of the present invention has the cathepsin S inhibitory effect, and can be used as an agent for preventing and/or treating autoimmune disease, allergic disease, graft rejection of an organ, bone marrow or tissue, systemic lupus erythematosus, or the like.Type: ApplicationFiled: April 17, 2013Publication date: May 7, 2015Applicant: ASTELLAS PHARMA INCInventors: Yutaka Nakajima, Sunao Imada, Yuji Takasuna, Naohiro Aoyama, Takahiro Nigawara, Shohei Shirakami, Fumiyuki Shirai, Junji Sato, Keita Nakanishi, Kaori Kubo
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Patent number: 7750155Abstract: This invention relates to novel N-hydroxyacrylamide compounds of formula (I) and pharmaceutically acceptable salts thereof. More particularly, it relates to novel N-hydroxyacrylamide compounds and pharmaceutically acceptable salts thereof which act as a HDAC inhibitor, to a pharmaceutical composition comprising the same and to a method of using the same therapeutically in the treatment and/or prevention of HDAC-related disease.Type: GrantFiled: February 6, 2007Date of Patent: July 6, 2010Assignee: Astellas Pharma Inc.Inventors: Fumiyuki Shirai, Hideo Tsutsumi, Hiromichi Itani, Yoshihiro Kozuki, Yoshiteru Eikyu, Taro Masunaga
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Publication number: 20100069388Abstract: A compound having the following formula (I): wherein —R1 is hydrogen, optionally substituted lower alkyl, cyclo(lower)alkyl, cyclo(higher)alkyl, optionally substituted aryl, optionally substituted heterocyclyl, or aryl-fused cyclo(lower)alkyl, R2 is hydrogen or halogen, Z is CH or N, X is formula (II) R3 is lower alkyl which may be substituted with —OH or optionally substituted aryl, or lower alkanoyl, R4 is hydrogen or lower alkyl, Y is optionally substituted lower alkylene, or a salt thereof. The compound is useful as a histone deacetylase inhibitor.Type: ApplicationFiled: December 14, 2007Publication date: March 18, 2010Applicant: ASTELLAS PHARMA INC.Inventors: Yoshikazu Inoue, Yoshiteru Eikyu, Fumiyuki Shirai
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Patent number: 7557127Abstract: Compounds having the formula (I): wherein R1 is hydrogen, lower alkyl, lower alkenyl, lower or higher alkynyl, cyclo(lower)alkyl, cyclo(higher)alkyl, cyclo(lower)alkyl(lower)alkyl, cyclo(higher)alkyl(lower)alkyl, cyclo(lower)alkenyl(lower)alkyl, aryl-fused cyclo(lower)alkyl, lower alkoxy, acyl, aryl, ar(lower)alkoxy, ar(lower)alkyl, heteroar(lower)alkyl, amino, heteroaryl, heterocyclyl or heterocyclyl(lower)alkyl, which may be substituted with one or more suitable substituent(s), R2 is hydrogen or lower alkyl, X is pyrrolidinylene or piperidinylene, Y is pyridylene, which may be substituted with one or more suitable substituent(s), Z is lower alkenylene, which may be substituted with lower alkyl or halogen, and salts thereof are useful as a histone deacetylase inhibitors.Type: GrantFiled: November 4, 2008Date of Patent: July 7, 2009Assignee: Astellas Pharma Inc.Inventors: Naoki Ishibashi, Yuki Sawada, Yasuharu Urano, Shigeki Satoh, Yoshikazu Inoue, Yoshiteru Eikyu, Koichiro Mukoyoshi, Kazunori Kamijo, Fumiyuki Shirai, Hisashi Takasugi
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Publication number: 20090054464Abstract: Compounds having the formula (I): wherein R1 is hydrogen, lower alkyl, lower alkenyl, lower or higher alkynyl, cyclo(lower)alkyl, cyclo(higher)alkyl, cyclo(lower)alkyl(lower)alkyl, cyclo(higher)alkyl(lower)alkyl, cyclo(lower)alkenyl(lower)alkyl, aryl-fused cyclo(lower)alkyl, lower alkoxy, acyl, aryl, ar(lower)alkoxy, ar(lower)alkyl, heteroar(lower)alkyl, amino, heteroaryl, heterocyclyl or heterocyclyl(lower)alkyl, which may be substituted with one or more suitable substituent(s), R2 is hydrogen or lower alkyl, X is pyrrolidinylene or piperidinylene, Y is pyridylene, which may be substituted with one or more suitable substituent(s), Z is lower alkenylene, which may be substituted with lower alkyl or halogen, and salts thereof are useful as a histone deacetylase inhibitors.Type: ApplicationFiled: November 4, 2008Publication date: February 26, 2009Applicant: Astellas Pharma Inc.Inventors: Naoki ISHIBASHI, Yuki SAWADA, Yasuharu URANO, Shigeki SATOH, Yoshikazu INOUE, Yoshiteru EIKYU, Koichiro MUKOYOSHI, Kazunori KAMIJO, Fumiyuki SHIRAI, Hisashi TAKASUGI
