Patents by Inventor Susumu Muto
Susumu Muto 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: 20240182908Abstract: An object of the present application is to overcome problems in obtaining DNA aptamers in conventional methods, including the lack of diversification of interactions with target molecules, the increase in the cost for obtaining aptamers by post modification, and the limitation of target molecule species because of electric charges, and to provide a technique for obtaining highly active aptamers as inexpensively as possible. Provided is a nucleoside or nucleotide having, as a base, a structure of formula I. In formula I, R1 is a substituted C1-C3 alkyl group, a substituted or unsubstituted C4-C9 alkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted cycloalkyl group, a substituted or unsubstituted aralkyl group, or a substituted or unsubstituted heteroaryl group.Type: ApplicationFiled: December 16, 2021Publication date: June 6, 2024Inventors: Susumu MUTO, Tatsuhiko SOMEYA, Yoji HAYASE, Daichi JITSUZAKI
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Publication number: 20240116924Abstract: Provided is a method for producing an imidazopyridine derivative represented by the following Formula (I), in which X is H, a substituted or unsubstituted propenyl group, a substituted or unsubstituted propynyl group, or a substituted or unsubstituted aryl group; and Y is H or OH. The method involves conducting a coupling reaction of a compound having a 5-X-2-thienyl group with 2-amino-3-nitro-4-chloropyridine under Suzuki-Miyaura coupling reaction conditions to obtain 2-amino-3-nitro-4-(5-X-2-thienyl)pyridine.Type: ApplicationFiled: January 27, 2022Publication date: April 11, 2024Inventor: Susumu MUTO
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Patent number: 11420997Abstract: The present invention has an object of shortening the process time and reducing use of a poor solvent for solidifying a carrier (Tag)-peptide component, by removing impurities without conducting solid-liquid separation (condensation, solid-liquid separation and drying operation) of a Tag-peptide component, in an Fmoc method using a Tag for liquid phase peptide synthesis.Type: GrantFiled: April 13, 2019Date of Patent: August 23, 2022Inventors: Hideaki Suzuki, Susumu Muto, Shuji Fujita, Daisuke Kubo
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Patent number: 11098078Abstract: The present invention has an object of providing a peptide synthesis method using a carrier capable of reversibly repeating the dissolved state and the insolubilized state, wherein the problem of an amino acid active species existing in the reaction system in de-protection reaction can be easily solved. The present invention provides a peptide synthesis method comprising the following steps: a step of condensing an N-Fmoc protected amino acid with a peptide having a C-terminal protected with a carrier which is crystallized according to a change of a composition of a dissolving solvent, in the presence of a condensing agent, to obtain an N-Fmoc-C-carrier protected peptide, a step of adding an alkylamine having 1 to 14 carbon atoms or hydroxyl amine to the reaction system, a step of de-protecting the N-terminal, and a step of changing the composition of the solvent dissolving the C-carrier protected peptide, to crystallize and separate the peptide.Type: GrantFiled: March 2, 2016Date of Patent: August 24, 2021Assignee: JITSUBO Co., Ltd.Inventors: Yusuke Kono, Hideaki Suzuki, Susumu Muto
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Publication number: 20210139532Abstract: The present invention has an object of shortening the process time and reducing use of a poor solvent for solidifying a carrier (Tag)-peptide component, by removing impurities without conducting solid-liquid separation (condensation, solid-liquid separation and drying operation) of a Tag-peptide component, in an Fmoc method using a Tag for liquid phase peptide synthesis.Type: ApplicationFiled: April 13, 2019Publication date: May 13, 2021Applicant: JITSUBO Co., Ltd.Inventors: Hideaki SUZUKI, Susumu MUTO, Shuji FUJITA, Daisuke KUBO
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Publication number: 20180215782Abstract: The present invention has an object of providing a peptide synthesis method using a carrier capable of reversibly repeating the dissolved state and the insolubilized state, wherein the problem of an amino acid active species existing in the reaction system in de-protection reaction can be easily solved. The present invention provides a peptide synthesis method comprising the following steps: a step of condensing an N-Fmoc protected amino acid with a peptide having a C-terminal protected with a carrier which is crystallized according to a change of a composition of a dissolving solvent, in the presence of a condensing agent, to obtain an N-Fmoc-C-carrier protected peptide, a step of adding an alkylamine having 1 to 14 carbon atoms or hydroxyl amine to the reaction system, a step of de-protecting the N-terminal, and a step of changing the composition of the solvent dissolving the C-carrier protected peptide, to crystallize and separate the peptide.Type: ApplicationFiled: March 2, 2016Publication date: August 2, 2018Inventors: Yusuke KONO, Hideaki SUZUKI, Susumu MUTO
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Patent number: 8633245Abstract: The compound represented by the following formula (I) and the like have PAI-1 inhibition activity; wherein: R1 represents a C6-10 aryl group which may be substituted or the like; T represents a single bond or the like; m represents 0 or 1; when m is 0, G represents —N—C(?O)—CO2H or the like; when m is 1, G represents an oxygen atom or the like; R2 represents a C6-10 aryl group which may be substituted or the like; E represents the following formula (II) wherein one of R31, R32, R33 and R34 represents the formula R1-T-, each of the other three independently represents a hydrogen atom or the like, and R35 represents the formula —X—Y?, a hydrogen atom or the like; X represents —CH2— or the like; Y? represents a carboxy group or the like; M represents a single bond or the like.Type: GrantFiled: April 10, 2009Date of Patent: January 21, 2014Assignee: Institute of Medicinal Molecular Design, Inc.Inventors: Youichi Yamaguchi, Takeshi Yanase, Susumu Muto, Akiko Itai
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Patent number: 8263657Abstract: A medicament having inhibitory activity against NF-?B activation, which comprises a compound represented by the following general formula (I) or a pharmacologically acceptable salt as an active ingredient: wherein X represents a connecting group, A represents hydrogen atom or acetyl group, E represents an aryl group or a heteroaryl group, and ring X represents an arene or a heteroarene.Type: GrantFiled: December 18, 2001Date of Patent: September 11, 2012Assignee: Institute of Medicinal Molecular Design, Inc.Inventors: Susumu Muto, Tatsuo Nagano, Tomomi Sotome, Akiko Itai
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Patent number: 8097610Abstract: A compound of the formula (I): or a pharmaceutically acceptable salt thereof.Type: GrantFiled: August 24, 2006Date of Patent: January 17, 2012Assignees: Shionogi & Co., Ltd., Institute of Medicinal Molecular Design, Inc.Inventors: Akiko Itai, Susumu Muto, Ryuko Tokuyama, Hiroshi Fukasawa, Takafumi Ohara, Terukazu Kato
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Patent number: 8097759Abstract: A medicament having inhibitory activity against NF-?B activation, which comprises a compound represented by the following general formula (I) or a pharmacologically acceptable salt as an active ingredient: wherein X represents a connecting group, A represents hydrogen atom or acetyl group, E represents an aryl group or a heteroaryl group, and ring X represents an arene or a heteroarene.Type: GrantFiled: July 2, 2010Date of Patent: January 17, 2012Assignee: Institute of Medicinal Molecular Design, Inc.Inventors: Susumu Muto, Tatsuo Nagano, Tomomi Sotome, Akiko Itai
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Publication number: 20110294813Abstract: Disclosed is a compound which is useful as an 11?-hydroxysteroid dehydrogenase type 1 inhibitor. A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein R1 is optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted heterocycle or optionally substituted heterocyclealkyl, X is —O—, —NR3—, —NR3C(?O)— or —NR3S(?O)2—, R2 is optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heteroaryl or optionally substituted heteroarylalkyl, R3 is hydrogen or optionally substituted alkyl.Type: ApplicationFiled: June 30, 2011Publication date: December 1, 2011Applicants: SHIONOGI & CO., LTD., INSTITUTE OF MEDICINAL MOLECULAR DESIGN, INC.Inventors: Akiko Itai, Susumu Muto, Ryuko Tokuyama, Hiroshi Fukasawa, Takeshi Yanase