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Publication number: 20090054465Abstract: This invention relates to novel N-hydroxyacrylamide compounds of formula (I) and pharmaceutically acceptable salts thereof. More particularly, it relates to novel N-hydroxyacrylamide compounds and pharmaceutically acceptable salts thereof which act as a HDAC inhibitor, to a pharmaceutical composition comprising the same and to a method of using the same therapeutically in the treatment and/or prevention of HDAC-related disease.Type: ApplicationFiled: February 6, 2007Publication date: February 26, 2009Applicant: Astella Pharma Inc.Inventors: Fumiyuki Shirai, Hideo Tsutsumi, Hiromichi Itani, Yoshihiro Kozuki, Yoshiteru Eikyu, Taro Masunaga
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Patent number: 7465731Abstract: A compound having the formula (I): wherein R1 is hydrogen, lower alkyl, lower alkenyl, lower or higher alkynyl, cyclo(lower)alkyl, cyclo(higher)alkyl, cyclo(lower)alkyl(lower)alkyl, cyclo(higher)alkyl(lower)alkyl, cyclo(lower)alkenyl(lower)alkyl, aryl-fused cyclo(lower)alkyl, lower alkoxy, acyl, aryl, ar(lower)alkoxy, ar(lower)alkyl, heteroar(lower)alkyl, amino, heteroaryl, heterocyclyl or heterocyclyl(lower)alkyl, which may be substituted with one or more suitable substituent(s), R2 is hydrogen or lower alkyl, X is arylene, heterorarylene, cycloalkylene, heterocycloalkylene or aryl-fused cycloalkene, Y is arylene, heteroarylene, which may be substituted with one or more suitable substituent(s), Z lower alenylene, which may be substituted with lower alkyl or halogen, or a salt thereof. The compound is useful as a histone deacetylase inhibitor.Type: GrantFiled: August 9, 2005Date of Patent: December 16, 2008Assignee: Astellas Pharma Inc.Inventors: Naoki Ishibashi, Yuki Sawada, Yasuharu Urano, Shigeki Satoh, Yoshikazu Inoue, Yoshiteru Eikyu, Koichiro Mukoyoshi, Kazunori Kamijo, Fumiyuki Shirai, Hisashi Takasugi
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Publication number: 20070112037Abstract: A compound of the formula (I): wherein R1 is hydrogen or lower alkyl; R2 is lower alkyl, etc.; R3 is lower alkoxy, etc.; R4 is hydroxy, etc.; X is O, S, etc.; Y is CH or N; Z is lower alkylene or lower alkenylene; and m is 0 or 1; or salts thereof, which are useful as a medicament.Type: ApplicationFiled: December 13, 2006Publication date: May 17, 2007Applicant: FUJISAWA PHARMACEUTICAL CO., LTD.Inventors: Fumiyuki SHIRAI, Hidenori Azami, Natsuko Kayakiri, Kazuo Okumura, Katsuya Nakamura
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Patent number: 7183306Abstract: A compound of the formula (I): wherein R1 is hydrogen or lower alkyl; R2 is lower alkyl, etc.; R3 is lower alkoxy, etc.; R4 is hydroxy, etc.; X is O, S, etc.; Y is CH or N; Z is lower alkylene or lower alkenylene; and m is 0 or 1; or salts thereof, which are useful as a medicament.Type: GrantFiled: November 14, 2003Date of Patent: February 27, 2007Assignee: Astellas Pharma Inc.Inventors: Fumiyuki Shirai, Hidenori Azami, Natsuko Kayakiri, Kazuo Okumura, Katsuya Nakamura
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Publication number: 20060052599Abstract: A compound having the following formula (I): wherein R1 is hydrogen, lower alkyl, lower alkenyl, lower or higher alkynyl, cyclo(lower)alkyl, cyclo(higher)alkyl, cyclo(lower)alkyl(lower)alkyl, cyclo(higher)alkyl(lower)alkyl, cyclo(lower)alkenyl(lower)alkyl, aryl-fused cyclo(lower)alkyl, lower alkoxy, acyl, aryl, ar(lower)alkoxy, ar(lower)alkyl, heteroar(lower) alkyl, amino, heteroaryl, heterocyclyl or heterocyclyl(lower)alkyl, which may be substituted with one or more suitable substituent(s), R2 is hydrogen or lower alkyl, X is arylene, heteroarylene, cycloalkylene, heterocycloalkylene or aryl-fused cycloalkylene, Y is arylene or heteroarylene, which may be substituted with one or more suitable substituent(s), Z is lower alkenylene, which may be substituted with lower alkyl or halogen, or a salt thereof. The compound is useful as a histone deacetylase inhibitor.Type: ApplicationFiled: August 9, 2005Publication date: March 9, 2006Applicant: Astellas Pharma Inc.Inventors: Naoki Ishibashi, Yuki Sawada, Yasuharu Urano, Shigeki Satoh, Yoshikazu Inoue, Yoshiteru Eikyu, Koichiro Mukoyoshi, Kazunori Kamijo, Fumiyuki Shirai, Hisashi Takasugi