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Patent number: 8044236Abstract: A compound represented by the following general formula (I) or a salt thereof, or a hydrate thereof or a solvate thereof having an inhibitory action against plasminogen activator inhibitor-1 (PAI-1): wherein R1 represents a C6-10 aryl group; or a substituted C6-10 aryl group, R2 represents a C6-10 aryl group; or a C6-10 aryl group substituted with a group or groups selected from the group consisting of a halogen atom, nitro group, a C1-6 alkyl group, a halogenated C1-6 alkyl group, a C1-6 alkoxy group, a halogenated C1-6 alkoxy group, a phenyl group and carboxy group, X represents —CH2—, —CH2CH2—, —CH?CH— or —N(R3)—C(?O)—, Y represents carboxy group or a bioisostere of carboxy group, R3 represents hydrogen atom, a C1-4 alkyl group or a C7-12 aralkyl group, m represents 0 or 1.Type: GrantFiled: October 11, 2007Date of Patent: October 25, 2011Assignee: Institute of Medicinal Molecular Design, Inc.Inventors: Youichi Yamaguchi, Takeshi Yanase, Susumu Muto, Akiko Itai
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Patent number: 7998992Abstract: Disclosed is a compound which is useful as an 11?-hydroxysteroid dehydrogenase type 1 inhibitor. A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein R1 is optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted heterocycle or optionally substituted heterocyclealkyl, X is —O—, —NR3—, —NR3C(?O)— or —NR3S(?O)2—, R2 is optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heteroaryl or optionally substituted heteroarylalkyl, R3 is hydrogen or optionally substituted alkyl.Type: GrantFiled: March 27, 2008Date of Patent: August 16, 2011Assignees: Institute of Medicinal Molecular Design, Inc., Shionogi & Co., Ltd.Inventors: Akiko Itai, Susumu Muto, Ryuko Tokuyama, Hiroshi Fukasawa, Takeshi Yanase
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Patent number: 7884234Abstract: A compound represented by the following general formula (I) or a salt thereof, or a hydrate thereof or a solvate thereof having an inhibitory action against plasminogen activator inhibitor-1 (PAI-1): wherein R1 represents a C6-10 aryl group; or a C6-10 aryl group substituted with a group or groups selected from the group consisting of a halogen atom, cyano group, nitro group, a C1-6 alkyl group, a halogenated C1-6 alkyl group, a C1-6 alkoxy group, a halogenated C1-6 alkoxy group and a C1-6 alkylsulfanyl group, R2 represents a C6-10 aryl group; or a C6-10 aryl group substituted with a group or groups selected from the group consisting of a halogen atom, hydroxy group, a C1-6 alkyl group, a halogenated C1-6 alkyl group, a C1-6 alkoxy group, a halogenated C1-6 alkoxy group, a C1-6 alkylsulfanyl group and phenyl group, X represents a single bond or oxygen atom, Z represents a phenylene group or a substituted phenylene group, m represents 0 or 1.Type: GrantFiled: October 11, 2007Date of Patent: February 8, 2011Assignee: Institute of Medicinal Molecular Design, inc.Inventors: Youichi Yamaguchi, Takeshi Yanase, Susumu Muto, Akiko Itai
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Publication number: 20100274051Abstract: A medicament having inhibitory activity against NF-?B activation, which comprises a compound represented by the following general formula (I) or ? pharmacologically acceptable salt as an active ingredient: wherein X represents a connecting group, A represents hydrogen atom or acetyl group, E represents an aryl group or a heteroaryl group, and ring X represents an arene or a heteroarene.Type: ApplicationFiled: July 2, 2010Publication date: October 28, 2010Applicant: Institute of Medicinal Molecular Design. Inc.Inventors: Susumu MUTO, Tatsuo Nagano, Tomomi Sotome, Akiko Itai
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Publication number: 20100234363Abstract: Disclosed is a compound which is useful as an 11?-hydroxysteroid dehydrogenase type 1 inhibitor.Type: ApplicationFiled: September 17, 2008Publication date: September 16, 2010Applicants: INSTITUTE OF MEDICINAL MOLECULAR DESIGN, INC., SHIONOGI & CO., LTD.Inventors: Akiko Itai, Susumu Muto, Ryuko Tokuyama, Hiroshi Fukasawa, Takeshi Yanase
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Publication number: 20100113770Abstract: A medicament having inhibitory activity against NF-?B activation which comprises as an active ingredient a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, and a hydrate thereof and a solvate thereof: wherein X represents a connecting group whose number of atoms in a main chain is 2 to 5 (said connecting group may be substituted), “A” represents an acyl group which may be substituted, (provided that unsubstituted acetyl group and unsubstituted acryloyl group are excluded,) or a C1 to C6 alkyl group which may be substituted, or A may bind to connecting group X to form a cyclic structure which may be substituted, “E” represents an aryl group which may be substituted or a heteroaryl group which may be substituted, ring Z represents an arene which may have one or more substituents in addition to the group represented by formula —O-A wherein A has the same meaning as that defined above and the group rType: ApplicationFiled: October 14, 2009Publication date: May 6, 2010Applicant: INSTITUTE OF MEDICINAL MOLECULAR DESIGN, INC.Inventors: Susumu MUTO, Akiko ITAI
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Publication number: 20100113448Abstract: Disclosed is a compound which is useful as an 11?-hydroxysteroid dehydrogenase type 1 inhibitor. A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein R1 is optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted heterocycle or optionally substituted heterocyclealkyl, X is —O—, —NR3—, —NR3C(?O)— or —NR3S(?O)2—, R2 is optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heteroaryl or optionally substituted heteroarylalkyl, R3 is hydrogen or optionally substituted alkyl.Type: ApplicationFiled: March 27, 2008Publication date: May 6, 2010Applicants: INSTITUTE OF MEDICINAL MOLECULAR DESIGN, INC., SHIONOGI & CO., LTD.Inventors: Akiko Itai, Susumu Muto, Ryuko Tokuyama, Hiroshi Fukasawa, Takeshi Yanase
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Patent number: 7700655Abstract: A medicament for the preventive and/or therapeutic treatment of allergic diseases and/or endometriosis and/or hysteromyoma which comprises as an active ingredient a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, and a hydrate thereof and a solvate thereof: wherein X represents a connecting group whose number of atoms in the main chain is 2 to 5 (said connecting group may be substituted), A represents hydrogen atom or acetyl group, E represents an aryl group which may be substituted or a hetero aryl group which may be substituted, ring Z represents an arene which may have one or more substitutents in addition to the group represented by formula —O-A wherein A has the same meaning as that defined above and the group represented by formula —X-E wherein each of X and E has the same meaning as that defined above, or a heteroarene which may have one or more substitutents in addition to the group represeType: GrantFiled: April 9, 2007Date of Patent: April 20, 2010Assignee: Institute of Medicinal Molecular Design, Inc.Inventors: Susumu Muto, Akiko Itai
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Patent number: 7671058Abstract: A compound represented by the following formula (I) or a salt thereof: wherein R1, R2, R3 and R4 represent hydrogen atom, a halogen atom, cyano group, nitro group, a C1-4 alkyl group, a halogenated C1-4 alkyl group or a C1-4 alkoxy group, R5 represents a halogen atom, cyano group, a C1-4 alkyl group, a halogenated C1-4 alkyl group or a C1-4 alkoxy group, R6 represents a C5-7 cycloalkyl group, a substituted C5-7 cycloalkyl group, a 5 to 7-membered completely saturated heterocyclic group or a substituted 5 to 7-membered completely saturated heterocyclic group, X represents a single bond, oxygen atom, sulfur atom, NR7, —O—CH2— or —N(R8)—CH2—, R7 represents hydrogen atom or a C1-4 alkyl group, or R7 may combine with a substituent of R6 to represent a single bond, methylene group or ethylene group, R8 represents hydrogen atom, a C1-4 alkyl group or a C7-12 aralkyl group, which is useful as an active ingredient of a medicament for prophylactic and/or therapeutic treatment of diseases caused by an activation ofType: GrantFiled: June 19, 2007Date of Patent: March 2, 2010Assignee: Institute of Medicinal Molecular Design, Inc.Inventors: Ryukou Tokuyama, Toshifumi Wakamatsu, Tatsurou Ichige, Susumu Muto, Akiko Itai